AR112690A1 - PYRUVATE KINASE ACTIVATORS FOR USE IN THE TREATMENT OF BLOOD DISORDERS - Google Patents

PYRUVATE KINASE ACTIVATORS FOR USE IN THE TREATMENT OF BLOOD DISORDERS

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Publication number
AR112690A1
AR112690A1 ARP180102343A AR112690A1 AR 112690 A1 AR112690 A1 AR 112690A1 AR P180102343 A ARP180102343 A AR P180102343A AR 112690 A1 AR112690 A1 AR 112690A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
alkyl
protecting group
hydrogen
independently
Prior art date
Application number
Other languages
Spanish (es)
Inventor
Giovanni Cianchetta
Tao Liu
Anil Kumar Padyana
Zhihua Sui
Zhenwei Cai
Dawei Cui
Jingjing Ji
Original Assignee
Agios Pharmaceuticals 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 Agios Pharmaceuticals Inc filed Critical Agios Pharmaceuticals Inc
Publication of AR112690A1 publication Critical patent/AR112690A1/en

Links

Abstract

Reivindicación 1: Un compuesto caracterizado porque está representado por la fórmula estructural (1), o una sal aceptable farmacéuticamente del mismo, donde: R¹ es hidrógeno, un alquilo opcionalmente sustituido, un haloalquilo opcionalmente sustituido, un alquenilo opcionalmente sustituido, un alquinilo opcionalmente sustituido, un cicloalquilo opcionalmente sustituido, un heterociclo opcionalmente sustituido, un arilo opcionalmente sustituido, -ORᵒ¹, -C(=O)Rᶜ¹, o un grupo protector de nitrógeno; donde: Rᵒ¹ es hidrógeno, alquilo opcionalmente sustituido, o un grupo protector de oxígeno; Rᶜ¹ se sustituye opcionalmente alquilo o -N(Rᶜⁿ)₂, donde cada caso de Rᶜⁿ es independientemente hidrógeno, -C₁₋₆ alquilo, o un grupo protector de nitrógeno; R² y Q son independientemente entre sí un heteroarilo monocíclico opcionalmente sustituido de 5 ó 6 miembros; Rᵃ y Rᵇ son independientemente entre sí hidrógeno, un halógeno, -CN, -NO₂, -N₃, un alquilo opcionalmente sustituido, -ORᵒ³, -N(Rⁿ¹)₂, -C(=O)N(Rⁿ¹)₂, o -C(=O)Rᶜ²; o de manera alternativa Rᵃ y Rᵇ se pueden tomar junto con el átomo de carbono al cual se encuentran unidos para formar un cicloalquilo opcionalmente sustituido o un heterociclo opcionalmente sustituido; donde: cada caso de Rⁿ¹ es independientemente hidrógeno, un -C₁₋₆ alquilo opcionalmente sustituido, o un grupo protector de nitrógeno; Rᵒ³ es hidrógeno, un -C₁₋₆ alquilo opcionalmente sustituido, o un grupo protector de oxígeno; y Rᶜ² es un -C₁₋₆ alquilo opcionalmente sustituido; y Rʲ y Rᵏ son independientemente entre sí hidrógeno, un halógeno, -CN, -ORᵒ⁷, -N(Rⁿ⁵)₂, -N(Rⁿ⁵)C(=O)Rᶜ⁵, -C(=O)N(Rⁿ⁵)₂, -C(=O)Rᶜ⁵, -C(=O)ORᵒ⁷, -SRʲˢ, -S(=O)₂Rʲˢ, -S(=O)Rʲˢ, o un -C₁₋₆ alquilo opcionalmente sustituido; o de manera alternativa Rʲ y Rᵏ se pueden tomar junto con el átomo de carbono al cual se encuentran unidos para formar C=O, un anillo C₁₋₆ cicloalquilo monocíclico opcionalmente sustituido, o un anillo C₃₋₆ monocíclico heterociclilo opcionalmente sustituido; donde: cada caso de Rⁿ⁵ es independientemente hidrógeno, un -C₁₋₆ alquilo opcionalmente sustituido, -ORᵒ⁸, o un grupo protector de nitrógeno, donde Rᵒ⁸ es hidrógeno, un -C₁₋₆ alquilo opcionalmente sustituido, o un grupo protector de oxígeno; cada caso de Rᵒ⁷ es independientemente hidrógeno, un -C₁₋₆ alquilo opcionalmente sustituido, o un grupo protector de oxígeno; cada caso de Rᶜ⁵ es independientemente un C₁₋₆ alquilo opcionalmente sustituido; y cada caso de Rʲˢ es independientemente un -C₁₋₆ alquilo opcionalmente sustituido, un C₆₋₁₂ arilo opcionalmente sustituido, un heteroarilo opcionalmente sustituido, o un grupo protector de azufre.Claim 1: A compound characterized in that it is represented by the structural formula (1), or a pharmaceutically acceptable salt thereof, where: R¹ is hydrogen, an optionally substituted alkyl, an optionally substituted haloalkyl, an optionally substituted alkenyl, an optionally substituted alkynyl , an optionally substituted cycloalkyl, an optionally substituted heterocycle, an optionally substituted aryl, -ORᵒ¹, -C (= O) Rᶜ¹, or a nitrogen protecting group; where: Rᵒ¹ is hydrogen, optionally substituted alkyl, or an oxygen protecting group; Rᶜ¹ is optionally substituted for alkyl or -N (Rᶜⁿ) ₂, where each occurrence of Rᶜⁿ is independently hydrogen, -C₁₋₆ alkyl, or a nitrogen protecting group; R² and Q are independently of one another a 5- or 6-membered optionally substituted monocyclic heteroaryl; Rᵃ and Rᵇ are independently from each other hydrogen, a halogen, -CN, -NO₂, -N₃, an optionally substituted alkyl, -ORᵒ³, -N (Rⁿ¹) ₂, -C (= O) N (Rⁿ¹) ₂, or - C (= O) Rᶜ²; or alternatively Rᵃ and Rᵇ can be taken together with the carbon atom to which they are attached to form an optionally substituted cycloalkyl or an optionally substituted heterocycle; where: each occurrence of Rⁿ¹ is independently hydrogen, an optionally substituted -C₁₋₆ alkyl, or a nitrogen protecting group; Rᵒ³ is hydrogen, an optionally substituted -C₁₋₆ alkyl, or an oxygen protecting group; and Rᶜ² is an optionally substituted -C₁₋₆ alkyl; and Rʲ and Rᵏ are independently hydrogen, a halogen, -CN, -ORᵒ⁷, -N (Rⁿ⁵) ₂, -N (Rⁿ⁵) C (= O) Rᶜ⁵, -C (= O) N (Rⁿ⁵) ₂, -C (= O) Rᶜ⁵, -C (= O) ORᵒ⁷, -SRʲˢ, -S (= O) ₂Rʲˢ, -S (= O) Rʲˢ, or an optionally substituted -C₁₋₆ alkyl; or alternatively Rʲ and Rᵏ may be taken together with the carbon atom to which they are attached to form C = O, an optionally substituted monocyclic C₁₋₆ cycloalkyl ring, or an optionally substituted monocyclic heterocyclyl C₃₋₆ ring; where: each occurrence of Rⁿ⁵ is independently hydrogen, an optionally substituted -C₁₋₆ alkyl, -ORᵒ⁸, or a nitrogen protecting group, where Rᵒ⁸ is hydrogen, an optionally substituted -C₁₋₆ alkyl, or an oxygen protecting group; each occurrence of Rᵒ⁷ is independently hydrogen, an optionally substituted -C₁₋₆ alkyl, or an oxygen protecting group; each occurrence of Rᶜ⁵ is independently an optionally substituted C₁₋₆ alkyl; and each occurrence of Rʲˢ is independently an optionally substituted -C₁₋₆ alkyl, an optionally substituted C₆₋₁₂ aryl, an optionally substituted heteroaryl, or a sulfur protecting group.

ARP180102343 2017-08-15 2018-08-15 PYRUVATE KINASE ACTIVATORS FOR USE IN THE TREATMENT OF BLOOD DISORDERS AR112690A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2017097496 2017-08-15

Publications (1)

Publication Number Publication Date
AR112690A1 true AR112690A1 (en) 2019-11-27

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Family Applications (2)

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ARP180102347 AR112475A1 (en) 2017-08-15 2018-08-15 PYRUVATE KINASE MODULATORS AND THE USE OF THEM
ARP180102343 AR112690A1 (en) 2017-08-15 2018-08-15 PYRUVATE KINASE ACTIVATORS FOR USE IN THE TREATMENT OF BLOOD DISORDERS

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AR (2) AR112475A1 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11872225B2 (en) 2017-08-15 2024-01-16 Agios Pharmaceuticals, Inc. Pyruvate kinase modulators and use thereof

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11872225B2 (en) 2017-08-15 2024-01-16 Agios Pharmaceuticals, Inc. Pyruvate kinase modulators and use thereof
US11957680B2 (en) 2017-08-15 2024-04-16 Agios Pharmaceuticals, Inc. Pyruvate kinase activators for use in treating blood disorders

Also Published As

Publication number Publication date
AR112475A1 (en) 2019-10-30

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