KR960705808A - Piperidines, pyrrolidines and hexahydro-1 H-azepines promote release of growth hormone - Google Patents

Piperidines, pyrrolidines and hexahydro-1 H-azepines promote release of growth hormone

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KR960705808A
KR960705808A KR1019960702427A KR19960702427A KR960705808A KR 960705808 A KR960705808 A KR 960705808A KR 1019960702427 A KR1019960702427 A KR 1019960702427A KR 19960702427 A KR19960702427 A KR 19960702427A KR 960705808 A KR960705808 A KR 960705808A
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alkyl
aryl
hydrogen
substituted
cycloalkyl
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제이. 모리엘로 그레고리
에이. 파쳇트 아써
뤼 양
멩 에이치. 첸
나르군드 라비
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조셉 에프. 디프리마
머크 앤드 캄파니, 인코포레이티드
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Priority claimed from US08/323,998 external-priority patent/US5492920A/en
Priority claimed from US08/323,988 external-priority patent/US5492916A/en
Priority claimed from US08/323,994 external-priority patent/US5494919A/en
Application filed by 조셉 에프. 디프리마, 머크 앤드 캄파니, 인코포레이티드 filed Critical 조셉 에프. 디프리마
Publication of KR960705808A publication Critical patent/KR960705808A/en

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    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
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    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
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Abstract

본 발명은 다음 일반식(I)의 특정 피페리딘, 피롤리딘 및 헥사하이드로-1H-아제핀 화합물에 관한 것이다.The present invention relates to certain piperidine, pyrrolidine and hexahydro-1H-azepine compounds of the general formula (I).

상기식에서, R1, R3, R4, R5, A, W, X, Y 및 n 은 본원에서 정의한 바와 같다. 이들 화합물은 사람 및 동물의 체내에서 성장 호르몬의 방출을 촉진하다, 이러한 특성은 식용 동물의 성장을 촉진시키는데 이용되어 식용 육류 제품의 생산을 보다 효율화할 수 있고, 사람의 경우 성장 호르몬 결핍 아동의 작은 키와 같은 성장 호르몬 분비의 결핍에 의해 특징지워지는 생리학적 또는 의학적 증상을 치료하고 성장 호르몬의 동화작용효과에 의해 개선되는 의학적 증상을 치료할 수 있다. 활성 성분으로서 이러한 화합물을 함유하는 성장 호르몬 방출 조성물이 또한 기술되어 있다.Wherein R 1 , R 3 , R 4 , R 5 , A, W, X, Y and n are as defined herein. These compounds promote the release of growth hormone in the body of humans and animals. These properties can be used to promote the growth of edible animals to make the production of edible meat products more efficient, and in humans small children of growth hormone deficient children. It is possible to treat physiological or medical symptoms characterized by a deficiency of growth hormone secretion such as height and to treat medical symptoms ameliorated by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as active ingredients are also described.

Description

성장 호르몬의 방출을 촉진시키는 피페리딘, 피롤리딘 및 헥사하이드로-1H-아제핀(Piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone)Piperidines, pyrrolidines and hexahydro-1 H-azepines promote release of growth hormone

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

Claims (30)

다음 일반식(I)의 화합물 및 이의 약제학적으로 허용되는 염 및 개별적인 부분입체이성체.The compounds of formula (I) and their pharmaceutically acceptable salts and individual diastereomers. 상기식에서, R1은 C1-C10알킬, 아릴, 아릴( C1-C6알킬), (C3-C7사이클로알킬)( C1-C6알킬)-, ( C1-C5알킬)-K-( C1-C5알킬)-, 아릴( C0-C5알킬)-K-( C1-C5알킬)-, 및 (C3-C7사이클로알킬)( C0-C5알킬)-K-( C1-C5알킬)-로 이루어진 그룹 중에서 선택되며, 여기서 K은 O, S(O)m, N(R2)C(O), C(O)N(R2), OC(O), C(O)O, -CR2=CR2-, 또는 -C≡C- 이고, 아릴은 페닐, 나프틸, 인돌릴, 아자인돌, 피리딜, 벤조티에닐, 벤조푸라닐, 티아졸릴 및 벤즈이미다졸릴 중에서 선택되고, R2및 알킬은 1 내지 9개의 할로겐, S(O)mR2a1 내지 3개의 OR2a또는 C(O)OR2a에 의해 추가로 치환될 수 있고, 아릴은 1 내지 3개의 C1-C6알킬, 1 내지 3개의 할로겐, 1 내지 2개의 OR2, 메틸렌디옥시, -S(O)mR2, 1 내지 2개의 -CF3, -OCF3, 니트로, -N(R2)C(O)(R2), -C(O)OR2, -C(O)N(R2)(R2), -1H-테트라졸-5-일, -SO2N(R2)(R2), -N(R2)SO2페닐, 또는 -N(R2)SO2R2에 의해 추가로 치환될 수 있고, R2는 수소, C1-C6알킬 및 C3-C7사이클로알킬 중에서 선택되고, 2개의 C1-C6알킬 그룹이 한 원자에 존재하는 경우, 이들은 함께 결합하여 산소, 황 또는 NR3a를 포함할 수 있는 C3-C8사이클릭 환을 형성할 수도 있고, R2a는 수소, 또는 하이드록실에 의해 치환될 수 있는 C1-C6알킬이고, R3는 수소, -(CH2)r페닐, -(CH2)r나프틸, -C1-C10알킬, -C3-C7사이클로알킬 중에서 선택되고, 여기서 페닐, 나프틸 및 C3-C7사이클로알킬 환은 C1-C6알킬, 할로겐, -OR2, -NHSO2CF3, -(CH2)rOR6, -(CH2)rN(R2)(R6), -(CH2)r(R6), -(CH2)rC(O)OR2, -(CH2)rC(O)OR6, -(CH2)rOC(O)R2, -(CH2)rOC(O)R6, -(CH2)rC(O)OR2, -(CH2)rC(O)R6, -(CH2)rC(O)N(R2)(R2), -(CH2)rC(O)N(R2)(R6), -(CH2)rN(R2)C(O)R2, -(CH2)rN(R2)C(O)R6, -(CH2)rN(R6)C(O)R2, -(CH2)rN(R6)C(O)R6, -(CH2)rN(R2)C(O)OR2, -(CH2)rN(R2)C(O)OR6, -(CH2)rN(R6)C(O)OR2, -(CH2)rN(R6)C(O)OR6, -(CH2)rN(R2)C(O)N(R2)(R6), -(CH2)rN(R2)C(O)N(R2)(R2), -(CH2)rN(R6)C(O)N(R2)(R6), -(CH2)rN(R2)SO2R6, -(CH2)rN(R2)SO2R2, -(CH2)rN(R6)SO2R2, -(CH2)rN(R6)SO2R6, -(CH2)rOC(O)N(R2)(R6), -(CH2)rOC(O)N(R2)(R2), -(CH2)rSO2N(R2)(R6), -(CH2)rSO2N(R2)(R2), -(CH2)rSO2NHC(O)R6, -(CH2)rSO2NHC(O)R2, -(CH2)rSO2NHC(O)OR6, -(CH2)rC(O)NHC(O)NR2, -(CH2)rC(O)NHC(O)NR6, -(CH2)rC(O)NHC(O)R2, -(CH2)rCONHC(O)R6, -(CH2)rCONHSO2R6, -(CH2)rCONHSO2R2, -(CH2)rCONHSO2N(R2)R2), -(CH2)rCONHSO2N(R2)R6), -(CH2)rN(R2)SO2N(R2)R6), -(CH2)rN(R6)SO2N(R2)R6), -(CH2)rS(O)mR6, 및 -(CH2)rS(O)mR2로 이루어진 그룹 중에서 선택된 1 내지 3개의 치환체에 의해 치환될 수 있고, R3a는 수소, 또는 하이드록실에 의해 치환될 수 있는 C1-C6알킬이고, W는 수소, -CN, -C(O)OR8, -C(O)OR2, -C(O)O(CH2)1아릴, -C(O)N(R2)(R2); -C(O)N(R2)(R8). -C(O)N(R2)(CH2)1아릴, -CH2N(R2)C(O)R8)-CH2N(R2)C(O)(CH2)1아릴, -(CH)2rOR2, -CH(OH)R2, -CH(OH)(CH2)1아릴, -C(O)R2, -C(O)(CH2)1아릴, 1H-테트라졸-5-일, 5-아미노-1,2,4-옥사디아졸-3-일, 및 5-메틸-1,2,4-옥사디아졸-3-일로 이루어진 그룹 중에서 선택되고, 여기서 R8은 수소, C1-C6알킬, 또는 OR2, C(O)OR2, CON(R2)(R2), N(R2)C(O)R2, N(R2)C(O)H(R2)(R2)에 치환된 C1-C6알킬이고, 아릴은 페닐, 피리딜, 또는 1H-테트라졸-5-일이고, X는 수소, -C≡N, -(CH2)qN(R2)C(O)R2, -(CH2)qN(R2)C(O)(CH2)t아릴, -(CH2)qN(R2)SO2(CH2)t아릴, -(CH2)qN(R2)SO2R2, -(CH2)qN(R2)C(O)N(R2)(CH2)t아릴, -(CH2)qN(R2)C(O)N(R2)(R2), -(CH2)qC(O)N(R2)(R2), -(CH2)qC(O)N(R2)(CH2)t아릴, -(CH2)qC(O)OR2, -(CH2)qC(O)O(CH2)t아릴, -(CH2)qOR2, -(CH2)qOC(O)OR2, -(CH2)qOC(O)(CH2)t아릴, -(CH2)qOC(O)N(R2)(CH2)t아릴, -(CH2)qOC(O)N(R2)(R2), -(CH2)qC(O)R2, -(CH2)qC(O)(CH2)t아릴, -(CH2)qN(R2)C(O)OR2, -(CH2)qN(R2)SO2N(R2)(R2), -(CH2)qS(O)mR2, 및 -(CH2)qS(O)m(CH2)t아릴로 이루어진 그룹 중에서 선택되고, 여기서 R2, (CH2)q및 (CH)t그룹은 1 내지 2개의 C1-C4알킬, 하이드록실, C1-C4저급 알콕시, 카복실, CONH2, S(O)mCH3, 카복실레이트 C1-C4알킬 에스테르, 또는 1H-테트라졸-5-일에 의해 치환될 수도 있고, 아릴은 1 내지 3개의 할로겐, 1 내지 3개의 -OR2, -CON(R2)(R2), -C(O)OR2, 1 내지 3개의 C1-C4알킬, -S(O)mR2또는 1H-테트라졸-5-일에 의해 치환될 수도 있는, 페닐, 나프틸, 피리딜, 티아졸릴 또는 1H-테트라졸-5-일 그룹이고, Y는 수소, C1-C10알킬, -(CH2)t아릴, (CH2)q(C3-C7사이클로알킬), -(CH2)q-K-(C1-C6알킬), -(CH2)q-K-(CH2)t아릴, -(CH2)q-K-(CH2)t(O,NR2또는 S 함유 C3-C7사이클로알킬), 및 -(CH2)q-K-(CH2)t(C3-C7사이클로알킬)로 이루어진 그룹 중에서 선택되고, 여기서 K는 O, S(O)m, C(O)NR2, CH=CH, C≡C, N(R2)C(O), C(O)NR2, C(O)O, 또는 OC(O)이고, 알킬, R2, (CH2)q및 (CH2)t그룹은 C1-C4알킬, 하이드록실, C1-C4저급 알콕시, 카복실, CONH2,또는 카복실레이트 C1-C4알킬 에스테르에 의해 치환될 수도 있고, 아릴은 1 내지 3개의 할로겐, 1 내지 3개의 -OR2, -C(O)OR2, -C(O)N(R2)(R2), 니트로, 시아노, 벤질, 1 내지 3개의 C1-C4알킬, S(O)mR2또는 1H-테트라졸-5-일에 의해 치환될 수 있는, 페닐, 나프틸, 피리딜, 1H-테트라졸-5-일, 티아졸릴, 이미다졸릴, 인돌릴, 피리미디닐, 티아디아졸릴, 피라졸릴, 옥사졸릴, 이속사졸릴, 티오펜일, 퀴놀리닐, 피라지닐 또는 이소티아졸릴이고, 단 R3, W, X 및 Y 중 적어도 하나가 수소가 아니고, R4및 R5는 독립적으로 수소, C1-C6알킬, 또는 1 내지 5개의 할로, 1 내지 3개의 하이드록시, 1 내지 3개의 C1-C10알카노일옥시, 1 내지 3개의 C1-C6알콕시, 페닐, 페녹시, 2-푸릴, C1-C6알콕시카보닐 또는 S(O)m(C1-C6)알킬에 의해 치환된 C1-C6알킬이거나, R4및 R5는 함께 결합하여 -C(H2)dLa(CH2)e-(여기서, La는 C(R2)2, 0, S(O)m 또는 N(R2)이고, d 및 e는 독립적으로 1 내지 3이고, R2는 상술한 바와 같다)를 형성하고, A는Wherein R 1 is C 1 -C 10 alkyl, aryl, aryl (C 1 -C 6 alkyl), (C 3 -C 7 cycloalkyl) (C 1 -C 6 alkyl)-, (C 1 -C 5 Alkyl) -K- (C 1 -C 5 alkyl)-, aryl (C 0 -C 5 alkyl) -K- (C 1 -C 5 alkyl)-, and (C 3 -C 7 cycloalkyl) (C 0 -C 5 alkyl) -K- (C 1 -C 5 alkyl)-, wherein K is O, S (O) m, N (R 2 ) C (O), C (O) N (R 2 ), OC (O), C (O) O, -CR 2 = CR 2- , or -C≡C-, where aryl is phenyl, naphthyl, indolyl, azaindole, pyridyl, benzothier Alkyl, benzofuranyl, thiazolyl and benzimidazolyl, and R 2 and alkyl are added by 1 to 9 halogens, S (O) mR 2a 1 to 3 OR 2a or C (O) OR 2a And aryl is 1 to 3 C 1 -C 6 alkyl, 1 to 3 halogen, 1 to 2 OR 2 , methylenedioxy, -S (O) mR 2 , 1 to 2 -CF 3 , -OCF 3 , nitro, -N (R 2 ) C (O) (R 2 ), -C (O) OR 2 , -C (O) N (R 2 ) (R 2 ), -1H-tetra Sol-5-yl, -SO 2 N (R 2 ) (R 2 ), —N (R 2 ) SO 2 phenyl, or —N (R 2 ) SO 2 R 2 , wherein R 2 is hydrogen, C 1 -C 6 alkyl and C When selected from 3 -C 7 cycloalkyl and two C 1 -C 6 alkyl groups are present at one atom, they can be bonded together to form a C 3 -C 8 cyclic ring which may comprise oxygen, sulfur or NR 3a May be formed, R 2a is hydrogen, or C 1 -C 6 alkyl which may be substituted by hydroxyl, and R 3 is hydrogen, — (CH 2 ) rphenyl, — (CH 2 ) rnaphthyl, -C 1 -C 10 alkyl, -C 3 -C 7 cycloalkyl, wherein the phenyl, naphthyl and C 3 -C 7 cycloalkyl rings are C 1 -C 6 alkyl, halogen, -OR 2 , -NHSO 2 CF 3 ,-(CH 2 ) r OR 6 ,-(CH 2 ) r N (R 2 ) (R 6 ),-(CH 2 ) r (R 6 ),-(CH 2 ) r C (O) OR 2 ,-(CH 2 ) r C (O) OR 6 ,-(CH 2 ) r OC (O) R 2 ,-(CH 2 ) r OC (O) R 6 ,-(CH 2 ) r C (O ) OR 2 ,-(CH 2 ) r C (O) R 6 ,-(CH 2 ) r C (O) N (R 2 ) (R 2 ),-(CH 2 ) r C (O) N (R 2 ) (R 6 ),-(CH 2 ) r N (R 2 ) C (O) R 2 ,-(CH 2 ) r N (R 2 ) C (O) R 6 ,-(CH 2 ) r N (R 6 ) C (O) R 2 ,-(CH 2 ) r N (R 6 ) C (O) R 6 ,-(CH 2 ) r N (R 2 ) C (O) OR 2 ,-(CH 2 ) r N (R 2 ) C (O) OR 6 ,-(CH 2 ) r N (R 6 ) C (O) OR 2 ,-(CH 2 ) r N (R 6 ) C (O) OR 6 ,-(CH 2 ) r N (R 2 ) C (O) N ( R 2 ) (R 6 ),-(CH 2 ) r N (R 2 ) C (O) N (R 2 ) (R 2 ),-(CH 2 ) r N (R 6 ) C (O) N ( R 2 ) (R 6 ),-(CH 2 ) r N (R 2 ) SO 2 R 6 ,-(CH 2 ) r N (R 2 ) SO 2 R 2 ,-(CH 2 ) r N (R 6 ) SO 2 R 2 ,-(CH 2 ) r N (R 6 ) SO 2 R 6 ,-(CH 2 ) r OC (O) N (R 2 ) (R 6 ),-(CH 2 ) r OC ( O) N (R 2 ) (R 2 ),-(CH 2 ) r SO 2 N (R 2 ) (R 6 ),-(CH 2 ) r SO 2 N (R 2 ) (R 2 ),-( CH 2 ) r SO 2 NHC (O) R 6 ,-(CH 2 ) r SO 2 NHC (O) R 2 ,-(CH 2 ) r SO 2 NHC (O) OR 6 ,-(CH 2 ) r C (O) NHC (O) NR 2 ,-(CH 2 ) r C (O) NHC (O) NR 6 ,-(CH 2 ) r C (O) NHC (O) R 2 ,-(CH 2 ) r CONHC (O) R 6 ,-(CH 2 ) r CONHSO 2 R 6 ,-(CH 2 ) r CONHSO 2 R 2 ,-(CH 2 ) r CONHSO 2 N (R 2 ) R 2 ),-(CH 2 ) r CONHSO 2 N (R 2 ) R 6 ),-(CH 2 ) r N (R 2 ) SO 2 N (R 2 ) R 6 ),-(CH 2 ) r N (R 6 ) SO 2 N ( r 2) r 6), - (CH 2) r S (O) m r 6, and - (CH 2) r S ( O) m r 2 Can be optionally substituted with one to three substituents selected from the group consisting of, R 3a is a C 1 -C 6 alkyl which may be substituted by hydrogen, or hydroxyl, W is hydrogen, -CN, -C (O) OR 8 , -C (O) OR 2 , -C (O) O (CH 2 ) 1 aryl, -C (O) N (R 2 ) (R 2 ); -C (O) N (R 2 ) (R 8 ). -C (O) N (R 2 ) (CH 2 ) 1 aryl, -CH 2 N (R 2 ) C (O) R 8 ) -CH 2 N (R 2 ) C (O) (CH 2 ) 1 aryl ,-(CH) 2r OR 2 , -CH (OH) R 2 , -CH (OH) (CH 2 ) 1 aryl, -C (O) R 2 , -C (O) (CH 2 ) 1 aryl, 1H -Tetrazol-5-yl, 5-amino-1,2,4-oxadiazol-3-yl, and 5-methyl-1,2,4-oxadiazol-3-yl, Wherein R 8 is hydrogen, C 1 -C 6 alkyl, or OR 2 , C (O) OR 2 , CON (R 2 ) (R 2 ), N (R 2 ) C (O) R 2 , N (R 2 C 1 -C 6 alkyl substituted with) C (O) H (R 2 ) (R 2 ), aryl is phenyl, pyridyl, or 1H-tetrazol-5-yl, X is hydrogen, -C≡ N,-(CH 2 ) q N (R 2 ) C (O) R 2 ,-(CH 2 ) q N (R 2 ) C (O) (CH 2 ) t aryl,-(CH 2 ) q N ( R 2 ) SO 2 (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) SO 2 R 2 ,-(CH 2 ) q N (R 2 ) C (O) N (R 2 ) (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) C (O) N (R 2 ) (R 2 ),-(CH 2 ) q C (O) N (R 2 ) (R 2 ), -(CH 2 ) q C (O) N (R 2 ) (CH 2 ) t aryl,-(CH 2 ) q C (O) OR 2 ,-(CH 2 ) q C (O) O (CH 2 ) t aryl,-(CH 2 ) q OR 2 ,-(CH 2 ) q OC (O) OR 2 ,-(CH 2 ) q OC (O) (CH 2 ) t aryl,-(CH 2 ) q OC (O) N (R 2 ) (CH 2 ) t aryl,-(CH 2 ) q OC (O) N (R 2 ) (R 2 ),-(CH 2 ) q C (O) R 2 , -(CH 2 ) q C (O) (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) C (O) OR 2 ,-(CH 2 ) q N (R 2 ) SO 2 N ( R 2 ) (R 2 ), — (CH 2 ) q S (O) m R 2 , and — (CH 2 ) q S (O) m (CH 2 ) t aryl, wherein R 2 , (CH 2 ) q and (CH) t groups include 1 to 2 C 1 -C 4 alkyl, hydroxyl, C 1 -C 4 lower alkoxy, carboxyl, CONH 2 , S (O) m CH 3 , carboxylate May be substituted by C 1 -C 4 alkyl esters, or 1H-tetrazol-5-yl, aryl being 1 to 3 halogens, 1 to 3 —OR 2 , —CON (R 2 ) (R 2 ) , Phenyl, naphthyl, pyri, which may be substituted by -C (O) OR 2 , 1 to 3 C 1 -C 4 alkyl, -S (O) m R 2 or 1H-tetrazol-5-yl Dill, thiazolyl or 1H-tetrazol-5-yl group, Y is hydrogen, C 1 -C 10 alkyl,-(CH 2 ) t aryl, (CH 2 ) q (C 3 -C 7 cycloalkyl), -(CH 2 ) q -K- (C 1 -C 6 alkyl),-(CH 2 ) q -K- (CH 2 ) t aryl, - (CH 2) q -K- ( CH 2) t ( O, NR 2, or S-containing C 3 -C 7 cycloalkyl), and - (CH 2) q -K- ( CH 2) t ( C 3 -C 7 cycloalkyl), wherein K is O, S (O) m , C (O) NR 2 , CH = CH, C≡C, N (R 2 ) C (O) , C (O) NR 2 , C (O) O, or OC (O), alkyl, R 2 , (CH 2 ) q and (CH 2 ) t groups are C 1 -C 4 alkyl, hydroxyl, C May be substituted by 1- C 4 lower alkoxy, carboxyl, CONH 2 , or carboxylate C 1 -C 4 alkyl ester, aryl being 1 to 3 halogens, 1 to 3 —OR 2 , —C (O) OR 2 , -C (O) N (R 2 ) (R 2 ), nitro, cyano, benzyl, 1-3 C 1 -C 4 alkyl, S (O) m R 2 or 1H-tetrazol-5 Phenyl, naphthyl, pyridyl, 1H-tetrazol-5-yl, thiazolyl, imidazolyl, indolyl, pyrimidinyl, thiadiazolyl, pyrazolyl, oxazolyl, which may be substituted by- Isoxazolyl, thiophenyl, quinolinyl, pyrazinyl or isothiazolyl, provided At least one of R 3 , W, X and Y is not hydrogen, and R 4 and R 5 are independently hydrogen, C 1 -C 6 alkyl, or 1 to 5 halo, 1 to 3 hydroxy, 1 to 3 C 1 -C 10 alkanoyloxy, 1 to 3 C 1 -C 6 alkoxy, phenyl, phenoxy, 2-furyl, C 1 -C 6 alkoxycarbonyl or S (O) m (C 1 -C 6 Or C 1 -C 6 alkyl substituted by alkyl, or R 4 and R 5 are bonded together to form —C (H 2 ) dLa (CH 2 ) e—, wherein La is C (R 2 ) 2 , 0, S (O) m or N (R 2 ), d and e are independently 1 to 3, R 2 is as described above), and A is 여기서 x 및 y는 독립적으로 0, 1, 2 또는 3이고, Z는 N-R6a또는 0이고, 여기서 R6a는 수소 또는 C1-C6알킬이고, R6은 수소, C1-C6알킬 또는 (CH2)v아릴이고, 여기서 알킬 및 (CH2)v그룹은 1 내지 2개의 O(R2), S(O)mR2, 1H-테트라졸-5-일, C(O)OR2, C(O)N(R2)(R2), 또는 SO2N(R2)(R2), N(R2)C(O)N(R2)(R2)에 의해 치환될 수도 있고, 아릴은 C1-C6알킬, C3-C8사이클로알킬, 아미노 또는 하이드록실에 의해 치환될 수 있는, 페닐, 피리딜, 1H-테트라졸-5-일, 트리아졸릴, 이미다졸릴, 티아졸릴, 피라졸릴, 티아디아졸릴, 이미다졸론-1-일, 벤즈이미다졸-2-일, 트리아졸리논-일이고, R7및 R7a는 독립적으로 수소, C1-C6알킬, 트리플루오로메틸, 페닐, 또는 이미다졸릴, 페닐, 인돌릴, p-하이드록시페닐, OR2, S(O)nR2, C(O)O(C1-C6알킬), C3-C7사이클로알킬, N(R2)(R2), C(O)N(R2)(R2)에 의해 치환된 C1-C6알킬이거나, R7및 R7a는 독립적으로 R4및 R5그룹 중의 하나 또는 이들 둘다와 결합하여 R7또는 R7a그룹의 말단 질소와 알킬 부분사이에 탄소수 1 내지 5의 알킬렌 브릿지를 형성하거나, R7및 R7a는 서로 결합하여 C3-C7사이클로알킬을 형성할 수 있고, 1 은 0, 1 또는 2이고, m 은 0, 1 또는 2이고, n 은 1, 2 또는 3이고 q 는 0, 1, 2, 3 또는 4이고, r은 0, 1, 2 또는 3이고, t는 0, 1, 2 또는 3이고, v 는 0, 1 또는 2이다.Wherein x and y are independently 0, 1, 2 or 3, Z is NR 6a or 0, where R 6a is hydrogen or C 1 -C 6 alkyl and R 6 is hydrogen, C 1 -C 6 alkyl or (CH 2 ) v aryl, wherein the alkyl and (CH 2 ) v group is one to two O (R 2 ), S (O) m R 2 , 1H-tetrazol-5-yl, C (O) OR 2 , substituted by C (O) N (R 2 ) (R 2 ), or SO 2 N (R 2 ) (R 2 ), N (R 2 ) C (O) N (R 2 ) (R 2 ) Aryl may be substituted by C 1 -C 6 alkyl, C 3 -C 8 cycloalkyl, amino or hydroxyl, phenyl, pyridyl, 1H-tetrazol-5-yl, triazolyl, Dazolyl, thiazolyl, pyrazolyl, thiadiazolyl, imidazolon-1-yl, benzimidazol-2-yl, triazolinone-yl, R 7 and R 7a are independently hydrogen, C 1 -C 6 alkyl, trifluoromethyl, phenyl, or imidazolyl, phenyl, indolyl, p-hydroxyphenyl, OR 2 , S (O) n R 2 , C (O) O (C 1 -C 6 alkyl) , C 3 -C 7 cycloalkyl, N (R 2 ) (R 2 ), C Or C 7 -C 6 alkyl substituted by (O) N (R 2 ) (R 2 ), or R 7 and R 7a are independently linked to one or both of the R 4 and R 5 groups or R 7 or R An alkylene bridge having 1 to 5 carbon atoms may be formed between the terminal nitrogen of the 7a group and the alkyl moiety, or R 7 and R 7a may be bonded to each other to form C 3 -C 7 cycloalkyl, 1 is 0, 1 or 2, m is 0, 1 or 2, n is 1, 2 or 3, q is 0, 1, 2, 3 or 4, r is 0, 1, 2 or 3, t is 0, 1, 2 or 3 and v is 0, 1 or 2. 다음 일반식(AI)의 화합물, 및 이의 약제학적으로 허용되는 염 및 개별적인 부분입체이성체.The compounds of formula (AI) and pharmaceutically acceptable salts and individual diastereomers thereof. 상기식에서, R1은 C1-C10알킬, 아릴, 아릴( C1-C6알킬), (C3-C7사이클로알킬)( C1-C6알킬)-, ( C1-C5알킬)-K-( C1-C5알킬)-, 아릴( C0-C5알킬)-K-( C1-C5알킬)-, 및 (C3-C7사이클로알킬)( C0-C5알킬)-K-( C1-C5알킬)-로 이루어진 그룹 중에서 선택되며, 여기서 K은 O, S(O)m, N(R2)C(O), C(O)N(R2), OC(O), C(O)O, -CR2=CR2-, 또는 -C≡C- 이고, 아릴은 페닐, 나프틸, 인돌릴, 아자인돌, 피리딜, 벤조티에닐, 벤조푸라닐, 티아졸릴 및 벤즈이미다졸릴 중에서 선택되고, R2및 알킬은 1 내지 9개의 할로겐, S(O)mR2a1 내지 3개의 OR2a또는 C(O)OR2a에 의해 추가로 치환될 수 있고, 아릴은 1 내지 3개의 C1-C6알킬, 1 내지 3개의 할로겐, 1 내지 2개의 OR2, 메틸렌디옥시, -S(O)mR2, 1 내지 2개의 -CF3, -OCF3, 니트로, -N(R2)C(O)(R2), -C(O)OR2, -C(O)N(R2)(R2), -1H-테트라졸-5-일, -SO2N(R2)(R2), -N(R2)SO2페닐, 또는 -N(R2)SO2R2에 의해 추가로 치환될 수 있고, R2는 수소, C1-C6알킬 및 C3-C7사이클로알킬 중에서 선택되고, 2개의 C1-C6알킬 그룹이 한 원자에 존재하는 경우, 이들은 함께 결합하여 산소, 황 또는 NR3a를 포함할 수 있는 C3-C8사이클릭 환을 형성할 수도 있고, R2a는 수소, 또는 하이드록실에 의해 치환될 수 있는 C1-C6알킬이고, R3은 수소, -(CH2)r페닐, -(CH2)r나프틸, -C1-C10알킬, -C3-C7사이클로알킬 중에서 선택되고, 여기서 페닐, 나프틸 및 C3-C7사이클로알킬 환은 C1-C6알킬, 할로겐, -OR2, -NHSO2CF3, -(CH2)rOR6, -(CH2)rN(R2)(R6), -(CH2)r(R6), -(CH2)rC(O)OR2, -(CH2)rC(O)OR6, -(CH2)rOC(O)R2, -(CH2)rOC(O)R6, -(CH2)rC(O)OR2, -(CH2)rC(O)R6, -(CH2)rC(O)N(R2)(R2), -(CH2)rC(O)N(R2)(R6), -(CH2)rN(R2)C(O)R2, -(CH2)rN(R2)C(O)R6, -(CH2)rN(R6)C(O)R2, -(CH2)rN(R6)C(O)R6, -(CH2)rN(R2)C(O)OR2, -(CH2)rCN(R2)(O)OR6, -(CH2)rN(R6)C(O)OR2, -(CH2)rN(R6)C(O)OR6, -(CH2)rN(R2)C(O)N(R2)(R2), -(CH2)rN(R6)C(O)N(R2)(R6), -(CH2)rN(R6)C(O)N(R2)(R6), -(CH2)rN(R2)SO2R6, (CH2)rN(R2)SO2R2, (CH2)rN(R6)SO2R2, -(CH2)rN(R6)SO2R6, -(CH2)rOC(O)N(R2)(R6), -(CH2)rOC(O)N(R2)(R2), -(CH2)rSO2N(R2)(R6), -(CH2)rSO2N(R2)(R2), -(CH2)rSO2NHC(O)R6, -(CH2)rSO2NHC(O)R2, -(CH2)rSO2NHC(O)OR6, -(CH2)rSO2NHC(O)OR2, -(CH2)rC(O)NHC(O)NR2, -(CH2)rC(O)NHC(O)NR6, -(CH2)rC(O)NHC(O)R2, -(CH2)rCONHC(O)R6, -(CH2)rCONHSO2R6, -(CH2)rCONHSO2R2, -(CH2)rCONHSO2N(R2)R2), -(CH2)rCONHSO2N(R2)R6), -(CH2)rN(R2)SO2N(R2)R6), -(CH2)rN(R6)SO2N(R2)R6), -(CH2)rS(O)mR6, 및 -(CH2)rS(O)mR2로 이루어진 그룹 중에서 선택된 1 내지 3개의 치환체에 의해 치환될 수 있고, R3a는 수소, 또는 하이드록실에 의해 치환될 수 있는 C1-C6알킬이고, W는 수소, -CN, -C(O)OR8, -C(O)OR2, -C(O)O(CH2)1아릴, -C(O)N(R2)(R2); -C(O)N(R2)(R8). -C(O)N(R2)(CH2)1아릴, -CH2N(R2)C(O)R8-CH2N(R2)C(O)(CH2)1아릴, -(CH)2rOR2, -CH(OH)R2, -CH(OH)(CH2)1아릴, -C(O)R2, -C(O)(CH2)1아릴, 1H-테트라졸-5-일, 5-아미노-1,2,4-옥사디아졸-3-일, 및 5-메틸-1,2,4-옥사디아졸-3-일로 이루어진 그룹 중에서 선택되고, 여기서 R8은 수소, C1-C6알킬, 또는 OR2, COOR2, C(O)N(R2)(R2), N(R2)C(O)R2, N(R2)C(O)N(R2)(R2)에 치환된 C1-C6알킬이고, 아릴은 페닐, 피리딜, 또는 1H-테트라졸-5-일이고, X는 수소, -C≡N, -(CH2)qN(R2)C(O)R2, -(CH2)qN(R2)C(O)(CH2)t아릴, -(CH2)qN(R2)SO2(CH2)t아릴, -(CH2)qN(R2)SO2R2, -(CH2)qN(R2)C(O)N(R2)(CH2)t아릴, -(CH2)qN(R2)C(O)N(R2)(R2), -(CH2)qC(O)N(R2)(R2), -(CH2)qC(O)N(R2)(CH2)t아릴, -(CH2)qC(O)OR2, -(CH2)qC(O)O(CH2)t아릴, -(CH2)qOR2, -(CH2)qOC(O)OR2, -(CH2)qOC(O)(CH2)t아릴, -(CH2)qOC(O)N(R2)(CH2)t아릴, -(CH2)qOC(O)N(R2)(R2), -(CH2)qC(O)R2, -(CH2)qC(O)(CH2)t아릴, -(CH2)qN(R2)C(O)OR2, -(CH2)qN(R2)SO2N(R2)(R2), -(CH2)qS(O)mR2, 및 -(CH2)qS(O)m(CH2)t아릴중에서 선택되고, 여기서 R2, (CH2)q및 (CH)t그룹은 1 내지 2개의 C1-C4알킬, 하이드록실, C1-C4저급 알콕시, 카복실, CONH2, S(O)mCH3, 카복실레이트 C1-C4알킬 에스테르, 또는 1H-테트라졸-5-일에 의해 치환될 수도 있고, 아릴은 1 내지 3개의 할로겐, 1 내지 3개의 -OR2, -CON(R2)(R2), -C(O)OR2, 1 내지 3개의 C1-C4알킬, S(O)mR2또는 1H-테트라졸-5-일에 의해 치환될 수도 있는, 페닐, 나프틸, 피리딜, 티아졸릴 또는 1H-테트라졸-5-일 그룹이고, Y는 수소, C1-C10알킬, -(CH2)t아릴, (CH2)q(C3-C7사이클로알킬), -(CH2)q-K-(C1-C8알킬), -(CH2)q-K-(CH2)t아릴, -(CH2)q-K-(CH2)t(O,NR2또는 S 함유 C3-C7사이클로알킬), 및 -(CH2)q-K-(CH2)t(C3-C7사이클로알킬)중에서 선택되고, 여기서 K는 O, S(O)m, C(O)NR2, CH=CH, C≡C, N(R2)C(O), C(O)NR2, C(O)O, 또는 OC(O)이고, 알킬, R2, (CH2)q및 (CH2)t그룹은 C1-C4알킬, 하이드록실, C1-C4저급 알콕시, 카복실, CONH2, 또는 카복실레이트 C1-C4알킬 에스테르에 의해 치환될 수도 있고, 아릴은 1 내지 3개의 할로겐, 1 내지 3개의 -OR2, -C(O)OR2, -C(O)N(R2)(R2), 니트로, 시아노, 벤질, 1 내지 3개의 C1-C4알킬, S(O)mR2또는 1H-테트라졸-5-일에 의해 치환될 수도 있는, 페닐, 나프틸, 피리딜, 1H-테트라졸-5-일, 티아졸릴, 이미다졸릴, 인돌릴, 피리미디닐, 티아디아졸릴, 피라졸릴, 옥사졸릴, 이속사졸릴, 티오펜일, 퀴놀리닐, 피라지닐 또는 이소티아졸릴이고, R4및 R5는 독립적으로 수소, C1-C6알킬, 또는 1 내지 5개의 할로, 1 내지 3개의 하이드록시, 1 내지 3개의 C1-C10알카노일옥시, 1 내지 3개의 C1-C6알콕시, 페닐, 페녹시, 2-푸릴, C1-C6알콕시카보닐 또는 S(O)m(C1-C6)알킬에 의해 치환된 C1-C6알킬이거나, R4및 R5는 함께 결합하여 -C(H2)dLa(CH2)e-(여기서, La는 C(R2)2, 0, S(O)m 또는 N(R2)이고, d 및 e는 독립적으로 1 내지 3이고, R2는 상술한 바와 같다)를 형성하고, A는Wherein R 1 is C 1 -C 10 alkyl, aryl, aryl (C 1 -C 6 alkyl), (C 3 -C 7 cycloalkyl) (C 1 -C 6 alkyl)-, (C 1 -C 5 Alkyl) -K- (C 1 -C 5 alkyl)-, aryl (C 0 -C 5 alkyl) -K- (C 1 -C 5 alkyl)-, and (C 3 -C 7 cycloalkyl) (C 0 -C 5 alkyl) -K- (C 1 -C 5 alkyl)-, wherein K is O, S (O) m, N (R 2 ) C (O), C (O) N (R 2 ), OC (O), C (O) O, -CR 2 = CR 2- , or -C≡C-, where aryl is phenyl, naphthyl, indolyl, azaindole, pyridyl, benzothier Alkyl, benzofuranyl, thiazolyl and benzimidazolyl, and R 2 and alkyl are added by 1 to 9 halogens, S (O) mR 2a 1 to 3 OR 2a or C (O) OR 2a And aryl is 1 to 3 C 1 -C 6 alkyl, 1 to 3 halogen, 1 to 2 OR 2 , methylenedioxy, -S (O) mR 2 , 1 to 2 -CF 3 , -OCF 3 , nitro, -N (R 2 ) C (O) (R 2 ), -C (O) OR 2 , -C (O) N (R 2 ) (R 2 ), -1H-tetra Sol-5-yl, -SO 2 N (R 2 ) (R 2 ), —N (R 2 ) SO 2 phenyl, or —N (R 2 ) SO 2 R 2 , wherein R 2 is hydrogen, C 1 -C 6 alkyl and C When selected from 3 -C 7 cycloalkyl and two C 1 -C 6 alkyl groups are present at one atom, they can be bonded together to form a C 3 -C 8 cyclic ring which may comprise oxygen, sulfur or NR 3a May be formed, R 2a is hydrogen, or C 1 -C 6 alkyl which may be substituted by hydroxyl, R 3 is hydrogen, — (CH 2 ) rphenyl, — (CH 2 ) rnaphthyl, -C 1 -C 10 alkyl, -C 3 -C 7 cycloalkyl, wherein the phenyl, naphthyl and C 3 -C 7 cycloalkyl rings are C 1 -C 6 alkyl, halogen, -OR 2 , -NHSO 2 CF 3 ,-(CH 2 ) r OR 6 ,-(CH 2 ) r N (R 2 ) (R 6 ),-(CH 2 ) r (R 6 ),-(CH 2 ) r C (O) OR 2 ,-(CH 2 ) r C (O) OR 6 ,-(CH 2 ) r OC (O) R 2 ,-(CH 2 ) r OC (O) R 6 ,-(CH 2 ) r C (O ) OR 2 ,-(CH 2 ) r C (O) R 6 ,-(CH 2 ) r C (O) N (R 2 ) (R 2 ),-(CH 2 ) r C (O) N (R 2 ) (R 6 ),-(CH 2 ) r N (R 2 ) C (O) R 2 ,-(CH 2 ) r N (R 2 ) C (O) R 6 ,-(CH 2 ) r N (R 6 ) C (O) R 2 ,-(CH 2 ) r N (R 6 ) C (O) R 6 ,-(CH 2 ) r N (R 2 ) C (O) OR 2 ,-(CH 2 ) r CN (R 2 ) (O) OR 6 ,-(CH 2 ) r N (R 6 ) C (O) OR 2 ,-(CH 2 ) r N (R 6 ) C (O) OR 6 ,-(CH 2 ) r N (R 2 ) C (O) N (R 2 ) (R 2 ),-(CH 2 ) r N (R 6 ) C (O) N (R 2 ) (R 6 ),-(CH 2 ) r N (R 6 ) C (O) N (R 2 ) (R 6 ),-(CH 2 ) r N (R 2 ) SO 2 R 6 , (CH 2 ) r N (R 2 ) SO 2 R 2 , (CH 2 ) r N (R 6 ) SO 2 R 2 ,-(CH 2 ) r N (R 6 ) SO 2 R 6 ,-(CH 2 ) r OC (O) N (R 2 ) (R 6 ),-(CH 2 ) r OC (O) N (R 2 ) (R 2 ),-(CH 2 ) r SO 2 N (R 2 ) (R 6 ),-(CH 2 ) r SO 2 N (R 2 ) (R 2 ),-(CH 2 ) r SO 2 NHC (O) R 6 ,-(CH 2 ) r SO 2 NHC (O) R 2 ,-(CH 2 ) r SO 2 NHC (O) OR 6 ,-(CH 2 ) r SO 2 NHC ( O) OR 2 ,-(CH 2 ) r C (O) NHC (O) NR 2 ,-(CH 2 ) r C (O) NHC (O) NR 6 ,-(CH 2 ) r C (O) NHC (O) R 2 ,-(CH 2 ) r CONHC (O) R 6 ,-(CH 2 ) r CONHSO 2 R 6 ,-(CH 2 ) r CONHSO 2 R 2 ,-(CH 2 ) r CONHSO 2 N (R 2 ) R 2 ),-(CH 2 ) r CONHSO 2 N (R 2 ) R 6 ),-(CH 2 ) r N (R 2 ) SO 2 N (R 2 ) R 6 ),-(CH 2) r N (R 6) SO 2 N (R 2) R 6), - (CH 2) r S (O) m R 6, - (CH 2) r S ( O) m R 2 may be substituted by one to three substituents selected from the group consisting of and, R 3a is C 1 -C 6 alkyl which may be substituted by a hydrogen or a hydroxyl W is hydrogen, -CN, -C (O) OR 8 , -C (O) OR 2 , -C (O) O (CH 2 ) 1 aryl, -C (O) N (R 2 ) (R 2 ); -C (O) N (R 2 ) (R 8 ). -C (O) N (R 2 ) (CH 2 ) 1 aryl, -CH 2 N (R 2 ) C (O) R 8 -CH 2 N (R 2 ) C (O) (CH 2 ) 1 aryl, -(CH) 2r OR 2 , -CH (OH) R 2 , -CH (OH) (CH 2 ) 1 aryl, -C (O) R 2 , -C (O) (CH 2 ) 1 aryl, 1H- Tetrazol-5-yl, 5-amino-1,2,4-oxadiazol-3-yl, and 5-methyl-1,2,4-oxadiazol-3-yl, wherein R 8 is hydrogen, C 1 -C 6 alkyl, or OR 2 , COOR 2 , C (O) N (R 2 ) (R 2 ), N (R 2 ) C (O) R 2 , N (R 2 ) C 1 -C 6 alkyl substituted with C (O) N (R 2 ) (R 2 ), aryl is phenyl, pyridyl, or 1H-tetrazol-5-yl, X is hydrogen, -C≡N ,-(CH 2 ) q N (R 2 ) C (O) R 2 ,-(CH 2 ) q N (R 2 ) C (O) (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) SO 2 (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) SO 2 R 2 ,-(CH 2 ) q N (R 2 ) C (O) N (R 2 ) (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) C (O) N (R 2 ) (R 2 ),-(CH 2 ) q C (O) N (R 2 ) (R 2 ),- (CH 2 ) q C (O) N (R 2 ) (CH 2 ) t aryl,-(CH 2 ) q C (O) OR 2 ,-(CH 2 ) q C (O) O (CH 2 ) t Aryl,-(CH 2 ) q OR 2 ,-(CH 2 ) q OC (O) OR 2 ,-(CH 2 ) q OC (O) (CH 2 ) t aryl,-(CH 2 ) q OC (O) N (R 2 ) (CH 2 ) t aryl,-(CH 2 ) q OC (O) N (R 2 ) (R 2 ),-(CH 2 ) q C (O) R 2 ,- (CH 2 ) q C (O) (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) C (O) OR 2 ,-(CH 2 ) q N (R 2 ) SO 2 N (R 2 ) (R 2 ), — (CH 2 ) q S (O) m R 2 , and — (CH 2 ) q S (O) m (CH 2 ) t aryl, wherein R 2 , (CH 2 ) q and (CH) t groups are 1 to 2 C 1 -C 4 alkyl, hydroxyl, C 1 -C 4 lower alkoxy, carboxyl, CONH 2 , S (O) m CH 3 , carboxylate C 1 -C 4 alkyl ester, or 1H-tetrazol-5-yl, wherein aryl is 1 to 3 halogens, 1 to 3 -OR 2 , -CON (R 2 ) (R 2 ), -C ( O) OR 2 , phenyl, naphthyl, pyridyl, thiazolyl, which may be substituted by 1 to 3 C 1 -C 4 alkyl, S (O) m R 2 or 1H-tetrazol-5-yl Is a 1H-tetrazol-5-yl group, Y is hydrogen, C 1 -C 10 alkyl, — (CH 2 ) t aryl, (CH 2 ) q (C 3 -C 7 cycloalkyl),-(CH 2 ) q -K- (C 1 -C 8 alkyl),-(CH 2 ) q -K- (CH 2 ) t aryl,-(CH 2 ) q -K- ( CH 2) t (O, NR 2 , or S-containing C 3 -C 7 cycloalkyl), and - is selected from (CH 2) q -K- (CH 2) t (C 3 -C 7 cycloalkyl), wherein K is O, S (O) m , C (O) NR 2 , CH = CH, C≡C, N (R 2 ) C (O), C (O) NR 2 , C (O) O, or OC (O) and alkyl, R 2 , (CH 2 ) q and (CH 2 ) t groups are C 1 -C 4 alkyl, hydroxyl, C 1 -C 4 lower alkoxy, carboxyl, CONH 2 , or carboxylate C May be substituted by 1- C 4 alkyl ester, aryl being 1 to 3 halogens, 1 to 3 —OR 2 , —C (O) OR 2 , —C (O) N (R 2 ) (R 2 ), Nitro, cyano, benzyl, phenyl, naphthyl, pyridyl, which may be substituted by 1 to 3 C 1 -C 4 alkyl, S (O) m R 2 or 1H-tetrazol-5-yl , 1H-tetrazol-5-yl, thiazolyl, imidazolyl, indolyl, pyrimidinyl, thiadiazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiophenyl, quinolinyl, pyrazinyl or iso Thiazolyl, R 4 and R 5 are independently hydrogen, C 1 -C 6 Alkyl, or 1 to 5 halo, 1 to 3 hydroxy, 1 to 3 C 1 -C 10 alkanoyloxy, 1 to 3 C 1 -C 6 alkoxy, phenyl, phenoxy, 2-furyl, C 1 -C 6 alkoxycarbonyl or S (O) m (C 1 -C 6), or a C 1 -C 6 alkyl optionally substituted by alkyl, R 4 and R 5 is -C (H 2) dLa in combination with ( CH 2 ) e-, wherein La is C (R 2 ) 2 , 0, S (O) m or N (R 2 ), d and e are independently 1 to 3, and R 2 is as described above ), A is 여기서 x 및 y는 독립적으로 0, 1, 2 또는 3이고, Z는 N-R6a또는 0이고, 여기서 R6a는 수소 또는 C1-C6알킬이고, R6은 수소, C1-C6알킬 또는 (CH2)v아릴이고, 여기서 알킬 및 (CH2)v그룹은 1 내지 2개의 O(R2), S(O)mR2, 1H-테트라졸-5-일, C(O)OR2, C(O)N(R2)(R2), 또는 SO2N(R2)(R2), N(R2)C(O)N(R2)(R2)에 의해 치환될 수도 있고, 아릴은 C1-C6알킬, C3-C8사이클로알킬, 아미노 또는 하이드록실에 의해 치환될 수 있는, 페닐, 피리딜, 1H-테트라졸-5-일, 트리아졸릴, 이미다졸릴, 티아졸릴, 피라졸릴, 티아디아졸릴, 이미다졸론-1-일, 벤즈이미다졸-2-일, 트리아졸리논-일이고, R7및 R7a는 독립적으로 수소, C1-C6알킬, 트리플루오로메틸, 페닐, 또는 이미다졸릴, 페닐, 인돌릴, p-하이드록시페닐, O(R2), S(O)nR2, C(O)O(C1-C6알킬), C3-C7사이클로알킬, N(R2)(R2), C(O)N(R2)(R2)에 의해 치환된 C1-C6알킬이거나, R7및 R7a는 독립적으로 R4및 R5그룹 중의 하나 또는 이들 둘다와 결합하여 R7또는 R7a그룹의 말단 질소와 알킬 부분 사이에 탄소수 1 내지 5의 알킬렌 브릿지를 형성하거나, R7및 R7a는 서로 결합하여 C3-C7사이클로알킬을 형성할 수 있고, 1 은 0, 1 또는 2이고, m 은 0, 1 또는 2이고, n 은 1, 2 또는 3이고 q 는 0, 1, 2, 3 또는 4이고, r은 0, 1, 2 또는 3이고, t는 0, 1, 2 또는 3이고, v 는 0, 1 또는 2이다.Wherein x and y are independently 0, 1, 2 or 3, Z is NR 6a or 0, where R 6a is hydrogen or C 1 -C 6 alkyl and R 6 is hydrogen, C 1 -C 6 alkyl or (CH 2 ) v aryl, wherein the alkyl and (CH 2 ) v group is one to two O (R 2 ), S (O) m R 2 , 1H-tetrazol-5-yl, C (O) OR 2 , substituted by C (O) N (R 2 ) (R 2 ), or SO 2 N (R 2 ) (R 2 ), N (R 2 ) C (O) N (R 2 ) (R 2 ) Aryl may be substituted by C 1 -C 6 alkyl, C 3 -C 8 cycloalkyl, amino or hydroxyl, phenyl, pyridyl, 1H-tetrazol-5-yl, triazolyl, Dazolyl, thiazolyl, pyrazolyl, thiadiazolyl, imidazolon-1-yl, benzimidazol-2-yl, triazolinone-yl, R 7 and R 7a are independently hydrogen, C 1 -C 6 alkyl, trifluoromethyl, phenyl, or imidazolyl, phenyl, indolyl, p-hydroxyphenyl, O (R 2 ), S (O) n R 2 , C (O) O (C 1 -C 6 alkyl), C 3 -C 7 cycloalkyl, N (R 2 ) (R 2 ), C 1 -C 6 alkyl substituted by C (O) N (R 2 ) (R 2 ), or R 7 and R 7a are independently R 7 or in combination with one or both of the R 4 and R 5 groups An alkylene bridge having 1 to 5 carbon atoms may be formed between the terminal nitrogen of the R 7a group and the alkyl moiety, or R 7 and R 7a may be bonded to each other to form a C 3 -C 7 cycloalkyl, 1 is 0, 1 Or 2, m is 0, 1 or 2, n is 1, 2 or 3, q is 0, 1, 2, 3 or 4, r is 0, 1, 2 or 3, t is 0, 1 , 2 or 3, and v is 0, 1 or 2. 제2항에 있어서, R1이 C1-C10알킬, 아릴( C1-C4알킬)-, C3-C6사이클로알킬( C1-C4알킬)-, ( C1-C4알킬)-K-( C1-C2알킬)-, 아릴( C0-C2알킬)-K-( C1-C2알킬)-, 및 (C3-C7사이클로알킬)( C0-C2알킬)-K-( C1-C2알킬)-로 이루어진 그룹 중에서 선택되고, 여기서 K는 O, S(O)m, OC(O), C(O)O 이고, 알킬그룹은 1 내지 7개의 할로겐, S(O)mR2, 1 내지 3개의 OR2a또는 C(O)OR2에 의해 추가로 치환될 수 있고, 아릴은 1 내지 2개의 C1-C4알킬, 1 내지 2개의 할로겐, 1 내지 2개의 OR2, S(O)mR2,또는 C(O)OR2에 의해 추가로 치환될 수 있는 페닐, 나프틸, 인돌릴, 피리딜, 벤조티에닐 또는 벤조푸라닐이고, R2가 수소, C1-C6알킬 또는 C3-C7사이클로알킬이고, 2개의 C1-C6알킬 그룹이 한 원자상에 존재하는 경우, 이들은 함께 결합하여 산소, 황 또는 NR3a를 함유할 수 있는 C4-C7사이클릭 환을 형성할 수도 있고, R3이 수소이거나, C1-C6알킬 그룹, -NHSO2CF3, -(CH2)r(1H-테트라졸-5-일), -(CH2)rC(O)OR2또는 -(CH2)rC(O)N(R2)(R6), 에 의해 오르토 위치에서 치환될 수 있는 페닐이고, R3a가 수소, 또는 C1-C4알킬이고, W가 -CN, -C(O)OR2, -C(O)N(R2)(R2), -C(O)N(R2)(CH2)1페닐, 1H-테트라졸-5-일, 또는 -(CH2)rOR2이고, X가 수소, -(CH2)q(CO)N(R2)(R6), 또는-(CH2)qC(O)OR2, 이고, Y가 수소, C1-C8알킬, -(CH2)t페닐, -(CH2)t피리딜, 또는 -(CH2)t티아졸릴이고, R4및 R5가 독립적으로 수소, C1-C6알킬, 또는 1 내지 5개의 할로, 1 내지 3개의 하이드록실, S(O)m(C1-C6알킬) 또는 페닐에 의해 치환된 C1-C6알킬이고, R6이 수소, 또는 C1-C6알킬이고, A가이고, 여기서 x는 0 또는 1이고, R7및 R7a가 독립적으로 수소, C1-C6알킬, 트리플루오로메틸, 페닐, 또는 이미다졸릴, 페닐, 인돌릴, p-하이드록시페닐, OR2, S(O)mR2, C(O)O(C1-C6알킬), C5-C7사이클로알킬, N(R2)(R2), C(O)N(R2)(R2)에 의해 치환된 C1-C6알킬이거나, R7및 R7a는 독립적으로 R4및 R5그룹 중의 하나에 결합하여 R7또는 R7a그룹의 말단 질소와 알킬 부분 사이에 알킬렌 브릿지를 형성하여 5원 또는 6원 환을 형성하거나, R7및 R7a가 서로 결합하여 C3사이클로알킬을 형성하고, 1 이 0 또는 1이고, n 은 2이고, m 이 0, 1 또는 2이고, r이 0, 1, 2 또는 3이고, q 가 0 또는 1이고, t가 0 또는 1인 화합물, 및 이의 약제학적으로 허용되는 염 및 개별적인 부분입체이성체.The compound of claim 2, wherein R 1 is C 1 -C 10 alkyl, aryl (C 1 -C 4 alkyl)-, C 3 -C 6 cycloalkyl (C 1 -C 4 alkyl)-, (C 1 -C 4 Alkyl) -K- (C 1 -C 2 alkyl)-, aryl (C 0 -C 2 alkyl) -K- (C 1 -C 2 alkyl)-, and (C 3 -C 7 cycloalkyl) (C 0 -C 2 alkyl) -K- (C 1 -C 2 alkyl)-, wherein K is O, S (O) m , OC (O), C (O) O, and the alkyl group is May be further substituted by 1 to 7 halogens, S (O) m R 2 , 1 to 3 OR 2a or C (O) OR 2 , with aryl being 1 to 2 C 1 -C 4 alkyl, 1 Phenyl, naphthyl, indolyl, pyridyl, benzothienyl, which may be further substituted by from 2 halogens, 1 or 2 OR 2 , S (O) m R 2 , or C (O) OR 2 or Benzofuranyl, R 2 is hydrogen, C 1 -C 6 alkyl or C 3 -C 7 cycloalkyl, and when two C 1 -C 6 alkyl groups are on one atom, they are bonded together to form oxygen, May contain sulfur or NR 3a May form a C 4 -C 7 cyclic ring and R 3 is hydrogen or a C 1 -C 6 alkyl group, -NHSO 2 CF 3 ,-(CH 2 ) r (1H-tetrazol-5-yl) ,-(CH 2 ) r C (O) OR 2 or-(CH 2 ) r C (O) N (R 2 ) (R 6 ), is phenyl which may be substituted at the ortho position by R 3a is hydrogen Or C 1 -C 4 alkyl, W is —CN, —C (O) OR 2 , —C (O) N (R 2 ) (R 2 ), —C (O) N (R 2 ) (CH 2 ) 1phenyl, 1H-tetrazol-5-yl, or-(CH 2 ) r OR 2 , X is hydrogen,-(CH 2 ) q (CO) N (R 2 ) (R 6 ), or- (CH 2 ) q C (O) OR 2 , wherein Y is hydrogen, C 1 -C 8 alkyl,-(CH 2 ) t phenyl,-(CH 2 ) t pyridyl, or-(CH 2 ) t thia Zolyl and R 4 and R 5 are independently hydrogen, C 1 -C 6 alkyl, or 1 to 5 halo, 1 to 3 hydroxyl, S (O) m (C 1 -C 6 alkyl) or phenyl Is C 1 -C 6 alkyl substituted by R 6 is hydrogen or C 1 -C 6 alkyl and A is Wherein x is 0 or 1, and R 7 and R 7a are independently hydrogen, C 1 -C 6 alkyl, trifluoromethyl, phenyl, or imidazolyl, phenyl, indolyl, p-hydroxyphenyl, OR 2 , S (O) m R 2 , C (O) O (C 1 -C 6 alkyl), C 5 -C 7 cycloalkyl, N (R 2 ) (R 2 ), C (O) N (R 2 ) C 1 -C 6 alkyl substituted by (R 2 ), or R 7 and R 7a are independently bound to one of the R 4 and R 5 groups, between the terminal nitrogen and the alkyl moiety of the R 7 or R 7a group An alkylene bridge is formed to form a 5 or 6 membered ring, or R 7 and R 7a are bonded to each other to form C 3 cycloalkyl, 1 is 0 or 1, n is 2, m is 0, 1 or 2, r is 0, 1, 2 or 3, q is 0 or 1, t is 0 or 1, and pharmaceutically acceptable salts and individual diastereomers thereof. 제2항에 있어서, 다음 일반식(AIb)의 화합물, 및 이의 약제학적으로 허용되는 염 및 개별적인 부분입체이성체.The compound of formula (AIb) according to claim 2, and pharmaceutically acceptable salts and individual diastereomers thereof. 상기 식에서, R1은 C1-C10알킬, 아릴(C1-C3알킬)-, 및 아릴(C0-C1알킬)-K-(C1-C2알킬)-로 이루어진 그룹중에서 선택되고, 여기서 K 는 0 또는 S(O)m이고, 아릴은 1 내지 2개의 C1-C4알킬, 1 내지 2개의 할로겐, 1 내지 2개의 OR2, S(O)mR2또는 C(O)OR2에 의해 치환될 수 있는, 페닐, 피리딜, 나프틸 또는 인돌릴이고, R2는 수소, C1-C6알킬, 또는 C3-C7사이클로알킬이고, 2개의 C1-C6알킬 그룹이 한 원자에 존재하는 경우, 이들은 함께 결합하여 산소, 황 또는 NR3a를 포함할 수 있는 C5-C7사이클릭 환을 형성할 수 있고, R3은 수소이거나, C1-C3알킬 그룹, (CH2)r(1H-테트라졸-5-일) 또는 (CH2)rC(O)OR2에 의해 오르토 위치에서 치환될 수 있는 페닐이고, R3a는 수소, 또는 C1-C4알킬이고, W는 -CN, -C(O)OR2, 또는 -C(O)N(R2)(R2)이고, X는 수소 또는 C(O)0R2이고, Y는 수소, 벤질, 피코일, 또는 티아졸릴메틸이고, R4및 R5는 독립적으로 수소, C1-C3알킬, 또는 1개 또는 2개의 하이드록실에 의해 치환된 C1-C3알킬이고, A는이고, 여기서 x는 0 또는 1이고, R7및 R7a는 독립적으로 수소 또는 C1-C4알킬이고, m 은 0, 1 또는 2이고, r은 0, 1 또는 2이다.Wherein R 1 is selected from the group consisting of C 1 -C 10 alkyl, aryl (C 1 -C 3 alkyl)-, and aryl (C 0 -C 1 alkyl) -K- (C 1 -C 2 alkyl)- Wherein K is 0 or S (O) m and aryl is 1 to 2 C 1 -C 4 alkyl, 1 to 2 halogen, 1 to 2 OR 2 , S (O) m R 2 or C (O) phenyl, pyridyl, naphthyl or indolyl, which may be substituted by OR 2 , R 2 is hydrogen, C 1 -C 6 alkyl, or C 3 -C 7 cycloalkyl, two C 1 When a -C 6 alkyl group is present at one atom, they can be joined together to form a C 5 -C 7 cyclic ring which can include oxygen, sulfur or NR 3a , and R 3 is hydrogen or C 1 Phenyl which may be substituted at the ortho position by an —C 3 alkyl group, (CH 2 ) r (1H-tetrazol-5-yl) or (CH 2 ) r C (O) OR 2 , and R 3a is hydrogen, Or C 1 -C 4 alkyl, W is —CN, —C (O) OR 2 , or —C (O) N (R 2 ) (R 2 ) and X is hydrogen or C (O) 0R 2 And Y is hydrogen, benzyl, picoyl, or thiazolylmethyl, and R 4 and R 5 are independently hydrogen, C 1 -C 3 alkyl, or C 1 -C substituted by one or two hydroxyls; 3 alkyl, A is Wherein x is 0 or 1, R 7 and R 7a are independently hydrogen or C 1 -C 4 alkyl, m is 0, 1 or 2, and r is 0, 1 or 2. 제2항에 있어서, 다음 일반식의 입체특이적으로 정의된 화합물.The compound according to claim 2, defined stereospecifically of the general formula 상기식에서, R1, R3, R4, R5, A, W, X, Y 및 n 은 제2항에서 정의한 바와 같다.Wherein R 1 , R 3 , R 4 , R 5 , A, W, X, Y and n are as defined in claim 2. 제2항에 있어서,The method of claim 2, 로 이루어진 그룹 중에서 선택된 화합물, 및 이의 약제학적으로 허용되는 염 및 개별적인 부분입체이성체.Compounds selected from the group consisting of, and pharmaceutically acceptable salts and individual diastereomers thereof. 다음 일반식(BI)의 화합물, 및 이의 약제학적으로 허용되는 염 및 개별적인 부분입체이성체Of a compound of formula (BI) and pharmaceutically acceptable salts and individual diastereomers thereof 상기식에서, R1은 C1-C10알킬, 아릴, 아릴( C1-C6알킬), (C3-C7사이클로알킬)( C1-C6알킬)-, ( C1-C5알킬)-K-( C1-C5알킬)-, 아릴( C0-C5알킬)-K-( C1-C5알킬)-, 및 (C3-C7사이클로알킬)( C0-C5알킬)-K-( C1-C5알킬)-로 이루어진 그룹 중에서 선택되며, 여기서 K은 O, S(O)m, N(R2)C(O), C(O)N(R2), OC(O), C(O)O, -CR2=CR2-, 또는 -C≡C- 이고, 아릴은 페닐, 나프틸, 인돌릴, 아자인돌, 피리딜, 벤조티에닐, 벤조푸라닐, 티아졸릴 및 벤즈이미다졸릴 중에서 선택되고, R2및 알킬은 1 내지 9개의 할로겐, S(O)mR2a1 내지 3개의 OR2a또는 C(O)OR2a에 의해 추가로 치환될 수 있고, 아릴은 1 내지 3개의 C1-C6알킬, 1 내지 3개의 할로겐, 1 내지 2개의 OR2, 메틸렌디옥시, -S(O)mOR2, 1 내지 2개의 -CF3, -OCF3, 니트로, -N(R2)C(O)(R2), -C(O)OR2, -C(O)N(R2)(R2), -1H-테트라졸-5-일, -SO2N(R2)(R2), -N(R2)SO2페닐, 또는 -N(R2)SO2R2에 의해 추가로 치환될 수 있고, R2는 수소, C1-C6알킬 및 C3-C7사이클로알킬 중에서 선택되고, 2개의 C1-C6알킬 그룹이 한 원자에 존재하는 경우, 이들은 함께 결합하여 산소, 황 또는 NR3a를 포함할 수 있는 C3-C8사이클릭 환을 형성할 수도 있고, R3a는 수소, 또는 하이드록실에 의해 치환될 수 있는 C1-C6알킬이고, R2a는 수소, 또는 하이드록실에 의해 치환될 수 있는 C1-C6알킬이고, R3은 -(CH2)r페닐, -(CH2)r나프틸, -C1-C10알킬, -C3-C7사이클로알킬 중에서 선택되고, 여기서 페닐, 나프틸 및 C3-C7사이클로알킬 환은 C1-C6알킬, 할로겐, -OR2, -NHSO2CF3, -(CH2)rOR6, -(CH2)rN(R2)(R6), -(CH2)r(R6), -(CH2)rC(O)OR2, -(CH2)rC(O)OR6, -(CH2)rOC(O)R2, -(CH2)rOC(O)R6, -(CH2)rC(O)OR2, -(CH2)rC(O)R6, -(CH2)rC(O)N(R2)(R2), -(CH2)rC(O)N(R2)(R6), -(CH2)rN(R2)C(O)R2, -(CH2)rN(R2)C(O)R6, -(CH2)rN(R6)C(O)R2, -(CH2)rN(R6)C(O)R6, -(CH2)rN(R2)C(O)OR2, -(CH2)rN(R2)C(O)OR6, -(CH2)rN(R6)C(O)OR2, -(CH2)rN(R6)C(O)OR6, -(CH2)rN(R2)C(O)N(R2)(R6), -(CH2)rN(R2)C(O)N(R2)(R2), -(CH2)rN(R6)C(O)N(R2)(R6), -(CH2)rN(R2)SO2R6, -(CH2)rN(R2)SO2R2, -(CH2)rN(R6)SO2R2, -(CH2)rN(R6)SO2R6, -(CH2)rOC(O)N(R2)(R6), -(CH2)rOC(O)N(R2)(R2), -(CH2)rSO2N(R2)(R6), -(CH2)rSO2N(R2)(R2), -(CH2)rSO2NHC(O)R6, -(CH2)rSO2NHC(O)R2, -(CH2)rSO2NHC(O)OR6, -(CH2)rSO2NHC(O)OR2, -(CH2)rC(O)NHC(O)NR2, -(CH2)rC(O)NHC(O)NR6, -(CH2)rC(O)NHC(O)R2, -(CH2)rCONHC(O)R6, -(CH2)rCONHSO2R6, -(CH2)rCONHSO2R2, -(CH2)rCONHSO2N(R2)R2), -(CH2)rCONHSO2N(R2)R6), -(CH2)rN(R2)SO2N(R2)R6), -(CH2)rN(R6)SO2N(R2)R6), -(CH2)rS(O)mR6, 및 -(CH2)rS(O)mR2로 이루어진 그룹 중에서 선택된 1 내지 3개의 치환체에 의해 치환될 수 있고, R3a는 수소, 또는 하이드록실에 의해 치환될 수 있는 C1-C6알킬이고, X는 수소, -C≡N, -(CH2)qN(R2)C(O)R2, -(CH2)qN(R2)C(CH2)t아릴, -(CH2)qN(R2)SO2(CH2)t아릴, -(CH2)qN(R2)SO2R2, -(CH2)qN(R2)C(O)N(R2)(CH2)t아릴, -(CH2)qN(R2)C(O)N(R2)(R2), -(CH2)qC(O)N(R2)(R2), -(CH2)qC(O)N(R2)(CH2)t아릴, -(CH2)qC(O)OR2, -(CH2)qC(O)O(CH2)t아릴, -(CH2)qOR2, -(CH2)qOC(O)OR2, -(CH2)qOC(O)(CH2)t아릴, -(CH2)qOC(O)N(R2)(CH2)아릴, -(CH2)qOC(O)N(R2)(R2), -(CH2)qC(O)R2, -(CH2)qC(O)(CH2)t아릴, -(CH2)qN(R2)C(O)OR2, -(CH2)qN(R2)SO2N(R2)(R2), -(CH2)qS(O)mR2, 및 -(CH2)qS(O)m(CH2)t아릴 중에서 선택되고, 여기서 R2, (CH2)q및 (CH)t그룹은 1 내지 2개의 C1-C4알킬, 하이드록실, C1-C4저급 알콕시, 카복실, CONH2, S(O)mCH3, 카복실레이트 C1-C4알킬 에스테르 또는 1H-테트라졸-5-일에 의해 치환될 수도 있고, 아릴은 1 내지 3개의 할로겐, 1 내지 3개의 -OR2, -CON(R2)(R2), -C(O)OR2, 1 내지 3개의 C1-C4알킬, S(O)mR2또는 1H-테트라졸-5-일에 의해 치환될 수도 있는, 페닐, 나프틸, 피리딜, 티아졸릴 또는 1H-테트라졸-5-일 그룹이고, Y는 수소, C1-C10알킬, -(CH2)t아릴, (CH2)q(C3-C7사이클로알킬), -(CH2)q-K-(C1-C6알킬), -(CH2)q-K-(CH2)t아릴, -(CH2)q-K-(CH2)t(O,NR2또는 S 함유 C3-C7사이클로알킬), 및 -(CH2)q-K-(CH2)t(C3-C7사이클로알킬)중에서 선택되고, 여기서 K는 O, S(O)m, C(O)NR2, CH=CH, C≡C, N(R2)C(O), C(O)NR2, C(O)O, 또는 OC(O)이고, 알킬, R2, (CH2)q및 (CH2)t그룹은 C1-C4알킬, 하이드록실, C1-C4저급 알콕시, 카복실, CONH2,또는 카복실레이트 C1-C4알킬 에스테르에 의해 치환될 수도 있고, 아릴은 1 내지 3개의 할로겐, 1 내지 3개의 -OR2, 1 내지 2개의 -N(R2)(R2), -C(O)OR2, -C(O)N(R2)(R2), 니트로, -NHC(O)R2, 시아노, 벤질, 1 내지 3개의 C1-C4알킬, S(O)mR2또는 1H-테트라졸-5-일에 의해 치환될 수 있는, 페닐, 나프틸, 피리딜, 1H-테트라졸-5-일, 티아졸릴, 이미다졸릴, 인돌릴, 피리미디닐, 티아디아졸릴, 피라졸릴, 옥사졸릴, 이속사졸릴, 티오펜일, 퀴놀리닐, 피라지닐 또는 이소티아졸릴이고, R4및 R5는 독립적으로 수소, C1-C6알킬 또는 1 내지 5개의 할로, 1 내지 3개의 하이드록시, 1 내지 3개의 C1-C10알카노일옥시, 1 내지 3개의 C1-C6알콕시, 페닐, 페녹시, 2-푸릴, C1-C6알콕시카보닐 또는 S(O)m(C1-C6알킬)에 의해 치환된 C1-C6알킬이거나, R4및 R5는 함께 결합하여 -C(H2)dLa(CH2)e-(여기서, La는 C(R2)2, 0, S(O)m또는 N(R2)이고, d 및 e는 독립적으로 1 내지 3이고, R2는 상술한 바와 같다)를 형성하고, A는Wherein R 1 is C 1 -C 10 alkyl, aryl, aryl (C 1 -C 6 alkyl), (C 3 -C 7 cycloalkyl) (C 1 -C 6 alkyl)-, (C 1 -C 5 Alkyl) -K- (C 1 -C 5 alkyl)-, aryl (C 0 -C 5 alkyl) -K- (C 1 -C 5 alkyl)-, and (C 3 -C 7 cycloalkyl) (C 0 -C 5 alkyl) -K- (C 1 -C 5 alkyl)-, wherein K is O, S (O) m, N (R 2 ) C (O), C (O) N (R 2 ), OC (O), C (O) O, -CR 2 = CR 2- , or -C≡C-, where aryl is phenyl, naphthyl, indolyl, azaindole, pyridyl, benzothier Alkyl, benzofuranyl, thiazolyl and benzimidazolyl, and R 2 and alkyl are added by 1 to 9 halogens, S (O) mR 2a 1 to 3 OR 2a or C (O) OR 2a And aryl is 1 to 3 C 1 -C 6 alkyl, 1 to 3 halogen, 1 to 2 OR 2 , methylenedioxy, -S (O) mOR 2 , 1 to 2 -CF 3 , -OCF 3 , nitro, -N (R 2 ) C (O) (R 2 ), -C (O) OR 2 , -C (O) N (R 2 ) (R 2 ), -1H-tetra Sol-5-yl, -SO 2 N ( R 2 ) (R 2 ), —N (R 2 ) SO 2 phenyl, or —N (R 2 ) SO 2 R 2 , wherein R 2 is hydrogen, C 1 -C 6 alkyl and When selected from C 3 -C 7 cycloalkyl and two C 1 -C 6 alkyl groups are present on one atom, they are bonded together and C 3 -C 8 cyclic which may include oxygen, sulfur or NR 3a May form a ring, R 3a is hydrogen or C 1 -C 6 alkyl which may be substituted by hydroxyl and R 2a is hydrogen or C 1 -C 6 alkyl which may be substituted by hydroxyl , R 3 is selected from-(CH 2 ) r phenyl,-(CH 2 ) r naphthyl, -C 1 -C 10 alkyl, -C 3 -C 7 cycloalkyl, wherein phenyl, naphthyl and C 3- C 7 cycloalkyl ring is C 1 -C 6 alkyl, halogen, -OR 2 , -NHSO 2 CF 3 ,-(CH 2 ) r OR 6 ,-(CH 2 ) r N (R 2 ) (R 6 ),- (CH 2 ) r (R 6 ),-(CH 2 ) r C (O) OR 2 ,-(CH 2 ) r C (O) OR 6 ,-(CH 2 ) r OC (O) R 2 ,- (CH 2 ) r OC (O) R 6 ,-(CH 2 ) r C (O) OR 2 ,-(CH 2 ) r C (O) R 6 ,-(CH 2 ) r C (O) N (R 2 ) (R 2 ),-(CH 2 ) r C (O) N (R 2 ) (R 6 ),-( CH 2 ) r N (R 2 ) C (O) R 2 ,-(CH 2 ) r N (R 2 ) C (O) R 6 ,-(CH 2 ) r N (R 6 ) C (O) R 2 ,-(CH 2 ) r N (R 6 ) C (O) R 6 ,-(CH 2 ) r N (R 2 ) C (O) OR 2 ,-(CH 2 ) r N (R 2 ) C (O) OR 6 ,-(CH 2 ) r N (R 6 ) C (O) OR 2 ,-(CH 2 ) r N (R 6 ) C (O) OR 6 ,-(CH 2 ) r N ( R 2 ) C (O) N (R 2 ) (R 6 ),-(CH 2 ) r N (R 2 ) C (O) N (R 2 ) (R 2 ),-(CH 2 ) r N ( R 6 ) C (O) N (R 2 ) (R 6 ),-(CH 2 ) r N (R 2 ) SO 2 R 6 ,-(CH 2 ) r N (R 2 ) SO 2 R 2 ,- (CH 2 ) r N (R 6 ) SO 2 R 2 ,-(CH 2 ) r N (R 6 ) SO 2 R 6 ,-(CH 2 ) r OC (O) N (R 2 ) (R 6 ) ,-(CH 2 ) r OC (O) N (R 2 ) (R 2 ),-(CH 2 ) r SO 2 N (R 2 ) (R 6 ),-(CH 2 ) r SO 2 N (R 2 ) (R 2 ),-(CH 2 ) r SO 2 NHC (O) R 6 ,-(CH 2 ) r SO 2 NHC (O) R 2 ,-(CH 2 ) r SO 2 NHC (O) OR 6 ,-(CH 2 ) r SO 2 NHC (O) OR 2 ,-(CH 2 ) r C (O) NHC (O) NR 2 ,-(CH 2 ) r C (O) NHC (O) NR 6 ,-(CH 2 ) r C (O) NHC (O) R 2 ,-(CH 2 ) r CONHC (O) R 6 ,-(CH 2 ) r CONHSO 2 R 6 ,-(CH 2 ) r CONHSO 2 R 2 ,-(CH 2 ) r CONHSO 2 N (R 2 ) R 2 ),-(CH 2 ) r CONHSO 2 N (R 2 ) R 6 ),-(CH 2 ) r N (R 2 ) SO 2 N (R 2 ) R 6 ),-(CH 2 ) r N (R 6 ) SO 2 N (R 2 ) R 6 ),-(CH 2 ) r S (O) m R 6 , and — (CH 2 ) r S (O) m R 2 may be substituted by 1 to 3 substituents selected from the group consisting of R 3a is hydrogen or C which may be substituted by hydroxyl 1- C 6 alkyl, X is hydrogen, -C≡N,-(CH 2 ) q N (R 2 ) C (O) R 2 ,-(CH 2 ) q N (R 2 ) C (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) SO 2 (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) SO 2 R 2 ,-(CH 2 ) q N (R 2 ) C (O) N (R 2 ) (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) C (O) N (R 2 ) (R 2 ),-(CH 2 ) q C (O ) N (R 2 ) (R 2 ),-(CH 2 ) q C (O) N (R 2 ) (CH 2 ) t aryl,-(CH 2 ) q C (O) OR 2 ,-(CH 2 ) q C (O) O (CH 2 ) t aryl,-(CH 2 ) q OR 2 ,-(CH 2 ) q OC (O) OR 2 ,-(CH 2 ) q OC (O) (CH 2 ) t aryl,-(CH 2 ) q OC (O) N (R 2 ) (CH 2 ) aryl,-(CH 2 ) q OC (O) N (R 2 ) (R 2 ),-(CH 2 ) q C (O) R 2 ,-(CH 2 ) q C (O) (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) C (O) OR 2 ,-(CH 2 ) q N ( R 2 ) SO 2 N (R 2 ) (R 2 ),-(CH 2 ) q S (O) m R 2 , and-(CH 2 ) q S (O) m (CH 2 ) t aryl, wherein the R 2 , (CH 2 ) q and (CH) t groups are 1-2 C 1 -C 4 alkyl, hydroxyl, C 1 -C 4 lower alkoxy, carboxyl, CONH 2 , S (O) m CH 3 , carboxylate C 1 -C 4 alkyl ester or 1H-tetrazol-5-yl, aryl may be 1 to 3 halogen, 1 to 3 -OR 2 , -CON (R 2 ) (R 2 ), -C (O) OR 2 , which may be substituted by 1 to 3 C 1 -C 4 alkyl, S (O) m R 2 or 1H-tetrazol-5-yl , Phenyl, naphthyl, pyridyl, thiazolyl or 1H-tetrazol-5-yl group, Y is hydrogen, C 1 -C 10 alkyl,-(CH 2 ) t aryl, (CH 2 ) q (C 3 -C 7 cycloalkyl),-(CH 2 ) q -K- (C 1 -C 6 alkyl),-(CH 2 ) q -K- (CH 2 ) t aryl,-(CH 2 ) q -K- It is selected from (CH 2) q -K- (CH 2) t (C 3 -C 7 cycloalkyl), - (CH 2) t (O, NR 2 , or S-containing C 3 -C 7 cycloalkyl), and Where K is O, S (O) m , C (O) NR 2 , CH = CH, C≡C, N (R 2 ) C (O), C (O) NR 2 , C (O) O, or OC ( O) and alkyl, R 2 , (CH 2 ) q and (CH 2 ) t groups are C 1 -C 4 alkyl, hydroxyl, C 1 -C 4 lower alkoxy, carboxyl, CONH 2 , or carboxylate C 1 May be substituted by a -C 4 alkyl ester, with aryl being 1 to 3 halogens, 1 to 3 -OR 2 , 1 to 2 -N (R 2 ) (R 2 ), -C (O) OR 2 , -C (O) N (R 2 ) (R 2 ), nitro, -NHC (O) R 2 , cyano, benzyl, 1 to 3 C 1 -C 4 alkyl, S (O) m R 2 or Phenyl, naphthyl, pyridyl, 1H-tetrazol-5-yl, thiazolyl, imidazolyl, indolyl, pyrimidinyl, thiadiazolyl, which may be substituted by 1H-tetrazol-5-yl, Pyrazolyl, oxazolyl, isoxazolyl, thiophenyl, quinolinyl, pyrazinyl or isothiazolyl, R 4 and R 5 are independently hydrogen, C 1 -C 6 alkyl or 1 to 5 halo, 1 To 3 hydroxy, 1 to 3 C 1 -C 10 alkanoyloxy, 1 to 3 C 1 -C 6 alkoxy, phenyl, phenoxy, 2-furyl, C 1 -C 6 Alkoxycarbonyl or S (O), or a C 1 -C 6 alkyl substituted by m (C 1 -C 6 alkyl), R 4 and R 5 is a bond and -C (H 2) dLa (CH 2) e with -Wherein La is C (R 2 ) 2 , 0, S (O) m or N (R 2 ), d and e are independently 1 to 3 and R 2 is as described above; and , A 이고, 여기서 x 및 y는 독립적으로 0, 1, 2 또는 3이고, Z는 N-R6a또는 0이고, 여기서 R6a는 수소 또는 C1-C6알킬이고, R6은 수소, C1-C6알킬 또는 (CH2)v아릴이고, 여기서 알킬 및 (CH2)v그룹은 1 내지 2개의 O(R2), S(O)mR2, 1H-테트라졸-5-일, C(O)OR2, C(O)N(R2)(R2), 또는 SO2N(R2)(R2), N(R2)C(O)N(R2)(R2)에 의해 치환될 수도 있고, 아릴은 C1-C6알킬, C3-C6사이클로알킬, 아미노 또는 하이드록실에 의해 치환될 수 있는, 페닐, 피리딜, 1H-테트라졸-5-일, 트리아졸릴, 이미다졸릴, 티아졸릴, 피라졸릴, 티아디아졸릴, 이미다졸론-1-일, 옥사디아졸릴, 벤즈이미다졸-2-일, 트리아졸리논-일이고, R7및 R7a는 독립적으로 수소, C1-C6알킬, 트리플루오로메틸, 페닐, 또는 이미다졸릴, 페닐, 인돌릴, p-하이드록시페닐, OR2, S(O)mR2, C(O)OR2, C3-C7사이클로알킬, N(R2)(R2), C(O)N(R2)(R2)에 의해 치환된 C1-C6알킬이거나, R7및 R7a는 독립적으로 R4및 R5그룹 중의 하나 또는 이들 둘다와 결합하여 R7또는 R7a그룹의 말단 질소와 알킬 부분 사이에 탄소수 1 내지 5의 알킬렌 브릿지를 형성하거나, R7및 R7a는 서로 결합하여 C3-C7사이클로알킬을 형성하고, m 은 0, 1 또는 2이고, n 은 1, 2 또는 3이고, q 는 0, 1, 2, 3 또는 4이고, r은 0, 1, 2 또는 3이고, t는 0, 1, 2 또는 3이고, v는 0, 1 또는 2이다.Wherein x and y are independently 0, 1, 2 or 3, Z is NR 6a or 0, where R 6a is hydrogen or C 1 -C 6 alkyl, R 6 is hydrogen, C 1 -C 6 Alkyl or (CH 2 ) v aryl, wherein the alkyl and (CH 2 ) v group is one to two O (R 2 ), S (O) m R 2 , 1H-tetrazol-5-yl, C (O ) OR 2 , C (O) N (R 2 ) (R 2 ), or SO 2 N (R 2 ) (R 2 ), N (R 2 ) C (O) N (R 2 ) (R 2 ) Aryl, phenyl, pyridyl, 1H-tetrazol-5-yl, triazolyl, which may be substituted by C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, amino or hydroxyl , Imidazolyl, thiazolyl, pyrazolyl, thiadiazolyl, imidazolon-1-yl, oxadiazolyl, benzimidazol-2-yl, triazolinone-yl, and R 7 and R 7a are independently Hydrogen, C 1 -C 6 alkyl, trifluoromethyl, phenyl, or imidazolyl, phenyl, indolyl, p-hydroxyphenyl, OR 2 , S (O) m R 2 , C (O) OR 2 , C 3 -C 7 cycloalkyl, N (R 2 ) (R 2 ), C 1 -C 6 alkyl substituted by C (O) N (R 2 ) (R 2 ), or R 7 and R 7a are independently one of the R 4 and R 5 groups Or combine with both to form an alkylene bridge of 1 to 5 carbon atoms between the terminal nitrogen of the R 7 or R 7a group and the alkyl moiety, or R 7 and R 7a combine with each other to form C 3 -C 7 cycloalkyl M is 0, 1 or 2, n is 1, 2 or 3, q is 0, 1, 2, 3 or 4, r is 0, 1, 2 or 3, t is 0, 1, 2 or 3, and v is 0, 1 or 2. 제7항에 있어서, R1이 C1-C10알킬, 아릴( C1-C4알킬), (C3-C6사이클로알킬)( C1-C4알킬)-, ( C1-C4알킬)-K-( C1-C2알킬)-, 아릴( C0-C2알킬)-K-( C1-C2알킬)-, 및 (C3-C7사이클로알킬)( C0-C2알킬)-K-( C1-C2알킬)-로 이루어진 그룹 중에서 선택되고, 여기서 K는 O, S(O)m, OC(O), C(O)O, 이고, 알킬 그룹이 1 내지 7개의 할로겐, S(O)mR2, 1 내지 3개의 OR2또는 C(O)OR2에 의해 추가로 치환될 수 있고, 아릴은 1 내지 2개의 C1-C4알킬, 1 내지 2개의 할로겐, 1 내지 2개의 -OR2, S(O)mR2, 또는 -C(O)OR2에 의해 추가로 치환될 수 있는 페닐, 나프틸, 인돌릴, 피리딜, 벤즈이미다졸릴, 이자인돌레일, 벤조티에닐 또는 벤조푸라닐이고, R2가 수소, C1-C6알킬, 및 C3-C7사이클로알킬중에서 선택되고, 2개의 C1-C6알킬 그룹이 한 원자에 존재하는 경우, 이들은 함께 결합하여 산소, 황 또는 NR3a를 포함할 수 있는 C4-C7사이클릭 환을 형성할 수도 있고, R3이 1 내지 2개의 C1-C6알킬 그룹, 1 내지 2개의 할로겐 또는 1 내지 2개의 -OR2에 의해 치환될 수 있는 페닐이며, 이는 추가로 NHSO2CF3, -(CH2)rOR6, -(CH2)rN(R2)(R6), -(CH2)r(R6), -(CH2)rC(O)OR2, -(CH2)rC(O)OR6, -(CH2)rOC(O)R2, -(CH2)rOC(O)R6, -(CH2)rC(O)R2, -(CH2)rC(O)R6, -(CH2)rC(O)N(R2)(R2), -(CH2)rC(O)N(R2)(R6), -(CH2)rN(R2)C(O)R2, -(CH2)rN(R2)C(O)R6, -(CH2)rN(R6)C(O)R2, -(CH2)rN(R6)C(O)R6, -(CH2)rN(R2)C(O)OR2, -(CH2)rN(R2)C(O)OR6, -(CH2)rN(R6)C(O)OR2, -(CH2)rN(R6)C(O)OR6, -(CH2)rN(R2)C(O)N(R2)(R6), -(CH2)rN(R2)C(O)N(R2)(R2), -(CH2)rN(R6)C(O)N(R2)(R6), -(CH2)rN(R2)SO2R6, -(CH2)rN(R2)SO2R2, -(CH2)rN(R6)SO2R2, -(CH2)rN(R6)SO2R6, -(CH2)rOC(O)N(R2)(R6), -(CH2)rOC(O)N(R2)(R2), -(CH2)rSO2N(R2)(R6), -(CH2)rSO2N(R2)(R2), -(CH2)rSO2NHC(O)R6, -(CH2)rSO2NHC(O)R2, -(CH2)rSO2NHC(O)OR6, -(CH2)rSO2NHC(O)OR2, -(CH2)rC(O)NHC(O)NR2, (CH)rC(O)NHC(O)NR6, -(CH2)rC(O)NHC(O)R2, -(CH2)rCONHC(O)R6, -(CH2)rCONHSO2R6, -(CH2)rCONHSO2R2, -(CH2)rCONHSO2N(R2)(R2), -(CH2)rCONHSO2N(R2)(R6), -(CH2)rN(R2)SO2N(R2)(R6), -(CH2)rN(R6)SO2N(R2)(R6), -(CH2)rS(O)mR6, 및 -(CH2)rS(O)mR2로 이루어진 그룹 중에서 선택된 치환체에 의해 오르토 위치에서 치환될 수 있고, R3a가 수소, 또는 C1-C4알킬이고, X가 수소, -(CH2)qN(R2)C(O)R2, -(CH2)qN(R2)C(0)(CH2)t아릴, -(CH2)qN(R2)C(0)OR2, -(CH2)qN(R2)SO2(CH2)t아릴, -(CH2)qN(R2)SO2R2, -(CH2)qN(R2)C(O)N(R2)(CH2)t아릴, -(CH2)qN(R2)C(O)N(R2)(R2), -(CH2)qC(O)N(R2)(R2), -(CH2)qC(O)N(R2)(CH2)t아릴, -(CH2)qC(O)OR2, -(CH2)qC(O)O(CH2)t아릴, -(CH2)qOC(O)R2, -(CH2)qOC(O)(CH2)t아릴, -(CH2)qS(O)mR2, 및 -(CH2)qS(O)m(CH2)t아릴 중에서 선택되고, 여기서 R2그룹은 하이드록실, 카복실, CONH2, S(O)mCH3, 카복실레이트 C1-C4알킬 에스테르, 또는 테트라졸에 의해 치환될 수 있고, 아릴은 1 내지 2개의 할로겐, 1 내지 2개의 -OR2, -CONH2, -C(O)OR2, 1 내지 3개의 C1-C4알킬, -S(O)mR2또는 1H-테트라졸-5-일에 의해 치환될 수 있는, 페닐, 나프틸, 피리딜 또는 1-H-테트라졸릴이고, Y가 수소, C1-C8알킬, -(CH2)t아릴, -(CH2)q(C5-C6사이클로알킬), -(CH2)q-K-(C1-C6알킬), -(CH2)q-K-(CH2)t아릴, -(CH2)q-K-(CH2)t(O,NR2또는 S 함유 C3-C7사이클로알킬), 및 -(CH2)q-K-(CH2)t(C5-C6사이클로알킬)중에서 선택되고, K는 O 또는 S(O)m이고, 알킬 그룹은 하이드록실, 카복실, -CONH2, 카복실레이트 C1-C4알킬 에스테르 또는 1H-테트라졸-5-일에 의해 치환될 수도 있고, 아릴은 페닐, 나프틸, 피리딜, 1-H-테트라졸릴, 티아졸릴, 이미다졸릴, 피리미디닐, 티아디아졸릴, 피라졸릴, 옥사졸릴, 이속사졸릴 또는 티오펜일이고, 이는 1 내지 3개의 할로겐, 1 내지 3개의 -OR2, 1 내지 2개의 -N(R2)(R2), -C(O)OR2, -C(O)N(R2)(R2), 시아노, 1 내지 2개의 C1-C4알킬, 벤질, -S(O)mR2또는 1H-테트라졸-5-일에 의해 치환될 수 있고, R4및 R5가 독립적으로 수소, C1-C6알킬 또는 1 내지 5개의 할로, 1 내지 3개의 하이드록실, S(O)m(C1-C6알킬) 또는 페닐에 의해 치환된 C1-C6알킬이고, R6이 H, C1-C6알킬 또는 (CH2)v아릴이고, 여기서 (CH2)v및 알킬 그룹은 1 내지 2개의 O(R2), S(O)mR2, C(O)OR2, C(O)N(R2)(R2) 또는 SO2N(R2)(R2), N(R2)C(O)N(R2)(R2)에 의해 치환될 수도 있고, 아릴 그룹은, C1-C6알킬, C3-C6사이클로알킬, 아미노 또는 하이드록실에 의해 치환될 수 있는 페닐, 피리딜, 1H-테트라졸-5-일, 트리아졸릴, 이미다졸릴, 티아졸릴, 옥사디아졸린, 피라졸릴, 티아디아졸릴, 벤즈이미다졸-2-일이고, A가이고, 여기서 x는 0 또는 1이고, R7및 R7a가 독립적으로 수소, C1-C6알킬, 트리푸루오로메틸, 페닐, 또는 이미다졸릴, 페닐, 인돌릴, p-하이드록시페닐, OR2, S(O)mR2, C(O)O(R2), C5-C7사이클로알킬, N(R2)(R2), C(O)N(R2)(R2)에 의해 치환된 C1-C6알킬이거나, R7및 R7a가 독립적으로 R4및 R5중의 하나와 결합하여 R7또는 R7a그룹의 말단 질소와 알킬 부분 사이에 알킬렌 브릿지를 형성하여 5원 또는 6원 환을 형성하거나, R7및 R7a가 서로 결합하여 C3사이클로알킬을 형성하고, n이 2이고, m 이 0, 1 또는 2이고, r이 0, 1, 2 또는 3이고, q가 0, 1, 2 또는 3이고, t가 0, 1, 2 또는 3이고, v가 0, 1 또는 2인 화합물, 및 이의 약제학적으로 허용되는 염 및 개별적인 부분입체이성체.8. A compound according to claim 7, wherein R 1 is C 1 -C 10 alkyl, aryl (C 1 -C 4 alkyl), (C 3 -C 6 cycloalkyl) (C 1 -C 4 alkyl)-, (C 1 -C 4 alkyl) -K- (C 1 -C 2 alkyl)-, aryl (C 0 -C 2 alkyl) -K- (C 1 -C 2 alkyl)-, and (C 3 -C 7 cycloalkyl) (C 0- C 2 alkyl) -K- (C 1 -C 2 alkyl)-, wherein K is O, S (O) m , OC (O), C (O) O, and alkyl The group may be further substituted by 1 to 7 halogens, S (O) m R 2 , 1 to 3 OR 2 or C (O) OR 2 , with aryl being 1 to 2 C 1 -C 4 alkyl , Phenyl, naphthyl, indolyl, pyridyl, which may be further substituted by 1 to 2 halogens, 1 to 2 -OR 2 , S (O) m R 2 , or -C (O) OR 2 , Benzimidazolyl, isazindolyl, benzothienyl or benzofuranyl, R 2 is selected from hydrogen, C 1 -C 6 alkyl, and C 3 -C 7 cycloalkyl, and two C 1 -C 6 alkyl If groups exist in one atom, they form together And that may contain oxygen, sulfur or NR 3a C 4 -C 7 may form a cyclic ring, R 3 is one to two C 1 -C 6 alkyl group, one to two halogen or one to two Phenyl which may be substituted by -OR 2 , which is further NHSO 2 CF 3 ,-(CH 2 ) r OR 6 ,-(CH 2 ) r N (R 2 ) (R 6 ),-(CH 2 ) r (R 6 ),-(CH 2 ) r C (O) OR 2 ,-(CH 2 ) r C (O) OR 6 ,-(CH 2 ) r OC (O) R 2 ,-(CH 2) ) r OC (O) R 6 ,-(CH 2 ) r C (O) R 2 ,-(CH 2 ) r C (O) R 6 ,-(CH 2 ) r C (O) N (R 2 ) (R 2 ),-(CH 2 ) r C (O) N (R 2 ) (R 6 ),-(CH 2 ) r N (R 2 ) C (O) R 2 ,-(CH 2 ) r N (R 2 ) C (O) R 6 ,-(CH 2 ) r N (R 6 ) C (O) R 2 ,-(CH 2 ) r N (R 6 ) C (O) R 6 ,-(CH 2 ) r N (R 2 ) C (O) OR 2 ,-(CH 2 ) r N (R 2 ) C (O) OR 6 ,-(CH 2 ) r N (R 6 ) C (O) OR 2 ,-(CH 2 ) r N (R 6 ) C (O) OR 6 ,-(CH 2 ) r N (R 2 ) C (O) N (R 2 ) (R 6 ),-(CH 2 ) r N (R 2 ) C (O) N (R 2 ) (R 2 ),-(CH 2 ) r N (R 6 ) C (O) N (R 2 ) (R 6 ),-(CH 2 ) r N (R 2 ) SO 2 R 6 ,-(CH 2 ) r N (R 2 ) SO 2 R 2 ,-(CH 2 ) r N (R 6 ) SO 2 R 2 ,-(CH 2 ) r N ( R 6 ) SO 2 R 6 ,-(CH 2 ) r OC (O) N (R 2 ) (R 6 ),-(CH 2 ) r OC (O) N (R 2 ) (R 2 ),-(CH 2 ) r SO 2 N (R 2 ) (R 6 ),-(CH 2 ) r SO 2 N (R 2 ) (R 2 ),-(CH 2 ) r SO 2 NHC (O) R 6 ,-(CH 2 ) r SO 2 NHC (O) R 2 ,-(CH 2 ) r SO 2 NHC (O) OR 6 ,-(CH 2 ) r SO 2 NHC (O) OR 2 ,-(CH 2 ) r C (O) NHC ( O) NR 2 , (CH) r C (O) NHC (O) NR 6 ,-(CH 2 ) r C (O) NHC (O) R 2 ,-(CH 2 ) r CONHC (O) R 6 , -(CH 2 ) r CONHSO 2 R 6 ,-(CH 2 ) r CONHSO 2 R 2 ,-(CH 2 ) r CONHSO 2 N (R 2 ) (R 2 ),-(CH 2 ) r CONHSO 2 N ( R 2 ) (R 6 ),-(CH 2 ) r N (R 2 ) SO 2 N (R 2 ) (R 6 ),-(CH 2 ) r N (R 6 ) SO 2 N (R 2 ) ( R 6 ),-(CH 2 ) r S (O) m R 6 , and-(CH 2 ) r S (O) m R 2 can be substituted at the ortho position by a substituent selected from the group consisting of R 3a Is hydrogen, or C 1 -C 4 alkyl, X is hydrogen, — (CH 2 ) q N (R 2 ) C (O) R 2 , — (CH 2 ) q N (R 2 ) C (0) ( CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) C (0) OR 2 ,-(CH 2 ) q N (R 2 ) SO 2 (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) SO 2 R 2 ,-(CH 2 ) q N (R 2 ) C (O) N (R 2 ) (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) C ( O) N (R 2 ) (R 2 ),-(CH 2 ) q C (O) N (R 2 ) (R 2 ),-(CH 2 ) q C (O) N (R 2 ) (CH 2 ) t aryl ,-(CH 2 ) q C (O) OR 2 ,-(CH 2 ) q C (O) O (CH 2 ) t aryl,-(CH 2 ) q OC (O) R 2 ,-(CH 2 ) q OC (O) (CH 2 ) t aryl,-(CH 2 ) q S (O) m R 2 , and-(CH 2 ) q S (O) m (CH 2 ) t aryl, wherein R The 2 group may be substituted by hydroxyl, carboxyl, CONH 2 , S (O) m CH 3 , carboxylate C 1 -C 4 alkyl ester, or tetrazole, aryl being 1 to 2 halogens, 1 to 2 May be substituted by -OR 2 , -CONH 2 , -C (O) OR 2 , 1 to 3 C 1 -C 4 alkyl, -S (O) m R 2 or 1H-tetrazol-5-yl Phenyl, naphthyl, pyridyl or 1-H-tetrazolyl, Y is hydrogen, C 1 -C 8 alkyl,-(CH 2 ) t aryl,-(CH 2 ) q (C 5 -C 6 cyclo Alkyl),-(CH 2 ) q -K- (C 1 -C 6 alkyl),-(CH 2 ) q -K- (CH 2 ) t aryl,-(CH 2 ) q -K- (CH 2 ) t (O, NR 2, or S-containing C 3 -C 7 cycloalkyl), and - (CH 2) q -K- ( CH 2) t (C 5 -C 6 cycloalkyl Is selected from the keel), K is O or S (O) m, and the alkyl group is optionally substituted by hydroxyl, carboxyl, -CONH 2, C 1 -C 4 alkyl carboxylate ester, or 1H- tetrazol-5-yl Aryl may be phenyl, naphthyl, pyridyl, 1-H-tetrazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiadiazolyl, pyrazolyl, oxazolyl, isoxazolyl or thiophenyl , 1 to 3 halogens, 1 to 3 -OR 2 , 1 to 2 -N (R 2 ) (R 2 ), -C (O) OR 2 , -C (O) N (R 2 ) ( R 2 ), cyano, 1 to 2 C 1 -C 4 alkyl, benzyl, —S (O) m R 2 or 1H-tetrazol-5-yl, wherein R 4 and R 5 may be substituted independently represent hydrogen, C 1 -C 6 alkyl, 1 to 5 halo, 1 to 3 hydroxyl, S (O) m (C 1 -C 6 alkyl) or a C 1 -C 6 alkyl substituted by phenyl, and , R 6 is H, C 1 -C 6 alkyl or (CH 2 ) v aryl, wherein (CH 2 ) v and the alkyl group are one to two O (R 2 ), S (O) m R 2 , C (O) OR 2 , C (O) N (R 2 ) (R 2 ) or SO 2 N (R 2 ) (R 2 ), N (R 2 ) C (O) N (R 2 ) (R 2 ), and the aryl group is phenyl which may be substituted by C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, amino or hydroxyl, Pyridyl, 1H-tetrazol-5-yl, triazolyl, imidazolyl, thiazolyl, oxadiazolin, pyrazolyl, thiadiazolyl, benzimidazol-2-yl, and A is Wherein x is 0 or 1, and R 7 and R 7a are independently hydrogen, C 1 -C 6 alkyl, tripuruomethyl, phenyl, or imidazolyl, phenyl, indolyl, p-hydroxyphenyl , OR 2 , S (O) m R 2 , C (O) O (R 2 ), C 5 -C 7 cycloalkyl, N (R 2 ) (R 2 ), C (O) N (R 2 ) ( C 1 -C 6 alkyl substituted by R 2 ) or R 7 and R 7a are independently bonded to one of R 4 and R 5 to form an alkylene bridge between the terminal nitrogen and the alkyl moiety of the R 7 or R 7a group To form a 5- or 6-membered ring, or R 7 and R 7a combine with each other to form C 3 cycloalkyl, n is 2, m is 0, 1 or 2, r is 0, 1, 2 or 3, q is 0, 1, 2 or 3, t is 0, 1, 2 or 3, v is 0, 1 or 2, and pharmaceutically acceptable salts and individual diastereomers thereof . 제7항에 있어서, 다음 일반식(BIb)의 화합물, 및 이의 약제학적으로 허용되는 염 및 개별적인 부분입체이성체.8. Compounds of the following formula (BIb), and pharmaceutically acceptable salts and individual diastereomers thereof. 상기식에서, R1은 C1-C10알킬, 아릴(C1-C3알킬)-, (C3-C7사이클로알킬)(C1-C3알킬)-, 및 아릴(C0-C1알킬)-K-(C1-C2알킬)-로 이루어진 그룹 중에서 선택되고, 여기서 K은 0 또는 S(O)m이고, 아릴은 1 내지 2개의 C1-C4알킬, 1 내지 2개의 할로겐, 1 내지 2개의 OR2, S(O)mR2또는 C(O)OR2에 의해 치환될 수 있는, 페닐, 피리딜, 나프틸, 인돌릴, 아자인돌릴 또는 벤즈이미다졸릴이고, R2는 수소, C1-C6알킬, 또는 C3-C7사이클로알킬이고, 2개의 C1-C6알킬 그룹이 한 원자에 존재하는 경우, 이들은 함께 결합하여 산소, 황 또는 NR3a를 포함할 수 있는 C5-C7사이클릭 환을 형성할 수 있고, R3은 1 내지 2개의 C1-C6알킬 그룹, 1 내지 2개의 할로겐 또는 1 내지 2개의 OR2에 의해 치환될 수 있는 페닐이고, 이는 추가로, -NHSO2CF3, -(CH2)rOR6, -(CH2)rN(R2)(R6), -(CH2)r(R6), -(CH2)rC(O)OR2, -(CH2)rOC(O)R2, -(CH2)rOC(O)R6, -(CH2)rC(O)R2, -(CH2)rC(O)R6, -(CH2)rC(O)N(R2)(R2), -(CH2)rC(O)N(R2)(R6), -(CH2)rN(R2)C(O)R2, -(CH2)rN(R2)C(O)R6, -(CH2)rN(R6)C(O)R2, -(CH2)rN(R6)C(O)R6, -(CH2)rN(R2)C(O)OR2, -(CH2)rN(R2)C(O)OR6, -(CH2)rN(R6)C(O)OR2, -(CH2)rN(R6)C(O)OR6, -(CH2)rN(R2)C(O)N(R2)(R6), -(CH2)rN(R6)C(O)N(R2)(R2), -(CH2)rN(R2)C(O)N(R2)(R6), (CH2)rN(R2)SO2R6, -(CH2)rN(R2)SO2R2, -(CH2)rN(R6)SO2R2, -(CH2)rN(R6)SO2R6, -(CH2)rOC(O)N(R2)(R6), -(CH2)rOC(O)N(R2)(R2), -(CH2)rSO2N(R2)(R6), -(CH2)rSO2N(R2)(R2), (CH2)rSO2NHC(O)R6, -(CH2)rSO2NHC(O)R2, -(CH2)rSO2NHC(O)OR6, -(CH2)rSO2NHC(O)OR2, (CH2)rCONHSO2R6, -(CH2)rCONHSO2R2, -(CH2)rS(O)mR6, 및 -(CH2)rS(O)mR2로 이루어진 그룹 중에서 선택된 치환체에 의해 오르토 위치에서 치환될 수 있고, R3a는 수소, 또는 C1-C6알킬이고, X는 수소, -(CH2)qN(R2)C(O)R2, -(CH2)qN(R2)C(0)(CH2)t아릴, -(CH2)qN(R2)SO2(CH2)t아릴, -(CH2)qN(R2)SO2R2, -(CH2)qN(R2)C(O)N(R2)(CH2)t아릴, -(CH2)qN(R2)C(O)N(R2)(R2), -(CH2)qC(O)N(R2)(R2), -(CH2)qN(R2)C(O)OR2, -(CH2)qC(O)N(R2)(CH2)t아릴, -(CH2)qC(O)OR2, -(CH2)qC(O)O(CH2)t아릴, -(CH2)qOC(O)R2, -(CH2)qOC(O)(CH2)t아릴, -(CH2)qS(O)mR2, 및 -(CH2)qS(O)m(CH2)t아릴 중에서 선택되고, R2그룹은 하이드록실, 카복실, CONH2, S(O)mCH3, 카복실레이트 C1-C4알킬 에스테르 또는 테트라졸에 의해 치환될 수 있고, 아릴은 페닐, 나프틸 또는 피리딜이며, 이는 추가로 1 내지 2개의 할로겐, 1 내지 2개의 OR2, C(O)OR2, 1 내지 3개의 C1-C4알킬, S(O)mR2또는 1H-테트라졸-5-일에 치환될 수 있고, Y는 수소, C1-C8알킬, (CH2)t아릴, -(CH2)qC5-C7사이클로알킬, -(CH2)q-K-(C1-C6알킬), -(CH2)qK-(CH2)t아릴, 및 -(CH2)qK-(CH2)t(C5-C6사이클로알킬)중에서 선택되고, 여기서 K는 S(O)m이고, 알킬 그룹은 하이드록실, 카복실, CONH2, 카복실레이트 C1-C4알킬 에스테르 또는 1H-테트라졸-5-일에 의해 치환될 수 있고, 아릴은 특정하게는 1 내지 2개의 할로겐, 1 내지 2개의 OR2, 1 내지 2개의 -N(R2)(R2), -CO(OR2), 1 내지 2개의 C1-C4알킬, S(O)mR2또는 1H-테트라졸-5-일에 의해 치환될 수 있는, 페닐, 나프틸, 피리딜, 티아졸릴, 티오펜일, 피라졸릴, 옥사졸릴, 이속사졸릴 또는 이미다졸릴이고, R4및 R5는 독립적으로 수소, C1-C4알킬, 또는 1 내지 2개의 하이드록실에 의해 치환된 C1-C3알킬이고, R6은 수소, C1-C6알킬 또는 (CH2)v아릴이고, 여기서 C1-C6알킬 및 (CH2)v아릴 그룹은 1 내지 2개의 O(R2), S(O)mR2, C(O)OR2, C(O)N(R2)(R2) 또는 SO2N(R2)(R2), N(R2)C(O)N(R2)(R2)에 의해 치환될 수도 있고, 아릴은 특정하게는 C1-C6알킬, C3-C6사이클로알킬, 아미노 또는 하이드록실에 의해 치환될 수 있는 페닐, 피리딜, 1H-테트라졸-5-일, 트리아졸릴, 이미다졸릴, 티아졸릴, 옥사디아졸린, 피라졸릴, 티아디아졸릴, 벤즈이미다졸-2-일이고, A는이고, 여기서 x는 0 또는 1이고, R7및 R7a가 독립적으로 수소, C1-C2알킬, 페닐, 또는 이미다졸릴, 페닐, 인돌릴, p-하이드록시페닐, OR2, 또는 S(O)mR2에 의해 치환된 C1-C6알킬이거나, R7및 R7a는 독립적으로 서로 결합하여 C3사이클로알킬을 형성할 수 있고, m 은 0, 1 또는 2이고, r은 0, 1, 2 또는 3이고, q는 0, 1, 2 또는 3이고, t는 0, 1, 2 또는 3이고, v는 0, 1 또는 2이다.Wherein R 1 is C 1 -C 10 alkyl, aryl (C 1 -C 3 alkyl)-, (C 3 -C 7 cycloalkyl) (C 1 -C 3 alkyl)-, and aryl (C 0 -C 1 alkyl) -K- (C 1 -C 2 alkyl)-, wherein K is 0 or S (O) m and aryl is 1 to 2 C 1 -C 4 alkyl, 1 to 2 Phenyl, pyridyl, naphthyl, indolyl, azaindoleyl or benzimidazolyl, which may be substituted by 1 halogen, 1 or 2 OR 2 , S (O) m R 2 or C (O) OR 2 R 2 is hydrogen, C 1 -C 6 alkyl, or C 3 -C 7 cycloalkyl, and when two C 1 -C 6 alkyl groups are present at one atom, they are bonded together to form oxygen, sulfur or NR May form a C 5 -C 7 cyclic ring which may comprise 3a , and R 3 is substituted by 1 to 2 C 1 -C 6 alkyl groups, 1 to 2 halogens or 1 to 2 OR 2 Phenyl, which may additionally be —NHSO 2 CF 3 , — (CH 2 ) r OR 6 , — (CH 2 ) r N (R 2 ) (R 6 ),-(CH 2 ) r (R 6 ),-(CH 2 ) r C (O) OR 2 ,-(CH 2 ) r OC (O) R 2 ,-(CH 2 ) r OC (O) R 6 ,-(CH 2 ) r C (O) R 2 ,-(CH 2 ) r C (O) R 6 ,-(CH 2 ) r C (O) N (R 2 ) (R 2 ),-( CH 2 ) r C (O) N (R 2 ) (R 6 ),-(CH 2 ) r N (R 2 ) C (O) R 2 ,-(CH 2 ) r N (R 2 ) C (O ) R 6 ,-(CH 2 ) r N (R 6 ) C (O) R 2 ,-(CH 2 ) r N (R 6 ) C (O) R 6 ,-(CH 2 ) r N (R 2 ) C (O) OR 2 ,-(CH 2 ) r N (R 2 ) C (O) OR 6 ,-(CH 2 ) r N (R 6 ) C (O) OR 2 ,-(CH 2 ) r N (R 6 ) C (O) OR 6 ,-(CH 2 ) r N (R 2 ) C (O) N (R 2 ) (R 6 ),-(CH 2 ) r N (R 6 ) C ( O) N (R 2 ) (R 2 ),-(CH 2 ) r N (R 2 ) C (O) N (R 2 ) (R 6 ), (CH 2 ) r N (R 2 ) SO 2 R 6 ,-(CH 2 ) r N (R 2 ) SO 2 R 2 ,-(CH 2 ) r N (R 6 ) SO 2 R 2 ,-(CH 2 ) r N (R 6 ) SO 2 R 6 , -(CH 2 ) r OC (O) N (R 2 ) (R 6 ),-(CH 2 ) r OC (O) N (R 2 ) (R 2 ),-(CH 2 ) r SO 2 N ( R 2 ) (R 6 ),-(CH 2 ) r SO 2 N (R 2 ) (R 2 ), (CH 2 ) r SO 2 NHC (O) R 6 ,-(CH 2 ) r SO 2 NHC ( O) R 2 ,-(CH 2 ) r SO 2 NHC (O) OR 6 ,-(CH 2 ) r SO 2 NHC (O) OR 2 , (CH 2 ) r CONHSO 2 R 6 ,-(CH 2 ) r CONHSO 2 r 2, - ( CH 2) r S (O) m r 6, and - consisting of (CH 2) r S (O ) m r 2 The substituents of which are selected from the group may be substituted in the ortho position, R 3a is hydrogen, or C 1 -C 6 alkyl, X is hydrogen, - (CH 2) q N (R 2) C (O) R 2, -(CH 2 ) q N (R 2 ) C (0) (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) SO 2 (CH 2 ) t aryl,-(CH 2 ) q N ( R 2 ) SO 2 R 2 ,-(CH 2 ) q N (R 2 ) C (O) N (R 2 ) (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) C (O) N (R 2 ) (R 2 ),-(CH 2 ) q C (O) N (R 2 ) (R 2 ),-(CH 2 ) q N (R 2 ) C (O) OR 2 ,-( CH 2 ) q C (O) N (R 2 ) (CH 2 ) t aryl,-(CH 2 ) q C (O) OR 2 ,-(CH 2 ) q C (O) O (CH 2 ) t aryl ,-(CH 2 ) q OC (O) R 2 ,-(CH 2 ) q OC (O) (CH 2 ) t aryl,-(CH 2 ) q S (O) m R 2 , and-(CH 2 ) q S (O) m (CH 2 ) t aryl and the R 2 group is selected from hydroxyl, carboxyl, CONH 2 , S (O) m CH 3 , carboxylate C 1 -C 4 alkyl ester or tetrazole And aryl is phenyl, naphthyl or pyridyl, which is additionally 1 to 2 halogens, 1 to 2 OR 2 , C (O) OR 2 , 1 to 3 C 1 -C 4 alkyl , S (O) m R 2 or 1H-tetrazol-5-yl, Y is hydrogen, C 1 -C 8 alkyl, (CH 2 ) t aryl, — (CH 2 ) q C 5 − C 7 cycloalkyl,-(CH 2 ) q -K- (C 1 -C 6 alkyl),-(CH 2 ) q K- (CH 2 ) t aryl, and-(CH 2 ) q K- (CH 2 ) t (C 5 -C 6 cycloalkyl) wherein K is S (O) m and the alkyl group is hydroxyl, carboxyl, CONH 2 , carboxylate C 1 -C 4 alkyl ester or 1H-tetrazole May be substituted by -5-yl, and aryl is specifically 1 to 2 halogen, 1 to 2 OR 2 , 1 to 2 -N (R 2 ) (R 2 ), -CO (OR 2 ) Phenyl, naphthyl, pyridyl, thiazolyl, thiophenyl, which may be substituted by 1 to 2 C 1 -C 4 alkyl, S (O) m R 2 or 1H-tetrazol-5-yl, Pyrazolyl, oxazolyl, isoxazolyl or imidazolyl, and R 4 and R 5 are independently hydrogen, C 1 -C 4 alkyl, or C 1 -C 3 alkyl substituted by 1 to 2 hydroxyl; , R 6 is Hydrogen, C 1 -C 6 alkyl or (CH 2 ) v aryl, wherein the C 1 -C 6 alkyl and (CH 2 ) v aryl group is one to two O (R 2 ), S (O) m R 2 , C (O) OR 2 , C (O) N (R 2 ) (R 2 ) or SO 2 N (R 2 ) (R 2 ), N (R 2 ) C (O) N (R 2 ) (R 2 ), and aryl is specifically phenyl, pyridyl, 1H-tetrazol-5 which may be substituted by C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, amino or hydroxyl -Yl, triazolyl, imidazolyl, thiazolyl, oxadiazoline, pyrazolyl, thiadiazolyl, benzimidazol-2-yl, and A is Wherein x is 0 or 1 and R 7 and R 7a are independently hydrogen, C 1 -C 2 alkyl, phenyl, or imidazolyl, phenyl, indolyl, p-hydroxyphenyl, OR 2 , or S (O) C 1 -C 6 alkyl substituted by m R 2 , or R 7 and R 7a can independently combine with each other to form C 3 cycloalkyl, m is 0, 1 or 2, and r is 0, 1, 2 or 3, q is 0, 1, 2 or 3, t is 0, 1, 2 or 3 and v is 0, 1 or 2. 제7항에 있어서, 다음 일반식(BIc)의 화합물, 및 이의 약제학적으로 허용되는 염 및 개별적인 부분입체이성체.8. A compound according to claim 7, wherein the compound of formula (BIc), and pharmaceutically acceptable salts and individual diastereomers thereof. 상기식에서, R1Wherein R 1 is 또는 명시되지 않은 이의 레지오이성체로 이루어진 그룹 중에서 선택되고, R2는 수소, C1-C6알킬, 또는 C3-C7사이클로알킬이고, 2개의 C1-C6알킬 그룹이 한 원자에 존재하는 경우, 이들은 함께 결합하여 산소, 황 또는 NR3a를 포함할 수 있는 C5-C7사이클릭 환을 형성할 수 있고, R3은 -NHSO2CF3, -(CH2)rOR6, -(CH2)r(R6), -(CH2)rC(O)OR2), -(CH2)rC(O)OR6, -(CH2)rOC(O)R2, -(CH2)rOC(O)R6, -(CH2)rC(O)R2, -(CH2)rC(O)R6, -(CH2)rC(O)N(R2)(R2), -(CH2)rC(O)N(R2)(R6), -(CH2)rN(R2)C(O)R2, -(CH2)rN(R2)C(O)R6, -(CH2)rN(R6)C(O)R2, -(CH2)rN(R6)C(O)R6, -(CH2)rN(R2)C(O)OR2, -(CH2)rN(R2)C(O)OR6, -(CH2)rN(R6)C(O)OR2, -(CH2)rN(R6)C(O)OR6, -(CH2)rN(R2)C(O)N(R2)(R6), -(CH2)rN(R2)C(O)N(R2)(R2), -(CH2)rN(R6)C(O)N(R2)(R6), (CH2)rN(R2)SO2R6, -(CH2)rN(R2)SO2R2, -(CH2)rN(R6)SO2R2, (CH2)rN(R6)SO2R6, -(CH2)rOC(O)N(R2)(R6), -(CH2)rOC(O)N(R2)(R2), -(CH2)rSO2N(R2)(R6), -(CH2)rSO2N(R2)(R2), -(CH2)rSO2NHC(O)R6, -(CH2)rSO2NHC(O)R2, -(CH2)rSO2NHC(O)OR6, -(CH2)rSO2NHC(O)OR2, (CH2)rCONHSO2R6, -(CH2)rCONHSO2R2, -(CH2)rS(O)mR6, 및 -(CH2)rS(O)mR2로 이루어진 그룹 중에서 선택된 치환체에 의해 오르토 위치에서 치환될 수 페닐이고, R3a는 수소, 또는 C1-C4알킬이고, X는 수소,Or an unspecified group thereof, R 2 is hydrogen, C 1 -C 6 alkyl, or C 3 -C 7 cycloalkyl, and two C 1 -C 6 alkyl groups are present at one atom Where, they can be joined together to form a C 5 -C 7 cyclic ring which may comprise oxygen, sulfur or NR 3a , where R 3 is —NHSO 2 CF 3 , — (CH 2 ) r OR 6 , -(CH 2 ) r (R 6 ),-(CH 2 ) r C (O) OR 2 ),-(CH 2 ) r C (O) OR 6 ,-(CH 2 ) r OC (O) R 2 ,-(CH 2 ) r OC (O) R 6 ,-(CH 2 ) r C (O) R 2 ,-(CH 2 ) r C (O) R 6 ,-(CH 2 ) r C (O) N (R 2 ) (R 2 ),-(CH 2 ) r C (O) N (R 2 ) (R 6 ),-(CH 2 ) r N (R 2 ) C (O) R 2 ,-( CH 2 ) r N (R 2 ) C (O) R 6 ,-(CH 2 ) r N (R 6 ) C (O) R 2 ,-(CH 2 ) r N (R 6 ) C (O) R 6 ,-(CH 2 ) r N (R 2 ) C (O) OR 2 ,-(CH 2 ) r N (R 2 ) C (O) OR 6 ,-(CH 2 ) r N (R 6 ) C (O) OR 2 ,-(CH 2 ) r N (R 6 ) C (O) OR 6 ,-(CH 2 ) r N (R 2 ) C (O) N (R 2 ) (R 6 ),- (CH 2 ) r N (R 2 ) C (O) N (R 2 ) (R 2 ),-(CH 2 ) r N (R 6 ) C (O) N (R 2 ) (R 6 ), ( CH 2 ) r N (R 2 ) SO 2 R 6 ,-(CH 2 ) r N (R 2 ) SO 2 R 2 ,-(CH 2 ) r N (R 6 ) SO 2 R 2 , (CH 2 ) r N (R 6 ) SO 2 R 6 ,-(CH 2 ) r OC (O) N (R 2 ) (R 6 ),-(CH 2 ) r OC (O) N (R 2 ) (R 2 ),-(CH 2 ) r SO 2 N (R 2 ) (R 6 ) ,-(CH 2 ) r SO 2 N (R 2 ) (R 2 ),-(CH 2 ) r SO 2 NHC (O) R 6 ,-(CH 2 ) r SO 2 NHC (O) R 2 ,- (CH 2 ) r SO 2 NHC (O) OR 6 ,-(CH 2 ) r SO 2 NHC (O) OR 2 , (CH 2 ) r CONHSO 2 R 6 ,-(CH 2 ) r CONHSO 2 R 2 , Phenyl which may be substituted at the ortho position by a substituent selected from the group consisting of-(CH 2 ) r S (O) m R 6 , and-(CH 2 ) r S (O) m R 2 , R 3a is hydrogen, Or C 1 -C 4 alkyl, X is hydrogen, 로 이루어진 그룹 중에서 선택되고, Y는 수소, C1-C8알킬, (CH2)t아릴, -(CH2)qC5-C7사이클로알킬, -(CH2)q-K-(C1-C6알킬), -(CH2)q-K-(CH2)t아릴 또는 -(CH2)q-K-(CH2)t(C5-C6사이클로알킬)로 이루어진 그룹 중에서 선택되고, 여기서 K는 S(O)m이고, 알킬 그룹은 하이드록실, 카복실, CONH2, 카복실레이트 C1-C4알킬 에스테르 또는 1H-테트라졸-5-일에 의해 치환될 수 있고, 아릴은 특정하게는 1 내지 2개의 할로겐, 1 내지 2개의 OR2, -CO(OR2), 1 내지 2개의 C1-C4알킬, S(O)mR2또는 1H-테트라졸-5-일에 의해 치환될 수 있는, 페닐, 나프틸, 피리딜, 티아졸릴, 티오펜일, 피라졸릴, 옥사졸릴, 이속사졸릴, 티아디아졸릴, 피리미디닐 또는 이미다졸릴이고, A는And Y is hydrogen, C 1 -C 8 alkyl, (CH 2 ) t aryl,-(CH 2 ) q C 5 -C 7 cycloalkyl,-(CH 2 ) q -K- (C 1 -C 6 alkyl),-(CH 2 ) q -K- (CH 2 ) t aryl or-(CH 2 ) q -K- (CH 2 ) t (C 5 -C 6 cycloalkyl) Wherein K is S (O) m and the alkyl group may be substituted by hydroxyl, carboxyl, CONH 2 , carboxylate C 1 -C 4 alkyl ester or 1H-tetrazol-5-yl, aryl Is specifically 1 to 2 halogens, 1 to 2 OR 2 , -CO (OR 2 ), 1 to 2 C 1 -C 4 alkyl, S (O) m R 2 or 1H-tetrazol-5- Phenyl, naphthyl, pyridyl, thiazolyl, thiophenyl, pyrazolyl, oxazolyl, isoxazolyl, thiadiazolyl, pyrimidinyl or imidazolyl, which may be substituted by one, and A is 로 이루어진 그룹 중에서 선택되고, R4및 R5는 독립적으로 -H, -CH3, -CH2CH3,로 이루어진 그룹 중에서 선택되고, R6은 수소, C1-C6알킬 또는 (CH2)v아릴이고, 여기서 알킬 및 (CH2)v그룹은 할로겐, OR2, N(R2)(R2), C3-C6사이클로알킬, 1H-테트라졸-5-일, C(O)OR2, C(O)N(R2)(R2), SO2N(R2)(R2) 또는 N(R2)C(O)N(R2)(R2)에 의해 치환될 수 있고, 아릴은 방향족 그룹인It is selected from the group consisting of, R 4 and R 5 are independently -H, -CH 3 , -CH 2 CH 3 , And Is selected from the group consisting of R 6 is hydrogen, C 1 -C 6 alkyl or (CH 2 ) v aryl, wherein the alkyl and (CH 2 ) v group is halogen, OR 2 , N (R 2 ) (R 2 ), C 3 -C 6 cycloalkyl, 1H-tetrazol-5-yl, C (O) OR 2 , C (O) N (R 2 ) (R 2 ), SO 2 N (R 2 ) (R 2 ) Or N (R 2 ) C (O) N (R 2 ) (R 2 ), where aryl is an aromatic group 및 이들의 레지오이성체 중에서 선택되고, 이들 방향족 그룹은 C1-C2알킬, N(R2)(R2) 또는 하이드록시에 의해 치환될 수 있고, m 은 0, 1 또는 2이고, r은 0, 1, 2 또는 3이고, q는 0 또는 1이고, t는 0 또는 1이고, v는 0 또는 1이다.And their regioisomers, these aromatic groups can be substituted by C 1 -C 2 alkyl, N (R 2 ) (R 2 ) or hydroxy, m is 0, 1 or 2, r is 0, 1, 2 or 3, q is 0 or 1, t is 0 or 1 and v is 0 or 1. 제7항에 있어서, 다음 일반식의 입체특이적으로 정의된 화합물.8. The compound according to claim 7, wherein the stereospecific definition of the general formula 상기식에서, R1, R3, R4, R5, A, X, Y 및 n은 제7항에서 정의한 바와 같다.Wherein R 1 , R 3 , R 4 , R 5 , A, X, Y and n are as defined in claim 7. 제7항에 있어서,The method of claim 7, wherein 으로 이루어진 그룹 중에서 선택된 화합물, 및 이의 약제학적으로 허용되는 염 및 개별적인 부분입체이성체.Compounds selected from the group consisting of, and pharmaceutically acceptable salts and individual diastereomers thereof. 다음 일반식(CI)의 화합물, 및 이의 약제학적으로 허용되는 염 및 개별적인 부분입체이성체.The compounds of formula (CI) and pharmaceutically acceptable salts and individual diastereomers thereof. 상기식에서, R1은 C1-C10알킬, 아릴, 아릴(C1-C6알킬), (C3-C7사이클로알킬)(C1-C6알킬)-, (C1-C5알킬)-K-(C1-C5알킬)-, 아릴(C0-C5알킬)-K(C1-C5알킬)-, 및 (C3-C7사이클로알킬)(C1-C5알킬)-K-(C1-C5알킬)-로 이루어진 그룹 중에서 선택되며, 여기서 K는 O, S(O)m, N(R2)C(O), C(O)N(R2), OC(O), C(O)O, -CR2=CR2-, 또는 -C≡C- 이고, 아릴은 페닐, 나프틸, 인돌릴, 아자인돌, 피리딜, 벤조티에닐, 벤조푸라닐, 티아졸릴 및 벤즈이미다졸릴 중에서 선택되고, R2및 알킬은 1 내지 9개의 할로겐, S(O)mR2a1 내지 3개의 OR2a또는 C(O)OR2a에 의해 추가로 치환될 수 있고, 아릴은 1 내지 3개의 C1-C6알킬, 1 내지 3개의 할로겐, 1 내지 2개의 OR2, 메틸렌디옥시, -S(O)mOR2, 1 내지 2개의 -CF3, -OCF3, 니트로, -N(R2)C(O)(R2), -C(O)OR2, -C(O)N(R2)(R2), -1H-테트라졸-5-일, -SO2N(R2)(R2), -N(R2)SO2페닐, 또는 -N(R2)SO2R2에 의해 추가로 치환될 수 있고, R2는 수소, C1-C6알킬 및 C3-C7사이클로알킬 중에서 선택되고, 2개의 C1-C6알킬 그룹이 한 원자에 존재하는 경우, 이들은 함께 결합하여 산소, 황 또는 NR3a를 포함할 수 있는 C3-C8사이클릭 환을 형성할 수도 있고, R3a는 수소, 또는 하이드록실에 의해 치환될 수 있는 C1-C6알킬이고, R2a는 수소, 또는 하이드록실에 의해 치환될 수 있는 C1-C6알킬이고, X는 수소, -C≡N, -(CH2)qN(R2)C(O)R2, -(CH2)qN(R2)C(O)(CH2)t아릴, -(CH2)qN(R2)SO2(CH2)t아릴, -(CH2)qN(R2)SO2R2, -(CH2)qN(R2)C(O)N(R2)(CH2)t아릴, -(CH2)qN(R2)C(O)N(R2)(R2), -(CH2)qC(O)N(R2)(R2), -(CH2)qC(O)N(R2)(CH2)t아릴, -(CH2)qC(O)OR2, -(CH2)qC(O)O(CH2)t아릴, -(CH2)qOR2, -(CH2)qOC(O)R2, -(CH2)qOC(O)(CH2)t아릴, -(CH2)qOC(O)N(R2)(CH2)t아릴, -(CH2)qOC(O)N(R2)(R2), -(CH2)qC(O)R2, -(CH2)qC(O)(CH2)t아릴, -(CH2)qN(R2)C(O)OR2, -(CH2)qN(R2)SO2N(R2)(R2), -(CH2)qS(O)mR2, 및 -(CH2)qS(O)m(CH2)t아릴로 이루어진 그룹 중에서 선택되고, 여기서 R2, (CH2)q및 (CH)t그룹은 1 내지 2개의 C1-C4알킬, 하이드록실, C1-C4저급 알콕시, 카복실, CONH2, S(O)mCH3, 카복실레이트 C1-C4알킬 에스테르, 또는 1H-테트라졸-5-일에 의해 치환될 수도 있고, 아릴은 1 내지 3개의 할로겐, 1 내지 3개의 -OR2, -CON(R2)(R2), -C(O)OR2, 1 내지 3개의 C1-C4알킬, S(O)mR2또는 1H-테트라졸-5-일에 의해 치환될 수도 있는, 페닐, 나프틸, 피리딜, 티아졸릴 또는 1H-테트라졸-5-일 그룹이고, Y는 수소, C1-C10알킬, -(CH2)t아릴, (CH2)q(C3-C7사이클로알킬), -(CH2)q-K-(C1-C6알킬), -(CH2)q-K-(CH2)t아릴, -(CH2)q-K-(CH2)t(O,NR2또는 S 함유 C3-C7사이클로알킬), 및 -(CH2)q-K-(CH2)t(C3-C7사이클로알킬)중에서 선택되고, 여기서 K는 O, S(O)m, C(O)NR2, CH=CH, C≡C, N(R2)C(O), C(O)NR2, C(O)O, 또는 OC(O)이고, 알킬, R2, (CH2)q및 (CH2)t그룹은 C1-C4알킬, 하이드록실, C1-C4저급 알콕시, 카복실, -CONH2,또는 카복실레이트 C1-C4알킬 에스테르에 의해 치환될 수도 있고, 아릴은 1 내지 3개의 할로겐, 1 내지 3개의 -OR2, -C(O)OR2, -C(O)N(R2)(R2), 니트로, 시아노, 벤질, 1 내지 3개의 C1-C4알킬, S(O)mR2또는 1H-테트라졸-5-일에 의해 치환될 수 있는, 페닐, 나프틸, 피리딜, 1H-테트라졸-5-일, 티아졸릴, 이미다졸릴, 인돌릴, 피리미디닐, 티아디아졸릴, 피라졸릴, 옥사졸릴, 이속사졸릴, 티오펜일, 퀴놀리닐, 피라지닐 또는 이소티아졸릴이고, 단 X가 수소인 경우 Y는 수소가 아니고, R4및 R5는 독립적으로 수소, C1-C6알킬, 또는 1 내지 5개의 할로, 1 내지 3개의 하이드록시, 1 내지 3개의 C1-C10알카노일옥시, 1 내지 3개의 C1-C6알콕시, 페닐, 페닐옥시, 2-푸릴, C1-C6알콕시카보닐 또는 S(O)m(C1-C6알킬)에 의해 치환된 C1-C6알킬이거나, R4및 R5는 함께 결합하여 -C(H2)d-La(CH2)e-(여기서, La는 -C(R2)2-, O, S(O)m또는 N(R2)이고, d 및 e 는 독립적으로 1 내지 3이고, R2는 상술한 바와 같다)를 형성하고,Wherein R 1 is C 1 -C 10 alkyl, aryl, aryl (C 1 -C 6 alkyl), (C 3 -C 7 cycloalkyl) (C 1 -C 6 alkyl)-, (C 1 -C 5 Alkyl) -K- (C 1 -C 5 alkyl)-, aryl (C 0 -C 5 alkyl) -K (C 1 -C 5 alkyl)-, and (C 3 -C 7 cycloalkyl) (C 1- C 5 alkyl) -K- (C 1 -C 5 alkyl)-, wherein K is O, S (O) m , N (R 2 ) C (O), C (O) N ( R 2 ), OC (O), C (O) O, -CR 2 = CR 2- , or -C≡C-, where aryl is phenyl, naphthyl, indolyl, azaindole, pyridyl, benzothienyl , Benzofuranyl, thiazolyl and benzimidazolyl, R 2 and alkyl are further selected from 1 to 9 halogen, S (O) mR 2a 1 to 3 OR 2a or C (O) OR 2a Aryl may be substituted with 1 to 3 C 1 -C 6 alkyl, 1 to 3 halogens, 1 to 2 OR 2 , methylenedioxy, —S (O) m OR 2 , 1 to 2 —CF 3 , -OCF 3 , nitro, -N (R 2 ) C (O) (R 2 ), -C (O) OR 2 , -C (O) N (R 2 ) (R 2 ), -1H-tetra Sol-5-yl, -SO 2 N (R 2 ) (R 2 ), —N (R 2 ) SO 2 phenyl, or —N (R 2 ) SO 2 R 2 , wherein R 2 is hydrogen, C 1 -C 6 alkyl and C 3 − When selected from C 7 cycloalkyl and two C 1 -C 6 alkyl groups are present at one atom, they can be joined together to form a C 3 -C 8 cyclic ring which may comprise oxygen, sulfur or NR 3a Or R 3a is hydrogen or C 1 -C 6 alkyl which may be substituted by hydroxyl, R 2a is hydrogen or C 1 -C 6 alkyl which may be substituted by hydroxyl, and X is Hydrogen, -C≡N,-(CH 2 ) q N (R 2 ) C (O) R 2 ,-(CH 2 ) q N (R 2 ) C (O) (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) SO 2 (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) SO 2 R 2 ,-(CH 2 ) q N (R 2 ) C (O) N ( R 2 ) (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) C (O) N (R 2 ) (R 2 ),-(CH 2 ) q C (O) N (R 2 ) (R 2 ),-(CH 2 ) q C (O) N (R 2 ) (CH 2 ) t aryl,-(CH 2 ) q C (O) OR 2 ,-(CH 2 ) q C (O) O (CH 2 ) t aryl,-(CH 2 ) q OR 2 ,-(CH 2 ) q OC (O) R 2 ,-(CH 2 ) q OC (O) (CH 2 ) t aryl,-(CH 2 ) q OC (O) N (R 2 ) (CH 2 ) t aryl,-(CH 2 ) q OC (O) N (R 2 ) (R 2 ),- (CH 2 ) q C (O) R 2 ,-(CH 2 ) q C (O) (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) C (O) OR 2 ,-(CH 2 ) q N (R 2 ) SO 2 N (R 2 ) (R 2 ),-(CH 2 ) q S (O) m R 2 , and-(CH 2 ) q S (O) m (CH 2 ) t aryl, wherein the R 2 , (CH 2 ) q and (CH) t groups are 1 to 2 C 1 -C 4 alkyl, hydroxyl, C 1 -C 4 lower alkoxy, carboxyl, CONH 2 , S (O) m CH 3 , carboxylate C 1 -C 4 alkyl ester, or 1H-tetrazol-5-yl, wherein aryl is 1 to 3 halogens, 1 to 3 -OR 2 , -CON (R 2 ) (R 2 ), -C (O) OR 2 , by 1 to 3 C 1 -C 4 alkyl, S (O) m R 2 or 1H-tetrazol-5-yl Phenyl, naphthyl, pyridyl, thiazolyl or 1H-tetrazol-5-yl group, which may be substituted, Y is hydrogen, C 1 -C 10 alkyl, — (CH 2 ) t aryl, (CH 2 ) q (C 3 -C 7 cycloalkyl), - (CH 2) q -K- (C 1 -C 6 al ), - (CH 2) q -K- (CH 2) t aryl, - (CH 2) q -K- (CH 2) t (O, NR 2 , or S-containing C 3 -C 7 cycloalkyl), and -(CH 2 ) q -K- (CH 2 ) t (C 3 -C 7 cycloalkyl) wherein K is O, S (O) m , C (O) NR 2 , CH = CH, C ≡C, N (R 2 ) C (O), C (O) NR 2 , C (O) O, or OC (O) and are alkyl, R 2 , (CH 2 ) q and (CH 2 ) t groups May be substituted by C 1 -C 4 alkyl, hydroxyl, C 1 -C 4 lower alkoxy, carboxyl, -CONH 2 , or carboxylate C 1 -C 4 alkyl ester, aryl being 1 to 3 halogen, 1 to 3 -OR 2 , -C (O) OR 2 , -C (O) N (R 2 ) (R 2 ), nitro, cyano, benzyl, 1 to 3 C 1 -C 4 alkyl, S (O) phenyl, naphthyl, pyridyl, 1H-tetrazol-5-yl, thiazolyl, imidazolyl, indolyl, pyri, which may be substituted by m R 2 or 1H-tetrazol-5-yl Midinyl, thiadiazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiophenyl, quinolinyl, pyrazinyl or isothiazolyl, Provided that when X is hydrogen, Y is not hydrogen, and R 4 and R 5 are independently hydrogen, C 1 -C 6 alkyl, or 1 to 5 halo, 1 to 3 hydroxy, 1 to 3 C 1 − By C 10 alkanoyloxy, 1 to 3 C 1 -C 6 alkoxy, phenyl, phenyloxy, 2-furyl, C 1 -C 6 alkoxycarbonyl or S (O) m (C 1 -C 6 alkyl) Substituted C 1 -C 6 alkyl, or R 4 and R 5 are bonded together to form —C (H 2 ) d—La (CH 2 ) e —, wherein La is —C (R 2 ) 2 —, O, S (O) m or N (R 2 ), d and e are independently 1 to 3, R 2 is as described above), 이고, 여기서 x 및 y는 독립적으로 0, 1, 2 또는 3이고, Z는 N-R6a또는 0이고, 여기서 R6a는 수소 또는 C1-C6알킬이고, R7및 R7a는 독립적으로 수소, C1-C6알킬, 트리플루오로메틸, 페닐, 또는 이미다졸릴, 페닐, 인돌릴, p-하이드록시페닐, O(R2), S(O)mR2, C(O)O(R2), C3-C7사이클로알킬, N(R2)(R2), C(O)N(R2)(R2)에 의해 치환된 C1-C6알킬이거나, R7및 R7a는 독립적으로 R4및 R5그룹 중의 하나 또는 이들 둘다와 결합하여 R7또는 R7a그룹의 말단 질소와 알킬 부분사이에 탄소수 1 내지 5의 알킬렌 브릿지를 형성하거나, R7및 R7a는 서로 결합하여 C3-C7사이클로알킬을 형성할 수 있고, m 은 0, 1 또는 2이고, n 은 1, 2 또는 3이고, g 는 0, 1, 2, 3 또는4이고, t는 0, 1, 2 또는 3이다.Wherein x and y are independently 0, 1, 2 or 3, Z is NR 6a or 0, wherein R 6a is hydrogen or C 1 -C 6 alkyl, and R 7 and R 7a are independently hydrogen, C 1 -C 6 alkyl, trifluoromethyl, phenyl, or imidazolyl, phenyl, indolyl, p-hydroxyphenyl, O (R 2 ), S (O) m R 2 , C (O) O ( R 2 ), C 3 -C 7 cycloalkyl, N (R 2 ) (R 2 ), C 1 -C 6 alkyl substituted by C (O) N (R 2 ) (R 2 ), or R 7 and R 7a is independently bonded to one or both of the R 4 and R 5 groups to form an alkylene bridge having 1 to 5 carbon atoms between the terminal nitrogen and the alkyl moiety of the R 7 or R 7a group, or R 7 and R 7a May combine with each other to form C 3 -C 7 cycloalkyl, m is 0, 1 or 2, n is 1, 2 or 3, g is 0, 1, 2, 3 or 4, and t is 0, 1, 2 or 3. 제13항에 있어서, R1은 C1-C10알킬, 아릴( C1-C4알킬)-, C3-C6사이클로알킬( C1-C4알킬)-, ( C1-C4알킬)-K-( C1-C4알킬)-, 아릴( C0-C2알킬)-K-( C1-C2알킬)-, 및 (C3-C7사이클로알킬)( C0-C2알킬)-K-( C1-C2알킬)-로 이루어진 그룹 중에서 선택되며, 여기서 K은 O, S(O)m, OC(O) 또는 C(O)O이고, 알킬그룹이 1 내지 7개의 할로겐, S(O)mR2, 1 내지 3개의 OR2또는 C(O)OR2에 의해 추가로 치환될 수 있고, 아릴은 1 내지 2개의 C1-C4알킬, 1 내지 2개의 할로겐, 1 내지 2개의 -OR2, -S(O)mR2,또는 -C(O)OR2에 의해 추가로 치환될 수 있는 페닐, 나프틸, 인돌릴, 피리딜, 벤즈이미다졸릴, 아자인돌레일, 벤조티에닐 또는 벤조푸라닐이고, R2가 수소, C1-C6알킬, 또는 C3-C7사이클로알킬이고, 2개의 C1-C6알킬 그룹이 한 원자에 존재하는 경우, 이들은 함께 결합하여 산소, 황 또는 NR3a를 포함할 수 있는 C4-C7사이클릭 환을 형성할 수도 있고, R3a가 수소, 또는 C1-C4알킬이고, X가 수소, -(CH2)qN(R2)C(O)R2, -(CH2)qN(R2)C(0)(CH2)t아릴, -(CH2)qN(R2)C(0)OR2, -(CH2)qN(R2)SO2(CH2)t아릴, -(CH2)qN(R2)SO2R2, -(CH2)qN(R2)C(O)N(R2)(CH2)t아릴, -(CH2)qN(R2)C(O)N(R2)(R2), -(CH2)qC(O)N(R2)(R2), -(CH2)qC(O)N(R2)(CH2)t아릴, -(CH2)qC(O)OR2, -(CH2)qC(O)O(CH2)t아릴, -(CH2)qOC(O)R2, -(CH2)qOC(O)(CH2)t아릴, -(CH2)qS(O)mR2, 및 -(CH2)qS(O)m(CH2)t아릴중에서 선택되고, 여기서 R2그룹은 하이드록실, 카복실, CONH2, S(O)mCH3, 카복실레이트 C1-C4알킬 에스테르, 또는 테트라졸에 의해 치환될 수 있고, 아릴은 1 내지 2개의 할로겐, 1 내지 2개의 -OR2, -CONH2, -C(O)OR2, 1 내지 3개의 C1-C4알킬, -S(O)mR2또는 1H-테트라졸-5-일에 의해 치환될 수 있는, 페닐, 나프틸, 피리딜 또는 1-H-테트라졸릴이고, Y가 수소, C1-C8알킬, -(CH2)t아릴, -(CH2)q(C5-C6사이클로알킬), -(CH2)q-K-(C1-C6알킬), -(CH2)q-K-(CH2)t아릴, -(CH2)q-K-(CH2)t(O,NR2또는 S 함유 C3-C7사이클로알킬), 및 -(CH2)q-K-(CH2)t(C5-C6사이클로알킬)중에서 선택되고, 여기서 K는 O 또는 S(O)m이고, 알킬 그룹은 하이드록실, 카복실, -CONH2, 카복실레이트 C1-C4알킬 에스테르 또는 1H-테트라졸-5-일에 의해 치환될 수도 있고, 아릴은 페닐, 나프틸, 피리딜, 1-H-테트라졸릴, 티아졸릴, 이미다졸릴, 인돌릴, 피리미디닐, 티아디아졸릴, 피라졸릴, 옥사졸릴, 이속사졸릴 또는 티오펜일이고, 이는 1 내지 3개의 할로겐, 1 내지 3개의 -OR2, -C(O)OR2, -C(O)N(R2)(R2), 시아노, 1 내지 2개의 C1-C4알킬, 벤질, -S(O)mR2또는 1H-테트라졸-5-일에 의해 치환될 수 있고, 단 X가 수소인 경우, Y는 수소가 아니며, R4및 R5가 독립적으로 수소, C1-C6알킬 또는 1 내지 5개의 할로, 1 내지 3개의 하이드록실, S(O)m(C1-C6알킬) 또는 페닐에 치환된 C1-C6알킬이고, A가이고, 여기서 x는 0 또는 1이고, R7및 R7a가 독립적으로 수소, C1-C6알킬, 트리플루오로메틸, 페닐, 또는 이미다졸릴, 페닐, 인돌릴, p-하이드록시페닐, OR2, S(O)mR2, C(O)O(R2), C5-C7사이클로알킬, -N(R2)(R2), -C(O)N(R2)(R2)에 의해 치환된 C1-C6알킬이거나, R7및 R7a가 독립적으로 R4및 R5중의 하나와 결합하여 R7및 R7a그룹의 말단 질소와 알킬 부분 사이에 알킬렌 브릿지를 형성하여 5원 또는 6원 환을 형성하거나, R7및 R7a가 서로 결합하여 C3사이클로알킬을 형성하고, n이 2이고, m 이 0, 1 또는 2이고, q가 0, 1, 2 또는 3이고, t가 0, 1, 2 또는 3인 화합물, 및 이의 약제학적으로 허용되는 염 및 개별적인 부분입체이성체.The compound of claim 13, wherein R 1 is C 1 -C 10 alkyl, aryl (C 1 -C 4 alkyl)-, C 3 -C 6 cycloalkyl (C 1 -C 4 alkyl)-, (C 1 -C 4 Alkyl) -K- (C 1 -C 4 alkyl)-, aryl (C 0 -C 2 alkyl) -K- (C 1 -C 2 alkyl)-, and (C 3 -C 7 cycloalkyl) (C 0 -C 2 alkyl) -K- (C 1 -C 2 alkyl)-, wherein K is O, S (O) m , OC (O) or C (O) O, and the alkyl group is May be further substituted by 1 to 7 halogens, S (O) m R 2 , 1 to 3 OR 2 or C (O) OR 2 , with aryl being 1 to 2 C 1 -C 4 alkyl, 1 Phenyl, naphthyl, indolyl, pyridyl, benz which may be further substituted by from 2 to 2 halogens, 1 to 2 -OR 2 , -S (O) m R 2 , or -C (O) OR 2 Imidazolyl, azaindoleyl, benzothienyl or benzofuranyl, R 2 is hydrogen, C 1 -C 6 alkyl, or C 3 -C 7 cycloalkyl, and two C 1 -C 6 alkyl groups When present in an atom, they are bonded together Cattle, and sulfur, which may include NR 3a C 4 -C 7 may form a cyclic ring, R 3a is hydrogen, or C 1 -C 4 alkyl, X is hydrogen, - (CH 2) q N (R 2 ) C (O) R 2 ,-(CH 2 ) q N (R 2 ) C (0) (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) C (0) OR 2 ,-(CH 2 ) q N (R 2 ) SO 2 (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) SO 2 R 2 ,-(CH 2 ) q N (R 2 ) C ( O) N (R 2 ) (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) C (O) N (R 2 ) (R 2 ),-(CH 2 ) q C (O) N (R 2 ) (R 2 ),-(CH 2 ) q C (O) N (R 2 ) (CH 2 ) t aryl,-(CH 2 ) q C (O) OR 2 ,-(CH 2 ) q C (O) O (CH 2 ) t aryl,-(CH 2 ) q OC (O) R 2 ,-(CH 2 ) q OC (O) (CH 2 ) t aryl,-(CH 2 ) q S ( O) m R 2 , and — (CH 2 ) q S (O) m (CH 2 ) t aryl, wherein the R 2 group is hydroxyl, carboxyl, CONH 2 , S (O) m CH 3 , carboxyl May be substituted by a rate C 1 -C 4 alkyl ester, or tetrazole, aryl being 1 to 2 halogens, 1 to 2 —OR 2 , —CONH 2 , —C (O) OR 2 , 1 to 3 one C 1 -C 4 alkyl, -S (O) m R 2 or 1H- Tra and sol-5-yl which may be substituted by phenyl, naphthyl, pyridyl or 1-H- tetrazolyl, Y is hydrogen, C 1 -C 8 alkyl, - (CH 2) t aryl, - ( CH 2 ) q (C 5 -C 6 cycloalkyl),-(CH 2 ) q -K- (C 1 -C 6 alkyl),-(CH 2 ) q -K- (CH 2 ) t aryl,-( CH 2) q -K- (CH 2 ) t (O, NR 2 , or S-containing C 3 -C 7 cycloalkyl), and - (CH 2) q -K- ( CH 2) t (C 5 -C 6 Cycloalkyl), where K is O or S (O) m and the alkyl group is hydroxyl, carboxyl, -CONH 2 , carboxylate C 1 -C 4 alkyl ester or 1H-tetrazol-5-yl And aryl may be substituted by phenyl, naphthyl, pyridyl, 1-H-tetrazolyl, thiazolyl, imidazolyl, indolyl, pyrimidinyl, thiadiazolyl, pyrazolyl, oxazolyl, isoxazolyl Or thiophenyl, which is 1 to 3 halogens, 1 to 3 -OR 2 , -C (O) OR 2 , -C (O) N (R 2 ) (R 2 ), cyano, 1 to 2 C 1 -C 4 alkyl, benzyl, -S (O) m R 2 or 1H-tetrazol-5-yl, provided that when X is hydrogen, Y is not hydrogen and R 4 and R 5 are independently hydrogen, C 1 -C 6 alkyl or 1 to 5 Halo, 1 to 3 hydroxyl, S (O) m (C 1 -C 6 alkyl) or C 1 -C 6 alkyl substituted with phenyl, A is Wherein x is 0 or 1, and R 7 and R 7a are independently hydrogen, C 1 -C 6 alkyl, trifluoromethyl, phenyl, or imidazolyl, phenyl, indolyl, p-hydroxyphenyl, OR 2 , S (O) m R 2 , C (O) O (R 2 ), C 5 -C 7 cycloalkyl, -N (R 2 ) (R 2 ), -C (O) N (R 2 ) C 1 -C 6 alkyl substituted by (R 2 ) or R 7 and R 7a are independently bonded to one of R 4 and R 5 to form an alkylene between the terminal nitrogen and the alkyl moiety of the R 7 and R 7a groups Form a bridge to form a five or six membered ring, or R 7 and R 7a combine with each other to form C 3 cycloalkyl, n is 2, m is 0, 1 or 2, q is 0, 1 , 2 or 3, and t is 0, 1, 2 or 3, and pharmaceutically acceptable salts and individual diastereomers thereof. 제13항에 있어서, 다음 일반식(CIb)의 화합물, 및 이의 약제학적으로 허용되는 염 및 개별적인 부분입체이성체.A compound according to claim 13, wherein the compound of formula (CIb), and a pharmaceutically acceptable salt and individual diastereomer thereof. 상기식에서, R1은 C1-C10알킬, 아릴( C1-C3알킬)-, (C3-C7사이클로알킬)( C1-C3알킬)-, 및 아릴( C0-C1알킬)-K-( C1-C2알킬)-로 이루어진 그룹 중에서 선택되고, 여기서 K는 O, S(O)m이고, 아릴은 1 내지 2개의 C1-C4알킬, 1 내지 2개의 할로겐, 1 내지 2개의 OR2, S(O)mR2,또는 C(O)OR2에 의해 치환될 수 있는 페닐, 피리딜, 나프틸, 인돌릴, 아자인돌릴 또는 벤즈이미다졸릴이고, R2는 수소, C1-C6알킬, 또는 C3-C7사이클로알킬이고, 2개의 C1-C6알킬 그룹이 한 원자에 존재하는 경우, 이들은 함께 결합하여 산소, 황 또는 NR3a를 포함할 수 있는 C5-C7사이클릭 환을 형성할 수도 있고, R3a는 수소, 또는 C1-C4알킬이고, X는 수소, -(CH2)qN(R2)C(O)R2, -(CH2)qN(R2)C(0)(CH2)t아릴, -(CH2)qN(R2)SO2(CH2)t아릴, -(CH2)qN(R2)SO2R2, -(CH2)qN(R2)C(O)N(R2)(CH2)t아릴, -(CH2)qN(R2)C(O)N(R2)(R2), -(CH2)qC(O)N(R2)(R2), -(CH2)qN(R2)C(O)OR2, -(CH2)qC(O)N(R2)(CH2)t아릴, -(CH2)qC(O)0R2, -(CH2)qC(O)0(CH2)t아릴, -(CH2)q0C(O)R2, -(CH2)q0C(O)(CH2)t아릴, -(CH2)qS(O)mR2, 및 -(CH2)qS(O)m(CH2)t아릴중에서 선택되고, R2그룹은 하이드록실, 카복실, CONH2, S(O)mCH3, 카복실레이트 C1-C4알킬 에스테르, 또는 테트라졸에 의해 치환될 수 있고, 아릴은 페닐, 나프틸 또는 피리딜이고, 이는 추가로 1 내지 2개의 할로겐, 1 내지 2개의 OR2, C(O)OR2, 1 내지 3개의 C1-C4알킬, S(O)mR2또는 1H-테트라졸-5-일에 의해 치환될 수 있고, Y는 수소, C1-C8알킬, (CH2)t아릴, -(CH2)qC5-C7사이클로알킬, -(CH2)q-K-(C1-C6알킬), -(CH2)q-K-(CH2)t아릴 및 -(CH2)q-K-(CH2)t(C5-C6사이클로알킬)중에서 선택되고, 여기서 K는 S(O)m이고, 알킬 그룹은 하이드록실, 카복실, CONH2, 카복실레이트 C1-C4알킬 에스테르 또는 1H-테트라졸-5-일에 의해 치환될 수 있고, 아릴은 1 내지 2개의 할로겐, 1 내지 2개의 OR2, 1 내지 2개의 -N(R2)(R2), CO(OR2), 1 내지 2개의 C1-C4알킬, S(O)mR2또는 1H-테트라졸-5-일에 의해 치환될 수 있는, 페닐, 나프틸, 피리딜, 티아졸릴, 티오펜일, 피라졸릴, 옥사졸릴, 이속사졸릴 또는 이미다졸릴이고, 단 X가 수소이면 Y는 수소가 아니고, R4및 R5는 독립적으로 수소, C1-C4알킬 또는 1 내지 2개의 하이드록실에 의해 치환된 C1-C3알킬이고, A는이고, 여기서 x는 0 또는 1이고, R7및 R7a는 독립적으로 수소, C1-C6알킬, 페닐, 또는 이미다졸릴, 페닐, 인돌릴, p-하이드록시페닐, OR2, 또는 S(O)mR2에 의해 치환된 C1-C6알킬이거나, R7및 R7a는 독립적으로 서로 결합하여 C3사이클로알킬을 형성하고, m 은 0, 1 또는 2이고, q는 0, 1, 2 또는 3이고, t는 0, 1, 2 또는 3이다.Wherein R 1 is C 1 -C 10 alkyl, aryl (C 1 -C 3 alkyl)-, (C 3 -C 7 cycloalkyl) (C 1 -C 3 alkyl)-, and aryl (C 0 -C 1 alkyl) -K- (C 1 -C 2 alkyl)-, wherein K is O, S (O) m and aryl is 1 to 2 C 1 -C 4 alkyl, 1 to 2 Phenyl, pyridyl, naphthyl, indolyl, azaindoleyl or benzimidazolyl, which may be substituted by 1 halogen, 1 or 2 OR 2 , S (O) m R 2 , or C (O) OR 2 R 2 is hydrogen, C 1 -C 6 alkyl, or C 3 -C 7 cycloalkyl, and when two C 1 -C 6 alkyl groups are present at one atom, they are bonded together to form oxygen, sulfur or NR 3a can be C 5 -C 7 may form a cyclic ring, which comprise a, R 3a is hydrogen, or C 1 -C 4 alkyl, X is hydrogen, - (CH 2) q N (R 2) C (O) R 2 ,-(CH 2 ) q N (R 2 ) C (0) (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) SO 2 (CH 2 ) t aryl,-( CH 2 ) q N (R 2 ) SO 2 R 2 ,-(CH 2 ) q N (R 2 ) C (O) N ( R 2 ) (CH 2 ) t aryl,-(CH 2 ) q N (R 2 ) C (O) N (R 2 ) (R 2 ),-(CH 2 ) q C (O) N (R 2 ) (R 2 ),-(CH 2 ) q N (R 2 ) C (O) OR 2 ,-(CH 2 ) q C (O) N (R 2 ) (CH 2 ) t aryl,-(CH 2 ) q C (O) 0R 2 ,-(CH 2 ) q C (O) 0 (CH 2 ) t aryl,-(CH 2 ) q 0C (O) R 2 ,-(CH 2 ) q 0C (O) ( CH 2 ) t aryl, — (CH 2 ) q S (O) m R 2 , and — (CH 2 ) q S (O) m (CH 2 ) t aryl, R 2 group being hydroxyl, carboxyl , CONH 2 , S (O) m CH 3 , carboxylate C 1 -C 4 alkyl ester, or tetrazole, wherein aryl is phenyl, naphthyl or pyridyl, which is further 1 to 2 May be substituted by halogen, 1 to 2 OR 2 , C (O) OR 2 , 1 to 3 C 1 -C 4 alkyl, S (O) m R 2 or 1H-tetrazol-5-yl, Y is hydrogen, C 1 -C 8 alkyl, (CH 2 ) t aryl,-(CH 2 ) q C 5 -C 7 cycloalkyl,-(CH 2 ) q -K- (C 1 -C 6 alkyl), - (CH 2) q -K- ( CH 2) t aryl, and - (CH 2) q -K- ( CH 2) t is selected from (C 5 -C 6 cycloalkyl), where Wherein K is S (O) m , the alkyl group may be substituted by hydroxyl, carboxyl, CONH 2 , carboxylate C 1 -C 4 alkyl ester or 1H-tetrazol-5-yl, and aryl is 1 to 2 halogens, 1 or 2 OR 2 , 1 or 2 —N (R 2 ) (R 2 ), CO (OR 2 ), 1 or 2 C 1 -C 4 alkyl, S (O) m R 2 Or phenyl, naphthyl, pyridyl, thiazolyl, thiophenyl, pyrazolyl, oxazolyl, isoxazolyl or imidazolyl, which may be substituted by 1H-tetrazol-5-yl, provided that X is hydrogen Then Y is not hydrogen, R 4 and R 5 are independently hydrogen, C 1 -C 4 alkyl or C 1 -C 3 alkyl substituted by 1 to 2 hydroxyl, and A is Wherein x is 0 or 1 and R 7 and R 7a are independently hydrogen, C 1 -C 6 alkyl, phenyl, or imidazolyl, phenyl, indolyl, p-hydroxyphenyl, OR 2 , or S (O) C 1 -C 6 alkyl substituted by m R 2 , or R 7 and R 7a independently combine with each other to form C 3 cycloalkyl, m is 0, 1 or 2, q is 0, 1, 2 or 3 and t is 0, 1, 2 or 3. 제13항에 있어서, 다음 일반식(CIc)의 화합물, 및 이의 약제학적으로 허용되는 염 및 개별적인 부분입체이성체.14. A compound according to claim 13, wherein the compound of formula (CIc) and pharmaceutically acceptable salts and individual diastereomers thereof. 상기식에서, R1Wherein R 1 is 또는 명시되지 않은 이의 레지오이성체로 이루어진 그룹 중에서 선택되고, X는 수소,Or an unspecified regioisomer thereof, X is hydrogen, 로 이루어진 그룹 중에서 선택되고, Y는 수소.It is selected from the group consisting of, Y is hydrogen. 및 명시되지 않은 이의 레지오이성체로 이루어진 그룹 중에서 선택되고, 단 X가 수소인 경우 Y가 수소가 아니며, A는And unspecified regioisomers thereof, provided that when X is hydrogen, Y is not hydrogen, and A is 로 이루어진 그룹 중에서 선택되고, R4및 R5는 독립적으로 -H, -CH3, -CH2CH3,로 이루어진 그룹 중에서 선택된다.It is selected from the group consisting of, R 4 and R 5 are independently -H, -CH 3 , -CH 2 CH 3 , And It is selected from the group consisting of. 제13항에 있어서, 다음 일반식의 입체특이적으로 정의된 화합물.14. Compounds according to claim 13, defined stereospecifically of the general formula 상기식에서, R1, R4, R5, A, X, Y 및 n은 제13항에서 정의한 바와 같다.Wherein R 1 , R 4 , R 5 , A, X, Y and n are as defined in claim 13. 제13항에 있어서,The method of claim 13, 중에서 선택된 화합물, 달리 명시되지 않은 이의 약제학적으로 허용되는 염 및 이의 개별적인 부분입체이성체.And a pharmaceutically acceptable salt thereof and the individual diastereomers thereof. 불활성 담체 및 유효량의 제1항의 화합물을 포함하는, 사람 또는 동물에서 성장 호르몬의 내인성 생성 또는 증가시키기에 유용한 조성물.A composition useful for the endogenous production or increase in growth hormone in a human or animal comprising an inert carrier and an effective amount of the compound of claim 1. 불활성 담체, 유효량의 제1항의 화합물 및 추가의 성장 호르몬 분비 촉진물을 포함하는, 사람 또는 동물에서 성장 호르몬의 내인성 생성 또는 증가시키기에 유용한 조성물.A composition useful for the endogenous production or increase in growth hormone in a human or animal, comprising an inert carrier, an effective amount of the compound of claim 1 and an additional growth hormone secretagogue. 제20항에 있어서, 추가의 성장 호르몬의 분비 촉진물질이 성장 호르몬 방출 펩티드 GHRP-, 6 성장 호르몬 방출 펩티드 GHRP-2, 성장 호르몬 방출 펩티드 GHRP-, B-HT920, 성장 호르몬 방출 인자, 성장 호르몬 방출 인자의 동족체, IGF-1 및 IGF-2로 이루어진 그룹 중에서 선택된 조성물.The method of claim 20, wherein the additional growth hormone secretagogue is growth hormone release peptide GHRP-, 6 growth hormone release peptide GHRP-2, growth hormone release peptide GHRP-, B-HT920, growth hormone release factor, growth hormone release A composition selected from the group consisting of homologues of factors, IGF-1 and IGF-2. 비스포스포네이트 화합물 및 제1항의 화합물의 배합물을 포함하는, 골다공증 치료에 유용한 조성물.A composition useful for the treatment of osteoporosis, comprising a combination of a bisphosphonate compound and a compound of claim 1. 제22항에 있어서, 비스포스포네이트 화합물이 알렌드로네이트인 조성물.The composition of claim 22 wherein the bisphosphonate compound is an alendronate. 유효량의 제1항의 화합물을 사람 또는 동물에 투여함을 포함하며, 사람 또는 동물에서 내인성 성장 호르몬의 농도를 증가시키는 방법.A method of increasing the concentration of endogenous growth hormone in a human or animal, comprising administering an effective amount of the compound of claim 1 to a human or animal. 유효량의 제1항의 화합물을 가축에게 투여함을 포함하여, 가축의 사료 효율을 증가시키고 성장을 촉진시키며 유즙 생성을 증가시키고 고가의 품질을 향상시키는 방법.A method for increasing feed efficiency, promoting growth, increasing milk production and improving expensive quality of a livestock, comprising administering an effective amount of the compound of claim 1 to the livestock. 골다공증; 퇴행성 질환; T4/T8세포비율이 감소된 개인별 면역결핍증을 포함하는 면역결핍증; 고관절부골절; 노인의 근골격 손상; 성인 또는 어린이의 성장 호르몬 결핍; 비만증; AIDS 또는 암과 같은 만성 질환으로 인한 악액질 및 단백질 손실로 이루어진 그룹 중에서 선택된 질환의 치료 또는 예방을 요하는 환자 또는 외과 대수술, 외상 또는 화상으로부터 회복기에 있는 환자에게 유효량의 제1항의 화합물을 투여함으로써 상기 질환을 치료 또는 예방하고 상기와 같은 회복기의 환자를 치료하는 방법.osteoporosis; Degenerative diseases; Immunodeficiency, including individual immunodeficiency with reduced T 4 / T 8 cell ratios; Hip fracture; Musculoskeletal injury in the elderly; Growth hormone deficiency in adults or children; Obesity; By administering an effective amount of the compound of claim 1 to a patient in need of treatment or prevention of a disease selected from the group consisting of cachexia and protein loss due to chronic disease, such as AIDS or cancer, or a patient recovering from surgical major surgery, trauma or burn A method of treating or preventing a disease and treating a patient in such a recovery phase. 골다공증의 치료를 요하는 환자에게 비스포스네이트 화합물 및 제1항의 화합물의 배합물을 투여함을 포함하는 골다공증의 치료 방법.A method of treating osteoporosis comprising administering a combination of a bisphosphonate compound and a compound of claim 1 to a patient in need thereof. 제27항에 있어서, 비스포스포네이트 화합물이 알렌드로네이트인 방법.The method of claim 27, wherein the bisphosphonate compound is an alendronate. 일반식(4)의 화합물을 일반식(5) 또는 일반식(6)의 화합물과 반응시켜 일반식(1) 또는 일반식(7)의 화합물을 수득하고, 필요한 경우 염을 형성시킴을 포함하는, 제1항의 화합물의 제조 방법.Reacting a compound of formula (4) with a compound of formula (5) or (6) to give a compound of formula (1) or formula (7), forming salts if necessary , The method for producing the compound of claim 1. 상기식에서, R1, R3, R4, R5, A, W, X, Y 및 n은 제1항에서 정의한 바와 같고, L은 존재할 경우 후속적으로 제거되어야 하는 보호 그룹이다.Wherein R 1 , R 3 , R 4 , R 5 , A, W, X, Y and n are as defined in claim 1 and L is a protecting group which must be subsequently removed if present. 일반식(12) 또는 일반식(12a)의 화합물을 일반식(2)의 화합물과 반응시켜 일반식(1) 또는 일반식(7)의 화합물을 수득하고, 필요한 경우 염을 형성시킴을 포함하는, 제1항의 화합물의 제조 방법.Reacting a compound of formula (12) or formula (12a) with a compound of formula (2) to give a compound of formula (1) or formula (7), forming salts if necessary , The method for producing the compound of claim 1. 상기식에서, R1, R3, R4, R5, A, W, X, Y 및 n은 제1항에서 정의한 바와 같고, L은 존재할 경우 후속적으로 제거되어야 하는 보호 그룹이다.Wherein R 1 , R 3 , R 4 , R 5 , A, W, X, Y and n are as defined in claim 1 and L is a protecting group which must be subsequently removed if present. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019960702427A 1993-11-09 1994-11-07 Piperidines, pyrrolidines and hexahydro-1 H-azepines promote release of growth hormone KR960705808A (en)

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US5492916A (en) * 1993-12-23 1996-02-20 Merck & Co., Inc. Di- and tri-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone
US5721251A (en) * 1993-12-10 1998-02-24 Merck & Co., Inc. Piperidine, pyrrolidine and hexahydro-1H-azepines promote release of growth hormone
US5721250A (en) * 1993-12-23 1998-02-24 Merck & Co. Inc. Di-and tri-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone
US5767118A (en) * 1994-10-26 1998-06-16 Merck & Co., Inc. 4-Heterocyclic peperidines promote release of growth hormone
US5798337A (en) * 1994-11-16 1998-08-25 Genentech, Inc. Low molecular weight peptidomimetic growth hormone secretagogues
US20020111461A1 (en) 1999-05-21 2002-08-15 Todd C. Somers Low molecular weight peptidomimetic growth hormone secretagogues
US5731317A (en) * 1995-03-10 1998-03-24 Merck & Co., Inc. Bridged piperidines promote release of growth hormone
US5559128A (en) * 1995-04-18 1996-09-24 Merck & Co., Inc. 3-substituted piperidines promote release of growth hormone
WO1996035713A1 (en) * 1995-05-08 1996-11-14 Pfizer, Inc. Dipeptides which promote release of growth hormone
US5620993A (en) * 1995-06-07 1997-04-15 Merck & Co., Inc. Alpha-1a adrenergic receptor antagonists
WO1997022004A1 (en) 1995-12-13 1997-06-19 Merck & Co., Inc. Assays for growth hormone secretagogue receptors
US6531314B1 (en) 1996-12-10 2003-03-11 Merck & Co., Inc. Growth hormone secretagogue receptor family
TW432073B (en) * 1995-12-28 2001-05-01 Pfizer Pyrazolopyridine compounds
GB9526645D0 (en) * 1995-12-28 1996-02-28 Chiroscience Ltd Stereoselective synthesis
HN1996000101A (en) 1996-02-28 1997-06-26 Inc Pfizer COMBINED THERAPY FOR OSTEOPOROSIS
US6011155A (en) * 1996-11-07 2000-01-04 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
UA59384C2 (en) 1996-12-20 2003-09-15 Пфайзер, Інк. Preventing bone mass loss and recovery thereof by means of prostaglandin agonists
UA64751C2 (en) 1997-06-25 2004-03-15 Пфайзер Продактс Інк. Treatment of insulin tolerance using substances increasing growth hormone secretion
DE69837264T2 (en) * 1997-06-25 2008-01-31 Pfizer Inc. Dipeptide compounds that are growth hormone secretagogues
UA53716C2 (en) * 1997-06-25 2003-02-17 Пфайзер Продактс Інк. A substituted dipeptide tartaric salt as an agent stimulating the growth hormone secretion
IL125658A0 (en) 1997-08-18 1999-04-11 Hoffmann La Roche Ccr-3 receptor antagonists
US6339087B1 (en) 1997-08-18 2002-01-15 Syntex (U.S.A.) Llc Cyclic amine derivatives-CCR-3 receptor antagonists
US6303620B1 (en) 1998-05-11 2001-10-16 Novo Nordisk A/S Compounds with growth hormone releasing properties
AU757217B2 (en) * 1998-05-11 2003-02-06 Helsinn Healthcare Sa Compounds with growth hormone releasing properties
DZ2815A1 (en) * 1998-06-12 2003-12-01 Smithkline Beecham Corp Protease inhibitors.
US6682908B1 (en) 1998-07-10 2004-01-27 Merck & Co., Inc. Mouse growth hormone secretagogue receptor
CA2333857A1 (en) 1998-07-13 2000-01-20 Merck & Co., Inc. Growth hormone secretagogue related receptors and nucleic acids
US6645726B1 (en) 1998-08-10 2003-11-11 Merck & Co., Inc. Canine growth hormone secretagogue receptor
US6468974B1 (en) 1998-08-14 2002-10-22 The Administrators Of The Tulane Educational Fund Compounds having growth hormone releasing activity
CO5150173A1 (en) * 1998-12-10 2002-04-29 Novartis Ag COMPOUNDS N- (REPLACED GLYCLE) -2-DIPEPTIDYL-IV PEPTIDASE INHIBITING CYANOPIRROLIDINS (DPP-IV) WHICH ARE EFFECTIVE IN THE TREATMENT OF CONDITIONS MEDIATED BY DPP-IV INHIBITION
CA2362290A1 (en) 1999-02-18 2000-08-24 Kaken Pharmaceutical Co., Ltd. Novel amide derivatives as growth hormone secretagogues
JP2002523368A (en) * 1999-02-19 2002-07-30 イーライ・リリー・アンド・カンパニー Growth hormone secretagogue
US6541634B2 (en) 1999-02-26 2003-04-01 Pfizer Inc. Process for preparing growth hormone secretagogues
BR0009043A (en) 1999-03-15 2002-01-08 Axys Pharm Inc Compound, pharmaceutical composition, and method of treating a disease in an animal in which the activity of the cysteine protease contributes to the pathology and / or symptomatology of the disease
US6110949A (en) * 1999-06-24 2000-08-29 Novartis Ag N-(substituted glycyl)-4-cyanothiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
US6172081B1 (en) 1999-06-24 2001-01-09 Novartis Ag Tetrahydroisoquinoline 3-carboxamide derivatives
US6617340B1 (en) 1999-07-29 2003-09-09 Novartis Ag N-(substituted glycyl)-pyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
US6784200B2 (en) 2000-10-13 2004-08-31 Bristol-Myers Squibb Pharma Company Bicyclic and tricyclic amines as modulators of chemokine receptor activity
AU1201101A (en) 1999-10-15 2001-04-30 Du Pont Pharmaceuticals Company Bicyclic and tricyclic amines as modulators of chemokine receptor activity
JP2003512349A (en) 1999-10-15 2003-04-02 デュポン ファーマシューティカルズ カンパニー Benzylcycloalkylamines as modulators of chemokine receptor activity
UA73530C2 (en) * 1999-11-10 2005-08-15 Ново Нордіск А/С A compound having properties to release the growth hormone
ES2252230T3 (en) 2000-05-11 2006-05-16 Bristol-Myers Squibb Company USEFUL TETRAHYDROISOQUINOLINE ANALOGS AS SECRETORS OF GROWTH HORMONE.
ATE446758T1 (en) 2000-05-31 2009-11-15 Pfizer Prod Inc USE OF GROWTH HORMONE SECRETAGOGENES TO PROMOTE DIGESTIVE MOTILITY
US6638950B2 (en) 2000-06-21 2003-10-28 Bristol-Myers Squibb Pharma Company Piperidine amides as modulators of chemokine receptor activity
US7030116B2 (en) 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
JP2004523506A (en) 2000-12-22 2004-08-05 アクシス・ファーマシューティカルズ・インコーポレイテッド Novel compounds and compositions as cathepsin inhibitors
DE10105041A1 (en) * 2001-02-05 2002-08-14 Tell Pharm Ag Hergiswil Tripeptides and tripeptide derivatives for the treatment of neurodegenerative diseases
MXPA04002282A (en) 2001-09-14 2005-03-07 Axis Pharmaceutical Inc Novel compounds and compositions as cathepsin inhibitors.
AU2002326948A1 (en) 2001-09-18 2003-04-01 Bristol-Myers Squibb Company Piperizinones as modulators of chemokine receptor activity
WO2003026649A1 (en) * 2001-09-27 2003-04-03 Applied Research Systems Ars Holding N.V. Methods of increasing endogenous testosterone levels
AU2002357692A1 (en) 2001-11-09 2003-05-26 Bristol-Myers Squibb Company Tetrahydroisoquinoline analogs as modulators of chemokine receptor activity
KR20050044497A (en) 2001-11-14 2005-05-12 아벤티스 파마슈티칼스 인크. Oligopeptides and compositions containing them as cathepsin s inhibitors
US7153822B2 (en) 2002-01-29 2006-12-26 Wyeth Compositions and methods for modulating connexin hemichannels
TW200409630A (en) 2002-09-12 2004-06-16 Bristol Myers Squibb Co N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
WO2004028530A1 (en) 2002-09-26 2004-04-08 Bristol-Myers Squibb Company N-substituted heterocyclic amines as modulators of chemokine receptor activity
US7659305B2 (en) 2002-10-31 2010-02-09 Pfizer Inc. Therapeutic proline derivatives
US7476653B2 (en) 2003-06-18 2009-01-13 Tranzyme Pharma, Inc. Macrocyclic modulators of the ghrelin receptor
UA87854C2 (en) 2004-06-07 2009-08-25 Мерк Энд Ко., Инк. N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators
CN103772483A (en) * 2004-06-29 2014-05-07 赫尔辛医疗股份公司 Crystal form of(3r)-1-(2-methylalanyl-d-tryptophyl)-3-(phenylmethyl)-3-piperidinecarboxylic acid 1,2,2-trimethylhydrazide
GB0428526D0 (en) 2004-12-30 2005-02-09 Novartis Ag Organic compounds
EP1760076A1 (en) 2005-09-02 2007-03-07 Ferring B.V. FAP Inhibitors
PL1966130T3 (en) 2005-12-23 2014-05-30 Zealand Pharma As Modified lysine-mimetic compounds
CU23558A1 (en) 2006-02-28 2010-07-20 Ct Ingenieria Genetica Biotech COMPOUNDS ANALOG TO THE PEPTIDIC SECRETAGOGS OF THE GROWTH HORMONE
EP1897956A1 (en) 2006-09-06 2008-03-12 Lonza AG Process for preparation of optically active amines by optical resolution of racemic amines employing a bacterial omega-transaminase
EP2468724B1 (en) 2006-12-21 2015-11-18 Zealand Pharma A/S Synthesis of pyrrolidine compounds
EP2118080B1 (en) 2007-02-09 2016-08-31 Ocera Therapeutics, Inc. Macrocyclic ghrelin receptor modulators and methods of using the same
EP2155769B1 (en) 2007-05-04 2012-06-27 Katholieke Universiteit Leuven KU Leuven Research & Development Tissue degeneration protection
JP2009256298A (en) * 2008-03-26 2009-11-05 Sumitomo Chemical Co Ltd Optical resolution method for piperidin-3-ylcarbamate compound, and its intermediate
WO2013190520A2 (en) 2012-06-22 2013-12-27 The General Hospital Corporation Gh-releasing agents in the treatment of vascular stenosis and associated conditions
US9119832B2 (en) 2014-02-05 2015-09-01 The Regents Of The University Of California Methods of treating mild brain injury
CN106572997A (en) 2014-05-30 2017-04-19 辉瑞公司 Carbonitrile derivatives as selective androgen receptor modulators
MX2017001408A (en) * 2014-08-05 2017-05-10 Raqualia Pharma Inc Serine derivatives as ghrelin receptor agonists.
WO2017075535A1 (en) 2015-10-28 2017-05-04 Oxeia Biopharmaceuticals, Inc. Methods of treating neurodegenerative conditions
HU231150B1 (en) 2017-03-13 2021-03-29 Richter Gedeon Nyrt Process for the separation of optical isomers of racemic ethyl 3-alkylpiperidine-3-carboxylic acid
EP3618847B1 (en) 2017-05-05 2021-04-07 Zealand Pharma A/S Gap junction intercellular communication modulators and their use for the treatment of diabetic eye disease
BR112020016256A2 (en) 2018-02-21 2020-12-15 AI Therapeutics, Inc. COMBINATION THERAPY WITH APILIMOD AND GLUTEN-MATERIAL AGENTS
CN112204007B (en) * 2018-06-01 2023-06-20 施万生物制药研发Ip有限责任公司 Process for preparing 2- (1- (tert-butoxycarbonyl) piperidin-4-yl) benzoic acid
WO2023275715A1 (en) 2021-06-30 2023-01-05 Pfizer Inc. Metabolites of selective androgen receptor modulators

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4411890A (en) * 1981-04-14 1983-10-25 Beckman Instruments, Inc. Synthetic peptides having pituitary growth hormone releasing activity
HU180925B (en) * 1979-06-28 1983-05-30 Richter Gedeon Vegyeszet Process for producing tripeptide-amides trh-analogues,effectives on the central nerve systhem
GB8332704D0 (en) * 1983-12-07 1984-01-11 Pfizer Ltd Growth promotants for animals
US5036045A (en) * 1985-09-12 1991-07-30 The University Of Virginia Alumni Patents Foundation Method for increasing growth hormone secretion
US4782139A (en) * 1985-10-28 1988-11-01 Eli Lilly And Company Selective chemical removal of a protein amino-terminal residue
US4997825A (en) * 1986-12-22 1991-03-05 Eli Lilly And Company Synergistic treatment method
US5162302A (en) * 1988-03-18 1992-11-10 University Of Delaware Endocrine manipulation to improve body composition of poultry
US5084442A (en) * 1988-09-06 1992-01-28 Hoffmann-La Roche Inc. Cyclic growth hormone releasing factor analogs and method for the manufacture thereof
US5137872A (en) * 1989-09-18 1992-08-11 Pitman-Moore, Inc. Growth hormone-releasing factor analogs
IE912345A1 (en) * 1990-08-03 1992-02-12 Pharmacia Ab Treatment of human lactation failure
JP2557779B2 (en) * 1990-11-26 1996-11-27 アール. レッカー,ロバート Two-component drug for osteoporosis
US5206235A (en) * 1991-03-20 1993-04-27 Merck & Co., Inc. Benzo-fused lactams that promote the release of growth hormone
JP3098082B2 (en) * 1991-12-12 2000-10-10 三井化学株式会社 Method for producing amino-containing compound
US5366965A (en) * 1993-01-29 1994-11-22 Boehringer Mannheim Gmbh Regimen for treatment or prophylaxis of osteoporosis
US5284841A (en) * 1993-02-04 1994-02-08 Merck & Co., Inc. Benzo-fused lactams promote release of growth hormone

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