GB1040548A - Benzodiazepine derivatives and the manufacture thereof - Google Patents
Benzodiazepine derivatives and the manufacture thereofInfo
- 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
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.
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) | CH438336A (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)
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 |
-
1963
- 1963-02-20 BR BR14710863A patent/BR6347108D0/en unknown
- 1963-02-22 CH CH231263A patent/CH438336A/en unknown
- 1963-02-22 CH CH5067A patent/CH455815A/en unknown
- 1963-02-22 CH CH1370566A patent/CH454887A/en unknown
- 1963-02-25 DE DE19631445874 patent/DE1445874A1/de active Pending
- 1963-02-28 BE BE629005A patent/BE629005A/en unknown
- 1963-03-01 SE SE225463A patent/SE302127B/xx unknown
- 1963-03-01 GB GB4791164A patent/GB1040548A/en not_active Expired
- 1963-03-01 GB GB823863A patent/GB1040547A/en not_active Expired
-
1967
- 1967-11-30 CY CY41867A patent/CY418A/en unknown
-
1968
- 1968-12-31 MY MY6800032A patent/MY6800032A/en unknown
Also Published As
Publication number | Publication date |
---|---|
CY418A (en) | 1967-11-30 |
CH455815A (en) | 1968-05-15 |
MY6800032A (en) | 1968-12-31 |
BE629005A (en) | 1963-08-28 |
GB1040547A (en) | 1966-09-01 |
SE302127B (en) | 1968-07-08 |
CH438336A (en) | 1967-06-30 |
CH454887A (en) | 1968-04-30 |
BR6347108D0 (en) | 1973-07-19 |
DE1445874A1 (en) | 1970-07-23 |
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