KR960007568A - 트리사이클릭 피라졸 유도체 - Google Patents
트리사이클릭 피라졸 유도체 Download PDFInfo
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- KR960007568A KR960007568A KR1019950024636A KR19950024636A KR960007568A KR 960007568 A KR960007568 A KR 960007568A KR 1019950024636 A KR1019950024636 A KR 1019950024636A KR 19950024636 A KR19950024636 A KR 19950024636A KR 960007568 A KR960007568 A KR 960007568A
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- A61P25/26—Psychostimulants, e.g. nicotine, cocaine
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- 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
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- A—HUMAN NECESSITIES
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Abstract
본 발명은 일반식(I)로 트리사이클릭 피라졸 유도체 및 또한 약제학적으로 허용되는 이의 염에 관한 것이다.
상기식에서, R1내지 R4는 각각 수소, 하이드록시, 할로겐, 저급 알킬, 저급알콕시 또는 페닐이고, R5는 수소 또는 저급알킬이고, R6은 수소, 저급알킬 또는 저급 알콕시이고, X는 -(CR7R8)n-또는 -CH=CH-이고, R7및 R8은 수소 또는 저급 알킬이며, n은 1 또는 2이다.
이들 화합물 및 염은 특히 우울증, 이극성 질환, 불안상태, 수면 및 성적 장애, 정신병, 정신분열증, 편두통 및 두통 또는 상이한 종류의 통증과 관련이 기타의 상태, 개인적인 질환 또는 비만성 강박 질환, 사회 공포증 또는 공황 상태, 정신적 기관 장애, 아동 정신 질환, 공격증, 노인성 기억 질환 및 행동 질환, 중독, 비만, 병적 기아 등과 같은 중추신경 질환, 종양, 발작, 신경 퇴화성 질환 등에 의한 신경계의 손상, 고혈압, 혈전증, 발작 등과 같은 심혈관 질환 및 위장관 운동성 기능 부전과 같은 위장 질환을 치료 또는 예방하기 위한 약제학적으로 활성인 물질로서 사용하기에 적합하다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (14)
- 일반식(I)의 화합물 및 약제학적으로 허용되는 이들의 염.상기식에서, R1내지 R4는 각각 수소, 하이드록시, 할로겐, 저급 알킬, 저급알콕시 또는 페닐이고, R5는 수소 또는 저급알킬이고, R6은 수소, 저급알킬 또는 저급 알콕시이고, X는 -(CR7R8)n-또는 -CH=CH-이고, R7및 R8은 수소 또는 저급 알킬이며, n은 1 또는 2이다.
- 제1항에 있어서, R5가 메틸인 화합물.
- 제1항 또는 제2항에 있어사, R2가 메틸 또는 메톡시이고 X가 -CH2- 또는 -C(CH3)2-이며 R1, R3, R4및 R6이 수소인 화합물.
- (RS)-2-(7-메톡시-1,4-디하이드로-인데노[2,1-c]피라졸-1-일)-1-메틸-에틸아민 푸마레이트(1:1).
- (S)-2-(7-메톡시-1,4-디하이드로-인데노[2,1-c]피라졸-1-일)-1-메틸-에틸아민 푸마레이트(1:1).
- (S)-2-(4,4,7-트리메틸-1,4-디하이드로-인데노[2,1-c]피라졸-1-일)-1-메틸-에틸아민 푸마레이트(1:1).
- (S)-2-(7-메톡시-4,4-디메틸-1,4-디하이드로-인데노[2,1-c]피라졸-1-일)-1-메틸-에틸아민 푸마레이트(1:1).
- (RS)-2-(7-메톡시-4,4-디메틸-1,4-디하이드로-인덴올[2,1-c]피라졸-1-일)-1-메틸-에틸아민 푸마레이트(1:1).
- (RS)-2-(7-에톡시-1,4-디하이드로-인데노[2,1-c]피라졸-1-일)-1-메틸-에틸아민 푸마레이트(1:1).
- (RS)-2-(7-메톡시-1,4-디하이드로-인데노[2,1-c]피라졸-1-일)-1-메틸-에틸아민 푸마레이트(1:1).
- (RS)-2-(8-메톡시-1-벤즈[g]인다졸-1-일)-메틸-에틸아민 푸마레이트(1:0.5).
- 일반식(Ⅱ)의 화합물.상기식에서, R1 내지 R6 및 X는 제1항에 정의한 바와 같고, R9는 아지도 그룹, 하이드록시 그룹 또는 보호된 아미노 그룹이다.
- 우울증, 이극성 질환, 불안상태, 수면 및 성적 장애, 정신병, 정신분열증, 편두통 및 두통 또는 상이한 종류의 통증과 관련이 기타의 상태, 개인적인 질환 또는 비만성 강박 질환, 사회 공포증 또는 공황 상태, 정신적 기관 장애, 아동 정신 질환, 공격증, 노인성 기억 질환 및 행동 질환, 중독, 비만, 병적 기아 등과 같은 중추신경 질환, 종양, 발작, 신경 퇴화성 질환 등에 의한 신경계의 손상, 고혈압, 혈전증, 발작 등과 같은 심혈관 질환 및 위장관 운동성 기능 부전과 같은 위장 질환을 치료 또는 예방하기 위한, 제1항 내지 제11항 중의 어느 한 항에 따르는 화합물과 약제학적으로 불활성인 담체 물질을 포함하는 약제학적 조성물.
- 일반식(Ⅱa)의 화합물을 일반식(I)의 상응하는 아미노 화합물로 전환시킴을 포함하는, 제1항 내지 제11항 중의 어느 한 항에 따르는 화합물 및 약제학적으로 허용되는 이들의 염의 제조방법.상기식에서, R1내지 R6및 X는 제1항에서 정의한 바와 같고, R91은 아미노 그룹으로 전환될 수 있는 그룹이다.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CH02490/94-0 | 1994-08-12 | ||
CH249094 | 1994-08-12 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR960007568A true KR960007568A (ko) | 1996-03-22 |
KR100385384B1 KR100385384B1 (ko) | 2003-09-19 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019950024636A KR100385384B1 (ko) | 1994-08-12 | 1995-08-10 | 트리사이클릭피라졸유도체,이의제조방법및이를포함하는약제학적조성물 |
Country Status (31)
Country | Link |
---|---|
US (1) | US5561150A (ko) |
EP (1) | EP0700905B1 (ko) |
JP (1) | JP2755560B2 (ko) |
KR (1) | KR100385384B1 (ko) |
CN (1) | CN1056607C (ko) |
AT (1) | ATE207905T1 (ko) |
AU (1) | AU691310B2 (ko) |
BR (1) | BR9503630A (ko) |
CA (1) | CA2153937C (ko) |
CO (1) | CO4410331A1 (ko) |
CZ (1) | CZ289027B6 (ko) |
DE (1) | DE59509777D1 (ko) |
DK (1) | DK0700905T3 (ko) |
ES (1) | ES2164730T3 (ko) |
FI (1) | FI113264B (ko) |
HK (1) | HK1012342A1 (ko) |
HU (1) | HUT72066A (ko) |
IL (1) | IL114849A (ko) |
MA (1) | MA23643A1 (ko) |
MY (1) | MY133619A (ko) |
NO (1) | NO305026B1 (ko) |
NZ (1) | NZ272731A (ko) |
PE (1) | PE34096A1 (ko) |
PH (1) | PH31424A (ko) |
PL (1) | PL182480B1 (ko) |
PT (1) | PT700905E (ko) |
RU (1) | RU2152388C1 (ko) |
TR (1) | TR199500977A2 (ko) |
TW (1) | TW403738B (ko) |
UY (1) | UY24016A1 (ko) |
ZA (1) | ZA956553B (ko) |
Families Citing this family (34)
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AU727654B2 (en) * | 1997-06-13 | 2000-12-21 | Yamanouchi Pharmaceutical Co., Ltd. | Tricyclic pyrazole derivative |
US7189753B1 (en) | 1997-11-06 | 2007-03-13 | Cady Roger K | Preemptive prophylaxis of migraine |
US6960579B1 (en) | 1998-05-19 | 2005-11-01 | Alcon Manufacturing, Ltd. | Serotonergic 5HT7 receptor compounds for treating ocular and CNS disorders |
GB9819019D0 (en) * | 1998-09-01 | 1998-10-28 | Cerebrus Ltd | Chemical compounds II |
GB9820767D0 (en) * | 1998-09-23 | 1998-11-18 | Cerebrus Ltd | Chemical compounds VIII |
GB9918965D0 (en) * | 1999-08-11 | 1999-10-13 | Cerebrus Ltd | Chemical compounds xxi |
GB9918962D0 (en) * | 1999-08-11 | 1999-10-13 | Cerebrus Ltd | Chemical compounds xxii |
US6291504B1 (en) * | 1999-10-20 | 2001-09-18 | Dupont Pharmaceuticals Company | Acylsemicarbazides and their uses |
US20040048844A1 (en) * | 1999-10-20 | 2004-03-11 | Bristol-Myers Squibb Pharma Company | Acylsemicarbazides as cyclin dependent kinase inhibitors useful as anti-cancer and anti-proliferative agents |
EP1132389A1 (en) | 2000-03-06 | 2001-09-12 | Vernalis Research Limited | New aza-indolyl derivatives for the treatment of obesity |
DE60117247D1 (de) * | 2000-03-31 | 2006-04-20 | Purdue Research Foundation West Lafayette | Phosphoramidat-prodrugs |
WO2004098807A1 (en) * | 2000-11-21 | 2004-11-18 | Barsplice Products, Inc. | Method of making steel couplers for joining concrete reinforcing bars |
CA2432122A1 (en) | 2000-12-20 | 2002-08-01 | Bristol-Myers Squibb Pharma Company | Aryl and aminoaryl substituted serotonin receptor agonist and antagonist ligands |
RU2273641C2 (ru) * | 2001-06-01 | 2006-04-10 | Алькон, Инк. | Пираноиндазолы, фармацевтическая композиция на их основе и их использование при лечении глаукомы |
EP1392658A4 (en) * | 2001-06-01 | 2004-10-13 | Alcon Inc | NOVEL FUSED INDAZOLES AND INDOLES AND THEIR USE IN THE TREATMENT OF GLAUCOMES |
US6884816B2 (en) * | 2001-08-31 | 2005-04-26 | Alcon, Inc. | Hydroxy substituted fused naphthyl-azoles and fused indeno-azoles and their use for the treatment of glaucoma |
US20050080143A1 (en) * | 2001-11-29 | 2005-04-14 | Steiner Mitchell S. | Treatment of androgen-deprivation induced osteoporosis |
US20080249183A1 (en) * | 2001-11-29 | 2008-10-09 | Steiner Mitchell S | Treatment of androgen-deprivation induced osteoporosis |
US20070197664A1 (en) * | 2001-11-29 | 2007-08-23 | Steiner Mitchell S | Prevention and treatment of androgen-deprivation induced osteoporosis |
US20040214898A1 (en) * | 2001-11-29 | 2004-10-28 | Steiner Mitchell S. | Methods for treating hot flashes |
US20060269611A1 (en) * | 2001-11-29 | 2006-11-30 | Steiner Mitchell S | Prevention and treatment of androgen-deprivation induced osteoporosis |
TW593302B (en) * | 2001-12-20 | 2004-06-21 | Alcon Inc | Novel benzodifuranimidazoline and benzofuranimidazoline derivatives and their use for the treatment of glaucoma |
AU2002367323A1 (en) * | 2001-12-28 | 2003-07-24 | Bayer Pharmaceuticals Corporation | Benzothieno (3,2- |
WO2003057673A1 (en) * | 2001-12-28 | 2003-07-17 | Bayer Pharmaceuticals Corporation | 1h-pyrazolyl derivative compounds, for use in diseases associated with the 5-ht2c receptor |
US20050119489A1 (en) * | 2001-12-28 | 2005-06-02 | Ladouceur Gaetan H. | 4-Sulfide/sulfoxide/sulfonyl-1h-pyrazolyl derivative compounds, for use in diseases associated with the 5-ht2c receptor |
BR0314419A (pt) * | 2002-08-30 | 2005-07-19 | Alcon Inc | Compostos de 5-croman-5-il-etilamina substituìdos, seu uso e composição farmacêutica incluindo-o |
WO2004054572A2 (en) * | 2002-12-13 | 2004-07-01 | Alcon, Inc. | Novel benzopyran analogs and their use for the treatment of glaucoma |
US7476687B2 (en) * | 2003-11-26 | 2009-01-13 | Alcon, Inc. | Substituted furo[2,3-g]indazoles for the treatment of glaucoma |
US7338972B1 (en) | 2003-12-15 | 2008-03-04 | Alcon, Inc. | Substituted 1-alkylamino-1H-indazoles for the treatment of glaucoma |
US7129257B1 (en) * | 2003-12-15 | 2006-10-31 | Alcon, Inc. | Pyrazolo[3,4- e]benzoxazoles for the treatment of glaucoma |
AR046890A1 (es) * | 2003-12-15 | 2005-12-28 | Alcon Inc | [1,4] oxazino [2,3-g] indazoles sustituidos para el tratamiento del glaucoma. |
US7425572B2 (en) * | 2004-12-08 | 2008-09-16 | Alcon, Inc. | Use of dioxindoindazoles and dioxoloindazoles for treating glaucoma |
TW200744567A (en) * | 2005-09-23 | 2007-12-16 | Alcon Inc | Phenylethylamine analogs and their use for treating glaucoma |
WO2007149728A2 (en) * | 2006-06-20 | 2007-12-27 | Alcon Research, Ltd. | Aryl and heteroaryl tetrahydrobenzazepine derivatives and their use for treating glaucoma |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
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US392430A (en) * | 1888-11-06 | Tubular lantern | ||
GB1228792A (ko) * | 1967-07-20 | 1971-04-21 | ||
BE789948A (fr) * | 1971-10-13 | 1973-04-11 | Sandoz Sa | Nouveaux derives du pyrazole, leur preparation et leur application comme medicaments |
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1995
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- 1995-07-14 CA CA002153937A patent/CA2153937C/en not_active Expired - Fee Related
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1998
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