ES2183288T3 - Compuestos de indeno con actividad como moduladores selectivos de receptores de estrogenos. - Google Patents
Compuestos de indeno con actividad como moduladores selectivos de receptores de estrogenos.Info
- Publication number
- ES2183288T3 ES2183288T3 ES98303132T ES98303132T ES2183288T3 ES 2183288 T3 ES2183288 T3 ES 2183288T3 ES 98303132 T ES98303132 T ES 98303132T ES 98303132 T ES98303132 T ES 98303132T ES 2183288 T3 ES2183288 T3 ES 2183288T3
- Authority
- ES
- Spain
- Prior art keywords
- activity
- indene
- compounds
- pyrrolidinyl
- possess
- 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 - Lifetime
Links
Classifications
-
- 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
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C43/00—Ethers; Compounds having groups, groups or groups
- C07C43/02—Ethers
- C07C43/20—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
- C07C43/23—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing hydroxy or O-metal groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D339/00—Heterocyclic compounds containing rings having two sulfur atoms as the only ring hetero atoms
- C07D339/08—Six-membered rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2602/00—Systems containing two condensed rings
- C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
- C07C2602/04—One of the condensed rings being a six-membered aromatic ring
- C07C2602/08—One of the condensed rings being a six-membered aromatic ring the other ring being five-membered, e.g. indane
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (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)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Hydrogenated Pyridines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
LA PRESENTE INVENCION PROPORCIONA UNA CLASE DE COMPUESTOS DE INDENO SUSTITUIDOS Y SUS SALES FARMACEUTICAMENTE ACEPTABLES, QUE POSEEN ACTIVIDAD MODULADORA SELECTIVA DE LOS RECEPTORES DE ESTROGENO (SERM) Y SON UTILES POR TANTO PARA EL TRATAMIENTO DE LA OSTEOPOROSIS Y LA ENFERMEDAD CARDIOVASCULAR, ESPECIALMENTE LA HIPERLIPIDEMIA EN MUJERES. DICHOS COMPUESTOS POSEEN LA ESTRUCTURA: DONDE R 1 ES HIDROGENO, HIDROXILO, ALCOXI, FENILC ARBONILOXI, ALQUILCARBONILOXI O ALQUILSULFONILOXI; R 2 ES HIDROGENO, HIDROXILO, HALO, ALCOXI, FENILCARBONILOXI, ALQUILCARBONILOXI O ALQUILSULFONILOXI; R 3 ES 1 - PIPERIDINILO, 1 PIRROLIDINILO, METIL - 1 - PIRROLIDINILO, DIMETIL - 1 PIRROLIDINILO, 4 - MORFOLINO, DIMETILAMINO, DIETILAMINO, DIISOPROPILAMINO O 1 - HEXAMETILENIMINO; Y N ES 1, 2 O 3. EL ENLACE REPRESENTADO POR LA LINEA DISCONTINUA ENTRE LOS ATOMOS DE CARBONO SITUADOS EN LAS POSICIONES 1 Y 2 DEL NUCLEO DE INDENO REPRESENTA UN ENLACE DOBLE OPCIONAL, CON LA CONDICION DE QUE CUANDO EL ENLACE DOBLE ESTA AUSENTE,EL GRUPO HIDROXILO ENTRE PARENTESIS SITUADO EN POSICION 1 ESTA PRESENTE Y VICEVERSA. CIERTOS PRECURSORES 2, 3 - DIHIDRO - 1H - INDENO DE LOS COMPUESTOS DE INDENO DESCRITOS POSEEN TAMBIEN ACTIVIDAD SERM Y SON UTILES PARA LOS MISMOS FINES.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US4492397P | 1997-04-25 | 1997-04-25 |
Publications (1)
Publication Number | Publication Date |
---|---|
ES2183288T3 true ES2183288T3 (es) | 2003-03-16 |
Family
ID=21935066
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES98303132T Expired - Lifetime ES2183288T3 (es) | 1997-04-25 | 1998-04-23 | Compuestos de indeno con actividad como moduladores selectivos de receptores de estrogenos. |
Country Status (9)
Country | Link |
---|---|
US (1) | US5994370A (es) |
EP (1) | EP0873992B1 (es) |
JP (1) | JP2002510289A (es) |
AT (1) | ATE224883T1 (es) |
AU (1) | AU7467398A (es) |
CA (1) | CA2287244A1 (es) |
DE (1) | DE69808169T2 (es) |
ES (1) | ES2183288T3 (es) |
WO (1) | WO1998048806A1 (es) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2252273T3 (es) * | 2000-08-23 | 2006-05-16 | Akzo Nobel N.V. | Derivados de 10-aril-11h-benzo(b)fluoreno y analogos destinados para una utilizacion medicinal. |
JP2004523508A (ja) * | 2001-01-04 | 2004-08-05 | カロ バイオ アクチェブラーグ | 新規エストロゲン受容体リガンドおよび方法i |
WO2002056903A2 (en) * | 2001-01-17 | 2002-07-25 | Praecis Pharmaceuticals Inc. | Methods for treating hormone associated conditions using a combination of lhrh antagonists and specific estrogen receptor modulators |
TW200304371A (en) | 2002-02-22 | 2003-10-01 | Akzo Nobel Nv | Substituted 10-ary1-11H-benzo [b] fluorenes and 7-ary1-5, 6-dihydro-benz [a] anthracenes for selective effects on estrogen receptors |
AU2003263402A1 (en) | 2002-09-20 | 2004-04-08 | Pfizer Products Inc. | Amide and sulfonamide ligands for the estrogen receptor |
KR100595963B1 (ko) | 2004-04-13 | 2006-07-05 | 한국화학연구원 | 인덴 유도체 및 이의 제조방법 |
WO2011159769A2 (en) * | 2010-06-17 | 2011-12-22 | Aragon Pharmaceuticals, Inc. | Indane estrogen receptor modulators and uses thereof |
Family Cites Families (26)
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 |
GB1138163A (en) * | 1965-05-21 | 1968-12-27 | Bristol Myers Co | Benzothiophene derivatives having anti-fertility properties |
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 |
US3483293A (en) * | 1967-12-15 | 1969-12-09 | Upjohn Co | Method for controlling birds and rodents |
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 |
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 |
NZ200204A (en) * | 1981-04-03 | 1985-05-31 | Lilly Co Eli | Benzothiophene derivatives and process for preparation |
US4380635A (en) * | 1981-04-03 | 1983-04-19 | Eli Lilly And Company | Synthesis of acylated benzothiophenes |
US4729999A (en) * | 1984-10-12 | 1988-03-08 | Bcm Technologies | Antiestrogen therapy for symptoms of estrogen deficiency |
US4916126A (en) * | 1987-09-25 | 1990-04-10 | Ciba-Geigy Corporation | Diacyl derivatives of 4-(trialkylbenzyl)-piperazinyl compounds |
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 |
US6756388B1 (en) * | 1993-10-12 | 2004-06-29 | Pfizer Inc. | Benzothiophenes and related compounds as estrogen agonists |
US5591753A (en) * | 1994-01-28 | 1997-01-07 | Eli Lilly And Company | Combination treatment for osteoporosis |
US7501441B1 (en) * | 1994-09-20 | 2009-03-10 | Eli Lilly And Company | Naphthyl compounds, intermediates, processes, compositions, and methods |
US5552412A (en) * | 1995-01-09 | 1996-09-03 | Pfizer Inc | 5-substitued-6-cyclic-5,6,7,8-tetrahydronaphthalen2-ol compounds which are useful for treating osteoporosis |
US6391892B1 (en) * | 1995-03-10 | 2002-05-21 | Eli Lilly And Company | Naphthyl pharmaceutical compounds |
US6451817B1 (en) * | 1995-03-10 | 2002-09-17 | Eli Lilly And Company | Alpha-substituted-1-benzyl-napthyls |
US5811421A (en) * | 1995-07-31 | 1998-09-22 | Eli Lilly And Company | Naphthyl and dihydronaphthyl intermediates, compounds, compositions, and methods |
CA2213814A1 (en) * | 1996-08-29 | 1998-02-28 | Henry Uhlman Bryant | Naphthalene compounds, intermediates, formulations, and methods |
CA2217810A1 (en) * | 1996-10-10 | 1998-04-10 | Eli Lilly And Company | 2-aryl-3-aminoaryloxynaphthyl compounds, intermediates, compositions and methods |
US5916916A (en) * | 1996-10-10 | 1999-06-29 | Eli Lilly And Company | 1-aryloxy-2-arylnaphthyl compounds, intermediates, compositions, and methods |
-
1998
- 1998-04-20 WO PCT/US1998/007816 patent/WO1998048806A1/en active Search and Examination
- 1998-04-20 JP JP54706698A patent/JP2002510289A/ja active Pending
- 1998-04-20 AU AU74673/98A patent/AU7467398A/en not_active Abandoned
- 1998-04-20 CA CA002287244A patent/CA2287244A1/en not_active Abandoned
- 1998-04-22 US US09/064,548 patent/US5994370A/en not_active Expired - Fee Related
- 1998-04-23 AT AT98303132T patent/ATE224883T1/de not_active IP Right Cessation
- 1998-04-23 EP EP98303132A patent/EP0873992B1/en not_active Expired - Lifetime
- 1998-04-23 ES ES98303132T patent/ES2183288T3/es not_active Expired - Lifetime
- 1998-04-23 DE DE69808169T patent/DE69808169T2/de not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
WO1998048806A1 (en) | 1998-11-05 |
AU7467398A (en) | 1998-11-24 |
DE69808169T2 (de) | 2003-05-22 |
US5994370A (en) | 1999-11-30 |
DE69808169D1 (de) | 2002-10-31 |
EP0873992A1 (en) | 1998-10-28 |
ATE224883T1 (de) | 2002-10-15 |
CA2287244A1 (en) | 1998-11-05 |
JP2002510289A (ja) | 2002-04-02 |
EP0873992B1 (en) | 2002-09-25 |
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