JP2019218375A5 - - Google Patents
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- JP2019218375A5 JP2019218375A5 JP2019150947A JP2019150947A JP2019218375A5 JP 2019218375 A5 JP2019218375 A5 JP 2019218375A5 JP 2019150947 A JP2019150947 A JP 2019150947A JP 2019150947 A JP2019150947 A JP 2019150947A JP 2019218375 A5 JP2019218375 A5 JP 2019218375A5
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- Prior art keywords
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- 150000001875 compounds Chemical class 0.000 claims 11
- 201000010099 disease Diseases 0.000 claims 10
- 239000000203 mixture Substances 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 3
- 239000000654 additive Substances 0.000 claims 3
- 125000001118 alkylidene group Chemical group 0.000 claims 3
- OQMYZVWIXPPDDE-UHFFFAOYSA-N 2-(cyclohexylazaniumyl)acetate Chemical compound OC(=O)CNC1CCCCC1 OQMYZVWIXPPDDE-UHFFFAOYSA-N 0.000 claims 2
- WQMQRNCPZFUGID-UHFFFAOYSA-N 2-azaniumyladamantane-2-carboxylate Chemical compound C1C(C2)CC3CC1C(C(O)=O)(N)C2C3 WQMQRNCPZFUGID-UHFFFAOYSA-N 0.000 claims 2
- 230000000996 additive Effects 0.000 claims 2
- 150000001413 amino acids Chemical class 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 238000002405 diagnostic procedure Methods 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- FHJXLSAWYORMMX-UHFFFAOYSA-N 9-aminobicyclo[3.3.1]nonane-9-carboxylic acid Chemical compound C1CCC2CCCC1C2(N)C(O)=O FHJXLSAWYORMMX-UHFFFAOYSA-N 0.000 claims 1
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims 1
- 102100017850 NTSR1 Human genes 0.000 claims 1
- 108060003371 NTSR1 Proteins 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 102000017922 Neurotensin receptor family Human genes 0.000 claims 1
- 108060003370 Neurotensin receptor family Proteins 0.000 claims 1
- 238000004458 analytical method Methods 0.000 claims 1
- 125000004981 cycloalkylmethyl group Chemical group 0.000 claims 1
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 238000002372 labelling Methods 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 238000000746 purification Methods 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Claims (16)
- 式(I)の化合物:
[式中、
R1は、水素、メチルおよびシクロプロピルメチルからなる群から選択され;
AA−COOHは、2−アミノ−2−アダマンタンカルボン酸、シクロヘキシルグリシンおよび9−アミノ−ビシクロ[3.3.1]ノナン−9−カルボン酸からなる群から選択されるアミノ酸であり;
R2は、(C1〜C6)アルキル、(C3〜C8)シクロアルキル、(C3〜C8)シクロアルキルメチル、ハロゲン、ニトロおよびトリフルオロメチルからなる群から選択され;
ALKは、(C2〜C5)アルキリデンであり;
R3、R4およびR5は、それぞれ独立して、水素および(C1〜C4)アルキルからなる群から選択され、但し、R3、R4およびR5の1つは次式(II)
ALK’は、(C2〜C5)アルキリデンであり;
R6は、水素および(C1〜C4)アルキルからなる群から選択され;
R7は、水素である]
またはそれらの薬理学的に許容される塩、溶媒和物もしくは水和物。 - R1がメチルである、請求項1に記載の化合物。
- AA−COOHが2−アミノ−2−アダマンタンカルボン酸およびシクロヘキシルグリシンからなる群から選択されるアミノ酸である、請求項1または2に記載の化合物。
- R2がイソプロピルである、請求項1、2および3のいずれか1項に記載の化合物。
- R3、R4およびR5が、それぞれ独立して、水素およびメチルからなる群から選択され、但し、R3、R4およびR5の1つは次式(II)
ALK’は、(C2〜C5)アルキリデンであり;
R6は、水素および(C1〜C4)アルキルからなる群から選択される]
のものであり、
R7は、請求項1と同様に定義される、
請求項1、2、3または4のいずれか1項に記載の化合物。 - R6が水素およびメチルからなる群から選択される、請求項5に記載の化合物。
- 請求項1から6のいずれか1項に記載の化合物および薬学的に許容される添加剤を含む組成物。
- 請求項1から6のいずれか1項に記載の化合物および薬学的に許容される添加剤を含む医薬組成物。
- 疾患の診断方法において使用するための、請求項7または8のいずれか1項に記載の組成物。
- 疾患の処置方法において使用するための、請求項7または8のいずれか1項に記載の組成物。
- 請求項1から6のいずれか1項に記載の化合物を使用する診断方法を実施することを含む、疾患の処置に応答する可能性が高い、または応答しない可能性が高い対象の同定方法において使用するための、請求項7または8のいずれか1項に記載の組成物。
- 請求項1から6のいずれか1項に記載の化合物を使用する診断方法を実施することを含む、疾患の処置に応答する可能性が高い対象、および疾患の処置に応答しない可能性が高い対象への対象群の層化方法において使用するための、請求項7または8のいずれか1項に記載の組成物。
- 前記疾患がニューロテンシン受容体関連疾患である、請求項9から12のいずれか1項に記載の組成物。
- 前記疾患がニューロテンシン受容体1関連疾患である、請求項13に記載の組成物。
- 前記疾患が腫瘍および血液悪性腫瘍を含む群から選択される、請求項9から12のいずれか1項に記載の組成物。
- 請求項1から6のいずれか1項に記載の化合物、1つまたは複数の任意選択の添加剤および1つまたは複数の任意選択のデバイスを含むキットであって、前記デバイスが標識デバイス、精製デバイス、操作デバイス、放射線防護デバイス、分析デバイスまたは投与デバイスを含む群から選択される、キット。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP12008208.6 | 2012-12-07 | ||
EP12008208.6A EP2740726A1 (en) | 2012-12-07 | 2012-12-07 | Neurotensin receptor ligands |
Related Parent Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2015545697A Division JP6576828B2 (ja) | 2012-12-07 | 2013-12-06 | ニューロテンシン受容体リガンド |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2019218375A JP2019218375A (ja) | 2019-12-26 |
JP2019218375A5 true JP2019218375A5 (ja) | 2020-05-07 |
JP7042776B2 JP7042776B2 (ja) | 2022-03-28 |
Family
ID=47355771
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2015545697A Active JP6576828B2 (ja) | 2012-12-07 | 2013-12-06 | ニューロテンシン受容体リガンド |
JP2019150947A Active JP7042776B2 (ja) | 2012-12-07 | 2019-08-21 | ニューロテンシン受容体リガンド |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2015545697A Active JP6576828B2 (ja) | 2012-12-07 | 2013-12-06 | ニューロテンシン受容体リガンド |
Country Status (21)
Country | Link |
---|---|
US (2) | US10961199B2 (ja) |
EP (3) | EP2740726A1 (ja) |
JP (2) | JP6576828B2 (ja) |
KR (1) | KR102290803B1 (ja) |
CN (2) | CN109320502B (ja) |
AU (1) | AU2013354422B2 (ja) |
BR (1) | BR112015012530B1 (ja) |
CA (1) | CA2893605C (ja) |
DK (2) | DK3712131T3 (ja) |
ES (2) | ES2795923T3 (ja) |
FI (1) | FI3712131T3 (ja) |
HK (1) | HK1210148A1 (ja) |
HU (2) | HUE061839T2 (ja) |
IL (1) | IL239080B (ja) |
MX (1) | MX370354B (ja) |
PL (2) | PL3712131T3 (ja) |
PT (2) | PT2928870T (ja) |
RU (1) | RU2671970C2 (ja) |
SG (2) | SG11201503880YA (ja) |
WO (1) | WO2014086499A1 (ja) |
ZA (1) | ZA201503446B (ja) |
Families Citing this family (17)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2954933A1 (en) * | 2014-06-10 | 2015-12-16 | 3B Pharmaceuticals GmbH | Conjugate comprising a neurotensin receptor ligand |
EP3154638A1 (en) * | 2014-06-10 | 2017-04-19 | 3B Pharmaceuticals GmbH | Conjugate comprising a neurotensin receptor ligand and use thereof |
EP2954934A1 (en) * | 2014-06-11 | 2015-12-16 | 3B Pharmaceuticals GmbH | Conjugate comprising a neurotensin receptor ligand and use thereof |
PT3380495T (pt) | 2015-11-24 | 2021-08-19 | Transfert Plus Sec | Compostos peptídicos e conjugados peptídicos para o tratamento de cancro através de quimioterapia mediada por recetores |
EP3279197A1 (en) | 2016-08-03 | 2018-02-07 | Friedrich-Alexander-Universität Erlangen-Nürnberg | Diagnosis, treatment and prevention of neurotensin receptor-related conditions |
CA3045466A1 (en) | 2016-12-01 | 2018-06-07 | Regeneron Pharmaceuticals, Inc. | Radiolabeled anti-pd-l1 antibodies for immuno-pet imaging |
AU2018219909A1 (en) | 2017-02-10 | 2019-09-12 | Regeneron Pharmaceuticals, Inc. | Radiolabeled anti-LAG3 antibodies for immuno-PET imaging |
BR112020001360A2 (pt) | 2017-07-24 | 2020-08-11 | Regeneron Pharmaceuticals, Inc. | anticorpo monoclonal isolado ou fragmento de ligação a antígeno deste que se liga a cd8, composição farmacêutica, molécula de ácido nucleico, vetor de expressão, célula hospedeira, conjugado de anticorpo, métodos para gerar imagens de um tecido que expressa cd8, para tratar um sujeito tendo um tumor sólido, para prever uma resposta positiva a uma terapia antitumoral, para monitorar uma resposta de um tumor em um sujeito a uma terapia antitumoral, para prever ou monitorar a eficácia da terapia antitumoral e para monitorar a presença de células t em um tumor ao longo do tempo, e, composto. |
CA3145340A1 (en) * | 2019-07-08 | 2021-01-14 | 3B Pharmaceuticals Gmbh | Compounds comprising a fibroblast activation protein ligand and use thereof |
CN111875667B (zh) * | 2020-07-16 | 2021-12-21 | 南方科技大学 | 有机金属螯合物及其制备方法与应用、探针 |
KR20230092982A (ko) * | 2020-10-22 | 2023-06-26 | 니혼 메디피직스 가부시키가이샤 | 방사성 지르코늄 착체의 제조 방법 |
EP4352044A1 (en) * | 2021-05-13 | 2024-04-17 | The General Hospital Corporation | Molecular probes for in vivo detection of aldehydes |
EP4355377A1 (en) * | 2021-06-16 | 2024-04-24 | Fusion Pharmaceuticals Inc. | Combination comprising a neurotensin receptor binding compound, gemcitabine and nab-paclitaxel |
WO2022261770A1 (en) * | 2021-06-16 | 2022-12-22 | Fusion Pharmaceuticals Inc. | Combination comprising a neurotensin receptor binding compound and folfirinox |
WO2023141722A1 (en) * | 2022-01-28 | 2023-08-03 | Fusion Pharmaceuticals Inc. | Ntsr1-targeted radiopharmaceuticals and checkpoint inhibitor combination therapy |
WO2023158802A1 (en) * | 2022-02-18 | 2023-08-24 | Full-Life Technologies U.S. Inc. | Compounds and radioligands for targeting neurotensin receptor and uses thereof |
WO2023215778A1 (en) * | 2022-05-03 | 2023-11-09 | The University Of North Carolina At Chapel Hill | Development of ntsr targeted agents for imaging and therapy applications |
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-
2012
- 2012-12-07 EP EP12008208.6A patent/EP2740726A1/en not_active Withdrawn
-
2013
- 2013-12-06 FI FIEP20166422.4T patent/FI3712131T3/fi active
- 2013-12-06 HU HUE20166422A patent/HUE061839T2/hu unknown
- 2013-12-06 CN CN201811305966.0A patent/CN109320502B/zh active Active
- 2013-12-06 EP EP13814827.5A patent/EP2928870B1/en active Active
- 2013-12-06 PT PT138148275T patent/PT2928870T/pt unknown
- 2013-12-06 PL PL20166422.4T patent/PL3712131T3/pl unknown
- 2013-12-06 PL PL13814827T patent/PL2928870T3/pl unknown
- 2013-12-06 DK DK20166422.4T patent/DK3712131T3/da active
- 2013-12-06 MX MX2015007193A patent/MX370354B/es active IP Right Grant
- 2013-12-06 BR BR112015012530-1A patent/BR112015012530B1/pt active IP Right Grant
- 2013-12-06 CN CN201380063364.8A patent/CN104837819B9/zh active Active
- 2013-12-06 ES ES13814827T patent/ES2795923T3/es active Active
- 2013-12-06 KR KR1020157018171A patent/KR102290803B1/ko active IP Right Grant
- 2013-12-06 HU HUE13814827A patent/HUE050388T2/hu unknown
- 2013-12-06 DK DK13814827.5T patent/DK2928870T3/da active
- 2013-12-06 ES ES20166422T patent/ES2941629T3/es active Active
- 2013-12-06 CA CA2893605A patent/CA2893605C/en active Active
- 2013-12-06 SG SG11201503880YA patent/SG11201503880YA/en unknown
- 2013-12-06 US US14/650,437 patent/US10961199B2/en active Active
- 2013-12-06 EP EP20166422.4A patent/EP3712131B1/en active Active
- 2013-12-06 RU RU2015127086A patent/RU2671970C2/ru active
- 2013-12-06 SG SG10201704564QA patent/SG10201704564QA/en unknown
- 2013-12-06 PT PT201664224T patent/PT3712131T/pt unknown
- 2013-12-06 JP JP2015545697A patent/JP6576828B2/ja active Active
- 2013-12-06 AU AU2013354422A patent/AU2013354422B2/en active Active
- 2013-12-06 WO PCT/EP2013/003700 patent/WO2014086499A1/en active Application Filing
-
2015
- 2015-05-18 ZA ZA2015/03446A patent/ZA201503446B/en unknown
- 2015-05-28 IL IL239080A patent/IL239080B/en active IP Right Grant
- 2015-11-03 HK HK15110838.8A patent/HK1210148A1/xx unknown
-
2019
- 2019-08-21 JP JP2019150947A patent/JP7042776B2/ja active Active
-
2020
- 2020-12-04 US US17/112,258 patent/US20210087149A1/en active Pending
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