AR122586A1 - Compuestos heterocíclicos y agentes de imagen para la imagen de la proteína huntingtina - Google Patents

Compuestos heterocíclicos y agentes de imagen para la imagen de la proteína huntingtina

Info

Publication number
AR122586A1
AR122586A1 ARP210101580A ARP210101580A AR122586A1 AR 122586 A1 AR122586 A1 AR 122586A1 AR P210101580 A ARP210101580 A AR P210101580A AR P210101580 A ARP210101580 A AR P210101580A AR 122586 A1 AR122586 A1 AR 122586A1
Authority
AR
Argentina
Prior art keywords
alkyl
haloalkyl
alkoxy
haloalkoxy
dialkylamino
Prior art date
Application number
ARP210101580A
Other languages
English (en)
Inventor
Longbin Liu
Matthew Lee
Celia Dominguez
Peter David Johnson
Catherine Jane Greenaway
Kanika Khurana
Matthew Robert Mills
Filippo Rota
Original Assignee
Chdi Foundation Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Chdi Foundation Inc filed Critical Chdi Foundation Inc
Publication of AR122586A1 publication Critical patent/AR122586A1/es

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/041—Heterocyclic compounds
    • A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0459—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/041—Heterocyclic compounds
    • A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0455—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/041—Heterocyclic compounds
    • A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0463—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Optics & Photonics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Physics & Mathematics (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Reivindicación 1: Un compuesto de fórmula (1) o un análogo enriquecido isotópicamente, sal, profármaco, tautómero, estereoisómero o una mezcla de estereoisómeros farmacéuticamente aceptables del mismo, en el que el compuesto está marcado con uno o más isótopos radiactivos; A¹ es C; A² es C o N; A³ es CR²¹, NR³, o N; A⁴ es CR²², NR³, o N; A⁵ es CR²³, NR³, o N; donde el anillo Z formado por -A¹-A²-A³-A⁴-A⁵- es un heteroarilo de 5 miembros que tiene hasta tres átomos de nitrógeno; cada uno de R²¹, R²², y R²³ es independientemente hidrógeno, halo, ciano, hidroxi, amino, alquilamino, dialquilamino, alquilo C₁₋₄, haloalquilo C₁₋₄, alcoxi C₁₋₄, haloalcoxi C₁₋₄, o cicloalquilo C₃₋₆; cada R³ es independientemente hidrógeno, alquilo C₁₋₄, haloalquilo C₁₋₄, o cicloalquilo C₃₋₆; A⁶ es CR¹¹ o N, A⁷ es CR¹² o N, A⁸ es CR¹³ o N, y A⁹ es CR¹⁴ o N, donde no más de dos de A⁶, A⁷, A⁸, y A⁹ son N; cada uno de R¹¹, R¹², R¹³, y R¹⁴ es hidrógeno, halo, ciano, hidroxi, amino, alquilamino, dialquilamino, alquilo C₁₋₄, haloalquilo C₁₋₄, alcoxi C₁₋₄, o haloalcoxi C₁₋₄; X¹ es alquilo C₁₋₆, cicloalquilo C₃₋₁₀, arilo C₆₋₁₀, heteroarilo, o heterociclilo, donde X¹ está opcionalmente sustituido con 1 a 4 R⁴; cada R⁴ es independientemente halo, ciano, hidroxi, amino, alquilamino, dialquilamino, alquilo C₁₋₄, haloalquilo C₁₋₄, alcoxi C₁₋₄, o haloalcoxi C₁₋₄; X² es O, S, o NR⁵; R⁵ es hidrógeno, alquilo C₁₋₆, haloalquilo C₁₋₆, o alcoxi C₁₋₆; L es (C(R⁶)₂)ₘ-, donde m es 1, 2, 3, ó 4; cada R⁶ es independientemente hidrógeno, halo, ciano, hidroxi, amino, alquilamino, dialquilamino, alquilo C₁₋₄, haloalquilo C₁₋₄, alcoxi C₁₋₄, o haloalcoxi C₁₋₄; o dos R⁶, junto con los átomos que intervienen, se unen para formar un anillo de 3- a 6- miembros; L¹ es C(O), C(O)NRᵃ, NRᵃC(O), ó O, o L¹ está ausente; Rᵃ es hidrógeno, alquilo C₁₋₆, o haloalquilo C₁₋₆; L² es alquileno C₁₋₂ opcionalmente sustituido con 1 a 4 R⁷, o L² está ausente; cada R⁷ es independientemente halo, ciano, hidroxi, amino, alquilamino, dialquilamino, alquilo C₁₋₄, haloalquilo C₁₋₄, alcoxi C₁₋₄, o haloalcoxi C₁₋₄.
ARP210101580A 2020-06-11 2021-06-10 Compuestos heterocíclicos y agentes de imagen para la imagen de la proteína huntingtina AR122586A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US202063037751P 2020-06-11 2020-06-11

Publications (1)

Publication Number Publication Date
AR122586A1 true AR122586A1 (es) 2022-09-21

Family

ID=76744966

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP210101580A AR122586A1 (es) 2020-06-11 2021-06-10 Compuestos heterocíclicos y agentes de imagen para la imagen de la proteína huntingtina

Country Status (13)

Country Link
US (1) US11918662B2 (es)
EP (1) EP4165044A1 (es)
JP (1) JP2023530089A (es)
KR (1) KR20230034222A (es)
CN (1) CN116075512A (es)
AR (1) AR122586A1 (es)
AU (1) AU2021288104A1 (es)
BR (1) BR112022025238A2 (es)
CA (1) CA3186583A1 (es)
IL (1) IL298941A (es)
MX (1) MX2022015829A (es)
TW (1) TW202214637A (es)
WO (1) WO2021252775A1 (es)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114394967B (zh) * 2022-01-28 2023-12-15 宁夏农林科学院农业资源与环境研究所（宁夏土壤与植物营养重点实验室） 一种2-吡唑苯胺与1,3-二羰基化合物合成吡唑并喹啉衍生物的方法

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4228095A1 (de) 1992-08-24 1994-03-03 Asta Medica Ag Neue 4,5-Dihydro-4-oxo-pyrrolo[1,2-a]chinoxaline und entsprechende Aza-analoga und Verfahren zu deren Herstellung
GB9423910D0 (en) 1994-11-26 1995-01-11 Pfizer Ltd Therapeutic agents
WO2005028474A2 (en) 2003-05-29 2005-03-31 Millennium Pharmaceuticals, Inc. Pyrazoloquinoline derivatives as chk-1 inhibitors
AU2004285449A1 (en) 2003-10-20 2005-05-12 Merck & Co., Inc. Hydroxy pyridopyrrolopyrazine dione compounds useful as HIV integrase inhibitors
JP2008526715A (ja) 2005-01-03 2008-07-24 ユニベルシタ デグリ ストゥディ ディ シエナ 神経精神障害の治療のためのアリールピペラジン誘導体
WO2006094210A2 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. Tetrahydroquinoxalinone sirtuin modulators
EP1798233A1 (en) 2005-12-19 2007-06-20 Faust Pharmaceuticals Pyrrolo[1,2-a]quinoxaline derivatives as Adenosine A3 receptor modulators and uses thereof
GB0615809D0 (en) 2006-08-09 2006-09-20 Istituto Di Ricerche D Biolog Therapeutic compounds
ITRM20060518A1 (it) 2006-10-02 2008-04-03 Univ Palermo Derivati isoindolo-chinossalinici ad attivita' antitumorale procedimento per la loro produzione e loro uso
JP5583592B2 (ja) 2007-11-30 2014-09-03 ニューリンク ジェネティクス コーポレイション Ｉｄｏ阻害剤
US20130023498A1 (en) 2008-02-20 2013-01-24 The Wistar Institute and North Carolina State University MicroRNA Modulators and Method for Identifying and Using the Same
US20100168084A1 (en) 2008-05-08 2010-07-01 Huber L Julie Therapeutic compounds and related methods of use
WO2010016005A1 (en) * 2008-08-06 2010-02-11 Pfizer Inc. 6 substituted 2-heterocyclylamino pyrazine compounds as chk-1 inhibitors
WO2010135571A1 (en) 2009-05-20 2010-11-25 Cylene Pharmaceuticals, Inc. Novel protein kinase modulators
US8673913B2 (en) 2009-11-13 2014-03-18 Case Western Reserve University SHP-2 phosphatase inhibitor
US8435993B2 (en) 2010-12-07 2013-05-07 Philadelphia Health And Education Corporation Methods of inhibiting metastasis from cancer
CA2840060A1 (en) 2011-06-27 2013-01-03 Kyorin Pharmaceutical Co., Ltd. Bridged bicyclic compounds for the treatment of bacterial infections
US9345703B2 (en) 2011-09-15 2016-05-24 University Of Kansas Kappa opioid receptor effectors and uses thereof
SI3340796T1 (sl) * 2015-08-28 2022-02-28 Chdi Foundation, Inc. Sonde za slikanje proteina huntingtina
US11413278B2 (en) 2015-10-08 2022-08-16 The Regents Of The University Of California Compounds and methods for promoting stress resistance
US11267817B2 (en) 2017-05-02 2022-03-08 Drexel University Substituted pyrrolo[1,2-a]quinoxalin-4(5H)-ones as CX3CR1 antagonists
EP3700527A4 (en) 2017-10-25 2021-03-10 Children's Medical Center Corporation PAPD5 INHIBITORS AND THEIR METHODS OF USE

Also Published As

Publication number Publication date
IL298941A (en) 2023-02-01
US20210393812A1 (en) 2021-12-23
MX2022015829A (es) 2023-04-05
WO2021252775A1 (en) 2021-12-16
CA3186583A1 (en) 2021-12-16
BR112022025238A2 (pt) 2023-02-14
CN116075512A (zh) 2023-05-05
EP4165044A1 (en) 2023-04-19
KR20230034222A (ko) 2023-03-09
JP2023530089A (ja) 2023-07-13
AU2021288104A1 (en) 2023-01-19
US11918662B2 (en) 2024-03-05
TW202214637A (zh) 2022-04-16

Similar Documents

Publication Publication Date Title
PE20190329A1 (es) Compuestos moduladores de fxr (nr1h4)
AR109315A1 (es) Composiciones farmacéuticas que contienen derivados de piridona policíclica sustituida y profármaco de las mismas
AR105820A1 (es) Análogos de nucleósidos sustituidos en el anillo aromático bicíclico 6-6 para su uso como inhibidores de prmt5
PE20220931A1 (es) Inhibidores de shp2 fosfatasa de tipo pirazolo[3,4-b]pirazina
AR119698A2 (es) Compuesto amida n-urea sustituida derivado de aminoácido
PE20220140A1 (es) Compuestos triciclicos condensados utiles como agentes anticancerigenos
AR119651A1 (es) Compuestos heterocíclicos y de heteroarilo para tratar la enfermedad de huntington
PE20221457A1 (es) Degradadores de moleculas pequenas de helios y procedimientos de uso
UY37513A (es) Modulador del regulador de conductancia transmembrana de fibrosis quística, composiciones farmacéuticas, métodos de tratamiento y proceso para producir el modulador
AR109805A1 (es) Derivados de oxadiazol microbiocidas
AR112774A1 (es) Análogos de 1,2-dihidro-3h-pirazolo[3,4-d]pirimidin-3-ona
AR111983A1 (es) ANILLOS 6 - 5 FUSIONADOS COMO INHIBIDORES DE C5a
CU24393B1 (es) Nuevos derivados de pirazolo pirimidina y su uso como inhibidores de malt1
AR092108A1 (es) Piridazina 1,4 disustituida, analogos de la misma y metodos para tratar las enfermedades relacionadas con deficiencia del smn
AR110153A1 (es) ÁCIDOS PROPIÓNICOS 3-SUSTITUIDOS COMO INHIBIDORES DE LA INTEGRINA aV
CO5640152A2 (es) Composiciones farmaceuticas para inhibidores de la proteasa del virus de la hepatitis c
AR072952A1 (es) Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso
AR095426A1 (es) Inhibidores tripeptídicos de la epoxicetona proteasa
AR080859A1 (es) Derivados 1,2,4 triazolo-piridinicos inhibidores no nucleosidicos de la transcriptasa inversa, utiles para tratar infecciones por vih y composiciones farmaceuticas que los contienen.
AR114828A1 (es) Compuestos de pteridinona y sus usos
AR108778A1 (es) Compuestos antibacterianos
AR098432A1 (es) Compuestos heterocíclicos
AR118771A1 (es) Sulfonamidas de acilo para el tratamiento del cáncer
AR085976A1 (es) Inhibidores de la poli(adp-ribosa)polimerasa (parp) para el tratamiento de neuropatia periferica inducida por un quimioterapia (cipn)
AR122586A1 (es) Compuestos heterocíclicos y agentes de imagen para la imagen de la proteína huntingtina