IT1269178B - DERIVATIVES OF PIPERAZIN- AND PIPERIDINISOSSAZOLO - Google Patents
DERIVATIVES OF PIPERAZIN- AND PIPERIDINISOSSAZOLOInfo
- Publication number
- IT1269178B IT1269178B ITMI940025A ITMI940025A IT1269178B IT 1269178 B IT1269178 B IT 1269178B IT MI940025 A ITMI940025 A IT MI940025A IT MI940025 A ITMI940025 A IT MI940025A IT 1269178 B IT1269178 B IT 1269178B
- Authority
- IT
- Italy
- Prior art keywords
- carbon
- atoms
- benzyloxyl
- halogen
- carbon atoms
- Prior art date
Links
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 6
- 229910052799 carbon Inorganic materials 0.000 abstract 6
- 125000004432 carbon atom Chemical group C* 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- -1 benzyloxyl Chemical group 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 125000004429 atom Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 150000002367 halogens Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 2
- 101150047265 COR2 gene Proteins 0.000 abstract 1
- 101100467189 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) QCR2 gene Proteins 0.000 abstract 1
- 125000004450 alkenylene group Chemical group 0.000 abstract 1
- 150000001413 amino acids Chemical class 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 208000015114 central nervous system disease Diseases 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 206010015037 epilepsy Diseases 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D261/12—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
Sono descritti composti di formula (I) (FORMULA I) in cui R è OH, COR2, PO(R2)2, alcossile da 1 a 4 atomi di carbonio o alogeno;R1 è idrogeno, alogeno, trifluorometile, alchile da 1 a 4 atomi di carbonio, cicloalchile da 3 a 7 atomi di carbonio. Alcossile da 1 a 4 atomi di carbonio, benzilossile, benzilossile in cui il residuo fenilico è sostituito mediante alogeno o mediante alchile da 1 a 4 atomi di carbonio, fenile o fenile sostituito mediante alogeno;R2 è OH, alcossile da 1 a 4 atomi di carbonio, benzilossile, benzilossile sostituito, ammino o ammino sostituito mediante uno o due gruppi alchilici da 1 a 4 atomi di carbonio;A è alchile da 1 a 4 atomi di carbonio e Y è azoto o carbonio, A è alchenilene da 2 a 4 atomi di carbonio o (CH2)t -CH= in cui t è 0, 1, 2 o 3 e Y è carbonio, oppure A è(CH2)p -CO- o -CO-(CH2)q in cui p e q, indipendentemente uno dall'altro, sono 0, 1 o 2 e Y è azoto; e rappresenta un legame singolo o doppio; o un loro sale farmaceuticamente accettabile. E' anche descritto un processo per la loro preparazione. I composti di formula I sono antagonisti degli amminoacidi eccitanti e sono utili nel trattamento di stati patologici, come l'epilessia e altri disordini del CNS.Compounds of formula (I) (FORMULA I) are described wherein R is OH, COR2, PO (R2) 2, alkoxyl from 1 to 4 carbon or halogen atoms; R1 is hydrogen, halogen, trifluoromethyl, alkyl from 1 to 4 carbon atoms, cycloalkyl from 3 to 7 carbon atoms. Alkoxyl from 1 to 4 carbon atoms, benzyloxyl, benzyloxyl in which the phenyl residue is replaced by halogen or by alkyl from 1 to 4 carbon, phenyl or phenyl substituted by halogen; R2 is OH, alkoxyl from 1 to 4 atoms of carbon, benzyloxyl, substituted benzyloxyl, amino or amino substituted by one or two alkyl groups of 1 to 4 carbon atoms; A is alkyl from 1 to 4 carbon atoms and Y is nitrogen or carbon, A is alkenylene from 2 to 4 atoms of carbon or (CH2) t -CH = where t is 0, 1, 2 or 3 and Y is carbon, or A is (CH2) p -CO- or -CO- (CH2) q where peq, independently one on the other, they are 0, 1 or 2 and Y is nitrogen; and represents a single or double bond; or a pharmaceutically acceptable salt thereof. A process for their preparation is also described. The compounds of formula I are antagonists of exciting amino acids and are useful in the treatment of pathological states, such as epilepsy and other CNS disorders.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB9300950A GB2274282B (en) | 1993-01-19 | 1993-01-19 | Piperazine-and piperidine-isoxazole derivatives |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| ITMI940025A0 ITMI940025A0 (en) | 1994-01-12 |
| ITMI940025A1 ITMI940025A1 (en) | 1995-07-12 |
| IT1269178B true IT1269178B (en) | 1997-03-21 |
Family
ID=10728919
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ITMI940025A IT1269178B (en) | 1993-01-19 | 1994-01-12 | DERIVATIVES OF PIPERAZIN- AND PIPERIDINISOSSAZOLO |
Country Status (4)
| Country | Link |
|---|---|
| JP (1) | JPH06247965A (en) |
| DE (1) | DE4401159A1 (en) |
| GB (1) | GB2274282B (en) |
| IT (1) | IT1269178B (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100616099B1 (en) * | 2004-09-20 | 2006-08-28 | 한국과학기술연구원 | Novel piperazinylalkylisoxazole derivatives effective as T-type calcium channel antagonists |
| US20100022590A1 (en) * | 2008-01-17 | 2010-01-28 | Biovitrum Ab (Publ.) | Novel compounds |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3515093A1 (en) * | 1985-04-26 | 1986-10-30 | Hoechst Ag, 6230 Frankfurt | 4-AMINOALKYLIDE-SUBSTITUTED 3-ARYL-5 (4H) -ISOXAZOLONE, METHOD FOR THE PRODUCTION THEREOF, MEDICINAL PRODUCTS CONTAINING THESE COMPOUNDS AND THEIR USE |
-
1993
- 1993-01-19 GB GB9300950A patent/GB2274282B/en not_active Expired - Fee Related
-
1994
- 1994-01-12 IT ITMI940025A patent/IT1269178B/en active IP Right Grant
- 1994-01-17 DE DE4401159A patent/DE4401159A1/en not_active Withdrawn
- 1994-01-18 JP JP6003580A patent/JPH06247965A/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| GB2274282A (en) | 1994-07-20 |
| DE4401159A1 (en) | 1994-07-21 |
| ITMI940025A0 (en) | 1994-01-12 |
| JPH06247965A (en) | 1994-09-06 |
| GB9300950D0 (en) | 1993-03-10 |
| ITMI940025A1 (en) | 1995-07-12 |
| GB2274282B (en) | 1996-08-14 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 0001 | Granted | ||
| TA | Fee payment date (situation as of event date), data collected since 19931001 |
Effective date: 19971231 |