PE20160648A1 - Compuestos espirociclicos como inhibidores de triptofano hidroxilasa - Google Patents

Compuestos espirociclicos como inhibidores de triptofano hidroxilasa

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Publication number
PE20160648A1
PE20160648A1 PE2016000340A PE2016000340A PE20160648A1 PE 20160648 A1 PE20160648 A1 PE 20160648A1 PE 2016000340 A PE2016000340 A PE 2016000340A PE 2016000340 A PE2016000340 A PE 2016000340A PE 20160648 A1 PE20160648 A1 PE 20160648A1
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Peru
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halo
compounds
tryptophan hydroxylase
spirocyclic compounds
hydroxylase inhibitors
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PE2016000340A
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English (en)
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Andrew Scribner
Eric Brian Sjogren
Lombaert Stephane De
Daniel R Goldberg
Kenneth Brameld
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Karos Pharmaceuticals Inc
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Publication of PE20160648A1 publication Critical patent/PE20160648A1/es

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    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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Abstract

La presente invencion se refiere a compuestos espirociclicos de formula (I) en donde el anillo A es cicloalquilo C3-C10, entre otros; L es O o NR4; W es N o CR5; X es N o CR6; Y es N o CR7; R1 es H, alquilo C1-C10, entre otros; R2 y R3 son H, alquilo C1-C4 y haloalquilo C1-C4; RA es H, halo, entre otros; RB es H, halo, entre otros; RC y RD son H, halo, entre otros; n es 1 o 2. Son compuestos preferidos: acido (S)-8-(2-amino-6-((R)-2,2,2-trifluoro-1-(3-(3-metiI-1H-pirazol-1-il)-4'-(metiltio)-[1,1'-bifenil]-4-il)etoxi)pirimidin-4-il)-2,8-diazaspiro[4.5]decano-3-carboxilico, acido (S)-8-(2-amino-6-((R)-1-(3'-carboxi-3-(3-metil-1H-pirazol-1-il)-[1,1'-bifenil]-4-il)-2,2,2-trifluoroetoxi)pirimidin-4-il)-2,8-diazaspiro[4.5]decano-3-carboxilico, entre otros. Dichos compuestos son inhibidores de triptofano hidroxilasa (TPH), particularmente la isoforma 1, siendo utiles en el tratamiento de enfermedades relacionadas con serotonina periferica, por ejemplo, enfermedades gastrointestinales, cardiovasculares, pulmonares, inflamatorias, entre otros y cancer
PE2016000340A 2013-09-06 2014-09-05 Compuestos espirociclicos como inhibidores de triptofano hidroxilasa PE20160648A1 (es)

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US201361874545P 2013-09-06 2013-09-06
US201361899943P 2013-11-05 2013-11-05
US201462004385P 2014-05-29 2014-05-29

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US (8) US9199994B2 (es)
EP (1) EP3041842B8 (es)
JP (1) JP6470290B2 (es)
KR (1) KR102336075B1 (es)
CN (1) CN105764902B (es)
AR (1) AR097571A1 (es)
AU (1) AU2014315109B2 (es)
CA (1) CA2922933C (es)
CL (1) CL2016000509A1 (es)
CY (1) CY1122652T1 (es)
DK (1) DK3041842T3 (es)
EA (1) EA032304B1 (es)
EC (1) ECSP16014324A (es)
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HK (1) HK1225720A1 (es)
HR (1) HRP20200098T1 (es)
HU (1) HUE047574T2 (es)
IL (1) IL244315B (es)
LT (1) LT3041842T (es)
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MY (1) MY186265A (es)
PE (1) PE20160648A1 (es)
PH (1) PH12016500416A1 (es)
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PT (1) PT3041842T (es)
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