KR970069997A - 2,3-benzodiazepine derivative - Google Patents

2,3-benzodiazepine derivative Download PDF

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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
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group
hydrogen
general formula
compound
alkyl group
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KR1019970012301A
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이스트반 링
기젤라 아브라함
팔 베르제나이
이스트반 타르나와
산도르 솔리옴
페렝크 안드라시
타마스 하모리
에메세 슈즈디
카탈린 호르바쓰
멜린다 갈
임레 모라브쉭
마르타 죌로시
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야노스 톰페, 아틸라 만디
에기스 괴기스제르기아르 알티
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Priority claimed from HU9600871A external-priority patent/HU9600871D0/en
Application filed by 야노스 톰페, 아틸라 만디, 에기스 괴기스제르기아르 알티 filed Critical 야노스 톰페, 아틸라 만디
Publication of KR970069997A publication Critical patent/KR970069997A/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/02Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
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  • 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

2,3-벤조디아제핀 유도체2,3-benzodiazepine derivative

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음As this is a public information case, the full text was not included.

Claims (10)

하기 일반식을 갖는 화합물, 상기 화합물의 이성체, 및 상기 화합물 또는 상기 이성체의 산부가염.A compound having the following general formula, an isomer of the compound, and an acid addition salt of the compound or the isomer. (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 의미와 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 아니여야 한다)(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 a general formula of -NR 8 R 9 R 8 and R 9 each independently represent a hydrogen, a C 1-4 alkyl group or a group having a general formula of —COR 10 , and R 10 is hydrogen, a C 1-6 alkyl group which may be substituted, C 6-10 An aryl group, a C 1-4 alkoxy group, a C 3-5 cycloalkyl group, a C 2-6 alkenyl group, a 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 represents 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 -CO-R 13 Means a group having the general formula of wherein R 13 is as defined in relation to R 10 , R 4 and R 5 are each independently hydrogen or a C 1-3 alkyl group, R 6 and Each R 7 independently represents hydrogen, chlorine or bromine, but if one of R 6 and R 7 is hydrogen, the other must not be hydrogen) 3-아세틸-1-(4-아미노페닐)-8-클로로-4-메틸-4,5-디하이드로-3H-2,3-벤조디아제핀.3-acetyl-1- (4-aminophenyl) -8-chloro-4-methyl-4,5-dihydro-3H-2,3-benzodiazepine. 1-(4-아미노페닐)-8-클로로-4-메틸-3-메틸카바모일-4,5-디하이드로-3H-2,3-벤조디아제핀.1- (4-aminophenyl) -8-chloro-4-methyl-3-methylcarbamoyl-4,5-dihydro-3H-2,3-benzodiazepine. R1및 R7은 청구항 1항에서 정의한 바와 같은 화학식 (Ⅰ)의 화합물, 이의 이성체, 또는 상기 화합물 또는 상기 이성체의 약제학적으로 허용 가능한 산부가염을 약제학적 조성물의 제조에 사용되는 통상적인 담체, 용매, 희석제 및 부형제를 사용하여 활성 성분으로서 함유하는 약제학적 조성물.R 1 and R 7 are compounds of formula (I) as defined in claim 1, isomers thereof, or pharmaceutically acceptable acid addition salts of said compounds or said isomers for use in the preparation of pharmaceutical compositions, Pharmaceutical compositions containing as active ingredients using solvents, diluents and excipients. 제1항의 화합물을 사용한 약제.A drug using the compound of claim 1. 청구항 1항의 화합물을 사용하여 제조되는, 근육 경련에 수반되는 질병의 치료에 유용한 약제학적 조성물.A pharmaceutical composition useful for the treatment of diseases associated with muscle spasms, prepared using the compound of claim 1. 청구항 1항의 화합물을 사용하여 제조되는, 간질의 치료에 유용한 약제학적 조성물.A pharmaceutical composition useful for the treatment of epilepsy prepared using the compound of claim 1. 청구항 1항의 화합물을 사용하여 제조되는, 급성 또는 만성 신경 변성 질병의 치료에 유용한 약제학적 조성물.A pharmaceutical composition useful for the treatment of acute or chronic neurodegenerative diseases, prepared using the compound of claim 1. R1, R2, R3, R4, R5, R6및 R7은 청구항 1항에서 정의한 것과 동일한 의미를 가지며, R1, R2, R4, R5, R6및 R7이 상기와 같은 의미를 갖는 화학식(Ⅱ)의 화합물의 3번 위치에 R3기를 도입하는 단계, 및 화학식(Ⅰ)의 화합물을 화학식(Ⅰ)의 다른 화합물로 변환하는 단계, 및 화학식(Ⅰ)의 화합물을 이의 산부가염으로 변환하거나 산부가염으로부터 화학식(Ⅰ)의 화합물을 분리하는 단계를 포함하는, 화학식(Ⅰ)의 화합물, 이의 이성체 및 이의 산부가염의 제조 방법.R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 have the same meanings as defined in claim 1, wherein R 1 , R 2 , R 4 , R 5 , R 6 and R 7 are Introducing a R 3 group at position 3 of the compound of formula (II) having the same meaning as described above, converting the compound of formula (I) to another compound of formula (I), and A process for preparing a compound of formula (I), isomers thereof and acid addition salts thereof, comprising converting the compound to an acid addition salt thereof or separating the compound of formula (I) from the acid addition salt. 하기 일반식을 갖는 화합물.Compounds having the following general formula. (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 수소를 나타내며, 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 아니여야 한다)(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 a general formula of -NR 8 R 9 R 8 and R 9 each independently represent a hydrogen, a C 1-4 alkyl group or a group having a general formula of —COR 10 , and R 10 is hydrogen, a C 1-6 alkyl group which may be substituted, C 6-10 An aryl group, a C 1-4 alkoxy group, a C 3-5 cycloalkyl group, a C 2-6 alkenyl group, a 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 represents hydrogen, a C 1-4 alkyl group, a C 3-5 cycloalkyl group, or a C 6-10 aryl group, R 3 represents hydrogen, and R 4 and R 5 each independently represents hydrogen or C 1- 3 means an alkyl group, and R 6 and R 7 each independently represent hydrogen, chlorine or bromine, and if one of R 6 and R 7 is hydrogen, the other is not hydrogen do) ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019970012301A 1996-04-04 1997-04-03 2,3-benzodiazepine derivative KR970069997A (en)

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

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KR970069997A true KR970069997A (en) 1997-11-07

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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)
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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

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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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