AU2012357169B2 - 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
AU2012357169B2
AU2012357169B2 AU2012357169A AU2012357169A AU2012357169B2 AU 2012357169 B2 AU2012357169 B2 AU 2012357169B2 AU 2012357169 A AU2012357169 A AU 2012357169A AU 2012357169 A AU2012357169 A AU 2012357169A AU 2012357169 B2 AU2012357169 B2 AU 2012357169B2
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Prior art keywords
mmol
title compound
tetraaza
hplc
uplc
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AU2012357169A1 (en
Inventor
Patrick Gerber
Jerome Molette
Cyril Montagne
Vincent Pomel
Anna Quattropani
Dominique Swinnen
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Merck Patent GmbH
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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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Publication of AU2012357169A1 publication Critical patent/AU2012357169A1/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)
  • 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)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2012357169A 2011-12-22 2012-11-30 Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators Active AU2012357169B2 (en)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201161578931P 2011-12-22 2011-12-22
US61/578,931 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
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
AU2012357169A1 AU2012357169A1 (en) 2014-08-07
AU2012357169B2 true AU2012357169B2 (en) 2017-03-30

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AU2012357169A Active AU2012357169B2 (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 (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
JP6569678B2 (ja) * 2014-08-26 2019-09-04 アステラス製薬株式会社 ２−アミノチアゾール誘導体またはその塩
US9758529B2 (en) * 2015-02-11 2017-09-12 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
BR112019001407A2 (pt) 2016-07-29 2019-07-09 Sunovion Pharmaceuticals Inc. compostos e composições e usos dos mesmos
MX2020000523A (es) 2017-08-02 2020-08-20 Sunovion Pharmaceuticals Inc Compuestos de isocromano y usos de los mismos.
PT3728207T (pt) 2017-12-21 2023-03-14 Ribon Therapeutics Inc Quinazolinonas como inibidores de parp14

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011137049A1 (en) * 2010-04-30 2011-11-03 Merck Sharp & Dohme Corp. Heterocyclic quinolizine derived m1 receptor positive allosteric modulators

Family Cites Families (4)

* 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
MX2007006896A (es) * 2004-12-15 2007-06-26 Hoffmann La Roche Fenil-metanonas bi- y triciclicas sustituidas como inhibidores del transportador 1 de glicina (glyt-1) para el tratamiento de la enfermedad de alzheimer.
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
EP2813505A1 (en) * 2013-06-14 2014-12-17 Asceneuron SA Tetraaza-cyclopenta[a]indenyl derivatives

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CA2860008A1 (en) 2013-06-27
EP2794608A1 (en) 2014-10-29
JP2015502371A (ja) 2015-01-22
ES2606839T3 (es) 2017-03-28
US20150018343A1 (en) 2015-01-15
EP2794608B1 (en) 2016-09-14
AU2012357169A1 (en) 2014-08-07
US9403835B2 (en) 2016-08-02
CN104039789B (zh) 2016-09-07
WO2013091773A1 (en) 2013-06-27
CA2860008C (en) 2020-11-10
CN104039789A (zh) 2014-09-10
JP6112316B2 (ja) 2017-04-12

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