PE20170245A1 - Pirazinas moduladoras de gpr 6 - Google Patents

Pirazinas moduladoras de gpr 6

Info

Publication number
PE20170245A1
PE20170245A1 PE2016001477A PE2016001477A PE20170245A1 PE 20170245 A1 PE20170245 A1 PE 20170245A1 PE 2016001477 A PE2016001477 A PE 2016001477A PE 2016001477 A PE2016001477 A PE 2016001477A PE 20170245 A1 PE20170245 A1 PE 20170245A1
Authority
PE
Peru
Prior art keywords
alkyl
cycloalkyl
optionally substituted
pirazines
gpr
Prior art date
Application number
PE2016001477A
Other languages
English (en)
Inventor
Huikai Sun
Holly Reichard
Holger Monenschein
Betty Lam
Mark E Adams
Maria Hopkins
Stephen Hitchcock
Jason W Brown
Shota Kikuchi
Original Assignee
Takeda Pharmaceuticals Co
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 Takeda Pharmaceuticals Co filed Critical Takeda Pharmaceuticals Co
Publication of PE20170245A1 publication Critical patent/PE20170245A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • C07D241/28Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond

Abstract

La presente invencion se refiere a un compuestos de pirazina de formula I donde: R1 es cicloalquilo C3-C8, heterociclilo C3-C6 o heteroarilo C1-C10 opcionalmente sustituidos; cuando X1 es N, X2 es N o CH y Z es alquileno C1-C6, haloalquileno C1-C6, entre otros y cuando X1 es CH, X2 es N y Z es haloalquileno C1-C6, -O-, entre otros; q, s y p son 0,1 o 2; ; r es 1 o 2; R2 es -OR5 o -NR6R7; R3 es alquilo C1-C6, cicloalquilo C3-C8, entre otros; R4 es alquilo C1-C6 opcionalmente sustituido, ciano, entre otros;R5 es alquilo C1-C6 o cicloalquilo C3-C8; R6 es H o alquilo C1-C6; R7 es alquilo C1-C6 opcionalmente sustituido, cicloalquilo C3-C8, entre otros. Tambien se refiere a una composicion farmaceutica. Dichos compuestos modulan el receptor 6 acoplado a la proteina G (GPR6), siendo utiles en el tratamiento de trastornos neurologicos y psiquiatricos
PE2016001477A 2014-02-14 2015-02-13 Pirazinas moduladoras de gpr 6 PE20170245A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201461940294P 2014-02-14 2014-02-14

Publications (1)

Publication Number Publication Date
PE20170245A1 true PE20170245A1 (es) 2017-03-30

Family

ID=52598823

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2016001477A PE20170245A1 (es) 2014-02-14 2015-02-13 Pirazinas moduladoras de gpr 6

Country Status (24)

Country Link
US (2) US10000468B2 (es)
EP (1) EP3105216B1 (es)
JP (1) JP6484640B2 (es)
KR (1) KR20160122215A (es)
CN (1) CN106103421B (es)
AU (1) AU2015218402B2 (es)
BR (1) BR112016018418A2 (es)
CA (1) CA2939382A1 (es)
CL (1) CL2016002043A1 (es)
CR (1) CR20160428A (es)
DO (1) DOP2016000211A (es)
EA (1) EA033861B1 (es)
EC (1) ECSP16074207A (es)
ES (1) ES2702205T3 (es)
GE (1) GEP20186893B (es)
IL (1) IL247140B (es)
MA (1) MA39337B1 (es)
MX (1) MX369857B (es)
MY (1) MY184366A (es)
PE (1) PE20170245A1 (es)
PH (1) PH12016501613B1 (es)
UA (1) UA117779C2 (es)
WO (1) WO2015123533A1 (es)
ZA (1) ZA201606077B (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA39337B1 (fr) * 2014-02-14 2019-11-29 Takeda Pharmaceuticals Co Modulateurs de pyrazines de gpr6
EP4108659A1 (en) 2016-06-07 2022-12-28 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
AU2018239542C1 (en) 2017-03-23 2021-02-11 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as SHP2 inhibitors
CA3054945A1 (en) 2017-03-26 2018-10-04 Takeda Pharmaceutical Company Limited Piperidinyl- and piperazinyl-substituted heteroaromatic carboxamides as modulators of gpr6
JOP20180057A1 (ar) * 2017-06-15 2019-01-30 Takeda Pharmaceuticals Co مركبات رابع هيدروبيريدو بيرازين والتي تعمل كمعدلات gpr6

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4159331A (en) * 1978-05-05 1979-06-26 The Upjohn Company Antihypertensive 4-aminoquinolines
US5563142A (en) * 1989-12-28 1996-10-08 The Upjohn Company Diaromatic substituted compounds as anti-HIV-1 agents
JP2004515449A (ja) * 1999-02-26 2004-05-27 アリーナ・フアーマシユーチカルズ・インコーポレーテツド 第6gタンパク質共役型受容体の小分子調節物質
US6774138B2 (en) 1999-08-31 2004-08-10 Merck & Co., Inc. Thiazolyl(pyridyl)ethyne compounds
WO2001060806A2 (en) 2000-02-16 2001-08-23 Neurogen Corporation Substituted arylpyrazines
AU2002319183B2 (en) * 2001-06-01 2007-05-10 F. Hoffmann-La Roche Ag Pyrimidine, triazine and pyrazine derivatives as glutamate receptors
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
CN101450934B (zh) 2002-03-13 2012-10-10 詹森药业有限公司 用作组蛋白去乙酰酶抑制剂的磺酰基衍生物
AU2003289330A1 (en) * 2002-12-13 2004-07-09 Kyowa Hakko Kogyo Co., Ltd. Preventives and/or remedies for central diseases
SG145701A1 (en) 2003-07-30 2008-09-29 Xenon Pharmaceuticals Inc Piperazine derivatives and their use as therapeutic agents
US20050070718A1 (en) * 2003-09-30 2005-03-31 Abbott Gmbh & Co. Kg Heteroaryl-substituted 1,3-dihydroindol-2-one derivatives and medicaments containing them
US8580842B2 (en) * 2003-09-30 2013-11-12 Abbott Gmbh & Co. Kg Heteroaryl-substituted 1,3-dihydroindol-2-one derivatives and medicaments containing them
AU2005215379A1 (en) * 2004-02-12 2005-09-01 Merck & Co., Inc. Bipyridyl amides as modulators of metabotropic glutamate receptor-5
DE602005019556D1 (de) 2004-04-13 2010-04-08 Icagen Inc Polycyclische pyrazine als kaliumionenkanal-modulatoren
GB0414438D0 (en) * 2004-06-28 2004-07-28 Syngenta Participations Ag Chemical compounds
US20060199828A1 (en) 2005-03-04 2006-09-07 Georg Jaeschke Pyrazine-2-carboxyamide derivatives
KR20080014775A (ko) 2005-05-13 2008-02-14 렉시컨 파마슈티컬스 인코퍼레이티드 다환 화합물 및 그의 사용 방법
WO2007044085A2 (en) 2005-05-19 2007-04-19 Xenon Pharmaceuticals Inc. Heteroaryl compounds and their uses as therapeutic agents
US8495335B2 (en) * 2006-06-16 2013-07-23 Raytheon Company Data translation system and method
JP2011524917A (ja) 2008-06-20 2011-09-08 メタボレックス, インコーポレイテッド アリールgpr119作動薬およびその使用
DK2563776T3 (en) 2010-04-27 2016-09-19 Calcimedica Inc Relations that modulate intracellular calcium
CA2798325A1 (en) 2010-05-13 2011-11-17 Amgen Inc. Heteroaryloxyheterocyclyl compounds as pde10 inhibitors
MA34300B1 (fr) * 2010-05-13 2013-06-01 Amgen Inc Composés azotés hétérocycliques convenant comme inhibiteurs de la pde10
US20120184572A1 (en) 2011-01-13 2012-07-19 Metabolex, Inc. Aryl gpr119 agonists and uses thereof
US10252984B2 (en) * 2011-10-27 2019-04-09 Mayo Foundation For Medical Education And Research Inhibiting G protein coupled receptor 6 kinase polypeptides
US9487526B2 (en) * 2012-08-13 2016-11-08 Takeda Pharmaceutical Company Limited Quinoxaline derivatives as GPR6 modulators
AU2014340318B2 (en) 2013-10-21 2019-01-17 Merck Patent Gmbh Heteroaryl compounds as BTK inhibitors and uses thereof
MA39337B1 (fr) * 2014-02-14 2019-11-29 Takeda Pharmaceuticals Co Modulateurs de pyrazines de gpr6

Also Published As

Publication number Publication date
US10273225B2 (en) 2019-04-30
CA2939382A1 (en) 2015-08-20
KR20160122215A (ko) 2016-10-21
BR112016018418A2 (pt) 2017-08-08
EP3105216A1 (en) 2016-12-21
EA201691632A1 (ru) 2017-02-28
CN106103421A (zh) 2016-11-09
GEP20186893B (en) 2018-09-10
WO2015123533A1 (en) 2015-08-20
EP3105216B1 (en) 2018-10-10
US10000468B2 (en) 2018-06-19
CN106103421B (zh) 2019-04-09
UA117779C2 (uk) 2018-09-25
MA39337B1 (fr) 2019-11-29
AU2015218402A1 (en) 2016-09-15
CR20160428A (es) 2017-04-04
CL2016002043A1 (es) 2017-02-17
US20180258073A1 (en) 2018-09-13
DOP2016000211A (es) 2016-10-16
ES2702205T3 (es) 2019-02-27
MX369857B (es) 2019-11-25
IL247140A0 (en) 2016-09-29
PH12016501613A1 (en) 2017-02-06
MA39337A1 (fr) 2017-10-31
MY184366A (en) 2021-04-01
JP2017509601A (ja) 2017-04-06
AU2015218402B2 (en) 2019-07-11
MX2016010529A (es) 2016-10-31
ZA201606077B (en) 2018-11-28
IL247140B (en) 2020-02-27
EA033861B1 (ru) 2019-12-03
ECSP16074207A (es) 2017-09-29
PH12016501613B1 (en) 2017-02-06
US20170174659A1 (en) 2017-06-22
JP6484640B2 (ja) 2019-03-13

Similar Documents

Publication Publication Date Title
PE20170245A1 (es) Pirazinas moduladoras de gpr 6
PE20141202A1 (es) Compuesto de ciclopropanoamina
PE20191478A1 (es) Compuestos moduladores del receptor de hidorcarburos de arilo (ahr)
PE20200292A1 (es) Compuestos de heteroarilo biciclicos 6-6 fusionados y su uso como inhibidores de lats
PE20191479A1 (es) Compuestos moduladores del receptor de hidrocarburos de arilo (ahr)
PE20151781A1 (es) Piridonamidas como moduladores de canales de sodio
PE20170268A1 (es) Compuestos de heteroarilo para la inhibicion de cinasa
PE20161443A1 (es) Compuestos
PE20240221A1 (es) Pirimidin-2-ilamino-1h-pirazoles como inhibidores de lrrk2 para el uso en el tratamiento de trastornos neurodegenerativos
CY1120325T1 (el) Τρικυκλικες ετεροκυκλικες ενωσεις ως αναστολεις φωσφοϊνοσιτιδιου 3-κινασης
PE20171623A1 (es) Agentes inmunomoduladores
PE20181015A1 (es) 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1
AR061644A1 (es) Derivados de benzofurano
GEP201706608B (en) 1 - arylcarbonyl - 4 - oxy – piperidine compounds useful for the treatment of neurodegenerative diseases
PE20141791A1 (es) Compuestos de enediino, conjugados de los mismos y sus usos y metodos
PE20110397A1 (es) Compuestos que modulan selectivamente el receptor cb2
PE20180355A1 (es) Desacetoxitubulisina h y analogos de esta
PE20161444A1 (es) 1,2-ciclopentanos sustituidos como antagonistas del receptor de orexina
PE20140703A1 (es) Derivados de heteroarilo como moduladores de nachr alfa 7
PE20110196A1 (es) 5-alquinil-pirimidinas
PE20191082A1 (es) Inhibidores de la tirosina quinasa de bruton
PE20120063A1 (es) Derivados de ciclopropilamida dirigidos contra el receptor de histamina h3
MX2018014164A (es) Intermedios para la sintesis de derivados de acido biliar, en particular, de acido obeticolico.
PE20191103A1 (es) Inhibidores de dopamina-b-hidroxilasa
PE20141940A1 (es) Compuestos triciclicos, composiciones que los comprenden y usos de los mismos