GB1445765A - Phenoxy-substituted malonic acid derivatives their prepration and pharmaceutical compositions containing them - Google Patents
Phenoxy-substituted malonic acid derivatives their prepration and pharmaceutical compositions containing themInfo
- Publication number
- GB1445765A GB1445765A GB4331873A GB4331873A GB1445765A GB 1445765 A GB1445765 A GB 1445765A GB 4331873 A GB4331873 A GB 4331873A GB 4331873 A GB4331873 A GB 4331873A GB 1445765 A GB1445765 A GB 1445765A
- Authority
- GB
- United Kingdom
- Prior art keywords
- sulphur
- oxygen
- compound
- hydrogen
- pharmaceutical compositions
- 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
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- -1 Phenoxy-substituted malonic acid Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 6
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 5
- 239000005864 Sulphur Chemical group 0.000 abstract 5
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 5
- 229910052760 oxygen Inorganic materials 0.000 abstract 5
- 239000001301 oxygen Substances 0.000 abstract 5
- 239000002253 acid Substances 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 150000002431 hydrogen Chemical class 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000004423 acyloxy group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 230000001430 anti-depressive effect Effects 0.000 abstract 1
- 239000000935 antidepressant agent Substances 0.000 abstract 1
- 229940005513 antidepressants Drugs 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003230 pyrimidines Chemical class 0.000 abstract 1
- 125000001453 quaternary ammonium group Chemical group 0.000 abstract 1
- 150000003242 quaternary ammonium salts Chemical class 0.000 abstract 1
- PXQLVRUNWNTZOS-UHFFFAOYSA-N sulfanyl Chemical class [SH] PXQLVRUNWNTZOS-UHFFFAOYSA-N 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- 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
- A61K31/551—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic 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
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- 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
- A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/26—Psychostimulants, e.g. nicotine, cocaine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Anesthesiology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
1445765 Tetracyclic pyrimidines AKZO NV 14 Sept 1973 [23 Sept 1972] 43318/73 Heading C2C Novel compounds of the Formula I wherein X is oxygen, sulphur, r and s are integers from 1 to 4; R 1 and R 2 are hydrogen, halogen, hydroxy, C 1-6 alkyl or alkoxy, trifluoromethyl, or a C 1-8 acyloxy derived from a hydrocarbon-carboxylic acid; R 3 is hydrogen, C 1-6 alkyl, C 7-10 aralkyl or aryl and R 4 , R 5 and R 6 are hydrogen or a C 1-6 alkyl group, and pharmaceutically acceptable acid addition and quaternary ammonium salts thereof may be prepared by cyclizing a compound of the Formula II or an acid addition salt thereof in which Q is H 2 or oxygen with a compound Y : CZ 1 Z 2 wherein Y is H 2 , sulphur or oxygen, Z 1 and Z 2 are halogen, a substituted or unsubstituted amino, a free, etherified or esterified hydroxy or mercapto or Z 1 and Z 2 together are sulphur if Y is sulphur, after which, if Y is oxygen or sulphur and/or Q is oxygen, the resulting compound is reduced to a compound I and optionally converted into a quaternary ammonium or acid addition salt. Pharmaceutical compositions of the compounds I with the usual excipients show antidepressant and auxiolytic properties when administered orally or parenterally.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| NLAANVRAGE7212915,A NL176458C (en) | 1972-09-23 | 1972-09-23 | PROCESS FOR PREPARING A PHARMACEUTICAL PREPARATION AND PROCESS FOR PREPARING ACTIVE SUBSTANCES SUITABLE. |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| GB1445765A true GB1445765A (en) | 1976-08-11 |
Family
ID=19816997
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GB4331873A Expired GB1445765A (en) | 1972-09-23 | 1973-09-14 | Phenoxy-substituted malonic acid derivatives their prepration and pharmaceutical compositions containing them |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US3892695A (en) |
| JP (1) | JPS5912678B2 (en) |
| AR (1) | AR203090A1 (en) |
| AU (1) | AU472312B2 (en) |
| BE (1) | BE805178A (en) |
| CA (1) | CA1019733A (en) |
| CH (1) | CH592094A5 (en) |
| DE (1) | DE2347727C2 (en) |
| DK (1) | DK140668B (en) |
| ES (1) | ES418996A1 (en) |
| FI (1) | FI54311C (en) |
| FR (1) | FR2199996B1 (en) |
| GB (1) | GB1445765A (en) |
| HU (1) | HU167206B (en) |
| IE (1) | IE38221B1 (en) |
| NL (1) | NL176458C (en) |
| SE (1) | SE407686B (en) |
| ZA (1) | ZA737131B (en) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4217452A (en) * | 1974-02-09 | 1980-08-12 | Akzona Incorporated | Synthesis for the preparation of tetracyclic compounds |
| NL179906C (en) * | 1974-02-09 | 1986-12-01 | Akzo Nv | PROCESS FOR PREPARING 1,2,3,4,10,14B-HEXAHYDRODIBENZO (C, F) PYRAZINO (1,2-A) AZEPINE DERIVATIVES. |
| NL7414038A (en) * | 1974-10-28 | 1976-05-03 | Akzo Nv | NEW TETRACYCLIC PYRROLIDINO DERIVATIVES. |
| GB1472382A (en) * | 1975-01-16 | 1977-05-04 | Wyeth John & Brother Ltd | Dibenzopyrimidoazepines |
| NL7610942A (en) * | 1976-10-02 | 1978-04-04 | Akzo Nv | PROCESS FOR PREPARING 1,4-DIAZEPINE DERIVATIVES. |
| NL7809726A (en) * | 1978-09-26 | 1980-03-28 | Akzo Nv | NEW TETRACYCLIC CONNECTIONS. |
| HU195491B (en) * | 1985-12-20 | 1988-05-30 | Egyt Gyogyszervegyeszeti Gyar | Process for production of optically active 2-chlor-12-/3-/dimethil-amin/-2-methil-prophil/-12h-dibenzol /d,g/ /1,3,6/-diaxazocine and medical compositions containing such compounds |
| CH678623A5 (en) * | 1989-05-17 | 1991-10-15 | Sochinaz Societe Chimique De V | Prepn. of di:benzo pyrazino azepine(s) |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL154511B (en) * | 1967-07-07 | 1977-09-15 | Organon Nv | PROCESS FOR PREPARING PIPERAZINE DERIVATIVES, PROCESS FOR PREPARING A PHARMACEUTICAL PREPARATION CONTAINING SUCH A COMPOUND AND MOLDS PREPARED ACCORDING TO THIS PROCEDURE. |
| US3470181A (en) * | 1967-10-23 | 1969-09-30 | American Home Prod | Fused 2-pyrimidinepropionic acid compounds,related compounds,and the process for their preparation |
-
1972
- 1972-09-23 NL NLAANVRAGE7212915,A patent/NL176458C/en not_active IP Right Cessation
-
1973
- 1973-09-06 ZA ZA737131*A patent/ZA737131B/en unknown
- 1973-09-06 IE IE1587/73A patent/IE38221B1/en unknown
- 1973-09-07 US US396251A patent/US3892695A/en not_active Expired - Lifetime
- 1973-09-11 AU AU60197/73A patent/AU472312B2/en not_active Expired
- 1973-09-14 GB GB4331873A patent/GB1445765A/en not_active Expired
- 1973-09-17 DK DK507673AA patent/DK140668B/en not_active IP Right Cessation
- 1973-09-18 CA CA181,312A patent/CA1019733A/en not_active Expired
- 1973-09-20 AR AR250175A patent/AR203090A1/en active
- 1973-09-20 FR FR7333768A patent/FR2199996B1/fr not_active Expired
- 1973-09-21 SE SE7312873A patent/SE407686B/en unknown
- 1973-09-21 FI FI2963/73A patent/FI54311C/en active
- 1973-09-21 HU HUAO373A patent/HU167206B/hu unknown
- 1973-09-21 JP JP48106809A patent/JPS5912678B2/en not_active Expired
- 1973-09-21 BE BE135926A patent/BE805178A/en not_active IP Right Cessation
- 1973-09-21 CH CH1358173A patent/CH592094A5/xx not_active IP Right Cessation
- 1973-09-21 DE DE2347727A patent/DE2347727C2/en not_active Expired
- 1973-09-22 ES ES418996A patent/ES418996A1/en not_active Expired
Also Published As
| Publication number | Publication date |
|---|---|
| BE805178A (en) | 1974-03-21 |
| CH592094A5 (en) | 1977-10-14 |
| IE38221B1 (en) | 1978-01-18 |
| NL7212915A (en) | 1974-03-26 |
| DE2347727A1 (en) | 1974-04-04 |
| DE2347727C2 (en) | 1986-12-11 |
| ZA737131B (en) | 1974-08-28 |
| NL176458B (en) | 1984-11-16 |
| FR2199996A1 (en) | 1974-04-19 |
| FI54311C (en) | 1978-11-10 |
| FR2199996B1 (en) | 1977-09-09 |
| JPS4985098A (en) | 1974-08-15 |
| AR203090A1 (en) | 1975-08-14 |
| AU472312B2 (en) | 1976-05-20 |
| HU167206B (en) | 1975-09-27 |
| NL176458C (en) | 1985-04-16 |
| SE407686B (en) | 1979-04-09 |
| JPS5912678B2 (en) | 1984-03-24 |
| DK140668C (en) | 1980-03-24 |
| US3892695A (en) | 1975-07-01 |
| DK140668B (en) | 1979-10-22 |
| ES418996A1 (en) | 1976-07-01 |
| AU6019773A (en) | 1975-03-13 |
| FI54311B (en) | 1978-07-31 |
| IE38221L (en) | 1974-03-23 |
| CA1019733A (en) | 1977-10-25 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PS | Patent sealed [section 19, patents act 1949] | ||
| PCNP | Patent ceased through non-payment of renewal fee |