AU2018285677B2 - Tetrahydropyridopyrazine modulators of GPR6 - Google Patents

Tetrahydropyridopyrazine modulators of GPR6 Download PDF

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Publication number
AU2018285677B2
AU2018285677B2 AU2018285677A AU2018285677A AU2018285677B2 AU 2018285677 B2 AU2018285677 B2 AU 2018285677B2 AU 2018285677 A AU2018285677 A AU 2018285677A AU 2018285677 A AU2018285677 A AU 2018285677A AU 2018285677 B2 AU2018285677 B2 AU 2018285677B2
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Prior art keywords
compound
dose
pharmaceutically acceptable
certain embodiments
acceptable salt
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Active
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AU2018285677A
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English (en)
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AU2018285677A1 (en
Inventor
Jason W. Brown
Stephen Hitchcock
Maria HOPKINS
Shota Kikuchi
Todd MACKLIN
Holger Monenschein
Holly REICHARD
Kristin SCHLEICHER
Huikai SUN
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Takeda Pharmaceutical Co Ltd
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Takeda Pharmaceutical Co Ltd
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    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2018285677A 2017-06-15 2018-06-15 Tetrahydropyridopyrazine modulators of GPR6 Active AU2018285677B2 (en)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201762520430P 2017-06-15 2017-06-15
US62/520,430 2017-06-15
US201762591247P 2017-11-28 2017-11-28
US62/591,247 2017-11-28
US201862649856P 2018-03-29 2018-03-29
US62/649,856 2018-03-29
US201862672261P 2018-05-16 2018-05-16
US62/672,261 2018-05-16
PCT/US2018/037687 WO2018232202A1 (en) 2017-06-15 2018-06-15 Tetrahydropyridopyrazine modulators of gpr6

Publications (2)

Publication Number Publication Date
AU2018285677A1 AU2018285677A1 (en) 2019-12-19
AU2018285677B2 true AU2018285677B2 (en) 2022-07-14

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Application Number Title Priority Date Filing Date
AU2018285677A Active AU2018285677B2 (en) 2017-06-15 2018-06-15 Tetrahydropyridopyrazine modulators of GPR6

Country Status (25)

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US (1) US10406157B2 (enExample)
EP (1) EP3638673B9 (enExample)
JP (2) JP7460369B2 (enExample)
KR (1) KR102802861B1 (enExample)
CN (1) CN110730781B (enExample)
AU (1) AU2018285677B2 (enExample)
CA (1) CA3067032A1 (enExample)
CO (1) CO2019015086A2 (enExample)
DK (1) DK3638673T3 (enExample)
ES (1) ES2988680T3 (enExample)
FI (1) FI3638673T3 (enExample)
HR (1) HRP20241231T1 (enExample)
HU (1) HUE068346T2 (enExample)
IL (1) IL271332B2 (enExample)
JO (1) JOP20180057A1 (enExample)
LT (1) LT3638673T (enExample)
MX (1) MX2019014940A (enExample)
PH (1) PH12019502792A1 (enExample)
PL (1) PL3638673T3 (enExample)
PT (1) PT3638673T (enExample)
RS (1) RS66018B1 (enExample)
SG (1) SG11201912149WA (enExample)
SI (1) SI3638673T1 (enExample)
TW (1) TWI775874B (enExample)
WO (1) WO2018232202A1 (enExample)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2026067262A1 (zh) * 2024-09-26 2026-04-02 四川科伦药物研究院有限公司 并环化合物、包含其的药物组合物及其用途和方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015123533A1 (en) * 2014-02-14 2015-08-20 Takeda Pharmaceutical Company Limited Pyrazines modulators of gpr6
WO2015123505A1 (en) * 2014-02-14 2015-08-20 Takeda Pharmaceutical Company Limited Pyridopyrazines modulators of gpr6
US20160031881A1 (en) * 2013-12-20 2016-02-04 Jason W. Brown Tetrahydropyridopyrazines as modulators of gpr6

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
GB9518953D0 (en) 1995-09-15 1995-11-15 Pfizer Ltd Pharmaceutical formulations
GB9711643D0 (en) 1997-06-05 1997-07-30 Janssen Pharmaceutica Nv Glass thermoplastic systems
US7229557B2 (en) 2004-02-04 2007-06-12 Konec, Inc. Method to separate stereoisomers
WO2011005636A1 (en) 2009-07-09 2011-01-13 Merck Sharp & Dohme Corp. Tetrahydronapthyridine orexin receptor antagonists

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20160031881A1 (en) * 2013-12-20 2016-02-04 Jason W. Brown Tetrahydropyridopyrazines as modulators of gpr6
WO2015123533A1 (en) * 2014-02-14 2015-08-20 Takeda Pharmaceutical Company Limited Pyrazines modulators of gpr6
WO2015123505A1 (en) * 2014-02-14 2015-08-20 Takeda Pharmaceutical Company Limited Pyridopyrazines modulators of gpr6

Also Published As

Publication number Publication date
EP3638673B9 (en) 2024-11-20
CN110730781A (zh) 2020-01-24
PT3638673T (pt) 2024-10-07
IL271332B2 (en) 2023-02-01
CN110730781B (zh) 2023-05-05
AU2018285677A1 (en) 2019-12-19
FI3638673T3 (fi) 2024-09-13
PH12019502792A1 (en) 2020-09-14
KR20200014796A (ko) 2020-02-11
TWI775874B (zh) 2022-09-01
HUE068346T2 (hu) 2024-12-28
JP2020523287A (ja) 2020-08-06
JP7497400B2 (ja) 2024-06-10
PL3638673T3 (pl) 2024-11-18
EP3638673B1 (en) 2024-07-17
SG11201912149WA (en) 2020-01-30
US20180360831A1 (en) 2018-12-20
US10406157B2 (en) 2019-09-10
KR102802861B1 (ko) 2025-04-30
LT3638673T (lt) 2024-09-10
WO2018232202A1 (en) 2018-12-20
CA3067032A1 (en) 2018-12-20
EP3638673A4 (en) 2021-03-24
RU2019144408A (ru) 2021-07-15
IL271332B (en) 2022-10-01
TW201906844A (zh) 2019-02-16
IL271332A (en) 2020-01-30
HRP20241231T1 (hr) 2024-12-20
JP7460369B2 (ja) 2024-04-02
MX2019014940A (es) 2020-02-19
SI3638673T1 (sl) 2025-01-31
DK3638673T3 (da) 2024-09-16
NZ759708A (en) 2024-04-26
EP3638673A1 (en) 2020-04-22
JP2022188199A (ja) 2022-12-20
ES2988680T3 (es) 2024-11-21
RS66018B1 (sr) 2024-11-29
CO2019015086A2 (es) 2020-04-13
RU2019144408A3 (enExample) 2021-09-07
BR112019026430A2 (pt) 2020-07-14
JOP20180057A1 (ar) 2019-01-30

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