JP2014528958A5 - - Google Patents
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- JP2014528958A5 JP2014528958A5 JP2014533851A JP2014533851A JP2014528958A5 JP 2014528958 A5 JP2014528958 A5 JP 2014528958A5 JP 2014533851 A JP2014533851 A JP 2014533851A JP 2014533851 A JP2014533851 A JP 2014533851A JP 2014528958 A5 JP2014528958 A5 JP 2014528958A5
- Authority
- JP
- Japan
- Prior art keywords
- pro
- tyr
- cys
- trp
- lys
- 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
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- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims 38
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 18
- 125000003118 aryl group Chemical group 0.000 claims 16
- 239000012453 solvate Substances 0.000 claims 16
- 125000001072 heteroaryl group Chemical group 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 14
- 125000004432 carbon atom Chemical group C* 0.000 claims 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 13
- 125000005842 heteroatom Chemical group 0.000 claims 13
- 235000005311 Pandanus odoratissimus Nutrition 0.000 claims 12
- 240000002390 Pandanus odoratissimus Species 0.000 claims 12
- 125000003226 pyrazolyl group Chemical group 0.000 claims 12
- 201000010099 disease Diseases 0.000 claims 11
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 11
- 150000007649 L alpha amino acids Chemical class 0.000 claims 10
- KAFHLONDOVSENM-HNNXBMFYSA-N O-Benzyl-L-tyrosine Chemical compound C1=CC(C[C@H](N)C(O)=O)=CC=C1OCC1=CC=CC=C1 KAFHLONDOVSENM-HNNXBMFYSA-N 0.000 claims 6
- AYFVYJQAPQTCCC-UHFFFAOYSA-N THREONINE Chemical compound CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 239000000047 product Substances 0.000 claims 6
- 125000003373 pyrazinyl group Chemical group 0.000 claims 6
- QIVBCDIJIAJPQS-UHFFFAOYSA-N tryptophan Chemical compound C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 claims 6
- 150000007650 D alpha amino acids Chemical class 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 5
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims 4
- 125000003682 3-furyl group Chemical group O1C([H])=C([*])C([H])=C1[H] 0.000 claims 4
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Chemical compound CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims 4
- -1 aromatic Lα-amino acids Chemical class 0.000 claims 4
- 125000000524 functional group Chemical group 0.000 claims 4
- 230000001404 mediated effect Effects 0.000 claims 4
- 125000006239 protecting group Chemical group 0.000 claims 4
- RWCOTTLHDJWHRS-YUMQZZPRSA-N Pro-Pro Chemical compound OC(=O)[C@@H]1CCCN1C(=O)[C@H]1NCCC1 RWCOTTLHDJWHRS-YUMQZZPRSA-N 0.000 claims 3
- 150000001413 amino acids Chemical group 0.000 claims 3
- 125000005349 heteroarylcycloalkyl group Chemical group 0.000 claims 3
- 150000004677 hydrates Chemical class 0.000 claims 3
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 3
- 230000002062 proliferating effect Effects 0.000 claims 3
- 108010077112 prolyl-proline Proteins 0.000 claims 3
- 239000007787 solid Substances 0.000 claims 3
- 206010027654 Allergic conditions Diseases 0.000 claims 2
- ODKSFYDXXFIFQN-UHFFFAOYSA-N Arginine Chemical compound OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- XUJNEKJLAYXESH-UHFFFAOYSA-N Cysteine Chemical compound SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 2
- 201000004624 Dermatitis Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- 208000036110 Neuroinflammatory disease Diseases 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 206010035664 Pneumonia Diseases 0.000 claims 2
- 102000029797 Prion Human genes 0.000 claims 2
- 108091000054 Prion Proteins 0.000 claims 2
- 230000001154 acute effect Effects 0.000 claims 2
- 125000000539 amino acid group Chemical group 0.000 claims 2
- 125000004350 aryl cycloalkyl group Chemical group 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 230000008878 coupling Effects 0.000 claims 2
- 238000010168 coupling process Methods 0.000 claims 2
- 238000005859 coupling reaction Methods 0.000 claims 2
- 125000004367 cycloalkylaryl group Chemical group 0.000 claims 2
- 125000005215 cycloalkylheteroaryl group Chemical group 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 101150057222 fpr gene Proteins 0.000 claims 2
- 208000026278 immune system disease Diseases 0.000 claims 2
- 208000015181 infectious disease Diseases 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 230000003959 neuroinflammation Effects 0.000 claims 2
- 201000001119 neuropathy Diseases 0.000 claims 2
- 230000007823 neuropathy Effects 0.000 claims 2
- 210000000440 neutrophil Anatomy 0.000 claims 2
- 230000000414 obstructive effect Effects 0.000 claims 2
- 230000036407 pain Effects 0.000 claims 2
- 208000033808 peripheral neuropathy Diseases 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 208000023504 respiratory system disease Diseases 0.000 claims 2
- 239000000243 solution Substances 0.000 claims 2
- HCUOEKSZWPGJIM-IYNMRSRQSA-N (e,2z)-2-hydroxyimino-6-methoxy-4-methyl-5-nitrohex-3-enamide Chemical compound COCC([N+]([O-])=O)\C(C)=C\C(=N\O)\C(N)=O HCUOEKSZWPGJIM-IYNMRSRQSA-N 0.000 claims 1
- 208000002874 Acne Vulgaris Diseases 0.000 claims 1
- 208000035143 Bacterial infection Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010048768 Dermatosis Diseases 0.000 claims 1
- 201000004315 EAST syndrome Diseases 0.000 claims 1
- 206010014561 Emphysema Diseases 0.000 claims 1
- 208000009388 Job Syndrome Diseases 0.000 claims 1
- 201000001779 Leukocyte adhesion deficiency Diseases 0.000 claims 1
- IWIANZLCJVYEFX-RYUDHWBXSA-N Pro-Phe Chemical compound C([C@@H](C(=O)O)NC(=O)[C@H]1NCCC1)C1=CC=CC=C1 IWIANZLCJVYEFX-RYUDHWBXSA-N 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 241001303601 Rosacea Species 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 206010000496 acne Diseases 0.000 claims 1
- 230000001476 alcoholic effect Effects 0.000 claims 1
- 230000003042 antagnostic effect Effects 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 208000022362 bacterial infectious disease Diseases 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 239000007795 chemical reaction product Substances 0.000 claims 1
- 239000006071 cream Substances 0.000 claims 1
- 239000008298 dragée Substances 0.000 claims 1
- 230000009881 electrostatic interaction Effects 0.000 claims 1
- 208000012610 eosinophil disease Diseases 0.000 claims 1
- 239000012467 final product Substances 0.000 claims 1
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
- 239000000499 gel Substances 0.000 claims 1
- 125000005350 hydroxycycloalkyl group Chemical group 0.000 claims 1
- 208000014796 hyper-IgE recurrent infection syndrome 1 Diseases 0.000 claims 1
- 206010051040 hyper-IgE syndrome Diseases 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 230000003993 interaction Effects 0.000 claims 1
- 210000002540 macrophage Anatomy 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 210000001616 monocyte Anatomy 0.000 claims 1
- 239000006199 nebulizer Substances 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 239000002674 ointment Substances 0.000 claims 1
- 230000003239 periodontal effect Effects 0.000 claims 1
- 206010034674 peritonitis Diseases 0.000 claims 1
- 239000008177 pharmaceutical agent Substances 0.000 claims 1
- 239000011505 plaster Substances 0.000 claims 1
- 230000002685 pulmonary effect Effects 0.000 claims 1
- 201000004700 rosacea Diseases 0.000 claims 1
- 208000017520 skin disease Diseases 0.000 claims 1
- 239000002002 slurry Substances 0.000 claims 1
- 239000007921 spray Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 239000000829 suppository Substances 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
- 239000006188 syrup Substances 0.000 claims 1
- 235000020357 syrup Nutrition 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
- 0 *C([C@]1*=CC=I)C(*)=NN=C1I Chemical compound *C([C@]1*=CC=I)C(*)=NN=C1I 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11008121 | 2011-10-07 | ||
| EP11008121.3 | 2011-10-07 | ||
| PCT/EP2012/069412 WO2013050346A1 (en) | 2011-10-07 | 2012-10-02 | Template -fixed peptidomimetics as inhibitors of fpr1 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014528958A JP2014528958A (ja) | 2014-10-30 |
| JP2014528958A5 true JP2014528958A5 (enExample) | 2015-11-19 |
| JP6294227B2 JP6294227B2 (ja) | 2018-03-14 |
Family
ID=46970289
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014533851A Expired - Fee Related JP6294227B2 (ja) | 2011-10-07 | 2012-10-02 | Ｆｐｒ１の阻害剤としてのテンプレート固定ペプチド模倣薬 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9957297B2 (enExample) |
| EP (1) | EP2764010B9 (enExample) |
| JP (1) | JP6294227B2 (enExample) |
| CN (1) | CN103842373B (enExample) |
| AU (2) | AU2012320674A1 (enExample) |
| CA (1) | CA2848584C (enExample) |
| ES (1) | ES2576959T3 (enExample) |
| IL (1) | IL231756B (enExample) |
| MX (1) | MX349788B (enExample) |
| SG (1) | SG11201400354PA (enExample) |
| WO (1) | WO2013050346A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2009008843A (es) | 2007-02-28 | 2009-08-28 | Polyphor Ltd | Peptidomimeticos fijados a un patron. |
| US10654897B2 (en) * | 2014-09-30 | 2020-05-19 | Polyphor Ag | β-hairpin peptidomimetics |
| US10259847B2 (en) | 2014-09-30 | 2019-04-16 | Polyphor Ag | Beta-hairpin peptidomimetics |
| US10829520B2 (en) * | 2015-03-23 | 2020-11-10 | Polyphor Ag | Beta-hairpin peptidomimetics |
| CA3032885C (en) * | 2016-09-06 | 2023-06-20 | Mainline Biosciences | Cxcr4 antagonists and methods of use |
| CN112094316B (zh) * | 2017-06-29 | 2022-04-08 | 安徽省农业科学院农产品加工研究所 | 一种Ser和Cys分列在两端的高锌螯合活性锌鳌合肽及其应用 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7253146B2 (en) | 2001-02-23 | 2007-08-07 | Polyphor Ltd | Template-fixed peptidomimetics with antimicrobial activity |
| AU2002342618C1 (en) * | 2002-08-20 | 2008-10-30 | Polyphor Ltd. | Template-fixed peptidomimetics with antibacterial activity |
| AU2003232253A1 (en) | 2003-05-02 | 2004-11-23 | Polyphor Ag | Template-fixed beta-hairpin peptidomimetics with cxcr4 antagonizing activity |
| US7671028B2 (en) * | 2004-02-04 | 2010-03-02 | Postech Foundation | Peptides that antagonize FPR class receptor mediated signaling |
| EP1879911B1 (en) | 2005-05-02 | 2011-08-17 | Polyphor Ltd. | Dye conjugates of template-fixed peptidomimetics |
| MX2009008843A (es) * | 2007-02-28 | 2009-08-28 | Polyphor Ltd | Peptidomimeticos fijados a un patron. |
| US8883720B2 (en) | 2008-11-26 | 2014-11-11 | Polyphor Ag | Template-fixed beta-hairpin peptidomimetics with CXCR4 antagonizing activity |
| US8865656B2 (en) * | 2009-05-07 | 2014-10-21 | Polyphor Ag | Beta-hairpin peptidomimetics having CXCR4 antagonizing activity |
| EP2438047B1 (en) * | 2009-06-02 | 2014-07-30 | Nikan Pharmaceuticals, LLC | Antagonism of human formyl peptide receptor for treatment of disease |
| WO2011066869A1 (en) * | 2009-12-04 | 2011-06-09 | Polyphor Ag | Beta-hairpin peptidomimetics |
-
2012
- 2012-10-02 SG SG11201400354PA patent/SG11201400354PA/en unknown
- 2012-10-02 US US14/349,683 patent/US9957297B2/en not_active Expired - Fee Related
- 2012-10-02 MX MX2014003960A patent/MX349788B/es active IP Right Grant
- 2012-10-02 WO PCT/EP2012/069412 patent/WO2013050346A1/en not_active Ceased
- 2012-10-02 ES ES12768803.4T patent/ES2576959T3/es active Active
- 2012-10-02 JP JP2014533851A patent/JP6294227B2/ja not_active Expired - Fee Related
- 2012-10-02 CA CA2848584A patent/CA2848584C/en active Active
- 2012-10-02 EP EP12768803.4A patent/EP2764010B9/en active Active
- 2012-10-02 AU AU2012320674A patent/AU2012320674A1/en not_active Abandoned
- 2012-10-02 CN CN201280048985.4A patent/CN103842373B/zh not_active Expired - Fee Related
-
2014
- 2014-03-27 IL IL231756A patent/IL231756B/en active IP Right Grant
-
2017
- 2017-06-19 AU AU2017204122A patent/AU2017204122B2/en not_active Ceased
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