DE60210283T2 - 2-substituierte 1,2,3,4-tetrahydrochinoline und derivate davon, zusammensetzungen und verfahren - Google Patents
2-substituierte 1,2,3,4-tetrahydrochinoline und derivate davon, zusammensetzungen und verfahren Download PDFInfo
- Publication number
- DE60210283T2 DE60210283T2 DE60210283T DE60210283T DE60210283T2 DE 60210283 T2 DE60210283 T2 DE 60210283T2 DE 60210283 T DE60210283 T DE 60210283T DE 60210283 T DE60210283 T DE 60210283T DE 60210283 T2 DE60210283 T2 DE 60210283T2
- Authority
- DE
- Germany
- Prior art keywords
- piperidin
- estrogen
- pharmaceutically acceptable
- compound according
- 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.)
- Expired - Fee Related
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/38—Nitrogen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
-
- 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
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/20—Oxygen atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Endocrinology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Reproductive Health (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Quinoline Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US29270401P | 2001-05-22 | 2001-05-22 | |
| US292704P | 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 |
|---|---|
| DE60210283D1 DE60210283D1 (de) | 2006-05-18 |
| DE60210283T2 true DE60210283T2 (de) | 2006-11-09 |
Family
ID=23125830
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60210283T Expired - Fee Related DE60210283T2 (de) | 2001-05-22 | 2002-05-09 | 2-substituierte 1,2,3,4-tetrahydrochinoline und derivate davon, zusammensetzungen und verfahren |
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
Also Published As
| Publication number | Publication date |
|---|---|
| JP2004531562A (ja) | 2004-10-14 |
| US20040215018A1 (en) | 2004-10-28 |
| WO2002094788A1 (en) | 2002-11-28 |
| ATE321754T1 (de) | 2006-04-15 |
| DE60210283D1 (de) | 2006-05-18 |
| ES2259376T3 (es) | 2006-10-01 |
| EP1395563A1 (en) | 2004-03-10 |
| EP1395563B1 (en) | 2006-03-29 |
| US7056931B2 (en) | 2006-06-06 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 8364 | No opposition during term of opposition | ||
| 8328 | Change in the person/name/address of the agent |
Representative=s name: KROHER, STROBEL RECHTS- UND PATENTANWAELTE, 80336 |
|
| 8339 | Ceased/non-payment of the annual fee |