AR102180A1 - MODULATORS OF THE TRANSMEMBRANE DRIVING REGULATOR OF CHYSICAL FIBROSIS - Google Patents

MODULATORS OF THE TRANSMEMBRANE DRIVING REGULATOR OF CHYSICAL FIBROSIS

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Publication number
AR102180A1
AR102180A1 ARP150103214A ARP150103214A AR102180A1 AR 102180 A1 AR102180 A1 AR 102180A1 AR P150103214 A ARP150103214 A AR P150103214A AR P150103214 A ARP150103214 A AR P150103214A AR 102180 A1 AR102180 A1 AR 102180A1
Authority
AR
Argentina
Prior art keywords
ring
independently
heteroaryl
cycloalkyl
aryl
Prior art date
Application number
ARP150103214A
Other languages
Spanish (es)
Inventor
Thomas Miller Mark
Anderson Corey
Arumugam Vijayalaksmi
Richard Bear Brian
j clemens Jeremy
Cleveland Thomas
Conroy Erica
Richard Coon Timothy
A Frieman Bryan
Diederik Jan Grootenhuis Peter
Stanley Gross Raymond
Sabina Hadida-Ruah Sara
Haripada Khatuya
Virupax Joshi Pramod
John Krenitsky Paul
Lin Chun
Erdgogan Chieh - Marelius Gulin
Melillo Vito
Mcartney Jason
Mgaughey Nicholls Georgia
Jean Denis Pierre Fabrice
Silina Alina
P Termin Andreas
Uy Johnny
Zhou Jinglan
Original Assignee
Vertex Pharma
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 Vertex Pharma filed Critical Vertex Pharma
Publication of AR102180A1 publication Critical patent/AR102180A1/en

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  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Para el tratamiento de enfermedades mediadas por CFTR, como fibrosis quística. La presente también caracteriza composiciones farmacéuticas, método de tratamiento y sus kits. Reivindicación 1: Un compuesto de la fórmula (1), una de sus sales farmacéuticamente aceptables, en donde, de modo independiente para cada aparición: Anillo A es un anillo arilo C₆₋₁₀; anillo cicloalquilo C₃₋₁₀; o un anillo heteroarilo o heterocíclico C₃₋₁₄, en donde cualquiera de 1 a 4 átomos de anillo son, de modo independiente, O, S, N o NR; Anillo B es un anillo cicloalquilo C₃₋₁₀; un anillo arilo C₆₋₁₀; o un anillo heteroarilo o heterocíclico C₄₋₁₀, en donde cualquiera de 1 a 4 átomos de anillo son, de modo independiente, O, S, N o NR; Anillo C es un anillo arilo C₆₋₁₀; un anillo heteroarilo o heterocíclico C₃₋₁₄, en donde cualquiera de 1 a 4 átomos de anillo son, de modo independiente, N, NR, O ó S; o un anillo cicloalquilo C₃₋₁₀; W es O, NR o S; X es O ó NR; Y es, de modo independiente, CRR, CO, O, S, SO, SO₂, S(O)NH o NR; Z es NR o CHR; R¹ es halo; CN; F₅S; SiR₃; OH; NRR; alquilo C₁₋₆ o fluoroalquilo; alcoxi C₁₋₆ o fluoroalcoxi; alquenilo C₁₋₆; alquinilo C₁₋₆, (alquilen C₁₋₉)-R⁴, en donde hasta cuatro unidades de CH₂ son reemplazadas, de modo independiente, con O, CO, S, SO, SO₂ o NR; arilo C₆₋₁₀; anillo heteroarilo o heterocíclico C₃₋₁₀, en donde cualquiera de 1 a 4 átomos de anillo son, de modo independiente, O, S, N o NR; o cicloalquilo C₃₋₁₀; R² es halo; OH; NRR; azida; CN; CO₂R; alquilo C₁₋₆ o fluoroalquilo; alcoxi C₁₋₆ o fluoroalcoxi; alquenilo C₁₋₆; alquinilo C₁₋₆; arilo C₆₋₁₀; anillo heteroarilo o heterocíclico C₃₋₁₃, en donde cualquiera de 1 a 4 átomos de anillo son, de modo independiente, O, S, N o NR; cicloalquilo C₃₋₁₀; o un (alquilen C₁₋₉)-R⁴, en donde hasta cuatro unidades de CH₂ son reemplazadas, de modo independiente, con O, CO, S, SO, SO₂ o NR; dos R² pueden formar un grupo =CH₂ u =O; R³ es halo; CN; OH; CO₂R; alquilo C₁₋₆ o fluoroalquilo; alquenilo C₁₋₆; alquinilo C₁₋₆; alcoxi C₁₋₆ o fluoroalcoxi; o arilo C₆₋₁₀; anillo heteroarilo o heterocíclico C₃₋₁₀, en donde cualquiera de 1 a 4 átomos de anillo son, de modo independiente, O, S, N o NR; cicloalquilo C₃₋₁₀; o un (alquilen C₁₋₉)-R⁴, en donde hasta cuatro unidades de CH₂ son reemplazadas, de modo independiente, con O, CO, S, SO, SO₂ o NR; dos R³ pueden formar un grupo =CH₂ u =O; R⁴ es H; azida; CF₃; CHF₂; OR; CCH; CO₂R; OH; arilo C₆₋₁₀, heteroarilo C₃₋₁₀ o heterocicloalquilo, en donde cualquiera de 1 a 4 átomos de anillo son, de modo independiente, O, S, N o NR; cicloalquilo C₃₋₁₀; NRR, NRCOR, CONRR, CN, halo o SO₂R; R es, de modo independiente, H; OH; CO₂H; CO₂-alquilo C₁₋₆; alquilo C₁₋₆; alquenilo C₁₋₆; alquinilo C₁₋₆; arilo C₆₋₁₀; heteroarilo C₃₋₁₀ o heterocicloalquilo, en donde cualquiera de 1 a 4 átomos de anillo son, de modo independiente, O, S, N o NR; o cicloalquilo C₃₋₁₀; n es 0, 1, 2 ó 3; o es 0 1, 2, 3, 4 ó 5; p es 0, 1, 2 ó 3; y q es 0, 1, 2, 3, 4 ó 5; ⁻ ⁻ ⁻ ⁻ ⁻ es un enlace simple o un enlace doble; siempre que los restos que contienen anillo B y anillo C se sustituyan en posiciones adyacentes en el anillo A.For the treatment of diseases mediated by CFTR, such as cystic fibrosis. The present also characterizes pharmaceutical compositions, method of treatment and their kits. Claim 1: A compound of the formula (1), one of its pharmaceutically acceptable salts, wherein, independently for each occurrence: Ring A is a C₆₋₁₀ aryl ring; C₃₋₁₀ cycloalkyl ring; or a heteroaryl or heterocyclic C₃₋₁₄ ring, wherein any of 1 to 4 ring atoms are, independently, O, S, N or NR; Ring B is a C₃₋₁₀ cycloalkyl ring; an aryl ring C₆₋₁₀; or a heteroaryl or heterocyclic C₄₋₁₀ ring, wherein any of 1 to 4 ring atoms are, independently, O, S, N or NR; Ring C is an aryl ring C₆₋₁₀; a heteroaryl or heterocyclic C₃₋₁₄ ring, wherein any of 1 to 4 ring atoms are, independently, N, NR, O or S; or a C₃₋₁₀ cycloalkyl ring; W is O, NR or S; X is O or NR; Y is, independently, CRR, CO, O, S, SO, SO₂, S (O) NH or NR; Z is NR or CHR; R¹ is halo; CN; F₅S; SiR₃; OH; NRR; C₁₋₆ alkyl or fluoroalkyl; C₁₋₆ alkoxy or fluoroalkoxy; C₁₋₆ alkenyl; C₁₋₆ alkynyl, (C₁₋₉ alkylene) -R⁴, where up to four CH₂ units are independently replaced with O, CO, S, SO, SO₂ or NR; C₆₋₁₀ aryl; C₃₋₁₀ heteroaryl or heterocyclic ring, wherein any of 1 to 4 ring atoms are, independently, O, S, N or NR; or C₃₋₁₀ cycloalkyl; R² is halo; OH; NRR; azide; CN; CO₂R; C₁₋₆ alkyl or fluoroalkyl; C₁₋₆ alkoxy or fluoroalkoxy; C₁₋₆ alkenyl; C₁₋₆ alkynyl; C₆₋₁₀ aryl; C₃₋₁₃ heteroaryl or heterocyclic ring, wherein any of 1 to 4 ring atoms are, independently, O, S, N or NR; C₃₋₁₀ cycloalkyl; or a (rent C₁₋₉) -R⁴, where up to four CH₂ units are replaced, independently, with O, CO, S, SO, SO₂ or NR; two R² can form a group = CH₂ u = O; R³ is halo; CN; OH; CO₂R; C₁₋₆ alkyl or fluoroalkyl; C₁₋₆ alkenyl; C₁₋₆ alkynyl; C₁₋₆ alkoxy or fluoroalkoxy; or aryl C₆₋₁₀; C₃₋₁₀ heteroaryl or heterocyclic ring, wherein any of 1 to 4 ring atoms are, independently, O, S, N or NR; C₃₋₁₀ cycloalkyl; or a (rent C₁₋₉) -R⁴, where up to four CH₂ units are replaced, independently, with O, CO, S, SO, SO₂ or NR; two R³ can form a group = CH₂ u = O; R⁴ is H; azide; CF₃; CHF₂; OR; CCH; CO₂R; OH; C₆₋₁₀ aryl, C₃₋₁₀ heteroaryl or heterocycloalkyl, wherein any of 1 to 4 ring atoms are, independently, O, S, N or NR; C₃₋₁₀ cycloalkyl; NRR, NRCOR, CONRR, CN, halo or SO₂R; R is, independently, H; OH; CO₂H; CO₂-C₁₋₆ alkyl; C₁₋₆ alkyl; C₁₋₆ alkenyl; C₁₋₆ alkynyl; C₆₋₁₀ aryl; C₃₋₁₀ heteroaryl or heterocycloalkyl, wherein any of 1 to 4 ring atoms are, independently, O, S, N or NR; or C₃₋₁₀ cycloalkyl; n is 0, 1, 2 or 3; or is 0 1, 2, 3, 4 or 5; p is 0, 1, 2 or 3; and q is 0, 1, 2, 3, 4 or 5; ⁻ ⁻ ⁻ ⁻ ⁻ Is a single link or a double link; provided that the remains containing ring B and ring C are replaced at adjacent positions in ring A.

ARP150103214A 2014-10-06 2015-10-06 MODULATORS OF THE TRANSMEMBRANE DRIVING REGULATOR OF CHYSICAL FIBROSIS AR102180A1 (en)

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US201462060182P 2014-10-06 2014-10-06

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AR102180A1 true AR102180A1 (en) 2017-02-08

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115004024A (en) * 2020-01-31 2022-09-02 现代药品株式会社 Method for evaluating quality of (3s) -3- (4- (3- (1, 4-dioxaspiro [4,5] dec-7-en-8-yl) benzyloxy) phenyl) hex-4-alkynoic acid

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115004024A (en) * 2020-01-31 2022-09-02 现代药品株式会社 Method for evaluating quality of (3s) -3- (4- (3- (1, 4-dioxaspiro [4,5] dec-7-en-8-yl) benzyloxy) phenyl) hex-4-alkynoic acid
CN115004024B (en) * 2020-01-31 2024-04-26 现代药品株式会社 Method for evaluating quality of (3 s) -3- (4- (3- (1, 4-dioxaspiro [4,5] dec-7-en-8-yl) benzyloxy) phenyl) hex-4-ynoic acid

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