JP2013528180A5 - - Google Patents
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- JP2013528180A5 JP2013528180A5 JP2013512234A JP2013512234A JP2013528180A5 JP 2013528180 A5 JP2013528180 A5 JP 2013528180A5 JP 2013512234 A JP2013512234 A JP 2013512234A JP 2013512234 A JP2013512234 A JP 2013512234A JP 2013528180 A5 JP2013528180 A5 JP 2013528180A5
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- compound
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- acceptable salt
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- 150000001875 compounds Chemical class 0.000 claims 21
- 150000003839 salts Chemical class 0.000 claims 7
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 claims 5
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 102000005962 receptors Human genes 0.000 claims 3
- 108020003175 receptors Proteins 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 238000003384 imaging method Methods 0.000 claims 2
- 230000002285 radioactive effect Effects 0.000 claims 2
- 102000040125 5-hydroxytryptamine receptor family Human genes 0.000 claims 1
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 1
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
Claims (14)
- 次の式(I)の化合物又はその薬学的に許容される塩。
Z−Y−L2−N(R1)−L1−X(R2)−Ar
(I)
式中、
Arはアリール又は3員乃至9員の芳香族複素環であり、
N(R 1 )−L 1 −X(R 2 )は、以下の連結性を有するピペラジン基を形成し、
L3は3員乃至9員のシクロアルキル又はヘテロシクロアルキルであり、
Yは存在しないか、或いは結合、S、O、NH、CONH、NHCO又はSO2NHであり、
Zは3員乃至9員の芳香族複素環、アリール、アルキル、シクロアルキル及びヘテロシクロアルキルを含む群から選択されるものであるが、
式(I)の化合物が以下の式の化合物ではないことを条件とする。
- 当該化合物が放射性標識されている、請求項1記載の化合物。
- 当該化合物が放射性標識されていない、請求項1記載の化合物。
- 当該化合物が18F又は11C原子を含む、請求項1記載の化合物。
- 18F又は11C原子がArに直接結合している、請求項1記載の化合物。
- −OCnHm 18F基(式中、nは1〜4であり、mは2〜8である。)又は−O11CH3基がArに直接結合している、請求項1記載の化合物。
- 18F又は11C原子がZ又はZ上の適当な基に直接結合している、請求項1記載の化合物。
- 18F又は11C原子がL2又はL3或いはL2又はL3上の適当な基に直接結合している、請求項1記載の化合物
- 請求項1記載の化合物又は又はその薬学的に許容される塩及び生理学的に許容されるキャリヤー又はビヒクルを含んでなる組成物。
- 被験体における1種以上の5−HT1A受容体をインビボでイメージングするための方法であって、
(a)請求項2記載の化合物又はその薬学的に許容される塩のイメージング有効量を被験体に投与する段階、及び
(b)被験体への投与後、請求項2記載の化合物又はその塩上の放射性標識からの放射性放出物を検出する段階
を含んでなる方法。 - 当該化合物が他のセロトニン受容体に比べて5−HT1A受容体と選択的に結合する、請求項12記載の方法。
- 異常な5−HT1A受容体機能に関連する疾患を治療するための方法に使用される請求項1記載の化合物であって、前記方法がそれを必要とする被験体に請求項1記載の化合物又はその薬学的に許容される塩の有効量を投与することを含む、化合物。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IN1232DE2010 | 2010-05-28 | ||
IN1231DE2010 | 2010-05-28 | ||
IN1232/DEL/2010 | 2010-05-28 | ||
IN1231/DEL/2010 | 2010-05-28 | ||
PCT/US2011/038099 WO2011150183A1 (en) | 2010-05-28 | 2011-05-26 | Radiolabeled compounds and methods thereof |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2013528180A JP2013528180A (ja) | 2013-07-08 |
JP2013528180A5 true JP2013528180A5 (ja) | 2014-07-10 |
Family
ID=44246551
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2013512234A Withdrawn JP2013528180A (ja) | 2010-05-28 | 2011-05-26 | 放射性標識化合物及びその製造方法 |
Country Status (5)
Country | Link |
---|---|
US (1) | US20130064770A1 (ja) |
EP (1) | EP2576520A1 (ja) |
JP (1) | JP2013528180A (ja) |
CN (1) | CN102918031A (ja) |
WO (1) | WO2011150183A1 (ja) |
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CN106831541B (zh) | 2011-11-18 | 2019-09-06 | 赫普泰雅治疗有限公司 | 毒蕈碱性m1受体激动剂 |
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CN104337812B (zh) | 2013-07-29 | 2018-09-14 | 广东东阳光药业有限公司 | 取代的杂芳基化合物及其使用方法和用途 |
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US9714232B2 (en) | 2013-12-20 | 2017-07-25 | Sunshine Lake Pharma Co., Ltd. | Substituted piperazine compounds and methods of use thereof |
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CN103864761B (zh) * | 2014-03-12 | 2016-01-20 | 天津药物研究院有限公司 | 一种含吡啶的哌嗪类衍生物及其制备方法和用途 |
CN107074824B (zh) | 2014-09-05 | 2021-01-08 | 基因泰克公司 | 作为用于治疗癌症的pcaf和gcn5抑制剂的式(i)的酞嗪衍生物 |
JP6814730B2 (ja) * | 2014-09-05 | 2021-01-20 | ジェネンテック, インコーポレイテッド | 治療用化合物およびその使用 |
JP6659703B2 (ja) | 2015-01-09 | 2020-03-04 | ジェネンテック, インコーポレイテッド | ピリダジノン誘導体および癌の処置におけるそれらの使用 |
CN106243088B (zh) | 2015-06-03 | 2019-01-04 | 广东东阳光药业有限公司 | 取代的哌嗪化合物及其使用方法和用途 |
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GB201617454D0 (en) | 2016-10-14 | 2016-11-30 | Heptares Therapeutics Limited | Pharmaceutical compounds |
US10259787B2 (en) | 2016-10-14 | 2019-04-16 | Heptares Therapeutics Limited | Substituted cyclohexanes as muscarinic M1 receptor and/or M4 receptor agonists |
CN110382478A (zh) * | 2017-03-13 | 2019-10-25 | 大日本住友制药株式会社 | 2,6-二取代的吡啶衍生物 |
US11285153B2 (en) | 2017-09-29 | 2022-03-29 | Sunshine Lake Pharma Co., Ltd. | Substituted pyrimidine piperazine compound and use thereof |
CN108440505A (zh) * | 2018-03-30 | 2018-08-24 | 中南大学 | 依他匹隆的全合成方法 |
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JP7382188B2 (ja) * | 2018-09-19 | 2023-11-16 | 住友ファーマ株式会社 | 2,6-ジ置換ピリジン誘導体からなる医薬 |
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GB202020191D0 (en) | 2020-12-18 | 2021-02-03 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
US20220274978A1 (en) * | 2021-02-19 | 2022-09-01 | High Point University | Novel compounds useful for treatment of substance use disorder |
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-
2011
- 2011-05-26 JP JP2013512234A patent/JP2013528180A/ja not_active Withdrawn
- 2011-05-26 US US13/699,155 patent/US20130064770A1/en not_active Abandoned
- 2011-05-26 WO PCT/US2011/038099 patent/WO2011150183A1/en active Application Filing
- 2011-05-26 CN CN2011800265647A patent/CN102918031A/zh active Pending
- 2011-05-26 EP EP11724884.9A patent/EP2576520A1/en not_active Withdrawn