JP2016519106A5 - - Google Patents
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- JP2016519106A5 JP2016519106A5 JP2016507631A JP2016507631A JP2016519106A5 JP 2016519106 A5 JP2016519106 A5 JP 2016519106A5 JP 2016507631 A JP2016507631 A JP 2016507631A JP 2016507631 A JP2016507631 A JP 2016507631A JP 2016519106 A5 JP2016519106 A5 JP 2016519106A5
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- Japan
- Prior art keywords
- compound
- glycine
- use according
- bond
- phenylalanine
- 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.)
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- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 29
- 150000001875 compounds Chemical class 0.000 claims 26
- 239000004471 Glycine Substances 0.000 claims 11
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims 8
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims 8
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims 8
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 8
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims 8
- 235000008729 phenylalanine Nutrition 0.000 claims 8
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims 7
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 claims 7
- 239000004474 valine Substances 0.000 claims 7
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 claims 5
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims 5
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 claims 5
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 claims 5
- QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 claims 5
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims 5
- QIVBCDIJIAJPQS-UHFFFAOYSA-N Tryptophan Natural products C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 claims 5
- 235000004279 alanine Nutrition 0.000 claims 5
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- 229960001230 asparagine Drugs 0.000 claims 5
- 229930182817 methionine Natural products 0.000 claims 5
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims 5
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims 4
- 102000004877 Insulin Human genes 0.000 claims 4
- 108090001061 Insulin Proteins 0.000 claims 4
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 claims 4
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 claims 4
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims 4
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims 4
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 claims 4
- 239000004473 Threonine Substances 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 claims 4
- 235000004554 glutamine Nutrition 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 229940125396 insulin Drugs 0.000 claims 4
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 claims 4
- 229960000310 isoleucine Drugs 0.000 claims 4
- 239000004475 Arginine Substances 0.000 claims 3
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 3
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims 3
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 claims 3
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 claims 3
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims 3
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 3
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 claims 3
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 3
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 3
- 239000004472 Lysine Substances 0.000 claims 3
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims 3
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims 3
- 235000003704 aspartic acid Nutrition 0.000 claims 3
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 claims 3
- 239000008280 blood Substances 0.000 claims 3
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- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 3
- 235000018417 cysteine Nutrition 0.000 claims 3
- 239000008103 glucose Substances 0.000 claims 3
- 235000013922 glutamic acid Nutrition 0.000 claims 3
- 239000004220 glutamic acid Substances 0.000 claims 3
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 claims 3
- 108010074051 C-Reactive Protein Proteins 0.000 claims 2
- 102100032752 C-reactive protein Human genes 0.000 claims 2
- 206010022489 Insulin Resistance Diseases 0.000 claims 2
- 102000016267 Leptin Human genes 0.000 claims 2
- 108010092277 Leptin Proteins 0.000 claims 2
- 230000005856 abnormality Effects 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 230000037396 body weight Effects 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 208000019622 heart disease Diseases 0.000 claims 2
- NRYBAZVQPHGZNS-ZSOCWYAHSA-N leptin Chemical compound O=C([C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(C)C)CCSC)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CS)C(O)=O NRYBAZVQPHGZNS-ZSOCWYAHSA-N 0.000 claims 2
- 229940039781 leptin Drugs 0.000 claims 2
- 239000002207 metabolite Substances 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
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- 239000000651 prodrug Substances 0.000 claims 2
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- -1 2-hydroxypropyl Chemical group 0.000 claims 1
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- RHGKLRLOHDJJDR-BYPYZUCNSA-N L-citrulline Chemical compound NC(=O)NCCC[C@H]([NH3+])C([O-])=O RHGKLRLOHDJJDR-BYPYZUCNSA-N 0.000 claims 1
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- 229940122028 Methionine aminopeptidase-2 inhibitor Drugs 0.000 claims 1
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- RHGKLRLOHDJJDR-UHFFFAOYSA-N Ndelta-carbamoyl-DL-ornithine Natural products OC(=O)C(N)CCCNC(N)=O RHGKLRLOHDJJDR-UHFFFAOYSA-N 0.000 claims 1
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- 125000004423 acyloxy group Chemical group 0.000 claims 1
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- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
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- 206010008118 cerebral infarction Diseases 0.000 claims 1
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- 150000004820 halides Chemical class 0.000 claims 1
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- 125000000623 heterocyclic group Chemical group 0.000 claims 1
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- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims 1
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- 0 CC(C)(C(C(C(CC1)OC(N[C@](CC2)CC[C@@]2NC(CN****)=O)=O)OC)[C@]11OC1)OCC=C(C)C Chemical compound CC(C)(C(C(C(CC1)OC(N[C@](CC2)CC[C@@]2NC(CN****)=O)=O)OC)[C@]11OC1)OCC=C(C)C 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361810468P | 2013-04-10 | 2013-04-10 | |
| US61/810,468 | 2013-04-10 | ||
| US201461925918P | 2014-01-10 | 2014-01-10 | |
| US61/925,918 | 2014-01-10 | ||
| PCT/US2014/033476 WO2014169026A1 (en) | 2013-04-10 | 2014-04-09 | Metap2 inhibitors and methods of treating obesity |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018192578A Division JP2019023219A (ja) | 2013-04-10 | 2018-10-11 | Ｍｅｔａｐ２阻害剤及び肥満症の治療方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016519106A JP2016519106A (ja) | 2016-06-30 |
| JP2016519106A5 true JP2016519106A5 (enExample) | 2017-04-13 |
| JP6420314B2 JP6420314B2 (ja) | 2018-11-07 |
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Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016507631A Active JP6420314B2 (ja) | 2013-04-10 | 2014-04-09 | Ｍｅｔａｐ２阻害剤及び肥満症の治療方法 |
| JP2018192578A Pending JP2019023219A (ja) | 2013-04-10 | 2018-10-11 | Ｍｅｔａｐ２阻害剤及び肥満症の治療方法 |
| JP2021043481A Pending JP2021091738A (ja) | 2013-04-10 | 2021-03-17 | Ｍｅｔａｐ２阻害剤及び肥満症の治療方法 |
| JP2023061783A Active JP7681054B2 (ja) | 2013-04-10 | 2023-04-05 | Ｍｅｔａｐ２阻害剤及び肥満症の治療方法 |
| JP2025078682A Pending JP2025109807A (ja) | 2013-04-10 | 2025-05-09 | Ｍｅｔａｐ２阻害剤及び肥満症の治療方法 |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018192578A Pending JP2019023219A (ja) | 2013-04-10 | 2018-10-11 | Ｍｅｔａｐ２阻害剤及び肥満症の治療方法 |
| JP2021043481A Pending JP2021091738A (ja) | 2013-04-10 | 2021-03-17 | Ｍｅｔａｐ２阻害剤及び肥満症の治療方法 |
| JP2023061783A Active JP7681054B2 (ja) | 2013-04-10 | 2023-04-05 | Ｍｅｔａｐ２阻害剤及び肥満症の治療方法 |
| JP2025078682A Pending JP2025109807A (ja) | 2013-04-10 | 2025-05-09 | Ｍｅｔａｐ２阻害剤及び肥満症の治療方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (8) | US9173956B2 (enExample) |
| EP (2) | EP2984085B1 (enExample) |
| JP (5) | JP6420314B2 (enExample) |
| CN (2) | CN112494476A (enExample) |
| AU (1) | AU2014250983B2 (enExample) |
| BR (1) | BR112015025892A2 (enExample) |
| CA (1) | CA2908993C (enExample) |
| DK (2) | DK3574922T3 (enExample) |
| EA (1) | EA033912B1 (enExample) |
| ES (2) | ES2749746T3 (enExample) |
| MX (2) | MX371095B (enExample) |
| WO (1) | WO2014169026A1 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9895449B2 (en) | 2010-05-25 | 2018-02-20 | Syndevrx, Inc. | Polymer-conjugated MetAP2 inhibitors, and therapeutic methods of use thereof |
| EP2576638B1 (en) | 2010-05-25 | 2020-12-23 | Syndevrx, Inc. | Polymer-conjugated metap2 inhibitors, and therapeutic methods of use thereof |
| BR112015025892A2 (pt) * | 2013-04-10 | 2017-07-25 | Syndevrx Inc | inibidores de metap2 e métodos para tratar obesidade |
| CN106432255A (zh) * | 2015-08-11 | 2017-02-22 | 扎夫根公司 | 烟曲霉素醇螺环化合物和制备和使用其的方法 |
| DK3386956T3 (da) | 2015-12-10 | 2021-10-11 | Syndevrx Inc | Fumagillolderivater og polymorfer deraf |
| CA3239447A1 (en) * | 2016-01-11 | 2017-07-20 | Syndevrx, Inc. | Treatment for tumors driven by metabolic dysfunction |
| CA3117666A1 (en) | 2018-10-26 | 2020-04-30 | Syndevrx, Inc. | Biomarkers of metap2 inhibitors and applications thereof |
| CN114656372B (zh) * | 2020-09-14 | 2024-06-18 | 广州药本君安医药科技股份有限公司 | 对苯二胺桥连化合物及其在制备治疗糖代谢紊乱疾病的药物中的应用 |
| IL314677A (en) * | 2022-02-16 | 2024-10-01 | Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd | Metap2 inhibitors and uses thereof |
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| US2803586A (en) | 1953-06-29 | 1957-08-20 | Abbott Lab | ph control in production of fumagillin |
| GB8500209D0 (en) * | 1985-01-04 | 1985-02-13 | Ceskoslovenska Akademie Ved | Synthetic polymeric drugs |
| SE8702550D0 (sv) * | 1987-06-18 | 1987-06-18 | Anders Grubb | Cysteinproteashemmare |
| US5166172A (en) | 1988-09-01 | 1992-11-24 | Takeda Chemical Industries, Ltd. | Fumagillol derivatives and pharmaceutical compositions thereof |
| US4997878A (en) | 1988-12-29 | 1991-03-05 | Exxon Research And Engineering Company | Hydrophobically associating polymers containing dimethyl acrylamide functionality |
| US5258453A (en) | 1992-01-21 | 1993-11-02 | University Of Utah | Drug delivery system for the simultaneous delivery of drugs activatable by enzymes and light |
| GB9320781D0 (en) * | 1993-10-08 | 1993-12-01 | Erba Carlo Spa | Polymer-bound camptothecin derivatives |
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