ES2148681T3 - Compuestos de benzotiofeno de uso farmaceutico. - Google Patents
Compuestos de benzotiofeno de uso farmaceutico.Info
- Publication number
- ES2148681T3 ES2148681T3 ES96301534T ES96301534T ES2148681T3 ES 2148681 T3 ES2148681 T3 ES 2148681T3 ES 96301534 T ES96301534 T ES 96301534T ES 96301534 T ES96301534 T ES 96301534T ES 2148681 T3 ES2148681 T3 ES 2148681T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- rdurule
- aryl
- compounds
- progestin
- 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
- 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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- 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
- A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Gynecology & Obstetrics (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
LA PRESENTE INVENCION PROPORCIONA UN COMPUESTO DE FORMULA I DONDE R{SUB,1} ES H, OH, HALO, OCO(C{SUB,1}-C{SUB,6} ALQUILO), OCO(ARILO), OSO{SUB,2} (C{SUB,4}-C{SUB,6} ALQUILO), OCOO (C{SUB,1}-C{SUB,6} ALQUILO),OCOO(ARILO), OCONH(C{SUB,1}-C{SUB,6} ALQUILO), O OCON(C{SUB,1}-C{SUB,6}ALQUILO){SUB,2}; R{SUB,2} ES ARILO, C{SUB,1}-C{SUB,6} ALQUILO, C{SUB,3}-C{SUB,6} CICLOALQUILO, O 4-CICLOHEXANOL; R{SUB,3} ES O(CH{SUB,2}){SUB,2} O O(CH{SUB,2}){SUB,3}; R{SUB,4} Y R{SUB,5} SON OPCIONALMENTE CO(CH{SUB,2}){SUB,3}, CO(CH{SUB,2}){SUB,4}, C{SUB,1}-C{SUB,6} ALQUILO, O R{SUB,4} Y R{SUB,5} SE COMBINA PARA FORMAR, CON EL NITROGENO PARA EL QUE ELLOS ESTAN LIGADOS, PIPERIDINA, MORFOLINA, PIRROLIDINA, 3METILPIROLLIDINA, 3,3-DIMETILPIROLLIDINA, 3,4-DIMETILPIROLLIDINA, AZEPINA O PIPECOLINA; R{SUB,6} ES C=CH{SUB,2}, CH(C{SUB,1}-C{SUB,5}ALQUILO), CH(C{SUB,2}-C{SUB,5} ALQUENILO), C=CH(C{SUB,1}-C{SUB,5} ALQUILO, CH(ARILO),C(OH)(C{SUB,1}C{SUB,5}ALQUILO), C(OH)(C{SUB,2}-C{SUB,5}ALQUENILO), C(OH)ARILO; Y SALES DE LAS MISMA ACEPTABLES FARMACEUTICAMENTE. LA PRESENTE INVENCION PROPORCIONA POSTERIORMENTE COMPOSICIONES FARMACEUTICAS CONTENIENDO COMPUESTOS DE LA FORMULA I, OPCIONALMENTE CONTENIENDO ESTROGENO O PROGESTINA, Y EL USO DE DICHOS COMPUESTOS SOLOS, O EN COMBINACION CON ESTROGENO O PROGESTINA, PARA ALIVIAR LOS SINTOMAS DEL SINDROME POSTMENOPAUSICO, PARTICULARMENTE OSTEOPOROSIS, CONDICIONES CARDIOVASCULARES PATOLOGICAMENTE RELACIONADAS Y CANCER DEPENDIENTE DE ESTROGENO. COMO SE USA AQUI , EL TERMINO "PROGESTINA" INCLUYE COMPUESTOS QUE CONTIENEN ACTIVIDAD PROGESTINACIONAL, COMO POR EJEMPLO, PROGESTERONA, NORETILNODRELO, NONGESTROL, ACETATO MEGESTROL, NORETINDRONE. LOS COMPUESTOS DE LA PRESENTE INVENCION TAMBIEN SON UTILES PARA LA INHIBICION DE ENFERMEDADES DE LAS FIBRAS UTERINAS Y ENDOMETRIOSIS EN MUJERES Y PROLIFERACION DE CELULAS MUSCULARES SUAVIZANTES DE LA AORTA, PARTICULARMENTE RESTENOSIS EN HUMANOS.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08/402,415 US6395755B1 (en) | 1995-03-10 | 1995-03-10 | Benzothiophene pharmaceutical compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2148681T3 true ES2148681T3 (es) | 2000-10-16 |
Family
ID=23591799
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES99202800T Expired - Lifetime ES2205702T3 (es) | 1995-03-10 | 1996-03-06 | Compuesto farmaceuticos de benzotiofeno. |
| ES96301534T Expired - Lifetime ES2148681T3 (es) | 1995-03-10 | 1996-03-06 | Compuestos de benzotiofeno de uso farmaceutico. |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES99202800T Expired - Lifetime ES2205702T3 (es) | 1995-03-10 | 1996-03-06 | Compuesto farmaceuticos de benzotiofeno. |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US6395755B1 (es) |
| EP (2) | EP0731100B1 (es) |
| JP (1) | JPH11501930A (es) |
| AT (2) | ATE195519T1 (es) |
| AU (1) | AU697502B2 (es) |
| BR (1) | BR9607775A (es) |
| CA (1) | CA2214261A1 (es) |
| DE (2) | DE69609748T2 (es) |
| DK (1) | DK0731100T3 (es) |
| ES (2) | ES2205702T3 (es) |
| GR (1) | GR3034762T3 (es) |
| IL (1) | IL117398A (es) |
| PT (1) | PT731100E (es) |
| SI (1) | SI0731100T1 (es) |
| WO (1) | WO1996028155A1 (es) |
| ZA (1) | ZA961883B (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6432982B1 (en) * | 1996-02-21 | 2002-08-13 | Eli Lilly And Company | Benzothiophenes, and formulations and methods using same |
| EP0801066A1 (en) * | 1996-03-12 | 1997-10-15 | Eli Lilly And Company | Heterocyclic substituted benzothiophenes and pharmaceutical compositions |
| CA2214072C (en) * | 1996-08-29 | 2006-11-14 | Eli Lilly And Company | Benzo [b] thiophene compounds, intermediates, processes, compositions, and methods |
| CA2214196A1 (en) * | 1996-09-26 | 1998-03-26 | Eli Lilly And Company | Benzo[b]indeno[2,1-d]thiophene compounds, intermediates, processes, compositions and methods |
| CA2216592C (en) * | 1996-10-24 | 2006-07-18 | Brian Stephen Muehl | Benzothiophene compounds, intermediates, compositions, and methods |
| US7056931B2 (en) | 2001-05-22 | 2006-06-06 | Eli Lilly And Company | 2-substituted 1,2,3,4-tetrahydroquinolines and derivatives thereof, compositions and methods |
| ES2236536T3 (es) | 2001-05-22 | 2005-07-16 | Eli Lilly And Company | Derivados tetrahidroquinolino para la inhibicion de enfermedades asociadas con la privacion de estrogenos o con una respuesta fisiologica aberrante a estrogenos endogenos. |
| IL158871A0 (en) | 2001-07-31 | 2004-05-12 | Pfizer Prod Inc | Pharmaceutical compositions, kits and methods comprising combinations of estrogen agonists/antagonists, estrogens and progestins |
| ATE448215T1 (de) * | 2004-01-22 | 2009-11-15 | Lilly Co Eli | Selektive östrogen-rezeptor-modulatoren |
| GR1005694B (el) * | 2005-06-08 | 2007-10-22 | Αλεξης Μιχαηλ | Ιστοειδικα αντιοιστρογονα ειδικα για τον αλφα υποδοχεα των οιστρογονων |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1300575B (de) * | 1965-05-21 | 1969-08-07 | Bristol Myers Co | Benzo[b]thiophene |
| US3947470A (en) | 1974-06-20 | 1976-03-30 | Smithkline Corporation | Substituted benzofurans and benzothiophenes |
| US4133814A (en) * | 1975-10-28 | 1979-01-09 | Eli Lilly And Company | 2-Phenyl-3-aroylbenzothiophenes useful as antifertility agents |
| IT1154888B (it) * | 1980-11-12 | 1987-01-21 | Menarini Sas | Derivati del benzofurano 2-sostituiti e relativi metodi di preparazione |
| IL65379A0 (en) * | 1981-04-03 | 1982-05-31 | Lilly Co Eli | Process for preparing acylated benzothiophenes |
| IL65404A0 (en) * | 1981-04-03 | 1982-07-30 | Lilly Co Eli | Benzothiophene compounds and process for preparing them |
| US4380635A (en) | 1981-04-03 | 1983-04-19 | Eli Lilly And Company | Synthesis of acylated benzothiophenes |
| US4418068A (en) * | 1981-04-03 | 1983-11-29 | Eli Lilly And Company | Antiestrogenic and antiandrugenic benzothiophenes |
| US4851554A (en) | 1987-04-06 | 1989-07-25 | University Of Tennessee Research Corporation | Certain 3-substituted 2-alkyl benzofuran derivatives |
| AU2543388A (en) * | 1987-09-30 | 1989-04-18 | University Of Tennessee Research Corporation, The | Certain 3-substituted 2-alkyl benzothiophene derivatives |
| US5395842A (en) * | 1988-10-31 | 1995-03-07 | Endorecherche Inc. | Anti-estrogenic compounds and compositions |
| FR2665444B1 (fr) * | 1990-08-06 | 1992-11-27 | Sanofi Sa | Derives d'amino-benzofuranne, benzothiophene ou indole, leur procede de preparation ainsi que les compositions les contenant. |
| 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 |
| 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 |
| US5523309A (en) * | 1995-03-10 | 1996-06-04 | Eli Lilly And Company | Benzofuran pharmaceutical compounds |
-
1995
- 1995-03-10 US US08/402,415 patent/US6395755B1/en not_active Expired - Fee Related
-
1996
- 1996-03-06 EP EP96301534A patent/EP0731100B1/en not_active Expired - Lifetime
- 1996-03-06 AT AT96301534T patent/ATE195519T1/de not_active IP Right Cessation
- 1996-03-06 SI SI9630256T patent/SI0731100T1/xx unknown
- 1996-03-06 EP EP99202800A patent/EP0953568B1/en not_active Expired - Lifetime
- 1996-03-06 DE DE69609748T patent/DE69609748T2/de not_active Expired - Fee Related
- 1996-03-06 ES ES99202800T patent/ES2205702T3/es not_active Expired - Lifetime
- 1996-03-06 AT AT99202800T patent/ATE247100T1/de not_active IP Right Cessation
- 1996-03-06 DE DE69629500T patent/DE69629500T2/de not_active Expired - Fee Related
- 1996-03-06 DK DK96301534T patent/DK0731100T3/da active
- 1996-03-06 ES ES96301534T patent/ES2148681T3/es not_active Expired - Lifetime
- 1996-03-06 PT PT96301534T patent/PT731100E/pt unknown
- 1996-03-07 CA CA002214261A patent/CA2214261A1/en not_active Abandoned
- 1996-03-07 AU AU53048/96A patent/AU697502B2/en not_active Ceased
- 1996-03-07 JP JP8527729A patent/JPH11501930A/ja active Pending
- 1996-03-07 WO PCT/US1996/003164 patent/WO1996028155A1/en active Application Filing
- 1996-03-07 IL IL11739896A patent/IL117398A/xx not_active IP Right Cessation
- 1996-03-07 BR BR9607775A patent/BR9607775A/pt not_active Application Discontinuation
- 1996-03-07 ZA ZA9601883A patent/ZA961883B/xx unknown
-
2000
- 2000-11-07 GR GR20000402451T patent/GR3034762T3/el not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| ZA961883B (en) | 1997-09-08 |
| ES2205702T3 (es) | 2004-05-01 |
| JPH11501930A (ja) | 1999-02-16 |
| US6395755B1 (en) | 2002-05-28 |
| DE69629500T2 (de) | 2004-07-01 |
| ATE195519T1 (de) | 2000-09-15 |
| IL117398A (en) | 2000-11-21 |
| DK0731100T3 (da) | 2000-09-18 |
| GR3034762T3 (en) | 2001-02-28 |
| AU5304896A (en) | 1996-10-02 |
| DE69609748D1 (de) | 2000-09-21 |
| EP0953568A1 (en) | 1999-11-03 |
| PT731100E (pt) | 2001-01-31 |
| EP0731100A1 (en) | 1996-09-11 |
| DE69609748T2 (de) | 2001-04-12 |
| IL117398A0 (en) | 1996-07-23 |
| AU697502B2 (en) | 1998-10-08 |
| DE69629500D1 (de) | 2003-09-18 |
| ATE247100T1 (de) | 2003-08-15 |
| WO1996028155A1 (en) | 1996-09-19 |
| SI0731100T1 (en) | 2001-02-28 |
| EP0731100B1 (en) | 2000-08-16 |
| MX9706737A (es) | 1997-11-29 |
| CA2214261A1 (en) | 1996-09-19 |
| EP0953568B1 (en) | 2003-08-13 |
| BR9607775A (pt) | 1998-07-07 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG2A | Definitive protection |
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