JP2010511687A5 - - Google Patents
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- Publication number
- JP2010511687A5 JP2010511687A5 JP2009539809A JP2009539809A JP2010511687A5 JP 2010511687 A5 JP2010511687 A5 JP 2010511687A5 JP 2009539809 A JP2009539809 A JP 2009539809A JP 2009539809 A JP2009539809 A JP 2009539809A JP 2010511687 A5 JP2010511687 A5 JP 2010511687A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- compound
- item
- target molecule
- chelate
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims description 60
- 238000000034 method Methods 0.000 claims description 22
- 239000013522 chelant Substances 0.000 claims description 20
- 238000006352 cycloaddition reaction Methods 0.000 claims description 18
- 239000001257 hydrogen Substances 0.000 claims description 16
- 229910052739 hydrogen Inorganic materials 0.000 claims description 16
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 16
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 14
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 14
- 125000000524 functional group Chemical group 0.000 claims description 14
- 125000006239 protecting group Chemical group 0.000 claims description 14
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 12
- 150000002431 hydrogen Chemical group 0.000 claims description 12
- 125000001072 heteroaryl group Chemical group 0.000 claims description 10
- 125000002344 aminooxy group Chemical group [H]N([H])O[*] 0.000 claims description 9
- 125000003118 aryl group Chemical group 0.000 claims description 9
- 206010028980 Neoplasm Diseases 0.000 claims description 8
- 125000000217 alkyl group Chemical group 0.000 claims description 8
- 239000003054 catalyst Substances 0.000 claims description 8
- 229910052751 metal Inorganic materials 0.000 claims description 8
- 239000002184 metal Substances 0.000 claims description 8
- 230000015572 biosynthetic process Effects 0.000 claims description 7
- 238000006243 chemical reaction Methods 0.000 claims description 7
- 238000003745 diagnosis Methods 0.000 claims description 7
- 238000003786 synthesis reaction Methods 0.000 claims description 7
- RRBYUSWBLVXTQN-UHFFFAOYSA-N tricyclene Chemical compound C12CC3CC2C1(C)C3(C)C RRBYUSWBLVXTQN-UHFFFAOYSA-N 0.000 claims description 7
- RRBYUSWBLVXTQN-VZCHMASFSA-N tricyclene Natural products C([C@@H]12)C3C[C@H]1C2(C)C3(C)C RRBYUSWBLVXTQN-VZCHMASFSA-N 0.000 claims description 7
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims description 6
- 230000001588 bifunctional effect Effects 0.000 claims description 6
- 239000002738 chelating agent Substances 0.000 claims description 6
- 230000003463 hyperproliferative effect Effects 0.000 claims description 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 6
- RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 claims description 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 4
- 125000002355 alkine group Chemical group 0.000 claims description 4
- 230000029936 alkylation Effects 0.000 claims description 4
- 238000005804 alkylation reaction Methods 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 230000000295 complement effect Effects 0.000 claims description 4
- 229910052802 copper Inorganic materials 0.000 claims description 4
- 239000010949 copper Substances 0.000 claims description 4
- 125000000468 ketone group Chemical group 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 229910052703 rhodium Inorganic materials 0.000 claims description 4
- 239000010948 rhodium Substances 0.000 claims description 4
- MHOVAHRLVXNVSD-UHFFFAOYSA-N rhodium atom Chemical compound [Rh] MHOVAHRLVXNVSD-UHFFFAOYSA-N 0.000 claims description 4
- -1 fluorenylmethyl Chemical group 0.000 claims description 3
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 3
- 125000001399 1,2,3-triazolyl group Chemical group N1N=NC(=C1)* 0.000 claims description 2
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 2
- 229910052692 Dysprosium Inorganic materials 0.000 claims description 2
- GYHNNYVSQQEPJS-OIOBTWANSA-N Gallium-67 Chemical compound [67Ga] GYHNNYVSQQEPJS-OIOBTWANSA-N 0.000 claims description 2
- GYHNNYVSQQEPJS-YPZZEJLDSA-N Gallium-68 Chemical compound [68Ga] GYHNNYVSQQEPJS-YPZZEJLDSA-N 0.000 claims description 2
- VWQVUPCCIRVNHF-OIOBTWANSA-N Yttrium-86 Chemical compound [86Y] VWQVUPCCIRVNHF-OIOBTWANSA-N 0.000 claims description 2
- VWQVUPCCIRVNHF-OUBTZVSYSA-N Yttrium-90 Chemical compound [90Y] VWQVUPCCIRVNHF-OUBTZVSYSA-N 0.000 claims description 2
- QQINRWTZWGJFDB-YPZZEJLDSA-N actinium-225 Chemical compound [225Ac] QQINRWTZWGJFDB-YPZZEJLDSA-N 0.000 claims description 2
- 229940125666 actinium-225 Drugs 0.000 claims description 2
- IVRMZWNICZWHMI-UHFFFAOYSA-N azide group Chemical group [N-]=[N+]=[N-] IVRMZWNICZWHMI-UHFFFAOYSA-N 0.000 claims description 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 2
- JCXGWMGPZLAOME-AKLPVKDBSA-N bismuth-212 Chemical compound [212Bi] JCXGWMGPZLAOME-AKLPVKDBSA-N 0.000 claims description 2
- JCXGWMGPZLAOME-RNFDNDRNSA-N bismuth-213 Chemical compound [213Bi] JCXGWMGPZLAOME-RNFDNDRNSA-N 0.000 claims description 2
- 125000006243 carbonyl protecting group Chemical group 0.000 claims description 2
- 230000009918 complex formation Effects 0.000 claims description 2
- 230000021615 conjugation Effects 0.000 claims description 2
- RYGMFSIKBFXOCR-IGMARMGPSA-N copper-64 Chemical compound [64Cu] RYGMFSIKBFXOCR-IGMARMGPSA-N 0.000 claims description 2
- RYGMFSIKBFXOCR-AKLPVKDBSA-N copper-67 Chemical compound [67Cu] RYGMFSIKBFXOCR-AKLPVKDBSA-N 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- KBQHZAAAGSGFKK-UHFFFAOYSA-N dysprosium atom Chemical compound [Dy] KBQHZAAAGSGFKK-UHFFFAOYSA-N 0.000 claims description 2
- KBQHZAAAGSGFKK-BJUDXGSMSA-N dysprosium-162 Chemical compound [162Dy] KBQHZAAAGSGFKK-BJUDXGSMSA-N 0.000 claims description 2
- KBQHZAAAGSGFKK-NJFSPNSNSA-N dysprosium-165 Chemical compound [165Dy] KBQHZAAAGSGFKK-NJFSPNSNSA-N 0.000 claims description 2
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims description 2
- GYHNNYVSQQEPJS-AHCXROLUSA-N gallium-66 Chemical compound [66Ga] GYHNNYVSQQEPJS-AHCXROLUSA-N 0.000 claims description 2
- 229940006110 gallium-67 Drugs 0.000 claims description 2
- 125000000623 heterocyclic group Chemical group 0.000 claims description 2
- KJZYNXUDTRRSPN-OUBTZVSYSA-N holmium-166 Chemical compound [166Ho] KJZYNXUDTRRSPN-OUBTZVSYSA-N 0.000 claims description 2
- 239000005556 hormone Substances 0.000 claims description 2
- 229940088597 hormone Drugs 0.000 claims description 2
- APFVFJFRJDLVQX-AHCXROLUSA-N indium-111 Chemical compound [111In] APFVFJFRJDLVQX-AHCXROLUSA-N 0.000 claims description 2
- 229940055742 indium-111 Drugs 0.000 claims description 2
- APFVFJFRJDLVQX-YPZZEJLDSA-N indium-113 Chemical compound [113In] APFVFJFRJDLVQX-YPZZEJLDSA-N 0.000 claims description 2
- WABPQHHGFIMREM-AHCXROLUSA-N lead-203 Chemical compound [203Pb] WABPQHHGFIMREM-AHCXROLUSA-N 0.000 claims description 2
- OHSVLFRHMCKCQY-NJFSPNSNSA-N lutetium-177 Chemical compound [177Lu] OHSVLFRHMCKCQY-NJFSPNSNSA-N 0.000 claims description 2
- 229910021645 metal ion Inorganic materials 0.000 claims description 2
- 230000001613 neoplastic effect Effects 0.000 claims description 2
- PUDIUYLPXJFUGB-OUBTZVSYSA-N praseodymium-142 Chemical compound [142Pr] PUDIUYLPXJFUGB-OUBTZVSYSA-N 0.000 claims description 2
- PUDIUYLPXJFUGB-NJFSPNSNSA-N praseodymium-143 Chemical compound [143Pr] PUDIUYLPXJFUGB-NJFSPNSNSA-N 0.000 claims description 2
- 238000002360 preparation method Methods 0.000 claims description 2
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 2
- VQMWBBYLQSCNPO-RNFDNDRNSA-N promethium-149 Chemical compound [149Pm] VQMWBBYLQSCNPO-RNFDNDRNSA-N 0.000 claims description 2
- 238000007363 ring formation reaction Methods 0.000 claims description 2
- 229910052979 sodium sulfide Inorganic materials 0.000 claims description 2
- GRVFOGOEDUUMBP-UHFFFAOYSA-N sodium sulfide (anhydrous) Chemical compound [Na+].[Na+].[S-2] GRVFOGOEDUUMBP-UHFFFAOYSA-N 0.000 claims description 2
- 239000002904 solvent Substances 0.000 claims description 2
- 230000002194 synthesizing effect Effects 0.000 claims description 2
- GZCRRIHWUXGPOV-CBESVEIWSA-N terbium-149 Chemical compound [149Tb] GZCRRIHWUXGPOV-CBESVEIWSA-N 0.000 claims description 2
- 238000002560 therapeutic procedure Methods 0.000 claims description 2
- 229910052723 transition metal Inorganic materials 0.000 claims description 2
- 150000003624 transition metals Chemical class 0.000 claims description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 2
- QBPPRVHXOZRESW-UHFFFAOYSA-N 1,4,7,10-tetraazacyclododecane Chemical compound C1CNCCNCCNCCN1 QBPPRVHXOZRESW-UHFFFAOYSA-N 0.000 claims 1
- 238000010189 synthetic method Methods 0.000 claims 1
- 0 *CN(CCN(C*)CC1)CCN(C*)CCN1C(*)C(O)=O Chemical compound *CN(CCN(C*)CC1)CCN(C*)CCN1C(*)C(O)=O 0.000 description 5
- 125000003277 amino group Chemical group 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0624587.2A GB0624587D0 (en) | 2006-12-08 | 2006-12-08 | Chelating agent |
| GB0624587.2 | 2006-12-08 | ||
| PCT/GB2007/004733 WO2008068516A1 (en) | 2006-12-08 | 2007-12-10 | Chelating agent |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015034980A Division JP2015155407A (ja) | 2006-12-08 | 2015-02-25 | キレート剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010511687A JP2010511687A (ja) | 2010-04-15 |
| JP2010511687A5 true JP2010511687A5 (enExample) | 2012-01-05 |
| JP5705434B2 JP5705434B2 (ja) | 2015-04-22 |
Family
ID=37711827
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009539809A Expired - Fee Related JP5705434B2 (ja) | 2006-12-08 | 2007-12-10 | キレート剤 |
| JP2015034980A Pending JP2015155407A (ja) | 2006-12-08 | 2015-02-25 | キレート剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015034980A Pending JP2015155407A (ja) | 2006-12-08 | 2015-02-25 | キレート剤 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20100081799A1 (enExample) |
| EP (1) | EP2099776B1 (enExample) |
| JP (2) | JP5705434B2 (enExample) |
| CN (1) | CN101605768A (enExample) |
| CA (1) | CA2671788A1 (enExample) |
| GB (1) | GB0624587D0 (enExample) |
| IN (1) | IN2009CN02681A (enExample) |
| WO (1) | WO2008068516A1 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0624587D0 (en) * | 2006-12-08 | 2007-01-17 | Univ Muenchen Tech | Chelating agent |
| CN102898392B (zh) * | 2012-09-06 | 2015-08-12 | 中国工程物理研究院核物理与化学研究所 | N-乙酰氧苄基-3-[-三叔丁氧甲酰基-四氮杂环十二烷基]中间体及其制备方法 |
| CN104230832B (zh) * | 2014-08-25 | 2018-07-27 | 曲靖师范学院 | 一种4，4’，4”，4”’-(1，4，7，10-四氮杂环十二烷-1，4，7，10-四基)四亚甲基四苯甲醛的合成方法 |
| CN104307495A (zh) * | 2014-10-14 | 2015-01-28 | 常州大学 | 一种含有四氮杂环的新型螯合树脂及其制备方法 |
| WO2018183906A1 (en) | 2017-03-30 | 2018-10-04 | Cornell University | Macrocyclic complexes of alpha-emitting radionuclides and their use in targeted radiotherapy of cancer |
| CN117603148A (zh) | 2017-05-05 | 2024-02-27 | 探针技术开发及商业化中心 | 双官能螯合物的药代动力学增强及其用途 |
| KR20200004861A (ko) * | 2017-05-05 | 2020-01-14 | 퓨전 파마슈티칼즈 인크. | Igf-1r 모노클로날 항체 및 그의 용도 |
| US10093741B1 (en) | 2017-05-05 | 2018-10-09 | Fusion Pharmaceuticals Inc. | IGF-1R monoclonal antibodies and uses thereof |
| KR102152939B1 (ko) * | 2019-04-30 | 2020-09-07 | 한국화학연구원 | 공유결합성 트리아졸로 연결된 가시광선 흡수 광촉매, 이의 제조방법 및 이를 이용한 아자이드-알카인 고리화 첨가반응으로 트리아졸 유도체를 제조하는 방법 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1033030C (zh) * | 1988-06-24 | 1996-10-16 | 唐化学原料公司 | 大环双官能螯合剂及其配合物和抗体共轭物的制备方法 |
| DE353450T1 (de) * | 1988-06-24 | 1990-09-06 | The Dow Chemical Co., Midland, Mich. | Macrocyclische bifunktionelle chelatbildner, komplexe davon und ihre konjugierten antikoerper. |
| US6093382A (en) * | 1998-05-16 | 2000-07-25 | Bracco Research Usa Inc. | Metal complexes derivatized with folate for use in diagnostic and therapeutic applications |
| ES2312983T3 (es) * | 2003-03-19 | 2009-03-01 | Universitatsspital Basel | Conjugados radiomarcados basados en sustancia p y sus usos. |
| WO2005001415A2 (en) * | 2003-05-23 | 2005-01-06 | Epix Pharmaceuticals, Inc. | Optically pure and enriched isomers of chelating ligands and contrast agents |
| WO2006110745A2 (en) * | 2005-04-08 | 2006-10-19 | Cytogen Corporation | Conjugated anti-psma antibodies |
| GB0624587D0 (en) * | 2006-12-08 | 2007-01-17 | Univ Muenchen Tech | Chelating agent |
-
2006
- 2006-12-08 GB GBGB0624587.2A patent/GB0624587D0/en not_active Ceased
-
2007
- 2007-10-10 IN IN2681CHN2009 patent/IN2009CN02681A/en unknown
- 2007-12-10 JP JP2009539809A patent/JP5705434B2/ja not_active Expired - Fee Related
- 2007-12-10 WO PCT/GB2007/004733 patent/WO2008068516A1/en not_active Ceased
- 2007-12-10 EP EP07848478.9A patent/EP2099776B1/en not_active Not-in-force
- 2007-12-10 US US12/517,206 patent/US20100081799A1/en not_active Abandoned
- 2007-12-10 CA CA002671788A patent/CA2671788A1/en not_active Abandoned
- 2007-12-10 CN CNA2007800452581A patent/CN101605768A/zh active Pending
-
2015
- 2015-02-25 JP JP2015034980A patent/JP2015155407A/ja active Pending
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