JP2006502128A5 - - Google Patents
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- Publication number
- JP2006502128A5 JP2006502128A5 JP2004525241A JP2004525241A JP2006502128A5 JP 2006502128 A5 JP2006502128 A5 JP 2006502128A5 JP 2004525241 A JP2004525241 A JP 2004525241A JP 2004525241 A JP2004525241 A JP 2004525241A JP 2006502128 A5 JP2006502128 A5 JP 2006502128A5
- Authority
- JP
- Japan
- Prior art keywords
- hydrogen
- alkyl
- amino
- cycloalkyl
- group
- Prior art date
- Legal status (The legal status 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 status listed.)
- Withdrawn
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- 150000001875 compounds Chemical class 0.000 claims description 23
- -1 nitro, cyano, amino Chemical group 0.000 claims description 22
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 37
- 239000001257 hydrogen Substances 0.000 claims 37
- 125000001424 substituent group Chemical group 0.000 claims 25
- 125000000217 alkyl group Chemical group 0.000 claims 21
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 18
- 150000002431 hydrogen Chemical class 0.000 claims 18
- 125000000753 cycloalkyl group Chemical group 0.000 claims 13
- 125000004663 dialkyl amino group Chemical group 0.000 claims 13
- 125000003282 alkyl amino group Chemical group 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 12
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 125000000623 heterocyclic group Chemical group 0.000 claims 12
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 9
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 9
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 8
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 8
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 7
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 7
- 125000004473 dialkylaminocarbonyl group Chemical group 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 7
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 5
- 208000035143 Bacterial infection Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 2
- 125000003275 alpha amino acid group Chemical group 0.000 claims 2
- 125000000539 amino acid group Chemical group 0.000 claims 2
- 150000001413 amino acids Chemical class 0.000 claims 2
- 125000003277 amino group Chemical group 0.000 claims 2
- 125000005129 aryl carbonyl group Chemical group 0.000 claims 2
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 2
- 208000022362 bacterial infectious disease Diseases 0.000 claims 2
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 claims 2
- 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 claims 2
- 125000005223 heteroarylcarbonyl group Chemical group 0.000 claims 2
- 125000005143 heteroarylsulfonyl group Chemical group 0.000 claims 2
- 125000006517 heterocyclyl carbonyl group Chemical group 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 claims 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 230000000844 anti-bacterial effect Effects 0.000 claims 1
- 125000005100 aryl amino carbonyl group Chemical group 0.000 claims 1
- 125000001769 aryl amino group Chemical group 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([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
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 6
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 4
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 3
- 238000002330 electrospray ionisation mass spectrometry Methods 0.000 description 3
- 238000004895 liquid chromatography mass spectrometry Methods 0.000 description 3
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 2
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 229910000041 hydrogen chloride Inorganic materials 0.000 description 1
- IXCSERBJSXMMFS-UHFFFAOYSA-N hydrogen chloride Substances Cl.Cl IXCSERBJSXMMFS-UHFFFAOYSA-N 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- WGYKZJWCGVVSQN-UHFFFAOYSA-N propylamine Chemical group CCCN WGYKZJWCGVVSQN-UHFFFAOYSA-N 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- DYHSDKLCOJIUFX-UHFFFAOYSA-N tert-butoxycarbonyl anhydride Chemical compound CC(C)(C)OC(=O)OC(=O)OC(C)(C)C DYHSDKLCOJIUFX-UHFFFAOYSA-N 0.000 description 1
- XTLUOZCORWVQAR-UHFFFAOYSA-N tert-butyl 2-hydroxyethyl carbonate Chemical compound CC(C)(C)OC(=O)OCCO XTLUOZCORWVQAR-UHFFFAOYSA-N 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10234422A DE10234422A1 (de) | 2002-07-29 | 2002-07-29 | Antibakterielle Ester-Makrozyklen |
| PCT/EP2003/007824 WO2004012816A1 (de) | 2002-07-29 | 2003-07-18 | Antibakterielle ester-makrozyklen |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006502128A JP2006502128A (ja) | 2006-01-19 |
| JP2006502128A5 true JP2006502128A5 (enExample) | 2006-08-31 |
Family
ID=30128472
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004525241A Withdrawn JP2006502128A (ja) | 2002-07-29 | 2003-07-18 | 抗菌性エステル−マクロサイクル |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20060258571A1 (enExample) |
| EP (1) | EP1526896A1 (enExample) |
| JP (1) | JP2006502128A (enExample) |
| AU (1) | AU2003246716A1 (enExample) |
| CA (1) | CA2495479A1 (enExample) |
| DE (1) | DE10234422A1 (enExample) |
| WO (1) | WO2004012816A1 (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10226921A1 (de) * | 2002-06-17 | 2003-12-24 | Bayer Ag | Antibakterielle Amid-Makrozyklen |
| JP4928261B2 (ja) | 2003-06-18 | 2012-05-09 | トランザイム・ファーマ・インコーポレイテッド | モチリン受容体の大環状拮抗薬 |
| DE10358824A1 (de) | 2003-12-16 | 2005-07-21 | Bayer Healthcare Ag | Antibakterielle Makrozyklen mit substituiertem Biphenyl |
| DE102004025731A1 (de) * | 2004-05-26 | 2005-12-15 | Bayer Healthcare Ag | Antibakterielle Amid-Makrozyklen III |
| DE102005014240A1 (de) * | 2004-09-24 | 2006-03-30 | Bayer Healthcare Ag | Antibakterielle Amid-Makrozyklen IV |
| DE102005014245A1 (de) * | 2005-03-30 | 2006-10-05 | Aicuris Gmbh & Co. Kg | Antibakterielle Amid-Makrozyklen V |
| DE102005014247A1 (de) * | 2005-03-30 | 2006-10-05 | Aicuris Gmbh & Co. Kg | Antibakterielle Amid-Makrozyklen VI |
| DE102005032781A1 (de) * | 2005-07-14 | 2007-01-18 | Aicuris Gmbh & Co. Kg | Antibakterielle Amid-Markozyklen VII |
| CN101351451B (zh) * | 2005-12-29 | 2013-02-20 | 莱西肯医药有限公司 | 多环氨基酸衍生物及其使用方法 |
| RU2729609C2 (ru) | 2015-10-27 | 2020-08-11 | Ф. Хоффманн-Ля Рош Аг | Пептидные макроциклы против acinetobacter baumannii |
| US11505573B2 (en) | 2018-03-28 | 2022-11-22 | Hoffmann-La Roche Inc. | Peptide macrocycles against Acinetobacter baumannii |
| US11819532B2 (en) | 2018-04-23 | 2023-11-21 | Hoffmann-La Roche Inc. | Peptide macrocycles against Acinetobacter baumannii |
| WO2019239880A1 (ja) * | 2018-06-15 | 2019-12-19 | 国立大学法人東京工業大学 | アミドの製造方法 |
| AU2019284745B2 (en) * | 2018-06-15 | 2023-05-11 | Yokogawa Electric Corporation | Method for producing amide |
| JPWO2020137545A1 (ja) * | 2018-12-25 | 2021-11-04 | 国立大学法人東京工業大学 | アミドの製造方法 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2801591B1 (fr) * | 1999-11-30 | 2002-03-01 | Aventis Pharma Sa | Derives macrocycliques de l'acide hydroxamique, leur preparation et les compositions qui les contiennent |
| DE10358824A1 (de) * | 2003-12-16 | 2005-07-21 | Bayer Healthcare Ag | Antibakterielle Makrozyklen mit substituiertem Biphenyl |
-
2002
- 2002-07-29 DE DE10234422A patent/DE10234422A1/de not_active Withdrawn
-
2003
- 2003-07-18 AU AU2003246716A patent/AU2003246716A1/en not_active Abandoned
- 2003-07-18 CA CA002495479A patent/CA2495479A1/en not_active Abandoned
- 2003-07-18 JP JP2004525241A patent/JP2006502128A/ja not_active Withdrawn
- 2003-07-18 EP EP03766214A patent/EP1526896A1/de not_active Withdrawn
- 2003-07-18 US US10/522,667 patent/US20060258571A1/en not_active Abandoned
- 2003-07-18 WO PCT/EP2003/007824 patent/WO2004012816A1/de not_active Ceased
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