KR940701258A - Use of tetrahydrobenzazine derivatives for the treatment of portal hypertension and migraine headaches - Google Patents

Use of tetrahydrobenzazine derivatives for the treatment of portal hypertension and migraine headaches

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Publication number
KR940701258A
KR940701258A KR1019930703940A KR930703940A KR940701258A KR 940701258 A KR940701258 A KR 940701258A KR 1019930703940 A KR1019930703940 A KR 1019930703940A KR 930703940 A KR930703940 A KR 930703940A KR 940701258 A KR940701258 A KR 940701258A
Authority
KR
South Korea
Prior art keywords
benzazine
tetrahydro
compound
hydroxy
hydrogen
Prior art date
Application number
KR1019930703940A
Other languages
Korean (ko)
Inventor
게라드 워드 죤
크리스토퍼 영 로드니
쥴리오 카우만 알베르토
Original Assignee
피터 죤 기딩즈
스미스클라인 비참 피엘씨
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GB919113377A external-priority patent/GB9113377D0/en
Priority claimed from GB919113379A external-priority patent/GB9113379D0/en
Application filed by 피터 죤 기딩즈, 스미스클라인 비참 피엘씨 filed Critical 피터 죤 기딩즈
Publication of KR940701258A publication Critical patent/KR940701258A/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16—Benzazepines; Hydrogenated benzazepines
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

본 발명은 테트라하이드로벤즈아제핀 유도체를 약물로서 기재하고 있다.The present invention describes tetrahydrobenzazine derivatives as drugs.

Description

문맥압 항진증 및 편두통의 치료를 위한 테트라하이드로벤즈아제핀 유도체의 용도Use of tetrahydrobenzazine derivatives for the treatment of portal hypertension and migraine headaches

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (12)

문맥압항진증 및/또는 편두통을 치료하는 약물제조를 위한 구조식(I)의 화합물 또는 이의 약제학적으로 허용되는 염의 용도:Use of a compound of formula (I) or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for treating portal hypertension and / or migraine: 상기식에서, R은 수소, C1-6알킬 또는 C3-5알케닐이고; R1은 NO2, 시아노, 할로, COR3, SOaNR5R6이고; R2는 수소, 하이드록시 또는 C1-4알콕시이고; R3은 수소, C1-4알, OR5또는 NR5R6이고; R4는 C1-6알킬 또는 할로 C1-6알킬이고; R5및 R6은 수소, C3-6사이클로알키링고; n은 1 또는 2이다.Wherein R is hydrogen, C 1-6 alkyl or C 3-5 alkenyl; R 1 is NO 2 , cyano, halo, COR 3 , SO a NR 5 R 6 ; R 2 is hydrogen, hydroxy or C 1-4 alkoxy; R 3 is hydrogen, C 1-4 al, OR 5 or NR 5 R 6 ; R 4 is C 1-6 alkyl or halo C 1-6 alkyl; R 5 and R 6 are hydrogen, C 3-6 cycloalkyringo; n is 1 or 2. 제1항에 있어서, R1이 구조식(I)의 화합물의 환의 8-위치에 있고 R2가 7-위치에 있는 화합물의 용도.The use of a compound according to claim 1, wherein R 1 is at the 8-position of the ring of the compound of formula (I) and R 2 is at the 7-position. 제1항 또는 제2항에 있어서, R1이 SO2R3이고, R2가 수소, 알콕시 또는 하이드록시이고 R이 수소인 화합물의 용도.3. The use according to claim 1, wherein R 1 is SO 2 R 3 , R 2 is hydrogen, alkoxy or hydroxy and R is hydrogen. 제1항 내지 제3항중 어느 한 항에 있어서, R3이 메틸이고 R2가 하이드록시인 화합물의 용도.The use according to any one of claims 1 to 3, wherein R 3 is methyl and R 2 is hydroxy. 제1항에 있어서, 7-하이드록시-8-메틸설포닐-2,3,4,5-테트라하이드로-1H-벤즈아제핀인 화합물의 용도.Use of a compound according to claim 1 which is 7-hydroxy-8-methylsulfonyl-2,3,4,5-tetrahydro-1H-benzazine. 7-메톡시-8-메틸설피닐-2,3,4,5-테트라하이드로-1H-벤즈아제핀; 7-메톡시-8-니트로-2,3,4,5-테트라하이드로-1H-벤즈아제핀; 7-하이드록시-8-니트로-2,3,4,5-테트라하이드로-1H-벤즈아제핀; 7-메톡시-8-브로모-2,3,4,5-테트라하이드로-1H-벤즈아제핀; 7-브로모-8-하이드록시-2,3,4,5-테트라하이드로-1H-벤즈아제핀; 7-메톡시-6-니트로-2,3,4,5-테트라하이드로-1H-벤즈아제핀; 6-브로모-7-메톡시-2,3,4,5-테트라하이드로-1H-벤즈아제핀; 8-아세틸-7-하이드록시-2,3,4,5-테트라하이드로-1H-벤즈아제핀; 7-하이드록시-8-메틸설피닐-2,3,4,5-테트라하이드로-1H-벤즈아제핀; 또는 7-하이드록시-8-트리플루오로메틸설포닐-2,3,4,5-테트라하이드로-1H-벤즈아제핀인 제1항의 화합물 또는 이의 약제학적으로 허용되는 염.7-methoxy-8-methylsulfinyl-2,3,4,5-tetrahydro-1H-benzazine; 7-methoxy-8-nitro-2,3,4,5-tetrahydro-1H-benzazine; 7-hydroxy-8-nitro-2,3,4,5-tetrahydro-1H-benzazine; 7-methoxy-8-bromo-2,3,4,5-tetrahydro-1H-benzazine; 7-bromo-8-hydroxy-2,3,4,5-tetrahydro-1H-benzazine; 7-methoxy-6-nitro-2,3,4,5-tetrahydro-1H-benzazine; 6-bromo-7-methoxy-2,3,4,5-tetrahydro-1H-benzazine; 8-acetyl-7-hydroxy-2,3,4,5-tetrahydro-1H-benzazine; 7-hydroxy-8-methylsulfinyl-2,3,4,5-tetrahydro-1H-benzazine; Or 7-hydroxy-8-trifluoromethylsulfonyl-2,3,4,5-tetrahydro-1H-benzazine, or a pharmaceutically acceptable salt thereof. 제6항의 화합물 또는 이의 약제학적으로 허용되는 염과 함께 약제학적으로 허용되는 담체 또는 부형제를 함유하는 약제학적 조성물.A pharmaceutical composition comprising a pharmaceutically acceptable carrier or excipient together with the compound of claim 6 or a pharmaceutically acceptable salt thereof. a) 구조식(II)의 화합물을 삼염화티타늄의 존재하에 산화제와 반응시켜, R1이 -SOaR4를 나타내는 구조식(I)의 화합물을 제조하거나; b) 구조식(III)의 화합물을 적절한 아실화제, 니트로화제 또는 할로겐화제와 각각 반응시켜, R1이 -COR3, NO2또는 할로겐을 나타내는 구조식(I)의 화합물을 제조한후; 각각의 경우에 N-보호그룹을 제거하고, 필요한 경우 염을 형성시킴을 포함하는, 구조식(I)의 화합물의 제조방법:a) reacting a compound of formula (II) with an oxidizing agent in the presence of titanium trichloride to produce a compound of formula (I) wherein R 1 represents -SO a R 4 ; b) reacting the compound of formula (III) with an appropriate acylating agent, nitrating agent or halogenating agent, respectively, to prepare a compound of formula (I) wherein R 1 represents -COR 3 , NO 2 or halogen; A process for preparing a compound of formula (I) comprising removing in each case an N-protecting group and forming a salt if necessary: 할로 C1-6알킬이고; R5및 R6은 수소, C1-6알킬 또는 C3-6사이클로알킬이고; n은 1 또는 2이고; R7은 n-보호그룹이다.Halo C 1-6 alkyl; R 5 and R 6 are hydrogen, C 1-6 alkyl or C 3-6 cycloalkyl; n is 1 or 2; R 7 is an n-protecting group. 문맥압항진증 치료를 위한 5-HT2수용체 효능제의 용도.Use of 5-HT 2 receptor agonists for the treatment of portal hypertension. 문맥압항진증 치료를 위한 5-HT1-유사-수용체 효능제의 용도.Use of 5-HT 1 -like-receptor agonists for the treatment of portal hypertension. 문맥압항진증 치료를 위한 5-HT2수용체와 5-HT1-유사-수용체 모두에 효능제인 화합물의 용도.Use of a compound that is an agonist for both 5-HT 2 receptor and 5-HT 1 -like-receptor for the treatment of hypertension. 편두통의 치료 및 예방을 위한 5-HT2수용체 효능제의 용도.Use of 5-HT 2 receptor agonists for the treatment and prevention of migraine headaches. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019930703940A 1991-06-21 1992-06-17 Use of tetrahydrobenzazine derivatives for the treatment of portal hypertension and migraine headaches KR940701258A (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GB9113379.3 1991-06-21
GB919113377A GB9113377D0 (en) 1991-06-21 1991-06-21 Medicaments
GB9113377.7 1991-06-21
GB919113379A GB9113379D0 (en) 1991-06-21 1991-06-21 Medicaments
PCT/GB1992/001083 WO1993000094A2 (en) 1991-06-21 1992-06-17 Use of tetrahydrobenzazepine derivatives for the treatment of portal hypertension and migraine

Publications (1)

Publication Number Publication Date
KR940701258A true KR940701258A (en) 1994-05-28

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KR1019930703940A KR940701258A (en) 1991-06-21 1992-06-17 Use of tetrahydrobenzazine derivatives for the treatment of portal hypertension and migraine headaches

Country Status (9)

Country Link
EP (1) EP0589973A1 (en)
JP (1) JPH06508352A (en)
KR (1) KR940701258A (en)
AU (1) AU1927992A (en)
CA (1) CA2110575A1 (en)
IE (1) IE921990A1 (en)
MX (1) MX9203012A (en)
PT (1) PT100602A (en)
WO (1) WO1993000094A2 (en)

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BRPI0411470A (en) 2003-06-17 2006-07-11 Arena Pharm Inc benzazepine derivatives useful for the treatment of 5ht2c receptor-associated diseases
TW200510324A (en) * 2003-08-11 2005-03-16 Lilly Co Eli 6-(2,2,2-trifluoroethylamino)-7-chiloro-2, 3, 4, 5-tetrahydro-1h-benzo[d]azepine as a 5-ht2c receptor agonist
ATE442359T1 (en) 2004-12-21 2009-09-15 Arena Pharm Inc CRYSTALLINE FORMS OF (R)-8-CHLORINE-1-METHYL-2,3,4,5-TETRAHYDRO-1H-3-BE ZAZEPINE HYDROCHLORIDE
NZ555482A (en) 2004-12-23 2011-01-28 Arena Pharm Inc Compositions comprising a 5HT2C receptor modulator and 2-methylamphetamine and methods of use
CN101466684B (en) 2006-04-03 2012-06-20 艾尼纳制药公司 Processes for the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine and intermediates related thereto
SG177128A1 (en) 2006-12-05 2012-01-30 Arena Pharm Inc Processes for preparing (r)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine and intermediates thereof
WO2009111004A1 (en) 2008-03-04 2009-09-11 Arena Pharmaceuticals, Inc. Processes for the preparation of intermediates related to the 5-ht2c agonist (r)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine
US8952197B2 (en) 2009-06-18 2015-02-10 Arena Pharmaceuticals, Inc. Processes for the preparation of 5-HT2C receptor agonists
KR20130112848A (en) 2010-06-02 2013-10-14 아레나 파마슈티칼스, 인크. Processes for the preparation of 5-ht2c receptor agonists
EP2611449A1 (en) 2010-09-01 2013-07-10 Arena Pharmaceuticals, Inc. Administration of lorcaserin to individuals with renal impairment
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AU2011296014A1 (en) * 2010-09-01 2013-04-04 Arena Pharmaceuticals, Inc. Salts of lorcaserin with optically active acids
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Also Published As

Publication number Publication date
MX9203012A (en) 1993-07-01
CA2110575A1 (en) 1993-01-07
AU1927992A (en) 1993-01-25
EP0589973A1 (en) 1994-04-06
IE921990A1 (en) 1992-12-30
WO1993000094A3 (en) 1993-03-04
JPH06508352A (en) 1994-09-22
PT100602A (en) 1993-09-30
WO1993000094A2 (en) 1993-01-07

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