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LTIP175A - New selective aromatase inhibiting 4(5)-imidazoles - Google Patents

New selective aromatase inhibiting 4(5)-imidazoles

Info

Publication number
LTIP175A
LTIP175A LTIP175A LTIP175A LTIP175A LT IP175 A LTIP175 A LT IP175A LT IP175 A LTIP175 A LT IP175A LT IP175 A LTIP175 A LT IP175A LT IP175 A LTIP175 A LT IP175A
Authority
LT
Lithuania
Prior art keywords
imidazoles
selective aromatase
aromatase inhibiting
new selective
halogen
Prior art date
Application number
LTIP175A
Other languages
Lithuanian (lt)
Inventor
Johannes Arto KARJALAINEN
Liisa Marja SOEDERVALL
Marketta Arja KALAPUDAS
Olavi Reino Pelkonen
Marja Aire LAINE
Arvo Sakari Risto Lammintausta
Sakari Jarmo Salonen
Original Assignee
Orion-Yhtymae Oy
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Priority claimed from GB919113142A external-priority patent/GB9113142D0/en
Application filed by Orion-Yhtymae Oy filed Critical Orion-Yhtymae Oy
Publication of LTIP175A publication Critical patent/LTIP175A/en
Publication of LT3164B publication Critical patent/LT3164B/en

Links

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
    • C07D233/64—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 substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Nauji 4(5)-imidazolodariniai, aprašomi formule@@@@@@@@@@@@@@@@kurioje vienas iš R1 ir R2 yra CN, o kitas yra H,CH3,OCH3,NO2,NH2,CN,CF3, CHF2,CH2F arba halogenas;@@R' yra H arba ,kur R3 yra H, Ch3 arba halogenas;@@@R4 yra H irR5 yra H arba R4 ir R5 kartu sudaro ryšį, n yra 1 arba 2 ir y yra nuo0 iki 2, jų stereoizomerai ir jų netoksiškos, farmaciškai priimtinos rūgščių druskos, pasižyminčios selektyviai aromatazę inhibuojančiomis savybes, palyginus su desmolazę inhibuojančiomis jų savybėmis. Išradimo junginiai yra vertingi, gydant nuo ekstrogeno priklausančias ligas, pvz., krūties vėžį arba gėrybinę prostatos hiperplaziją(GPH).New 4 (5) -imidazolodars described by the formula @@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@@ CF3, CHF2, CH2F or halogen; @@ R 'is H or where R3 is H, Ch3 or halogen; @@@ R4 is H and R5 is H or R4 and R5 together form a bond, n is 1 or 2 and y is from 0 to 2, their stereoisomers and their non-toxic pharmaceutically acceptable acid salts having selective aromatase inhibitory properties compared to their desmolase inhibitory properties. The compounds of the invention are valuable in the treatment of extragenic diseases such as breast cancer or benign prostatic hyperplasia (GPH).

LTIP175A 1991-06-18 1992-08-28 New selective aromatase inhibiting 4(5)-imidazoles LT3164B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB919113142A GB9113142D0 (en) 1991-06-18 1991-06-18 New selective aromatase inhibiting 4(5)-imidazoles
GB919125924A GB9125924D0 (en) 1991-06-18 1991-12-05 Stereoisomers of an imidazole derivative

Publications (2)

Publication Number Publication Date
LTIP175A true LTIP175A (en) 1994-08-25
LT3164B LT3164B (en) 1995-02-27

Family

ID=26299089

Family Applications (1)

Application Number Title Priority Date Filing Date
LTIP175A LT3164B (en) 1991-06-18 1992-08-28 New selective aromatase inhibiting 4(5)-imidazoles

Country Status (25)

Country Link
US (1) US5559141A (en)
EP (1) EP0589975A1 (en)
JP (1) JPH06508119A (en)
KR (1) KR940701386A (en)
CN (1) CN1068819A (en)
AU (1) AU665002B2 (en)
BG (1) BG98306A (en)
CA (1) CA2111469A1 (en)
CZ (1) CZ280293A3 (en)
FI (1) FI935658A (en)
GB (1) GB9125924D0 (en)
HR (1) HRP920170A2 (en)
HU (1) HUT67325A (en)
IE (1) IE921963A1 (en)
IL (2) IL102216A (en)
LT (1) LT3164B (en)
LV (1) LV10093B (en)
MX (1) MX9203000A (en)
NO (1) NO934688D0 (en)
NZ (1) NZ243139A (en)
PT (1) PT100604A (en)
SI (1) SI9200113A (en)
SK (1) SK144393A3 (en)
TW (1) TW206217B (en)
WO (1) WO1992022537A1 (en)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2273704B (en) * 1992-12-16 1997-01-22 Orion Yhtymae Oy Triazolyl diaryl selective aromatase inhibiting compounds
SE9302333D0 (en) * 1993-07-06 1993-07-06 Ab Astra NEW COMPOUNDS
US6063930A (en) * 1996-04-03 2000-05-16 Merck & Co., Inc. Substituted imidazole compounds useful as farnesyl-protein transferase inhibitors
WO1997036875A1 (en) * 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US6080870A (en) * 1996-04-03 2000-06-27 Merck & Co., Inc. Biaryl substituted imidazole compounds useful as farnesyl-protein transferase inhibitors
US6297239B1 (en) * 1997-10-08 2001-10-02 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
KR20030031132A (en) 2000-07-28 2003-04-18 스미또모 세이야꾸 가부시키가이샤 Pyrrole Derivatives
BRPI0415179A (en) 2003-10-07 2006-11-28 Renovis Inc amide derivatives such as ion channel ligands and pharmaceutical compositions and methods of employing them
US20080300243A1 (en) * 2005-02-28 2008-12-04 Kelly Michael G Amide Derivatives as Ion-Channel Ligands and Pharmaceutical Compositions and Methods of Using the Same
US7576099B2 (en) 2005-02-28 2009-08-18 Renovis, Inc. Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
US7902247B2 (en) * 2008-01-09 2011-03-08 Allergan, Inc. Substituted-aryl-2-phenylethyl-1H-imidazole compounds as subtype selective modulators of alpha 2B and/or alpha 2C adrenergic receptors
WO2024226608A2 (en) * 2023-04-25 2024-10-31 Aglaeapharma Inc. Imidazole containing compounds, derivatives therefore, and uses thereof

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4605661A (en) * 1984-06-18 1986-08-12 Eli Lilly And Company Aromastase inhibiting α,α-diarylimidazole-4(5)-propionitriles, α,α-diarylimidazole-4(5)-propionamides, and 4(5)-(2,2-diarylethyl)imidazoles
GB2210875B (en) * 1987-10-09 1991-05-29 Farmos Oy Aromatase inhibiting 4(5)-imidazoles
GB2248058B (en) * 1990-09-21 1994-09-14 Orion Yhtymae Oy Aromatase inhibiting 4(5)-imidazoles
JPH032168A (en) * 1989-03-30 1991-01-08 Farmos Yhtymae Oy Novel 4 (5)-imidazole having aromatase inhibitive activity
US5439928A (en) * 1989-03-30 1995-08-08 Orion-Yhtyma Oy Aromatase inhibiting 4(5)-imidazoles

Also Published As

Publication number Publication date
AU665002B2 (en) 1995-12-14
GB9125924D0 (en) 1992-02-05
HU9303653D0 (en) 1994-04-28
EP0589975A1 (en) 1994-04-06
IL115439A0 (en) 1995-12-31
IL102216A0 (en) 1993-01-14
US5559141A (en) 1996-09-24
NO934688L (en) 1993-12-17
NZ243139A (en) 1994-08-26
KR940701386A (en) 1994-05-28
SI9200113A (en) 1992-12-31
WO1992022537A1 (en) 1992-12-23
BG98306A (en) 1994-08-30
PT100604A (en) 1993-10-29
HUT67325A (en) 1995-03-28
TW206217B (en) 1993-05-21
LT3164B (en) 1995-02-27
JPH06508119A (en) 1994-09-14
FI935658A0 (en) 1993-12-16
LV10093A (en) 1994-05-10
MX9203000A (en) 1993-02-01
CA2111469A1 (en) 1992-12-23
AU1978392A (en) 1993-01-12
LV10093B (en) 1995-02-20
CZ280293A3 (en) 1994-05-18
FI935658A (en) 1993-12-16
CN1068819A (en) 1993-02-10
IL102216A (en) 1996-06-18
NO934688D0 (en) 1993-12-17
HRP920170A2 (en) 1994-08-31
SK144393A3 (en) 1994-11-09
IE921963A1 (en) 1992-12-30

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Legal Events

Date Code Title Description
MM9A Lapsed patents

Effective date: 19970828