JP5654190B2 - ベンジリデンアミノグアニジンおよびヒドロキシグアニジンのメラノコルチン受容体リガンドとしての使用 - Google Patents
ベンジリデンアミノグアニジンおよびヒドロキシグアニジンのメラノコルチン受容体リガンドとしての使用 Download PDFInfo
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- JP5654190B2 JP5654190B2 JP2002517052A JP2002517052A JP5654190B2 JP 5654190 B2 JP5654190 B2 JP 5654190B2 JP 2002517052 A JP2002517052 A JP 2002517052A JP 2002517052 A JP2002517052 A JP 2002517052A JP 5654190 B2 JP5654190 B2 JP 5654190B2
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- Prior art keywords
- hydroxyguanidine tosylate
- nitrobenzylideneamino
- hydroxyguanidine
- treatment
- compounds
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- C07C281/00—Derivatives of carbonic acid containing functional groups covered by groups C07C269/00 - C07C279/00 in which at least one nitrogen atom of these functional groups is further bound to another nitrogen atom not being part of a nitro or nitroso group
- C07C281/16—Compounds containing any of the groups, e.g. aminoguanidine
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- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
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Description
R1、R2、R3、R4、およびR5は、同じであっても異なっていてもよく、水素、ハロゲン、炭素原子を1〜5個有するアルキル、例えば、炭素原子を1〜5個有するアルコキシまたはヒドロキシのような電子供与基、シアノ、ニトロ、トリフルオロアルキル、またはアミドから選択される電子受容基、アルキルアミノ、ベンゾイルオキシ、ニトロキシ、フェニル、またはスルホから選択される。
一般式(I)で表される化合物は、以下に述べるような一般的方法で調製してもよい。
以下に示す実施例において挙げる化合物は、意図した用途において特に有用なものであるが、これらの実施例はあくまで説明目的に示すものであり、本発明の請求の範囲を何ら限定するものではない。実施例中の化合物にはa:bのような番号コードを付与しているが、aはその化合物の調製について記載している実施例の番号を表し、bはその化合物が該実施例中で調製された順番を表している。したがって、1:2というコードが付与された化合物の例は、方法1(実施例1参照)によって2番目に調製された化合物を意味する。
IR、NMR、MS、および元素分析により、化合物の構造を確認した。融点(mp)を記載している場合、未補正値を示している。
2−クロロ−3,4−ジメトキシベンズアルデヒド(1.0g、5mmol)、重炭酸アミノグアニジン(0.68g、5mmol)、および酢酸(1ml)をメタノール15ml中に溶解させた溶液を、10分間加熱還流した。得られた反応液を0℃まで冷却し、残留物をろ過により除去した。真空状態でろ液を蒸発させ、得られた生成物をエタノールから晶出(crystallised)させた。目的の化合物1:1の収量は1.1g(70%)であり、その融点は198〜200℃であった。
化合物1:2〜1:164を、上述の方法1を用い、基本的には化合物1:1の調製と同様の手法によって調製した。これら化合物を、データと共に以下に示す。
1 N−(2−クロロ−3,4−ジメトキシベンジリデンアミノ)グアニジンアセテート、mp:198〜200℃
2 N−(3−ブロモベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:177〜178.5℃
3 N−(3−ブロモ−4−メトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:209〜210.5℃
4 N−(5−クロロ−2−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:180〜181℃
5 N−(2,4−ジヒドロキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:194〜195℃
6 N−(2,3−ジヒドロキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:108〜109℃
7 N−(2,4,5−トリメトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:98.5〜99.5℃
8 N−(3−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:204.5〜206℃
9 N−(4,5−メチレンジオキシ−2−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:108〜111℃
10 N−(3,4,5−トリメトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:139〜141℃
11 N−(4−クロロ−3−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:184〜187℃
12 N−(4−メトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:175〜177℃
13 N−(2−ブロモベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:148.5〜150℃
14 N−(2,3,4−トリメトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:179〜181℃
15 N−(2−ヒドロキシ−4,6−ジメトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:133〜135℃
16 N−(2,5−ジメトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:137〜139℃
17 N−(2,3−ジメトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:91〜93℃
18 N−(2,5−ジフルオロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:186〜187.5℃
19 N−(5−ブロモ−2−ヒドロキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:217〜218℃
20 N−(4−ジメチルアミノベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:185.5〜187℃
21 N−(4−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:191〜193℃
22 N−(2−ヒドロキシ−3−メトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:173〜175℃
23 N−(3−クロロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:184〜186℃
24 N−(2−ヒドロキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:172〜174℃
25 N−(2,3,4−トリベンジルオキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:147〜149℃
26 N−(ベンジリデンアミノ)グアニジンアセテート、mp:196〜198℃
27 N−(3,4,5−トリメトキシベンジリデンアミノ)グアニジンアセテート、mp:223〜225℃
28 N−(4−クロロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:192〜194℃
29 N−(3,4−メチレンジオキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:204〜206℃
30 N−(4−ブロモベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:199〜200℃
31 N−(4−ジエチルアミノベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:100〜102℃
32 N−(2−ヒドロキシ−5−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:217〜219℃
33 N−(4−ヒドロキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:83〜85℃
34 N−(2,4,6−トリメトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:80〜82℃
35 N−(2,3,4−トリヒドロキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:100〜102℃
36 N−(3−ヒドロキシ−4−メトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:88〜89℃
37 N−(2−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:204〜206℃
38 N−(2−ブロモ−3,4,5−トリメトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:172〜175℃
39 N−(2,4−ジニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:208〜211℃
40 N−(2−クロロ−6−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:92〜94℃
41 N−(3,5−ジメトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:92〜95℃
42 N−(5−ヒドロキシ−2−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:182〜183℃
43 N−(3,6−ジメトキシ−2−ニトロキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:101〜102℃
44 N−(3,4−ジメトキシ−2−クロロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:95〜97℃
45 N−(3,4−ジメトキシ−2−クロロベンジリデンアミノ)グアニジンアセテート、mp:198〜200℃
46 N−(ベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:169〜171℃
47 N−(3,4−ジメトキシ−2−クロロベンジリデンアミノ)−N’−ヒドロキシグアニジン1.5塩酸塩、mp:214〜216℃
48 N−(2,3−ジメトキシ−5−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.3水和物、mp:174〜176℃
49 N−(2,3−ジメトキシ−5−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.3水和物、mp:174〜176℃
50 N−(2,3−ジメトキシ−5,6−ジニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.15水和物、mp:178〜179℃
51 N−(2,6−ジメトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:69〜71℃
52 N−(2,3−ジメトキシ−6−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:81〜83℃
53 N−(5−ブロモ−2,4−ジメトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:102〜105℃
54 N−(2−フルオロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.1水和物、mp:169〜171℃
55 N−(2−メトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:79〜82℃
56 N−(2,4,6−トリメトキシベンジリデンアミノ)グアニジンアセテート、mp:66〜68℃
57 N−(2,3−メチレンジオキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:163〜164.5℃
58 N−(4−ブロモ−3−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:201〜202.5℃
59 N−(5−ブロモ−2−ヒドロキシ−3−メトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:131.5〜134℃
60 N−(3−メトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:151〜153.5℃
61 N−(2,3−ジニトロ−6−クロロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:170〜172.5℃
62 N−(3,6−ジクロロ−2−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:183〜184.5℃
63 N−(2,6−ジニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:91〜93℃
64 N−(2−クロロ−3,4−ジメトキシ−6−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:104〜106.5℃ 65 N−(2,4−ジニトロベンジリデンアミノ)グアニジンアセテート、mp:224〜226℃
66 N−(2−クロロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:156〜158℃
67 N−(4−フルオロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.25水和物、mp:182〜184℃
68 N−(3−フルオロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.2水和物、mp:170〜171.5℃
69 N−(4−シアノベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.2水和物、mp:203〜204℃
70 N−(3,5−ジメトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.5水和物、mp:131〜133℃
71 N−(4−フルオロ−3−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:190〜192.5℃
72 N−(2−クロロ−5−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.2水和物、mp:189〜191℃
73 N−(4−クロロ−2−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.25水和物、mp:179〜181.5℃
74 N−(3,4−ジクロロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:200〜202.5℃
75 N−(2,4−ジクロロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.5水和物、mp:158〜161℃
76 N−(4−メトキシ−3−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジン、mp:219〜221℃
77 N−(2,3−ジクロロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:197〜199.5℃
78 N−(2−フルオロ−5−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.4水和物、mp:172〜175℃
79 N−(2−メトキシ−5−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.7水和物、mp:115〜117℃
80 N−(4−ヒドロキシ−3,5−ジメトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.4水和物、mp:114〜115℃
81 N−(2−ブロモ−5−クロロ3−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:195〜196.5℃
82 N−(3−ブロモ−2,6−ジニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.5水和物1.8プロパノール、mp:91〜93℃
83 N−(3,5−ジニトロ−2−メトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.2水和物、mp:185〜187℃
84 N−(5−ブロモ−2−ヒドロキシ−3−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.1水和物、mp:186〜189℃
85 N−(3−ニトロベンジリデンアミノ)グアニジンアセテート、mp:147〜148.5℃
86 N−(2−ヒドロキシ−4,6−ジメトキシベンジリデンアミノ)グアニジンアセテート、mp:115〜118℃
87 N−(4−ニトロベンジリデンアミノ)グアニジンアセテート、mp:184〜186℃
88 N−(3−メトキシ−2,6−ジニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:123.5〜125℃
89 N−(3−ブロモ−4−フルオロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:204.5〜206.5℃
90 N−(2,3−ジフルオロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:186.5〜187℃
91 N−(4−クロロ−3−フルオロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.5水和物、mp:166.5〜167.5℃
92 N−(4−ブロモ−3−フルオロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.6水和物、mp:183〜185.5℃
93 N−(3−ブロモ−4−フルオロベンジリデンアミノ)グアニジンアセテート、mp:172〜173.5℃
94 N−(2,3−ジフルオロベンジリデンアミノ)グアニジンアセテート、mp:149〜151.5℃
95 N−(4−クロロ−3−フルオロベンジリデンアミノ)グアニジンアセテート、mp:165〜171℃
96 N−(3−メトキシ−2,6−ジニトロベンジリデンアミノ)グアニジン塩酸塩、mp:217〜218℃
97 N−(3−ブロモ−2,6−ジニトロベンジリデンアミノ)グアニジン塩酸塩、mp:166.5〜168℃
98 N−(2,3−ジメトキシ−5,6−ジニトロベンジリデンアミノ)グアニジンアセテート、mp:165〜171℃
99 N−(5−ブロモ−2,4−ジメトキシベンジリデンアミノ)グアニジンアセテート0.5水和物、mp:221〜224℃
100 N−(2,3−ジメトキシ−5−ニトロベンジリデンアミノ)グアニジンアセテート、mp:191〜194℃
101 N−(3,4−ジフルオロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:199〜201℃
102 N−(4−フェニルベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:171〜173℃
103 N−(3−クロロ−2,6−ジニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:85〜88℃
104 N−(4−フェニルベンジリデンアミノ)グアニジンアセテート、mp:191〜194℃
105 N−(3,4−ジフルオロベンジリデンアミノ)グアニジンアセテート、mp:176〜178℃
106 N−(4−ブロモ−2−フルオロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.3水和物、mp:176〜179℃
107 N−(2−フルオロ−5−ニトロベンジリデンアミノ)グアニジンアセテート、mp:192〜195℃
108 N−(4−ブロモ−2−フルオロベンジリデンアミノ)グアニジンアセテート、mp:187〜188℃
109 N−(2−ブロモ−5−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:148〜150℃
110 N−(2,4−ジニトロベンジリデンアミノ)−N’−ヒドロキシグアニジン塩酸塩、mp:191〜193℃
111 N−(2,6−ジフルオロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:176〜179℃
112 N−(3−クロロ−4−フルオロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:198.5〜201℃
113 N−(3,5−ジクロロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:208〜210.5℃
114 N−(2−ブロモ−4−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:170〜173℃
115 N−(3,5−ジニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート0.5水和物、mp:202〜207℃
116 N−(2,3−ジニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:214〜216℃
117 N−(3,5−ジクロロベンジリデンアミノ)グアニジンアセテート、mp:131〜134℃
118 N−(3,5−ジニトロベンジリデンアミノ)グアニジンアセテート二水和物、mp:251〜254℃(分解)
119 N−(2,6−ジフルオロベンジリデンアミノ)グアニジンアセテート、mp:138.5〜141℃
120 N−(3−クロロ−4−フルオロベンジリデンアミノ)グアニジンアセテート、mp:141〜144℃
121 N−(2−ブロモ−4−ニトロベンジリデンアミノ(nitroobenzylideneamino))グアニジンアセテート、mp:145〜147℃
122 N−(2−ブロモ−5−ニトロベンジリデンアミノ(nitroobenzylideneamino))グアニジンアセテート、mp:205〜208℃(分解)
123 N−(2−ヨードベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:136〜139℃
124 N−(2−ヨードベンジリデンアミノ)グアニジンアセテート、mp:1714〜173℃
125 N−(2,3−ジメトキシ−5−ニトロベンジリデンアミノ)グアニジン塩酸塩、mp:237〜238℃
126 N−(2−ヒドロキシ−4−メトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:174〜176℃
127 N−(2−ヒドロキシ−4−メトキシベンジリデンアミノ)グアニジンアセテート、mp:161〜164℃
128 N−(4−ブロモ−3−ニトロベンジリデンアミノ)グアニジンアセテート、mp:152〜153℃
129 N−(6−クロロ−2,3−ジニトロベンジリデンアミノ)グアニジン塩酸塩、mp:153〜154.5℃
130 N−(3−ブロモ−4−メトキシベンジリデンアミノ)グアニジン塩酸塩、mp;261〜262.5℃
131 N−(3−ヨードベンジリデンアミノ)グアニジン塩酸塩、mp:203〜204℃
132 N−(3−ヨードベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:193.5〜195℃
133 N−(2−スルホベンジリデンアミノ)グアニジン塩酸塩、mp:>260℃
134 N−(2−スルホベンジリデンアミノ)−N’−ヒドロキシグアニジン、mp:243.5〜244℃
135 N−(3,4−ジクロロベンジリデンアミノ)グアニジンアセテート、mp:138〜140℃
136 N−(2−クロロ−5−ニトロベンジリデンアミノ)グアニジンアセテート、mp:222〜224℃(分解)
137 N−(4−クロロ−3−ニトロベンジリデンアミノ)グアニジンアセテート、mp:136〜139℃(分解)
138 N−(4−フルオロ−3−ニトロベンジリデンアミノ)グアニジンアセテート、mp:222〜224℃(分解)
139 N−(4−メトキシ−3−ニトロベンジリデンアミノ)グアニジンアセテート、mp:144〜147℃
140 N−(2−クロロ−3,4,5−トリメトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:176〜178℃
141 N−(3,5−ジフルオロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:210.5〜213℃
142 N−(5−ブロモ−2,3,4−トリメトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:195〜197℃
143 N−(3−クロロ−4−メトキシベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:204〜207℃
144 N−(2,3−ジメトキシ−5−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジン塩酸塩、mp:196〜197.5℃
145 N−(3,5−ジフルオロ−2−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:176〜178℃
146 N−(3,5−ジクロロ−2−ニトロベンジリデンアミノ)−N’−ヒドロキシグアニジントシレート、mp:205〜207℃
147 N−(3,5−ジフルオロ−2−ニトロベンジリデンアミノ)グアニジンアセテート、mp:231〜233℃
148 N−(3,5−ジクロロ−2−ニトロベンジリデンアミノ)グアニジンアセテート、mp:88〜91℃
149 N−(2−ヒドロキシ−3−メトキシ−5−ニトロベンジリデンアミノ)グアニジン塩酸塩、mp:243〜246℃
150 N−(2−ヒドロキシ−4−メトキシ−5−ニトロベンジリデンアミノ)グアニジンヘミアセテート、mp:227〜230℃
151 N−(3−クロロ−4−メトキシ−5−ニトロベンジリデンアミノ)グアニジンアセテート、mp:255〜258℃(分解)
152 N−(3,5−ジクロロ4−メトキシベンジリデンアミノ)グアニジンアセテート、mp:185〜190℃
153 N−(3−ブロモ−4−メトキシ−5−メチルベンジリデンアミノ)グアニジンアセテート、mp:163〜166℃
154 N−(2,3,4−トリメトキシベンジリデンアミノ)グアニジン塩酸塩、mp:181〜183℃
155 N−(4−クロロ−2−メトキシ−5−ニトロベンジリデンアミノ)グアニジンアセテート、mp:196〜199℃
156 N−(3,6−ジクロロ−2−ニトロベンジリデンアミノ)グアニジンアセテート、mp:219.5〜221℃
157 N−(2−ヒドロキシ−4−メチル−5−ニトロベンジリデンアミノ)グアニジン塩酸塩、mp:229〜230℃
158 N−(2−ブロモ−5−クロロ−3−ニトロベンジリデンアミノ)グアニジンアセテート、mp:136.5〜137℃
159 N−(3−ヒドロキシ−4−メチル−2−ニトロベンジリデンアミノ)グアニジンアセテート、mp:240〜241℃
160 N−(5−ブロモ−4−メチル−2−ニトロベンジリデンアミノ)グアニジン塩酸塩、mp:246.5〜248℃
161 N−(5−ブロモ−2−ヒドロキシ−3−ニトロベンジリデンアミノ)グアニジン塩酸塩、mp:>250℃
162 N−(5−ブロモ−2−メトキシ−3−ニトロベンジリデンアミノ)グアニジン塩酸塩、mp:258〜259℃
163 N−(2,4−ジメトキシ−5−ニトロベンジリデンアミノ)グアニジンアセテート、mp:207〜210℃
164 N−(4−ブロモ−2−フルオロ−5−ニトロベンジリデンアミノ)グアニジンアセテート、mp:175〜198℃(分解)
本実施例は、式(I)で表される化合物および治療上活性なそれらの酸付加塩の、精神障害の治療における力価を示すものである。
I125−NDP−αMSHをリガンドとして用い、基本的にはLunecらのMelanoma Res 1992; 2; 5-12に記載されている通りに結合アッセイを行った。
I125−NDP−αMSHをリガンドとして用い、基本的にはSzardeningsらのJ Biol Chem 1997; 272; 27943-27948およびSchioethらのFEBS Lett 1997; 410; 223-228に記載されている通りに結合アッセイを行った。
基本的にはSchioethらのBr J Pharmacol 1998; 124; 75-82に記載されている通りにcAMPの刺激を行った。
化合物 Ki(μM)
MC1 MC3 MC4 MC5
1:3 42 91 62 47
1:4 42 68 61 33
MC1c MC3c MC4c MC5c
1:3 8.4 16 31.8 4.7
1:4 6.4 1 17.1 8.7
以下に挙げる剤型は、本発明に係る薬理学的に活性なあらゆる化合物に適用できる剤型を例示するものである。
1カプセル当たり
塩としての活性成分 5mg
ラクトース 250mg
デンプン 120mg
ステアリン酸マグネシウム 5mg
合計 最大 385mg
活性成分の量を多くする場合は、使用するラクトースの量を減らせばよい。
1タブレット当たり
塩としての活性成分 5mg
バレイショデンプン 90mg
コロイドシリカ 10mg
タルク 20mg
ステアリン酸マグネシウム 2mg
ゼラチンの5%水溶液 25mg
合計 最大 385mg
Claims (1)
- N−(2−クロロ−3,4−ジメトキシベンジリデンアミノ)グアニジンの酢酸塩。
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Families Citing this family (67)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU2001269092A1 (en) * | 2000-06-27 | 2002-01-08 | Axxima Pharmaceuticals Ag | Inhibitors of hepatitis b virus infection |
GB0019357D0 (en) | 2000-08-07 | 2000-09-27 | Melacure Therapeutics Ab | Novel phenyl guanidines |
GB0108631D0 (en) * | 2001-04-05 | 2001-05-30 | Melacure Therapeutics Ab | Novel benzylideneamino guanidines and their uses as ligands to the melanocortin receptors |
GB0119172D0 (en) | 2001-08-06 | 2001-09-26 | Melacure Therapeutics Ab | Phenyl pyrrole derivatives |
US7344702B2 (en) | 2004-02-13 | 2008-03-18 | Bristol-Myers Squibb Pharma Company | Contrast agents for myocardial perfusion imaging |
EP1441712A4 (en) * | 2001-10-12 | 2007-05-30 | Cornell Res Foundation Inc | METHOD FOR INVERTING OR PREVENTING PREMATURE VASCULAR SENESCENCE |
EP1487474A4 (en) * | 2002-02-25 | 2006-11-29 | Chiron Corp | INTRANASAL ADMINISTRATION OF MC4-R AGONISTS |
US7105526B2 (en) | 2002-06-28 | 2006-09-12 | Banyu Pharmaceuticals Co., Ltd. | Benzimidazole derivatives |
US7772188B2 (en) | 2003-01-28 | 2010-08-10 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
ATE547404T1 (de) | 2003-09-22 | 2012-03-15 | Msd Kk | Piperidinderivate |
US20080125403A1 (en) | 2004-04-02 | 2008-05-29 | Merck & Co., Inc. | Method of Treating Men with Metabolic and Anthropometric Disorders |
US7737155B2 (en) | 2005-05-17 | 2010-06-15 | Schering Corporation | Nitrogen-containing heterocyclic compounds and methods of use thereof |
NZ562766A (en) | 2005-05-30 | 2011-03-31 | Banyu Pharma Co Ltd | Piperidine derivatives as histamine-H3 receptor antagonists |
JPWO2007018248A1 (ja) | 2005-08-10 | 2009-02-19 | 萬有製薬株式会社 | ピリドン化合物 |
US7875633B2 (en) | 2005-08-24 | 2011-01-25 | Banyu Pharmaceutical Co., Ltd. | Phenylpyridone derivative |
JPWO2007029847A1 (ja) | 2005-09-07 | 2009-03-19 | 萬有製薬株式会社 | 二環性芳香族置換ピリドン誘導体 |
AU2006297443B2 (en) | 2005-09-29 | 2010-08-12 | Merck Sharp & Dohme Corp. | Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators |
BRPI0617621A2 (pt) | 2005-10-21 | 2011-08-02 | Novartis Ag | combinação de compostos orgánicos |
JPWO2007049798A1 (ja) | 2005-10-27 | 2009-04-30 | 萬有製薬株式会社 | 新規ベンゾオキサチイン誘導体 |
NZ568292A (en) | 2005-11-10 | 2011-08-26 | Msd Kk | Spiro[cyclohexane-1,1'-(3'H)-4'-azaisobenzofuran]-4-carboxamide derivatives |
ATE508111T1 (de) | 2006-06-09 | 2011-05-15 | Action Pharma As | Phenylpyrrolaminoguanidinderivate |
CA2664113C (en) | 2006-09-22 | 2013-05-28 | Merck & Co., Inc. | Use of platencin and platensimycin as fatty acid synthesis inhibitors to treat obesity, diabetes and cancer |
EP2072519A4 (en) | 2006-09-28 | 2009-10-21 | Banyu Pharma Co Ltd | DIARYLKETIMINDERIVAT |
GB0623381D0 (en) * | 2006-11-23 | 2007-01-03 | Acure Pharma Ab | Use of a compound as VEGF inhibitor |
GB0624987D0 (en) * | 2006-12-14 | 2007-01-24 | Acure Pharma Ab | Novel aminoguanidines as melanocortin receptor ligands |
PL2114873T3 (pl) | 2006-12-26 | 2013-08-30 | Lantheus Medical Imaging Inc | N-[3-Bromo-4-(3-[18F]fluoropropoksy)-benzylo]-guanidyna do obrazowania unerwienia serca |
CA2682727C (en) | 2007-04-02 | 2016-03-22 | Banyu Pharmaceutical Co., Ltd. | Indoledione derivative |
US8969514B2 (en) | 2007-06-04 | 2015-03-03 | Synergy Pharmaceuticals, Inc. | Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases |
EP2170930B3 (en) | 2007-06-04 | 2013-10-02 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders |
US8442179B2 (en) * | 2007-10-19 | 2013-05-14 | The Boeing Company | Method and apparatus for tagging and identifying a target |
US20110213021A1 (en) * | 2008-03-04 | 2011-09-01 | Indigene Pharmaceuticals, Inc. | Compositions and methods for treating nos-associated diseases |
CA2714617A1 (en) | 2008-03-06 | 2009-09-11 | Banyu Pharmaceutical Co., Ltd. | Alkylaminopyridine derivative |
AU2009229860A1 (en) | 2008-03-28 | 2009-10-01 | Msd K.K. | Diarylmethylamide derivative having antagonistic activity on melanin-concentrating hormone receptor |
AU2009261248A1 (en) | 2008-06-19 | 2009-12-23 | Banyu Pharmaceutical Co., Ltd. | Spirodiamine-diarylketoxime derivative |
AU2009270833B2 (en) | 2008-07-16 | 2015-02-19 | Bausch Health Ireland Limited | Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders |
WO2010013595A1 (ja) | 2008-07-30 | 2010-02-04 | 萬有製薬株式会社 | 5員-5員又は5員-6員縮環シクロアルキルアミン誘導体 |
CN102264228A (zh) | 2008-10-22 | 2011-11-30 | 默沙东公司 | 用于抗糖尿病药的新的环状苯并咪唑衍生物 |
AU2009309037A1 (en) | 2008-10-31 | 2010-05-06 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
EP2379547A1 (en) | 2008-12-16 | 2011-10-26 | Schering Corporation | Pyridopyrimidine derivatives and methods of use thereof |
EP2379562A1 (en) | 2008-12-16 | 2011-10-26 | Schering Corporation | Bicyclic pyranone derivatives as nicotinic acid receptor agonists |
WO2010109192A1 (en) | 2009-03-24 | 2010-09-30 | Anamar Ab | Metabolic profiles |
CA2769541A1 (en) * | 2009-07-31 | 2011-02-03 | Anamar Ab | Compounds for treatment of inflammation |
JP6092628B2 (ja) | 2010-02-08 | 2017-03-08 | ランセウス メディカル イメージング, インコーポレイテッド | 造影剤およびその中間体を合成するための方法および装置 |
AU2011218830B2 (en) | 2010-02-25 | 2014-07-24 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
MX367382B (es) | 2010-05-11 | 2019-08-19 | Lantheus Medical Imaging Inc | Composiciones, metodos y sistemas para la sintesis y el uso de agentes trazadores. |
US9616097B2 (en) | 2010-09-15 | 2017-04-11 | Synergy Pharmaceuticals, Inc. | Formulations of guanylate cyclase C agonists and methods of use |
PE20140859A1 (es) | 2011-02-25 | 2014-07-25 | Merck Sharp & Dohme | Novedosos derivados de azabencimidazol ciclico utiles como agentes antidiabeticos |
SG2014013767A (en) * | 2011-09-09 | 2014-05-29 | Lantheus Medical Imaging Inc | Compositions, methods, and systems for the synthesis and use of imaging agents |
JP2015525782A (ja) | 2012-08-02 | 2015-09-07 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | 抗糖尿病性三環式化合物 |
AU2013203000B9 (en) | 2012-08-10 | 2017-02-02 | Lantheus Medical Imaging, Inc. | Compositions, methods, and systems for the synthesis and use of imaging agents |
GB201300435D0 (en) * | 2013-01-10 | 2013-02-27 | Medical Res Council | Benzylideneguanidine Derivatives and Therapeutic Use for the Treatment of Protein Misfolding Diseases |
EP2958562A4 (en) | 2013-02-22 | 2016-08-10 | Merck Sharp & Dohme | BICYCLIC ANTIDIABETIC COMPOUNDS |
US9650375B2 (en) | 2013-03-14 | 2017-05-16 | Merck Sharp & Dohme Corp. | Indole derivatives useful as anti-diabetic agents |
WO2014151206A1 (en) | 2013-03-15 | 2014-09-25 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase and their uses |
CA2905435A1 (en) | 2013-03-15 | 2014-09-25 | Synergy Pharmaceuticals Inc. | Compositions useful for the treatment of gastrointestinal disorders |
EP3004138B1 (en) | 2013-06-05 | 2024-03-13 | Bausch Health Ireland Limited | Ultra-pure agonists of guanylate cyclase c, method of making and using same |
WO2015051496A1 (en) | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
JP6621815B2 (ja) * | 2014-07-02 | 2019-12-18 | インフレクティス・バイオサイエンス | O−アルキル−ベンジリデングアニジン誘導体、及びミスフォールドタンパク質の蓄積と関連する障害の処置のための治療的使用 |
ES2812800T3 (es) * | 2014-07-02 | 2021-03-18 | Inflectis Bioscience | Nuevos usos terapéuticos de derivados de la bencilidenguanidina para el tratamiento de proteopatías |
AU2015308350B2 (en) | 2014-08-29 | 2020-03-05 | Tes Pharma S.R.L. | Inhibitors of alpha-amino-beta-carboxymuconic acid semialdehyde decarboxylase |
WO2016162689A1 (en) * | 2015-04-08 | 2016-10-13 | Medical Research Council | Inhibitors and their uses |
WO2018069532A1 (en) | 2016-10-14 | 2018-04-19 | Tes Pharma S.R.L. | Inhibitors of alpha-amino-beta-carboxymuconic acid semialdehyde decarboxylase |
EP3551176A4 (en) | 2016-12-06 | 2020-06-24 | Merck Sharp & Dohme Corp. | ANTIDIABETIC HETEROCYCLIC COMPOUNDS |
EP3558298A4 (en) | 2016-12-20 | 2020-08-05 | Merck Sharp & Dohme Corp. | ANTIDIABETIC SPIROCHROMAN COMPOUNDS |
CN108066763A (zh) * | 2017-12-21 | 2018-05-25 | 陈敏 | Pcsk9抑制剂在制备治疗t细胞介导的炎症免疫性疾病药中的应用 |
US20210177814A1 (en) * | 2018-05-09 | 2021-06-17 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of guanabenz or derivates thereof for the treatment of type i ifn-dependent pathologies |
CN113302189A (zh) | 2018-11-20 | 2021-08-24 | Tes制药有限责任公司 | α-氨基-β-羧基己二烯二酸半醛去羧酶的抑制剂 |
Family Cites Families (64)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2584784A (en) | 1949-05-21 | 1952-02-05 | Du Pont | Salts of 1-salicylalaminoguanidine |
GB892117A (en) | 1958-06-20 | 1962-03-21 | May & Baker Ltd | Phenanthridine salts and their preparation |
DE1165013B (de) | 1960-08-09 | 1964-03-12 | Vismara Francesco Spa | Verfahren zur Herstellung von Guanylhydrazonen |
GB923398A (en) | 1960-08-09 | 1963-04-10 | Vismara Francesco Spa | Diphenyl mono-and bis-formyl guanylhydrazones |
GB1019120A (en) | 1964-03-18 | 1966-02-02 | Shell Int Research | Novel hydrazine compounds and compositions containing them |
BE722109A (ja) | 1967-10-12 | 1969-04-10 | ||
GB1223492A (en) | 1967-10-13 | 1971-02-24 | American Home Prod | Guanidines |
CH500953A (de) | 1967-11-13 | 1970-12-31 | Sandoz Ag | Verfahren zur Herstellung von neuen N-Benzyliden-N'-amidinohydrazinen |
US3591636A (en) | 1968-09-16 | 1971-07-06 | Sandoz Ag | Substituted benzylideneamino guanidines |
GB1223493A (en) | 1968-10-11 | 1971-02-24 | American Home Prod | Guanidines |
US3592852A (en) | 1968-12-16 | 1971-07-13 | Sandoz Ag | Substituted benzylideneamino guanidine |
DE2015321A1 (en) | 1969-04-04 | 1970-10-08 | Sandoz Ag, Basel (Schweiz) | Novel guanidine derivs |
FR2036989A1 (en) * | 1969-04-28 | 1970-12-31 | Anvar | Amidino hydrazone antivirals |
US3541218A (en) | 1969-06-18 | 1970-11-17 | Lilly Co Eli | Omicron-fluorobenzylaminoguanidine for diabetes |
US3592935A (en) * | 1969-12-11 | 1971-07-13 | Sandoz Ag | Substituted benzylidene hydrazines as anti-inflammatory agents |
US3982020A (en) * | 1970-03-17 | 1976-09-21 | Sandoz, Inc. | Substituted benzylidene hydrazines for treating hyperglycemia, obesity and inflammation |
US4060640A (en) | 1970-04-29 | 1977-11-29 | Shell Oil Company | Therapeutic agents |
US3975533A (en) * | 1970-04-29 | 1976-08-17 | Shell Oil Company | Therapeutic agents |
JPS4842969B1 (ja) | 1970-12-30 | 1973-12-15 | ||
BE791536A (fr) | 1971-11-19 | 1973-05-17 | Merck & Co Inc | Nouvelles 1,3-diamino guanidines substituees |
US3896232A (en) * | 1973-01-11 | 1975-07-22 | Sandoz Ag | Substituted benzylidene hydrazines as anti-migraine syndrome agents |
US3941825A (en) | 1973-07-27 | 1976-03-02 | American Cyanamid Company | Substituted aminobenzylideneamino guanidine compounds |
US4006249A (en) * | 1975-08-06 | 1977-02-01 | American Home Products Corporation | Systemic treatment of psoriasis |
US4006250A (en) * | 1975-08-25 | 1977-02-01 | American Home Products Corporation | Systemic treatment of psoriasis |
FR2324294A1 (fr) | 1975-09-22 | 1977-04-15 | Roussel Uclaf | Nouveau medicament hypotenseur a action retardee, ainsi que le procede de preparation de ce nouveau medicament |
GB1550401A (en) | 1976-01-07 | 1979-08-15 | Hexachimie | Hydrazine derivatives their preparation and their use |
DE2620369C3 (de) | 1976-05-08 | 1979-01-04 | Bayer Ag, 5090 Leverkusen | Verfahren zur Wiedergewinnung von (l-S)-2-Oxo-bornansulfonat-(10) |
US4312886A (en) | 1978-07-20 | 1982-01-26 | American Home Products Corporation | Prevention of gastric ulcers and depression of gastric secretion by administration of guanabenz |
JPS5562017A (en) | 1978-11-01 | 1980-05-10 | Teijin Ltd | Anti-inflammatory agent comprising guanidine derivative |
US5958933A (en) * | 1982-11-23 | 1999-09-28 | Naftchi; N. Eric | Neurologically active compounds and compounds with multiple activities |
US4983604A (en) | 1987-11-13 | 1991-01-08 | The Rockefeller University | Inhibitors of nonenzymatic cross-linking |
ZA853488B (en) | 1984-05-10 | 1986-12-30 | American Home Prod | Transdermal dosage form |
DE3428342A1 (de) * | 1984-08-01 | 1986-02-13 | Boehringer Ingelheim Vetmedica GmbH, 6507 Ingelheim | Futtermittelzusatz zur verbesserung des wachstums bei landwirtschaftlichen nutztieren |
US6413962B1 (en) * | 1988-05-02 | 2002-07-02 | N. Eric Naftchi | Guanidino compounds effective as anesthetics |
EP0520032B1 (en) | 1990-03-16 | 1998-09-16 | Beth Israel Hospital Association | Use of spiperone as an immunosuppressant and anti-inflammatory agent |
EP0573581A4 (en) | 1991-02-26 | 1994-06-29 | Arc 1 Inc | Compositions and methods of treatment of sympathetically maintained pain |
HUT64023A (en) | 1991-03-22 | 1993-11-29 | Sandoz Ag | Process for producing aminoguanidine derivatives and pharmaceutical compositions comprising such compounds |
WO1993003714A2 (en) * | 1991-08-27 | 1993-03-04 | The Upjohn Company | Method for treatment of metabolic disorders |
US5696128A (en) | 1994-07-07 | 1997-12-09 | The Board Of Supervisors Of Louisiana University And Agricultural And Mechanical College | Method of regulating immune function |
WO1995003286A1 (fr) * | 1993-07-23 | 1995-02-02 | The Green Cross Corporation | Derive de triazole et son utilisation pharmaceutique |
US5599984A (en) * | 1994-01-21 | 1997-02-04 | The Picower Institute For Medical Research | Guanylhydrazones and their use to treat inflammatory conditions |
EP0711553A1 (en) | 1994-08-09 | 1996-05-15 | Mario Cagnoni | Use of the Melatonin in the traetment of the articular symptoms of trheumatoid arthritis |
US5559135A (en) * | 1994-09-14 | 1996-09-24 | Merck & Co., Inc. | Endothelin antagonists bearing pyridyl amides |
WO1996018607A1 (fr) * | 1994-12-12 | 1996-06-20 | Chugai Seiyaku Kabushiki Kaisha | Derive d'aniline inhibant la synthase du monoxyde d'azote |
US5602277A (en) | 1995-03-30 | 1997-02-11 | Biocryst Pharmaceuticals, Inc. | Substituted benzene derivatives useful as neuraminidase inhibitors |
US5958934A (en) | 1996-05-23 | 1999-09-28 | Syntex (U.S.A.) Inc. | Aryl pyrimidine derivatives and uses thereof |
SE9604348D0 (sv) * | 1996-11-26 | 1996-11-26 | Wapharm Ab | Användning av hydroxyguanidiner |
WO1999021571A1 (en) | 1997-10-27 | 1999-05-06 | Trega Biosciences, Inc. | Melanocortin receptor ligands and methods of using same |
WO1999052936A2 (en) | 1998-04-09 | 1999-10-21 | Eisai Co., Ltd. | Arginine peptide analogs useful as fibroblast growth factor antagonists |
WO1999055679A1 (en) | 1998-04-28 | 1999-11-04 | Trega Biosciences, Inc. | Isoquinoline compound melanocortin receptor ligands and methods of using same |
JP2002517444A (ja) | 1998-06-11 | 2002-06-18 | メルク エンド カムパニー インコーポレーテッド | メラノコルチン受容体作動薬としてのスピロピペリジン誘導体 |
AU5671699A (en) | 1998-08-14 | 2000-03-06 | Smithkline Beecham Corporation | Grp receptor ligands |
GB9827500D0 (en) | 1998-12-14 | 1999-02-10 | Wapharm Ab | Compounds for control of eating, growth and body weight |
US6544541B1 (en) * | 1999-06-02 | 2003-04-08 | Cardiovascular Solutions, Inc. | Devices and compounds for treating arterial restenosis |
WO2001005401A1 (en) | 1999-07-16 | 2001-01-25 | Trega Biosciences, Inc. | Melanocortin receptor-3 ligands to treat sexual dysfunction |
AU6528400A (en) | 1999-08-23 | 2001-03-19 | David M. Ockert | Triple drug therapy for the treatment of narcotic and alcohol withdrawal symptoms |
AU7802700A (en) * | 1999-10-06 | 2001-05-10 | Melacure Therapeutics Ab | Guanidine derivatives and their use in the production of a medicament for blocking xanthine oxidase/dehydrogenase |
GB0019357D0 (en) * | 2000-08-07 | 2000-09-27 | Melacure Therapeutics Ab | Novel phenyl guanidines |
GB0019359D0 (en) * | 2000-08-07 | 2000-09-27 | Melacure Therapeutics Ab | Novel guanidines |
GB0108631D0 (en) | 2001-04-05 | 2001-05-30 | Melacure Therapeutics Ab | Novel benzylideneamino guanidines and their uses as ligands to the melanocortin receptors |
GB0119172D0 (en) * | 2001-08-06 | 2001-09-26 | Melacure Therapeutics Ab | Phenyl pyrrole derivatives |
US7060711B2 (en) | 2001-10-25 | 2006-06-13 | Biofrontera Bioscience Gmbh | Derivatives of 4-(thio- or selenoxanthene-9-ylidene)-piperidine or acridine and its use as a selective 5-HT2B receptor antagonist |
GB0622826D0 (en) * | 2006-11-15 | 2006-12-27 | Acurepharma Ab | Novel amides acting on the adenosine receptors |
GB0624987D0 (en) * | 2006-12-14 | 2007-01-24 | Acure Pharma Ab | Novel aminoguanidines as melanocortin receptor ligands |
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KR20030022371A (ko) | 2003-03-15 |
US20070231267A1 (en) | 2007-10-04 |
IL154272A (en) | 2010-12-30 |
US20120178820A1 (en) | 2012-07-12 |
JP5683396B2 (ja) | 2015-03-11 |
US9227927B2 (en) | 2016-01-05 |
US8410174B2 (en) | 2013-04-02 |
JP2004505912A (ja) | 2004-02-26 |
US20040024060A1 (en) | 2004-02-05 |
US20110015437A1 (en) | 2011-01-20 |
WO2002011715A2 (en) | 2002-02-14 |
EP1313461A2 (en) | 2003-05-28 |
GB0019357D0 (en) | 2000-09-27 |
WO2002011715A3 (en) | 2003-01-16 |
US20130295009A1 (en) | 2013-11-07 |
US8148429B2 (en) | 2012-04-03 |
BR0113053A (pt) | 2003-07-08 |
US8309609B2 (en) | 2012-11-13 |
JP2011246471A (ja) | 2011-12-08 |
MXPA03001072A (es) | 2004-03-10 |
US20070088085A1 (en) | 2007-04-19 |
KR100929363B1 (ko) | 2009-12-02 |
ZA200300829B (en) | 2004-02-25 |
IL154272A0 (en) | 2003-09-17 |
CA2417098A1 (en) | 2002-02-14 |
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