KR880007075A - Anxiotic-N- (1-azabicyclo [2.2.2] oct-3-yl) benzamide and thiobenzamide - Google Patents

Anxiotic-N- (1-azabicyclo [2.2.2] oct-3-yl) benzamide and thiobenzamide Download PDF

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KR880007075A
KR880007075A KR870014303A KR870014303A KR880007075A KR 880007075 A KR880007075 A KR 880007075A KR 870014303 A KR870014303 A KR 870014303A KR 870014303 A KR870014303 A KR 870014303A KR 880007075 A KR880007075 A KR 880007075A
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oct
azabicyclo
amino
formula
methoxybenzamide
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KR870014303A
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Korean (ko)
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죤 네일러 로버트
네일러 브렌다
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원본미기재
에이 · 에이취 · 로빈스 캄파니 인코포레이티드
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Priority claimed from GB878709508A external-priority patent/GB8709508D0/en
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Abstract

내용 없음.No content.

Description

안크시올리틱－N－(1－아자비시클로[2.2.2]옥트－3－일)벤즈아미드와 티오벤즈아미드Anxiolytic-N- (1-azabicyclo [2.2.2] oct-3-yl) benzamide and thiobenzamide

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

제1도는 약리학적 실시예 D에서 니코틴 처리한 쥐를 니코틴에서 제거한 후에 나온 결과를 나타낸 그래프.1 is a graph showing the results after removing nicotine treated mice from nicotine in pharmacological Example D.

Claims (14)

다음 일반식(Ⅰ)의 화합물 또는 이의 약학적으로 수용할 수 있는 산부가염과 약학적으로 수용할 수 있는 담체와 혼합하여 매일 5mg 이하의 일반식(Ⅰ)의 화합물을 투여하는데 적합한 조성물을 제조함을 특징으로 하는 약학적 조성물의 제조방법.To prepare a composition suitable for the administration of a compound of formula (I) up to 5 mg daily by mixing with a compound of formula (I) or a pharmaceutically acceptable acid addition salt thereof and a pharmaceutically acceptable carrier Method for producing a pharmaceutical composition, characterized in that. (상기식에서 X는 산소 또는 황이고 ; R1은 저급알킬을 나타내고 ; R2는 수소, 할로겐, 4,5－벤조, 저급알콕시, 아미노, 메틸아미노 또는 디메틸아미노이고 ; R3는 수소 또는 저급알킬이고 ; n은 1또는 2이다).Wherein X is oxygen or sulfur; R 1 represents lower alkyl; R 2 is hydrogen, halogen, 4,5-benzo, lower alkoxy, amino, methylamino or dimethylamino; R 3 is hydrogen or lower alkyl N is 1 or 2). 다음 일반식(Ⅰ)의 화합물 또는 이의 약학적으로 수용할 수 있는 산부가염과, 약학적으로 수용할 수 있는 담체를 혼합하여 조성물이 500mcg까지의 일반식(Ⅰ)의 화합물을 함유함을 특징으로 하는 단위 투약 형태의 약학적 조성물의 제조방법.The composition comprises a compound of formula (I) up to 500 mcg by mixing a compound of formula (I) or a pharmaceutically acceptable acid addition salt thereof with a pharmaceutically acceptable carrier A method of preparing a pharmaceutical composition in unit dosage form. (상기식에서 X는 산소 또는 황을 나타내며 ; R1은 저급알킬을 나타내며 ; R2는 수소, 할로겐, 4,5－벤조, 저급알콕시, 아미노, 메틸아미노 또는 디메틸아미노를 나타내며 ; n은 1또는 2이다).Wherein X represents oxygen or sulfur; R 1 represents lower alkyl; R 2 represents hydrogen, halogen, 4,5-benzo, lower alkoxy, amino, methylamino or dimethylamino; n represents 1 or 2 to be). 제2항에 있어서, 50mcg의 화합물을 담체와 혼합함을 특징으로 하는 제조방법.A process according to claim 2, wherein 50 mcg of compound is mixed with a carrier. 제1항, 제2항 또는 제3항에 있어서, 일반식(Ⅰ)에서 R2가 3－또는 5－할로겐 치환기를 나타냄을 특징으로 하는 제조방법.The process according to claim 1, 2 or 3, wherein R 2 represents a 3-or 5-halogen substituent in the general formula (I). 제1항 내지 제4항 중 어느 한 항에 있어서, 일반식(Ⅰ)에서 R2가 4－아미노, 4－메틸아미노 또는 4－디메틸아미노 치환기임을 특징으로 하는 제조방법.The process according to any one of claims 1 to 4, wherein in formula (I), R 2 is a 4-amino, 4-methylamino or 4-dimethylamino substituent. 제1항 내지 제5항 중 어느 한 항에 있어서, 일반식(Ⅰ)에서 X가 산소임을 특징으로 하는 제조방법.The process according to any one of claims 1 to 5, wherein X in formula (I) is oxygen. 제1항 내지 제7항 중 어느 한 항에 있어서, 화합물이 4－아미노－N－(1－아자비시클로[2.2.2]옥트－3－일)－5클로로－2－메톡벤즈아미드, N－(1－아자비시클로[2.2.2]옥트－3－일)－5－클로로－2－메톡시－4－메틸아미노벤즈아미드, N－(1－아자비시클로[2.2.2]옥트－3－일)－2－메톡시벤즈아미드, N－(1－아자비시클로[2.2.2]옥트－3－일)－2,4－디메톡시벤즈아미드, 4－아미노－N－(1－아자비시클로[2.2.2]옥트－3－일－5－클로로－2－메톡시벤즈아미드, N－(1－아자비시클로[2.2.2]옥트－3－일)－5－클로로－2－메톡시－4－메틸아미노벤즈아미드, N－(1－아자－비시클로[2.2.2]옥트－3－일－메톡시－2－나프탈렌카르복스이미드 4－아미노－N－(1－아자－2－메틸－비시클로[2.2.2]옥트－3－일)－5－클로로－2－메톡시벤즈아미드, 또는 이의 약학적으로 수용할 수 있는 염임을 특징으로 하는 제조방법.The compound according to any one of claims 1 to 7, wherein the compound is 4-amino-N- (1-azabicyclo [2.2.2] oct-3-yl) -5chloro-2-methoxybenzamide, N- (1-Azabicyclo [2.2.2] oct-3-yl) -5-chloro-2-methoxy-4-methylaminobenzamide, N- (1-azabicyclo [2.2.2] oct-3-yl ) -2-methoxybenzamide, N- (1-azabicyclo [2.2.2] oct-3-yl) -2,4-dimethoxybenzamide, 4-amino-N- (1-azabicyclo [2.2 .2] oct-3-yl-5-chloro-2-methoxybenzamide, N- (1-azabicyclo [2.2.2] oct-3-yl) -5-chloro-2-methoxy-4- Methylaminobenzamide, N- (1-aza-bicyclo [2.2.2] oct-3-yl-methoxy-2-naphthalenecarboximide 4-amino-N- (1-aza-2-methyl-bi Cyclo [2.2.2] oct-3-yl) -5-chloro-2-methoxybenzamide, or a pharmaceutically acceptable thereof Method for producing a salt. 다음 일반식(ⅠA)의 화합물 또는 이의 약학적으로 수용할 수 있는 산부 가염과, 약학적으로 수용할 수 있는 담체를 혼합함을 특징으로 하는 약학적 조성물의 제조방법.A method for preparing a pharmaceutical composition comprising mixing a compound of formula (IA) or a pharmaceutically acceptable acid salt thereof and a pharmaceutically acceptable carrier. (상기식에서 X는 산소 또는 황이고 : R1은 저급알킬을 나타내며 ; R2는 수소, 할로겐, 4,5－벤조, 저급알콕시, 아미노, 메틸아미노 또는 디메틸아미노를 나타내며 ; R3는 저급알킬이고 ; n은 1또는 2이다)Wherein X is oxygen or sulfur: R 1 represents lower alkyl; R 2 represents hydrogen, halogen, 4,5-benzo, lower alkoxy, amino, methylamino or dimethylamino; R 3 is lower alkyl n is 1 or 2) 4－아미노－N－(1－아자－2－메틸－비시클로[2.2.2]옥트－3－일)－5－클로로－2－메톡시벤즈아미드 또는 이의 약학적으로 수용할 수 있는 염과, 약학적으로 수용할 수 있는 담체를 혼합함을 특징으로 하는 약학적 조성물의 제조방법.With 4-amino-N- (1-aza-2-methyl-bicyclo [2.2.2] oct-3-yl) -5-chloro-2-methoxybenzamide or a pharmaceutically acceptable salt thereof , A method for producing a pharmaceutical composition comprising mixing a pharmaceutically acceptable carrier. 항불안에 유효한량의 다음 일반식(Ⅰ)의 화합물 또는 이의 약학적으로 수용할 수 있는 산부가염을 투여함을 특징으로 하는 불안을 치료 또는 예방하는 방법.A method of treating or preventing anxiety, characterized by administering an anti-anxiety effective amount of a compound of formula (I): or a pharmaceutically acceptable acid addition salt thereof. (상기식에서 X는 산소 또는 황을 나타내고 : R1은 저급알킬이고 ; R2는 수소, 할로겐, 4,5－벤조, 저급알콕시, 아미노, 메틸아미노 또는 디메틸아미노를 나타내고 ; R3는 수소 또는 저급알킬이고 ; n은 1또는 2이다)Wherein X represents oxygen or sulfur: R 1 is lower alkyl; R 2 represents hydrogen, halogen, 4,5-benzo, lower alkoxy, amino, methylamino or dimethylamino; R 3 represents hydrogen or lower Alkyl; n is 1 or 2) 제10항에 있어서, 일반식(Ⅰ)에서 R2가 3－또는 5－할로겐 치환기임을 특징으로 하는 불안 치료 또는 예방방법.The method for treating or preventing anxiety according to claim 10, wherein R 2 in formula (I) is a 3-or 5-halogen substituent. 제10항 또는 제11항에 있어서, 일반식(Ⅰ)에서 R2가 4－아미노, 4－메틸아미노 또는 4－디메틸아미노 치환기임을 특징으로 하는 불안 치료 또는 예방방법.The method for treating or preventing anxiety according to claim 10 or 11, wherein in formula (I), R 2 is a 4-amino, 4-methylamino or 4-dimethylamino substituent. 제10항, 제11항 또는 제12항에 있어서, 일반식(Ⅰ)에서, X가 산소임을 특징으로 하는 불안 치료 또는 예방방법.The method for treating or preventing anxiety according to claim 10, 11 or 12, wherein in formula (I), X is oxygen. 항불안에 유효한 양의 4－아미노－N－(1－아자비시클로[2.2.2]옥트－3－일)－5－클로로－2－메톡시벤즈아미드, N－(1－아자비시클로[2.2.2]옥트－3－일)－5－클로로－2－메톡시－4－메틸아미노벤즈아미드, N－(1－아자비시클로[2.2.2]옥트－3－일)－2메톡시벤즈아미드, N－(1－아자비시클로[2.2.2]옥트－3－일)－2,4－디메톡시벤즈아미드, N－(1－아자비시클로[2.2.2]옥트－3－일)－2－프로폭시벤즈아미드, 4－아미노－N－(1－아자비시클로[2.2.2]옥트－3－일)－5－클로로－2－메톡시벤즈아미드, N－(1－아자비시클로[2.2.2]옥트－3－일)－5－클로로－2－메톡시－4－메톡시벤즈아미드, N－(1－아자비시클로[2.2.2]옥트－3－일)－3－메톡시－2－나프탈렌카르복스이미드, 4－아미노－N－(1－아자－2－메틸－비시클로[2.2.2]옥트－3－일)－5－클로로－2－메톡시벤즈아미드, 또는 이의 약학적으로 수용할 수 있는 염을 투여함을 특징으로 하는 불안 치료 또는 예방방법.4-amino-N- (1-azabicyclo [2.2.2] oct-3-yl) -5-chloro-2-methoxybenzamide, N- (1-azabicyclo [2.2. 2] oct-3-yl) -5-chloro-2-methoxy-4-methylaminobenzamide, N- (1-azabicyclo [2.2.2] oct-3-yl) -2-methoxybenzamide, N- (1-azabicyclo [2.2.2] oct-3-yl) -2,4-dimethoxybenzamide, N- (1-azabicyclo [2.2.2] oct-3-yl) -2-pro Foxybenzamide, 4-amino-N- (1-azabicyclo [2.2.2] oct-3-yl) -5-chloro-2-methoxybenzamide, N- (1-azabicyclo [2.2.2] Oct-3-yl) -5-chloro-2-methoxy-4-methoxybenzamide, N- (1-azabicyclo [2.2.2] oct-3-yl) -3-methoxy-2-naphthalene Carboximide, 4-amino-N- (1-aza-2-methyl-bicyclo [2.2.2] oct-3-yl) -5-chloro-2-methoxybenzamide, Anxiety is the treatment or prevention method which comprises administering to a salt that can be accepted pharmaceutically. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR870014303A 1986-12-16 1987-12-15 Anxiotic-N- (1-azabicyclo [2.2.2] oct-3-yl) benzamide and thiobenzamide KR880007075A (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB868629962A GB8629962D0 (en) 1986-12-16 1986-12-16 Benzamides & thiobenzamides
GB8629962 1986-12-16
GB878709508A GB8709508D0 (en) 1987-04-22 1987-04-22 Benzamides & thiobenzamides
GB8709508 1987-04-22

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KR880007075A true KR880007075A (en) 1988-08-26

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