IT1290453B1 - New mono- or di-substituted 2,3-benzodiazepine derivatives - are non-competitive AMPA antagonists, useful as muscle relaxants, anti-epileptics and neuroprotectors - Google Patents
New mono- or di-substituted 2,3-benzodiazepine derivatives - are non-competitive AMPA antagonists, useful as muscle relaxants, anti-epileptics and neuroprotectorsInfo
- Publication number
- IT1290453B1 IT1290453B1 ITMI970776A IT1290453B1 IT 1290453 B1 IT1290453 B1 IT 1290453B1 IT MI970776 A ITMI970776 A IT MI970776A IT 1290453 B1 IT1290453 B1 IT 1290453B1
- Authority
- IT
- Italy
- Prior art keywords
- alkyl
- substituted
- neuroprotectors
- epileptics
- useful
- Prior art date
Links
- MGRVRXRGTBOSHW-UHFFFAOYSA-N (aminomethyl)phosphonic acid Chemical compound NCP(O)(O)=O MGRVRXRGTBOSHW-UHFFFAOYSA-N 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 230000003556 anti-epileptic effect Effects 0.000 title 1
- 239000001961 anticonvulsive agent Substances 0.000 title 1
- 229960003965 antiepileptics Drugs 0.000 title 1
- 229940053197 benzodiazepine derivative antiepileptics Drugs 0.000 title 1
- -1 di-substituted 2,3-benzodiazepine Chemical class 0.000 title 1
- 229940035363 muscle relaxants Drugs 0.000 title 1
- 239000003158 myorelaxant agent Substances 0.000 title 1
- 230000001067 neuroprotector Effects 0.000 title 1
- 230000036963 noncompetitive effect Effects 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- PIEXCQIOSMOEOU-UHFFFAOYSA-N 1-bromo-3-chloro-5,5-dimethylimidazolidine-2,4-dione Chemical group CC1(C)N(Br)C(=O)N(Cl)C1=O PIEXCQIOSMOEOU-UHFFFAOYSA-N 0.000 abstract 1
- RPBDCDQMCRHNLM-UHFFFAOYSA-N C1=NNC=C2C=CC=CC2=C1 Chemical class C1=NNC=C2C=CC=CC2=C1 RPBDCDQMCRHNLM-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 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
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/02—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 2
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Neurology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Mono- or di-halo substituted 2,3-benzodiazepine derivatives of formula (I), their isomers and acid addition salts are new. R1, R2 = H, halogen, 1-4C alkyl, 1-4C alkoxy, nitro, CF3 or NR8R9; R3 = 1-4C alkyl, 3-5C cycloalkyl or COR13; R4, R5 = H or 1-3C alkyl; R6, R7 = H, Cl or Br, provided that not both are H at the same time; R8, R9 = H, 1-4C alkyl or COR10; R10, R13 = H, optionally substituted 1-6C alkyl, 6-10C aryl, 1-4C alkoxy, 3-5C cycloalkyl, 2-6C alkenyl, 3-5C cycloalkoxy or NR11R12; and R11, R12 = H, 1-4C alkyl, 3-5C cycloalkyl or 6-10C aryl.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| HU9600871A HU9600871D0 (en) | 1996-04-04 | 1996-04-04 | New 2,3-benzodiazepine derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| ITMI970776A1 ITMI970776A1 (en) | 1998-10-04 |
| IT1290453B1 true IT1290453B1 (en) | 1998-12-03 |
Family
ID=89993864
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IT000776 IT1290453B1 (en) | 1996-04-04 | 1997-04-04 | New mono- or di-substituted 2,3-benzodiazepine derivatives - are non-competitive AMPA antagonists, useful as muscle relaxants, anti-epileptics and neuroprotectors |
Country Status (11)
| Country | Link |
|---|---|
| KR (1) | KR970069997A (en) |
| AT (1) | ATE254608T1 (en) |
| AU (1) | AU720745B2 (en) |
| BE (1) | BE1010962A4 (en) |
| DE (1) | DE59711013D1 (en) |
| ES (1) | ES2127699B1 (en) |
| IT (1) | IT1290453B1 (en) |
| NZ (1) | NZ314517A (en) |
| UA (1) | UA45358C2 (en) |
| YU (1) | YU13197A (en) |
| ZA (1) | ZA972746B (en) |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HU179018B (en) * | 1978-10-19 | 1982-08-28 | Gyogyszerkutato Intezet | Process for producing new 5h-2,3-benzodiazepine derivatives |
| HU186760B (en) * | 1981-03-12 | 1985-09-30 | Gyogyszerkutato Intezet | Process for preparing 3,4-dihydro-5h-2,3-aenzodiazepine derivatives |
| HU219778B (en) * | 1990-12-21 | 2001-07-30 | Gyógyszerkutató Intézet Közös Vállalat | Process for producing n-acyl-2,3-benzodiazepine derivatives, their acid additional salts and pharmaceutical compositions containing them and a grop of the compounds and pharmaceutical compositions containing them |
| HU208429B (en) * | 1991-05-03 | 1993-10-28 | Gyogyszerkutato Intezet | Process for producing 1-/3-chloro-phenyl/-4-methyl-7,8-dimethoxy-5h-2,3-benzodiazepine of high purity |
| WO1996006606A1 (en) * | 1994-08-31 | 1996-03-07 | Eli Lilly And Company | Dihydro-2,3-benzodiazepine derivatives |
-
1997
- 1997-04-01 ZA ZA972746A patent/ZA972746B/en unknown
- 1997-04-03 BE BE9700308A patent/BE1010962A4/en not_active IP Right Cessation
- 1997-04-03 KR KR1019970012301A patent/KR970069997A/en not_active Application Discontinuation
- 1997-04-03 UA UA97041584A patent/UA45358C2/en unknown
- 1997-04-03 YU YU13197A patent/YU13197A/en unknown
- 1997-04-03 NZ NZ314517A patent/NZ314517A/en unknown
- 1997-04-04 AU AU17734/97A patent/AU720745B2/en not_active Ceased
- 1997-04-04 DE DE59711013T patent/DE59711013D1/en not_active Expired - Fee Related
- 1997-04-04 IT IT000776 patent/IT1290453B1/en active IP Right Grant
- 1997-04-04 AT AT97105591T patent/ATE254608T1/en not_active IP Right Cessation
- 1997-04-04 ES ES009700703A patent/ES2127699B1/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| BE1010962A4 (en) | 1999-03-02 |
| DE59711013D1 (en) | 2003-12-24 |
| NZ314517A (en) | 2000-03-27 |
| ES2127699B1 (en) | 2000-01-16 |
| ATE254608T1 (en) | 2003-12-15 |
| YU13197A (en) | 1999-09-27 |
| ES2127699A1 (en) | 1999-04-16 |
| AU720745B2 (en) | 2000-06-08 |
| KR970069997A (en) | 1997-11-07 |
| ZA972746B (en) | 1998-10-09 |
| AU1773497A (en) | 1997-10-09 |
| UA45358C2 (en) | 2002-04-15 |
| ITMI970776A1 (en) | 1998-10-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 0001 | Granted |