KR970707101A - Substituted benzylamine derivatives; A new class of neuropeptide Y1 specific ligands (CERTAIN SUBSTITUTED BENZYLAMINE DERIVATIVES; A NEW CLASS OF NEUROPEPTIDE Y1 SPECIFIC LIGANDS) - Google Patents

Substituted benzylamine derivatives; A new class of neuropeptide Y1 specific ligands (CERTAIN SUBSTITUTED BENZYLAMINE DERIVATIVES; A NEW CLASS OF NEUROPEPTIDE Y1 SPECIFIC LIGANDS)

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KR970707101A
KR970707101A KR1019970702989A KR19970702989A KR970707101A KR 970707101 A KR970707101 A KR 970707101A KR 1019970702989 A KR1019970702989 A KR 1019970702989A KR 19970702989 A KR19970702989 A KR 19970702989A KR 970707101 A KR970707101 A KR 970707101A
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compound according
phenylpiperazin
straight
cyclohexane
carbon atoms
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KR1019970702989A
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존 엠 피터슨
찰스 에이 블럼
구올린 카이
알란 허치슨
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스피겔 알렌 제이
화이자 인코포레이티드
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Abstract

본 발명은 인간의 신경펩타이드 Y1 수용체에 대한 결합력에 기인하여 비만 및 병적 기아 등의 섭식 장애, 및 본질적인 고혈압 및 울혈성 심부전 등의 심혈관계 질환을 진단하고 치료하는데 유용한 화학식(Ⅰ)의 화합물 및 약학적으로 허용가능한 이의 염을 포함한다:The present invention relates to compounds of formula (I) useful for diagnosing and treating cardiovascular diseases, such as eating disorders such as obesity and pathological starvation, and intrinsic hypertension and congestive heart failure, due to binding capacity to human neuropeptide Y1 receptor Or a pharmaceutically acceptable salt thereof:

상기 식에서 W, X, Y, A 및 T는 유기 또는 무기 치환체이고, n은 1, 2 또는 3이고, m은 2, 3 또는 4이고, R1내지 R4는 수소 또는 유기 치환체이고, B는 질소, 탄소, 황 또는 산소이다.Wherein n is 1, 2 or 3, m is 2, 3 or 4, R 1 to R 4 are hydrogen or an organic substituent, and B is Nitrogen, carbon, sulfur or oxygen.

Description

치환된 벤질아민 유도체; 신규한 부류의 신경펩타이드 Y1 특이적 리간드(CERTAIN SUBSTITUTED BENZYLAMINE DERIVATIVES; A NEW CLASS OF NEUROPEPTIDE Y1 SPECIFIC LIGANDS)Substituted benzylamine derivatives; A new class of neuropeptide Y1 specific ligands (CERTAIN SUBSTITUTED BENZYLAMINE DERIVATIVES; A NEW CLASS OF NEUROPEPTIDE Y1 SPECIFIC LIGANDS)

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

Claims (28)

화학식(Ⅰ)의 화합물 또는 약학적으로 허용가능한 이의 염:A compound of formula (I) or a pharmaceutically acceptable salt thereof: 상기 식에서, Ar은 페닐, 2-, 3- 또는 4-피리딜, 2- 또는 3-티에닐, 2-, 4- 또는 5-피리미딜이고, 이들 각각은 임의로 할로겐, 하이드록시, 또는 탄소수 1 내지 6의 직쇄 또는 측쇄의 저급 알킬로 단치환 또는 이치환되고; B는 황, 산소, N(R5), 또는 C(R5)(R6)이고; n은 1, 2 또는 3이고; m은 2, 3 또는 4이고; W, XY 및 T는 동일하거나 상이하고, 수소, 할로겐, 하이드록시, 탄소수 1 내지 6의 직쇄 또는 측쇄의 저급 알킬, 또는 탄소수 1 내지 6의 직쇄는 측쇄의 저급 알콕시이고; R1및 R2는 동일하거나 상이하고, 수소, 또는 탄소수 1 내지 6의 직쇄 또는 측쇄의 저급 알킬이고; R3및 R4는 동일하거나 상이하고, 수소, 탄소수 1 내지 6의 직쇄 또는 측쇄의 저급 알킬, 또는 탄소수 1 내지 6의 직쇄 또는 측쇄의 저급 알콕시이고; R5는 탄소수 1 내지 6의 직쇄 또는 측쇄의 저급 알킬, 페닐, 2-, 3- 또는 4-피리딜 또는 탄소수 1 내지 6의 직쇄 또는 측쇄의 저급 알킬로 치환된 페닐, 2-, 3- 또는 4-피리딜이고; A 및 R6은 동일하거나 상이하고, 수소, 하이드록실, 아미노, 탄소수 1 내지 6의 직쇄 또는 측쇄의 저급 알킬, 탄소수 1 내지 6의 직쇄 또는 측쇄의 저급 알콕시, 페닐, 2-, 3- 또는 4-피리딜, 페녹시, 2-, 3- 또는 4-피리딜옥시, 또는 -(CH2)p-A'-(CH2)qB'이고, 이때 p는 0 내지 5이고, q는 1 내지 5이고, A'는 직접 결합, 산소 또는 황이고, B'는 수소, 탄소수 1 내지 6의 직쇄 또는 측쇄의 저급 알킬, 탄소수 1 내지 6의 직쇄 또는 측쇄의 저급 알콕시, 페닐, 2-, 3- 또는 4-피리딜, 페녹시, 2-, 3- 또는 4-피리딜옥시, 카복실, 카보알콕시, 카복스아미도, 모노 또는 디알킬카복스아미도, 아미노, 또는 모노 또는 디알킬아미노이다.Wherein Ar is phenyl, 2-, 3- or 4-pyridyl, 2- or 3-thienyl, 2-, 4- or 5-pyrimidyl, each of which is optionally substituted with halogen, ≪ / RTI > to 6, linear or branched, lower alkyl; B is sulfur, oxygen, N (R 5), or C (R 5) (R 6 ) , and; n is 1, 2 or 3; m is 2, 3 or 4; W, XY and T are the same or different and are hydrogen, halogen, hydroxy, straight or branched chain lower alkyl of 1 to 6 carbon atoms, or straight chain of 1 to 6 carbon atoms are lower alkoxy of side chain; R 1 and R 2 are the same or different and each is hydrogen or a straight or branched chain lower alkyl having 1 to 6 carbon atoms; R 3 and R 4 are the same or different and each is hydrogen, a straight or branched chain lower alkyl having 1 to 6 carbon atoms, or a straight or branched lower alkoxy having 1 to 6 carbon atoms; R 5 is a straight or branched chain lower alkyl having 1 to 6 carbon atoms, phenyl, 2-, 3- or 4-pyridyl, phenyl substituted with straight or branched chain lower alkyl having 1 to 6 carbon atoms, 2-, 4-pyridyl; A and R 6 are the same or different and are hydrogen, hydroxyl, amino, straight or branched chain alkyl of 1 to 6 carbon atoms, straight or branched chain lower alkoxy of 1 to 6 carbon atoms, phenyl, 2-, -pyridyl, phenoxy, 2-, 3- or 4-pyridyloxy, or - (CH 2) p -A ' - (CH 2) q B' , and wherein p is from 0 to 5, q is 1, And A 'is a direct bond, oxygen or sulfur, B' is hydrogen, straight or branched chain alkyl of 1 to 6 carbon atoms, straight or branched chain lower alkoxy of 1 to 6 carbon atoms, phenyl, 2- or 3 - or 4-pyridyl, phenoxy, 2-, 3- or 4-pyridyloxy, carboxyl, carboalkoxy, carboxamido, mono or dialkylcarboxamido, amino or mono or dialkylamino . 화학식(ⅠA)의 화합물:A compound of formula (IA): 상기 식에서, Ar은 페닐, 2-, 3- 또는 4-피리딜, 2- 또는 3-티에닐, 2-, 4- 또는 5-피리미딜이고, 이들 각각은 임의로 할로겐, 하이드록시, 또는 탄소수 1 내지 6의 직쇄 또는 측쇄의 저급 알킬에 의해 단치환 또는 이치환되고; A, W, X, Y 및 T는 동일하거나 상이하고, 수소, 할로겐, 하이드록시, 탄소수 1 내지 6 직쇄 또는 측쇄의 저급 알킬, 또는 탄소수 1 내지 6의 직쇄 또는 측쇄의 저급 알콕시이고; R1 및 R2는 동일하거나 상이하고, 수소, 또는 탄소수 1 내지 6의 직쇄 또는 측쇄의 저급 알킬이고; R3 및 R4는 동일하거나 상이하고, 수소 탄소수 1 내지 6의 직쇄 또는 측쇄의 저급 알킬, 또는 탄소수 1 내지 6의 직쇄 또는 측쇄의 저급 알콕시이고; R9는 수소, 탄소수 1 내지 6의 직쇄 또는 측쇄의 저급 알킬, 또는 페닐이다.Wherein Ar is phenyl, 2-, 3- or 4-pyridyl, 2- or 3-thienyl, 2-, 4- or 5-pyrimidyl, each of which is optionally substituted with halogen, ≪ / RTI > to 6, straight or branched chain lower alkyl; A, W, X, Y and T are the same or different and are hydrogen, halogen, hydroxy, lower alkyl of 1 to 6 carbon atoms straight or branched, or straight or branched chain lower alkoxy of 1 to 6 carbon atoms; R1 and R2 are the same or different and are hydrogen or a straight or branched chain lower alkyl having 1 to 6 carbon atoms; R3 and R4 are the same or different and are a straight chain or branched chain lower alkyl having 1 to 6 hydrogen atoms or a straight chain or branched lower alkoxy having 1 to 6 carbon atoms; R 9 is hydrogen, straight or branched chain lower alkyl of 1 to 6 carbon atoms, or phenyl. 제2항에 있어서, A가 저급 알콕시인 화합물.3. A compound according to claim 2, wherein A is lower alkoxy. 제1항에 있어서, 1-페닐-1-(4-페닐피페라진-1-일)-사이클로헥산인 화합물.2. The compound according to claim 1, which is 1-phenyl-1- (4-phenylpiperazin-1-yl) -cyclohexane. 제1항에 있어서, 1-(3-메톡시페닐)-1-(4-페닐피페라진-1-일)-사이클로헥산인 화합물.The compound according to claim 1, which is 1- (3-methoxyphenyl) -1- (4-phenylpiperazin-1-yl) -cyclohexane. 제1항에 있어서, 1-(3-메톡시페닐)-1-[4-(2-피리미디닐)-피페라진-1-일]-사이클로헥산인 화합물.The compound according to claim 1, which is 1- (3-methoxyphenyl) -1- [4- (2-pyrimidinyl) -piperazin-1-yl] -cyclohexane. 제1항에 있어서, 1-(3-메톡시페닐)-1-[4-(2-피리미디닐)-피페라진-1-일]-사이클로헥산인 화합물.The compound according to claim 1, which is 1- (3-methoxyphenyl) -1- [4- (2-pyrimidinyl) -piperazin-1-yl] -cyclohexane. 제1항에 있어서, 1-(3-메톡시페닐)-1-[4-(2-플루오로페닐)-피페라진-1-일]-사이클로헥산인 화합물.The compound according to claim 1, which is 1- (3-methoxyphenyl) -1- [4- (2-fluorophenyl) -piperazin-1-yl] -cyclohexane. 제1항에 있어서, 1-(3-메톡시페닐)-1-[4-(4-플루오로페닐)-피페라진-1-일]-사이클로헥산인 화합물.The compound according to claim 1, which is 1- (3-methoxyphenyl) -1- [4- (4-fluorophenyl) -piperazin-1-yl] -cyclohexane. 제1항에 있어서, 1-(3-하이드록시페닐)-1-(4-페닐피페라진-1-일]-사이클로헥산인 화합물.2. The compound according to claim 1, which is 1- (3-hydroxyphenyl) -1- (4-phenylpiperazin-1-yl) -cyclohexane. 제1항에 있어서, 1-(3,5-디메톡시페닐)-1-(4-페닐피페라진-1-일]-사이클로헥산인 화합물.The compound according to claim 1, which is 1- (3,5-dimethoxyphenyl) -1- (4-phenylpiperazin-1-yl) -cyclohexane. 제1항에 있어서, 1-(3-에톡시페닐)-1-(4-페닐피페라진-1-일)-사이클로헥산인 화합물.The compound according to claim 1, which is 1- (3-ethoxyphenyl) -1- (4-phenylpiperazin-1-yl) -cyclohexane. 제1항에 있어서, 1-(3-메톡시페닐)-1-(4-페닐피페라진-1-일)-4-페닐-사이클로헥산의 부분입체이성체 둘다인 화합물.The compound according to claim 1, which is both diastereomers of 1- (3-methoxyphenyl) -1- (4-phenylpiperazin-1-yl) -4-phenyl-cyclohexane. 제1항에 있어서, 1-(3-n-부톡시페닐)-1-(4-페닐피페라진-1-일)-사이클로헥산인 화합물.The compound according to claim 1, which is 1- (3-n-butoxyphenyl) -1- (4-phenylpiperazin-1-yl) -cyclohexane. 제1항에 있어서, 1-(3-메톡시페닐)-1-(4-페닐피페라진-1-일)-4-메틸-사이클로헥산의 부분입체이성체 둘다인 화합물.4. The compound according to claim 1 which is both diastereomers of 1- (3-methoxyphenyl) -1- (4-phenylpiperazin-1-yl) -4-methyl-cyclohexane. 제1항에 있어서, 1-(4-메톡시페닐)-1-(4-페닐피페라진-1-일)-사이클록헥산인 화합물.The compound according to claim 1, which is 1- (4-methoxyphenyl) -1- (4-phenylpiperazin-1-yl) -cyclohexane. 제1항에 있어서, 1-(2-메톡시페닐)-1-(4-페닐피페라진-1-일)-사이클록헥산인 화합물.The compound according to claim 1, which is 1- (2-methoxyphenyl) -1- (4-phenylpiperazin-1-yl) -cyclohexane. 제1항에 있어서, 1-(3,4-메텐디옥시페닐)-1-(4-페닐피페라진-1-일)-사이클록헥산인 화합물.The compound according to claim 1, which is 1- (3,4-methylenedioxyphenyl) -1- (4-phenylpiperazin-1-yl) -cyclohexane. 제1항에 있어서, 1-(3-에톡시페닐)-1-(4-페닐피페라진-1-일)-4-메틸-사이클록헥산의 부분입체이성체 둘다인 화합물.The compound according to claim 1, which is both diastereomers of 1- (3-ethoxyphenyl) -1- (4-phenylpiperazin-1-yl) -4-methyl-cyclic hexane. 제1항에 있어서, 1-(3-에톡시페닐)-1-(4-페닐피페라진-1-일)-4-에틸-사이클록헥산의 부분입체이성체 둘다인 화합물.The compound according to claim 1, which is both diastereomers of 1- (3-ethoxyphenyl) -1- (4-phenylpiperazin-1-yl) -4-ethyl-cyclic hexane. 제1항에 있어서, 1-(3-이소프로폭시페닐)-1-(4-페닐피페라진-1-일)-4-메틸-사이클록헥산의 부분입체이성체 둘다인 화합물.The compound according to claim 1, which is both diastereomers of 1- (3-isopropoxyphenyl) -1- (4-phenylpiperazin-1-yl) -4-methyl-cyclohexane. 제1항에 있어서, 1-(3-메톡시페닐)-1-(4-페닐피페라진-1-일)-3-메틸-사이클록헥산의 부분입체이성체 둘다인 화합물.The compound according to claim 1, which is both diastereomers of 1- (3-methoxyphenyl) -1- (4-phenylpiperazin-1-yl) -3-methylcyclohexane. 제1항에 있어서, 1-(3-벤질옥시페닐)-1-(4-페닐피페라진-1-일)-사이클록헥산 디하이드로클로라이드인 화합물.The compound according to claim 1, which is 1- (3-benzyloxyphenyl) -1- (4-phenylpiperazin-1-yl) -cyclohexane dihydrochloride. 제1항에 있어서, 4-(3-에톡시페닐)-4-(4-페닐피페라진-1-일)-테트라하이드로피란인 화합물.The compound according to claim 1, which is 4- (3-ethoxyphenyl) -4- (4-phenylpiperazin-1-yl) -tetrahydropyran. 제1항에 있어서, 4-(3-에톡시페닐)-4-(4-페닐피페라진-1-일)-테라하이드로티오피란인 화합물.The compound according to claim 1, which is 4- (3-ethoxyphenyl) -4- (4-phenylpiperazin-1-yl) -tetrahydrothiopyran. 제1항에 있어서, 1-(3-메톡시메톡시페닐)-1-(4-페닐피페라진-1-일)-4-메틸-사이클록헥산의 부분입체 이상체 둘다인 화합물.The compound according to claim 1, which is both a diastereomer of 1- (3-methoxymethoxyphenyl) -1- (4-phenylpiperazin-1-yl) -4-methylcyclohexane. 제1항에 있어서, 1-(3-에톡시메톡시페닐)-1-(4-페닐피페라진-1-일)-4-메틸-사이클록헥산의 부분입체이성체 둘다인 화합물.The compound according to claim 1, which is both diastereomers of 1- (3-ethoxymethoxyphenyl) -1- (4-phenylpiperazin-1-yl) -4-methyl-cyclic hexane. 제1항에 있어서, 1-(3-에톡시페닐)-1-(4-페닐피페라진-1-일)-4-메톡시-사이클록헥산의 부분입체이성체 둘다인 화합물.The compound of claim 1, which is both diastereomers of 1- (3-ethoxyphenyl) -1- (4-phenylpiperazin-1-yl) -4-methoxy-cyclic hexane. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: It is disclosed by the contents of the first application.
KR1019970702989A 1994-11-07 1995-11-07 Substituted benzylamine derivatives; A new class of neuropeptide Y1 specific ligands (CERTAIN SUBSTITUTED BENZYLAMINE DERIVATIVES; A NEW CLASS OF NEUROPEPTIDE Y1 SPECIFIC LIGANDS) KR970707101A (en)

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