JP2006511446A5 - - Google Patents
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- Publication number
- JP2006511446A5 JP2006511446A5 JP2004513311A JP2004513311A JP2006511446A5 JP 2006511446 A5 JP2006511446 A5 JP 2006511446A5 JP 2004513311 A JP2004513311 A JP 2004513311A JP 2004513311 A JP2004513311 A JP 2004513311A JP 2006511446 A5 JP2006511446 A5 JP 2006511446A5
- Authority
- JP
- Japan
- Prior art keywords
- hydrogen
- alkyl
- cycloalkyl
- amino
- 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.)
- Granted
Links
- 229910052739 hydrogen Inorganic materials 0.000 claims 48
- 239000001257 hydrogen Substances 0.000 claims 48
- 125000001424 substituent group Chemical group 0.000 claims 32
- 125000000217 alkyl group Chemical group 0.000 claims 25
- 150000002431 hydrogen Chemical class 0.000 claims 24
- -1 nitro, cyano, amino Chemical group 0.000 claims 24
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 23
- 150000001875 compounds Chemical class 0.000 claims 23
- 125000000623 heterocyclic group Chemical group 0.000 claims 19
- 125000000753 cycloalkyl group Chemical group 0.000 claims 18
- 125000003118 aryl group Chemical group 0.000 claims 17
- 125000001072 heteroaryl group Chemical group 0.000 claims 16
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 14
- 125000003282 alkyl amino group Chemical group 0.000 claims 12
- 125000004663 dialkyl amino group Chemical group 0.000 claims 11
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 11
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 9
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 9
- 125000004473 dialkylaminocarbonyl group Chemical group 0.000 claims 9
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 150000002367 halogens Chemical class 0.000 claims 9
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 9
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 8
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 7
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 150000001413 amino acids Chemical class 0.000 claims 4
- 208000035143 Bacterial infection Diseases 0.000 claims 3
- 125000000539 amino acid group Chemical group 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 3
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 2
- 150000001412 amines 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
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 229940079593 drug Drugs 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
- 238000000034 method Methods 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 1
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 claims 1
- 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
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 1
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims 1
- 125000004471 alkyl aminosulfonyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 1
- 230000000844 anti-bacterial effect Effects 0.000 claims 1
- 125000005100 aryl amino carbonyl group Chemical group 0.000 claims 1
- 125000005141 aryl amino sulfonyl group Chemical group 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 125000004472 dialkylaminosulfonyl group Chemical group 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
- 125000001188 haloalkyl group Chemical group 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
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10226921A DE10226921A1 (de) | 2002-06-17 | 2002-06-17 | Antibakterielle Amid-Makrozyklen |
| PCT/EP2003/006078 WO2003106480A1 (de) | 2002-06-17 | 2003-06-10 | Antibakterielle amid-makrozyklen |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006511446A JP2006511446A (ja) | 2006-04-06 |
| JP2006511446A5 true JP2006511446A5 (https=) | 2006-07-27 |
| JP4437078B2 JP4437078B2 (ja) | 2010-03-24 |
Family
ID=29594575
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004513311A Expired - Fee Related JP4437078B2 (ja) | 2002-06-17 | 2003-06-10 | 抗菌性アミドマクロサイクル |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US20070129288A1 (https=) |
| EP (1) | EP1515983B1 (https=) |
| JP (1) | JP4437078B2 (https=) |
| KR (1) | KR20050010060A (https=) |
| CN (1) | CN1326870C (https=) |
| AT (1) | ATE354585T1 (https=) |
| AU (1) | AU2003245928B2 (https=) |
| BR (1) | BR0311948A (https=) |
| CA (1) | CA2489454A1 (https=) |
| DE (2) | DE10226921A1 (https=) |
| EC (1) | ECSP045499A (https=) |
| ES (1) | ES2282643T3 (https=) |
| HR (1) | HRP20050043A2 (https=) |
| MA (1) | MA28613B1 (https=) |
| MX (1) | MXPA04012438A (https=) |
| NO (1) | NO20050210L (https=) |
| PL (1) | PL374554A1 (https=) |
| PT (1) | PT1515983E (https=) |
| RU (1) | RU2005100954A (https=) |
| WO (1) | WO2003106480A1 (https=) |
| ZA (1) | ZA200410006B (https=) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1633774T3 (da) | 2003-06-18 | 2010-05-25 | Tranzyme Pharma Inc | Makrocykliske motilinreceptorantagonister |
| WO2005033129A1 (de) * | 2003-10-01 | 2005-04-14 | Bayer Healthcare Ag | Antibakterielle amid-makrozyklen |
| DE10358824A1 (de) | 2003-12-16 | 2005-07-21 | Bayer Healthcare Ag | Antibakterielle Makrozyklen mit substituiertem Biphenyl |
| DE102004018405A1 (de) * | 2004-04-16 | 2005-11-03 | Bayer Healthcare Ag | Antibakterielle Amid-Makrozyklen II |
| 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 |
| DE102005014247A1 (de) * | 2005-03-30 | 2006-10-05 | Aicuris Gmbh & Co. Kg | Antibakterielle Amid-Makrozyklen VI |
| DE102005014245A1 (de) * | 2005-03-30 | 2006-10-05 | Aicuris Gmbh & Co. Kg | Antibakterielle Amid-Makrozyklen V |
| DE102005032781A1 (de) * | 2005-07-14 | 2007-01-18 | Aicuris Gmbh & Co. Kg | Antibakterielle Amid-Markozyklen VII |
| CA2635531C (en) | 2005-12-29 | 2014-06-17 | Lexicon Pharmaceutical Inc. | Multicyclic amino acid derivatives and methods of their use |
| EP2373597A2 (en) * | 2008-12-04 | 2011-10-12 | Bayer Pharma Aktiengesellschaft | Radioisotope-labeled lysine and ornithine derivatives, their use and processes for their preparation |
| US10501493B2 (en) | 2011-05-27 | 2019-12-10 | Rqx Pharmaceuticals, Inc. | Broad spectrum antibiotics |
| KR20150088292A (ko) * | 2012-11-21 | 2015-07-31 | 알큐엑스 파마슈티컬스, 인크. | 광범위한 마크로사이클릭 항생제 |
| JP5437525B1 (ja) * | 2012-12-28 | 2014-03-12 | 株式会社ナード研究所 | チロシン誘導体およびチロシン誘導体の製造方法 |
| WO2015179441A2 (en) | 2014-05-20 | 2015-11-26 | Rqx Pharmaceuticals, Inc. | Macrocyclic broad spectrum antibiotics |
| US10118890B2 (en) | 2014-10-10 | 2018-11-06 | The Research Foundation For The State University Of New York | Trifluoromethoxylation of arenes via intramolecular trifluoromethoxy group migration |
| AU2016347456B2 (en) | 2015-10-27 | 2018-12-13 | F. Hoffmann-La Roche Ag | Peptide macrocycles against acinetobacter baumannii |
| US11072635B2 (en) | 2015-11-20 | 2021-07-27 | Rqx Pharmaceuticals, Inc. | Macrocyclic broad spectrum antibiotics |
| EP3388444A1 (en) | 2017-04-10 | 2018-10-17 | F. Hoffmann-La Roche AG | Anti-bacterial peptide macrocycles and use thereof |
| 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 |
| JP7078807B2 (ja) | 2019-05-28 | 2022-05-31 | エフ．ホフマン－ラ ロシュ アーゲー | 大環状広域スペクトル抗生物質 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3452136A (en) * | 1968-04-17 | 1969-06-24 | American Cyanamid Co | Antibiotic af283 and production thereof |
| FR2720066B1 (fr) * | 1994-05-20 | 1996-06-28 | Rhone Poulenc Rorer Sa | Peptides antagonistes de la neurotensine. |
| DE10234422A1 (de) * | 2002-07-29 | 2004-02-12 | Bayer Ag | Antibakterielle Ester-Makrozyklen |
| WO2005033129A1 (de) * | 2003-10-01 | 2005-04-14 | Bayer Healthcare Ag | Antibakterielle amid-makrozyklen |
| DE10358824A1 (de) * | 2003-12-16 | 2005-07-21 | Bayer Healthcare Ag | Antibakterielle Makrozyklen mit substituiertem Biphenyl |
| DE102005014240A1 (de) * | 2004-09-24 | 2006-03-30 | Bayer Healthcare Ag | Antibakterielle Amid-Makrozyklen IV |
-
2002
- 2002-06-17 DE DE10226921A patent/DE10226921A1/de not_active Withdrawn
-
2003
- 2003-06-10 PT PT03738012T patent/PT1515983E/pt unknown
- 2003-06-10 BR BR0311948-3A patent/BR0311948A/pt not_active IP Right Cessation
- 2003-06-10 CA CA002489454A patent/CA2489454A1/en not_active Abandoned
- 2003-06-10 WO PCT/EP2003/006078 patent/WO2003106480A1/de not_active Ceased
- 2003-06-10 RU RU2005100954/04A patent/RU2005100954A/ru not_active Application Discontinuation
- 2003-06-10 DE DE50306587T patent/DE50306587D1/de not_active Expired - Lifetime
- 2003-06-10 CN CNB038192144A patent/CN1326870C/zh not_active Expired - Fee Related
- 2003-06-10 PL PL03374554A patent/PL374554A1/xx not_active IP Right Cessation
- 2003-06-10 KR KR10-2004-7020473A patent/KR20050010060A/ko not_active Abandoned
- 2003-06-10 AU AU2003245928A patent/AU2003245928B2/en not_active Ceased
- 2003-06-10 ES ES03738012T patent/ES2282643T3/es not_active Expired - Lifetime
- 2003-06-10 JP JP2004513311A patent/JP4437078B2/ja not_active Expired - Fee Related
- 2003-06-10 AT AT03738012T patent/ATE354585T1/de not_active IP Right Cessation
- 2003-06-10 MX MXPA04012438A patent/MXPA04012438A/es active IP Right Grant
- 2003-06-10 US US10/518,600 patent/US20070129288A1/en not_active Abandoned
- 2003-06-10 HR HR20050043A patent/HRP20050043A2/hr not_active Application Discontinuation
- 2003-06-10 EP EP03738012A patent/EP1515983B1/de not_active Expired - Lifetime
-
2004
- 2004-12-10 ZA ZA200410006A patent/ZA200410006B/xx unknown
- 2004-12-15 MA MA28006A patent/MA28613B1/fr unknown
- 2004-12-17 EC EC2004005499A patent/ECSP045499A/es unknown
-
2005
- 2005-01-13 NO NO20050210A patent/NO20050210L/no not_active Application Discontinuation
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