RU2000122441A - NEW CYTOTOXIC MACROLIDES CONTAINING TRIS (OXAZOL) - Google Patents
NEW CYTOTOXIC MACROLIDES CONTAINING TRIS (OXAZOL)Info
- Publication number
- RU2000122441A RU2000122441A RU2000122441/04A RU2000122441A RU2000122441A RU 2000122441 A RU2000122441 A RU 2000122441A RU 2000122441/04 A RU2000122441/04 A RU 2000122441/04A RU 2000122441 A RU2000122441 A RU 2000122441A RU 2000122441 A RU2000122441 A RU 2000122441A
- Authority
- RU
- Russia
- Prior art keywords
- compound
- lower alkyl
- formula
- paragraph
- hydrogen
- Prior art date
Links
- 229940041033 Macrolides Drugs 0.000 title 1
- 239000007983 Tris buffer Substances 0.000 title 1
- 230000001472 cytotoxic Effects 0.000 title 1
- 231100000433 cytotoxic Toxicity 0.000 title 1
- 239000003120 macrolide antibiotic agent Substances 0.000 title 1
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 101710024506 TH2 Proteins 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000001589 carboacyl group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- MYMOFIZGZYHOMD-UHFFFAOYSA-N oxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- XYKNXOJYKRVXBX-LBCSWZFUSA-N Kabiramide C Chemical compound N=1C2=COC=1C(N=1)=COC=1\C=C\C[C@H](OC)[C@@H](C)[C@@H](C[C@@H](OC)[C@H](C)CCC(=O)[C@H](C)[C@@H](OC)[C@H](C)\C=C\N(C)CO)OC(=O)C[C@H](O[C@@H](N)O)C[C@@H](C)C[C@H](O)[C@@H](C)[C@H](OC)C1=COC2=N1 XYKNXOJYKRVXBX-LBCSWZFUSA-N 0.000 claims 1
- 230000000259 anti-tumor Effects 0.000 claims 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000004432 carbon atoms Chemical group C* 0.000 claims 1
- 238000007385 chemical modification Methods 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- SVDMAXBQMZIUPX-QSPXEARGSA-N kabiramide B Chemical compound N=1C2=COC=1C(N=1)=COC=1\C=C\C[C@H](O)[C@@H](C)[C@H](C[C@H](OC)[C@@H](C)CCC(=O)[C@H](C)[C@H](OC)[C@H](C)\C=C\N(C)C=O)OC(=O)C[C@@H](OC(N)=O)C[C@H](C)C[C@H](O)[C@H](C)[C@@H](OC)C1=COC2=N1 SVDMAXBQMZIUPX-QSPXEARGSA-N 0.000 claims 1
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
Claims (1)
в которой Х представляет низший алкил; R1 и R2 представляют водород или низший алкил;
R3а представляет водород и R3b представляет
или
или R3a и R3b вместе представляют кислород; R4 представляет водород, низший алкокси или низший алкил; R5 представляет водород, карбамоил или низший алканоил; R6a представляет водород, a R6b представляет гидроксил, либо R6a и R6b вместе представляют кислород; R7 представляет водород, низший алкил или гидроксиметил; R8 представляет низший алкокси или низший алкил; Y1 представляет водород или метил, и Y2 представляет водород, или Y1 и Y2 вместе представляют двойную связь, причем в определениях групп формулы (I) низший алкил и низший алкильный фрагмент низшего алканоила или низшего алкоксил означает прямолинейную или разветвленную алкильную группу, имеющую 1-6 атомов углерода, такую, как метил, этил, пропил, изопропил, бутил, изобутил, втор. -бутил, трет. -бутил, пентил, неопентил и гексил.1. The compound having the formula I:
in which X represents lower alkyl; R 1 and R 2 are hydrogen or lower alkyl;
R 3A represents hydrogen and R 3b represents
or
or R 3a and R 3b together represent oxygen; R 4 represents hydrogen, lower alkoxy or lower alkyl; R 5 is hydrogen, carbamoyl or lower alkanoyl; R 6a represents hydrogen, and R 6b represents hydroxyl, or R 6a and R 6b together represent oxygen; R 7 is hydrogen, lower alkyl or hydroxymethyl; R 8 is lower alkoxy or lower alkyl; Y 1 represents hydrogen or methyl, and Y 2 represents hydrogen, or Y 1 and Y 2 together represent a double bond, and in the definitions of groups of formula (I), lower alkyl and lower alkyl fragment of lower alkanoyl or lower alkoxy means straight or branched alkyl group, having 1-6 carbon atoms, such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec. -butyl, tert. -butyl, pentyl, neopentyl and hexyl.
3. Соединение ТН-2 по п. 1, имеющее следующую формулу:
4. Способ лечения млекопитающих, пораженных злокачественной опухолью, чувствительной к соединению формулы (I) по п. 1, включающий введение пораженному индивидууму терапевтически эффективного количества указанного соединения или его фармацевтической композиции.2. Connection ON-1 under item 1, having the following formula:
3. The compound TH-2 according to claim 1, having the following formula:
4. A method of treating a mammal affected by a malignant tumor sensitive to the compound of formula (I) of claim 1, comprising administering to the affected individual a therapeutically effective amount of said compound or a pharmaceutical composition thereof.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB9801741.1 | 1998-01-27 | ||
| GBGB9801741.1A GB9801741D0 (en) | 1998-01-27 | 1998-01-27 | New cytotoxic tris (oxazole)-containing macrolides |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2000122441A true RU2000122441A (en) | 2002-07-20 |
| RU2217433C2 RU2217433C2 (en) | 2003-11-27 |
Family
ID=10825984
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2000122441/04A RU2217433C2 (en) | 1998-01-27 | 1999-01-27 | New cytotoxic macrolides comprising tris(oxazol), method for their preparing, pharmaceutical composition based on thereof and methods for treatment |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US6391900B1 (en) |
| EP (1) | EP1051420B1 (en) |
| JP (1) | JP4511027B2 (en) |
| KR (1) | KR20010034413A (en) |
| CN (1) | CN1131869C (en) |
| AT (1) | ATE229024T1 (en) |
| AU (1) | AU760184B2 (en) |
| BR (1) | BR9907748A (en) |
| CA (1) | CA2319032C (en) |
| CZ (1) | CZ291931B6 (en) |
| DE (1) | DE69904294T2 (en) |
| DK (1) | DK1051420T3 (en) |
| ES (1) | ES2186324T3 (en) |
| GB (1) | GB9801741D0 (en) |
| HU (1) | HUP0101321A3 (en) |
| IL (1) | IL137545A0 (en) |
| MX (1) | MXPA00007381A (en) |
| PL (1) | PL342040A1 (en) |
| PT (1) | PT1051420E (en) |
| RU (1) | RU2217433C2 (en) |
| WO (1) | WO1999037653A1 (en) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100471727B1 (en) * | 2002-10-14 | 2005-02-21 | 학교법인 포항공과대학교 | Macrocyclic compounds containing isoxazoline ring and fluorine and method for preparing same |
| CN100360515C (en) * | 2004-04-09 | 2008-01-09 | 中国科学院上海药物研究所 | Lingshui alcohol with anti-cancer activity, its preparation and use |
| KR20110043653A (en) * | 2008-07-03 | 2011-04-27 | 파르마 마르 에스.에이. | Antitumoral macrolides |
| JOP20190254A1 (en) | 2017-04-27 | 2019-10-27 | Pharma Mar Sa | Antitumoral compounds |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6256493A (en) * | 1985-09-06 | 1987-03-12 | Yamanouchi Pharmaceut Co Ltd | Kabiramide |
| EP0729950A4 (en) * | 1994-09-13 | 2001-02-07 | Kyowa Hakko Kogyo Kk | Anti-hiv drug |
-
1998
- 1998-01-27 GB GBGB9801741.1A patent/GB9801741D0/en not_active Ceased
-
1999
- 1999-01-27 CN CN998045632A patent/CN1131869C/en not_active Expired - Fee Related
- 1999-01-27 JP JP2000528574A patent/JP4511027B2/en not_active Expired - Fee Related
- 1999-01-27 DE DE69904294T patent/DE69904294T2/en not_active Expired - Lifetime
- 1999-01-27 US US09/601,146 patent/US6391900B1/en not_active Expired - Fee Related
- 1999-01-27 AU AU24319/99A patent/AU760184B2/en not_active Ceased
- 1999-01-27 WO PCT/GB1999/000277 patent/WO1999037653A1/en not_active Application Discontinuation
- 1999-01-27 MX MXPA00007381A patent/MXPA00007381A/en unknown
- 1999-01-27 RU RU2000122441/04A patent/RU2217433C2/en not_active IP Right Cessation
- 1999-01-27 CZ CZ20002754A patent/CZ291931B6/en not_active IP Right Cessation
- 1999-01-27 PT PT99903797T patent/PT1051420E/en unknown
- 1999-01-27 ES ES99903797T patent/ES2186324T3/en not_active Expired - Lifetime
- 1999-01-27 HU HU0101321A patent/HUP0101321A3/en unknown
- 1999-01-27 DK DK99903797T patent/DK1051420T3/en active
- 1999-01-27 AT AT99903797T patent/ATE229024T1/en not_active IP Right Cessation
- 1999-01-27 BR BR9907748-5A patent/BR9907748A/en not_active IP Right Cessation
- 1999-01-27 KR KR1020007008182A patent/KR20010034413A/en not_active Application Discontinuation
- 1999-01-27 PL PL99342040A patent/PL342040A1/en unknown
- 1999-01-27 EP EP99903797A patent/EP1051420B1/en not_active Expired - Lifetime
- 1999-01-27 IL IL13754599A patent/IL137545A0/en unknown
- 1999-01-27 CA CA002319032A patent/CA2319032C/en not_active Expired - Fee Related
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