JP2004507465A5 - - Google Patents
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- JP2004507465A5 JP2004507465A5 JP2002518948A JP2002518948A JP2004507465A5 JP 2004507465 A5 JP2004507465 A5 JP 2004507465A5 JP 2002518948 A JP2002518948 A JP 2002518948A JP 2002518948 A JP2002518948 A JP 2002518948A JP 2004507465 A5 JP2004507465 A5 JP 2004507465A5
- Authority
- JP
- Japan
- Prior art keywords
- rapamycin
- carbon atoms
- hydroxy
- pharmaceutically acceptable
- product
- 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.)
- Withdrawn
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- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 description 29
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 description 29
- 229960002930 sirolimus Drugs 0.000 description 29
- 125000004432 carbon atom Chemical group C* 0.000 description 22
- 238000000034 method Methods 0.000 description 21
- 230000001833 anti-estrogenic effect Effects 0.000 description 19
- 239000000328 estrogen antagonist Substances 0.000 description 19
- 150000003839 salts Chemical class 0.000 description 12
- 239000000126 substance Substances 0.000 description 12
- 229940046836 anti-estrogen Drugs 0.000 description 10
- 241000124008 Mammalia Species 0.000 description 9
- 229910052736 halogen Inorganic materials 0.000 description 8
- 150000002367 halogens Chemical class 0.000 description 8
- PTBDIHRZYDMNKB-UHFFFAOYSA-N 2,2-Bis(hydroxymethyl)propionic acid Chemical compound OCC(C)(CO)C(O)=O PTBDIHRZYDMNKB-UHFFFAOYSA-N 0.000 description 6
- 201000009030 Carcinoma Diseases 0.000 description 6
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 6
- 125000004093 cyano group Chemical group *C#N 0.000 description 6
- 102000015694 estrogen receptors Human genes 0.000 description 6
- 108010038795 estrogen receptors Proteins 0.000 description 6
- 125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 5
- -1 idoxifine Chemical compound 0.000 description 5
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 description 4
- 125000003545 alkoxy group Chemical group 0.000 description 4
- 125000000217 alkyl group Chemical group 0.000 description 4
- 125000004428 fluoroalkoxy group Chemical group 0.000 description 4
- 229920006395 saturated elastomer Polymers 0.000 description 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 4
- 206010006187 Breast cancer Diseases 0.000 description 3
- 208000026310 Breast neoplasm Diseases 0.000 description 3
- 206010033128 Ovarian cancer Diseases 0.000 description 3
- 206010061535 Ovarian neoplasm Diseases 0.000 description 3
- 150000001875 compounds Chemical class 0.000 description 3
- 230000002401 inhibitory effect Effects 0.000 description 3
- 230000001629 suppression Effects 0.000 description 3
- 230000001836 utereotrophic effect Effects 0.000 description 3
- INEHJXCWEVNEDZ-LUDNRVPPSA-N (2s,3s)-2,3-dihydroxybutanedioic acid;(5r,6s)-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol Chemical compound OC(=O)[C@@H](O)[C@H](O)C(O)=O.C1([C@@H]2[C@@H](C3=CC=C(C=C3CC2)O)C=2C=CC(OCCN3CCCC3)=CC=2)=CC=CC=C1 INEHJXCWEVNEDZ-LUDNRVPPSA-N 0.000 description 2
- DODQJNMQWMSYGS-QPLCGJKRSA-N 4-[(z)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-1-phenylbut-1-en-2-yl]phenol Chemical compound C=1C=C(O)C=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 DODQJNMQWMSYGS-QPLCGJKRSA-N 0.000 description 2
- UTYMHSHRSOOSEY-BYYHNAKLSA-N 4-[4-[(e)-2-chloro-1,2-diphenylethenyl]phenoxy]-n,n-diethylbutan-1-amine Chemical compound C1=CC(OCCCCN(CC)CC)=CC=C1C(\C=1C=CC=CC=1)=C(\Cl)C1=CC=CC=C1 UTYMHSHRSOOSEY-BYYHNAKLSA-N 0.000 description 2
- ZQZFYGIXNQKOAV-OCEACIFDSA-N Droloxifene Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=C(O)C=CC=1)\C1=CC=C(OCCN(C)C)C=C1 ZQZFYGIXNQKOAV-OCEACIFDSA-N 0.000 description 2
- VWUXBMIQPBEWFH-WCCTWKNTSA-N Fulvestrant Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3[C@H](CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F)CC2=C1 VWUXBMIQPBEWFH-WCCTWKNTSA-N 0.000 description 2
- AVXURJPOCDRRFD-UHFFFAOYSA-N Hydroxylamine Chemical compound ON AVXURJPOCDRRFD-UHFFFAOYSA-N 0.000 description 2
- JEYWNNAZDLFBFF-UHFFFAOYSA-N Nafoxidine Chemical compound C1CC2=CC(OC)=CC=C2C(C=2C=CC(OCCN3CCCC3)=CC=2)=C1C1=CC=CC=C1 JEYWNNAZDLFBFF-UHFFFAOYSA-N 0.000 description 2
- OEKMGABCSLYWOP-DHUJRADRSA-N [4-[(2s)-7-(2,2-dimethylpropanoyloxy)-4-methyl-2-[4-(2-piperidin-1-ylethoxy)phenyl]-2h-chromen-3-yl]phenyl] 2,2-dimethylpropanoate Chemical compound C1=CC([C@H]2C(=C(C3=CC=C(OC(=O)C(C)(C)C)C=C3O2)C)C=2C=CC(OC(=O)C(C)(C)C)=CC=2)=CC=C1OCCN1CCCCC1 OEKMGABCSLYWOP-DHUJRADRSA-N 0.000 description 2
- 150000003973 alkyl amines Chemical class 0.000 description 2
- MCGDSOGUHLTADD-UHFFFAOYSA-N arzoxifene Chemical compound C1=CC(OC)=CC=C1C1=C(OC=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 MCGDSOGUHLTADD-UHFFFAOYSA-N 0.000 description 2
- UCJGJABZCDBEDK-UHFFFAOYSA-N bazedoxifene Chemical group C=1C=C(OCCN2CCCCCC2)C=CC=1CN1C2=CC=C(O)C=C2C(C)=C1C1=CC=C(O)C=C1 UCJGJABZCDBEDK-UHFFFAOYSA-N 0.000 description 2
- 229960003608 clomifene Drugs 0.000 description 2
- GKIRPKYJQBWNGO-OCEACIFDSA-N clomifene Chemical compound C1=CC(OCCN(CC)CC)=CC=C1C(\C=1C=CC=CC=1)=C(\Cl)C1=CC=CC=C1 GKIRPKYJQBWNGO-OCEACIFDSA-N 0.000 description 2
- 229950004203 droloxifene Drugs 0.000 description 2
- 150000002148 esters Chemical class 0.000 description 2
- 229940011871 estrogen Drugs 0.000 description 2
- 239000000262 estrogen Substances 0.000 description 2
- HKVAMNSJSFKALM-CPXURSODSA-N everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)\C(C)=C\C=C\C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-CPXURSODSA-N 0.000 description 2
- 229960002258 fulvestrant Drugs 0.000 description 2
- 125000005842 heteroatom Chemical group 0.000 description 2
- 125000000623 heterocyclic group Chemical group 0.000 description 2
- 150000007857 hydrazones Chemical class 0.000 description 2
- QZUHFMXJZOUZFI-ZQHSETAFSA-N miproxifene phosphate Chemical compound C=1C=C(C(C)C)C=CC=1C(/CC)=C(C=1C=CC(OP(O)(O)=O)=CC=1)\C1=CC=C(OCCN(C)C)C=C1 QZUHFMXJZOUZFI-ZQHSETAFSA-N 0.000 description 2
- 229950002366 nafoxidine Drugs 0.000 description 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 2
- 150000002923 oximes Chemical class 0.000 description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 2
- 229960004622 raloxifene Drugs 0.000 description 2
- GZUITABIAKMVPG-UHFFFAOYSA-N raloxifene Chemical compound C1=CC(O)=CC=C1C1=C(C(=O)C=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 GZUITABIAKMVPG-UHFFFAOYSA-N 0.000 description 2
- 229960001603 tamoxifen Drugs 0.000 description 2
- 229960005026 toremifene Drugs 0.000 description 2
- XFCLJVABOIYOMF-QPLCGJKRSA-N toremifene Chemical compound C1=CC(OCCN(C)C)=CC=C1C(\C=1C=CC=CC=1)=C(\CCCl)C1=CC=CC=C1 XFCLJVABOIYOMF-QPLCGJKRSA-N 0.000 description 2
- 239000003814 drug Substances 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22432600P | 2000-08-11 | 2000-08-11 | |
| PCT/US2001/024615 WO2002013802A2 (en) | 2000-08-11 | 2001-08-06 | Method of treating estrogen receptor positive carcinoma |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004507465A JP2004507465A (ja) | 2004-03-11 |
| JP2004507465A5 true JP2004507465A5 (enExample) | 2008-09-25 |
Family
ID=22840171
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002518948A Withdrawn JP2004507465A (ja) | 2000-08-11 | 2001-08-06 | エストロゲン受容体陽性癌腫の治療方法 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US6511986B2 (enExample) |
| EP (1) | EP1318837B1 (enExample) |
| JP (1) | JP2004507465A (enExample) |
| CN (1) | CN100448487C (enExample) |
| AR (1) | AR033555A1 (enExample) |
| AT (1) | ATE278421T1 (enExample) |
| AU (1) | AU2001283139A1 (enExample) |
| CA (1) | CA2416976C (enExample) |
| DE (1) | DE60106281T2 (enExample) |
| DK (1) | DK1318837T3 (enExample) |
| ES (1) | ES2228932T3 (enExample) |
| MX (1) | MXPA03001245A (enExample) |
| PT (1) | PT1318837E (enExample) |
| WO (1) | WO2002013802A2 (enExample) |
Families Citing this family (81)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN116490186B (zh) | 2020-08-05 | 2025-10-31 | C4医药公司 | 用于ret的靶向降解的化合物 |
| KR20240018446A (ko) | 2021-06-08 | 2024-02-13 | 씨4 테라퓨틱스, 인코포레이티드 | 돌연변이 braf의 분해를 위한 요법 |
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| CN119998285A (zh) | 2022-08-03 | 2025-05-13 | 百时美施贵宝公司 | 用于调控ret蛋白的化合物 |
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| CN120530116A (zh) | 2022-11-04 | 2025-08-22 | 百时美施贵宝公司 | Ret-ldd蛋白抑制剂 |
| WO2025006753A2 (en) | 2023-06-30 | 2025-01-02 | Merck Patent Gmbh | Heterobifunctional compounds for the degradation of kras protein |
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-
2001
- 2001-08-06 ES ES01961914T patent/ES2228932T3/es not_active Expired - Lifetime
- 2001-08-06 DE DE60106281T patent/DE60106281T2/de not_active Expired - Fee Related
- 2001-08-06 MX MXPA03001245A patent/MXPA03001245A/es active IP Right Grant
- 2001-08-06 EP EP01961914A patent/EP1318837B1/en not_active Expired - Lifetime
- 2001-08-06 AT AT01961914T patent/ATE278421T1/de not_active IP Right Cessation
- 2001-08-06 PT PT01961914T patent/PT1318837E/pt unknown
- 2001-08-06 JP JP2002518948A patent/JP2004507465A/ja not_active Withdrawn
- 2001-08-06 CN CNB018137539A patent/CN100448487C/zh not_active Expired - Fee Related
- 2001-08-06 WO PCT/US2001/024615 patent/WO2002013802A2/en not_active Ceased
- 2001-08-06 CA CA002416976A patent/CA2416976C/en not_active Expired - Fee Related
- 2001-08-06 AU AU2001283139A patent/AU2001283139A1/en not_active Abandoned
- 2001-08-06 DK DK01961914T patent/DK1318837T3/da active
- 2001-08-06 US US09/923,217 patent/US6511986B2/en not_active Expired - Fee Related
- 2001-08-10 AR ARP010103839A patent/AR033555A1/es unknown
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