JP2018058847A5 - - Google Patents
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- JP2018058847A5 JP2018058847A5 JP2017210775A JP2017210775A JP2018058847A5 JP 2018058847 A5 JP2018058847 A5 JP 2018058847A5 JP 2017210775 A JP2017210775 A JP 2017210775A JP 2017210775 A JP2017210775 A JP 2017210775A JP 2018058847 A5 JP2018058847 A5 JP 2018058847A5
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- 150000001875 compounds Chemical class 0.000 claims description 26
- 239000003937 drug carrier Substances 0.000 claims description 6
- 239000002738 chelating agent Substances 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims 9
- 102100001249 ALB Human genes 0.000 claims 1
- 101710027066 ALB Proteins 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N D-Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- FBPFZTCFMRRESA-KAZBKCHUSA-N D-Mannitol Natural products OC[C@@H](O)[C@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KAZBKCHUSA-N 0.000 claims 1
- GUBGYTABKSRVRQ-UUNJERMWSA-N Lactose Natural products O([C@@H]1[C@H](O)[C@H](O)[C@H](O)O[C@@H]1CO)[C@H]1[C@@H](O)[C@@H](O)[C@H](O)[C@H](CO)O1 GUBGYTABKSRVRQ-UUNJERMWSA-N 0.000 claims 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N Mannitol Chemical group OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
- 229940050528 albumin Drugs 0.000 claims 1
- 239000008366 buffered solution Substances 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N β-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
- 150000004696 coordination complex Chemical class 0.000 description 5
- 206010027476 Metastasis Diseases 0.000 description 2
- 206010060862 Prostate cancer Diseases 0.000 description 2
- WDLRUFUQRNWCPK-UHFFFAOYSA-N Tetraxetan Chemical compound OC(=O)CN1CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC1 WDLRUFUQRNWCPK-UHFFFAOYSA-N 0.000 description 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Natural products NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 2
- 239000004202 carbamide Substances 0.000 description 2
- 150000002148 esters Chemical class 0.000 description 1
- 238000003384 imaging method Methods 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 229910052751 metal Inorganic materials 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
Description
即ち、本発明の要旨は、
〔1〕式(Ia)または(Ib):
、式中
の化合物、
〔2〕R'-リンカー-R構造を有する化合物であり、ここでR'=-DOTAであり、R=-Glu-尿素-Lys:
であり、
式中、R'-リンカー-Rは、
から選択される、〔1〕記載の化合物、
〔3〕以下:
から選択される、〔1〕または〔2〕記載の化合物、
〔4〕放射線標識化合物の調製のための〔1〕〜〔3〕いずれか記載の化合物の使用、
〔5〕放射線核種および〔1〕〜〔3〕いずれか記載の化合物を含む、金属複合体、
〔6〕放射線核種が、111In、90Y、68Ga、177Lu、99mTc、64Cu、153Gd、155Gd、157Gd、213Bi、225AcまたはFeである、〔5〕記載の金属複合体、
〔7〕〔1〕〜〔3〕いずれか記載の化合物、または〔5〕または〔6〕記載の金属複合体、またはその薬学的に許容され得る塩もしくはエステル、および薬学的に許容され得る担体を含む、医薬組成物、
〔8〕患者における画像化方法における使用のための、〔1〕〜〔3〕いずれか記載の化合物または〔5〕または〔6〕記載の金属複合体、
〔9〕前立腺癌および/またはその転移の診断方法における使用のための、〔1〕〜〔3〕いずれか記載の化合物または〔5〕または〔6〕記載の金属複合体、
〔10〕前立腺癌および/またはその転移の治療方法における使用のための、〔1〕〜〔3〕いずれか記載の化合物または〔5〕または〔6〕記載の金属複合体
に関する。
〔1〕式(Ia)または(Ib):
〔2〕R'-リンカー-R構造を有する化合物であり、ここでR'=-DOTAであり、R=-Glu-尿素-Lys:
であり、
式中、R'-リンカー-Rは、
から選択される、〔1〕記載の化合物、
〔3〕以下:
から選択される、〔1〕または〔2〕記載の化合物、
〔4〕放射線標識化合物の調製のための〔1〕〜〔3〕いずれか記載の化合物の使用、
〔5〕放射線核種および〔1〕〜〔3〕いずれか記載の化合物を含む、金属複合体、
〔6〕放射線核種が、111In、90Y、68Ga、177Lu、99mTc、64Cu、153Gd、155Gd、157Gd、213Bi、225AcまたはFeである、〔5〕記載の金属複合体、
〔7〕〔1〕〜〔3〕いずれか記載の化合物、または〔5〕または〔6〕記載の金属複合体、またはその薬学的に許容され得る塩もしくはエステル、および薬学的に許容され得る担体を含む、医薬組成物、
〔8〕患者における画像化方法における使用のための、〔1〕〜〔3〕いずれか記載の化合物または〔5〕または〔6〕記載の金属複合体、
〔9〕前立腺癌および/またはその転移の診断方法における使用のための、〔1〕〜〔3〕いずれか記載の化合物または〔5〕または〔6〕記載の金属複合体、
〔10〕前立腺癌および/またはその転移の治療方法における使用のための、〔1〕〜〔3〕いずれか記載の化合物または〔5〕または〔6〕記載の金属複合体
に関する。
したがって、本発明は、一般式(Ia)または(Ib):
で表され、式中
である化合物に関する。
異なる好ましいリンカーを以下に示し、上述のように、式中、R=−Glu-尿素-Lysであり、R'=−DOTA(キレート剤についての好ましい例として)である。
Claims (20)
- 下記式:
- 前記化合物が凍結乾燥された請求項1に記載の化合物。
- 請求項1記載の化合物および薬学的に許容され得る担体を含む医薬組成物であって、請求項1記載の化合物および薬学的に許容され得る担体が凍結乾燥されている医薬組成物。
- 前記薬学的に許容され得る担体がマンニトール、ラクトース、グルコース、およびアルブミンから選択される請求項3に記載の医薬組成物。
- 請求項1に記載の化合物の立体異性体。
- 下記式:
(式中、R’は、下記式の−キレート剤:
を表し、
前記−キレート剤は、放射性核種と複合体化される。)の化合物。 - 前記放射性核種が、 89 Zr、 44 Sc、 111 In、 90 Y、 68 Ga、 177 Lu、 99m Tc、 64 Cu、 67 Cu、 153 Gd、 155 Gd、 157 Gd、 213 Bi、および 225 Acからなる群から選択される、請求項6に記載の化合物。
- 前記放射性核種が、 64 Cu、 67 Cu、 68 Ga、 177 Lu、および 225 Acからなる群から選択される、請求項6または7に記載の化合物。
- 前記放射性核種が、 68 Gaである、請求項6または7に記載の化合物。
- 前記放射性核種が、 177 Luである、請求項6または7に記載の化合物。
- 前記放射性核種が、 225 Acである、請求項6または7に記載の化合物。
- 前記放射性核種が、 64 Cuおよび 67 Cuからなる群から選択される、請求項6または7に記載の化合物。
- (1)下記式:
(式中、R’は、下記式の−キレート剤:
を表し、
前記−キレート剤は、放射性核種と複合体化される。)の化合物、および。
(2)薬学的に許容され得る担体、
を含む医薬組成物。 - 前記放射性核種が、 89 Zr、 44 Sc、 111 In、 90 Y、 68 Ga、 177 Lu、 99m Tc、 64 Cu、 67 Cu、 153 Gd、 155 Gd、 157 Gd、 213 Bi、および 225 Acからなる群から選択され、前記組成物はさらに賦形剤を含み、前記賦形剤は前記薬学的に許容され得る担体とは異なる、請求項13に記載の組成物。
- 前記放射性核種が、 64 Cu、 67 Cu、 68 Ga、 177 Lu、および 225 Acからなる群から選択される、請求項14に記載の組成物。
- 前記放射性核種が、 68 Gaである、請求項14または15に記載の組成物。
- 前記放射性核種が、 177 Luである、請求項14または15に記載の組成物。
- 前記放射性核種が、 225 Acである、請求項14または15に記載の組成物。
- 前記放射性核種が、 64 Cuおよび 67 Cuからなる群から選択される、請求項14または15に記載の組成物。
- 前記組成物が緩衝化された溶液である、請求項14または15に記載の組成物。
Priority Applications (1)
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JP2018193272A JP6901451B2 (ja) | 2013-10-18 | 2018-10-12 | 前立腺特異的膜抗原(psma)の標識インヒビター、前立腺癌の治療のための画像化剤および薬剤としてのその使用 |
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---|---|---|---|
EP13004991.9 | 2013-10-18 | ||
EP20130004991 EP2862857A1 (en) | 2013-10-18 | 2013-10-18 | Labeled inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer |
EP14175612.2 | 2014-07-03 | ||
EP14175612 | 2014-07-03 |
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JP2016524427A Division JP2016535013A (ja) | 2013-10-18 | 2014-10-17 | 前立腺特異的膜抗原(psma)の標識インヒビター、前立腺癌の治療のための画像化剤および薬剤としてのその使用 |
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JP2018193272A Division JP6901451B2 (ja) | 2013-10-18 | 2018-10-12 | 前立腺特異的膜抗原(psma)の標識インヒビター、前立腺癌の治療のための画像化剤および薬剤としてのその使用 |
JP2019128294A Division JP7036774B2 (ja) | 2013-10-18 | 2019-07-10 | 前立腺特異的膜抗原(psma)の標識インヒビター、前立腺癌の治療のための画像化剤および薬剤としてのその使用 |
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JP2018058847A JP2018058847A (ja) | 2018-04-12 |
JP2018058847A5 true JP2018058847A5 (ja) | 2018-08-30 |
JP6556805B2 JP6556805B2 (ja) | 2019-08-07 |
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JP2017210775A Active JP6556805B2 (ja) | 2013-10-18 | 2017-10-31 | 前立腺特異的膜抗原(psma)の標識インヒビター、前立腺癌の治療のための画像化剤および薬剤としてのその使用 |
JP2018193272A Active JP6901451B2 (ja) | 2013-10-18 | 2018-10-12 | 前立腺特異的膜抗原(psma)の標識インヒビター、前立腺癌の治療のための画像化剤および薬剤としてのその使用 |
JP2019128294A Active JP7036774B2 (ja) | 2013-10-18 | 2019-07-10 | 前立腺特異的膜抗原(psma)の標識インヒビター、前立腺癌の治療のための画像化剤および薬剤としてのその使用 |
JP2020203704A Active JP7194161B2 (ja) | 2013-10-18 | 2020-12-08 | 前立腺特異的膜抗原(psma)の標識インヒビター、前立腺癌の治療のための画像化剤および薬剤としてのその使用 |
JP2022122499A Active JP7393485B2 (ja) | 2013-10-18 | 2022-08-01 | 前立腺特異的膜抗原(psma)の標識インヒビター、前立腺癌の治療のための画像化剤および薬剤としてのその使用 |
JP2023198760A Pending JP2024028742A (ja) | 2013-10-18 | 2023-11-24 | 前立腺特異的膜抗原(psma)の標識インヒビター、前立腺癌の治療のための画像化剤および薬剤としてのその使用 |
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JP2019128294A Active JP7036774B2 (ja) | 2013-10-18 | 2019-07-10 | 前立腺特異的膜抗原(psma)の標識インヒビター、前立腺癌の治療のための画像化剤および薬剤としてのその使用 |
JP2020203704A Active JP7194161B2 (ja) | 2013-10-18 | 2020-12-08 | 前立腺特異的膜抗原(psma)の標識インヒビター、前立腺癌の治療のための画像化剤および薬剤としてのその使用 |
JP2022122499A Active JP7393485B2 (ja) | 2013-10-18 | 2022-08-01 | 前立腺特異的膜抗原(psma)の標識インヒビター、前立腺癌の治療のための画像化剤および薬剤としてのその使用 |
JP2023198760A Pending JP2024028742A (ja) | 2013-10-18 | 2023-11-24 | 前立腺特異的膜抗原(psma)の標識インヒビター、前立腺癌の治療のための画像化剤および薬剤としてのその使用 |
Country Status (32)
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US (7) | US20160228587A1 (ja) |
EP (6) | EP3495355A1 (ja) |
JP (7) | JP2016535013A (ja) |
KR (3) | KR102282378B1 (ja) |
CN (2) | CN109053616B (ja) |
AU (3) | AU2014336638C1 (ja) |
CA (1) | CA2924360C (ja) |
CL (1) | CL2016000883A1 (ja) |
DE (2) | DE202014011593U1 (ja) |
DK (1) | DK4095130T3 (ja) |
EA (1) | EA037778B1 (ja) |
FI (2) | FI4095130T3 (ja) |
GE (4) | GEP20237496B (ja) |
HK (1) | HK1221711A1 (ja) |
HR (1) | HRP20240398T1 (ja) |
HU (1) | HUE066137T2 (ja) |
IL (2) | IL245113B (ja) |
LT (1) | LT4095130T (ja) |
MX (3) | MX2016005013A (ja) |
MY (2) | MY188934A (ja) |
NL (1) | NL301281I2 (ja) |
NZ (1) | NZ718812A (ja) |
PE (2) | PE20211760A1 (ja) |
PH (1) | PH12016500656B1 (ja) |
PL (1) | PL4095130T3 (ja) |
RS (1) | RS65324B1 (ja) |
SA (1) | SA516370842B1 (ja) |
SG (1) | SG11201602249RA (ja) |
SI (1) | SI4095130T1 (ja) |
TN (1) | TN2016000137A1 (ja) |
WO (1) | WO2015055318A1 (ja) |
ZA (2) | ZA201603380B (ja) |
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