KR960037675A - 벤조니트릴 및 벤조플루오라이드 - Google Patents

벤조니트릴 및 벤조플루오라이드 Download PDF

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KR960037675A
KR960037675A KR1019960010119A KR19960010119A KR960037675A KR 960037675 A KR960037675 A KR 960037675A KR 1019960010119 A KR1019960010119 A KR 1019960010119A KR 19960010119 A KR19960010119 A KR 19960010119A KR 960037675 A KR960037675 A KR 960037675A
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piperazinyl
butyl
cyanoindole
general formula
cyanophenyl
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KR1019960010119A
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KR100437751B1 (ko
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뵈체르 헤닝
울리히 뷔링 카알
그라이너 하르트무트
바르토지크 게르트
지이프리트 크리스토프
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슈틀러, 하르트만
메르크 파텐트 게젤샤프트 미트 베쉬랭크터 하프퉁
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • 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
    • A61P9/12—Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Anesthesiology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

하기 일반식(Ⅰ)의 화합물 및 이들의 염들은 중추 신경계에 대해 작용을 나타낸다 :
상기 식에서, Q 및 Ar은 특허청구 범위 제1항에서 언급한 의미를 갖는다.

Description

벤조니트릴 및 벤조플루오라이드
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 하기 일반식(Ⅰ)의 화합물 및 이들의 산 부가염(3-〔4-플루오로페닐)-1-피페라지닐)부틸〕-5-시아노인돌 및 3-〔4-(4-(2-플루오로페닐)-1-피페라지닐)부틸〕-5-시아노인돌은 제외하나, 이들의 염은 제외하지 않는다) :
    상기 식에서, Ar은 CN 및/또는 F로 일치환 또는 이치환되는 페닐 라디칼이고, Q는 CnH2n이고, n은 3 또는 4이다.
  2. 제1항에 있어서, a) 3-〔4-(4-4-시아노페닐)-1-피페라지닐)부틸〕-5-시아노인돌 ; b) 3-〔3-(4-(4-(2-시아노페닐)-1-피페라지닐)프로필〕-5-시아노인돌 ; c) 3-〔4-(4-(2-시아노페닐)-1-피페라지닐)부틸〕-5-시아노인돌 ; d) 3-〔4-(4-(3-플루오로-4-시아노페닐)-1-피페라지닐)부틸〕-5-시아노인돌 및 언급한 화합물의 산 부가염.
  3. 제1항에 따른 3-〔4-(4-(4-플루오로페닐)-1-피페라지닐)부틸〕-5-시아노인돌, 하이드로클로라이드.
  4. 하기 일반식(Ⅱ)의 화합물을 하기 일반식(Ⅲ)의 화합물과 반응시키거나, 또는 하기 일반식(Ⅳ)의 화합물을 하기 일반식(Ⅴ)의 화합물과 반응시키거나, 또는 수득되는 일반식(Ⅰ)의 염기를 산 처리에 의해 그의 산부가염중 하나로 전환시킴을 특징으로 하는, 특허 청구 범위 제1항에 따른 일반식(Ⅰ)의 화합물 및 그의 산부가염의 제조 방법 :
    상기 식에서, X1은 X 또는 NH2이고, X는 Cl, Br, I, OH 또는 반응 작용기적으로 변형된 OH기이고, Q는 CnH2n이고, X2및 X3은 같거나 다를 수 있고, 만약 X1이 NH2인 경우, 각각 X이거나, 또는 달리는 함께 NH이고, Ar은 CN 및/또는 F로 일치환 또는 이치환되는 페닐 라디칼이다.
  5. 5-하이드록시트립타민 작동제 및 길항제로의 제1항에 따른 일반식(Ⅰ)의 약제 및 이들의 생리학적으로 허용되는 산 부가염.
  6. 제1항에 따른 일반식(Ⅰ)의 화합물 적어도 하나 및/또는 그의 생리학적으로 허용되는 산 부가염중 하나를 함유함을 특징으로 하는 약학 제제.
  7. 제6항에 있어서, a) 3-〔4-(4-(4-시아노페닐)-1-피페라지닐)부틸〕-5-시아노인돌; b) 3-〔3-(3-(4-시아노페닐)-1-피페라지닐)프로필〕-5-시아노인돌; c) 3-〔4-(4-(4-플루오로페닐)-1-피페라지닐)부틸〕-5-시아노인돌, 메탄설포네이트; d) 3-〔4-(4-(2-시아토페닐)-1피페라지닐)부틸〕-5-시아노인돌; e) 3-〔4-(4-(3-플루오로-4-시아노페닐)-1-피페라지닐)부틸〕-5-시아노인돌; f) 3-〔4-(4-(4-플루오로페닐)-1-피페라지닐)부틸〕-5-시아노인돌, 하이드로클로라이드 구성된 그룹중에서 선택된 적어도 하나의 화합물을 포함하는 약학 제제.
  8. 제1항에 따른 일반식(Ⅰ)의 화합물 및/또는 그의 생리학적으로 허용되는 산 부가염중 하나를 적어도 하나의 고체, 액체 또는 반고체 부형제 또는 보조제와 함께 적합한 투여 형태로 제공함을 특징으로 하는 약학 제제의 제조 방법.
  9. 약제를 제조하기 위한 제1항에 따른 일반식(Ⅰ)의 화합물 및/또는 그의 생리학적으로 허용되는 산 부가염의 용도.
  10. 병을 억제하기 위한 제1항에 따른 일반식(Ⅰ)의 화합물 및/또는 그의 생리학적으로 허용되는 염의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960010119A 1995-04-05 1996-04-04 벤조니트릴및벤조플루오라이드 KR100437751B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE19512639A DE19512639A1 (de) 1995-04-05 1995-04-05 Benzonitrile und -fluoride
DEP19512639.4 1995-04-05
DE19512639.4 1995-04-05

Publications (2)

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KR960037675A true KR960037675A (ko) 1996-11-19
KR100437751B1 KR100437751B1 (ko) 2004-08-25

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US (1) US6310068B1 (ko)
EP (1) EP0736525B1 (ko)
JP (1) JP3834098B2 (ko)
KR (1) KR100437751B1 (ko)
CN (1) CN1072209C (ko)
AR (1) AR002982A1 (ko)
AT (1) ATE194595T1 (ko)
AU (1) AU709708B2 (ko)
BR (1) BR9601275A (ko)
CA (1) CA2173418C (ko)
CO (1) CO4700469A1 (ko)
CY (1) CY2242B1 (ko)
CZ (1) CZ289449B6 (ko)
DE (2) DE19512639A1 (ko)
DK (1) DK0736525T3 (ko)
ES (1) ES2150039T3 (ko)
GR (1) GR3034514T3 (ko)
HU (1) HUP9600876A3 (ko)
NO (1) NO305903B1 (ko)
PL (1) PL183147B1 (ko)
PT (1) PT736525E (ko)
RU (1) RU2168508C2 (ko)
SI (1) SI0736525T1 (ko)
SK (1) SK281457B6 (ko)
TR (1) TR199600286A2 (ko)
TW (1) TW323279B (ko)
UA (1) UA45325C2 (ko)
ZA (1) ZA962768B (ko)

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AR004229A1 (es) * 1995-11-06 1998-11-04 Wyeth Corp Derivados indolalquilo de benzodioxanmetilamina y su uso para preparar medicamentos
US7189753B1 (en) 1997-11-06 2007-03-13 Cady Roger K Preemptive prophylaxis of migraine
DE60011570T2 (de) * 1999-01-07 2004-11-25 Wyeth Arylpiperazinyl-cyclohexyl indolderivate zur behandlung von depressionen
US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
ATE556713T1 (de) 1999-01-13 2012-05-15 Bayer Healthcare Llc Omega-carboxyarylsubstituierte-diphenyl- harnstoffe als p38-kinasehemmer
EP1140840B1 (en) * 1999-01-13 2006-03-22 Bayer Pharmaceuticals Corp. -g(v)-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
DE60131675T2 (de) * 2000-11-14 2008-11-20 Merck Patent Gmbh Neue verwendung von substanzen mit kombinierten 5-ht1a agonistischen und serotonin reuptake inhibitor-aktivitäten
UA76130C2 (en) * 2000-11-20 2006-07-17 Merck Patent Gmbh Use of compounds combining properties of selective inhibitors of serotonin re-uptake and agonists of 5-ht1a receptor for treatment of irritable bowel syndrome
AR035521A1 (es) * 2000-12-22 2004-06-02 Lundbeck & Co As H Derivados de 3-indolina y composicion farmaceutica que los comprende
US7371763B2 (en) * 2001-04-20 2008-05-13 Bayer Pharmaceuticals Corporation Inhibition of raf kinase using quinolyl, isoquinolyl or pyridyl ureas
WO2003047579A1 (en) * 2001-12-03 2003-06-12 Bayer Pharmaceuticals Corporation Aryl urea compounds in combination with other cytostatic or cytotoxic agents for treating human cancers
US20030207872A1 (en) * 2002-01-11 2003-11-06 Bayer Corporation Omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
AU2003209116A1 (en) 2002-02-11 2003-09-04 Bayer Pharmaceuticals Corporation Aryl ureas with angiogenesis inhibiting activity
WO2003068229A1 (en) 2002-02-11 2003-08-21 Bayer Pharmaceuticals Corporation Pyridine, quinoline, and isoquinoline n-oxides as kinase inhibitors
US7557129B2 (en) 2003-02-28 2009-07-07 Bayer Healthcare Llc Cyanopyridine derivatives useful in the treatment of cancer and other disorders
PT1636585E (pt) 2003-05-20 2008-03-27 Bayer Pharmaceuticals Corp Diarilureias com actividade inibidora de cinase
JP4777887B2 (ja) 2003-07-23 2011-09-21 バイエル、ファーマシューテイカルズ、コーポレイション 病気および状態の処置および防止のためのフロロ置換オメガカルボキシアリールジフェニル尿素
TWI367098B (en) * 2004-12-23 2012-07-01 Kowa Co Treating agent for glaucoma
CN102875538A (zh) * 2012-10-16 2013-01-16 北京诚创思达医药科技有限公司 维拉唑酮或其盐酸盐的制备方法
CN104337812B (zh) 2013-07-29 2018-09-14 广东东阳光药业有限公司 取代的杂芳基化合物及其使用方法和用途
US9714232B2 (en) 2013-12-20 2017-07-25 Sunshine Lake Pharma Co., Ltd. Substituted piperazine compounds and methods of use thereof
CN106243088B (zh) 2015-06-03 2019-01-04 广东东阳光药业有限公司 取代的哌嗪化合物及其使用方法和用途
JP7282082B2 (ja) 2017-09-29 2023-05-26 サンシャイン・レイク・ファーマ・カンパニー・リミテッド 置換ピリミジンピペラジン化合物及びその使用

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Also Published As

Publication number Publication date
KR100437751B1 (ko) 2004-08-25
EP0736525B1 (de) 2000-07-12
SK281457B6 (sk) 2001-03-12
ATE194595T1 (de) 2000-07-15
PT736525E (pt) 2000-12-29
HUP9600876A2 (hu) 1998-09-28
ES2150039T3 (es) 2000-11-16
NO961346L (no) 1996-10-07
TR199600286A2 (tr) 1997-03-21
CN1137036A (zh) 1996-12-04
HUP9600876A3 (en) 2000-04-28
JP3834098B2 (ja) 2006-10-18
UA45325C2 (uk) 2002-04-15
JPH09151174A (ja) 1997-06-10
DK0736525T3 (da) 2000-10-30
SI0736525T1 (en) 2001-02-28
SK40396A3 (en) 1996-11-06
AU709708B2 (en) 1999-09-02
AU5040896A (en) 1996-10-17
NO961346D0 (no) 1996-04-02
ZA962768B (en) 1996-11-13
PL313632A1 (en) 1996-10-14
DE59605568D1 (de) 2000-08-17
CO4700469A1 (es) 1998-12-29
CA2173418A1 (en) 1996-10-06
PL183147B1 (pl) 2002-05-31
TW323279B (ko) 1997-12-21
CA2173418C (en) 2007-06-12
BR9601275A (pt) 1998-01-13
EP0736525A1 (de) 1996-10-09
GR3034514T3 (en) 2000-12-29
DE19512639A1 (de) 1996-10-10
US6310068B1 (en) 2001-10-30
AR002982A1 (es) 1998-05-27
CN1072209C (zh) 2001-10-03
CZ96496A3 (en) 1996-10-16
NO305903B1 (no) 1999-08-16
RU2168508C2 (ru) 2001-06-10
CY2242B1 (en) 2003-07-04
CZ289449B6 (cs) 2002-01-16
HU9600876D0 (en) 1996-05-28

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