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GB972969A - Benzodiazepine derivatives and a process for the manufacture of same - Google Patents

Benzodiazepine derivatives and a process for the manufacture of same

Info

Publication number
GB972969A
GB972969A GB1168/61A GB116861A GB972969A GB 972969 A GB972969 A GB 972969A GB 1168/61 A GB1168/61 A GB 1168/61A GB 116861 A GB116861 A GB 116861A GB 972969 A GB972969 A GB 972969A
Authority
GB
United Kingdom
Prior art keywords
acid
benzodiazepine derivatives
general formula
manufacture
same
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
GB1168/61A
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 GB972969A publication Critical patent/GB972969A/en
Expired legal-status Critical Current

Links

Classifications

    • 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
    • C07D243/161,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/181,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24Oxygen atoms
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/004Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reaction with organometalhalides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/42Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by hydrolysis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/04Saturated compounds containing keto groups bound to acyclic carbon atoms
    • C07C49/16Saturated compounds containing keto groups bound to acyclic carbon atoms containing halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/76Ketones containing a keto group bound to a six-membered aromatic ring
    • C07C49/80Ketones containing a keto group bound to a six-membered aromatic ring containing halogen
    • C07C49/813Ketones containing a keto group bound to a six-membered aromatic ring containing halogen polycyclic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/74Quinazolines; Hydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
    • 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
    • C07D243/161,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/181,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/20Nitrogen atoms
    • 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
    • C07D243/161,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/181,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24Oxygen atoms
    • C07D243/26Preparation from compounds already containing the benzodiazepine skeleton

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

The invention comprises benzodiazepine derivatives of the general formula <FORM:0972969/C1/1> (in which the broken line denotes that the alkyl substituent is optional) and acid-addition salts thereof, and a process for their preparation comprising reacting a halide of the general formula <FORM:0972969/C1/2> with ammonia or a primary alkylamine and, if desired, converting the benzodiazepine compound produced into an acid-addition salt. The benzodiazepine derivatives and their acid-addition salts (e.g. with inorganic acids) are sedatives, tranquilizers, muscle relaxants and anticonvulsants. They may be administered orally or parenterally (e.g. in the form of elixirs, suspensions, capsules, powders, tablets or injectables). Specification 972,970 is referred to.
GB1168/61A 1959-12-10 1961-01-11 Benzodiazepine derivatives and a process for the manufacture of same Expired GB972969A (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US85856459A 1959-12-10 1959-12-10
US260560A 1960-01-15 1960-01-15
US2468660A 1960-04-26 1960-04-26
US3873260A 1960-06-27 1960-06-27

Publications (1)

Publication Number Publication Date
GB972969A true GB972969A (en) 1964-10-21

Family

ID=27485190

Family Applications (13)

Application Number Title Priority Date Filing Date
GB42400/60A Expired GB972962A (en) 1959-12-10 1960-12-09 A process for the manufacture of benzodiazepine derivatives
GB42405/60A Expired GB972967A (en) 1959-12-10 1960-12-09 A process for the manufacture of benzodiazepine derivatives
GB42404/60A Expired GB972966A (en) 1959-12-10 1960-12-09 A process for the manufacture of benzodiazepine derivatives
GB20071/63A Expired GB972976A (en) 1959-12-10 1960-12-09 Novel trifluoromethyl-benzophenones and the preparation thereof
GB40979/62A Expired GB972973A (en) 1959-12-10 1960-12-09 Novel trifluoromethyl-benzophenones and the preparation thereof
GB40978/62A Expired GB972972A (en) 1959-12-10 1960-12-09 Novel 2-amino-benzophenones and the preparation thereof
GB42401/60A Expired GB972963A (en) 1959-12-10 1960-12-09 A process for the manufacture of benzodiazepine derivatives
GB42399/60A Expired GB972961A (en) 1959-12-10 1960-12-09 A process for the manufacture of benzodiazepine derivatives
GB42403/60A Expired GB972965A (en) 1959-12-10 1960-12-09 A process for the manufacture of benzodiazepine derivatives
GB42402/60A Expired GB972964A (en) 1959-12-10 1960-12-09 A process for the manufacture of benzodiazepine derivatives
GB42408/60A Expired GB972968A (en) 1959-12-10 1960-12-09 Benzodiazepine derivatives
GB29834/62A Expired GB972970A (en) 1959-12-10 1961-01-11 Novel quinazoline 3-oxides and a process for the manufacture thereof
GB1168/61A Expired GB972969A (en) 1959-12-10 1961-01-11 Benzodiazepine derivatives and a process for the manufacture of same

Family Applications Before (12)

Application Number Title Priority Date Filing Date
GB42400/60A Expired GB972962A (en) 1959-12-10 1960-12-09 A process for the manufacture of benzodiazepine derivatives
GB42405/60A Expired GB972967A (en) 1959-12-10 1960-12-09 A process for the manufacture of benzodiazepine derivatives
GB42404/60A Expired GB972966A (en) 1959-12-10 1960-12-09 A process for the manufacture of benzodiazepine derivatives
GB20071/63A Expired GB972976A (en) 1959-12-10 1960-12-09 Novel trifluoromethyl-benzophenones and the preparation thereof
GB40979/62A Expired GB972973A (en) 1959-12-10 1960-12-09 Novel trifluoromethyl-benzophenones and the preparation thereof
GB40978/62A Expired GB972972A (en) 1959-12-10 1960-12-09 Novel 2-amino-benzophenones and the preparation thereof
GB42401/60A Expired GB972963A (en) 1959-12-10 1960-12-09 A process for the manufacture of benzodiazepine derivatives
GB42399/60A Expired GB972961A (en) 1959-12-10 1960-12-09 A process for the manufacture of benzodiazepine derivatives
GB42403/60A Expired GB972965A (en) 1959-12-10 1960-12-09 A process for the manufacture of benzodiazepine derivatives
GB42402/60A Expired GB972964A (en) 1959-12-10 1960-12-09 A process for the manufacture of benzodiazepine derivatives
GB42408/60A Expired GB972968A (en) 1959-12-10 1960-12-09 Benzodiazepine derivatives
GB29834/62A Expired GB972970A (en) 1959-12-10 1961-01-11 Novel quinazoline 3-oxides and a process for the manufacture thereof

Country Status (11)

Country Link
BE (4) BE598008A (en)
BR (1) BR6024755D0 (en)
CH (9) CH418342A (en)
CY (1) CY324A (en)
DE (5) DE1288609B (en)
ES (2) ES263123A1 (en)
GB (13) GB972962A (en)
MY (1) MY6500178A (en)
NL (2) NL6412250A (en)
OA (7) OA00816A (en)
SE (2) SE310887B (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1300114B (en) * 1963-05-29 1969-07-31 American Home Prod Process for the preparation of 5-chloro-2- (2'-hydroxylamino-acetamido) -benzophenone
GB1333501A (en) * 1971-03-05 1973-10-10 Ravizza Spa Process for the preparation of 7-chlorobenzodiazepine de rivatives
US4820834A (en) * 1984-06-26 1989-04-11 Merck & Co., Inc. Benzodiazepine analogs
CA1332410C (en) * 1984-06-26 1994-10-11 Roger M. Freidinger Benzodiazepine analogs
EP1392663A2 (en) 2001-06-07 2004-03-03 Neuro3D Cyclic nucleotide phosphodiesterase inhibitors, preparation and uses thereof
CA2485681C (en) * 2002-05-24 2012-10-16 Millennium Pharmaceuticals, Inc. Ccr9 inhibitors and methods of use thereof

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2893992A (en) * 1959-07-07 I ii i i

Also Published As

Publication number Publication date
CH411910A (en) 1966-04-30
BE598015A (en) 1961-06-09
CH418341A (en) 1966-08-15
CH414653A (en) 1966-06-15
CH408029A (en) 1966-02-28
CH408045A (en) 1966-02-28
CY324A (en) 1965-11-03
OA00817A (en) 1967-11-15
GB972964A (en) 1964-10-21
CH396016A (en) 1965-07-31
DE1445073A1 (en) 1968-10-31
DE1445908A1 (en) 1969-04-17
DE1290143B (en) 1969-03-06
CH408940A (en) 1966-03-15
MY6500178A (en) 1965-12-31
BE598013A (en) 1961-06-09
DE1288609B (en) 1969-02-06
CH418342A (en) 1966-08-15
GB972962A (en) 1964-10-21
GB972963A (en) 1964-10-21
OA00958A (en) 1968-03-22
CH414652A (en) 1966-06-15
SE310887B (en) 1969-05-19
GB972967A (en) 1964-10-21
NL6412251A (en) 1966-01-25
GB972968A (en) 1964-10-21
GB972976A (en) 1964-10-21
GB972965A (en) 1964-10-21
NL6412250A (en) 1966-01-25
OA02385A (en) 1970-05-05
OA00953A (en) 1968-03-22
BR6024755D0 (en) 1973-05-24
OA00959A (en) 1968-03-22
BE598008A (en) 1961-06-09
SE318283B (en) 1969-12-08
ES263124A1 (en) 1961-06-01
GB972961A (en) 1964-10-21
OA02384A (en) 1970-05-05
GB972966A (en) 1964-10-21
BE598012A (en) 1961-06-09
DE1288610B (en) 1969-02-06
GB972972A (en) 1964-10-21
GB972973A (en) 1964-10-21
ES263123A1 (en) 1961-06-01
GB972970A (en) 1964-10-21
OA00816A (en) 1967-11-15

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