MX9706738A - Nuevos compuestos farmaceuticos de benzofurano. - Google Patents
Nuevos compuestos farmaceuticos de benzofurano.Info
- Publication number
- MX9706738A MX9706738A MX9706738A MX9706738A MX9706738A MX 9706738 A MX9706738 A MX 9706738A MX 9706738 A MX9706738 A MX 9706738A MX 9706738 A MX9706738 A MX 9706738A MX 9706738 A MX9706738 A MX 9706738A
- Authority
- MX
- Mexico
- Prior art keywords
- compounds
- progestin
- estrogen
- formula
- present
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 6
- IANQTJSKSUMEQM-UHFFFAOYSA-N 1-benzofuran Chemical compound C1=CC=C2OC=CC2=C1 IANQTJSKSUMEQM-UHFFFAOYSA-N 0.000 title 2
- 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 abstract 5
- 239000000262 estrogen Substances 0.000 abstract 3
- 229940011871 estrogen Drugs 0.000 abstract 3
- 239000000583 progesterone congener Substances 0.000 abstract 3
- 201000009273 Endometriosis Diseases 0.000 abstract 1
- 206010027304 Menopausal symptoms Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 206010046798 Uterine leiomyoma Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000004663 cell proliferation Effects 0.000 abstract 1
- 230000001419 dependent effect Effects 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000002526 effect on cardiovascular system Effects 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 201000010260 leiomyoma Diseases 0.000 abstract 1
- 229960004296 megestrol acetate Drugs 0.000 abstract 1
- RQZAXGRLVPAYTJ-GQFGMJRRSA-N megestrol acetate Chemical compound C1=C(C)C2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 RQZAXGRLVPAYTJ-GQFGMJRRSA-N 0.000 abstract 1
- 229940053934 norethindrone Drugs 0.000 abstract 1
- VIKNJXKGJWUCNN-XGXHKTLJSA-N norethisterone Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 VIKNJXKGJWUCNN-XGXHKTLJSA-N 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000001072 progestational effect Effects 0.000 abstract 1
- 229960003387 progesterone Drugs 0.000 abstract 1
- 239000000186 progesterone Substances 0.000 abstract 1
- 208000037803 restenosis Diseases 0.000 abstract 1
- 210000000329 smooth muscle myocyte Anatomy 0.000 abstract 1
- 208000024891 symptom Diseases 0.000 abstract 1
- 208000010579 uterine corpus leiomyoma Diseases 0.000 abstract 1
- 201000007954 uterine fibroid Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
- C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
- C07D307/80—Radicals substituted by oxygen 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
- 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
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
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)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Furan Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invencion proporciona un compuesto de la formula (I) en donde R1 es hidrogeno, OH, halo, OCO(alquilo de 1 a 6 átomos de carbono), OCO(arilo), OSO2(alquilo de 4 a 6 átomos de carbono), OCOO(alquilo de 1 a 6 átomos de carbono), OCOO(arilo), OCONH(alquilo de 1 a 6 átomos de carbono), o OCON(alquilo de 1 a 6 átomos de carbono)2; R2 es arilo, alquilo de 1 a 6 átomos de carbono, cicloalquilo de 3 a 6 átomos de carbono, o 4-ciclohexanol; R3 es O(CH2)2 o O(CH2)3; R4 y R5 son opcionalmente CO(CH2)2CH3, CO(CH2)3CH3, alquilo de 1 a 6 átomos de carbono, o R4 y R5 se combinan para formar, con el nitrogeno, al cual están unidos, piperidina, morfolina, pirrolidina, 3-metilpirrolidina, 3,3-dimetilpirrolidina, 3,4-dimetilpirrolidina, azepina, o pipecolina; R6 es =C=CH2, =CH(alquilo de 1 a 5 átomos de carbono), =CH(alquenilo de 2 a 5 átomos de carbono), =C=CH(alquilo de 1 a 5 átomos de carbono), =CH(arilo), =C(OH) (alquilo de 1 a 5 átomos de carbono), =C(OH) (alquenilo de 2 a 5 átomos de carbono), =C(OH)arilo; y las sales farmacéuticamente aceptables de los mismos. La presente invencion proporciona además las composiciones farmacéuticas que contienen los compuestos de la formula (I), que contienen opcionalmente estrogeno o progestina y el uso de tales compuestos solos, o en combinacion con estrogeno o progestina, para aliviar los síntomas del síndrome post-menopáusico, particularmente la osteoporosis, condiciones patologicas relacionadas al sistema cardiovascular, y cáncer dependiente del estrogeno. Como se utiliza en la presente, el término "progestina" incluyen los compuestos que tienen actividad progestacional tales como, por ejemplo, progesterona, noretilnodrel, nongestrel, acetato de megestrol, noretindrona y similares. Los compuestos de la presente invencion son también utiles para inhibir la enfermedad fibroide uterina y la endometriosis en mujeres, y la proliferacion de células del musculo liso aortico, particularmente restenosis, en humanos.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08402285 | 1995-03-10 | ||
| US08/402,285 US5523309A (en) | 1995-03-10 | 1995-03-10 | Benzofuran pharmaceutical compounds |
| PCT/US1996/003163 WO1996028152A1 (en) | 1995-03-10 | 1996-03-07 | Novel benzofuran pharmaceutical compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX9706738A true MX9706738A (es) | 1997-11-29 |
| MXPA97006738A MXPA97006738A (es) | 1998-07-03 |
Family
ID=
Also Published As
| Publication number | Publication date |
|---|---|
| US5523309A (en) | 1996-06-04 |
| WO1996028152A1 (en) | 1996-09-19 |
| ES2142021T3 (es) | 2000-04-01 |
| JP2000510814A (ja) | 2000-08-22 |
| ZA961882B (en) | 1997-09-08 |
| PT731097E (pt) | 2000-07-31 |
| CA2214450A1 (en) | 1996-09-19 |
| AU692690B2 (en) | 1998-06-11 |
| GR3033326T3 (en) | 2000-09-29 |
| IL117396A0 (en) | 1996-07-23 |
| AU5187396A (en) | 1996-10-02 |
| DE69606566D1 (de) | 2000-03-16 |
| DK0731097T3 (da) | 2000-05-15 |
| DE69606566T2 (de) | 2000-06-29 |
| EP0731097A1 (en) | 1996-09-11 |
| EP0731097B1 (en) | 2000-02-09 |
| BR9607774A (pt) | 1998-07-07 |
| IL117396A (en) | 2000-01-31 |
| ATE189678T1 (de) | 2000-02-15 |
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