CN104039789B - 四氮杂-环戊二烯并[a]茚基及其作为正向变构调节剂的用途 - Google Patents

四氮杂-环戊二烯并[a]茚基及其作为正向变构调节剂的用途 Download PDF

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CN104039789B
CN104039789B CN201280062522.3A CN201280062522A CN104039789B CN 104039789 B CN104039789 B CN 104039789B CN 201280062522 A CN201280062522 A CN 201280062522A CN 104039789 B CN104039789 B CN 104039789B
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mmol
title compound
equiv
tetraaza
hplc
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CN104039789A (zh
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D·斯温南
C·蒙塔根
V·波梅尔
A·卡特勒帕尼
J·莫勒特
P·格比尔
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Merck Patent GmbH
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Priority claimed from EP11195214.9A external-priority patent/EP2607364A1/en
Priority claimed from EP12171415.8A external-priority patent/EP2674434A1/en
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/14Ortho-condensed systems
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • 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
    • A61P25/20Hypnotics; Sedatives
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201280062522.3A 2011-12-22 2012-11-30 四氮杂-环戊二烯并[a]茚基及其作为正向变构调节剂的用途 Active CN104039789B (zh)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201161578931P 2011-12-22 2011-12-22
EP11195214.9 2011-12-22
EP11195214.9A EP2607364A1 (en) 2011-12-22 2011-12-22 Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators
US61/578,931 2011-12-22
US201261657978P 2012-06-11 2012-06-11
EP12171415.8 2012-06-11
US61/657,978 2012-06-11
EP12171415.8A EP2674434A1 (en) 2012-06-11 2012-06-11 Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators
PCT/EP2012/004968 WO2013091773A1 (en) 2011-12-22 2012-11-30 Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators

Publications (2)

Publication Number Publication Date
CN104039789A CN104039789A (zh) 2014-09-10
CN104039789B true CN104039789B (zh) 2016-09-07

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Country Status (8)

Country Link
US (1) US9403835B2 (enExample)
EP (1) EP2794608B1 (enExample)
JP (1) JP6112316B2 (enExample)
CN (1) CN104039789B (enExample)
AU (1) AU2012357169B2 (enExample)
CA (1) CA2860008C (enExample)
ES (1) ES2606839T3 (enExample)
WO (1) WO2013091773A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2813505A1 (en) * 2013-06-14 2014-12-17 Asceneuron SA Tetraaza-cyclopenta[a]indenyl derivatives
GB201317363D0 (en) 2013-10-01 2013-11-13 Eisai Ltd Novel compounds
CN106573928B (zh) * 2014-08-26 2020-04-14 安斯泰来制药株式会社 2-氨基噻唑衍生物或其盐
CA2976092A1 (en) * 2015-02-11 2016-08-18 Sunovion Pharmaceuticals Inc. Fused dihydro-4h-pyrazolo[5,1-c][1,4]oxazinyl compounds and analogs for treating cns disorders
JP6116782B1 (ja) * 2015-08-28 2017-04-19 積水メディカル株式会社 ベンジル化合物
SG10202100751YA (en) 2016-07-29 2021-03-30 Sunovion Pharmaceuticals Inc Compounds and compositions and uses thereof
SG11202000669VA (en) 2017-08-02 2020-02-27 Sunovion Pharmaceuticals Inc Isochroman compounds and uses thereof
KR102835667B1 (ko) 2017-12-21 2025-07-21 애브비 바이오테크놀로지 리미티드 Parp14 억제제로서의 퀴나졸리논

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002076987A1 (en) * 2001-03-27 2002-10-03 Neurogen Corporation (oxo-pyrazolo[1,5a]pyrimidin-2-yl)alkyl-carboxamides
WO2008060488A1 (en) * 2006-11-14 2008-05-22 Merck & Co., Inc. Tricyclic heteroaromatic compounds as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
WO2011137049A1 (en) * 2010-04-30 2011-11-03 Merck Sharp & Dohme Corp. Heterocyclic quinolizine derived m1 receptor positive allosteric modulators

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2590316A1 (en) * 2004-12-15 2006-06-22 F. Hoffmann-La Roche Ag Bi- and tricyclic substituted phenyl methanones as glycine transporter i (glyt-1) inhibitors for the treatment of alzheimer's disease
EP2813505A1 (en) * 2013-06-14 2014-12-17 Asceneuron SA Tetraaza-cyclopenta[a]indenyl derivatives

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002076987A1 (en) * 2001-03-27 2002-10-03 Neurogen Corporation (oxo-pyrazolo[1,5a]pyrimidin-2-yl)alkyl-carboxamides
WO2008060488A1 (en) * 2006-11-14 2008-05-22 Merck & Co., Inc. Tricyclic heteroaromatic compounds as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
WO2011137049A1 (en) * 2010-04-30 2011-11-03 Merck Sharp & Dohme Corp. Heterocyclic quinolizine derived m1 receptor positive allosteric modulators

Also Published As

Publication number Publication date
EP2794608A1 (en) 2014-10-29
ES2606839T3 (es) 2017-03-28
US9403835B2 (en) 2016-08-02
WO2013091773A1 (en) 2013-06-27
CA2860008A1 (en) 2013-06-27
CA2860008C (en) 2020-11-10
AU2012357169A1 (en) 2014-08-07
JP2015502371A (ja) 2015-01-22
AU2012357169B2 (en) 2017-03-30
EP2794608B1 (en) 2016-09-14
US20150018343A1 (en) 2015-01-15
JP6112316B2 (ja) 2017-04-12
CN104039789A (zh) 2014-09-10

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