ES2148312T3 - Inhibidores selectivos de aromatasa. - Google Patents
Inhibidores selectivos de aromatasa.Info
- Publication number
- ES2148312T3 ES2148312T3 ES94901975T ES94901975T ES2148312T3 ES 2148312 T3 ES2148312 T3 ES 2148312T3 ES 94901975 T ES94901975 T ES 94901975T ES 94901975 T ES94901975 T ES 94901975T ES 2148312 T3 ES2148312 T3 ES 2148312T3
- Authority
- ES
- Spain
- Prior art keywords
- pirazolyl
- choh
- combined
- aromatase
- compounds
- 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
- 102000014654 Aromatase Human genes 0.000 title abstract 2
- 108010078554 Aromatase Proteins 0.000 title abstract 2
- 229940124639 Selective inhibitor Drugs 0.000 title 1
- -1 1-IMIDAZOLYL Chemical class 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 206010006187 Breast cancer Diseases 0.000 abstract 1
- 208000026310 Breast neoplasm Diseases 0.000 abstract 1
- 102000004317 Lyases Human genes 0.000 abstract 1
- 108090000856 Lyases Proteins 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- IYABWNGZIDDRAK-UHFFFAOYSA-N allene Chemical group C=C=C IYABWNGZIDDRAK-UHFFFAOYSA-N 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- VUWZPRWSIVNGKG-UHFFFAOYSA-N fluoromethane Chemical compound F[CH2] VUWZPRWSIVNGKG-UHFFFAOYSA-N 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 206010020718 hyperplasia Diseases 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 150000003254 radicals Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
- C07D233/61—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon 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
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (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)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Plant Substances (AREA)
- Pyridine Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Abstract
NUEVOS COMPUESTOS DE FORMULA (I), DONDE R1 ES H, CH3, OCH3, NO2, NH2, CN, CF3, CH2F O HALOGENO, R2 ES UN RADICAL HETEROCICLICO ELEGIDO ENTRE 1-IMIDAZOLILO, TRIAZOLILO, TETRAZOLILO, PIRAZOLILO, PIRIMIDINILO, OXAZOLILO, TIAZOLILO, ISOXAZOLILO E ISOTIAZOLILO, R3 ES H O OH, R4 ES H, R5 ES H O OH; O R4 ES H Y R3 Y R5 COMBINADOS FORMAN UN ENLACE; O R3 Y H Y R4 Y R5 COMBINADOS FORMAN = O, R6 ES METILENO, ETILENO, -CHOH-, -CH2-CHOH-, -CHOH-CH2-, -CH=CH- O -C(=0)-; O R4 ES H Y R5 Y R6 COMBINADOS ES =CH- O =CH-CH2-; SUS ESTEROISOMEROS Y SUS SALES DE ADICION DE ACIDO FARMACEUTICAMENTE ACEPTABLES MUESTRAN PROPIEDADES DE INHIBICION DE AROMATASA SELECTIVA, COMPARADAS CON SU PROPIEDADES DE INHIBICION DE DESMOLASA. LOS COMPUESTOS DE LA INVENCION SE PUEDE EVALUAR EN EL TRATAMIENTO DE ENFERMEDADES ESTROGENODEPENDIENTES, POR EJEMPLO CANCER DE MAMA O HIPERPLASIA PROTATICA BENIGNA (BPH).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB9226209A GB2273704B (en) | 1992-12-16 | 1992-12-16 | Triazolyl diaryl selective aromatase inhibiting compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2148312T3 true ES2148312T3 (es) | 2000-10-16 |
Family
ID=10726697
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES94901975T Expired - Lifetime ES2148312T3 (es) | 1992-12-16 | 1993-12-14 | Inhibidores selectivos de aromatasa. |
Country Status (31)
| Country | Link |
|---|---|
| US (2) | US5703109A (es) |
| EP (1) | EP0674626B1 (es) |
| JP (1) | JP3186771B2 (es) |
| KR (1) | KR100347639B1 (es) |
| CN (1) | CN1056835C (es) |
| AT (1) | ATE194833T1 (es) |
| AU (1) | AU682332B2 (es) |
| BG (1) | BG62930B1 (es) |
| CA (1) | CA2150904A1 (es) |
| CZ (1) | CZ283043B6 (es) |
| DE (1) | DE69329072T2 (es) |
| DK (1) | DK0674626T3 (es) |
| EE (1) | EE03155B1 (es) |
| ES (1) | ES2148312T3 (es) |
| FI (1) | FI952867A7 (es) |
| GB (1) | GB2273704B (es) |
| GR (1) | GR3034618T3 (es) |
| HR (1) | HRP931494B1 (es) |
| IL (1) | IL107714A (es) |
| LT (1) | LT3151B (es) |
| NO (1) | NO310237B1 (es) |
| NZ (1) | NZ258588A (es) |
| PL (1) | PL176413B1 (es) |
| PT (1) | PT674626E (es) |
| RO (1) | RO113986B1 (es) |
| RU (1) | RU2131418C1 (es) |
| SI (1) | SI9300663B (es) |
| SK (1) | SK281667B6 (es) |
| TW (1) | TW327169B (es) |
| WO (1) | WO1994013645A1 (es) |
| ZA (1) | ZA938717B (es) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6080870A (en) * | 1996-04-03 | 2000-06-27 | Merck & Co., Inc. | Biaryl substituted imidazole compounds useful as farnesyl-protein transferase inhibitors |
| US6063930A (en) * | 1996-04-03 | 2000-05-16 | Merck & Co., Inc. | Substituted imidazole compounds useful as farnesyl-protein transferase inhibitors |
| AU715658B2 (en) * | 1996-04-03 | 2000-02-10 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| US5972921A (en) * | 1997-12-12 | 1999-10-26 | Hormos Medical Oy Ltd. | Use of an aromatase inhibitor in the treatment of decreased androgen to estrogen ratio and detrusor urethral sphincter dyssynergia in men |
| DE60118363T2 (de) * | 2000-07-10 | 2006-12-07 | Hormos Medical Ltd. | Methoden zur behandlung des kryptorchysmus |
| LT2762140T (lt) * | 2001-02-19 | 2017-06-26 | Novartis Ag | Solidinių smegenų navikų gydymas rapamicino dariniu |
| FI20010905A0 (fi) * | 2001-05-02 | 2001-05-02 | Vetcare Oy | Uusi eläinlääke |
| CN1325482C (zh) * | 2001-12-11 | 2007-07-11 | 埃默里大学 | 双(氰基苯基)甲基－三唑在预防乳腺癌中的用途 |
| RU2222326C1 (ru) * | 2002-10-09 | 2004-01-27 | Российский онкологический научный центр им. Н.Н.Блохина РАМН | Способ лечения саркомы юинга |
| EP1431292A1 (en) * | 2002-12-16 | 2004-06-23 | Laboratoire Theramex | 1-N-phenylamino-1H-imidazole derivatives as aromatase inhibitors |
| JP2004196795A (ja) * | 2002-12-16 | 2004-07-15 | Wyeth | 外部寄生虫駆除剤としてのｎ−フェニル−３−シクロプロピルピラゾール−４−カルボニトリル |
| US7345073B2 (en) | 2003-02-07 | 2008-03-18 | Hormos Medical Ltd. | Method for treating cryptorchidism |
| US20040248989A1 (en) | 2003-06-05 | 2004-12-09 | Risto Santti | Method for the treatment or prevention of lower urinary tract symptoms |
| WO2005058842A1 (en) * | 2003-12-15 | 2005-06-30 | Laboratoire Theramex | 1-n-phenyl-amino-1h-imidazole derivatives and pharmaceutical compositions containing them |
| US7825107B2 (en) * | 2006-05-22 | 2010-11-02 | Hormos Medical Ltd. | Method of treating men suffering from chronic nonbacterial prostatitis with SERM compounds or aromatase inhibitors |
| GB0914767D0 (en) * | 2009-08-24 | 2009-09-30 | Sterix Ltd | Compound |
| CA2794565C (en) | 2010-04-08 | 2018-08-21 | Emory University | Substituted androst-4-ene diones |
| JP5870093B2 (ja) * | 2010-05-27 | 2016-02-24 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ | 殺菌剤としてのヘテロ環式アルカノール誘導体 |
| KR101583521B1 (ko) | 2015-07-31 | 2016-01-08 | (주) 엘림비엠에스 | 내오염, 내마모 성능과 시공 작업성 및 광도 성능이 개선된 피브이씨 타일 바닥의 코팅방법 |
| CA3115420C (en) | 2018-04-19 | 2023-11-07 | Wonderland Switzerland Ag | Child carrier |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1580535A (en) | 1976-08-27 | 1980-12-03 | Ici Ltd | Substituted ketones and their use as herbicides |
| US5071861A (en) | 1986-03-07 | 1991-12-10 | Ciba-Geigy Corporation | Alpha-heterocycle substituted tolunitriles |
| US4978672A (en) | 1986-03-07 | 1990-12-18 | Ciba-Geigy Corporation | Alpha-heterocyclc substituted tolunitriles |
| US4749713A (en) * | 1986-03-07 | 1988-06-07 | Ciba-Geigy Corporation | Alpha-heterocycle substituted tolunitriles |
| US4937250A (en) | 1988-03-07 | 1990-06-26 | Ciba-Geigy Corporation | Alpha-heterocycle substituted tolunitriles |
| US5112845A (en) * | 1986-03-07 | 1992-05-12 | Ciba-Geigy Corporation | Alpha-heterocycle substituted tolunitriles |
| AU627559B2 (en) * | 1989-03-30 | 1992-08-27 | Farmos-Yhtyma Oy | Novel aromatase inhibiting 4(5)-imidazoles |
| ATE135000T1 (de) * | 1989-07-14 | 1996-03-15 | Ciba Geigy Ag | Substituierte benzonitrile |
| US5077374A (en) * | 1990-04-20 | 1991-12-31 | Phillips Petroleum Company | Aromatic sulfide polymers and method of preparation |
| DE4039559A1 (de) * | 1990-12-07 | 1992-06-11 | Schering Ag | Funktionalisierte vinylazole, verfahren zu deren herstellung, pharmazeutische praeparate die diese vinylazole enthalten sowie deren verwendung zur herstellung von arzneimitteln |
| GB9125924D0 (en) * | 1991-06-18 | 1992-02-05 | Orion Yhtymae Oy | Stereoisomers of an imidazole derivative |
-
1992
- 1992-12-16 GB GB9226209A patent/GB2273704B/en not_active Expired - Fee Related
-
1993
- 1993-11-22 ZA ZA938717A patent/ZA938717B/xx unknown
- 1993-11-23 IL IL10771493A patent/IL107714A/xx not_active IP Right Cessation
- 1993-12-03 LT LTIP1524A patent/LT3151B/lt not_active IP Right Cessation
- 1993-12-14 US US08/436,389 patent/US5703109A/en not_active Expired - Fee Related
- 1993-12-14 NZ NZ258588A patent/NZ258588A/en unknown
- 1993-12-14 DE DE69329072T patent/DE69329072T2/de not_active Expired - Fee Related
- 1993-12-14 JP JP51384094A patent/JP3186771B2/ja not_active Expired - Fee Related
- 1993-12-14 EP EP94901975A patent/EP0674626B1/en not_active Expired - Lifetime
- 1993-12-14 SK SK778-95A patent/SK281667B6/sk unknown
- 1993-12-14 FI FI952867A patent/FI952867A7/fi unknown
- 1993-12-14 AT AT94901975T patent/ATE194833T1/de not_active IP Right Cessation
- 1993-12-14 PT PT94901975T patent/PT674626E/pt unknown
- 1993-12-14 RU RU95114360/04A patent/RU2131418C1/ru not_active IP Right Cessation
- 1993-12-14 DK DK94901975T patent/DK0674626T3/da active
- 1993-12-14 PL PL93309350A patent/PL176413B1/pl unknown
- 1993-12-14 CA CA002150904A patent/CA2150904A1/en not_active Abandoned
- 1993-12-14 KR KR1019950702444A patent/KR100347639B1/ko not_active Expired - Fee Related
- 1993-12-14 AU AU56523/94A patent/AU682332B2/en not_active Ceased
- 1993-12-14 TW TW082110583A patent/TW327169B/zh active
- 1993-12-14 ES ES94901975T patent/ES2148312T3/es not_active Expired - Lifetime
- 1993-12-14 CZ CZ951532A patent/CZ283043B6/cs not_active IP Right Cessation
- 1993-12-14 WO PCT/FI1993/000539 patent/WO1994013645A1/en not_active Ceased
- 1993-12-14 RO RO95-01149A patent/RO113986B1/ro unknown
- 1993-12-15 HR HR931494A patent/HRP931494B1/xx not_active IP Right Cessation
- 1993-12-15 CN CN93120844A patent/CN1056835C/zh not_active Expired - Fee Related
- 1993-12-16 SI SI9300663A patent/SI9300663B/sl unknown
-
1994
- 1994-11-22 EE EE9400434A patent/EE03155B1/xx not_active IP Right Cessation
-
1995
- 1995-06-05 BG BG99699A patent/BG62930B1/bg unknown
- 1995-06-15 NO NO19952365A patent/NO310237B1/no unknown
-
1997
- 1997-09-15 US US08/929,424 patent/US5962495A/en not_active Expired - Fee Related
-
2000
- 2000-10-13 GR GR20000402303T patent/GR3034618T3/el not_active IP Right Cessation
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG2A | Definitive protection |
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