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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

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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
    • C07D401/14—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 three or more hetero rings
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic 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
    • 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
    • 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
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic 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
    • C07D241/14—Heterocyclic 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
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic 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
    • C07D241/14—Heterocyclic 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
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon 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
    • C07D241/28—Carbon 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
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

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 (2) GEAP201814266A (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 (7)

* Cited by examiner, † Cited by third party
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MY184366A (en) * 2014-02-14 2021-04-01 Takeda Pharmaceuticals Co Pyrazines modulators of gpr6
KR20210141778A (ko) 2016-06-07 2021-11-23 자코바이오 파마슈티칼스 컴퍼니 리미티드 Shp2 억제제로서 유용한 신규한 헤테로환형 유도체
EA201992253A1 (ru) 2017-03-23 2020-03-31 Джакобио Фармасьютикалс Ко., Лтд. Новые гетероциклические производные, применимые в качестве ингибиторов shp2
CN110520127B (zh) * 2017-03-26 2023-05-16 武田药品工业株式会社 作为gpr6的调节剂的经哌啶基取代的杂芳族羧酰胺和经哌嗪基取代的杂芳族羧酰胺
JOP20180057A1 (ar) * 2017-06-15 2019-01-30 Takeda Pharmaceuticals Co مركبات رابع هيدروبيريدو بيرازين والتي تعمل كمعدلات gpr6
US20210393623A1 (en) 2018-09-26 2021-12-23 Jacobio Pharmaceuticals Co., Ltd. Novel Heterocyclic Derivatives Useful as SHP2 Inhibitors
EP4143163A1 (en) * 2020-04-30 2023-03-08 Oregon Health & Science University Antagonists of gpr39 protein

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Also Published As

Publication number Publication date
AU2015218402A1 (en) 2016-09-15
IL247140B (en) 2020-02-27
MX2016010529A (es) 2016-10-31
GEAP201814266A (en) 2018-05-10
CA2939382A1 (en) 2015-08-20
JP6484640B2 (ja) 2019-03-13
US20180258073A1 (en) 2018-09-13
MA39337B1 (fr) 2019-11-29
WO2015123533A1 (en) 2015-08-20
CN106103421B (zh) 2019-04-09
MY184366A (en) 2021-04-01
UA117779C2 (uk) 2018-09-25
US10273225B2 (en) 2019-04-30
PH12016501613B1 (en) 2021-10-01
CL2016002043A1 (es) 2017-02-17
CR20160428A (es) 2017-04-04
EA033861B1 (ru) 2019-12-03
JP2017509601A (ja) 2017-04-06
IL247140A0 (en) 2016-09-29
EA201691632A1 (ru) 2017-02-28
DOP2016000211A (es) 2016-10-16
AU2015218402B2 (en) 2019-07-11
US20170174659A1 (en) 2017-06-22
MX369857B (es) 2019-11-25
KR20160122215A (ko) 2016-10-21
ECSP16074207A (es) 2017-09-29
EP3105216B1 (en) 2018-10-10
EP3105216A1 (en) 2016-12-21
ES2702205T3 (es) 2019-02-27
CN106103421A (zh) 2016-11-09
GEP20186893B (en) 2018-09-10
US10000468B2 (en) 2018-06-19
BR112016018418A2 (pt) 2017-08-08
PH12016501613A1 (en) 2017-02-06
MA39337A1 (fr) 2017-10-31
ZA201606077B (en) 2018-11-28

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