JP2004531562A5 - - Google Patents
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- Publication number
- JP2004531562A5 JP2004531562A5 JP2002591461A JP2002591461A JP2004531562A5 JP 2004531562 A5 JP2004531562 A5 JP 2004531562A5 JP 2002591461 A JP2002591461 A JP 2002591461A JP 2002591461 A JP2002591461 A JP 2002591461A JP 2004531562 A5 JP2004531562 A5 JP 2004531562A5
- Authority
- JP
- Japan
- Prior art keywords
- ethoxy
- piperidin
- phenyl
- pharmaceutically acceptable
- acceptable salt
- 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- Withdrawn
Links
- 150000001875 compounds Chemical class 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 9
- -1 methyl-1-pyrrolidinyl Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 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 claims 3
- 125000006528 (C2-C6) alkyl group Chemical group 0.000 claims 2
- IQBSKHUUKFFBOG-UHFFFAOYSA-N 2-(4-hydroxyphenyl)-1-[[4-(2-piperidin-1-ylethoxy)phenyl]methyl]-3,4-dihydro-2h-quinolin-6-ol Chemical compound C1=CC(O)=CC=C1C1N(CC=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2CC1 IQBSKHUUKFFBOG-UHFFFAOYSA-N 0.000 claims 2
- SBYKRIWWAKRTSL-UHFFFAOYSA-N 6-methoxy-2-phenyl-1-[[4-(2-piperidin-1-ylethoxy)phenyl]methyl]-3,4-dihydro-2h-quinoline Chemical compound C=1C=CC=CC=1C1CCC2=CC(OC)=CC=C2N1CC(C=C1)=CC=C1OCCN1CCCCC1 SBYKRIWWAKRTSL-UHFFFAOYSA-N 0.000 claims 2
- 229940011871 estrogen Drugs 0.000 claims 2
- 239000000262 estrogen Substances 0.000 claims 2
- WSFSSNUMVMOOMR-BJUDXGSMSA-N methanone Chemical compound O=[11CH2] WSFSSNUMVMOOMR-BJUDXGSMSA-N 0.000 claims 2
- XSXHWVKGUXMUQE-UHFFFAOYSA-N osmium dioxide Inorganic materials O=[Os]=O XSXHWVKGUXMUQE-UHFFFAOYSA-N 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 230000001629 suppression Effects 0.000 claims 2
- DMRMYRIKDDOVCY-UHFFFAOYSA-N (6-hydroxy-2-phenyl-3,4-dihydro-2h-quinolin-1-yl)-[4-(2-piperidin-1-ylethoxy)phenyl]methanone Chemical compound C1CC2=CC(O)=CC=C2N(C(=O)C=2C=CC(OCCN3CCCCC3)=CC=2)C1C1=CC=CC=C1 DMRMYRIKDDOVCY-UHFFFAOYSA-N 0.000 claims 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- VPHDBSKPCLXHJV-UHFFFAOYSA-N 2-(3-hydroxyphenyl)-1-[[4-(2-piperidin-1-ylethoxy)phenyl]methyl]-3,4-dihydro-2h-quinolin-6-ol Chemical compound OC1=CC=CC(C2N(C3=CC=C(O)C=C3CC2)CC=2C=CC(OCCN3CCCCC3)=CC=2)=C1 VPHDBSKPCLXHJV-UHFFFAOYSA-N 0.000 claims 1
- OQJYJENHHOZHPV-UHFFFAOYSA-N 2-phenyl-1-[[4-(2-piperidin-1-ylethoxy)phenyl]methyl]-3,4-dihydro-2h-quinolin-6-ol Chemical compound C=1C=CC=CC=1C1CCC2=CC(O)=CC=C2N1CC(C=C1)=CC=C1OCCN1CCCCC1 OQJYJENHHOZHPV-UHFFFAOYSA-N 0.000 claims 1
- 125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- QVZRHXCUIQTJGV-UHFFFAOYSA-N 6-methoxy-2-(3-methoxyphenyl)-1-[[4-(2-piperidin-1-ylethoxy)phenyl]methyl]-3,4-dihydro-2h-quinoline Chemical compound COC1=CC=CC(C2N(C3=CC=C(OC)C=C3CC2)CC=2C=CC(OCCN3CCCCC3)=CC=2)=C1 QVZRHXCUIQTJGV-UHFFFAOYSA-N 0.000 claims 1
- YXEHOUBMVAITRA-UHFFFAOYSA-N 6-methoxy-2-(4-methoxyphenyl)-1-[[4-(2-pyrrolidin-1-ylethoxy)phenyl]methyl]-3,4-dihydro-2h-quinoline Chemical compound C1=CC(OC)=CC=C1C1N(CC=2C=CC(OCCN3CCCC3)=CC=2)C2=CC=C(OC)C=C2CC1 YXEHOUBMVAITRA-UHFFFAOYSA-N 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010030247 Oestrogen deficiency Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 206010067269 Uterine fibrosis Diseases 0.000 claims 1
- JUIRREDKTHAKLI-UHFFFAOYSA-N [6-methoxy-2-(4-methoxyphenyl)-3,4-dihydro-2h-quinolin-1-yl]-[4-(2-piperidin-1-ylethoxy)phenyl]methanone Chemical compound C1=CC(OC)=CC=C1C1N(C(=O)C=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(OC)C=C2CC1 JUIRREDKTHAKLI-UHFFFAOYSA-N 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 230000006461 physiological response Effects 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US29270401P | 2001-05-22 | 2001-05-22 | |
| PCT/US2002/011878 WO2002094788A1 (en) | 2001-05-22 | 2002-05-09 | 2-substituted 1,2,3,4-tetrahydroquinolines and derivatives thereof, compositions and methods |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004531562A JP2004531562A (ja) | 2004-10-14 |
| JP2004531562A5 true JP2004531562A5 (enExample) | 2005-12-22 |
Family
ID=23125830
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002591461A Withdrawn JP2004531562A (ja) | 2001-05-22 | 2002-05-09 | ２−置換１，２，３，４−テトラヒドロキノリンおよびその誘導体、組成物ならびに方法 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US7056931B2 (enExample) |
| EP (1) | EP1395563B1 (enExample) |
| JP (1) | JP2004531562A (enExample) |
| AT (1) | ATE321754T1 (enExample) |
| DE (1) | DE60210283T2 (enExample) |
| ES (1) | ES2259376T3 (enExample) |
| WO (1) | WO2002094788A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0224557D0 (en) * | 2002-10-22 | 2002-11-27 | Glaxo Group Ltd | Novel compounds |
| CL2004000985A1 (es) | 2003-05-16 | 2005-01-14 | Wyeth Corp | Compuestos derivados de fenilquinolinas; composicion farmaceutica, proceso de preparacion; y uso para tratar osteoporosis, enfermedad de paget, dano vascular, osteoartritis, cancer oseo, cancer ovarico, cancer prostatico, hipercolesterolemia, aterosc |
| JP2007523952A (ja) | 2004-02-25 | 2007-08-23 | スミスクライン ビーチャム コーポレーション | 選択的エストロゲンレセプターモジュレーターとして使用するための置換キノリン化合物 |
| EP1778656A1 (en) * | 2004-08-17 | 2007-05-02 | Janssen Pharmaceutica N.V. | Benzoxazepine derivatives as selective estrogen receptor modulators |
| DE102005027168A1 (de) * | 2005-06-13 | 2006-12-14 | Merck Patent Gmbh | Tetrahydrochinoline |
| MX2021000377A (es) * | 2018-07-12 | 2021-03-25 | Lilly Co Eli | Degradadores selectivos del receptor de estrogeno. |
| TWI702219B (zh) * | 2018-07-12 | 2020-08-21 | 美商美國禮來大藥廠 | 選擇性雌激素受體降解劑 |
Family Cites Families (68)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3819637A (en) * | 1971-06-23 | 1974-06-25 | Sterling Drug Inc | 1,2-diphenyl-1,2,3,4-tetrahydroquinolines |
| US3994902A (en) * | 1971-06-23 | 1976-11-30 | Sterling Drug Inc. | Certain 1,2-diphenyl-1,2,3,4-tetrahydroquinoline compounds |
| US4133814A (en) * | 1975-10-28 | 1979-01-09 | Eli Lilly And Company | 2-Phenyl-3-aroylbenzothiophenes useful as antifertility agents |
| US4230862A (en) * | 1975-10-28 | 1980-10-28 | Eli Lilly And Company | Antifertility compounds |
| AU509682B2 (en) * | 1975-10-28 | 1980-05-22 | Eli Lilly And Company | 2-Aroyl-3-Phenylbenzothiophene Derivatives |
| US4418068A (en) * | 1981-04-03 | 1983-11-29 | Eli Lilly And Company | Antiestrogenic and antiandrugenic benzothiophenes |
| JPS59124889A (ja) * | 1982-12-30 | 1984-07-19 | インタ−ナショナル ビジネス マシ−ンズ コ−ポレ−ション | 放電記録材 |
| US5395842A (en) * | 1988-10-31 | 1995-03-07 | Endorecherche Inc. | Anti-estrogenic compounds and compositions |
| US5686465A (en) * | 1988-10-31 | 1997-11-11 | Endorecherche Inc. | Sex steroid activity inhibitors |
| JPH04316557A (ja) | 1991-04-16 | 1992-11-06 | Kyorin Pharmaceut Co Ltd | ６−アリール環状アントラニル酸誘導体 |
| TW366342B (en) * | 1992-07-28 | 1999-08-11 | Lilly Co Eli | The use of 2-phenyl-3-aroylbenzothiophenes in inhibiting bone loss |
| US5403847A (en) * | 1992-11-13 | 1995-04-04 | Synaptic Pharmaceutical Corporation | Use of α1C specific compounds to treat benign prostatic hyperlasia |
| US5508306A (en) * | 1992-11-13 | 1996-04-16 | Synaptic Pharmaceutical Corporation | Aromatic amine derivatives |
| US5482949A (en) * | 1993-03-19 | 1996-01-09 | Eli Lilly And Company | Sulfonate derivatives of 3-aroylbenzo[b]thiophenes |
| US6756388B1 (en) | 1993-10-12 | 2004-06-29 | Pfizer Inc. | Benzothiophenes and related compounds as estrogen agonists |
| US5461065A (en) * | 1993-10-15 | 1995-10-24 | Eli Lilly And Company | Methods for inhibiting endometriosis |
| US5457116A (en) * | 1993-10-15 | 1995-10-10 | Eli Lilly And Company | Methods of inhibiting uterine fibrosis |
| JPH09506898A (ja) | 1993-12-21 | 1997-07-08 | イーライ・リリー・アンド・カンパニー | 非ペプチドタキキニン受容体アンタゴニスト |
| US5446053A (en) * | 1993-12-21 | 1995-08-29 | Eli Lilly And Company | Methods of inhibiting dysfunctional uterine bleeding |
| US5484798A (en) | 1994-09-20 | 1996-01-16 | Eli Lilly And Company | Benzothiopene compounds, compositions, and method of inhibiting restenosis |
| US7501441B1 (en) | 1994-09-20 | 2009-03-10 | Eli Lilly And Company | Naphthyl compounds, intermediates, processes, compositions, and methods |
| US6479517B1 (en) | 1995-02-28 | 2002-11-12 | Eli Lilly And Company | Phosphorous-containing benzothiophenes |
| US5510357A (en) * | 1995-02-28 | 1996-04-23 | Eli Lilly And Company | Benzothiophene compounds as anti-estrogenic agents |
| US5998401A (en) | 1995-02-28 | 1999-12-07 | Eli Lilly And Company | Naphthyl compounds, intermediates, compositions, and methods |
| US5523309A (en) * | 1995-03-10 | 1996-06-04 | Eli Lilly And Company | Benzofuran pharmaceutical compounds |
| US6384053B1 (en) | 1995-03-10 | 2002-05-07 | Eli Lilly And Company | α-substituted-1-benzyl-napthyls |
| US6395755B1 (en) | 1995-03-10 | 2002-05-28 | Eli Lilly And Company | Benzothiophene pharmaceutical compounds |
| US6391892B1 (en) | 1995-03-10 | 2002-05-21 | Eli Lilly And Company | Naphthyl pharmaceutical compounds |
| US6417199B1 (en) | 1995-03-10 | 2002-07-09 | Eli Lilly And Company | 3-benzyl-benzothiophenes |
| US6608090B1 (en) | 1995-04-21 | 2003-08-19 | Eli Lilly And Company | Benzothiophenes with novel basic side chains |
| CA2215902A1 (en) | 1995-04-21 | 1996-10-24 | Charles David Jones | Benzothiophenes with novel basic side chains |
| US6444688B1 (en) | 1995-06-07 | 2002-09-03 | Eli Lilly And Company | Compounds and compositions with nitrogen-containing non-basic side chains |
| DE69600709T2 (de) | 1995-06-07 | 1999-03-18 | Eli Lilly And Co., Indianapolis, Ind. | Verbindungen mit N-Acyliertem Piperidin in der Seitenkette und Zusammensetzungen |
| US5567828A (en) | 1995-06-07 | 1996-10-22 | Eli Lilly And Company | Compounds and compositions with nitrogen-containing non-basic side |
| DK0842169T3 (da) | 1995-06-26 | 2001-01-29 | Lilly Co Eli | Benzothiophenforbindelser |
| US5811421A (en) * | 1995-07-31 | 1998-09-22 | Eli Lilly And Company | Naphthyl and dihydronaphthyl intermediates, compounds, compositions, and methods |
| US5728724A (en) * | 1995-08-17 | 1998-03-17 | Eli Lilly And Company | Benzothiophene compounds |
| US5726168A (en) * | 1995-10-12 | 1998-03-10 | Eli Lilly And Company | Lipophilic benzothiophenes |
| ES2233982T3 (es) | 1995-10-31 | 2005-06-16 | Eli Lilly And Company | Diaminas antitromboticas. |
| WO1997017069A1 (en) | 1995-11-07 | 1997-05-15 | Eli Lilly And Company | Methods for treating resistant tumors |
| US6432982B1 (en) | 1996-02-21 | 2002-08-13 | Eli Lilly And Company | Benzothiophenes, and formulations and methods using same |
| US5688796A (en) | 1996-03-12 | 1997-11-18 | Eli Lilly And Company | Heterocyclic substituted benzothiophenes, compositions, and methods |
| TW397821B (en) | 1996-04-19 | 2000-07-11 | American Home Produits Corp | 3-[4-(2-phenyl-indole-1-ylmethyl)-phenyl]-acrylamides and 2-phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol as well as pharmaceutical compositions of estrogenic agents thereof |
| EP0802183B1 (en) | 1996-04-19 | 2001-10-10 | American Home Products Corporation | Estrogenic agents |
| CA2206752A1 (en) | 1996-07-02 | 1998-01-02 | George Joseph Cullinan | Benzothiophene compounds, intermediates, processes, and methods of use |
| CA2207141A1 (en) * | 1996-07-15 | 1998-01-15 | David Thompson Berg | Benzothiophene compounds, and uses and formulations thereof |
| US6599920B2 (en) | 1996-08-29 | 2003-07-29 | Eli Lilly And Company | Naphthalene compounds, intermediates, formulations, and methods |
| CA2214070C (en) * | 1996-08-29 | 2006-03-14 | Eli Lilly And Company | Dihydronaphthalene and naphthalene compounds, intermediates, formulations, and methods |
| ID19392A (id) | 1996-08-29 | 1998-07-09 | Lilly Co Eli | Senyawa naftil dan bahan pertengahan serta komposisi dan metode penggunaan |
| CA2213810C (en) | 1996-08-29 | 2006-06-06 | Lewis Dale Pennington | Benzo¬b|thiophene compounds, intermediates, processes, compositions and methods |
| CA2214072C (en) * | 1996-08-29 | 2006-11-14 | Eli Lilly And Company | Benzo [b] thiophene compounds, intermediates, processes, compositions, and methods |
| CA2214919A1 (en) * | 1996-09-24 | 1998-03-24 | Kenneth Lee Hauser | Benzothiophene compounds, intermediates, processes, compositions, and methods |
| CA2214922A1 (en) | 1996-09-27 | 1998-03-27 | Eli Lilly And Company | Benzothiophene compounds, compositions, and methods |
| US5948796A (en) * | 1996-10-10 | 1999-09-07 | Eli Lilly And Company | Benzo B!thiophene compounds, intermediates, formulations, and methods |
| US5958969A (en) * | 1996-10-10 | 1999-09-28 | Eli Lilly And Company | Benzo b!thiophene compounds, intermediates, formulations, and methods |
| US5916916A (en) | 1996-10-10 | 1999-06-29 | Eli Lilly And Company | 1-aryloxy-2-arylnaphthyl compounds, intermediates, compositions, and methods |
| CA2216592C (en) | 1996-10-24 | 2006-07-18 | Brian Stephen Muehl | Benzothiophene compounds, intermediates, compositions, and methods |
| CA2218756A1 (en) | 1996-10-25 | 1998-04-25 | Kristin Sue Marron | Substituted benzo¢b!thiophene compounds having activity as selective estrogen receptor modulators |
| IL122026A0 (en) | 1996-10-30 | 1998-03-10 | Lilly Co Eli | Improvements in or relating to the prophylaxis of breast cancer |
| CA2287922A1 (en) | 1997-04-30 | 1998-11-05 | Eli Lilly And Company | Intermediates and processes for preparing benzo[b]thiophenes |
| JP2001513501A (ja) | 1997-08-07 | 2001-09-04 | イーライ・リリー・アンド・カンパニー | エストロゲン阻害活性を有する１−［４−（置換アルコキシ）ベンジル］ナフタレン化合物 |
| US6090843A (en) | 1997-08-11 | 2000-07-18 | Eli Lilly And Company | Benzothiophenes compounds which have useful pharmaceutical activity |
| US6017914A (en) | 1997-09-03 | 2000-01-25 | Eli Lilly And Company | Benzo[b]thiophene compounds, intermediates, formulations, and methods |
| US5929090A (en) * | 1997-09-12 | 1999-07-27 | Eli Lilly And Company | 2-aryl-3-aminoaryloxynaphthy1 compounds, intermediates, compositions and methods |
| WO1999019293A1 (en) | 1997-10-15 | 1999-04-22 | American Home Products Corporation | Novel aryloxy-alkyl-dialkylamines |
| CN1309637A (zh) | 1998-05-15 | 2001-08-22 | 美国家用产品公司 | 包含2－苯基－吲哚化合物和雌激素制剂的组合物 |
| US6060488A (en) | 1998-09-22 | 2000-05-09 | Eli Lilly And Company | Benzothiophenes for treating estrogen deficiency |
| EP1113007A1 (en) | 1999-12-24 | 2001-07-04 | Pfizer Inc. | Tetrahydroisoquinoline compounds as estrogen agonists/antagonists |
-
2002
- 2002-05-09 DE DE60210283T patent/DE60210283T2/de not_active Expired - Fee Related
- 2002-05-09 JP JP2002591461A patent/JP2004531562A/ja not_active Withdrawn
- 2002-05-09 AT AT02746308T patent/ATE321754T1/de not_active IP Right Cessation
- 2002-05-09 US US10/475,593 patent/US7056931B2/en not_active Expired - Fee Related
- 2002-05-09 EP EP02746308A patent/EP1395563B1/en not_active Expired - Lifetime
- 2002-05-09 ES ES02746308T patent/ES2259376T3/es not_active Expired - Lifetime
- 2002-05-09 WO PCT/US2002/011878 patent/WO2002094788A1/en not_active Ceased
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