CN1829703A - 作为d3/d2受体拮抗剂的(硫代)氨基甲酰基-环己烷衍生物 - Google Patents
作为d3/d2受体拮抗剂的(硫代)氨基甲酰基-环己烷衍生物 Download PDFInfo
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- CN1829703A CN1829703A CNA2004800219507A CN200480021950A CN1829703A CN 1829703 A CN1829703 A CN 1829703A CN A2004800219507 A CNA2004800219507 A CN A2004800219507A CN 200480021950 A CN200480021950 A CN 200480021950A CN 1829703 A CN1829703 A CN 1829703A
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- Prior art keywords
- phenyl
- cyclohexyl
- ethyl
- piperazine
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- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
- C07D295/215—Radicals derived from nitrogen analogues of carbonic acid
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Abstract
Description
化合物 | D3IC-50(nM) | D2IC-50(nM) | α-1IC-50(nM) |
1 | +++ | ++ | >200 |
2 | ++++ | + | >200 |
4 | ++++ | ++ | >200 |
5 | ++++ | ++ | >200 |
6 | ++++ | ++ | >200 |
7 | +++ | ++ | >200 |
8 | ++++ | ++ | >200 |
9 | ++++ | +++ | >200 |
11 | ++++ | ++ | >200 |
12 | ++++ | ++ | >200 |
15 | ++++ | ++ | >200 |
20 | +++ | ++ | >200 |
22 | ++++ | ++ | >200 |
23 | ++++ | ++ | >200 |
24 | ++++ | ++ | >200 |
29 | +++ | ++ | >200 |
33 | ++++ | ++ | >200 |
35 | ++++ | ++ | >200 |
36 | ++++ | ++ | >200 |
38 | ++++ | ++ | >200 |
39 | ++++ | ++ | >200 |
40 | ++++ | + | >200 |
41 | ++++ | + | >200 |
42 | ++++ | ++ | >200 |
氟哌啶醇 | + | ++ | +++ |
阿立哌唑 | +++ | +++ | >200 |
利培酮 | ++ | ++ | +++ |
奥氮平 | + | + | ++ |
化合物 | 分子量 | k′ | 纯度(HPLC面积%) | Iupac |
19 | 505,49 | 5,768 | 99,4 | 反式-1-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-3-(2-甲氧基-苯基)-脲 |
20 | 505,49 | 5,807 | 95,59 | 反式-1-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-3-(3-甲氧基-苯基)-脲 |
21 | 439,43 | 4,816 | 96,25 | 反式-1-烯丙基-3-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-脲 |
22 | 535,52 | 5,901 | 99,52 | 反式-1-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-3-(2,4-二甲氧基-苯基)-脲 |
23 | 519,52 | 6,092 | 98,37 | 反式-1-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-3-(2-乙氧基-苯基)-脲 |
24 | 455,48 | 6,123 | 95,02 | 反式-1-丁基-3-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-脲 |
25 | 559,46 | 6,619 | 94,62 | 反式-1-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-3-(4-三氟甲氧基-苯基)-脲 |
26 | 533,59 | 6,324 | 99,43 | 反式-1-金刚烷-1-基-3-(4-{2-[4-(2,3-二氯-苯-哌嗪-1-基]-乙基}-环己基)-脲 |
27 | 521,56 | 5,976 | 88,03 | 反式-1-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-3-(4-甲基硫烷基(methylsulfanyl)-苯基)-脲 |
28 | 551,56 | 6,441 | 85,42 | 反式-1-二苯基-2-基-3-(4-(2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-脲 |
29 | 513,51 | 5,354 | 99,3 | 反式-2-[3-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-脲基]-3-甲基-丁酸甲酯 |
30 | 533,50 | 6,161 | 96,32 | 反式-2-[3-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-脲基]-苯甲酸甲酯 |
31 | 500,48 | 5,704 | 93,41 | 反式-1-(3-氰基-苯基)-3-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-脲 |
32 | 565,55 | 5,694 | 93,74 | 反式-1-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}环己基)-3-(3,4,5-三甲氧基-苯基)-脲 |
33 | 481,51 | 5,591 | 99 | 反式-1-环己基-3-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-脲 |
34 | 441,45 | 5,121 | 96,93 | 反式-1-(4-{2-[4-(2,3-二氯-苯基)-哌嗪1-基]-乙基}-环己基-3-丙基-脲 |
35 | 491,53 | 5,689 | 98,53 | 反式-1-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-3-苯基-硫脲 |
36 | 549,65 | 6,852 | 95,94 | 反式-1-金刚烷-1-基-3-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-硫脲 |
37 | 487,50 | 5,951 | 99 | 反式-1-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-3-乙氧羰基-硫脲 |
38 | 471,54 | 5,634 | 97,03 | 反式-1-叔丁基-3-(4-(2-[4-(2,3-二氯-苯基)- |
哌嗪-1-基]-乙基}-环己基)-硫脲 | ||||
39 | 505,56 | 5,909 | 99 | 反式-1-苯甲基-3-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-硫脲 |
40 | 521,56 | 5,77 | 94,24 | 反式-1-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-3-(2-甲氧基-苯基)-硫脲 |
41 | 471,54 | 5,786 | 99 | 反式-1-丁基-3-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-硫脲 |
42 | 457,51 | 5,387 | 96,79 | 反式-1-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-3-丙基-硫脲 |
43 | 519,54 | 6,459 | 97,68 | 反式-1-苯甲酰基-3-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-硫脲 |
44 | 501,52 | 5,382 | 96,17 | 反式-[3-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-硫脲基]-乙酸乙酯 |
45 | 443,49 | 5,007 | 99 | 反式-1-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-3-乙基-硫脲 |
46 | 541,59 | 6,401 | 96,26 | 反式-1-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-3-萘(naphthalen)-1-基-硫脲 |
47 | 455,48 | 5,143 | 94,98 | 反式-1-叔丁基-3-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-脲 |
48 | 475,47 | 5,481 | 95,69 | 反式-1-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-3-苯基-脲 |
49 | 489,49 | 5,491 | 94,42 | 反式-1-苯甲基-3-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-脲 |
50 | 505,49 | 5,666 | 90,78 | 反式-1-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-3-(4-甲氧基-苯基)-脲 |
51 | 485,46 | 4,754 | 97,78 | 反式-[3-(4-{2-[4-(2,3-二氯-苯基)-哌嗪-1-基]-乙基}-环己基)-脲基]-乙酸乙酯 |
Claims (24)
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HUP0302451 | 2003-08-04 | ||
HU0302451A HU227534B1 (en) | 2003-08-04 | 2003-08-04 | (thio)carbamoyl-cyclohexane derivatives, process for producing them and pharmaceutical compositions containing them |
PCT/HU2004/000056 WO2005012266A1 (en) | 2003-08-04 | 2004-05-21 | (thio) carbamoyl-cyclohexane derivatives as d3/d2 receptor antagonists |
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