TWI508959B - 用作pde10抑制劑的氮雜環丁烷和哌啶化合物 - Google Patents

用作pde10抑制劑的氮雜環丁烷和哌啶化合物 Download PDF

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Publication number
TWI508959B
TWI508959B TW102121229A TW102121229A TWI508959B TW I508959 B TWI508959 B TW I508959B TW 102121229 A TW102121229 A TW 102121229A TW 102121229 A TW102121229 A TW 102121229A TW I508959 B TWI508959 B TW I508959B
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TW
Taiwan
Prior art keywords
compound
pharmaceutically acceptable
acceptable salt
formula
group
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TW102121229A
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English (en)
Chinese (zh)
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TW201412729A (zh
Inventor
Jennifer R Allen
Jian J Chen
Michael J Frohn
Matthew R Kaller
Qingyian Liu
Thomas T Nguyen
Alexander J Pickrell
Wenyuan Qian
Robert M Rzasa
Wenge Zhong
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Amgen Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=48692687&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TWI508959(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Amgen Inc filed Critical Amgen Inc
Publication of TW201412729A publication Critical patent/TW201412729A/zh
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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
    • A61K31/4965—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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61P25/14—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
    • A61P25/18—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
    • A61P25/28—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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
TW102121229A 2012-06-14 2013-06-14 用作pde10抑制劑的氮雜環丁烷和哌啶化合物 TWI508959B (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261659911P 2012-06-14 2012-06-14

Publications (2)

Publication Number Publication Date
TW201412729A TW201412729A (zh) 2014-04-01
TWI508959B true TWI508959B (zh) 2015-11-21

Family

ID=48692687

Family Applications (1)

Application Number Title Priority Date Filing Date
TW102121229A TWI508959B (zh) 2012-06-14 2013-06-14 用作pde10抑制劑的氮雜環丁烷和哌啶化合物

Country Status (25)

Country Link
US (3) US8691986B2 (cg-RX-API-DMAC10.html)
EP (1) EP2864317A1 (cg-RX-API-DMAC10.html)
JP (1) JP2015519402A (cg-RX-API-DMAC10.html)
KR (1) KR20150023417A (cg-RX-API-DMAC10.html)
CN (1) CN104619694A (cg-RX-API-DMAC10.html)
AP (1) AP2014008136A0 (cg-RX-API-DMAC10.html)
AR (1) AR091436A1 (cg-RX-API-DMAC10.html)
AU (1) AU2013274153B2 (cg-RX-API-DMAC10.html)
BR (1) BR112014031368A2 (cg-RX-API-DMAC10.html)
CA (1) CA2875802A1 (cg-RX-API-DMAC10.html)
CL (1) CL2014003391A1 (cg-RX-API-DMAC10.html)
CO (1) CO7160011A2 (cg-RX-API-DMAC10.html)
CR (1) CR20150012A (cg-RX-API-DMAC10.html)
EA (1) EA201590014A1 (cg-RX-API-DMAC10.html)
HK (1) HK1203935A1 (cg-RX-API-DMAC10.html)
IL (1) IL235901A0 (cg-RX-API-DMAC10.html)
MA (1) MA37748B1 (cg-RX-API-DMAC10.html)
MX (1) MX2014014924A (cg-RX-API-DMAC10.html)
PE (1) PE20150348A1 (cg-RX-API-DMAC10.html)
PH (1) PH12014502780A1 (cg-RX-API-DMAC10.html)
SG (1) SG11201408168UA (cg-RX-API-DMAC10.html)
TN (1) TN2014000510A1 (cg-RX-API-DMAC10.html)
TW (1) TWI508959B (cg-RX-API-DMAC10.html)
UY (1) UY34858A (cg-RX-API-DMAC10.html)
WO (1) WO2013188724A1 (cg-RX-API-DMAC10.html)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103221404B (zh) 2010-05-13 2015-12-16 安姆根有限公司 可用作pde10抑制剂的不饱和氮杂环化合物
AR091436A1 (es) * 2012-06-14 2015-02-04 Amgen Inc Compuestos de azetidina y piperidina utiles como inhibidores de pde10

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011143365A1 (en) * 2010-05-13 2011-11-17 Amgen Inc. Nitrogen heterocyclic compounds useful as pde10 inhibitors
WO2011143366A1 (en) * 2010-05-13 2011-11-17 Amgen Inc. Heteroaryloxycarbocyclyl compounds as pde10 inhibitors

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4107288A (en) 1974-09-18 1978-08-15 Pharmaceutical Society Of Victoria Injectable compositions, nanoparticles useful therein, and process of manufacturing same
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
US5145684A (en) 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
CA2800578A1 (en) * 2010-05-13 2011-11-17 Amgen Inc. Nitrogen-heterocyclic compounds as phosphodiesterase 10 inhibitors
EP2569302A1 (en) * 2010-05-13 2013-03-20 Amgen, Inc Heteroaryloxyheterocyclyl compounds as pde10 inhibitors
AR091436A1 (es) * 2012-06-14 2015-02-04 Amgen Inc Compuestos de azetidina y piperidina utiles como inhibidores de pde10

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011143365A1 (en) * 2010-05-13 2011-11-17 Amgen Inc. Nitrogen heterocyclic compounds useful as pde10 inhibitors
WO2011143366A1 (en) * 2010-05-13 2011-11-17 Amgen Inc. Heteroaryloxycarbocyclyl compounds as pde10 inhibitors

Also Published As

Publication number Publication date
AU2013274153A1 (en) 2014-12-18
EA201590014A1 (ru) 2015-04-30
JP2015519402A (ja) 2015-07-09
WO2013188724A1 (en) 2013-12-19
MA37748A1 (fr) 2016-11-30
HK1203935A1 (en) 2015-11-06
US20140148435A1 (en) 2014-05-29
MX2014014924A (es) 2015-03-09
CO7160011A2 (es) 2015-01-15
TN2014000510A1 (en) 2016-03-30
TW201412729A (zh) 2014-04-01
US8691986B2 (en) 2014-04-08
US9303028B2 (en) 2016-04-05
PE20150348A1 (es) 2015-03-04
PH12014502780A1 (en) 2015-02-02
UY34858A (es) 2013-11-29
CR20150012A (es) 2015-02-11
US20130338138A1 (en) 2013-12-19
AR091436A1 (es) 2015-02-04
MA37748B1 (fr) 2017-07-31
AP2014008136A0 (en) 2014-12-31
BR112014031368A2 (pt) 2017-06-27
US9493459B2 (en) 2016-11-15
CL2014003391A1 (es) 2015-07-10
AU2013274153B2 (en) 2016-05-19
SG11201408168UA (en) 2015-01-29
IL235901A0 (en) 2015-09-24
KR20150023417A (ko) 2015-03-05
CA2875802A1 (en) 2013-12-19
CN104619694A (zh) 2015-05-13
EP2864317A1 (en) 2015-04-29
US20160176874A1 (en) 2016-06-23

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