KR970069997A - 2,3-benzodiazepine derivative - Google Patents
2,3-benzodiazepine derivative Download PDFInfo
- Publication number
- KR970069997A KR970069997A KR1019970012301A KR19970012301A KR970069997A KR 970069997 A KR970069997 A KR 970069997A KR 1019970012301 A KR1019970012301 A KR 1019970012301A KR 19970012301 A KR19970012301 A KR 19970012301A KR 970069997 A KR970069997 A KR 970069997A
- Authority
- KR
- South Korea
- Prior art keywords
- group
- hydrogen
- general formula
- compound
- alkyl group
- Prior art date
Links
- RPBDCDQMCRHNLM-UHFFFAOYSA-N C1=NNC=C2C=CC=CC2=C1 Chemical class C1=NNC=C2C=CC=CC2=C1 RPBDCDQMCRHNLM-UHFFFAOYSA-N 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 25
- 239000001257 hydrogen Substances 0.000 claims abstract 25
- 150000001875 compounds Chemical class 0.000 claims abstract 19
- 150000002431 hydrogen Chemical class 0.000 claims abstract 19
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims abstract 11
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 claims abstract 8
- 239000002253 acid Substances 0.000 claims abstract 7
- 150000003839 salts Chemical class 0.000 claims abstract 7
- 125000003545 alkoxy group Chemical group 0.000 claims abstract 6
- 125000003118 aryl group Chemical group 0.000 claims abstract 6
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims abstract 3
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims abstract 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims abstract 3
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims abstract 3
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims abstract 3
- 229910052794 bromium Inorganic materials 0.000 claims abstract 3
- 229910052801 chlorine Inorganic materials 0.000 claims abstract 3
- 239000000460 chlorine Substances 0.000 claims abstract 3
- 125000000000 cycloalkoxy group Chemical group 0.000 claims abstract 3
- 229910052736 halogen Inorganic materials 0.000 claims abstract 3
- 150000002367 halogens Chemical class 0.000 claims abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims abstract 2
- XBLLOPDJGYDQEU-UHFFFAOYSA-N 1-(4-aminophenyl)-8-chloro-n,4-dimethyl-4,5-dihydro-2,3-benzodiazepine-3-carboxamide Chemical compound C12=CC(Cl)=CC=C2CC(C)N(C(=O)NC)N=C1C1=CC=C(N)C=C1 XBLLOPDJGYDQEU-UHFFFAOYSA-N 0.000 claims 1
- JNKMFWULKBWFBY-UHFFFAOYSA-N 1-[1-(4-aminophenyl)-8-chloro-4-methyl-4,5-dihydro-2,3-benzodiazepin-3-yl]ethanone Chemical compound N=1N(C(C)=O)C(C)CC2=CC=C(Cl)C=C2C=1C1=CC=C(N)C=C1 JNKMFWULKBWFBY-UHFFFAOYSA-N 0.000 claims 1
- 208000007101 Muscle Cramp Diseases 0.000 claims 1
- 208000005392 Spasm Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- MGRVRXRGTBOSHW-UHFFFAOYSA-N (aminomethyl)phosphonic acid Chemical compound NCP(O)(O)=O MGRVRXRGTBOSHW-UHFFFAOYSA-N 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 230000036963 noncompetitive effect Effects 0.000 abstract 1
- 239000007858 starting material Substances 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
화학식(Ⅰ)를 갖는 비경쟁 AMPA 길항적 화합물, 이의 이성체 및 상기 화합물 또는 이성체의 산부가염이 개시된다. 이에 더하여 상기 화합물, 이성체 및 산부가염 중 어느 하나를 포함하는 약제학적 조성물이 개시된다. 상기 일반식에서 R1및 R2는 각각 독립적으로 수소, 할로겐, C1-4알킬기, C1-4알콕시기, 니트로기, 트리플루오로메틸기 또는 -NR8R9의 일반식을 갖는 기를 의미하며, R8및 R9는 각각 독립적으로 수소, C1-4알킬기 또는 -COR10의 일반식을 갖는 기를 의미하며, R10은 수소, 치환될 수 있는 C1-6알킬기, C6-10아릴기, C1-4알콕시기, C3-5사이클로알킬기, C2-6알케닐기, C3-5사이클로알콕시기 또는 -NR11R12의 일반식을 갖는 기를 의미하며, R11및 R12는 각각 독립적으로 수소, C1-4알킬기, C3-5사이클로알킬기 또는 C6-10아릴기를 의미하며, R3은 C1-4알킬기, C3-5사이클로알킬기 또는 -CO-R13의 일반식을 갖는 기를 의미하며, 여기서 R13은 R10과 관련하여 정의된 것과 동일하며, R4및 R5는 각각 독립적으로 수소 또는 C1-3알킬기를 의미하며, R6및 R7은 각각 독립적으로 수소, 염소 또는 브롬을 의미하되, R6및 R7중 하나가 수소이면 다른 하나는 수소가 아니어야 한다.Non-competitive AMPA antagonist compounds of formula (I), isomers thereof and acid addition salts of such compounds or isomers are disclosed. In addition, pharmaceutical compositions comprising any of the compounds, isomers and acid addition salts are disclosed. In the general formula, R 1 and R 2 are each independently hydrogen, halogen, C 1-4 alkyl group, C 1-4 alkoxy group, nitro group, trifluoromethyl group or group having the general formula of -NR 8 R 9 , R 8 and R 9 are each independently hydrogen, a C 1-4 alkyl group or a group having the general formula of —COR 10 , R 10 is hydrogen, a C 1-6 alkyl group which may be substituted, C 6-10 aryl Group, C 1-4 alkoxy group, C 3-5 cycloalkyl group, C 2-6 alkenyl group, C 3-5 cycloalkoxy group or a group having the general formula of —NR 11 R 12 , wherein R 11 and R 12 Each independently represent hydrogen, a C 1-4 alkyl group, a C 3-5 cycloalkyl group, or a C 6-10 aryl group, and R 3 represents a C 1-4 alkyl group, a C 3-5 cycloalkyl group, or a —CO—R 13 group. A group having the general formula wherein R 13 is the same as defined in relation to R 10, and R 4 and R 5 each independently represent hydrogen or a C 1-3 alkyl group, and R 6 and R 7 Are each independently hydrogen, chlorine or bromine, but if one of R 6 and R 7 is hydrogen, the other must not be hydrogen.
본 발명에서 또한 화학식(Ⅱ)의 출발 물질을 개시하는데, 이때, R1, R2, R4, R5, R6및 R7은 화학식(Ⅰ)과 관련하여 정의된 의미와 동일하다.The present invention also discloses starting materials of formula (II), wherein R 1 , R 2 , R 4 , R 5 , R 6 and R 7 have the same meanings as defined with respect to formula (I).
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음As this is a public information case, the full text was not included.
Claims (10)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
HUP9600871 | 1996-04-04 | ||
HU9600871A HU9600871D0 (en) | 1996-04-04 | 1996-04-04 | New 2,3-benzodiazepine derivatives |
Publications (1)
Publication Number | Publication Date |
---|---|
KR970069997A true KR970069997A (en) | 1997-11-07 |
Family
ID=89993864
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019970012301A KR970069997A (en) | 1996-04-04 | 1997-04-03 | 2,3-benzodiazepine derivative |
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 |
IT1290453B1 (en) | 1998-12-03 |
AU720745B2 (en) | 2000-06-08 |
ZA972746B (en) | 1998-10-09 |
AU1773497A (en) | 1997-10-09 |
UA45358C2 (en) | 2002-04-15 |
ITMI970776A1 (en) | 1998-10-04 |
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A201 | Request for examination | ||
E902 | Notification of reason for refusal | ||
E902 | Notification of reason for refusal | ||
E601 | Decision to refuse application |