GB1198349A - Benzdiaz[1,4]Epine Derivatives - Google Patents

Benzdiaz[1,4]Epine Derivatives

Info

Publication number
GB1198349A
GB1198349A GB3817068A GB3817068A GB1198349A GB 1198349 A GB1198349 A GB 1198349A GB 3817068 A GB3817068 A GB 3817068A GB 3817068 A GB3817068 A GB 3817068A GB 1198349 A GB1198349 A GB 1198349A
Authority
GB
United Kingdom
Prior art keywords
formula
compounds
oxime
compound
carboxylic acid
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
GB3817068A
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 GB1198349A publication Critical patent/GB1198349A/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

Landscapes

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

Abstract

1,198,349. Benzodiazepine derivatives. F. HOFFMANN-LA ROCHE & CO. A.G. 9 Aug., 1968 [9 Aug., 1967], No. 38170/68. Heading C2C. - Compounds of the general formula (R<SP>1</SP> = halogen, CF 3 , NO 2 , NH 2 ; R<SP>2</SP> = alkyl, alkenyl, cycloalkyl, cycloalkenyl, pyridyl, phenyl, halophenyl; R<SP>3</SP> = alkoxy, benzyloxy, phenoxy, NH 2 , dialkylamino, alkylthio; R<SP>4</SP> = alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, alkylaminoalkyl, dialkylaminoalkyl; broken line denotes optional substituent), acid addition salts of the basic compounds, alkali and alkaline earth metal, ammonium, alkylammonium, dialkylammonium and trialkylammonium salts of the corresponding 3- carboxylic acids, corresponding 4-desoxy compounds (which may carry an OH, alkanoyloxy, aroyloxy or aralkanoyloxy group in the 3- position) and the corresponding decarboxylated compounds are prepared by either cyclising a #-oxime of the formula (R<SP>5</SP> = leaving atom or group) in the presence of a basic or acidic agent and, if desired, subjecting the product to one or more of the steps: (a) alkylation, alkenylation or alkynylation in the case where the 1-position is unsubstituted; (b) nitration in the case where the 7-position is unsubstituted; (c) replacement of the NH 2 by halogen; (d) saponification of a 3-carboxylic acid ester or amide to yield a 3-carboxylic acid salt; (e) decarboxylation of a 3-carboxylic acid or salt; (f) deoxygenation of a 4-oxide; (g) conversion of a 4-oxide to a compound of the formula (R<SP>7</SP> = alkanoyl, aroyl, aralkanoyl); (h) hydrolysing the product of (g) to yield a compound of the formula and (i) acid addition salt formation or oxidizing the corresponding 4-desoxy compound. The #-oxime starting materials are prepared by reacting an oxime of the formula with a malonic acid derivative of the formula (R<SP>6</SP> = leaving atom or group). The benzodiazepine compounds are tranquillizers, muscle relaxants, anticonvulsants and sedatives and may be administered in the form of pharmaceutical preparations containing them, with or without other (unspecified) active ingredients, in association with a carrier.
GB3817068A 1967-08-09 1968-08-09 Benzdiaz[1,4]Epine Derivatives Expired GB1198349A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CH1059270A CH503750A (en) 1967-08-09 1967-08-09 Process for the preparation of benzodiazepine derivatives
CH1059070A CH506541A (en) 1967-08-09 1967-08-09 Process for the preparation of benzodiazepine derivatives
CH1129667A CH495366A (en) 1967-08-09 1967-08-09 Benzodiazepine derivs tranquillisers muscle relaxants

Publications (1)

Publication Number Publication Date
GB1198349A true GB1198349A (en) 1970-07-08

Family

ID=27176471

Family Applications (1)

Application Number Title Priority Date Filing Date
GB3817068A Expired GB1198349A (en) 1967-08-09 1968-08-09 Benzdiaz[1,4]Epine Derivatives

Country Status (6)

Country Link
BE (1) BE719208A (en)
CH (3) CH495366A (en)
DE (1) DE1770945A1 (en)
FR (2) FR1588550A (en)
GB (1) GB1198349A (en)
NL (1) NL6811366A (en)

Also Published As

Publication number Publication date
CH495366A (en) 1970-08-31
FR1588550A (en) 1970-04-17
DE1770945A1 (en) 1972-01-13
CH506541A (en) 1971-04-30
NL6811366A (en) 1969-02-11
BE719208A (en) 1969-02-10
CH503750A (en) 1971-02-28
FR7753M (en) 1970-03-16

Similar Documents

Publication Publication Date Title
GB1277132A (en) Pyridobenzo-diazepine derivatives
GB1413892A (en) 2-pyrimidinyl-thio-acetic acids and their derivatives
GB1142066A (en) New diphenyl-ureas and process for preparing them
GB1198349A (en) Benzdiaz[1,4]Epine Derivatives
GB1051221A (en)
IE32245B1 (en) Benzdiaz (1,4) epine derivatives
ES289813A1 (en) 5-phenyl-3h-1,4-benzodiazepine-2(ih)-thione and derivatives thereof
GB1239380A (en)
GB1256723A (en)
GB1362845A (en) Benzyl alcohol derivatives
GB1279438A (en) Cyclopropane-carboxylic acid derivatives and methods for its production
GB1505543A (en) Benzodiazepine derivatives and a process for the preparation thereof
GB1365176A (en) Benzodiazepine derivatives
GB1460325A (en) Pharmaceutical composition intended for relieving pain and producing analgesia
GB1332697A (en) Benzodiazepine derivatives
GB1222179A (en) A process for the preparation of sulfonyl urea derivatives
GB1171434A (en) Novel Barbituric Acid Derivatives and a Process for the Manufacture thereof
GB1283632A (en) Phenylethanolamine derivatives
GB1388513A (en) 5-aroyl-furans and pharmaceutical compositions containing them
IE32946L (en) Phenethylamine derivatives
GB1168801A (en) Quinoline Derivatives
GB1013229A (en) A process for the manufacture of benzodiazepine derivatives
GB1152894A (en) Guanidine Derivatives
GB1146110A (en) 5h-dibenzo[a,d]cycloheptene derivatives
GB1195096A (en) Tricyclic Ketones

Legal Events

Date Code Title Description
PS Patent sealed
PLNP Patent lapsed through nonpayment of renewal fees