AR129635A2 - Moduladores de tetrahidropiridopirazina de gpr6 - Google Patents

Moduladores de tetrahidropiridopirazina de gpr6

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Publication number
AR129635A2
AR129635A2 ARP230101544A ARP230101544A AR129635A2 AR 129635 A2 AR129635 A2 AR 129635A2 AR P230101544 A ARP230101544 A AR P230101544A AR P230101544 A ARP230101544 A AR P230101544A AR 129635 A2 AR129635 A2 AR 129635A2
Authority
AR
Argentina
Prior art keywords
group
optionally substituted
alkyl
cycloalkyl
hydrogen
Prior art date
Application number
ARP230101544A
Other languages
English (en)
Inventor
Jason Brown
Stephen Hitchcock
Maria Hopkins
Shota Kikuchi
Holger Monenschein
Holly Reichard
Kristein Schleicher
Huikai Sun
Todd Macklin
Original Assignee
Takeda Pharmaceuticals Co
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=52440811&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR129635(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Takeda Pharmaceuticals Co filed Critical Takeda Pharmaceuticals Co
Publication of AR129635A2 publication Critical patent/AR129635A2/es

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Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Psychology (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

La presente invención proporciona compuestos de fórmula (1) que son útiles como moduladores de GPR6, sus composiciones farmacéuticas, los métodos para el tratamiento de afecciones asociadas con GPR6, los procesos para realizar los compuestos y sus intermediarios. Reivindicación 1: El compuesto de fórmula (1), caracterizado porque R¹ se selecciona del grupo que consiste en cicloalquilo C₃₋₈ opcionalmente sustituido, heterociclilo C₃₋₆ opcionalmente sustituido, arilo C₆₋₁₀ opcionalmente sustituido y heteroarilo C₁₋₁₀ opcionalmente sustituido; X¹ es N y X² es CH; o X¹ es CH y X² es N; o X¹ es N y X² es N; cuando X¹ es N, Z se selecciona del grupo que consiste en alquileno C₁₋₆, haloalquileno C₁₋₆, -C(O)-, y -S(O)₂-; cuando X¹ es CH, Z se selecciona del grupo que consiste en alquileno C₁₋₆, haloalquileno C₁₋₆, -O-, -C(O)-, -NH-, -S-, -S(O)- y -S(O)₂-; q es 0, 1 o 2; s es 0, 1 o 2; R² es -OR⁵ o -NR⁶R⁷; R³, cada vez que se toma, se selecciona de forma independiente del grupo que consiste en alquilo C₁₋₆, cicloalquilo C₃₋₈ y trifluorometilo; p es 0, 1 o 2; R⁴, cada vez que se toma, se selecciona de forma independiente del grupo que consiste en alquilo C₁₋₆, hidroxi y halo; r es 0 o 1; R⁵ se selecciona del grupo que consiste en alquilo C₁₋₆ y cicloalquilo C₃₋₈; R⁶ se selecciona del grupo que consiste en hidrógeno y alquilo C₁₋₆; R⁷ se selecciona del grupo que consiste en alquilo C₁₋₆ opcionalmente sustituido, cicloalquilo C₃₋₈, arilo C₆₋₁₀ opcionalmente sustituido, heteroarilo C₁₋₁₀ opcionalmente sustituido y heterociclilo C₃₋₆ opcionalmente sustituido; X³ se selecciona del grupo que consiste en CH y CR⁴ y X⁴ es NR⁸; o X³ es NR⁸ y X⁴ se selecciona del grupo que consiste en CH y CR⁴; R⁸ se selecciona del grupo que consiste en alquilo C₁₋₆, haloalquilo C₁₋₆, cicloalquilo C₃₋₈, -S(O)₂-R⁹, -C(O)-R¹⁰, -C(O)-N(R¹¹)(R¹²) y -C(O)-OR¹³; R⁹ se selecciona del grupo que consiste en alquilo C₁₋₆, cicloalquilo C₃₋₈ y fenilo opcionalmente sustituido; R¹⁰ se selecciona del grupo que consiste en hidrógeno, alquilo C₁₋₆ opcionalmente sustituido, cicloalquilo C₃₋₈, arilo C₆₋₁₀ opcionalmente sustituido, heteroarilo C₁₋₁₀ opcionalmente sustituido y heterociclilo C₃₋₆ opcionalmente sustituido; R¹¹ se selecciona del grupo que consiste en hidrógeno y alquilo C₁₋₆; R¹² se selecciona del grupo que consiste en hidrógeno, alquilo C₁₋₆ y cicloalquilo C₃₋₈; o R¹¹ y R¹² se toman entre sí con el nitrógeno al que se unen para formar un anillo saturado de 4 a 7 miembros que tiene opcionalmente 1 heteroátomo en el anillo adicional que se selecciona del grupo N, O y S y se sustituye opcionalmente sobre cualquiera de los átomos de carbono del anillo con 1 a 5 sustituyentes que se seleccionan de forma independiente del grupo que consiste en ciano, halo, hidroxi, amino, heterociclilo C₃₋₆ opcionalmente sustituido, amida C₁₋₉, alquilo C₁₋₆ opcionalmente sustituido y alcoxi C₁₋₄ y se sustituye sobre cualquier nitrógeno en el anillo adicional por un sustituyente que se selecciona del grupo que consiste en hidrógeno, cicloalquilo C₃₋₈ y alquilo C₁₋₆ opcionalmente sustituido; R¹³ se selecciona del grupo que consiste en alquilo C₁₋₆ y cicloalquilo C₃₋₈; o su sal farmacéuticamente aceptable.
ARP230101544A 2013-12-20 2023-06-15 Moduladores de tetrahidropiridopirazina de gpr6 AR129635A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361919661P 2013-12-20 2013-12-20

Publications (1)

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AR129635A2 true AR129635A2 (es) 2024-09-11

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ARP140104807A AR098872A1 (es) 2013-12-20 2014-12-19 Moduladores de tetrahidropiridopirazinas de gpr6
ARP230101544A AR129635A2 (es) 2013-12-20 2023-06-15 Moduladores de tetrahidropiridopirazina de gpr6

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US (4) US9181249B2 (es)
EP (2) EP3453709A1 (es)
JP (1) JP6538697B2 (es)
KR (1) KR102441531B1 (es)
CN (2) CN108658978A (es)
AR (2) AR098872A1 (es)
AU (1) AU2014368992C1 (es)
BR (1) BR112016014020B1 (es)
CA (1) CA2934247C (es)
CL (1) CL2016001595A1 (es)
CR (1) CR20160321A (es)
CY (1) CY1121395T1 (es)
DK (1) DK3083620T3 (es)
DO (1) DOP2016000144A (es)
EA (1) EA032443B1 (es)
EC (1) ECSP16061758A (es)
ES (1) ES2702187T3 (es)
GE (1) GEP201706783B (es)
HR (1) HRP20182004T1 (es)
HU (1) HUE042443T2 (es)
IL (1) IL246177B (es)
JO (1) JO3466B1 (es)
LT (1) LT3083620T (es)
MA (1) MA39193B1 (es)
MX (1) MX2016008188A (es)
MY (1) MY177031A (es)
NZ (1) NZ721723A (es)
PE (1) PE20160751A1 (es)
PH (1) PH12016501192B1 (es)
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UA (1) UA120427C2 (es)
UY (1) UY35908A (es)
WO (1) WO2015095728A1 (es)
ZA (1) ZA201604703B (es)

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ES2702187T3 (es) 2019-02-27
BR112016014020B1 (pt) 2023-02-28
AU2014368992A1 (en) 2016-07-07
EP3453709A1 (en) 2019-03-13
EP3083620A1 (en) 2016-10-26
DK3083620T3 (en) 2019-01-14
MY177031A (en) 2020-09-02
DOP2016000144A (es) 2016-08-15
MA39193A1 (fr) 2017-06-30
EP3083620B1 (en) 2018-10-03
SG11201604921TA (en) 2016-07-28
US20180346464A1 (en) 2018-12-06
CL2016001595A1 (es) 2017-01-13
IL246177A0 (en) 2016-08-02
ECSP16061758A (es) 2018-02-28
PL3083620T4 (pl) 2019-09-30
NZ721723A (en) 2021-07-30
BR112016014020A2 (pt) 2017-08-08
TR201900038T4 (tr) 2019-01-21
RS58092B1 (sr) 2019-02-28
HUE042443T2 (hu) 2019-06-28
CN108658978A (zh) 2018-10-16
CA2934247C (en) 2023-01-17
US9181249B2 (en) 2015-11-10
WO2015095728A1 (en) 2015-06-25
SI3083620T1 (sl) 2019-02-28
US10077266B2 (en) 2018-09-18
PH12016501192A1 (en) 2016-08-15
EA201691272A1 (ru) 2017-05-31
US20170283414A1 (en) 2017-10-05
JP6538697B2 (ja) 2019-07-03
AR098872A1 (es) 2016-06-22
MA39193B1 (fr) 2018-04-30
US20160031881A1 (en) 2016-02-04
KR102441531B1 (ko) 2022-09-07
LT3083620T (lt) 2019-02-11
AU2014368992C1 (en) 2019-02-21
CY1121395T1 (el) 2020-05-29
BR112016014020A8 (pt) 2018-01-30
PE20160751A1 (es) 2016-08-01
CR20160321A (es) 2016-09-28
ZA201604703B (en) 2018-11-28
CN105829309A (zh) 2016-08-03
KR20160099705A (ko) 2016-08-22
TWI730937B (zh) 2021-06-21
US20150175602A1 (en) 2015-06-25
US10738046B2 (en) 2020-08-11
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