CA2860008C - Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators - Google Patents

Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators Download PDF

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Publication number
CA2860008C
CA2860008C CA2860008A CA2860008A CA2860008C CA 2860008 C CA2860008 C CA 2860008C CA 2860008 A CA2860008 A CA 2860008A CA 2860008 A CA2860008 A CA 2860008A CA 2860008 C CA2860008 C CA 2860008C
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Canada
Prior art keywords
mmol
title compound
tetraaza
hplc
uplc
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CA2860008A
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English (en)
French (fr)
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CA2860008A1 (en
Inventor
Dominique Swinnen
Cyril Montagne
Vincent Pomel
Anna Quattropani
Jerome Molette
Patrick Gerber
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Merck Patent GmbH
Original Assignee
Merck Patent GmbH
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Filing date
Publication date
Priority claimed from EP11195214.9A external-priority patent/EP2607364A1/en
Priority claimed from EP12171415.8A external-priority patent/EP2674434A1/en
Application filed by Merck Patent GmbH filed Critical Merck Patent GmbH
Publication of CA2860008A1 publication Critical patent/CA2860008A1/en
Application granted granted Critical
Publication of CA2860008C publication Critical patent/CA2860008C/en
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    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/14—Ortho-condensed systems
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CA2860008A 2011-12-22 2012-11-30 Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators Active CA2860008C (en)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201161578931P 2011-12-22 2011-12-22
EP11195214.9A EP2607364A1 (en) 2011-12-22 2011-12-22 Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators
EP11195214.9 2011-12-22
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
CA2860008A1 CA2860008A1 (en) 2013-06-27
CA2860008C true CA2860008C (en) 2020-11-10

Family

ID=48667735

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2860008A Active CA2860008C (en) 2011-12-22 2012-11-30 Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators

Country Status (8)

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

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
BR112017003901A2 (pt) * 2014-08-26 2017-12-12 Astellas Pharma Inc derivado de 2-aminotiazola ou sal do mesmo
CN111171047B (zh) * 2015-02-11 2023-06-23 赛诺维信制药公司 用于治疗cns障碍的稠合二氢-4h-吡唑并[5,1-c][1,4]噁嗪基化合物
KR102630720B1 (ko) 2015-08-28 2024-01-29 세키스이 메디칼 가부시키가이샤 벤질 화합물
CA3032141A1 (en) 2016-07-29 2018-02-01 Vadim ALEXANDROV Compounds and compositions and uses thereof
BR112020001433A2 (pt) 2017-08-02 2020-07-28 Sunovion Pharmaceuticals Inc. compostos de isocromano e usos dos mesmos
LT3728207T (lt) 2017-12-21 2023-05-25 Ribon Therapeutics Inc. Chinazolinonai kaip parp14 inhibitoriai

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1392692B1 (en) * 2001-03-27 2006-11-15 Neurogen Corporation (oxo-pyrazolo¬1,5a|pyrimidin-2-yl)alkyl-carboxamides
WO2006063709A1 (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
CA2668662A1 (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
US8507494B2 (en) * 2010-04-30 2013-08-13 Merck Sharp & Dohme Corp. Heterocyclic quinolizine derived M1 receptor positive allosteric modulators
EP2813505A1 (en) * 2013-06-14 2014-12-17 Asceneuron SA Tetraaza-cyclopenta[a]indenyl derivatives

Also Published As

Publication number Publication date
JP2015502371A (ja) 2015-01-22
CA2860008A1 (en) 2013-06-27
US9403835B2 (en) 2016-08-02
JP6112316B2 (ja) 2017-04-12
EP2794608B1 (en) 2016-09-14
AU2012357169A1 (en) 2014-08-07
CN104039789A (zh) 2014-09-10
US20150018343A1 (en) 2015-01-15
AU2012357169B2 (en) 2017-03-30
ES2606839T3 (es) 2017-03-28
CN104039789B (zh) 2016-09-07
EP2794608A1 (en) 2014-10-29
WO2013091773A1 (en) 2013-06-27

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