KR970704686A - Bicyclolactam compounds, uses thereof and intermediates thereof (BICYCLOLACTAM COMPOUNDS, USE OF THE SAME AND INTERMEDIATE IN THE PRODUCTION OF THE SAME) - Google Patents

Bicyclolactam compounds, uses thereof and intermediates thereof (BICYCLOLACTAM COMPOUNDS, USE OF THE SAME AND INTERMEDIATE IN THE PRODUCTION OF THE SAME) Download PDF

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KR970704686A
KR970704686A KR1019970700925A KR19970700925A KR970704686A KR 970704686 A KR970704686 A KR 970704686A KR 1019970700925 A KR1019970700925 A KR 1019970700925A KR 19970700925 A KR19970700925 A KR 19970700925A KR 970704686 A KR970704686 A KR 970704686A
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bicyclolactam
general formula
compound according
hydrogen atom
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KR1019970700925A
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KR100220172B1 (en
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가즈오 오가와
이치로 야마와키
마나부 가네다
다카시 아리마
준지 야마모토
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고바야시 유키오
다이호 야쿠힌 고교 가부시키가이샤
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    • 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
    • C07D209/52—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 condensed with a ring other than six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
    • 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
    • A61P25/22—Anxiolytics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/06—Ring systems of three rings
    • C07D221/16—Ring systems of three rings containing carbocyclic rings other than six-membered

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyrrole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Bicyclolactam compounds represented by general formula (1) are useful as the active ingredient of medicines having an excellent anxiolytic effect and a high safety with little side effects such as a hypnotic effect, a muscle relaxing effect, a sedative effect, etc. In said formula, R represents oxo or -OR<1> (wherein R<1> represents hydrogen or acyl); A represents one of the following groups (2) and (3); Q represents hydrogen or lower alkyl; l is 1 or 2, m is 0 or 1; and n is 0, 1 or 2, provided that m and n are not 0 at the same time; R<2> represents optionally substituted benzoyl.

Description

비시클로락탐 화합물, 그 용도 및 그 제조중간체(BICYCLOLACTAM COMPOUNDS, USE OF THE SAME AND INTERMEDIATE IN THE PRODUDTION OF THE SAME)Bicyclolactam compounds, uses thereof and intermediates thereof (BICYCLOLACTAM COMPOUNDS, USE OF THE SAME AND INTERMEDIATE IN THE PRODUTION OF THE SAME)

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is a trivial issue, I did not include the contents of the text.

Claims (17)

일반식(1)로 표시되는 비시클로락탐 화합물.A bicyclolactam compound represented by the general formula (1). 〔식 중, R은 옥소기 또는 -OR1이고, R1은 수소원자 또는 아실기이고, A는 식 (2) 또는 (3)의 기이며, Q는 수소원자 또는 저급알킬기이고, 1은 1 또는 2를, m은 0 또는 1을, n은 0,1 또는 2를 나타낸다. 단, m, n이 동시에 0인 경우를 제외한다.〕Wherein R is an oxo group or -OR 1 , R 1 is a hydrogen atom or an acyl group, A is a group of the formula (2) or (3), Q is a hydrogen atom or a lower alkyl group, Or 2, m represents 0 or 1, and n represents 0, 1 or 2. Provided that m and n are 0 at the same time. (R2는 치환기를 가져도 좋은 벤조일기를 나타낸다.)(R 2 represents a benzoyl group which may have a substituent) 일반식(4)로 표시되는 비시클로락탐 화합물.A bicyclolactam compound represented by the general formula (4). (식 중, A, Q, l, m, n은 상기와 같다. R3는 치환기를 가져도 좋은 벤조일기를 나타낸다.)(Wherein A, Q, l, m and n are as defined above, and R 3 represents a benzoyl group which may have a substituent.) 제1항 또는 제2항에 있어서, m 또는 n이 0인 것을 특징으로 하는 비시클로락탐 화합물.3. The bicyclic lactam compound according to claim 1 or 2, wherein m or n is 0. 제1항 또는 제2항에 있어서, 1이 l, m이 0, n이 2인 것을 특징으로 하는 비시클로락탐 화합물.3. The bicyclolactam compound according to claim 1 or 2, wherein 1 is 1, m is 0, and n is 2. 제1항에 있어서, R이 -OR1이고, R1이 수소원자 또는 아세틸기, R2가 저급알콕시기, 할로겐원자 또는 저급알킬기를 가져도 좋은 벤조일기, Q가 수소원자, 1이 l, m이 0, n이 2인 것을 특징으로 하는 비스클로락탐 화합물.The compound according to claim 1, wherein R is -OR 1 , R 1 is a hydrogen atom or an acetyl group, R 2 is a benzoyl group which may have a lower alkoxy group, a halogen atom or a lower alkyl group, Q is a hydrogen atom, m is 0, and n is 2. 제5항에 있어서, R이 -OR1이고, R1이 수소원자, R2가 메톡시기를 갖는 벤조일기, Q는 수소원자인 것을 특징으로 하는 비시클로락탐 화합물.The bicyclolactam compound according to claim 5, wherein R is -OR 1 , R 1 is a hydrogen atom, R 2 is a benzoyl group having a methoxy group, and Q is a hydrogen atom. 제1항에 있어서, R이 옥소기이고, R2가 저급알콕시기 또는 저급알킬기를 가져도 좋은 벤조일기, Q가 수소원자 또는 저급알킬기이고, 1이 l, m이 0, n이 2인 것을 특징으로 하는 비시클로락탐 화합물.2. The compound according to claim 1, wherein R is an oxo group, R 2 is a benzoyl group which may have a lower alkoxy group or a lower alkyl group, Q is a hydrogen atom or a lower alkyl group, 1 is 1, m is 0 and n is 2 Wherein the bicyclolactam compound is characterized by: 제7항에 있어서, R2가 메톡시기 또는 메틸시기를 갖는 벤조일기, Q가 수소원자 또는 메틸기인 것을 특징으로 하는 비시클로락탐 화합물.The bicyclolactam compound according to claim 7, wherein R 2 is a benzoyl group having a methoxy group or a methyl group, and Q is a hydrogen atom or a methyl group. 제2항에 있어서, R2가 저급알콕시기, 할로겐원자 또는 저급알킬기를 가져도 좋은 벤조일기, R3가 벤질기, Q가 수소원자이고, 1이 l, m이 0, n이 2인 것을 특징으로 비시클로락탐 화합물.The compound according to claim 2, wherein R 2 is a benzoyl group which may have a lower alkoxy group, a halogen atom or a lower alkyl group, R 3 is a benzyl group, Q is a hydrogen atom, 1 is 1, m is 0 and n is 2 Characterized in that the bicyclolactam compound. 제9항에 있어서, R2가 메톡시기를 갖는 벤조일기, R3가 벤질기인 것을 특징으로 하는 비시클로락탐 화합물.The bicyclolactam compound according to claim 9, wherein R 2 is a benzoyl group having a methoxy group, and R 3 is a benzyl group. 일반식(4)로 표시되는 비시클로락탐 화합물을 수소치환하는 것을 특징으로 하는 일반식(1')로 표시되는 비시클로락탐 화합물의 제조법.A process for producing a bicyclolactam compound represented by the general formula (1 ') wherein the bicyclolactam compound represented by the general formula (4) is substituted with hydrogen. (식 중, A, R3, Q, l, m, n은 상기와 같다).(Wherein A, R 3 , Q, l, m and n are as defined above). (식 중, A, Q, l, m 및 n은 상기와 같다.)(Wherein A, Q, l, m and n are as defined above). 일반식(1')로 표시되는 비시클로락탐 화합물을 아실화하는 것을 특징으로 하는 일반식(1')로 표시되는 비시클로락탐 화합물의 제조방법.A process for producing a bicyclolactam compound represented by the general formula (1 '), which comprises acylating a bicyclolactam compound represented by the general formula (1'). (식 중, A, Q, l, m 및 n은 상기와 같다.)(Wherein A, Q, l, m and n are as defined above). (식 중, A, Q, l, m 및 n은 상기와 같다. R1a는 아실기를 나타낸다.)(Wherein A, Q, l, m and n are as defined above, and R &lt; 1a &gt; represents an acyl group. 일반식(5)로 표시되는 화합물과 일반식(6)으로 표시되는 비시클로락탐 화합물을 염기존재하 반응시키는 것을 특징으로 하는 일반식(1')로 표시되는 비시클로락탐 화합물의 제조방법.A process for producing a bicyclolactam compound represented by the general formula (1 '), which comprises reacting a compound represented by the general formula (5) and a bicyclolactam compound represented by the general formula (6) in the presence of a base. (식 중, R2는 상기와 같다. X는 할로겐원자를 나타낸다.)(Wherein R 2 is as defined above), and X represents a halogen atom. (식 중, Q 및 l은 상기와 같다.)(Wherein Q and l are as defined above). (식 중, R2, Q 및 l은 상기와 같다.)(Wherein R 2 , Q and l are as defined above). 제1항에 기재된 비시클로락탐 화합물의 유효량과 약학적 담체를 함유하는 것을 특징으로 하는 의약조성물.A medicinal composition characterized by containing an effective amount of the bicyclolactam compound according to claim 1 and a pharmaceutical carrier. 제1항에 기재된 비시클로락탐 화합물의 유효량의 약학적 담체를 함유하는 것을 특징으로 하는 항불안약.An anxiolytic drug characterized by containing an effective amount of a pharmaceutical carrier of the non-cyclolactam compound according to claim 1. 제1항에 기재된 비시클로락탐 화합물의 유효량을 사람을 포함한 표유동물에 투여하는 것으로 이루어지는 불안증을 치료하기 위한 방법.A method for treating an anxiety disorder comprising administering an effective amount of the bicyclolactam compound according to claim 1 to a marine animal including a human. 불안증 치료용 의약을 제조하기 위한 제1항에 기재된 항불안약의 사용.Use of an anxiolytic drug according to claim 1 for the manufacture of a medicament for the treatment of anxiety. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: It is disclosed by the contents of the first application.
KR1019970700925A 1995-06-12 1996-06-07 Bicyclolactam compounds, use of the same and intermediates in the production of the same KR100220172B1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
JP17032995 1995-06-12
JP95-170329 1995-06-12
JP27465495A JP3161948B2 (en) 1995-06-12 1995-09-27 Bicyclolactam compound
JP95-274654 1995-09-27
PCT/JP1996/001565 WO1996041796A1 (en) 1995-06-12 1996-06-07 Bicyclolactam compounds, use of the same and intermediate in the production of the same

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KR970704686A true KR970704686A (en) 1997-09-06
KR100220172B1 KR100220172B1 (en) 1999-09-01

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KR1019970700925A KR100220172B1 (en) 1995-06-12 1996-06-07 Bicyclolactam compounds, use of the same and intermediates in the production of the same

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JP (1) JP3161948B2 (en)
KR (1) KR100220172B1 (en)
AT (1) ATE224369T1 (en)
AU (1) AU697656B2 (en)
CA (1) CA2197178C (en)
DE (1) DE69623747T2 (en)
DK (1) DK0790237T3 (en)
ES (1) ES2183956T3 (en)
PT (1) PT790237E (en)
WO (1) WO1996041796A1 (en)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0466933B1 (en) * 1990-02-02 1995-11-22 Taiho Pharmaceutical Company Limited Bicyclolactam derivative
PT713702E (en) * 1994-03-28 2005-01-31 Taiho Pharmaceutical Co Ltd ANSIOLITIC AGENT

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ES2183956T3 (en) 2003-04-01
KR100220172B1 (en) 1999-09-01
AU5911896A (en) 1997-01-09
JP3161948B2 (en) 2001-04-25
WO1996041796A1 (en) 1996-12-27
CA2197178C (en) 2001-05-01
ATE224369T1 (en) 2002-10-15
CA2197178A1 (en) 1996-12-27
DE69623747D1 (en) 2002-10-24
PT790237E (en) 2003-02-28
JPH0959251A (en) 1997-03-04
AU697656B2 (en) 1998-10-15
DE69623747T2 (en) 2003-05-22
DK0790237T3 (en) 2002-10-14

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