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1. 发明授权

US06103715A Dopamine receptor ligands 失效
标题翻译：多巴胺受体配体
公开(公告)号：US06103715A
公开(公告)日：2000-08-15
申请号：US139715
申请日：1998-08-25
申请人： Ashok Tehim , Jian-Min Fu , Sumanas Rakhit
发明人： Ashok Tehim , Jian-Min Fu , Sumanas Rakhit
IPC分类号： A61K31/00 , A61K31/55 , A61P25/18 , A61P25/20 , C07D243/10 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/12 , C07D491/00
CPC分类号： C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;R.sub.1 represents C.sub.1-4 alkyl;Y is selected from CH and N;n is 0, 1 or 2;q is 1 or 2;R.sub.2 is C.sub.1-6 alkyl optionally incorporating a heteroatom selected from N, O and S;D is cyclohexane or benzene; andE is a saturated or unsaturated 5- or 6-membered heterocycle incorporating 1, 2 or 3 heteroatoms selected from O, N, and S, wherein E is optionally substituted with 1 or 2 substituents selected from halogen, C.sub.1-4 alkyl and halogen-substituted C.sub.1-4 alkyl;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.
摘要翻译：本文描述的是具有以下通式的D4受体选择性化合物：其中：A和B独立地选择，任选取代的饱和或不饱和的5-或6-元，均 - 或杂环; X 1选自CH 2，O，NH，S，C = O，CH-OH，CH-N（C 1-4烷基）2，C = CHCl，C = CHCN，N-C 1-4烷基，N-乙酰基，所以; X2 - - - 选自N =，CH 2 - ，CH =，C（O） - ，O-和S-; R 1表示C 1-4烷基; Y选自CH和N; n为0,1或2; q为1或2; R2是任选地加入选自N，O和S的杂原子的C 1-6烷基; D是环己烷或苯; 并且E是掺杂有1,2或3个选自O，N和S的杂原子的饱和或不饱和的5-或6-元杂环，其中E任选被1或2个选自卤素，C 1-4烷基和卤素 - 取代的C 1-4烷基; 及其酸加成盐，溶剂化物和水合物。还描述了它们作为多巴胺受体鉴定和药物筛选程序的配体的用途，以及用于治疗其中涉及D4受体的适应症的药物，例如精神分裂症。

2. 发明授权

US5602124A 5-HT2 receptor ligands 失效
标题翻译： 5-HT2受体配体
公开(公告)号：US5602124A
公开(公告)日：1997-02-11
申请号：US354765
申请日：1994-12-12
申请人： Ashok Tehim , Jian-Min Fu , Sumanas Rakhit
发明人： Ashok Tehim , Jian-Min Fu , Sumanas Rakhit
IPC分类号： C07D243/38 , C07D267/20 , A61K31/55 , C07D403/04
CPC分类号： C07D243/38 , C07D267/20
摘要： Described herein are 5-HT2 receptor-selective compounds of Formula I: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;R.sub.1 is C.sub.1-6 alkyl optionally substituted with a substituent selected from OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; andR.sub.2, R.sub.3 and R.sub.4 are independently selected from H and R.sub.1 ;and acid addition salts, solvates and hydrates thereof. Their use as ligands for serotonin 5-HT2 receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the 5-HT2 receptor is implicated, such as hypertension, thrombosis, migraine, vasospasm, ischemia, depression, anxiety, schizophrenia, sleep disorders and appetite disorders is also described.
摘要翻译：本文描述的是式I的5-HT 2受体选择性化合物：其中：A和B独立地选择，任选取代的饱和或不饱和的5-或6-元，均 - 或杂环; X 1选自CH 2，O，NH，S，C = O，CH-OH，CH-N（C 1-4烷基）2，C = CHCl，C = CHCN，N-C 1-4烷基，N-乙酰基，所以; X2 - - - 选自N =，CH 2 - ，CH =，C（O） - ，O-和S-; R1是任选被选自OH，卤素，C 1-4烷基和C 1-4烷氧基的取代基取代的C 1-6烷基; 并且R 2，R 3和R 4独立地选自H和R 1; 及其酸加成盐，溶剂化物和水合物。它们用作5-羟色胺5-HT2受体鉴定和药物筛选程序的配体，以及用作治疗其中涉及5-HT2受体的适应症的药物，例如高血压，血栓形成，偏头痛，血管痉挛，局部缺血，抑郁，焦虑，还描述了精神分裂症，睡眠障碍和食欲障碍。

3. 发明授权

US5798350A Dopamine receptor ligands 失效
标题翻译：多巴胺受体配体
公开(公告)号：US5798350A
公开(公告)日：1998-08-25
申请号：US642264
申请日：1996-05-03
申请人： Ashok Tehim , Jian-Min Fu , Sumanas Rakhit
发明人： Ashok Tehim , Jian-Min Fu , Sumanas Rakhit
IPC分类号： A61K31/00 , A61K31/55 , A61P25/18 , A61P25/20 , C07D243/10 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/12 , C07D491/00 , A61K31/495 , A61K31/435 , C07D401/14 , C07D403/14
CPC分类号： C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings; X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO; X.sub.2 --is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--; R.sub.1 represents C.sub.1-4 alkyl; Y is selected from CH and N; n is 0, 1 or 2; q is 1 or 2; R.sub.2 is C.sub.1-6 alkyl optionally incorporating a heteroatom selected from N, O and S; D is cyclohexane or benzene; and E is a saturated or unsaturated 5- or 6-membered heterocycle incorporating 1, 2 or 3 heteroatoms selected from O, N, and S, wherein E is optionally substituted with 1 or 2 substituents selected from halogen, C.sub.1-4 alkyl and halogen-substituted C.sub.1-4 alkyl; and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.
摘要翻译：本文描述的是具有以下通式的D4受体选择性化合物：其中：A和B独立选择，任选取代的饱和或不饱和的5-或6-元，杂环或杂环; X 1选自CH 2，O，NH，S，C = O，CH-OH，CH-N（C 1-4烷基）2，C = CHCl，C = CHCN，N-C 1-4烷基，N-乙酰基，所以; X2-选自N =，CH 2 - ，CH =，C（O） - ，O-和S-; R 1表示C 1-4烷基; Y选自CH和N; n为0,1或2; q为1或2; R2是任选地加入选自N，O和S的杂原子的C 1-6烷基; D是环己烷或苯; 并且E是掺杂有1,2或3个选自O，N和S的杂原子的饱和或不饱和的5-或6-元杂环，其中E任选被1或2个选自卤素，C 1-4烷基和卤素 - 取代的C 1-4烷基; 及其酸加成盐，溶剂化物和水合物。还描述了它们作为多巴胺受体鉴定和药物筛选程序的配体的用途，以及用于治疗其中涉及D4受体的适应症的药物，例如精神分裂症。

4. 发明授权

US5824676A 5-HT2 receptor ligands 失效
标题翻译： 5-HT2受体配体
公开(公告)号：US5824676A
公开(公告)日：1998-10-20
申请号：US763255
申请日：1996-12-10
申请人： Ashok Tehim , Jian-min Fu , Sumanas Rakhit
发明人： Ashok Tehim , Jian-min Fu , Sumanas Rakhit
IPC分类号： C07D243/38 , C07D267/20 , A61K31/55 , C07D403/04 , C07D413/04 , C07D417/04
CPC分类号： C07D243/38 , C07D267/20
摘要： Described herein are 5-HT2 receptor-selective compounds of Formula I: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings; X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO; X.sub.2 --is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--; R.sub.1 is C.sub.1-6 alkyl optionally substituted with a substituent selected from OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; and R.sub.2, R.sub.3 and R.sub.4 are independently selected from H and R.sub.1 ; and acid addition salts, solvates and hydrates thereof. Their use as ligands for serotonin 5-HT2 receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the 5-HT2 receptor is implicated, such as hypertension, thrombosis, migraine, vasospasm, ischemia, depression, anxiety, schizophrenia, sleep disorders and appetite disorders is also described.
摘要翻译：本文描述的是式I的5-HT 2受体选择性化合物：其中：A和B独立地选择，任选取代的饱和或不饱和的5-或6-元，均 - 或杂环; X 1选自CH 2，O，NH，S，C = O，CH-OH，CH-N（C 1-4烷基）2，C = CHCl，C = CHCN，N-C 1-4烷基，N-乙酰基，所以; X2-选自N =，CH 2 - ，CH =，C（O） - ，O-和S-; R1是任选被选自OH，卤素，C 1-4烷基和C 1-4烷氧基的取代基取代的C 1-6烷基; 并且R 2，R 3和R 4独立地选自H和R 1; 及其酸加成盐，溶剂化物和水合物。它们用作5-羟色胺5-HT2受体鉴定和药物筛选程序的配体，以及用作治疗其中涉及5-HT2受体的适应症的药物，例如高血压，血栓形成，偏头痛，血管痉挛，局部缺血，抑郁，焦虑，还描述了精神分裂症，睡眠障碍和食欲障碍。

5. 发明授权

US5538965A Dopamine receptor ligands 失效
标题翻译：多巴胺受体配体
公开(公告)号：US5538965A
公开(公告)日：1996-07-23
申请号：US355297
申请日：1994-12-12
申请人： Ashok Tehim , Jian-Min Fu , Sumanas Rakhit
发明人： Ashok Tehim , Jian-Min Fu , Sumanas Rakhit
IPC分类号： A61K31/00 , A61K31/55 , A61P25/18 , A61P25/20 , C07D243/10 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/12 , C07D491/00 , C07D413/14 , C07D417/14
CPC分类号： C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N-C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 -- is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;R.sub.1 represents C.sub.1-4 alkyl;Y is selected from CH and N;n is 0, 1 or 2;q is 1 or 2;R.sub.2 is C.sub.1-6 alkyl optionally incorporating a heteroatom selected from N, O and S;D is cyclohexane or benzene; andE is a saturated or unsaturated 5- or 6-membered heterocycle incorporating 1, 2 or 3 heteroatoms selected from O, N, and S, wherein E is optionally substituted with 1 or 2 substituents selected from halogen, C.sub.1-4 alkyl and halogen-substituted C.sub.1-4 alkyl;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.
摘要翻译：本文描述的是具有以下通式的D4受体选择性化合物：其中：A和B独立选择，任选取代的饱和或不饱和的5-或6-元，杂环或杂环; X 1选自CH 2，O，NH，S，C = O，CH-OH，CH-N（C 1-4烷基）2，C = CHCl，C = CHCN，N-C 1-4烷基，N-乙酰基，所以; X2-选自N =，CH 2 - ，CH =，C（O） - ，O-和S-; R1表示C1-4烷基; Y选自CH和N; n为0,1或2; q为1或2; R2是任选地加入选自N，O和S的杂原子的C 1-6烷基; D是环己烷或苯; 并且E是掺杂有1,2或3个选自O，N和S的杂原子的饱和或不饱和的5-或6-元杂环，其中E任选被1或2个选自卤素，C 1-4烷基和卤素 - 取代的C 1-4烷基; 及其酸加成盐，溶剂化物和水合物。还描述了它们作为多巴胺受体鉴定和药物筛选程序的配体的用途，以及用于治疗其中涉及D4受体的适应症的药物，例如精神分裂症。

6. 发明授权

US5561127A Muscarinic receptor ligands 失效
标题翻译：毒蕈碱受体配体
公开(公告)号：US5561127A
公开(公告)日：1996-10-01
申请号：US358471
申请日：1994-12-19
申请人： Ashok Tehim , Sumanas Rakhit
发明人： Ashok Tehim , Sumanas Rakhit
IPC分类号： C07D487/08 , A61K31/55 , C07D403/04 , C07D413/04 , C07D417/00
CPC分类号： C07D487/08
摘要： Described herein are D4 receptor-selective compounds of the general formula I: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--NEt.sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 --is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;n is 1 or 2; andZ is selected from C.sub.1-6 alkyl optionally substituted with a substituent selected from OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the M1/M2 receptor is implicated, such as schizophrenia, is also described.
摘要翻译：本文描述的是通式I的D4受体选择性化合物：其中：A和B独立选择，任选取代的饱和或不饱和的5-或6-元的同或杂环; X 1选自CH 2，O，NH，S，C = O，CH-OH，CH-NEt 2，C = CHCl，C = CHCN，N-C 1-4烷基，N-乙酰基，SO 2和SO; X2-选自N =，CH 2 - ，CH =，C（O） - ，O-和S-; n为1或2; Z选自任选被选自OH，卤素，C 1-4烷基和C 1-4烷氧基的取代基取代的C 1-6烷基; 及其酸加成盐，溶剂化物和水合物。还描述了它们作为多巴胺受体鉴定和药物筛选程序的配体的用途，以及用于治疗M1 / M2受体涉及的指征的药物，例如精神分裂症。

7. 发明授权

US5849734A Muscarinic receptor ligands 失效
标题翻译：毒蕈碱受体配体
公开(公告)号：US5849734A
公开(公告)日：1998-12-15
申请号：US872935
申请日：1997-06-11
申请人： Ashok Tehim , Sumanas Rakhit
发明人： Ashok Tehim , Sumanas Rakhit
IPC分类号： C07D487/08 , A61K31/55 , C07D281/16 , C07D471/08
CPC分类号： C07D487/08
摘要： Described herein are D4 receptor-selective compounds of the general formula I: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings; X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--NEt.sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO; X.sub.2 --is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--; n is 1 or 2; and Z is selected from C.sub.1-8 alkyl optionally substituted with a substituent selected from OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the M1/M2 receptor is implicated, such as schizophrenia, is also described.
摘要翻译：本文描述的是通式I的D4受体选择性化合物：其中：A和B独立地选择，任选取代的饱和或不饱和的5-或6-元同或杂环; X 1选自CH 2，O，NH，S，C = O，CH-OH，CH-NEt 2，C = CHCl，C = CHCN，N-C 1-4烷基，N-乙酰基，SO 2和SO; X2-选自N =，CH 2 - ，CH =，C（O） - ，O-和S-; n为1或2; Z选自任选被选自OH，卤素，C 1-4烷基和C 1-4烷氧基的取代基取代的C 1-8烷基; 及其酸加成盐，溶剂化物和水合物。还描述了它们作为多巴胺受体鉴定和药物筛选程序的配体的用途，以及用于治疗M1 / M2受体涉及的指征的药物，例如精神分裂症。

8. 发明授权

US5674877A Muscarinic receptor ligands 失效
标题翻译：毒蕈碱受体配体
公开(公告)号：US5674877A
公开(公告)日：1997-10-07
申请号：US637181
申请日：1996-04-24
申请人： Ashok Tehim , Sumanas Rakhit
发明人： Ashok Tehim , Sumanas Rakhit
IPC分类号： C07D487/08 , A61K31/49 , C07D471/08
CPC分类号： C07D487/08
摘要： Described herein are D4 receptor-selective compounds of the general formula I: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings; X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--NEt.sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, So.sub.2 and SO; X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--; n is 1 or 2; and Z is selected from C.sub.1-6 alkyl optionally substituted with a substituent selected from OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the M1/M2 receptor is implicated, such as schizophrenia, is also described.
摘要翻译：本文描述的是通式I的D4受体选择性化合物：其中：A和B独立地选择，任选取代的饱和或不饱和的5-或6-元同或杂环; X 1选自CH 2，O，NH，S，C = O，CH-OH，CH-NEt 2，C = CHCl，C = CHCN，N-C 1-4烷基，N-乙酰基，So 2和SO; X2 - - - 选自N =，CH 2 - ，CH =，C（O） - ，O-和S-; n为1或2; Z选自任选被选自OH，卤素，C 1-4烷基和C 1-4烷氧基的取代基取代的C 1-6烷基; 及其酸加成盐，溶剂化物和水合物。还描述了它们作为多巴胺受体鉴定和药物筛选程序的配体的用途，以及用于治疗M1 / M2受体涉及的指征的药物，例如精神分裂症。

9. 发明授权

US5602120A Benzyl-substituted compounds having dopamine receptor affinity 失效
标题翻译：具有多巴胺受体亲和力的苄基取代的化合物
公开(公告)号：US5602120A
公开(公告)日：1997-02-11
申请号：US354766
申请日：1994-12-12
申请人： Jian-Min Fu , Ashok Tehim , Robert A. Kirby
发明人： Jian-Min Fu , Ashok Tehim , Robert A. Kirby
IPC分类号： C07D267/20 , A61K31/55 , C07D413/04 , C07D417/04
CPC分类号： C07D267/20
摘要： Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;Y is selected from CH and N;Z is cyanoR.sub.1 represents C.sub.1-4 alkyl;m is 0, 1, 2 or 3;n is 0, 1 or 2;q is 1 or 2; andD is a 5, 6 or 7-membered, saturated or unsaturated, homo- or heterocyclic ring; and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.
摘要翻译：本文描述的是具有以下通式的D4受体选择性化合物：其中：A和B独立选择，任选取代的饱和或不饱和的5-或6-元，杂环或杂环; X 1选自CH 2，O，NH，S，C = O，CH-OH，CH-N（C 1-4烷基）2，C = CHCl，C = CHCN，N-C 1-4烷基，N-乙酰基，所以; X2 - - - 选自N =，CH 2 - ，CH =，C（O） - ，O-和S-; Y选自CH和N; Z是氰基，R 1表示C 1-4烷基; m为0,1,2或3; n为0,1或2; q为1或2; 且D为5,6或7元饱和或不饱和的均聚或杂环; 及其酸加成盐，溶剂化物和水合物。还描述了它们作为多巴胺受体鉴定和药物筛选程序的配体的用途，以及用于治疗其中涉及D4受体的适应症的药物，例如精神分裂症。

10. 发明授权

US5814628A Benzyl-substituted compounds having dopamine receptor affinity 失效
标题翻译：具有多巴胺受体亲和力的苄基取代的化合物
公开(公告)号：US5814628A
公开(公告)日：1998-09-29
申请号：US762984
申请日：1996-12-10
申请人： Jian-Min Fu , Ashok Tehim , Robert A. Kirby
发明人： Jian-Min Fu , Ashok Tehim , Robert A. Kirby
IPC分类号： C07D267/20 , C07D401/14 , A61K31/55 , C07D403/14
CPC分类号： C07D267/20
摘要： Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings; X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCI, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO; X.sub.2 --is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--; Y is selected from CH and N; Z is cyano R.sub.1 represents C.sub.1-4 alkyl; m is 0, 1, 2 or 3; n is 0, 1 or 2; q is 1 or 2; and D is a 5, 6 or 7-membered, saturated or unsaturated, homo- or heterocyclic ring; and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.
摘要翻译：本文描述的是具有以下通式的D4受体选择性化合物：其中：A和B独立选择，任选取代的饱和或不饱和的5-或6-元，杂环或杂环; X 1选自CH 2，O，NH，S，C = O，CH-OH，CH-N（C 1-4烷基）2，C = CHCl，C = CHCN，N-C 1-4烷基，N-乙酰基，所以; X2-选自N =，CH 2 - ，CH =，C（O） - ，O-和S-; Y选自CH和N; Z是氰基，R 1表示C 1-4烷基; m为0,1,2或3; n为0,1或2; q为1或2; 且D为5,6或7元饱和或不饱和的均聚或杂环; 及其酸加成盐，溶剂化物和水合物。还描述了它们作为多巴胺受体鉴定和药物筛选程序的配体的用途，以及用于治疗其中涉及D4受体的适应症的药物，例如精神分裂症。

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