AR106113A1 - DERIVATIVES OF 2,3,4,5-TETRAHYDROPIRIDIN-6-AMINA - Google Patents

DERIVATIVES OF 2,3,4,5-TETRAHYDROPIRIDIN-6-AMINA

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Publication number
AR106113A1
AR106113A1 ARP160102894A ARP160102894A AR106113A1 AR 106113 A1 AR106113 A1 AR 106113A1 AR P160102894 A ARP160102894 A AR P160102894A AR P160102894 A ARP160102894 A AR P160102894A AR 106113 A1 AR106113 A1 AR 106113A1
Authority
AR
Argentina
Prior art keywords
alkyloxy
alkyl
cyclopropyl
monohalo
cyclopropyloxy
Prior art date
Application number
ARP160102894A
Other languages
Spanish (es)
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR106113A1 publication Critical patent/AR106113A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Compuestos de 2,3,4,5-tetrahidropiridin-6-amina inhibidores de b-secretasa. También se refiere a composiciones farmacéuticas que comprenden tales compuestos, a procesos para preparar tales compuestos y composiciones, y al uso de tales compuestos y composiciones para prevenir y tratar trastornos en los que participa la b-secreta, tales como la enfermedad de Alzheimer (EA), el deterioro cognitivo leve, senilidad, demencia, demencia con cuerpos de Lewy, síndrome de Down, demencia asociada con el accidente cerebrovascular, demencia asociada con la enfermedad de Parkinson o demencia asociada con b-amiloides. Reivindicación 1: Un compuesto de formula (1) o un tautómero o forma estereoisomérica de este, donde R¹ se selecciona del grupo que consiste en -alquilo C₁₋₃, -alquilo C₁₋₃-F y flúor; R² se selecciona del grupo que consiste en -SO₂-alquilo C₁₋₃, -SO₂-ciclopropilo, -CN, -O-alquilo C₁₋₃, CF₃ y SO(NCH₃)CH₃; Ar es homoarilo o heteroarilo; en donde homoarilo es fenilo o fenilo sustituido con uno, dos o tres sustituyentes, seleccionados cada uno independientemente entre el grupo que consiste en halo, ciano, alquilo C₁₋₃, ciclopropilo, alquiloxi C₁₋₃, ciclopropiloxi, (ciclopropil)alquiloxi C₁₋₃, monohalo-alquilo C₁₋₃ polihalo-alquilo C₁₋₃ monohalo-ciclopropilo, polihalo-ciclopropilo, monohalo-alquiloxi C₁₋₃, polihalo-alquiloxi C₁₋₃ monohalo-ciclopropiloxi, polihalo-ciclopropiloxi, (alquiloxi C₁₋₃)alquiloxi C₁₋₃, (ciclopropiloxi)alquiloxi C₁₋₃ y HCºCCH₂O; heteroarilo se selecciona del grupo constituido por piridilo, pirimidinilo, pirazinilo, piridazinilo, furanilo, tienilo, pirrolilo, pirazolilo, imidazolilo, triazolilo, tetrazolilo, tiazolilo, isotiazolilo, tiadiazolilo, oxazolilo, isoxazolilo y oxadiazolilo, cada uno opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados cada uno independientemente del grupo que consiste en halo, ciano, alquilo C₁₋₃, ciclopropilo, alquinilo C₂₋₃, alquiloxi C₁₋₃, ciclopropiloxi, (ciclopropil)alquiloxi C₁₋₃, monohalo-alquilo C₁₋₃, polihalo-alquilo C₁₋₃, monohalo-ciclopropilo, polihalo-ciclopropilo, monohalo-alquiloxi C₁₋₃, polihalo-alquiloxi C₁₋₃, monohalo-ciclopropiloxi, polihalo-ciclopropiloxi, (alquiloxi C₁₋₃)alquiloxi C₁₋₃, (ciclopropiloxi)alquiloxi C₁₋₃ y HCºCCH₂O; R³, R⁴, R⁵, y R⁶ se seleccionan cada uno independientemente del grupo que consiste en H, flúor, metilo y metoxi; y R⁷ es hidrógeno o flúor; o un solvato o una sal de adición farmacéuticamente aceptables de este.Compounds of 2,3,4,5-tetrahydropyridin-6-amine b-secretase inhibitors. It also refers to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions to prevent and treat disorders in which b-secretion participates, such as Alzheimer's disease (AD). ), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with b-amyloid. Claim 1: A compound of formula (1) or a stereoisomeric tautomer or form thereof, wherein R¹ is selected from the group consisting of -C₁₋₃ alkyl, -C₁₋₃-F alkyl and fluorine; R² is selected from the group consisting of -SO₂-C₁₋₃ alkyl, -SO₂-cyclopropyl, -CN, -O-C₁₋₃ alkyl, CF₃ and SO (NCH₃) CH₃; Ar is homoaryl or heteroaryl; wherein homoaryl is phenyl or phenyl substituted with one, two or three substituents, each independently selected from the group consisting of halo, cyano, C₁₋₃ alkyl, cyclopropyl, C₁₋₃ alkyloxy, cyclopropyloxy, (cyclopropyl) C₁₋ alkyloxy ₃, monohalo-C₁₋₃ alkyl polyhalo-C₁₋₃ alkyl monohalo-cyclopropyl, polyhalo-cyclopropyl, monohalo-C alquilo alkyloxy, polyhalo-C₁₋₃ monohalo-cyclopropyloxy, polyhalo-cyclopropyloxy, (C₁₋₃ alkyloxy) C₁₋₃, (cyclopropyloxy) C₁₋₃ alkyloxy and HCCCH₂O; heteroaryl is selected from the group consisting of pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, triazolyl, tetrazolyl, thiazolyl, isothiazolyl, thiadiazolyl, oxazolyl, isoxazolyl and oxadiazolyl, each optionally substituted with two three substituents each independently selected from the group consisting of halo, cyano, C₁₋₃ alkyl, cyclopropyl, C₂₋₃ alkynyl, C₁₋₃ alkyloxy, cyclopropyloxy, (cyclopropyl) C₁₋₃ alkyloxy, monohalo-C₁₋₃ alkyl, polyhalo -C₁₋₃ alkyl, monohalo-cyclopropyl, polyhalo-cyclopropyl, monohalo-C₁₋₃ alkyloxy, polyhalo-C₁₋₃ alkyloxy, monohalo-cyclopropyloxy, polyhalo-cyclopropyloxy, (C₁₋₃ alkyloxy), (cyclopropyloxy) C₁₋₃ alkyloxy and HCºCCH₂O; R³, R⁴, R⁵, and R⁶ are each independently selected from the group consisting of H, fluorine, methyl and methoxy; and R⁷ is hydrogen or fluorine; or a pharmaceutically acceptable solvate or addition salt thereof.

ARP160102894A 2015-09-23 2016-09-22 DERIVATIVES OF 2,3,4,5-TETRAHYDROPIRIDIN-6-AMINA AR106113A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP15186394 2015-09-23

Publications (1)

Publication Number Publication Date
AR106113A1 true AR106113A1 (en) 2017-12-13

Family

ID=54196872

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP160102894A AR106113A1 (en) 2015-09-23 2016-09-22 DERIVATIVES OF 2,3,4,5-TETRAHYDROPIRIDIN-6-AMINA

Country Status (1)

Country Link
AR (1) AR106113A1 (en)

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