JP2003519219A5 - - Google Patents
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- JP2003519219A5 JP2003519219A5 JP2001550213A JP2001550213A JP2003519219A5 JP 2003519219 A5 JP2003519219 A5 JP 2003519219A5 JP 2001550213 A JP2001550213 A JP 2001550213A JP 2001550213 A JP2001550213 A JP 2001550213A JP 2003519219 A5 JP2003519219 A5 JP 2003519219A5
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- JP
- Japan
- Prior art keywords
- composition
- compound
- alkyl
- substituted
- compound according
- 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.)
- Pending
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- 239000000203 mixture Substances 0.000 description 28
- 150000001875 compounds Chemical class 0.000 description 27
- 108010041356 Estrogen Receptor beta Proteins 0.000 description 12
- 102100029951 Estrogen receptor beta Human genes 0.000 description 12
- 125000000623 heterocyclic group Chemical group 0.000 description 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 6
- 229910052739 hydrogen Inorganic materials 0.000 description 5
- 239000001257 hydrogen Substances 0.000 description 5
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 5
- 210000001519 tissue Anatomy 0.000 description 5
- 108090000695 Cytokines Proteins 0.000 description 4
- 102000004127 Cytokines Human genes 0.000 description 4
- 206010028980 Neoplasm Diseases 0.000 description 4
- 208000019664 bone resorption disease Diseases 0.000 description 4
- 210000000481 breast Anatomy 0.000 description 4
- 201000011510 cancer Diseases 0.000 description 4
- 210000001035 gastrointestinal tract Anatomy 0.000 description 4
- 229910052736 halogen Inorganic materials 0.000 description 4
- 210000002307 prostate Anatomy 0.000 description 4
- 125000001424 substituent group Chemical group 0.000 description 4
- 108090001005 Interleukin-6 Proteins 0.000 description 3
- 206010003246 arthritis Diseases 0.000 description 3
- 210000000988 bone and bone Anatomy 0.000 description 3
- 210000000918 epididymis Anatomy 0.000 description 3
- 201000010063 epididymitis Diseases 0.000 description 3
- 229940011871 estrogen Drugs 0.000 description 3
- 239000000262 estrogen Substances 0.000 description 3
- 210000001508 eye Anatomy 0.000 description 3
- 150000002367 halogens Chemical class 0.000 description 3
- 210000002216 heart Anatomy 0.000 description 3
- 210000001320 hippocampus Anatomy 0.000 description 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 3
- 210000000987 immune system Anatomy 0.000 description 3
- 210000003734 kidney Anatomy 0.000 description 3
- 210000004072 lung Anatomy 0.000 description 3
- 210000001672 ovary Anatomy 0.000 description 3
- 230000001817 pituitary effect Effects 0.000 description 3
- 210000001550 testis Anatomy 0.000 description 3
- 210000003932 urinary bladder Anatomy 0.000 description 3
- 210000004291 uterus Anatomy 0.000 description 3
- 230000002792 vascular Effects 0.000 description 3
- 201000009273 Endometriosis Diseases 0.000 description 2
- 102100038595 Estrogen receptor Human genes 0.000 description 2
- 101710196141 Estrogen receptor Proteins 0.000 description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 2
- 208000034578 Multiple myelomas Diseases 0.000 description 2
- 208000001132 Osteoporosis Diseases 0.000 description 2
- 206010035226 Plasma cell myeloma Diseases 0.000 description 2
- 206010060862 Prostate cancer Diseases 0.000 description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 2
- 125000003118 aryl group Chemical group 0.000 description 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 2
- 239000003085 diluting agent Substances 0.000 description 2
- 239000003937 drug carrier Substances 0.000 description 2
- 230000014509 gene expression Effects 0.000 description 2
- 125000005843 halogen group Chemical group 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 239000008194 pharmaceutical composition Substances 0.000 description 2
- 150000003839 salts Chemical class 0.000 description 2
- 210000001103 thalamus Anatomy 0.000 description 2
- 125000004768 (C1-C4) alkylsulfinyl group Chemical group 0.000 description 1
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 description 1
- 0 *c(cc1)ccc1C1=C(c(cc2)ccc2OCCN2CCCCC2)c(ccc(O)c2)c2OC1=O Chemical compound *c(cc1)ccc1C1=C(c(cc2)ccc2OCCN2CCCCC2)c(ccc(O)c2)c2OC1=O 0.000 description 1
- 125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 208000002874 Acne Vulgaris Diseases 0.000 description 1
- 201000004384 Alopecia Diseases 0.000 description 1
- 208000024827 Alzheimer disease Diseases 0.000 description 1
- 208000000044 Amnesia Diseases 0.000 description 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 description 1
- 206010005949 Bone cancer Diseases 0.000 description 1
- 206010065687 Bone loss Diseases 0.000 description 1
- 208000018084 Bone neoplasm Diseases 0.000 description 1
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- DDDYIPPWPPAVJL-UHFFFAOYSA-N CCN(CC)CCOc(cc1)ccc1C(c(c(O1)c2)ccc2O)=C(c2ccccc2)C1=O Chemical compound CCN(CC)CCOc(cc1)ccc1C(c(c(O1)c2)ccc2O)=C(c2ccccc2)C1=O DDDYIPPWPPAVJL-UHFFFAOYSA-N 0.000 description 1
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- 208000002177 Cataract Diseases 0.000 description 1
- 206010008342 Cervix carcinoma Diseases 0.000 description 1
- 102000004457 Granulocyte-Macrophage Colony-Stimulating Factor Human genes 0.000 description 1
- 108010017213 Granulocyte-Macrophage Colony-Stimulating Factor Proteins 0.000 description 1
- 206010020112 Hirsutism Diseases 0.000 description 1
- 208000033830 Hot Flashes Diseases 0.000 description 1
- 206010060800 Hot flush Diseases 0.000 description 1
- 208000035150 Hypercholesterolemia Diseases 0.000 description 1
- 201000002980 Hyperparathyroidism Diseases 0.000 description 1
- 206010025323 Lymphomas Diseases 0.000 description 1
- 208000026139 Memory disease Diseases 0.000 description 1
- 206010027951 Mood swings Diseases 0.000 description 1
- 229910003827 NRaRb Inorganic materials 0.000 description 1
- 208000008589 Obesity Diseases 0.000 description 1
- MSAXETIFPYLUAN-UHFFFAOYSA-N Oc(cc1)cc(O2)c1C(c1ccc(COCCN3CCCCC3)cc1)=C(c1ccccc1)C2=O Chemical compound Oc(cc1)cc(O2)c1C(c1ccc(COCCN3CCCCC3)cc1)=C(c1ccccc1)C2=O MSAXETIFPYLUAN-UHFFFAOYSA-N 0.000 description 1
- PIQFHGVAOCMFMW-UHFFFAOYSA-N Oc(cc1O2)ccc1C(c1cc(OCCCN3CCCCC3)ccc1)=C(c(cc1)ccc1Cl)C2=O Chemical compound Oc(cc1O2)ccc1C(c1cc(OCCCN3CCCCC3)ccc1)=C(c(cc1)ccc1Cl)C2=O PIQFHGVAOCMFMW-UHFFFAOYSA-N 0.000 description 1
- 208000010191 Osteitis Deformans Diseases 0.000 description 1
- 208000003076 Osteolysis Diseases 0.000 description 1
- 208000027868 Paget disease Diseases 0.000 description 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 description 1
- 208000006265 Renal cell carcinoma Diseases 0.000 description 1
- 206010046543 Urinary incontinence Diseases 0.000 description 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 description 1
- 208000027418 Wounds and injury Diseases 0.000 description 1
- 206010000496 acne Diseases 0.000 description 1
- 125000003545 alkoxy group Chemical group 0.000 description 1
- 125000003710 aryl alkyl group Chemical group 0.000 description 1
- 125000004429 atom Chemical group 0.000 description 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 1
- 125000001246 bromo group Chemical group Br* 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 201000010881 cervical cancer Diseases 0.000 description 1
- 125000001309 chloro group Chemical group Cl* 0.000 description 1
- 230000002939 deleterious effect Effects 0.000 description 1
- 230000002357 endometrial effect Effects 0.000 description 1
- 239000003256 environmental substance Substances 0.000 description 1
- 125000001153 fluoro group Chemical group F* 0.000 description 1
- 208000024963 hair loss Diseases 0.000 description 1
- 230000003676 hair loss Effects 0.000 description 1
- 125000001072 heteroaryl group Chemical group 0.000 description 1
- 125000005842 heteroatom Chemical group 0.000 description 1
- 125000005343 heterocyclic alkyl group Chemical group 0.000 description 1
- 230000003054 hormonal effect Effects 0.000 description 1
- 230000002267 hypothalamic effect Effects 0.000 description 1
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 description 1
- 125000003037 imidazol-2-yl group Chemical group [H]N1C([*])=NC([H])=C1[H] 0.000 description 1
- -1 imidazolidine-2-yl Chemical group 0.000 description 1
- 239000007943 implant Substances 0.000 description 1
- 208000014674 injury Diseases 0.000 description 1
- 125000002346 iodo group Chemical group I* 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 208000029791 lytic metastatic bone lesion Diseases 0.000 description 1
- 208000027202 mammary Paget disease Diseases 0.000 description 1
- 230000006984 memory degeneration Effects 0.000 description 1
- 208000023060 memory loss Diseases 0.000 description 1
- 230000001394 metastastic effect Effects 0.000 description 1
- 206010061289 metastatic neoplasm Diseases 0.000 description 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 description 1
- 235000020824 obesity Nutrition 0.000 description 1
- 230000000399 orthopedic effect Effects 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 description 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 201000004240 prostatic hypertrophy Diseases 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 230000001850 reproductive effect Effects 0.000 description 1
- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 230000021595 spermatogenesis Effects 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 1
- 230000009441 vascular protection Effects 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US47577699A | 1999-12-30 | 1999-12-30 | |
| US09/475,776 | 1999-12-30 | ||
| US09/492,939 US6291456B1 (en) | 1998-12-30 | 2000-01-27 | Compounds and methods for modulation of estrogen receptors |
| US09/492,939 | 2000-01-27 | ||
| US09/611,156 US6331562B1 (en) | 1998-12-30 | 2000-07-06 | Compounds and methods for modulation of estrogen receptors |
| US09/611,156 | 2000-07-06 | ||
| PCT/US2000/035671 WO2001049673A2 (en) | 1999-12-30 | 2000-12-29 | Compounds and methods for modulation of estrogen receptors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2003519219A JP2003519219A (ja) | 2003-06-17 |
| JP2003519219A5 true JP2003519219A5 (enExample) | 2008-02-07 |
Family
ID=27413348
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001550213A Pending JP2003519219A (ja) | 1999-12-30 | 2000-12-29 | エストロゲン受容体をモジュレートするための化合物および方法 |
Country Status (13)
| Country | Link |
|---|---|
| EP (1) | EP1246814B1 (enExample) |
| JP (1) | JP2003519219A (enExample) |
| KR (1) | KR20020075388A (enExample) |
| CN (1) | CN1281598C (enExample) |
| AT (1) | ATE289300T1 (enExample) |
| AU (1) | AU781282B2 (enExample) |
| CA (1) | CA2396059A1 (enExample) |
| DE (1) | DE60018215T2 (enExample) |
| DK (1) | DK1246814T3 (enExample) |
| ES (1) | ES2238034T3 (enExample) |
| IL (1) | IL150463A0 (enExample) |
| PT (1) | PT1246814E (enExample) |
| WO (1) | WO2001049673A2 (enExample) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CO5271709A1 (es) * | 2000-01-12 | 2003-04-30 | Pfizer Prod Inc | Composiciones y procedimientos para el y tratamiento de afecciones que responden a estrogenos |
| EP1177787A3 (en) * | 2000-07-28 | 2003-09-10 | Pfizer Products Inc. | Use of an estrogen agonist/antagonist for treating cataracts |
| EP1281710A1 (en) * | 2001-08-03 | 2003-02-05 | CHIESI FARMACEUTICI S.p.A. | 2H-1-benzopyran derivatives, processes for their preparation and pharmaceutical compositions thereof |
| US7148252B2 (en) * | 2001-10-03 | 2006-12-12 | Signal Pharmaceuticals, Llc | Use of benzopyranones for treating or preventing a primary brain cancer or a brain metastasis |
| US7217734B2 (en) | 2001-11-19 | 2007-05-15 | Eli Lilly And Company | Substituted benzopyrans as selective estrogen receptor-beta agonists |
| US7524866B2 (en) | 2001-11-29 | 2009-04-28 | Gtx, Inc. | Prevention and treatment of androgen—deprivation induced osteoporosis |
| WO2003047504A2 (en) * | 2001-11-29 | 2003-06-12 | Gtx Inc. | Prevention and treatment of androgen-deprivation induced osteoporosis |
| AU2005202072B2 (en) * | 2001-11-29 | 2008-10-23 | Gtx, Inc. | Prevention and treatment of androgen-deprivation induced conditions |
| AU2003239155B2 (en) * | 2002-04-19 | 2008-12-04 | Novartis Ag | Benzopyranone compounds, compositions thereof, and methods of treatment therewith |
| US7091235B2 (en) | 2002-10-15 | 2006-08-15 | Signal Pharmaceuticals, Llc | Benzopyranone compounds, compositions thereof, and methods for treating or preventing cancer |
| US7674783B2 (en) * | 2002-11-22 | 2010-03-09 | Dimera Inc. | Estrogen beta receptor agonists to prevent or reduce the severity of cardiovascular disease |
| MXPA05011243A (es) | 2003-04-21 | 2005-12-15 | Lilly Co Eli | Benzopiranos substituidos como agonistas selectivos del receptor beta de estrogeno. |
| ES2338119T3 (es) | 2003-04-21 | 2010-05-04 | Eli Lilly And Company | Benzopiranos sustituidos como agonistas selectivos del receptor-beta de estrogeno. |
| US7098340B2 (en) * | 2003-05-14 | 2006-08-29 | Warner Lambert Company Llc | Benzyl sulfonamide derivatives |
| WO2005028472A1 (en) * | 2003-09-15 | 2005-03-31 | Signal Pharmaceuticals, Llc | Benzopyranone compounds, compositions thereof, and methods of treatment therewith |
| CA2595472A1 (en) * | 2005-01-21 | 2006-07-27 | Janssen Pharmaceutica N.V. | Novel coumarin derivatives as ion channel openers |
| WO2008002490A2 (en) * | 2006-06-23 | 2008-01-03 | Radius Health, Inc. | Treatment of vasomotor symptoms with selective estrogen receptor modulators |
| PL2568806T3 (pl) | 2010-05-12 | 2017-03-31 | Radius Health, Inc. | Schematy lecznicze |
| EP2621901B1 (en) | 2010-09-28 | 2015-07-29 | Radius Health, Inc | Selective androgen receptor modulators |
| US9421264B2 (en) | 2014-03-28 | 2016-08-23 | Duke University | Method of treating cancer using selective estrogen receptor modulators |
| SI3122426T1 (sl) | 2014-03-28 | 2023-04-28 | Duke University | Zdravljenje raka dojk z uporabo selektivnih modulatorjev estrogenskih receptorjev |
| CN105801544A (zh) * | 2016-04-18 | 2016-07-27 | 中国药科大学 | 3-芳基-4-芳香胺-香豆素衍生物及其制备方法和医药用途 |
| CN105801543B (zh) * | 2016-04-18 | 2019-08-02 | 中国药科大学 | 4-芳香胺-香豆素衍生物及其制备方法和医药用途 |
| PT3474841T (pt) | 2016-06-22 | 2022-06-20 | Radius Health Inc | Métodos de tratamento do cancro de mama ar+ |
| CN106492204A (zh) * | 2016-12-27 | 2017-03-15 | 郑州郑先医药科技有限公司 | 一种治疗白内障的药物组合物 |
| CN106727637A (zh) * | 2016-12-27 | 2017-05-31 | 郑州郑先医药科技有限公司 | 一种治疗白内障的西药组合物及其用途 |
| EP3565542B1 (en) | 2017-01-05 | 2024-04-10 | Radius Pharmaceuticals, Inc. | Polymorphic forms of rad1901-2hcl |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5883118A (en) * | 1996-01-11 | 1999-03-16 | Nova Nordisk A/S | Prostatic carcinoma |
| US5726202A (en) * | 1996-01-11 | 1998-03-10 | Novo Nordisk A/S | Benign prostatic hypertrophy |
| IL124882A0 (en) * | 1996-01-11 | 1999-01-26 | Novo Nordisk As | Use of 3, 4-diphenyl chromans for the manufacture of a pharmaceutical composition for the treatment or prophylaxis of menopausal symptoms |
| ATE248157T1 (de) * | 1998-12-30 | 2003-09-15 | Signal Pharm Inc | Verbindungen und verfahren zur modulation von estrogen rezeptoren |
-
2000
- 2000-12-29 AU AU30771/01A patent/AU781282B2/en not_active Ceased
- 2000-12-29 ES ES00990966T patent/ES2238034T3/es not_active Expired - Lifetime
- 2000-12-29 CN CNB008192227A patent/CN1281598C/zh not_active Expired - Fee Related
- 2000-12-29 CA CA002396059A patent/CA2396059A1/en not_active Abandoned
- 2000-12-29 IL IL15046300A patent/IL150463A0/xx unknown
- 2000-12-29 DE DE60018215T patent/DE60018215T2/de not_active Expired - Fee Related
- 2000-12-29 WO PCT/US2000/035671 patent/WO2001049673A2/en not_active Ceased
- 2000-12-29 EP EP00990966A patent/EP1246814B1/en not_active Expired - Lifetime
- 2000-12-29 PT PT00990966T patent/PT1246814E/pt unknown
- 2000-12-29 AT AT00990966T patent/ATE289300T1/de not_active IP Right Cessation
- 2000-12-29 JP JP2001550213A patent/JP2003519219A/ja active Pending
- 2000-12-29 DK DK00990966T patent/DK1246814T3/da active
- 2000-12-29 KR KR1020027008569A patent/KR20020075388A/ko not_active Abandoned
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