EA199800395A1 - Производные 2-хинолона, ингибирующие фарнезилтрансферазу - Google Patents
Производные 2-хинолона, ингибирующие фарнезилтрансферазуInfo
- Publication number
- EA199800395A1 EA199800395A1 EA199800395A EA199800395A EA199800395A1 EA 199800395 A1 EA199800395 A1 EA 199800395A1 EA 199800395 A EA199800395 A EA 199800395A EA 199800395 A EA199800395 A EA 199800395A EA 199800395 A1 EA199800395 A1 EA 199800395A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- 6alkyl
- 6alkyloxy
- alkyl
- amino
- hydroxy
- Prior art date
Links
- 102000007317 Farnesyltranstransferase Human genes 0.000 title abstract 2
- 108010007508 Farnesyltranstransferase Proteins 0.000 title abstract 2
- 230000002401 inhibitory effect Effects 0.000 title abstract 2
- LISFMEBWQUVKPJ-UHFFFAOYSA-N quinolin-2-ol Chemical class C1=CC=C2NC(=O)C=CC2=C1 LISFMEBWQUVKPJ-UHFFFAOYSA-N 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 12
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 150000002431 hydrogen Chemical class 0.000 abstract 5
- -1 C1-6alkyloxycarbonyl Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 abstract 1
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004966 cyanoalkyl group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Chemical group 0.000 abstract 1
- 239000011593 sulfur Chemical group 0.000 abstract 1
- 125000004951 trihalomethoxy group Chemical group 0.000 abstract 1
- 125000004953 trihalomethyl group Chemical group 0.000 abstract 1
Classifications
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
-
- 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
-
- 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
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Abstract
Настоящее изобретение относится к соединениям формулы (I)их стереохимически изомерным формам и фармацевтически приемлемым солям присоединения кислот или оснований, в которых пунктирная линия обозначает необязательную связь; X представляет кислород или серу; Rпредставляет водород, Cалкил, Ar, ArCалкил, хинолинил-Cалкил, пиридил-Cалкил, гидрокси-Cалкил, Cалкилокси-Cалкил, моно- или ди(Cалкил)амино-Cалкил, амино-Cалкил, или радикал формулы -Alk(=O)-R, -Alk-S(O)-Rили –Alk-S(O)-R; Rи R, каждый независимо представляет водород, гидрокси, галоген, циано, Cалкил, Cалкилокси, гидрокси-Cалкилокси, Cалкилокси-Cалкилокси, амино-Cалкилокси, моно- или ди(Cалкил)амино-Cалкилокси, Ar, ArCалкил, Arокси, ArCалкилокси, гидроксикарбонил, Cалкилоксикарбонил, тригалогенметил, тригалогенметокси, Cалкенил; или, находясь в смежных положениях, Rи R, взятые вместе, могут образовывать двухвалентный радикал; Rи R, каждый независимо представляет водород, Ar, Cалкил, Cалкилокси-Cалкил, Cалкилокси, Cалкилтио, амино, гидроксикарбонил, Cалкилоксикарбонил, CалкилS(О)Cалкил или CалкилS(O)Cалкил; Rи R, каждый независимо представляет водород, галоген, циано, Cалкил, CCалкилоксикарбонил, Cалкилкарбонил Cалкил, циано-Cалкил, Cалкилоксикаробонил Cалкил, гидроксикарбонил-Cалкил, гидрокси-Cалкил, амино-Cалкил, моно- или ди(Cалкил)амино-Cалкил, галоген-Cалкил, Cалкилокси-Cалкил, аминокарбонил-Cалкил, Ar, ArCалкилокси-Cалкил, Cалкилтио-Cалкил; Rпредставляет водород, Cалкил или галоген; Rпредставляет водород или Cалкил; которые обладают ингибирующей фарнезилтрансферазу активностью; к их получению, к содержащим их композициям и к их применению в качестве лекарственного средства.Международная заявка была опубликована вместе с отчетом о международном поиске.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP95202945 | 1995-10-31 | ||
PCT/EP1996/004661 WO1997016443A1 (en) | 1995-10-31 | 1996-10-25 | Farnesyl transferase inhibiting 2-quinolone derivatives |
Publications (2)
Publication Number | Publication Date |
---|---|
EA199800395A1 true EA199800395A1 (ru) | 1998-10-29 |
EA000719B1 EA000719B1 (ru) | 2000-02-28 |
Family
ID=8220785
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA199800395A EA000719B1 (ru) | 1995-10-31 | 1996-10-25 | Производные 2-хинолона, ингибирующие фарнезилтрансферазу |
Country Status (29)
Country | Link |
---|---|
US (1) | US5968952A (ru) |
EP (2) | EP1106610B1 (ru) |
JP (1) | JP4257869B2 (ru) |
KR (1) | KR100417620B1 (ru) |
CN (1) | CN1101391C (ru) |
AR (1) | AR004699A1 (ru) |
AT (2) | ATE212627T1 (ru) |
AU (1) | AU712435B2 (ru) |
CA (1) | CA2231143C (ru) |
CY (1) | CY2287B1 (ru) |
CZ (1) | CZ290954B6 (ru) |
DE (2) | DE69618999T2 (ru) |
DK (1) | DK1019395T3 (ru) |
EA (1) | EA000719B1 (ru) |
ES (2) | ES2171736T3 (ru) |
HK (2) | HK1027576A1 (ru) |
HU (1) | HU224032B1 (ru) |
IL (1) | IL123567A (ru) |
MY (1) | MY116577A (ru) |
NO (1) | NO314037B1 (ru) |
NZ (1) | NZ321576A (ru) |
PL (1) | PL184168B1 (ru) |
PT (1) | PT1019395E (ru) |
SI (1) | SI1019395T1 (ru) |
SK (1) | SK282642B6 (ru) |
TR (1) | TR199800720T2 (ru) |
TW (1) | TW349948B (ru) |
WO (1) | WO1997016443A1 (ru) |
ZA (1) | ZA969087B (ru) |
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US3900501A (en) * | 1970-12-23 | 1975-08-19 | Hoffmann La Roche | Benzophenone intermediates for 7-lower alkanoyl benzodiazepines |
IL65709A (en) * | 1981-05-18 | 1986-01-31 | Chevron Res | Electroactive polymers |
JPS63275548A (ja) * | 1987-05-02 | 1988-11-14 | Res Inst For Prod Dev | o−アミノベンゾイル化合物の製造方法 |
CA2002864C (en) * | 1988-11-29 | 1999-11-16 | Eddy J. E. Freyne | (1h-azol-1-ylmethyl) substituted quinoline, quinazoline or quinoxaline derivatives |
CA2002859C (en) * | 1988-11-29 | 1998-12-29 | Jean P. F. Van Wauwe | Method of treating epithelial disorders |
EP0574992A1 (en) * | 1992-06-17 | 1993-12-22 | Glaxo Group Limited | 5-(1,2,4-Triazol-1-ylmethyl)-3H-isobenzofuran-1-one derivatives, their preparation and use as aromatase inhibitors |
DE69511449T2 (de) * | 1994-04-15 | 2000-03-23 | Takeda Chemical Industries Ltd | Octahydro-2-Naphthalincarbonsäure-Derivate, ihre Herstellung und Verwendung |
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