GB1040548A - Benzodiazepine derivatives and the manufacture thereof - Google Patents

Benzodiazepine derivatives and the manufacture thereof

Info

Publication number
GB1040548A
GB1040548A GB4791164A GB4791164A GB1040548A GB 1040548 A GB1040548 A GB 1040548A GB 4791164 A GB4791164 A GB 4791164A GB 4791164 A GB4791164 A GB 4791164A GB 1040548 A GB1040548 A GB 1040548A
Authority
GB
United Kingdom
Prior art keywords
group
atom
nitrogen atom
formula
present
Prior art date
Legal status (The legal status 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 status listed.)
Expired
Application number
GB4791164A
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
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 F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of GB1040548A publication Critical patent/GB1040548A/en
Expired legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic 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
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24—Oxygen atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic 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
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24—Oxygen atoms
    • C07D243/26—Preparation from compounds already containing the benzodiazepine skeleton

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Compounds of the general formula <FORM:1040548/C2/1> (wherein R stands for an N,N-disubstituted aminoalkyl group of the formula (X)(Y)N-alkylene-, in which the alkylene group contains 2-7 carbon atoms and may be either a straight chain or branched chain group and X and Y are alkyl groups which may be joined directly or through an oxygen or nitrogen atom (which latter atom may bear as a substituent an alkyl, hydroxyalkyl or alkoxyalkyl group or, except where a single bond is present in the 4,5-position of the diazepine ring, an alkenyloxyalkyl group) to form with the nitrogen atom to which they are attached a 5-membered or 6-membered heterocyclic group, R1 stands for a halogen atom, R2 stands for a halogen atom or a trifluoromethyl group or, except where a single bond is present in the 4,5-position, a nitro group, and the broken lines denote optional bonds) and their acid addition salts are prepared by converting a compound of the formula <FORM:1040548/C2/2> into a 1-alkali metal derivative and treating the latter with a halide of the formula <FORM:1040548/C2/3> (wherein the alkylene group contains 2-7 carbon atoms and may be either a straight chain or branched chain group, and X1 and Y1 are alkyl groups which may be joined directly or through an oxygen or nitrogen atom (which latter atom may bear as a substituent an alkyl, hydroxyalkyl, alkoxyalkyl or alkenyloxyalkyl group) to form with the nitrogen atom to which they are attached a 5-membered or 6-membered heterocyclic group), optionally followed by hydrogenation in the presence of a noble metal catalyst of any product in which no nitro group is present in the benz ring and/or acid addition salt formation. Alternatively, the starting material may be replaced by its 4-oxide, the oxygen atom in the 4-position being removed by hydrogenation in the presence of a nickel catalyst (except where a nitro group is present in the benz ring) or by phosphorus halide treatment after the halide treatment. The compounds of the invention are anti-convulsants, analgesics, sedatives and muscle relaxants and may be administered enterally or parenterally in the form of pharmaceutical preparations containing them, with or without other (unspecified) active ingredients, in association with a carrier. Salts specified include salicylates and ascorbates.
GB4791164A 1962-03-02 1963-03-01 Benzodiazepine derivatives and the manufacture thereof Expired GB1040548A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US17690162A 1962-03-02 1962-03-02

Publications (1)

Publication Number Publication Date
GB1040548A true GB1040548A (en) 1966-09-01

Family

ID=22646360

Family Applications (2)

Application Number Title Priority Date Filing Date
GB4791164A Expired GB1040548A (en) 1962-03-02 1963-03-01 Benzodiazepine derivatives and the manufacture thereof
GB823863A Expired GB1040547A (en) 1962-03-02 1963-03-01 Benzodiazepine derivatives and their manufacture

Family Applications After (1)

Application Number Title Priority Date Filing Date
GB823863A Expired GB1040547A (en) 1962-03-02 1963-03-01 Benzodiazepine derivatives and their manufacture

Country Status (8)

Country Link
BE (1) BE629005A (en)
BR (1) BR6347108D0 (en)
CH (3) CH455815A (en)
CY (1) CY418A (en)
DE (1) DE1445874A1 (en)
GB (2) GB1040548A (en)
MY (1) MY6800032A (en)
SE (1) SE302127B (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5218114A (en) * 1991-04-10 1993-06-08 Merck & Co., Inc. Cholecystokinin antagonists
DE19503320A1 (en) * 1995-02-02 1996-08-08 Boehringer Mannheim Gmbh New benzodiazepine conjugates

Also Published As

Publication number Publication date
DE1445874A1 (en) 1970-07-23
MY6800032A (en) 1968-12-31
CH454887A (en) 1968-04-30
SE302127B (en) 1968-07-08
CY418A (en) 1967-11-30
GB1040547A (en) 1966-09-01
CH438336A (en) 1967-06-30
CH455815A (en) 1968-05-15
BE629005A (en) 1963-08-28
BR6347108D0 (en) 1973-07-19

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