DE69724733T2 - Substituierte Benzo(b)thiophene als selektive Östrogenrezeptormodulatoren - Google Patents
Substituierte Benzo(b)thiophene als selektive Östrogenrezeptormodulatoren Download PDFInfo
- Publication number
- DE69724733T2 DE69724733T2 DE69724733T DE69724733T DE69724733T2 DE 69724733 T2 DE69724733 T2 DE 69724733T2 DE 69724733 T DE69724733 T DE 69724733T DE 69724733 T DE69724733 T DE 69724733T DE 69724733 T2 DE69724733 T2 DE 69724733T2
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- Germany
- Prior art keywords
- compound according
- estrogen
- compounds
- pharmaceutically acceptable
- benzo
- Prior art date
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- FCEHBMOGCRZNNI-UHFFFAOYSA-N 1-benzothiophene Chemical class C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 title description 9
- 239000000333 selective estrogen receptor modulator Substances 0.000 title 1
- 229940095743 selective estrogen receptor modulator Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract description 98
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- 239000000262 estrogen Substances 0.000 claims abstract description 51
- 239000000583 progesterone congener Substances 0.000 claims abstract description 17
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical class C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 claims abstract description 15
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- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims abstract description 12
- 230000001419 dependent effect Effects 0.000 claims abstract description 11
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract description 10
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- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims abstract description 7
- 206010006187 Breast cancer Diseases 0.000 claims abstract description 7
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- 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 abstract description 7
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- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims abstract description 4
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- LQJUOZMHRXPLSM-UHFFFAOYSA-N (4-fluorophenyl)-[6-methoxy-2-(4-methoxyphenyl)-1-benzothiophen-3-yl]methanone Chemical compound C1=CC(OC)=CC=C1C1=C(C(=O)C=2C=CC(F)=CC=2)C2=CC=C(OC)C=C2S1 LQJUOZMHRXPLSM-UHFFFAOYSA-N 0.000 claims description 3
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- PWPXWKFGWFGAHG-UHFFFAOYSA-N (4-bromophenyl)-[6-methoxy-2-(4-methoxyphenyl)-1-benzothiophen-3-yl]methanone Chemical compound C1=CC(OC)=CC=C1C1=C(C(=O)C=2C=CC(Br)=CC=2)C2=CC=C(OC)C=C2S1 PWPXWKFGWFGAHG-UHFFFAOYSA-N 0.000 claims description 2
- 125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims description 2
- VSDZYLMQAJEJJU-UHFFFAOYSA-N [6-methoxy-2-(4-methoxyphenyl)-1-benzothiophen-3-yl]-(4-nitrophenyl)methanone Chemical compound C1=CC(OC)=CC=C1C1=C(C(=O)C=2C=CC(=CC=2)[N+]([O-])=O)C2=CC=C(OC)C=C2S1 VSDZYLMQAJEJJU-UHFFFAOYSA-N 0.000 claims description 2
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
- C07D333/56—Radicals substituted by oxygen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/02—Nutrients, e.g. vitamins, minerals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Nutrition Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US2905696P | 1996-10-25 | 1996-10-25 | |
| US29056P | 1996-10-25 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE69724733D1 DE69724733D1 (de) | 2003-10-16 |
| DE69724733T2 true DE69724733T2 (de) | 2004-07-08 |
Family
ID=21846972
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE69724733T Expired - Fee Related DE69724733T2 (de) | 1996-10-25 | 1997-10-22 | Substituierte Benzo(b)thiophene als selektive Östrogenrezeptormodulatoren |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US5962475A (OSRAM) |
| EP (1) | EP0838464B1 (OSRAM) |
| JP (1) | JPH10204082A (OSRAM) |
| AT (1) | ATE249454T1 (OSRAM) |
| CA (1) | CA2218756A1 (OSRAM) |
| DE (1) | DE69724733T2 (OSRAM) |
| ES (1) | ES2206664T3 (OSRAM) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2236007A1 (en) | 1995-10-31 | 1997-07-17 | Gerald Floyd Smith | Antithrombotic diamines |
| WO2001026651A2 (en) * | 1999-10-14 | 2001-04-19 | Endorecherche, Inc. | Selective estrogen receptor modulators in the treatment or reduction of the risk of acquiring hypertension, cardiovascular diseases, and insulin resistance |
| AU7993500A (en) * | 1999-11-15 | 2001-05-30 | New Millennium Pharmaceutical Research, Inc. | Intranasal administration of raloxifene and tamoxifen |
| US6471979B2 (en) | 1999-12-29 | 2002-10-29 | Estrogen Vascular Technology, Llc | Apparatus and method for delivering compounds to a living organism |
| WO2001047451A1 (en) * | 1999-12-29 | 2001-07-05 | Gishel New | Apparatus and method for delivering compounds to a living organism |
| AU2002235348A1 (en) * | 2001-01-17 | 2002-07-30 | Praecis Pharmaceuticals Inc. | Methods for treating hormone associated conditions using a combination of lhrh antagonists and specific estrogen receptor modulators |
| PL366453A1 (en) * | 2001-05-01 | 2005-02-07 | Pfizer Products Inc. | Method for manufacturing a low dose pharmaceutical composition having uniform drug distribution and potency |
| PT1401446E (pt) * | 2001-05-22 | 2005-05-31 | Lilly Co Eli | Derivados de tetrahidroquinolina para a inibicao de doencas associadas com a privacao de estrogenio ou com uma resposta fisiologica aberrante ao estrogenio endogeno |
| WO2002094788A1 (en) | 2001-05-22 | 2002-11-28 | Eli Lilly And Company | 2-substituted 1,2,3,4-tetrahydroquinolines and derivatives thereof, compositions and methods |
| HUP0401268A2 (hu) | 2001-07-31 | 2004-11-29 | Pfizer Products Inc. | Ösztrogén agonisták/antagonisták, ösztrogének és progesztinek kombinációját tartalmazó gyógyszerkészítmények, valamint eljárás ezek előállítására |
| BR0312675A (pt) | 2002-07-22 | 2005-05-03 | Lilly Co Eli | Composto ou um sal de adição de ácido farmacêutico do mesmo,m e, métodos para tratar endometriose, e para tratar leiomioma uterino |
| EP3608317A1 (en) * | 2012-01-12 | 2020-02-12 | Yale University | Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase |
| ES2774935T3 (es) | 2012-10-24 | 2020-07-23 | Univ Illinois | Composiciones y métodos para tratar trastornos médicos relacionados con estrógeno |
| WO2014066695A1 (en) | 2012-10-24 | 2014-05-01 | The Board Of Trustees Of The University Of Illinois | Compositions and methods for treating estrogen-related medical disorders |
| JP6644268B2 (ja) * | 2018-03-22 | 2020-02-12 | 横浜ゴム株式会社 | タイヤ用ゴム組成物及びスタッドレスタイヤ |
| JP7085056B2 (ja) * | 2018-07-12 | 2022-06-15 | イーライ リリー アンド カンパニー | 選択的エストロゲン受容体分解剤 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PH18628A (en) * | 1981-04-03 | 1985-08-23 | Lilly Co Eli | "6-hydroxy-2-(4-hydroxyphenyl)-3 4-(2- piperidine or 3-methylpyrollidine -benzo b thiophene compounds |
| JP3157882B2 (ja) * | 1991-11-15 | 2001-04-16 | 帝国臓器製薬株式会社 | 新規なベンゾチオフエン誘導体 |
| TW366342B (en) * | 1992-07-28 | 1999-08-11 | Lilly Co Eli | The use of 2-phenyl-3-aroylbenzothiophenes in inhibiting bone loss |
| 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 |
| US5484798A (en) * | 1994-09-20 | 1996-01-16 | Eli Lilly And Company | Benzothiopene compounds, compositions, and method of inhibiting restenosis |
| US6703407B1 (en) * | 1994-09-20 | 2004-03-09 | Eli Lilly And Company | Benzofuran compounds, compositions, and methods |
| US5589482A (en) * | 1994-12-14 | 1996-12-31 | Pfizer Inc. | Benzo-thiophene estrogen agonists to treat prostatic hyperplasia |
| US5552401A (en) * | 1995-02-28 | 1996-09-03 | Eli Lilly And Company | 2-benzyl-3-arylbenzothiophenes |
| US5705507A (en) * | 1995-03-10 | 1998-01-06 | Eli Lilly And Company | Aplha-substituted-3-benzyl-benzofurans |
| WO1996032937A1 (en) * | 1995-04-21 | 1996-10-24 | Eli Lilly And Company | Benzothiophenes with novel basic side chains |
-
1997
- 1997-10-20 CA CA002218756A patent/CA2218756A1/en not_active Abandoned
- 1997-10-20 JP JP9325116A patent/JPH10204082A/ja not_active Withdrawn
- 1997-10-22 DE DE69724733T patent/DE69724733T2/de not_active Expired - Fee Related
- 1997-10-22 AT AT97308412T patent/ATE249454T1/de not_active IP Right Cessation
- 1997-10-22 EP EP97308412A patent/EP0838464B1/en not_active Expired - Lifetime
- 1997-10-22 ES ES97308412T patent/ES2206664T3/es not_active Expired - Lifetime
- 1997-10-23 US US08/956,802 patent/US5962475A/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| ATE249454T1 (de) | 2003-09-15 |
| JPH10204082A (ja) | 1998-08-04 |
| DE69724733D1 (de) | 2003-10-16 |
| ES2206664T3 (es) | 2004-05-16 |
| CA2218756A1 (en) | 1998-04-25 |
| US5962475A (en) | 1999-10-05 |
| EP0838464B1 (en) | 2003-09-10 |
| EP0838464A1 (en) | 1998-04-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 8364 | No opposition during term of opposition | ||
| 8339 | Ceased/non-payment of the annual fee |