RU95114360A - Соединения, селективно ингибирующие ароматазу, способ получения, фармацевтическая композиция, способ лечения - Google Patents

Соединения, селективно ингибирующие ароматазу, способ получения, фармацевтическая композиция, способ лечения

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Publication number
RU95114360A
RU95114360A RU95114360/04A RU95114360A RU95114360A RU 95114360 A RU95114360 A RU 95114360A RU 95114360/04 A RU95114360/04 A RU 95114360/04A RU 95114360 A RU95114360 A RU 95114360A RU 95114360 A RU95114360 A RU 95114360A
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Russia
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rmeans
choh
treatment
synthesis
compounds
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RU95114360/04A
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English (en)
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RU2131418C1 (ru
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Йоханнес Карьялайнен Арто
Fi]
Седервалл Марья-Лииса
Маркетта Калапудас Арья
Олави Пельконен Рейно
Марья Лайне Айре
Арво Сакари Ламминтауста Ристо
Сакари Салонен Ярмо
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Орион-Ихтюмя Ой (FI)
Орион-Ихтюмя Ой
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Publication of RU95114360A publication Critical patent/RU95114360A/ru
Application granted granted Critical
Publication of RU2131418C1 publication Critical patent/RU2131418C1/ru

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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (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)
  • Engineering & Computer Science (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Diabetes (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)
  • Medicines Containing Plant Substances (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

Новые соединения формулы, в которой Rпредставляет собой H, CH, OCH, NO, NH, CH, CF, CHF, CHF или галоген, Rпредставляет собой гетероциклический радикал, выбранный из 1-имидазолила, триазолила, тетразолила, пиразолила, пиримидинила, оксазолила, тиазолила, изоксазолила и изотиазолила, Rпредставляет собой H или OH, Rпредставляет собой H, Rпредставляет собой H или OH или Rпредставляет собой H и Rи Rвместе образуют связь, или Rпредставляет собой водород и Rи Rвместе образуют = O, Rпредставляет собой метилен, этилен, -CHOH, -CH-CHOH-, -CHOH-CH-, -CH=CH- или -C(=O)-, или Rпредставляет собой H и Rи Rвместе образуют = CH- или = CH-CH-; их стереоизомеры и нетоксичные фармацевтически пригодные соли с кислотами их обладают селективными ингибирующими ароматазу свойствами по сравнению с их ингибирующими дезмолазу свойствами. Соединения изобретения пригодны для лечения экстрагензависимых заболеваний, например рака молочной железы или доброкачественной гиперплазии предстательной железы (ВРН).

Claims (1)

  1. Новые соединения формулы, в которой R1 представляет собой H, CH3, OCH3, NO2, NH2, CH, CF3, CHF2, CH2F или галоген, R2 представляет собой гетероциклический радикал, выбранный из 1-имидазолила, триазолила, тетразолила, пиразолила, пиримидинила, оксазолила, тиазолила, изоксазолила и изотиазолила, R3 представляет собой H или OH, R4 представляет собой H, R5 представляет собой H или OH или R4 представляет собой H и R3 и R5 вместе образуют связь, или R3 представляет собой водород и R4 и R5 вместе образуют = O, R6 представляет собой метилен, этилен, -CHOH, -CH2-CHOH-, -CHOH-CH2-, -CH=CH- или -C(=O)-, или R4 представляет собой H и R5 и R6 вместе образуют = CH- или = CH-CH2-; их стереоизомеры и нетоксичные фармацевтически пригодные соли с кислотами их обладают селективными ингибирующими ароматазу свойствами по сравнению с их ингибирующими дезмолазу свойствами. Соединения изобретения пригодны для лечения экстрагензависимых заболеваний, например рака молочной железы или доброкачественной гиперплазии предстательной железы (ВРН).
RU95114360/04A 1992-12-16 1993-12-14 Соединения, селективно ингибирующие ароматазу, способ получения и фармацевтическая композиция RU2131418C1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB9226209A GB2273704B (en) 1992-12-16 1992-12-16 Triazolyl diaryl selective aromatase inhibiting compounds
GB9226209.6 1992-12-16
PCT/FI1993/000539 WO1994013645A1 (en) 1992-12-16 1993-12-14 Novel selective aromatase inhibiting compounds

Publications (2)

Publication Number Publication Date
RU95114360A true RU95114360A (ru) 1997-06-10
RU2131418C1 RU2131418C1 (ru) 1999-06-10

Family

ID=10726697

Family Applications (1)

Application Number Title Priority Date Filing Date
RU95114360/04A RU2131418C1 (ru) 1992-12-16 1993-12-14 Соединения, селективно ингибирующие ароматазу, способ получения и фармацевтическая композиция

Country Status (31)

Country Link
US (2) US5703109A (ru)
EP (1) EP0674626B1 (ru)
JP (1) JP3186771B2 (ru)
KR (1) KR100347639B1 (ru)
CN (1) CN1056835C (ru)
AT (1) ATE194833T1 (ru)
AU (1) AU682332B2 (ru)
BG (1) BG62930B1 (ru)
CA (1) CA2150904A1 (ru)
CZ (1) CZ283043B6 (ru)
DE (1) DE69329072T2 (ru)
DK (1) DK0674626T3 (ru)
EE (1) EE03155B1 (ru)
ES (1) ES2148312T3 (ru)
FI (1) FI952867A0 (ru)
GB (1) GB2273704B (ru)
GR (1) GR3034618T3 (ru)
HR (1) HRP931494B1 (ru)
IL (1) IL107714A (ru)
LT (1) LT3151B (ru)
NO (1) NO310237B1 (ru)
NZ (1) NZ258588A (ru)
PL (1) PL176413B1 (ru)
PT (1) PT674626E (ru)
RO (1) RO113986B1 (ru)
RU (1) RU2131418C1 (ru)
SI (1) SI9300663B (ru)
SK (1) SK281667B6 (ru)
TW (1) TW327169B (ru)
WO (1) WO1994013645A1 (ru)
ZA (1) ZA938717B (ru)

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WO1997036876A1 (en) * 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US6063930A (en) * 1996-04-03 2000-05-16 Merck & Co., Inc. Substituted imidazole compounds useful as farnesyl-protein transferase inhibitors
US6080870A (en) * 1996-04-03 2000-06-27 Merck & Co., Inc. Biaryl substituted imidazole compounds useful as farnesyl-protein transferase inhibitors
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
WO2002009703A1 (en) * 2000-07-10 2002-02-07 Hormos Medical Corporation Method for treating cryptorchidism
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
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
EP1431292A1 (en) * 2002-12-16 2004-06-23 Laboratoire Theramex 1-N-phenylamino-1H-imidazole derivatives as aromatase inhibitors
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
MXPA06006837A (es) * 2003-12-15 2006-09-04 Theramex Derivados de 1-n-fenil-amino-ih-imidazol y composiciones farmaceuticas que los contienen.
RU2480207C2 (ru) * 2006-05-22 2013-04-27 Хормос Медикал Лтд. Способ лечения хронического абактериального простатита селективными модуляторами рецепторов эстрогена или ингибиторами ароматазы
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

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Also Published As

Publication number Publication date
DE69329072D1 (de) 2000-08-24
GB9226209D0 (en) 1993-02-10
PL309350A1 (en) 1995-10-02
NO952365L (no) 1995-06-15
EP0674626B1 (en) 2000-07-19
DE69329072T2 (de) 2000-12-21
AU5652394A (en) 1994-07-04
FI952867A (fi) 1995-06-09
IL107714A (en) 2003-07-31
NZ258588A (en) 1996-11-26
CZ153295A3 (en) 1995-11-15
JP3186771B2 (ja) 2001-07-11
CA2150904A1 (en) 1994-06-23
GB2273704B (en) 1997-01-22
RU2131418C1 (ru) 1999-06-10
TW327169B (en) 1998-02-21
SK281667B6 (sk) 2001-06-11
AU682332B2 (en) 1997-10-02
CZ283043B6 (cs) 1997-12-17
KR950704263A (ko) 1995-11-17
CN1056835C (zh) 2000-09-27
NO310237B1 (no) 2001-06-11
HRP931494B1 (en) 2001-06-30
SI9300663B (sl) 2002-02-28
FI952867A0 (fi) 1995-06-09
LTIP1524A (en) 1994-07-15
SI9300663A (en) 1994-09-30
HRP931494A2 (en) 1996-08-31
GR3034618T3 (en) 2001-01-31
EE03155B1 (et) 1999-02-15
GB2273704A (en) 1994-06-29
LT3151B (en) 1995-01-31
SK77895A3 (en) 1995-12-06
EP0674626A1 (en) 1995-10-04
ATE194833T1 (de) 2000-08-15
PT674626E (pt) 2000-11-30
PL176413B1 (pl) 1999-05-31
RO113986B1 (ro) 1998-12-30
BG62930B1 (bg) 2000-11-30
ZA938717B (en) 1994-06-30
IL107714A0 (en) 1994-02-27
NO952365D0 (no) 1995-06-15
BG99699A (bg) 1996-04-30
DK0674626T3 (da) 2000-11-13
ES2148312T3 (es) 2000-10-16
US5703109A (en) 1997-12-30
JPH08504424A (ja) 1996-05-14
US5962495A (en) 1999-10-05
CN1093357A (zh) 1994-10-12
WO1994013645A1 (en) 1994-06-23
KR100347639B1 (ko) 2002-11-29

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