ZA201603304B - Synthesis of trans-8-chloro-5-methyl-1 -[4-(pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4h-2,3,5,10b-tetraaza-benzo[e]azulene and crystalline forms thereof - Google Patents

Synthesis of trans-8-chloro-5-methyl-1 -[4-(pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4h-2,3,5,10b-tetraaza-benzo[e]azulene and crystalline forms thereof

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Publication number
ZA201603304B
ZA201603304B ZA2016/03304A ZA201603304A ZA201603304B ZA 201603304 B ZA201603304 B ZA 201603304B ZA 2016/03304 A ZA2016/03304 A ZA 2016/03304A ZA 201603304 A ZA201603304 A ZA 201603304A ZA 201603304 B ZA201603304 B ZA 201603304B
Authority
ZA
South Africa
Prior art keywords
tetraaza
azulene
yloxy
pyridin
benzo
Prior art date
Application number
ZA2016/03304A
Other languages
English (en)
Inventor
Benno Rothenhaeusler
RENé TRUSSARDI
Fabienne Hoffmann-Emery
Urs Schwitter
Jean-Michel Adam
Olaf Grassmann
Thomas Hartung
Frederic Ran
Ralph Diodone
Christophe Pfleger
Bjoern Bartels
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of ZA201603304B publication Critical patent/ZA201603304B/en

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Classifications

    • 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
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-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
    • A61K31/55Heterocyclic 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
    • A61K31/55171,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
ZA2016/03304A 2013-12-05 2016-05-16 Synthesis of trans-8-chloro-5-methyl-1 -[4-(pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4h-2,3,5,10b-tetraaza-benzo[e]azulene and crystalline forms thereof ZA201603304B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP13195864 2013-12-05
PCT/EP2014/076041 WO2015082370A1 (en) 2013-12-05 2014-12-01 Synthesis of trans-8-chloro-5-methyl-1 -[4-(pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4h-2,3,5,10b-tetraaza-benzo[e]azulene and crytalline forms thereof

Publications (1)

Publication Number Publication Date
ZA201603304B true ZA201603304B (en) 2022-05-25

Family

ID=49726573

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA2016/03304A ZA201603304B (en) 2013-12-05 2016-05-16 Synthesis of trans-8-chloro-5-methyl-1 -[4-(pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4h-2,3,5,10b-tetraaza-benzo[e]azulene and crystalline forms thereof

Country Status (19)

Country Link
US (3) US10246460B2 (enExample)
EP (1) EP3077396B1 (enExample)
JP (1) JP6454707B2 (enExample)
KR (3) KR102384629B1 (enExample)
CN (1) CN105793263B (enExample)
AR (1) AR098592A1 (enExample)
AU (2) AU2014359409A1 (enExample)
CA (2) CA2931016C (enExample)
ES (1) ES2875411T3 (enExample)
HR (1) HRP20210966T1 (enExample)
IL (2) IL245450A0 (enExample)
MX (1) MX372971B (enExample)
MY (1) MY175464A (enExample)
NZ (1) NZ720340A (enExample)
PL (1) PL3077396T3 (enExample)
SG (1) SG11201604502SA (enExample)
SI (1) SI3077396T1 (enExample)
WO (1) WO2015082370A1 (enExample)
ZA (1) ZA201603304B (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102384629B1 (ko) * 2013-12-05 2022-04-11 에프. 호프만-라 로슈 아게 트랜스-8-클로로-5-메틸-1-[4-(피리딘-2-일옥시)-사이클로헥실]-5,6-다이하이드로-4H-2,3,5,10b-테트라아자-벤조[e]아줄렌 및 그의 결정 형태의 합성
WO2017191117A1 (en) 2016-05-03 2017-11-09 Bayer Pharma Aktiengesellschaft V1a receptor antagonists for use in the treatment of renal diseases
IL275144B2 (en) * 2017-12-08 2024-12-01 Hoffmann La Roche Pharmaceutical formulation
WO2020139670A1 (en) 2018-12-27 2020-07-02 Teva Pharmaceuticals International Gmbh Solid state forms of balovaptan
CN116830362A (zh) 2021-10-06 2023-09-29 株式会社 Lg新能源 电池模块

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1197242A (en) * 1983-03-02 1985-11-26 Jean A. Gauthier Pyrimido¬1,2-a|pyrrolo¬2,1-c|¬1, 4|benzodiazepine-3-carboxylic acid derivatives
GB0303852D0 (en) 2003-02-19 2003-03-26 Pfizer Ltd Triazole compounds useful in therapy
AP2005003376A0 (en) * 2003-02-19 2005-09-30 Pfizer Triazole compounds useful in therapy.
GB0400700D0 (en) 2004-01-13 2004-02-18 Pfizer Ltd Compounds useful in therapy
WO2006021882A1 (en) 2004-08-25 2006-03-02 Pfizer Limited Triazolobenzodiazepines and their use as vasopressin antagonists
US7601715B2 (en) 2005-06-22 2009-10-13 Bristol-Myers Squibb Company Process for preparing triazole substituted azaindoleoxoacetic piperazine derivatives and novel salt forms produced therein
CA2739900C (en) * 2008-11-18 2016-11-08 F. Hoffmann-La Roche Ag Alkylcyclohexylethers of dihydrotetraazabenzoazulenes
NZ592076A (en) * 2008-11-28 2012-06-29 Hoffmann La Roche Arylcyclohexylethers of dihydrotetraazabenzoazulenes for use as vasopressin via receptor antagonists
US8492376B2 (en) 2010-04-21 2013-07-23 Hoffmann-La Roche Inc. Heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes
PL3035939T3 (pl) 2013-08-19 2020-07-27 F. Hoffmann-La Roche Ag Antagoniści V1a do leczenia zaburzeń snu z przesunięciem faz snu
KR102384629B1 (ko) 2013-12-05 2022-04-11 에프. 호프만-라 로슈 아게 트랜스-8-클로로-5-메틸-1-[4-(피리딘-2-일옥시)-사이클로헥실]-5,6-다이하이드로-4H-2,3,5,10b-테트라아자-벤조[e]아줄렌 및 그의 결정 형태의 합성

Also Published As

Publication number Publication date
JP2016539168A (ja) 2016-12-15
MX372971B (es) 2020-03-27
PL3077396T3 (pl) 2021-10-04
NZ720340A (en) 2020-03-27
RU2018135601A (ru) 2018-11-22
CA3142754C (en) 2024-01-02
KR102384629B1 (ko) 2022-04-11
SI3077396T1 (sl) 2021-08-31
US10246460B2 (en) 2019-04-02
US20190194210A1 (en) 2019-06-27
AU2014359409A1 (en) 2016-05-19
EP3077396A1 (en) 2016-10-12
CN105793263A (zh) 2016-07-20
US20160280712A1 (en) 2016-09-29
CA2931016C (en) 2022-11-01
KR20210134985A (ko) 2021-11-11
HRP20210966T1 (hr) 2021-09-17
SG11201604502SA (en) 2016-07-28
KR20160093709A (ko) 2016-08-08
KR102384630B1 (ko) 2022-04-11
CA3142754A1 (en) 2015-06-11
MX2016006558A (es) 2016-08-03
KR20210132745A (ko) 2021-11-04
US11040977B2 (en) 2021-06-22
US20210284648A1 (en) 2021-09-16
IL245450A0 (en) 2016-06-30
NZ759478A (en) 2021-06-25
KR102384608B1 (ko) 2022-04-08
RU2018135601A3 (enExample) 2022-05-05
US12459947B2 (en) 2025-11-04
HK1223918A1 (zh) 2017-08-11
CN105793263B (zh) 2019-08-23
CA2931016A1 (en) 2015-06-11
EP3077396B1 (en) 2021-04-21
WO2015082370A1 (en) 2015-06-11
AU2019201183A1 (en) 2019-03-14
IL264891B (en) 2021-02-28
AR098592A1 (es) 2016-06-01
MY175464A (en) 2020-06-29
AU2019201183B2 (en) 2021-03-04
ES2875411T3 (es) 2021-11-10
JP6454707B2 (ja) 2019-01-16

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