CA2214929A1 - Naphthofluorene compounds, intermediates, compositions and methods - Google Patents
Naphthofluorene compounds, intermediates, compositions and methods Download PDFInfo
- Publication number
- CA2214929A1 CA2214929A1 CA002214929A CA2214929A CA2214929A1 CA 2214929 A1 CA2214929 A1 CA 2214929A1 CA 002214929 A CA002214929 A CA 002214929A CA 2214929 A CA2214929 A CA 2214929A CA 2214929 A1 CA2214929 A1 CA 2214929A1
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- compound
- protecting group
- hydroxy protecting
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- 239000000203 mixture Substances 0.000 title abstract description 31
- 239000000543 intermediate Substances 0.000 title abstract description 14
- JPAMAQWNSMPRLT-UHFFFAOYSA-N 11h-indeno[2,1-a]phenanthrene Chemical class C1=CC=C2C3=CC=C4C5=CC=CC=C5CC4=C3C=CC2=C1 JPAMAQWNSMPRLT-UHFFFAOYSA-N 0.000 title abstract description 7
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- 150000001875 compounds Chemical class 0.000 claims description 127
- -1 methyl-1-pyrrolidinyl Chemical group 0.000 claims description 51
- 125000006239 protecting group Chemical group 0.000 claims description 26
- 150000003839 salts Chemical class 0.000 claims description 19
- 208000024891 symptom Diseases 0.000 claims description 15
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 11
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- NLXLAEXVIDQMFP-UHFFFAOYSA-N Ammonia chloride Chemical compound [NH4+].[Cl-] NLXLAEXVIDQMFP-UHFFFAOYSA-N 0.000 description 8
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 8
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- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical class CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 7
- 125000000217 alkyl group Chemical group 0.000 description 7
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- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 6
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 6
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
- C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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- 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
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- 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
- A61P3/06—Antihyperlipidemics
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- 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
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2603/00—Systems containing at least three condensed rings
- C07C2603/02—Ortho- or ortho- and peri-condensed systems
- C07C2603/52—Ortho- or ortho- and peri-condensed systems containing five condensed rings
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Physical Education & Sports Medicine (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (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)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pyrrole Compounds (AREA)
- Thin Film Transistor (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US2671596P | 1996-09-26 | 1996-09-26 | |
| US60/026,715 | 1996-09-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2214929A1 true CA2214929A1 (en) | 1998-03-26 |
Family
ID=21833411
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002214929A Abandoned CA2214929A1 (en) | 1996-09-26 | 1997-09-02 | Naphthofluorene compounds, intermediates, compositions and methods |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US5889000A (enExample) |
| EP (1) | EP0832882B1 (enExample) |
| JP (1) | JPH10147559A (enExample) |
| AT (1) | ATE215537T1 (enExample) |
| CA (1) | CA2214929A1 (enExample) |
| DE (1) | DE69711528T2 (enExample) |
| DK (1) | DK0832882T3 (enExample) |
| ES (1) | ES2175278T3 (enExample) |
| PT (1) | PT832882E (enExample) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005051898A2 (en) * | 2003-11-20 | 2005-06-09 | Eli Lilly And Company | Vitamin d receptor modulators |
| JP4589337B2 (ja) * | 2003-11-20 | 2010-12-01 | イーライ リリー アンド カンパニー | ビタミン受容体調節剤 |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3274213A (en) * | 1961-09-05 | 1966-09-20 | Upjohn Co | Alkoxy-substituted 2-phenyl-1-(tertiary-aminoalkoxy)phenyl-3, 4-dihydronaphthalenes |
| DE1300575B (de) * | 1965-05-21 | 1969-08-07 | Bristol Myers Co | Benzo[b]thiophene |
| US3394125A (en) * | 1965-10-23 | 1968-07-23 | Bristol Myers Co | 2-phenyl-3-tertiary-aminoalkoxy phenyl-and corresponding tertiaryaminoalkyl thio benzfurans substituted in the benzo nucleus with an alkoxy or tertiaryamino alkoxy or alkylthio group |
| US3974186A (en) * | 1970-05-14 | 1976-08-10 | Richardson-Merrell Inc. | Bis-basic ethers of 2,6- and 2,7-dihydroxyanthraquinones |
| CH564513A5 (en) * | 1971-05-24 | 1975-07-31 | Richardson Merrell Inc | Basically substd fluoranthene derivs - with antiviral activity |
| 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 |
| EP0065962A1 (en) * | 1980-12-03 | 1982-12-08 | Peabody Abc Corporation | Coupling for mine ventilation conduits |
| US4380635A (en) * | 1981-04-03 | 1983-04-19 | Eli Lilly And Company | Synthesis of acylated benzothiophenes |
| US4358593A (en) * | 1981-04-03 | 1982-11-09 | Eli Lilly And Company | Process for preparing 3-(4-aminoethoxybenzoyl)benzo[b]thiophenes |
| US4418068A (en) * | 1981-04-03 | 1983-11-29 | Eli Lilly And Company | Antiestrogenic and antiandrugenic benzothiophenes |
| IL65404A0 (en) * | 1981-04-03 | 1982-07-30 | Lilly Co Eli | Benzothiophene compounds and process for preparing them |
| DE3121175A1 (de) * | 1981-05-27 | 1982-12-16 | Klinge Pharma GmbH, 8000 München | Erythro-1,2,3-triphenyl-1-pentanon-derivate sowie verfahren zu ihrer herstellung und ihre verwendung als arzneimittel |
| WO1989002893A1 (en) * | 1987-09-30 | 1989-04-06 | The University Of Tennessee Research Corporation | Certain 3-substituted 2-alkyl benzothiophene derivatives |
| US5395842A (en) * | 1988-10-31 | 1995-03-07 | Endorecherche Inc. | Anti-estrogenic compounds and compositions |
| DE4117512A1 (de) * | 1991-05-25 | 1992-11-26 | Schering Ag | 2-phenylbenzo(b)furane und -thiophene, verfahren zu deren herstellung und diese enthaltende pharmazeutische praeparate |
| US5147880A (en) * | 1991-07-22 | 1992-09-15 | Eli Lilly And Company | Benzo[a]fluorene 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 |
| GB9220735D0 (en) * | 1992-10-02 | 1992-11-18 | British Tech Group | Heterocyclic amines |
| US6756388B1 (en) * | 1993-10-12 | 2004-06-29 | Pfizer Inc. | Benzothiophenes and related compounds as estrogen agonists |
| US7501441B1 (en) * | 1994-09-20 | 2009-03-10 | Eli Lilly And Company | Naphthyl compounds, intermediates, processes, compositions, and methods |
| US5998401A (en) * | 1995-02-28 | 1999-12-07 | Eli Lilly And Company | Naphthyl compounds, intermediates, compositions, and methods |
| GB2303628A (en) * | 1995-07-27 | 1997-02-26 | Lilly Co Eli | 5-Hydroxy- and 5-phenyl-substituted 1-[4-(aminoalkoxy)phenyl]-2-phenylbenzene derivatives for the treatment of post menopausal symptoms and intermediates |
| US5811421A (en) * | 1995-07-31 | 1998-09-22 | Eli Lilly And Company | Naphthyl and dihydronaphthyl intermediates, compounds, compositions, and methods |
-
1997
- 1997-09-02 CA CA002214929A patent/CA2214929A1/en not_active Abandoned
- 1997-09-22 US US08/934,988 patent/US5889000A/en not_active Expired - Fee Related
- 1997-09-24 JP JP9258346A patent/JPH10147559A/ja active Pending
- 1997-09-25 EP EP97307497A patent/EP0832882B1/en not_active Expired - Lifetime
- 1997-09-25 PT PT97307497T patent/PT832882E/pt unknown
- 1997-09-25 DE DE69711528T patent/DE69711528T2/de not_active Expired - Fee Related
- 1997-09-25 ES ES97307497T patent/ES2175278T3/es not_active Expired - Lifetime
- 1997-09-25 AT AT97307497T patent/ATE215537T1/de not_active IP Right Cessation
- 1997-09-25 DK DK97307497T patent/DK0832882T3/da active
-
1998
- 1998-09-30 US US09/163,424 patent/US5959103A/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| ATE215537T1 (de) | 2002-04-15 |
| JPH10147559A (ja) | 1998-06-02 |
| PT832882E (pt) | 2002-08-30 |
| US5889000A (en) | 1999-03-30 |
| DK0832882T3 (da) | 2002-06-17 |
| EP0832882A2 (en) | 1998-04-01 |
| EP0832882B1 (en) | 2002-04-03 |
| EP0832882A3 (en) | 1998-06-17 |
| ES2175278T3 (es) | 2002-11-16 |
| DE69711528D1 (de) | 2002-05-08 |
| US5959103A (en) | 1999-09-28 |
| DE69711528T2 (de) | 2002-10-31 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |