JP2004507465A5 - - Google Patents

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Publication number: JP2004507465A5
Authority: JP; Japan
Prior art keywords: rapamycin; carbon atoms; hydroxy; pharmaceutically acceptable; product
Prior art date: 2001-08-06
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 Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Withdrawn

Application number

JP2002518948A

Other languages

English (en)

Japanese (ja)

Other versions

JP2004507465A (ja

Filing date

2001-08-06

Publication date

2008-09-25

2001-08-06 Application filed filed Critical

2001-08-06 Priority claimed from PCT/US2001/024615 external-priority patent/WO2002013802A2/en

2004-03-11 Publication of JP2004507465A publication Critical patent/JP2004507465A/ja

2008-09-25 Publication of JP2004507465A5 publication Critical patent/JP2004507465A5/ja

Status Withdrawn legal-status Critical Current

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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

JP2002518948A 2000-08-11 2001-08-06 エストロゲン受容体陽性癌腫の治療方法 Withdrawn JP2004507465A (ja)

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 (2)	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 (2)
EP (1)	EP1318837B1 (2)
JP (1)	JP2004507465A (2)
CN (1)	CN100448487C (2)
AR (1)	AR033555A1 (2)
AT (1)	ATE278421T1 (2)
AU (1)	AU2001283139A1 (2)
CA (1)	CA2416976C (2)
DE (1)	DE60106281T2 (2)
DK (1)	DK1318837T3 (2)
ES (1)	ES2228932T3 (2)
MX (1)	MXPA03001245A (2)
PT (1)	PT1318837E (2)
WO (1)	WO2002013802A2 (2)

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