MX9706741A - Compuestos farmaceuticos novedosos de naftilo. - Google Patents
Compuestos farmaceuticos novedosos de naftilo.Info
- Publication number
- MX9706741A MX9706741A MX9706741A MX9706741A MX9706741A MX 9706741 A MX9706741 A MX 9706741A MX 9706741 A MX9706741 A MX 9706741A MX 9706741 A MX9706741 A MX 9706741A MX 9706741 A MX9706741 A MX 9706741A
- Authority
- MX
- Mexico
- Prior art keywords
- alkyl
- aryl
- compounds
- progestin
- estrogen
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 6
- 125000001624 naphthyl group Chemical group 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- 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
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 abstract 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 abstract 3
- 239000000262 estrogen Substances 0.000 abstract 3
- 229940011871 estrogen Drugs 0.000 abstract 3
- 239000000583 progesterone congener Substances 0.000 abstract 3
- 125000006729 (C2-C5) alkenyl group Chemical group 0.000 abstract 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 abstract 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- XBQNZPDIRJPFAI-UHFFFAOYSA-N 3,3-dimethylpyrrolidine Chemical compound CC1(C)CCNC1 XBQNZPDIRJPFAI-UHFFFAOYSA-N 0.000 abstract 1
- RDEHRKLSYJBKDV-UHFFFAOYSA-N 3,4-dimethylpyrrolidine Chemical compound CC1CNCC1C RDEHRKLSYJBKDV-UHFFFAOYSA-N 0.000 abstract 1
- KYINPWAJIVTFBW-UHFFFAOYSA-N 3-methylpyrrolidine Chemical compound CC1CCNC1 KYINPWAJIVTFBW-UHFFFAOYSA-N 0.000 abstract 1
- 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
- XYOVOXDWRFGKEX-UHFFFAOYSA-N azepine Chemical compound N1C=CC=CC=C1 XYOVOXDWRFGKEX-UHFFFAOYSA-N 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000004663 cell proliferation Effects 0.000 abstract 1
- HPXRVTGHNJAIIH-UHFFFAOYSA-N cyclohexanol Chemical group OC1CCCCC1 HPXRVTGHNJAIIH-UHFFFAOYSA-N 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
- 125000002573 ethenylidene group Chemical group [*]=C=C([H])[H] 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 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
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-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
- XSXHWVKGUXMUQE-UHFFFAOYSA-N osmium dioxide Inorganic materials O=[Os]=O XSXHWVKGUXMUQE-UHFFFAOYSA-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
- 150000003839 salts Chemical class 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
- 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
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P3/02—Nutrients, e.g. vitamins, minerals
-
- 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
- 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
-
- 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)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Nutrition Science (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyrrole Compounds (AREA)
Abstract
La presente invencion proporciona un compuesto de formula (I) en la que R1 es H, OH, halo, OCO(alquilo de C1-C6), OCO(arilo), OSO2(alquilo de C4-C6), OCOO(alquilo de C1-C6), OCOO(arilo), OCONH(alquilo de C1-C6) o OCON(alquilo de C1-C6)2; R2 es arilo, alquilo de C1-C6, cicloalquilo de C3-C6 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 C1-C6 o R4 y R5 se combinan para formar, junto con el nitrogeno al cual están unidos, piperidina, morfolina, pirrolidina, 3-metilpirrolidina, 3,3-dimetilpirrolidina, 3,4-dimetilpirrolidina, acepina o pipecolina; R6 es =C=CH2, =CH(alquilo de C1-C5), =CH(alquenilo de C2-C5), =C=CH(alquilo de C1-C5), =CH(arilo), =C(OH)(alquilo de C1-C5), =C(OH)(alquenilo de C2-C5), =C(OH)arilo; y sales farmacéuticamente aceptables de los mismos. La presente invencion proporciona de manera adicional composiciones farmacéuticas que contienen compuestos de formula (I) que opcionalmente contiene 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 osteoporosis, condiciones patologicas cardiovasculares relacionadas y cáncer dependiente de estrogeno. Como se utiliza en la presente, el término "progestina" incluye compuestos que tienen actividad progestacional tales como, por ejemplo, progesterona, noretilnodrel, acetato de megestrol, noretindrona y similares. Los compuestos de la presente invencion también son utiles para inhibir la enfermedad fibroide uterina y la endometrosis en mujeres y la proliferacion de células de musculo liso en aorta, particularmente la restenosis en humanos.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08402087 | 1995-03-10 | ||
| US08/402,087 US6391892B1 (en) | 1995-03-10 | 1995-03-10 | Naphthyl pharmaceutical compounds |
| PCT/US1996/003155 WO1996028146A1 (en) | 1995-03-10 | 1996-03-07 | Novel naphthyl pharmaceutical compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX9706741A true MX9706741A (es) | 1997-11-29 |
| MXPA97006741A MXPA97006741A (es) | 1998-07-03 |
Family
ID=
Also Published As
| Publication number | Publication date |
|---|---|
| IL117397A (en) | 2000-10-31 |
| US6391892B1 (en) | 2002-05-21 |
| IL117397A0 (en) | 1996-07-23 |
| EP0731093A1 (en) | 1996-09-11 |
| AU5187096A (en) | 1996-10-02 |
| US5691353A (en) | 1997-11-25 |
| CA2214416A1 (en) | 1996-09-19 |
| AU693016B2 (en) | 1998-06-18 |
| JPH11501929A (ja) | 1999-02-16 |
| ZA961884B (en) | 1997-09-09 |
| WO1996028146A1 (en) | 1996-09-19 |
| BR9607626A (pt) | 1999-06-01 |
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