JP2010519318A5 - - Google Patents
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- Publication number
- JP2010519318A5 JP2010519318A5 JP2009551061A JP2009551061A JP2010519318A5 JP 2010519318 A5 JP2010519318 A5 JP 2010519318A5 JP 2009551061 A JP2009551061 A JP 2009551061A JP 2009551061 A JP2009551061 A JP 2009551061A JP 2010519318 A5 JP2010519318 A5 JP 2010519318A5
- Authority
- JP
- Japan
- Prior art keywords
- macrocycle
- peptidomimetic macrocycle
- peptidomimetic
- methyl
- alkyl
- 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
- 150000002678 macrocyclic compounds Chemical class 0.000 claims 52
- 239000000816 peptidomimetic Substances 0.000 claims 49
- 238000000034 method Methods 0.000 claims 37
- 125000000217 alkyl group Chemical group 0.000 claims 15
- 239000003153 chemical reaction reagent Substances 0.000 claims 14
- 125000005647 linker group Chemical group 0.000 claims 10
- 125000003342 alkenyl group Chemical group 0.000 claims 9
- 125000000304 alkynyl group Chemical group 0.000 claims 9
- 125000003710 aryl alkyl group Chemical group 0.000 claims 9
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 9
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 9
- 150000001413 amino acids Chemical class 0.000 claims 8
- 239000011203 carbon fibre reinforced carbon Substances 0.000 claims 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 238000005710 macrocyclization reaction Methods 0.000 claims 8
- 108090000765 processed proteins & peptides Proteins 0.000 claims 8
- 229920001184 polypeptide Polymers 0.000 claims 7
- 239000002243 precursor Substances 0.000 claims 7
- 102000004196 processed proteins & peptides Human genes 0.000 claims 7
- 125000004404 heteroalkyl group Chemical group 0.000 claims 6
- 239000002904 solvent Substances 0.000 claims 5
- 125000001475 halogen functional group Chemical group 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 150000001345 alkine derivatives Chemical class 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- IVRMZWNICZWHMI-UHFFFAOYSA-N azide group Chemical group [N-]=[N+]=[N-] IVRMZWNICZWHMI-UHFFFAOYSA-N 0.000 claims 3
- -1 macrocycle compound Chemical class 0.000 claims 3
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 claims 2
- 125000004450 alkenylene group Chemical group 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 125000004419 alkynylene group Chemical group 0.000 claims 2
- 239000007864 aqueous solution Substances 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 230000015572 biosynthetic process Effects 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 125000002993 cycloalkylene group Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000004474 heteroalkylene group Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims 2
- 229920002521 macromolecule Polymers 0.000 claims 2
- 239000003960 organic solvent Substances 0.000 claims 2
- 238000010189 synthetic method Methods 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- JMHBRCHHTBVRNO-SSDOTTSWSA-N (2r)-2-amino-2-methylhex-5-ynoic acid Chemical compound OC(=O)[C@@](N)(C)CCC#C JMHBRCHHTBVRNO-SSDOTTSWSA-N 0.000 claims 1
- FSBNDYYRTZBHAN-ZCFIWIBFSA-N (2r)-2-amino-2-methylpent-4-ynoic acid Chemical compound OC(=O)[C@@](N)(C)CC#C FSBNDYYRTZBHAN-ZCFIWIBFSA-N 0.000 claims 1
- DGYHPLMPMRKMPD-SCSAIBSYSA-N (2r)-2-azaniumylpent-4-ynoate Chemical compound OC(=O)[C@H](N)CC#C DGYHPLMPMRKMPD-SCSAIBSYSA-N 0.000 claims 1
- JMHBRCHHTBVRNO-ZETCQYMHSA-N (2s)-2-amino-2-methylhex-5-ynoic acid Chemical compound OC(=O)[C@](N)(C)CCC#C JMHBRCHHTBVRNO-ZETCQYMHSA-N 0.000 claims 1
- WTFKXZRWELKUFM-VIFPVBQESA-N (2s)-2-amino-2-methyloct-7-ynoic acid Chemical compound OC(=O)[C@](N)(C)CCCCC#C WTFKXZRWELKUFM-VIFPVBQESA-N 0.000 claims 1
- FSBNDYYRTZBHAN-LURJTMIESA-N (2s)-2-amino-2-methylpent-4-ynoic acid Chemical compound OC(=O)[C@](N)(C)CC#C FSBNDYYRTZBHAN-LURJTMIESA-N 0.000 claims 1
- 239000004215 Carbon black (E152) Substances 0.000 claims 1
- DGYHPLMPMRKMPD-UHFFFAOYSA-N L-propargyl glycine Natural products OC(=O)C(N)CC#C DGYHPLMPMRKMPD-UHFFFAOYSA-N 0.000 claims 1
- DGYHPLMPMRKMPD-BYPYZUCNSA-N L-propargylglycine Chemical group OC(=O)[C@@H](N)CC#C DGYHPLMPMRKMPD-BYPYZUCNSA-N 0.000 claims 1
- KJTLSVCANCCWHF-UHFFFAOYSA-N Ruthenium Chemical compound [Ru] KJTLSVCANCCWHF-UHFFFAOYSA-N 0.000 claims 1
- DKGAVHZHDRPRBM-UHFFFAOYSA-N Tert-Butanol Chemical compound CC(C)(C)O DKGAVHZHDRPRBM-UHFFFAOYSA-N 0.000 claims 1
- HUZCMINOFBKDBN-NQPNHJOESA-N [(5r)-1,5-diamino-5-carboxyhexyl]-diazonioazanide Chemical compound OC(=O)[C@@](N)(C)CCCC(N)N=[N+]=[N-] HUZCMINOFBKDBN-NQPNHJOESA-N 0.000 claims 1
- QFLNJOIJUNDRFH-CNZKWPKMSA-N [(5r)-1,5-diamino-5-carboxypentyl]-diazonioazanide Chemical compound [N-]=[N+]=NC(N)CCC[C@@H](N)C(O)=O QFLNJOIJUNDRFH-CNZKWPKMSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000003125 aqueous solvent Substances 0.000 claims 1
- 125000000732 arylene group Chemical group 0.000 claims 1
- 230000004071 biological effect Effects 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000005549 heteroarylene group Chemical group 0.000 claims 1
- 229930195733 hydrocarbon Natural products 0.000 claims 1
- 150000002430 hydrocarbons Chemical class 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 229960003104 ornithine Drugs 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 230000017854 proteolysis Effects 0.000 claims 1
- 239000003586 protic polar solvent Substances 0.000 claims 1
- 229910052707 ruthenium Inorganic materials 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 239000000243 solution Substances 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 238000003786 synthesis reaction Methods 0.000 claims 1
- 230000002194 synthesizing effect Effects 0.000 claims 1
- 0 CC(*)=CCN=NN Chemical compound CC(*)=CCN=NN 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US90307307P | 2007-02-23 | 2007-02-23 | |
| US60/903,073 | 2007-02-23 | ||
| PCT/US2008/054922 WO2008104000A2 (en) | 2007-02-23 | 2008-02-25 | Triazole macrocycle systems |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012063887A Division JP5657594B6 (ja) | 2007-02-23 | 2012-03-21 | トリアゾール大環状系 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010519318A JP2010519318A (ja) | 2010-06-03 |
| JP2010519318A5 true JP2010519318A5 (https=) | 2011-04-14 |
| JP4997293B2 JP4997293B2 (ja) | 2012-08-08 |
Family
ID=39710801
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009551061A Expired - Fee Related JP4997293B2 (ja) | 2007-02-23 | 2008-02-25 | トリアゾール大環状系 |
| JP2014238716A Expired - Fee Related JP6046686B2 (ja) | 2007-02-23 | 2014-11-26 | トリアゾール大環状系 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014238716A Expired - Fee Related JP6046686B2 (ja) | 2007-02-23 | 2014-11-26 | トリアゾール大環状系 |
Country Status (10)
| Country | Link |
|---|---|
| US (6) | US7981999B2 (https=) |
| EP (4) | EP3301108A1 (https=) |
| JP (2) | JP4997293B2 (https=) |
| CN (3) | CN101663044B (https=) |
| AU (1) | AU2008218116B2 (https=) |
| BR (1) | BRPI0807578A2 (https=) |
| CA (1) | CA2678941C (https=) |
| ES (3) | ES2649941T3 (https=) |
| IL (2) | IL200532A (https=) |
| WO (1) | WO2008104000A2 (https=) |
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