SI9200113A - New selective aromatase inhibiting 4(5)-imidazoles - Google Patents
New selective aromatase inhibiting 4(5)-imidazoles Download PDFInfo
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- SI9200113A SI9200113A SI19929200113A SI9200113A SI9200113A SI 9200113 A SI9200113 A SI 9200113A SI 19929200113 A SI19929200113 A SI 19929200113A SI 9200113 A SI9200113 A SI 9200113A SI 9200113 A SI9200113 A SI 9200113A
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- SI
- Slovenia
- Prior art keywords
- imidazole
- compound according
- cyanophenyl
- pharmaceutically acceptable
- toxic
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- 102000014654 Aromatase Human genes 0.000 title claims abstract description 14
- 108010078554 Aromatase Proteins 0.000 title claims abstract description 14
- 230000002401 inhibitory effect Effects 0.000 title claims abstract description 11
- 150000001875 compounds Chemical class 0.000 claims abstract description 160
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- 150000003839 salts Chemical class 0.000 claims abstract description 32
- 231100000252 nontoxic Toxicity 0.000 claims abstract description 30
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- 229910052736 halogen Inorganic materials 0.000 claims abstract description 24
- 150000002367 halogens Chemical class 0.000 claims abstract description 24
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims description 39
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- JZJRCTXRFYSHPA-UHFFFAOYSA-N n-tert-butyl-4-[3-(4-fluorophenyl)-1-hydroxy-1-(1h-imidazol-5-yl)propyl]benzamide Chemical compound C1=CC(C(=O)NC(C)(C)C)=CC=C1C(O)(C=1N=CNC=1)CCC1=CC=C(F)C=C1 JZJRCTXRFYSHPA-UHFFFAOYSA-N 0.000 description 1
- SYTPXAXERSBEQM-UHFFFAOYSA-N n-tert-butyl-4-[3-(4-fluorophenyl)-3-hydroxy-3-(1h-imidazol-5-yl)propyl]benzamide Chemical compound C1=CC(C(=O)NC(C)(C)C)=CC=C1CCC(O)(C=1C=CC(F)=CC=1)C1=CNC=N1 SYTPXAXERSBEQM-UHFFFAOYSA-N 0.000 description 1
- 150000002823 nitrates Chemical class 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 239000012299 nitrogen atmosphere Substances 0.000 description 1
- 238000013421 nuclear magnetic resonance imaging Methods 0.000 description 1
- 238000000655 nuclear magnetic resonance spectrum Methods 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 235000019198 oils Nutrition 0.000 description 1
- 239000004006 olive oil Substances 0.000 description 1
- 235000008390 olive oil Nutrition 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 239000012044 organic layer Substances 0.000 description 1
- 239000012074 organic phase Substances 0.000 description 1
- 230000002018 overexpression Effects 0.000 description 1
- 230000037361 pathway Effects 0.000 description 1
- 239000000312 peanut oil Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 235000021317 phosphate Nutrition 0.000 description 1
- 150000003013 phosphoric acid derivatives Chemical class 0.000 description 1
- 230000035479 physiological effects, processes and functions Effects 0.000 description 1
- 230000003169 placental effect Effects 0.000 description 1
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 description 1
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000035935 pregnancy Effects 0.000 description 1
- ORNBQBCIOKFOEO-QGVNFLHTSA-N pregnenolone Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 ORNBQBCIOKFOEO-QGVNFLHTSA-N 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 230000002285 radioactive effect Effects 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 239000013558 reference substance Substances 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 150000003873 salicylate salts Chemical class 0.000 description 1
- 239000012047 saturated solution Substances 0.000 description 1
- 230000007017 scission Effects 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- 238000001228 spectrum Methods 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 150000003871 sulfonates Chemical class 0.000 description 1
- 150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 150000003892 tartrate salts Chemical class 0.000 description 1
- YBRBMKDOPFTVDT-UHFFFAOYSA-N tert-butylamine Chemical compound CC(C)(C)N YBRBMKDOPFTVDT-UHFFFAOYSA-N 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- CZDYPVPMEAXLPK-UHFFFAOYSA-N tetramethylsilane Chemical compound C[Si](C)(C)C CZDYPVPMEAXLPK-UHFFFAOYSA-N 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 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
- C07D233/64—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)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
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 (1)
| Publication Number | Publication Date |
|---|---|
| SI9200113A true SI9200113A (en) | 1992-12-31 |
Family
ID=26299089
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SI19929200113A SI9200113A (en) | 1991-06-18 | 1992-06-18 | New selective aromatase inhibiting 4(5)-imidazoles |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US5559141A (cs) |
| EP (1) | EP0589975A1 (cs) |
| JP (1) | JPH06508119A (cs) |
| KR (1) | KR940701386A (cs) |
| CN (1) | CN1068819A (cs) |
| AU (1) | AU665002B2 (cs) |
| BG (1) | BG98306A (cs) |
| CA (1) | CA2111469A1 (cs) |
| CZ (1) | CZ280293A3 (cs) |
| FI (1) | FI935658A7 (cs) |
| GB (1) | GB9125924D0 (cs) |
| HR (1) | HRP920170A2 (cs) |
| HU (1) | HUT67325A (cs) |
| IE (1) | IE921963A1 (cs) |
| IL (2) | IL102216A (cs) |
| LT (1) | LT3164B (cs) |
| LV (1) | LV10093B (cs) |
| MX (1) | MX9203000A (cs) |
| NO (1) | NO934688L (cs) |
| NZ (1) | NZ243139A (cs) |
| PT (1) | PT100604A (cs) |
| SI (1) | SI9200113A (cs) |
| SK (1) | SK144393A3 (cs) |
| TW (1) | TW206217B (cs) |
| WO (1) | WO1992022537A1 (cs) |
Families Citing this family (12)
| 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 (sv) * | 1993-07-06 | 1993-07-06 | Ab Astra | New compounds |
| US6080870A (en) * | 1996-04-03 | 2000-06-27 | Merck & Co., Inc. | Biaryl substituted imidazole compounds useful as farnesyl-protein transferase inhibitors |
| EP0891333A1 (en) * | 1996-04-03 | 1999-01-20 | 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 |
| US6297239B1 (en) * | 1997-10-08 | 2001-10-02 | Merck & Co., Inc. | Inhibitors of prenyl-protein transferase |
| AU2001275794A1 (en) | 2000-07-28 | 2002-02-13 | Sumitomo Pharmaceuticals Co. Ltd. | Pyrrole derivatives |
| AR046276A1 (es) | 2003-10-07 | 2005-11-30 | Renovis Inc | Derivados de amida como ligandos de canales ionicos y composiciones farmaceuticas y metodos que los utilizan. |
| EA200701835A1 (ru) * | 2005-02-28 | 2008-02-28 | Реновис, Инк. | Амидные производные в качестве лигандов ионных каналов, их фармацевтические композиции и способы их применения |
| 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)
| 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 |
| US5439928A (en) * | 1989-03-30 | 1995-08-08 | Orion-Yhtyma Oy | Aromatase inhibiting 4(5)-imidazoles |
| JPH032168A (ja) * | 1989-03-30 | 1991-01-08 | Farmos Yhtymae Oy | アロマターゼ阻害活性を有する新規な４（５）―イミダゾール |
-
1991
- 1991-12-05 GB GB919125924A patent/GB9125924D0/en active Pending
-
1992
- 1992-06-12 US US08/167,873 patent/US5559141A/en not_active Expired - Fee Related
- 1992-06-12 CA CA002111469A patent/CA2111469A1/en not_active Abandoned
- 1992-06-12 CZ CS932802A patent/CZ280293A3/cs unknown
- 1992-06-12 JP JP4511061A patent/JPH06508119A/ja active Pending
- 1992-06-12 SK SK1443-93A patent/SK144393A3/sk unknown
- 1992-06-12 AU AU19783/92A patent/AU665002B2/en not_active Ceased
- 1992-06-12 EP EP92912309A patent/EP0589975A1/en not_active Withdrawn
- 1992-06-12 KR KR1019930703934A patent/KR940701386A/ko not_active Withdrawn
- 1992-06-12 WO PCT/FI1992/000184 patent/WO1992022537A1/en not_active Application Discontinuation
- 1992-06-15 LV LVP-92-29A patent/LV10093B/en unknown
- 1992-06-15 NZ NZ243139A patent/NZ243139A/en unknown
- 1992-06-16 IL IL10221692A patent/IL102216A/en not_active IP Right Cessation
- 1992-06-17 PT PT100604A patent/PT100604A/pt not_active Application Discontinuation
- 1992-06-17 HR HR920170A patent/HRP920170A2/hr not_active Application Discontinuation
- 1992-06-17 TW TW081104752A patent/TW206217B/zh active
- 1992-06-18 CN CN92105664A patent/CN1068819A/zh active Pending
- 1992-06-18 SI SI19929200113A patent/SI9200113A/sl unknown
- 1992-06-18 MX MX9203000A patent/MX9203000A/es unknown
- 1992-07-01 IE IE196392A patent/IE921963A1/en not_active Application Discontinuation
- 1992-08-28 LT LTIP175A patent/LT3164B/lt not_active IP Right Cessation
-
1993
- 1993-12-16 FI FI935658A patent/FI935658A7/fi not_active Application Discontinuation
- 1993-12-17 HU HU9303653A patent/HUT67325A/hu active IP Right Revival
- 1993-12-17 BG BG98306A patent/BG98306A/bg unknown
- 1993-12-17 NO NO934688A patent/NO934688L/no unknown
-
1995
- 1995-09-27 IL IL11543995A patent/IL115439A0/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| NO934688D0 (no) | 1993-12-17 |
| LV10093B (en) | 1995-02-20 |
| KR940701386A (ko) | 1994-05-28 |
| NO934688L (no) | 1993-12-17 |
| MX9203000A (es) | 1993-02-01 |
| LTIP175A (lt) | 1994-08-25 |
| BG98306A (bg) | 1994-08-30 |
| HUT67325A (en) | 1995-03-28 |
| IL102216A (en) | 1996-06-18 |
| CZ280293A3 (en) | 1994-05-18 |
| WO1992022537A1 (en) | 1992-12-23 |
| IL102216A0 (en) | 1993-01-14 |
| GB9125924D0 (en) | 1992-02-05 |
| LV10093A (lv) | 1994-05-10 |
| HU9303653D0 (en) | 1994-04-28 |
| FI935658A0 (fi) | 1993-12-16 |
| SK144393A3 (en) | 1994-11-09 |
| CN1068819A (zh) | 1993-02-10 |
| HRP920170A2 (en) | 1994-08-31 |
| NZ243139A (en) | 1994-08-26 |
| IL115439A0 (en) | 1995-12-31 |
| FI935658A7 (fi) | 1993-12-16 |
| TW206217B (cs) | 1993-05-21 |
| PT100604A (pt) | 1993-10-29 |
| AU665002B2 (en) | 1995-12-14 |
| EP0589975A1 (en) | 1994-04-06 |
| CA2111469A1 (en) | 1992-12-23 |
| JPH06508119A (ja) | 1994-09-14 |
| AU1978392A (en) | 1993-01-12 |
| US5559141A (en) | 1996-09-24 |
| LT3164B (en) | 1995-02-27 |
| IE921963A1 (en) | 1992-12-30 |
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