PT1017713E - Antagonistas cíclicos de receptores de c5a e de receptores acoplados à proteína g - Google Patents
Antagonistas cíclicos de receptores de c5a e de receptores acoplados à proteína g Download PDFInfo
- Publication number
- PT1017713E PT1017713E PT98930536T PT98930536T PT1017713E PT 1017713 E PT1017713 E PT 1017713E PT 98930536 T PT98930536 T PT 98930536T PT 98930536 T PT98930536 T PT 98930536T PT 1017713 E PT1017713 E PT 1017713E
- Authority
- PT
- Portugal
- Prior art keywords
- ref ref
- quot
- compound according
- side chain
- receptor
- Prior art date
Links
- 102000005590 Anaphylatoxin C5a Receptor Human genes 0.000 title claims description 17
- 108010059426 Anaphylatoxin C5a Receptor Proteins 0.000 title claims description 17
- 125000004122 cyclic group Chemical group 0.000 title abstract description 30
- 102000003688 G-Protein-Coupled Receptors Human genes 0.000 title abstract description 15
- 108090000045 G-Protein-Coupled Receptors Proteins 0.000 title abstract description 15
- 239000005557 antagonist Substances 0.000 title description 68
- 230000000694 effects Effects 0.000 claims abstract description 33
- 238000011282 treatment Methods 0.000 claims abstract description 13
- 230000001404 mediated effect Effects 0.000 claims abstract description 7
- 230000004968 inflammatory condition Effects 0.000 claims abstract description 5
- 101000941598 Homo sapiens Complement C5 Proteins 0.000 claims description 69
- 102100031506 Complement C5 Human genes 0.000 claims description 68
- 150000001875 compounds Chemical class 0.000 claims description 53
- 239000000556 agonist Substances 0.000 claims description 20
- 229910052739 hydrogen Inorganic materials 0.000 claims description 15
- 229940024606 amino acid Drugs 0.000 claims description 12
- QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 claims description 11
- QIVBCDIJIAJPQS-UHFFFAOYSA-N Tryptophan Natural products C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 claims description 11
- 238000000034 method Methods 0.000 claims description 11
- 150000008575 L-amino acids Chemical class 0.000 claims description 10
- 150000001413 amino acids Chemical class 0.000 claims description 10
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims description 8
- 125000000217 alkyl group Chemical group 0.000 claims description 8
- 239000004475 Arginine Substances 0.000 claims description 7
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims description 7
- 239000004472 Lysine Substances 0.000 claims description 7
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims description 7
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 6
- 125000004432 carbon atom Chemical group C* 0.000 claims description 6
- 230000002757 inflammatory effect Effects 0.000 claims description 6
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims description 6
- 206010052779 Transplant rejections Diseases 0.000 claims description 5
- 239000003814 drug Substances 0.000 claims description 5
- 238000004519 manufacturing process Methods 0.000 claims description 5
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims description 4
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 claims description 4
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims description 4
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims description 4
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims description 4
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims description 4
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims description 4
- 239000002464 receptor antagonist Substances 0.000 claims description 4
- 229940044551 receptor antagonist Drugs 0.000 claims description 4
- 208000011580 syndromic disease Diseases 0.000 claims description 4
- 201000001320 Atherosclerosis Diseases 0.000 claims description 3
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 claims description 3
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 claims description 3
- LRQKBLKVPFOOQJ-YFKPBYRVSA-N L-norleucine Chemical compound CCCC[C@H]([NH3+])C([O-])=O LRQKBLKVPFOOQJ-YFKPBYRVSA-N 0.000 claims description 3
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims description 3
- 201000004681 Psoriasis Diseases 0.000 claims description 3
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims description 3
- 206010040070 Septic Shock Diseases 0.000 claims description 3
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 claims description 3
- 125000002252 acyl group Chemical group 0.000 claims description 3
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims description 3
- 206010003246 arthritis Diseases 0.000 claims description 3
- 208000007565 gingivitis Diseases 0.000 claims description 3
- 125000000623 heterocyclic group Chemical group 0.000 claims description 3
- 229960000310 isoleucine Drugs 0.000 claims description 3
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 claims description 3
- 229930182817 methionine Natural products 0.000 claims description 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 3
- 230000036303 septic shock Effects 0.000 claims description 3
- 239000004474 valine Substances 0.000 claims description 3
- ADJZXDVMJPTFKT-JTQLQIEISA-N (2s)-2-azaniumyl-4-(1h-indol-3-yl)butanoate Chemical compound C1=CC=C2C(CC[C@H](N)C(O)=O)=CNC2=C1 ADJZXDVMJPTFKT-JTQLQIEISA-N 0.000 claims description 2
- FMUMEWVNYMUECA-LURJTMIESA-N (2s)-2-azaniumyl-5-methylhexanoate Chemical compound CC(C)CC[C@H](N)C(O)=O FMUMEWVNYMUECA-LURJTMIESA-N 0.000 claims description 2
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- RDFMDVXONNIGBC-LURJTMIESA-N L-2-aminoheptanoic acid Chemical compound CCCCC[C@H](N)C(O)=O RDFMDVXONNIGBC-LURJTMIESA-N 0.000 claims description 2
- QUOGESRFPZDMMT-UHFFFAOYSA-N L-Homoarginine Natural products OC(=O)C(N)CCCCNC(N)=N QUOGESRFPZDMMT-UHFFFAOYSA-N 0.000 claims description 2
- QUOGESRFPZDMMT-YFKPBYRVSA-N L-homoarginine Chemical compound OC(=O)[C@@H](N)CCCCNC(N)=N QUOGESRFPZDMMT-YFKPBYRVSA-N 0.000 claims description 2
- JTTHKOPSMAVJFE-VIFPVBQESA-N L-homophenylalanine Chemical compound OC(=O)[C@@H](N)CCC1=CC=CC=C1 JTTHKOPSMAVJFE-VIFPVBQESA-N 0.000 claims description 2
- 208000004852 Lung Injury Diseases 0.000 claims description 2
- 206010063837 Reperfusion injury Diseases 0.000 claims description 2
- 206010069363 Traumatic lung injury Diseases 0.000 claims description 2
- 231100000515 lung injury Toxicity 0.000 claims description 2
- 201000006417 multiple sclerosis Diseases 0.000 claims description 2
- 208000031225 myocardial ischemia Diseases 0.000 claims description 2
- 230000002018 overexpression Effects 0.000 claims description 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims description 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- BVAUMRCGVHUWOZ-ZETCQYMHSA-N (2s)-2-(cyclohexylazaniumyl)propanoate Chemical compound OC(=O)[C@H](C)NC1CCCCC1 BVAUMRCGVHUWOZ-ZETCQYMHSA-N 0.000 claims 1
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 claims 1
- SIKJAQJRHWYJAI-UHFFFAOYSA-N benzopyrrole Natural products C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 239000013256 coordination polymer Substances 0.000 claims 1
- 125000006165 cyclic alkyl group Chemical group 0.000 claims 1
- ORQXBVXKBGUSBA-UHFFFAOYSA-N cyclohexyl D-alanine Natural products OC(=O)C(N)CC1CCCCC1 ORQXBVXKBGUSBA-UHFFFAOYSA-N 0.000 claims 1
- 230000003828 downregulation Effects 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 201000003068 rheumatic fever Diseases 0.000 claims 1
- ORQXBVXKBGUSBA-QMMMGPOBSA-N β-cyclohexyl-alanine Chemical compound OC(=O)[C@@H](N)CC1CCCCC1 ORQXBVXKBGUSBA-QMMMGPOBSA-N 0.000 claims 1
- 150000001260 acyclic compounds Chemical class 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 description 59
- 108020003175 receptors Proteins 0.000 description 59
- 230000027455 binding Effects 0.000 description 35
- 108090000765 processed proteins & peptides Proteins 0.000 description 35
- 210000004027 cell Anatomy 0.000 description 25
- 102000004196 processed proteins & peptides Human genes 0.000 description 23
- 239000001257 hydrogen Substances 0.000 description 14
- 238000005481 NMR spectroscopy Methods 0.000 description 12
- 102100032957 C5a anaphylatoxin chemotactic receptor 1 Human genes 0.000 description 11
- 101710098483 C5a anaphylatoxin chemotactic receptor 1 Proteins 0.000 description 11
- -1 ioxinole Chemical compound 0.000 description 11
- 230000036515 potency Effects 0.000 description 11
- 235000001014 amino acid Nutrition 0.000 description 10
- 210000004899 c-terminal region Anatomy 0.000 description 10
- 201000010099 disease Diseases 0.000 description 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 10
- 210000003622 mature neutrocyte Anatomy 0.000 description 10
- 239000000679 carrageenan Substances 0.000 description 9
- 229920001525 carrageenan Polymers 0.000 description 9
- 235000010418 carrageenan Nutrition 0.000 description 9
- 229940113118 carrageenan Drugs 0.000 description 9
- 238000002474 experimental method Methods 0.000 description 9
- 229920006008 lipopolysaccharide Polymers 0.000 description 9
- 230000003389 potentiating effect Effects 0.000 description 9
- 239000000243 solution Substances 0.000 description 9
- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 9
- 239000002158 endotoxin Substances 0.000 description 8
- 241000282412 Homo Species 0.000 description 7
- 206010030113 Oedema Diseases 0.000 description 7
- 241000700159 Rattus Species 0.000 description 7
- 125000002015 acyclic group Chemical group 0.000 description 7
- 235000009697 arginine Nutrition 0.000 description 7
- 230000005764 inhibitory process Effects 0.000 description 7
- 208000004235 neutropenia Diseases 0.000 description 7
- ODKSFYDXXFIFQN-BYPYZUCNSA-N L-arginine Chemical compound OC(=O)[C@@H](N)CCCN=C(N)N ODKSFYDXXFIFQN-BYPYZUCNSA-N 0.000 description 6
- 102000003896 Myeloperoxidases Human genes 0.000 description 6
- 108090000235 Myeloperoxidases Proteins 0.000 description 6
- 230000004913 activation Effects 0.000 description 6
- 229960003121 arginine Drugs 0.000 description 6
- 238000003556 assay Methods 0.000 description 6
- 230000015572 biosynthetic process Effects 0.000 description 6
- 150000007942 carboxylates Chemical class 0.000 description 6
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N dimethyl sulfoxide Natural products CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 6
- 239000000203 mixture Substances 0.000 description 6
- 230000001225 therapeutic effect Effects 0.000 description 6
- 229960004799 tryptophan Drugs 0.000 description 6
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 description 5
- 150000001408 amides Chemical class 0.000 description 5
- 150000001412 amines Chemical class 0.000 description 5
- 230000003042 antagnostic effect Effects 0.000 description 5
- 238000001727 in vivo Methods 0.000 description 5
- 238000002347 injection Methods 0.000 description 5
- 239000007924 injection Substances 0.000 description 5
- 230000003993 interaction Effects 0.000 description 5
- 210000000440 neutrophil Anatomy 0.000 description 5
- 230000001175 peptic effect Effects 0.000 description 5
- 239000012071 phase Substances 0.000 description 5
- 238000012360 testing method Methods 0.000 description 5
- 230000002792 vascular Effects 0.000 description 5
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 description 4
- 241001465754 Metazoa Species 0.000 description 4
- 241000700157 Rattus norvegicus Species 0.000 description 4
- 125000004429 atom Chemical group 0.000 description 4
- 230000008859 change Effects 0.000 description 4
- 230000001684 chronic effect Effects 0.000 description 4
- 230000000295 complement effect Effects 0.000 description 4
- 230000004154 complement system Effects 0.000 description 4
- 239000006185 dispersion Substances 0.000 description 4
- 239000012530 fluid Substances 0.000 description 4
- 230000002209 hydrophobic effect Effects 0.000 description 4
- 230000004054 inflammatory process Effects 0.000 description 4
- 229960003646 lysine Drugs 0.000 description 4
- 230000007246 mechanism Effects 0.000 description 4
- 230000019491 signal transduction Effects 0.000 description 4
- 238000001228 spectrum Methods 0.000 description 4
- 238000001551 total correlation spectroscopy Methods 0.000 description 4
- 229960004441 tyrosine Drugs 0.000 description 4
- 238000005160 1H NMR spectroscopy Methods 0.000 description 3
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 3
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 description 3
- 108091006027 G proteins Proteins 0.000 description 3
- 102000030782 GTP binding Human genes 0.000 description 3
- 108091000058 GTP-Binding Proteins 0.000 description 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 3
- 206010061218 Inflammation Diseases 0.000 description 3
- 229930064664 L-arginine Natural products 0.000 description 3
- 235000014852 L-arginine Nutrition 0.000 description 3
- 230000001154 acute effect Effects 0.000 description 3
- 239000002671 adjuvant Substances 0.000 description 3
- 229960003767 alanine Drugs 0.000 description 3
- 235000004279 alanine Nutrition 0.000 description 3
- 230000008485 antagonism Effects 0.000 description 3
- 229940121363 anti-inflammatory agent Drugs 0.000 description 3
- 239000002260 anti-inflammatory agent Substances 0.000 description 3
- 230000003110 anti-inflammatory effect Effects 0.000 description 3
- 238000013459 approach Methods 0.000 description 3
- 230000008901 benefit Effects 0.000 description 3
- 210000004369 blood Anatomy 0.000 description 3
- 239000008280 blood Substances 0.000 description 3
- 229910052799 carbon Inorganic materials 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 150000001923 cyclic compounds Chemical class 0.000 description 3
- 230000006378 damage Effects 0.000 description 3
- 229910052805 deuterium Inorganic materials 0.000 description 3
- 238000011161 development Methods 0.000 description 3
- 230000008570 general process Effects 0.000 description 3
- 238000004128 high performance liquid chromatography Methods 0.000 description 3
- 238000000338 in vitro Methods 0.000 description 3
- 230000028709 inflammatory response Effects 0.000 description 3
- 239000003446 ligand Substances 0.000 description 3
- 210000002540 macrophage Anatomy 0.000 description 3
- 239000000463 material Substances 0.000 description 3
- 238000005259 measurement Methods 0.000 description 3
- 239000012528 membrane Substances 0.000 description 3
- 210000001616 monocyte Anatomy 0.000 description 3
- 229910052757 nitrogen Inorganic materials 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- 229960002429 proline Drugs 0.000 description 3
- 235000018102 proteins Nutrition 0.000 description 3
- 102000004169 proteins and genes Human genes 0.000 description 3
- 108090000623 proteins and genes Proteins 0.000 description 3
- 230000017854 proteolysis Effects 0.000 description 3
- 238000000425 proton nuclear magnetic resonance spectrum Methods 0.000 description 3
- 230000009467 reduction Effects 0.000 description 3
- 230000002441 reversible effect Effects 0.000 description 3
- 206010039073 rheumatoid arthritis Diseases 0.000 description 3
- 238000007363 ring formation reaction Methods 0.000 description 3
- 239000002904 solvent Substances 0.000 description 3
- 238000003786 synthesis reaction Methods 0.000 description 3
- 210000001519 tissue Anatomy 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- 125000003088 (fluoren-9-ylmethoxy)carbonyl group Chemical group 0.000 description 2
- NCYCYZXNIZJOKI-IOUUIBBYSA-N 11-cis-retinal Chemical compound O=C/C=C(\C)/C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C NCYCYZXNIZJOKI-IOUUIBBYSA-N 0.000 description 2
- 238000005084 2D-nuclear magnetic resonance Methods 0.000 description 2
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 description 2
- 241000894006 Bacteria Species 0.000 description 2
- 108010017384 Blood Proteins Proteins 0.000 description 2
- 102000004506 Blood Proteins Human genes 0.000 description 2
- 241000283690 Bos taurus Species 0.000 description 2
- 208000017667 Chronic Disease Diseases 0.000 description 2
- ODKSFYDXXFIFQN-SCSAIBSYSA-N D-arginine Chemical compound OC(=O)[C@H](N)CCCNC(N)=N ODKSFYDXXFIFQN-SCSAIBSYSA-N 0.000 description 2
- 229930028154 D-arginine Natural products 0.000 description 2
- IAZDPXIOMUYVGZ-WFGJKAKNSA-N Dimethyl sulfoxide Chemical compound [2H]C([2H])([2H])S(=O)C([2H])([2H])[2H] IAZDPXIOMUYVGZ-WFGJKAKNSA-N 0.000 description 2
- 208000009386 Experimental Arthritis Diseases 0.000 description 2
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 2
- XKMLYUALXHKNFT-UUOKFMHZSA-N Guanosine-5'-triphosphate Chemical compound C1=2NC(N)=NC(=O)C=2N=CN1[C@@H]1O[C@H](COP(O)(=O)OP(O)(=O)OP(O)(O)=O)[C@@H](O)[C@H]1O XKMLYUALXHKNFT-UUOKFMHZSA-N 0.000 description 2
- AHLPHDHHMVZTML-BYPYZUCNSA-N L-Ornithine Chemical compound NCCC[C@H](N)C(O)=O AHLPHDHHMVZTML-BYPYZUCNSA-N 0.000 description 2
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 description 2
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 description 2
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 2
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 2
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 description 2
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 description 2
- 241000699670 Mus sp. Species 0.000 description 2
- 206010028980 Neoplasm Diseases 0.000 description 2
- AHLPHDHHMVZTML-UHFFFAOYSA-N Orn-delta-NH2 Natural products NCCCC(N)C(O)=O AHLPHDHHMVZTML-UHFFFAOYSA-N 0.000 description 2
- UTJLXEIPEHZYQJ-UHFFFAOYSA-N Ornithine Natural products OC(=O)C(C)CCCN UTJLXEIPEHZYQJ-UHFFFAOYSA-N 0.000 description 2
- 108091005804 Peptidases Proteins 0.000 description 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 description 2
- 239000004365 Protease Substances 0.000 description 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 2
- 102100040756 Rhodopsin Human genes 0.000 description 2
- 108090000820 Rhodopsin Proteins 0.000 description 2
- PXIPVTKHYLBLMZ-UHFFFAOYSA-N Sodium azide Chemical compound [Na+].[N-]=[N+]=[N-] PXIPVTKHYLBLMZ-UHFFFAOYSA-N 0.000 description 2
- HEDRZPFGACZZDS-MICDWDOJSA-N Trichloro(2H)methane Chemical compound [2H]C(Cl)(Cl)Cl HEDRZPFGACZZDS-MICDWDOJSA-N 0.000 description 2
- 108060008682 Tumor Necrosis Factor Proteins 0.000 description 2
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 description 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 description 2
- 208000027418 Wounds and injury Diseases 0.000 description 2
- 238000004458 analytical method Methods 0.000 description 2
- 125000000637 arginyl group Chemical group N[C@@H](CCCNC(N)=N)C(=O)* 0.000 description 2
- 229960001230 asparagine Drugs 0.000 description 2
- 235000009582 asparagine Nutrition 0.000 description 2
- 229940009098 aspartate Drugs 0.000 description 2
- 210000001130 astrocyte Anatomy 0.000 description 2
- 239000000872 buffer Substances 0.000 description 2
- 239000011575 calcium Substances 0.000 description 2
- 210000000170 cell membrane Anatomy 0.000 description 2
- 210000003169 central nervous system Anatomy 0.000 description 2
- 210000001175 cerebrospinal fluid Anatomy 0.000 description 2
- 238000012512 characterization method Methods 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
- 208000037976 chronic inflammation Diseases 0.000 description 2
- 238000005100 correlation spectroscopy Methods 0.000 description 2
- 238000013461 design Methods 0.000 description 2
- 102000038379 digestive enzymes Human genes 0.000 description 2
- 108091007734 digestive enzymes Proteins 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 229940049906 glutamate Drugs 0.000 description 2
- 229930195712 glutamate Natural products 0.000 description 2
- ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 description 2
- 229960002743 glutamine Drugs 0.000 description 2
- 238000005534 hematocrit Methods 0.000 description 2
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 description 2
- 229960002885 histidine Drugs 0.000 description 2
- 208000015181 infectious disease Diseases 0.000 description 2
- 208000027866 inflammatory disease Diseases 0.000 description 2
- 208000014674 injury Diseases 0.000 description 2
- 230000003902 lesion Effects 0.000 description 2
- 229960003136 leucine Drugs 0.000 description 2
- 238000012417 linear regression Methods 0.000 description 2
- 238000004949 mass spectrometry Methods 0.000 description 2
- 238000000329 molecular dynamics simulation Methods 0.000 description 2
- 238000000655 nuclear magnetic resonance spectrum Methods 0.000 description 2
- 229960003104 ornithine Drugs 0.000 description 2
- 230000008506 pathogenesis Effects 0.000 description 2
- 229960005190 phenylalanine Drugs 0.000 description 2
- YBYRMVIVWMBXKQ-UHFFFAOYSA-N phenylmethanesulfonyl fluoride Chemical compound FS(=O)(=O)CC1=CC=CC=C1 YBYRMVIVWMBXKQ-UHFFFAOYSA-N 0.000 description 2
- 229920001184 polypeptide Polymers 0.000 description 2
- 230000005855 radiation Effects 0.000 description 2
- 238000001525 receptor binding assay Methods 0.000 description 2
- 230000001105 regulatory effect Effects 0.000 description 2
- 230000004044 response Effects 0.000 description 2
- 238000000926 separation method Methods 0.000 description 2
- 241000894007 species Species 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- ZGYICYBLPGRURT-UHFFFAOYSA-N tri(propan-2-yl)silicon Chemical compound CC(C)[Si](C(C)C)C(C)C ZGYICYBLPGRURT-UHFFFAOYSA-N 0.000 description 2
- 229960004295 valine Drugs 0.000 description 2
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 description 1
- GHYOCDFICYLMRF-UTIIJYGPSA-N (2S,3R)-N-[(2S)-3-(cyclopenten-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[[(2S)-2-[(2-morpholin-4-ylacetyl)amino]propanoyl]amino]propanamide Chemical compound C1(=CCCC1)C[C@@H](C(=O)[C@@]1(OC1)C)NC([C@H]([C@@H](C1=CC=C(C=C1)OC)O)NC([C@H](C)NC(CN1CCOCC1)=O)=O)=O GHYOCDFICYLMRF-UTIIJYGPSA-N 0.000 description 1
- DEVSOMFAQLZNKR-RJRFIUFISA-N (z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-n'-pyrazin-2-ylprop-2-enehydrazide Chemical compound FC(F)(F)C1=CC(C(F)(F)F)=CC(C2=NN(\C=C/C(=O)NNC=3N=CC=NC=3)C=N2)=C1 DEVSOMFAQLZNKR-RJRFIUFISA-N 0.000 description 1
- JKMHFZQWWAIEOD-UHFFFAOYSA-N 2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonic acid Chemical compound OCC[NH+]1CCN(CCS([O-])(=O)=O)CC1 JKMHFZQWWAIEOD-UHFFFAOYSA-N 0.000 description 1
- 208000030090 Acute Disease Diseases 0.000 description 1
- QYPPJABKJHAVHS-UHFFFAOYSA-N Agmatine Natural products NCCCCNC(N)=N QYPPJABKJHAVHS-UHFFFAOYSA-N 0.000 description 1
- 102000013455 Amyloid beta-Peptides Human genes 0.000 description 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 description 1
- 108010089414 Anaphylatoxins Proteins 0.000 description 1
- IYMAXBFPHPZYIK-BQBZGAKWSA-N Arg-Gly-Asp Chemical class NC(N)=NCCC[C@H](N)C(=O)NCC(=O)N[C@@H](CC(O)=O)C(O)=O IYMAXBFPHPZYIK-BQBZGAKWSA-N 0.000 description 1
- 208000023275 Autoimmune disease Diseases 0.000 description 1
- 241000282817 Bovidae Species 0.000 description 1
- 125000001433 C-terminal amino-acid group Chemical group 0.000 description 1
- OBMZMSLWNNWEJA-XNCRXQDQSA-N C1=CC=2C(C[C@@H]3NC(=O)[C@@H](NC(=O)[C@H](NC(=O)N(CC#CCN(CCCC[C@H](NC(=O)[C@@H](CC4=CC=CC=C4)NC3=O)C(=O)N)CC=C)NC(=O)[C@@H](N)C)CC3=CNC4=C3C=CC=C4)C)=CNC=2C=C1 Chemical compound C1=CC=2C(C[C@@H]3NC(=O)[C@@H](NC(=O)[C@H](NC(=O)N(CC#CCN(CCCC[C@H](NC(=O)[C@@H](CC4=CC=CC=C4)NC3=O)C(=O)N)CC=C)NC(=O)[C@@H](N)C)CC3=CNC4=C3C=CC=C4)C)=CNC=2C=C1 OBMZMSLWNNWEJA-XNCRXQDQSA-N 0.000 description 1
- WSNMPAVSZJSIMT-UHFFFAOYSA-N COc1c(C)c2COC(=O)c2c(O)c1CC(O)C1(C)CCC(=O)O1 Chemical compound COc1c(C)c2COC(=O)c2c(O)c1CC(O)C1(C)CCC(=O)O1 WSNMPAVSZJSIMT-UHFFFAOYSA-N 0.000 description 1
- 101100512078 Caenorhabditis elegans lys-1 gene Proteins 0.000 description 1
- 241000282472 Canis lupus familiaris Species 0.000 description 1
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- 102000014914 Carrier Proteins Human genes 0.000 description 1
- 241000288673 Chiroptera Species 0.000 description 1
- 108090000317 Chymotrypsin Proteins 0.000 description 1
- 102000016574 Complement C3-C5 Convertases Human genes 0.000 description 1
- 108010067641 Complement C3-C5 Convertases Proteins 0.000 description 1
- 108010034753 Complement Membrane Attack Complex Proteins 0.000 description 1
- 108010069514 Cyclic Peptides Proteins 0.000 description 1
- 102000001189 Cyclic Peptides Human genes 0.000 description 1
- 108090000695 Cytokines Proteins 0.000 description 1
- 102000004127 Cytokines Human genes 0.000 description 1
- 150000008574 D-amino acids Chemical class 0.000 description 1
- 150000008555 D-arginines Chemical class 0.000 description 1
- 108050009340 Endothelin Proteins 0.000 description 1
- 102000002045 Endothelin Human genes 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 241000283086 Equidae Species 0.000 description 1
- 241000282326 Felis catus Species 0.000 description 1
- 206010016654 Fibrosis Diseases 0.000 description 1
- 239000004471 Glycine Substances 0.000 description 1
- 239000007995 HEPES buffer Substances 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 108060003951 Immunoglobulin Proteins 0.000 description 1
- 108010002352 Interleukin-1 Proteins 0.000 description 1
- 108090001005 Interleukin-6 Proteins 0.000 description 1
- 108090001007 Interleukin-8 Proteins 0.000 description 1
- 108010063738 Interleukins Proteins 0.000 description 1
- 102000015696 Interleukins Human genes 0.000 description 1
- YQEZLKZALYSWHR-UHFFFAOYSA-N Ketamine Chemical compound C=1C=CC=C(Cl)C=1C1(NC)CCCCC1=O YQEZLKZALYSWHR-UHFFFAOYSA-N 0.000 description 1
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 description 1
- RHGKLRLOHDJJDR-BYPYZUCNSA-N L-citrulline Chemical compound NC(=O)NCCC[C@H]([NH3+])C([O-])=O RHGKLRLOHDJJDR-BYPYZUCNSA-N 0.000 description 1
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 description 1
- 208000019693 Lung disease Diseases 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 241000237852 Mollusca Species 0.000 description 1
- VHWBWHBJEXGPNM-UHFFFAOYSA-N N(2)-(2,4-dichlorophenyl)-N-(7-{[(2,4-dichlorophenyl)amino]sulfonyl}-1-oxo-1,2-dihydronaphthalen-2-yl)glycinamide Chemical compound ClC1=CC(Cl)=CC=C1NCC(=O)NC1C(=O)C2=CC(S(=O)(=O)NC=3C(=CC(Cl)=CC=3)Cl)=CC=C2C=C1 VHWBWHBJEXGPNM-UHFFFAOYSA-N 0.000 description 1
- RHGKLRLOHDJJDR-UHFFFAOYSA-N Ndelta-carbamoyl-DL-ornithine Natural products OC(=O)C(N)CCCNC(N)=O RHGKLRLOHDJJDR-UHFFFAOYSA-N 0.000 description 1
- 102100034574 P protein Human genes 0.000 description 1
- 101710181008 P protein Proteins 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 206010033645 Pancreatitis Diseases 0.000 description 1
- 208000030852 Parasitic disease Diseases 0.000 description 1
- 241001494479 Pecora Species 0.000 description 1
- 108090000284 Pepsin A Proteins 0.000 description 1
- 102000057297 Pepsin A Human genes 0.000 description 1
- 102000035195 Peptidases Human genes 0.000 description 1
- 101710176384 Peptide 1 Proteins 0.000 description 1
- 108010033276 Peptide Fragments Proteins 0.000 description 1
- 102000007079 Peptide Fragments Human genes 0.000 description 1
- 101710177166 Phosphoprotein Proteins 0.000 description 1
- 206010037660 Pyrexia Diseases 0.000 description 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 description 1
- 206010039020 Rhabdomyolysis Diseases 0.000 description 1
- 206010039710 Scleroderma Diseases 0.000 description 1
- 206010040047 Sepsis Diseases 0.000 description 1
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 description 1
- 108010071390 Serum Albumin Proteins 0.000 description 1
- 102000007562 Serum Albumin Human genes 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 102000005157 Somatostatin Human genes 0.000 description 1
- 108010056088 Somatostatin Proteins 0.000 description 1
- 238000000692 Student's t-test Methods 0.000 description 1
- 206010042674 Swelling Diseases 0.000 description 1
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 description 1
- 239000004473 Threonine Substances 0.000 description 1
- 108090000631 Trypsin Proteins 0.000 description 1
- 102000004142 Trypsin Human genes 0.000 description 1
- 108700033771 Tyr(65)-Phe(67)-Pro(69,71)-Ala(73)- (65-74) complement C5a Proteins 0.000 description 1
- 208000036142 Viral infection Diseases 0.000 description 1
- 241000700605 Viruses Species 0.000 description 1
- 230000009102 absorption Effects 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- 230000021736 acetylation Effects 0.000 description 1
- 238000006640 acetylation reaction Methods 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 239000008186 active pharmaceutical agent Substances 0.000 description 1
- QYPPJABKJHAVHS-UHFFFAOYSA-P agmatinium(2+) Chemical compound NC(=[NH2+])NCCCC[NH3+] QYPPJABKJHAVHS-UHFFFAOYSA-P 0.000 description 1
- 239000013566 allergen Substances 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- OMOZGSRMZAYUCI-UHFFFAOYSA-N amino cyanate Chemical compound NOC#N OMOZGSRMZAYUCI-UHFFFAOYSA-N 0.000 description 1
- 229940124277 aminobutyric acid Drugs 0.000 description 1
- 230000003321 amplification Effects 0.000 description 1
- 238000000540 analysis of variance Methods 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 229940124599 anti-inflammatory drug Drugs 0.000 description 1
- 150000001484 arginines Chemical class 0.000 description 1
- 108010072041 arginyl-glycyl-aspartic acid Proteins 0.000 description 1
- 238000003491 array Methods 0.000 description 1
- 230000003286 arthritogenic effect Effects 0.000 description 1
- WXNRAKRZUCLRBP-UHFFFAOYSA-N avridine Chemical compound CCCCCCCCCCCCCCCCCCN(CCCN(CCO)CCO)CCCCCCCCCCCCCCCCCC WXNRAKRZUCLRBP-UHFFFAOYSA-N 0.000 description 1
- 229950010555 avridine Drugs 0.000 description 1
- 239000011324 bead Substances 0.000 description 1
- 230000006399 behavior Effects 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 108091008324 binding proteins Proteins 0.000 description 1
- 230000000975 bioactive effect Effects 0.000 description 1
- 230000033228 biological regulation Effects 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- 230000004856 capillary permeability Effects 0.000 description 1
- 150000001720 carbohydrates Chemical class 0.000 description 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 1
- 230000002612 cardiopulmonary effect Effects 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 125000002091 cationic group Chemical group 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- 230000001413 cellular effect Effects 0.000 description 1
- 230000002490 cerebral effect Effects 0.000 description 1
- 238000001311 chemical methods and process Methods 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 230000006020 chronic inflammation Effects 0.000 description 1
- 208000037893 chronic inflammatory disorder Diseases 0.000 description 1
- 229960002376 chymotrypsin Drugs 0.000 description 1
- 235000013477 citrulline Nutrition 0.000 description 1
- 229960002173 citrulline Drugs 0.000 description 1
- 238000003776 cleavage reaction Methods 0.000 description 1
- 210000001520 comb Anatomy 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 230000024203 complement activation Effects 0.000 description 1
- 229940125797 compound 12 Drugs 0.000 description 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 229960002433 cysteine Drugs 0.000 description 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 description 1
- 235000018417 cysteine Nutrition 0.000 description 1
- JVHIPYJQMFNCEK-UHFFFAOYSA-N cytochalasin Natural products N1C(=O)C2(C(C=CC(C)CC(C)CC=C3)OC(C)=O)C3C(O)C(=C)C(C)C2C1CC1=CC=CC=C1 JVHIPYJQMFNCEK-UHFFFAOYSA-N 0.000 description 1
- ZMAODHOXRBLOQO-UHFFFAOYSA-N cytochalasin-A Natural products N1C(=O)C23OC(=O)C=CC(=O)CCCC(C)CC=CC3C(O)C(=C)C(C)C2C1CC1=CC=CC=C1 ZMAODHOXRBLOQO-UHFFFAOYSA-N 0.000 description 1
- 230000009089 cytolysis Effects 0.000 description 1
- 238000007405 data analysis Methods 0.000 description 1
- 230000034994 death Effects 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 230000007123 defense Effects 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 238000010511 deprotection reaction Methods 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 230000001627 detrimental effect Effects 0.000 description 1
- 238000003745 diagnosis Methods 0.000 description 1
- 238000000502 dialysis Methods 0.000 description 1
- 230000001079 digestive effect Effects 0.000 description 1
- UXGNZZKBCMGWAZ-UHFFFAOYSA-N dimethylformamide dmf Chemical compound CN(C)C=O.CN(C)C=O UXGNZZKBCMGWAZ-UHFFFAOYSA-N 0.000 description 1
- CETRZFQIITUQQL-UHFFFAOYSA-N dmso dimethylsulfoxide Chemical compound CS(C)=O.CS(C)=O CETRZFQIITUQQL-UHFFFAOYSA-N 0.000 description 1
- 238000012581 double quantum filtered COSY Methods 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 239000012636 effector Substances 0.000 description 1
- 238000000132 electrospray ionisation Methods 0.000 description 1
- 239000006274 endogenous ligand Substances 0.000 description 1
- 210000002889 endothelial cell Anatomy 0.000 description 1
- ZUBDGKVDJUIMQQ-UBFCDGJISA-N endothelin-1 Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(O)=O)NC(=O)[C@H]1NC(=O)[C@H](CC=2C=CC=CC=2)NC(=O)[C@@H](CC=2C=CC(O)=CC=2)NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CSSC[C@@H](C(N[C@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N2)=O)NC(=O)[C@@H](CO)NC(=O)[C@H](N)CSSC1)C1=CNC=N1 ZUBDGKVDJUIMQQ-UBFCDGJISA-N 0.000 description 1
- 229940088598 enzyme Drugs 0.000 description 1
- 210000000416 exudates and transudate Anatomy 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 230000004761 fibrosis Effects 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 230000014509 gene expression Effects 0.000 description 1
- 239000004220 glutamic acid Substances 0.000 description 1
- 150000004676 glycans Chemical class 0.000 description 1
- 229960002449 glycine Drugs 0.000 description 1
- 210000003714 granulocyte Anatomy 0.000 description 1
- 208000037824 growth disorder Diseases 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 208000019622 heart disease Diseases 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 210000003630 histaminocyte Anatomy 0.000 description 1
- 210000002758 humerus Anatomy 0.000 description 1
- 210000004276 hyalin Anatomy 0.000 description 1
- 150000002431 hydrogen Chemical class 0.000 description 1
- 125000001165 hydrophobic group Chemical group 0.000 description 1
- 230000009610 hypersensitivity Effects 0.000 description 1
- 230000006450 immune cell response Effects 0.000 description 1
- 230000007124 immune defense Effects 0.000 description 1
- 230000001900 immune effect Effects 0.000 description 1
- 210000000987 immune system Anatomy 0.000 description 1
- 102000018358 immunoglobulin Human genes 0.000 description 1
- 230000000495 immunoinflammatory effect Effects 0.000 description 1
- 238000005462 in vivo assay Methods 0.000 description 1
- 230000000937 inactivator Effects 0.000 description 1
- 238000011534 incubation Methods 0.000 description 1
- 230000002458 infectious effect Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 238000011081 inoculation Methods 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 229940047122 interleukins Drugs 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- 150000002500 ions Chemical class 0.000 description 1
- 229960003299 ketamine Drugs 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 125000001909 leucine group Chemical group [H]N(*)C(C(*)=O)C([H])([H])C(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 150000002617 leukotrienes Chemical class 0.000 description 1
- 229920005610 lignin Polymers 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 238000004811 liquid chromatography Methods 0.000 description 1
- 150000002642 lithium compounds Chemical class 0.000 description 1
- 230000002132 lysosomal effect Effects 0.000 description 1
- 150000002678 macrocyclic compounds Chemical class 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- 229960004452 methionine Drugs 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 description 1
- 230000000813 microbial effect Effects 0.000 description 1
- 210000000274 microglia Anatomy 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 239000003068 molecular probe Substances 0.000 description 1
- BAVYZALUXZFZLV-UHFFFAOYSA-N mono-methylamine Natural products NC BAVYZALUXZFZLV-UHFFFAOYSA-N 0.000 description 1
- 230000036651 mood Effects 0.000 description 1
- 210000000066 myeloid cell Anatomy 0.000 description 1
- SYSQUGFVNFXIIT-UHFFFAOYSA-N n-[4-(1,3-benzoxazol-2-yl)phenyl]-4-nitrobenzenesulfonamide Chemical class C1=CC([N+](=O)[O-])=CC=C1S(=O)(=O)NC1=CC=C(C=2OC3=CC=CC=C3N=2)C=C1 SYSQUGFVNFXIIT-UHFFFAOYSA-N 0.000 description 1
- WOOWBQQQJXZGIE-UHFFFAOYSA-N n-ethyl-n-propan-2-ylpropan-2-amine Chemical compound CCN(C(C)C)C(C)C.CCN(C(C)C)C(C)C WOOWBQQQJXZGIE-UHFFFAOYSA-N 0.000 description 1
- RUDCBGCNXOSCTI-UHFFFAOYSA-N n-methoxy-4-[4-(methoxyamino)phenyl]aniline Chemical compound C1=CC(NOC)=CC=C1C1=CC=C(NOC)C=C1 RUDCBGCNXOSCTI-UHFFFAOYSA-N 0.000 description 1
- 230000010807 negative regulation of binding Effects 0.000 description 1
- 239000012454 non-polar solvent Substances 0.000 description 1
- 230000009871 nonspecific binding Effects 0.000 description 1
- 238000005016 nuclear Overhauser enhanced spectroscopy Methods 0.000 description 1
- 238000003199 nucleic acid amplification method Methods 0.000 description 1
- 229940012843 omega-3 fatty acid Drugs 0.000 description 1
- 235000020660 omega-3 fatty acid Nutrition 0.000 description 1
- 239000006014 omega-3 oil Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 125000004430 oxygen atom Chemical group O* 0.000 description 1
- 229940094443 oxytocics prostaglandins Drugs 0.000 description 1
- 239000005022 packaging material Substances 0.000 description 1
- 206010033675 panniculitis Diseases 0.000 description 1
- 244000045947 parasite Species 0.000 description 1
- 229940111202 pepsin Drugs 0.000 description 1
- 238000010647 peptide synthesis reaction Methods 0.000 description 1
- 210000001428 peripheral nervous system Anatomy 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 230000035790 physiological processes and functions Effects 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
- 239000011148 porous material Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 230000000770 proinflammatory effect Effects 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 150000003180 prostaglandins Chemical class 0.000 description 1
- 238000000159 protein binding assay Methods 0.000 description 1
- 230000002797 proteolythic effect Effects 0.000 description 1
- 230000006337 proteolytic cleavage Effects 0.000 description 1
- 230000002685 pulmonary effect Effects 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- 239000000018 receptor agonist Substances 0.000 description 1
- 229940044601 receptor agonist Drugs 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 230000008844 regulatory mechanism Effects 0.000 description 1
- 230000027425 release of sequestered calcium ion into cytosol Effects 0.000 description 1
- 230000001850 reproductive effect Effects 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 239000011347 resin Substances 0.000 description 1
- 229920005989 resin Polymers 0.000 description 1
- 230000005801 respiratory difficulty Effects 0.000 description 1
- 230000004043 responsiveness Effects 0.000 description 1
- 238000007894 restriction fragment length polymorphism technique Methods 0.000 description 1
- 230000000717 retained effect Effects 0.000 description 1
- 238000004007 reversed phase HPLC Methods 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 230000007017 scission Effects 0.000 description 1
- 208000013223 septicemia Diseases 0.000 description 1
- 229960001153 serine Drugs 0.000 description 1
- 239000000952 serotonin receptor agonist Substances 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 201000006681 severe congenital neutropenia Diseases 0.000 description 1
- 238000004088 simulation Methods 0.000 description 1
- 150000003384 small molecules Chemical class 0.000 description 1
- 210000002460 smooth muscle Anatomy 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 238000010532 solid phase synthesis reaction Methods 0.000 description 1
- NHXLMOGPVYXJNR-ATOGVRKGSA-N somatostatin Chemical compound C([C@H]1C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N1)[C@@H](C)O)NC(=O)CNC(=O)[C@H](C)N)C(O)=O)=O)[C@H](O)C)C1=CC=CC=C1 NHXLMOGPVYXJNR-ATOGVRKGSA-N 0.000 description 1
- 229960000553 somatostatin Drugs 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- 238000013179 statistical model Methods 0.000 description 1
- 239000008174 sterile solution Substances 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 230000035882 stress Effects 0.000 description 1
- 238000005556 structure-activity relationship Methods 0.000 description 1
- 210000004304 subcutaneous tissue Anatomy 0.000 description 1
- 125000001424 substituent group Chemical group 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 230000008719 thickening Effects 0.000 description 1
- 150000003573 thiols Chemical class 0.000 description 1
- 229960002898 threonine Drugs 0.000 description 1
- 210000001541 thymus gland Anatomy 0.000 description 1
- 230000036962 time dependent Effects 0.000 description 1
- 230000000451 tissue damage Effects 0.000 description 1
- 231100000827 tissue damage Toxicity 0.000 description 1
- 238000002627 tracheal intubation Methods 0.000 description 1
- 230000001052 transient effect Effects 0.000 description 1
- 238000002054 transplantation Methods 0.000 description 1
- 230000001960 triggered effect Effects 0.000 description 1
- 229960001322 trypsin Drugs 0.000 description 1
- 239000012588 trypsin Substances 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
- 210000003556 vascular endothelial cell Anatomy 0.000 description 1
- 230000008728 vascular permeability Effects 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
- 230000003612 virological effect Effects 0.000 description 1
- 235000012431 wafers Nutrition 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 239000003643 water by type Substances 0.000 description 1
- BPICBUSOMSTKRF-UHFFFAOYSA-N xylazine Chemical compound CC1=CC=CC(C)=C1NC1=NCCCS1 BPICBUSOMSTKRF-UHFFFAOYSA-N 0.000 description 1
- 229960001600 xylazine Drugs 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/50—Cyclic peptides containing at least one abnormal peptide link
- C07K7/54—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
- C07K7/56—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
- C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
- C07K14/4701—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals not used
- C07K14/472—Complement proteins, e.g. anaphylatoxin, C3a, C5a
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2299/00—Coordinates from 3D structures of peptides, e.g. proteins or enzymes
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Immunology (AREA)
- Biochemistry (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Toxicology (AREA)
- Zoology (AREA)
- Gastroenterology & Hepatology (AREA)
- Rheumatology (AREA)
- Transplantation (AREA)
- Cardiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AUPO7550A AUPO755097A0 (en) | 1997-06-25 | 1997-06-25 | Receptor agonist and antagonist |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PT1017713E true PT1017713E (pt) | 2007-12-18 |
Family
ID=3801840
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PT98930536T PT1017713E (pt) | 1997-06-25 | 1998-06-25 | Antagonistas cíclicos de receptores de c5a e de receptores acoplados à proteína g |
Country Status (11)
| Country | Link |
|---|---|
| US (5) | USRE41287E1 (https=) |
| EP (1) | EP1017713B1 (https=) |
| JP (1) | JP4686696B2 (https=) |
| AT (1) | ATE377606T1 (https=) |
| AU (2) | AUPO755097A0 (https=) |
| CY (1) | CY1107133T1 (https=) |
| DE (1) | DE69838678T2 (https=) |
| DK (1) | DK1017713T3 (https=) |
| ES (1) | ES2294816T3 (https=) |
| PT (1) | PT1017713E (https=) |
| WO (1) | WO1999000406A1 (https=) |
Families Citing this family (54)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AUPO755097A0 (en) * | 1997-06-25 | 1997-07-17 | University Of Queensland, The | Receptor agonist and antagonist |
| AUPQ339899A0 (en) | 1999-10-13 | 1999-11-04 | University Of Queensland, The | Novel molecules |
| CA2418652C (en) | 2000-08-10 | 2010-03-23 | Mitsubishi Pharma Corporation | Novel 3-substituted urea derivatives and medicinal use thereof |
| WO2002022556A1 (en) | 2000-09-14 | 2002-03-21 | Mitsubishi Pharma Corporation | Novel amide derivatives and medicinal use thereof ugs |
| AUPR833401A0 (en) * | 2001-10-17 | 2001-11-08 | University Of Queensland, The | G protein-coupled receptor antagonists |
| US8524862B2 (en) | 2002-03-19 | 2013-09-03 | Cincinnati Children's Hospital Medical Center | Muteins of C5a anaphylatoxin and methods of inhibiting C5a |
| CA2480082A1 (en) * | 2002-03-29 | 2003-10-16 | Neurogen Corporation | Combination therapy for the treatment of conditions with pathogenic inflammatory components |
| AUPS160602A0 (en) * | 2002-04-08 | 2002-05-16 | University Of Queensland, The | Therapeutic method |
| AU2002950657A0 (en) | 2002-08-08 | 2002-09-12 | Alchemia Limited | Derivatives of monosaccharides for drug discovery |
| AU2003266858B2 (en) * | 2002-10-11 | 2006-09-14 | Vast Bioscience Pty Limited | Classes of compounds that interact with GPCRs |
| AU2002951995A0 (en) * | 2002-10-11 | 2002-10-31 | Alchemia Limited | Classes of compounds that interact with gpcrs |
| JP4818726B2 (ja) * | 2002-10-16 | 2011-11-16 | プロミクス・プロプライエタリー・リミテッド | 炎症性腸疾患の治療 |
| AU2002952086A0 (en) * | 2002-10-16 | 2002-11-07 | The University Of Queensland | Treatment of osteoarthritis |
| AU2002952129A0 (en) * | 2002-10-17 | 2002-10-31 | The University Of Queensland | Treatment of hypersensitivity conditions |
| AU2003902354A0 (en) * | 2003-05-15 | 2003-05-29 | Harkin, Denis W. | Treatment of haemorrhagic shock |
| AU2003902586A0 (en) * | 2003-05-26 | 2003-06-12 | The University Of Queensland | Treatment of burns |
| WO2005014849A2 (en) * | 2003-07-03 | 2005-02-17 | Euro-Celtique, S.A. | Genes associated with responses to neuropathic pain |
| EP1498422A1 (de) | 2003-07-17 | 2005-01-19 | Jerini AG | C5a-Rezeptor-Antagonisten |
| JP2008516194A (ja) * | 2004-10-04 | 2008-05-15 | アルケミア リミティッド | 選択的阻害剤 |
| RU2007131267A (ru) * | 2005-01-17 | 2009-02-27 | Йерини Аг (De) | АНТАГОНИСТЫ РЕЦЕПТОРА С5a |
| EP1861114B1 (en) * | 2005-03-11 | 2011-02-02 | Potentia Pharmaceuticals, Inc. | Compositions comprising modulators of g-protein-coupled receptor for treatment of macular degeneration |
| EP1739078A1 (de) | 2005-05-30 | 2007-01-03 | Jerini AG | C5a-Rezeptor-Antagonisten |
| US20070292421A1 (en) * | 2005-07-28 | 2007-12-20 | Feinberg Bruce B | Method for treating preeclampsia |
| US8168584B2 (en) | 2005-10-08 | 2012-05-01 | Potentia Pharmaceuticals, Inc. | Methods of treating age-related macular degeneration by compstatin and analogs thereof |
| HUE026001T2 (en) | 2007-02-05 | 2016-04-28 | Apellis Pharmaceuticals Inc | Compstatin analogues for use in the treatment of the inflammatory condition of the respiratory system |
| WO2009015087A2 (en) * | 2007-07-20 | 2009-01-29 | Potentia Pharmaceuticals, Inc. | Compositions and methods for treatment of trauma |
| US20110190221A1 (en) * | 2008-03-28 | 2011-08-04 | Apellis Ag | Modulation and repletion/enhancement of the complement system for treatment of trauma |
| US20100000605A1 (en) * | 2008-07-02 | 2010-01-07 | Saint-Gobain Performance Plastics Chaineux | Framed device, seal, and method for manufacturing same |
| CA2742802C (en) | 2008-11-10 | 2019-11-26 | Alexion Pharmaceuticals, Inc. | Methods and compositions for treating complement-associated disorders |
| WO2011091366A2 (en) * | 2010-01-22 | 2011-07-28 | University Of Louisville Research Foundation, Inc. | Methods of treating or preventing periodontitis and diseases associated with periodontitis |
| MX340696B (es) | 2010-04-30 | 2016-07-21 | Alexion Pharma Inc | Anticuerpos anti-c5a y metodos para usar los anticuerpos. |
| WO2012006149A2 (en) * | 2010-06-29 | 2012-01-12 | Board Of Regents Of The University Of Nebraska | Analogs of c5a and methods of using same |
| EP2468295A1 (en) * | 2010-12-21 | 2012-06-27 | Affiris AG | Vaccines based on peptides of the complement protein C5a |
| EP3524258B1 (en) | 2011-06-22 | 2025-10-01 | Apellis Pharmaceuticals, Inc. | Methods of treating chronic disorders with complement inhibitors |
| US9289467B2 (en) | 2011-08-10 | 2016-03-22 | Case Western Reserve University | Compositions and methods for treating bone conditions |
| WO2014043223A1 (en) * | 2012-09-11 | 2014-03-20 | Hospital For Special Surgery | Irhom2 inhibition for the treatment of complement mediated disorders |
| MX366404B (es) | 2012-11-15 | 2019-07-08 | Apellis Pharmaceuticals Inc | Analogos de compstatina de celula reactiva, de acción prolongada u objetivos y composiciones y metodos relacionados. |
| WO2014152391A1 (en) | 2013-03-15 | 2014-09-25 | Apellis Pharmaceuticals, Inc. | Cell-penetrating compstatin analogs and uses thereof |
| US10092620B2 (en) * | 2013-04-02 | 2018-10-09 | The Scripps Research Institute | Uses of cyclic peptides for treating and preventing atherosclerosis |
| SI3011345T1 (sl) | 2013-08-07 | 2017-12-29 | Alexion Pharmaceuticals, Inc. | Biomarkerski proteini za atipični hemolitični uremični sindrom (ahus) |
| US11903994B2 (en) | 2015-10-07 | 2024-02-20 | Apellis Pharmaceuticals, Inc. | Dosing regimens |
| US20190270778A1 (en) | 2016-07-29 | 2019-09-05 | Pfizer Inc. | Cyclic Peptides As C5a Receptor Antagonists |
| US20200057046A1 (en) | 2016-10-27 | 2020-02-20 | Alexion Pharmaceuticals, Inc. | Assay for c5b-9 deposition in complement-associated disorders |
| TWI826364B (zh) | 2017-04-03 | 2023-12-21 | 德商因夫萊亞斯有限公司 | 活性抑制劑於發炎性疾病之治療 |
| IL269844B2 (en) | 2017-04-07 | 2025-01-01 | Apellis Pharmaceuticals Inc | Dosage regimens and related compositions and methods |
| TWI786132B (zh) | 2017-06-23 | 2022-12-11 | 德商因夫萊亞斯有限公司 | 活性抑制劑於發炎性疾病之治療 |
| WO2019118938A1 (en) | 2017-12-15 | 2019-06-20 | Apellis Pharmaceuticals, Inc. | Dosing regimens and related compositions and methods |
| US20220356234A1 (en) | 2019-10-02 | 2022-11-10 | Alexion Pharmaceuticals, Inc. | Complement inhibitors for treating drug-induced complement-mediated response |
| PH12022552556A1 (en) | 2020-03-27 | 2024-04-22 | Inflarx Gmbh | Inhibitors of c5a for the treatment of corona virus infection |
| TW202208427A (zh) | 2020-05-06 | 2022-03-01 | 德商因夫萊亞斯有限公司 | 人源化抗ｃ５ａ抗體 |
| JP2023525581A (ja) | 2020-05-15 | 2023-06-16 | アレクシオン ファーマシューティカルズ， インコーポレイテッド | 補体の活性化を検出するための細胞外小胞の使用方法、並びに補体性疾患の処置を評価及び／又は監視するためのその使用 |
| WO2024238422A1 (en) | 2023-05-12 | 2024-11-21 | Alexion Pharmaceuticals, Inc. | Use of a panel of lectins for detection of complement biomarkers in urine extracellular vesicles |
| WO2024238421A1 (en) | 2023-05-12 | 2024-11-21 | Alexion Pharmaceuticals, Inc. | Use of biomarkers for the identification and treatment of complement-mediated disorders |
| US12180274B2 (en) | 2023-05-26 | 2024-12-31 | Inflarx Gmbh | Treatment of pneumonia and ARDS with inhibitors of C5a and IL-6 activity |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5386011A (en) | 1990-12-27 | 1995-01-31 | Abbott Laboratories | Hexapeptide anaphylatoxin-receptor ligands |
| WO1995016033A1 (en) | 1993-12-06 | 1995-06-15 | Ciba-Geigy Ag | C5a RECEPTOR ANTAGONISTS HAVING SUBSTANTIALLY NO AGONIST ACTIVITY |
| US5807824A (en) * | 1993-12-06 | 1998-09-15 | Ciba-Geigy Corporation | C5A receptor antagonists having substantially no agonist activity |
| US5614370A (en) | 1994-03-18 | 1997-03-25 | Merck & Co., Inc. | Assay to identify human C5a antagonists and agonists |
| US5696230A (en) * | 1994-08-31 | 1997-12-09 | The Board Of Regents Of The University Of Nebraska | High-affinity response-selective C-terminal analogs of C5a anaphylatoxin |
| AUPO755097A0 (en) | 1997-06-25 | 1997-07-17 | University Of Queensland, The | Receptor agonist and antagonist |
| AUPR833401A0 (en) | 2001-10-17 | 2001-11-08 | University Of Queensland, The | G protein-coupled receptor antagonists |
| AUPS160602A0 (en) * | 2002-04-08 | 2002-05-16 | University Of Queensland, The | Therapeutic method |
| AU2002952086A0 (en) * | 2002-10-16 | 2002-11-07 | The University Of Queensland | Treatment of osteoarthritis |
-
1997
- 1997-06-25 AU AUPO7550A patent/AUPO755097A0/en not_active Abandoned
-
1998
- 1998-06-25 WO PCT/AU1998/000490 patent/WO1999000406A1/en not_active Ceased
- 1998-06-25 EP EP98930536A patent/EP1017713B1/en not_active Expired - Lifetime
- 1998-06-25 DK DK98930536T patent/DK1017713T3/da active
- 1998-06-25 JP JP50515499A patent/JP4686696B2/ja not_active Expired - Fee Related
- 1998-06-25 AU AU80926/98A patent/AU744991B2/en not_active Ceased
- 1998-06-25 US US12/045,088 patent/USRE41287E1/en not_active Expired - Fee Related
- 1998-06-25 ES ES98930536T patent/ES2294816T3/es not_active Expired - Lifetime
- 1998-06-25 US US09/446,109 patent/US6821950B1/en not_active Expired - Lifetime
- 1998-06-25 AT AT98930536T patent/ATE377606T1/de active
- 1998-06-25 DE DE69838678T patent/DE69838678T2/de not_active Expired - Lifetime
- 1998-06-25 PT PT98930536T patent/PT1017713E/pt unknown
-
2004
- 2004-09-10 US US10/937,852 patent/US20060160726A1/en not_active Abandoned
-
2008
- 2008-01-10 CY CY20081100033T patent/CY1107133T1/el unknown
- 2008-08-19 US US12/193,943 patent/US20090203760A1/en not_active Abandoned
-
2012
- 2012-01-12 US US13/348,869 patent/US20130005644A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| DE69838678D1 (de) | 2007-12-20 |
| US20130005644A1 (en) | 2013-01-03 |
| US20060160726A1 (en) | 2006-07-20 |
| EP1017713A1 (en) | 2000-07-12 |
| WO1999000406A1 (en) | 1999-01-07 |
| US20090203760A1 (en) | 2009-08-13 |
| AU744991B2 (en) | 2002-03-07 |
| AUPO755097A0 (en) | 1997-07-17 |
| AU8092698A (en) | 1999-01-19 |
| EP1017713A4 (en) | 2002-07-24 |
| ATE377606T1 (de) | 2007-11-15 |
| US6821950B1 (en) | 2004-11-23 |
| DE69838678T2 (de) | 2008-10-30 |
| EP1017713B1 (en) | 2007-11-07 |
| CY1107133T1 (el) | 2012-10-24 |
| HK1029595A1 (en) | 2001-04-06 |
| DK1017713T3 (da) | 2008-02-11 |
| JP4686696B2 (ja) | 2011-05-25 |
| USRE41287E1 (en) | 2010-04-27 |
| ES2294816T3 (es) | 2008-04-01 |
| JP2002508767A (ja) | 2002-03-19 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PT1017713E (pt) | Antagonistas cíclicos de receptores de c5a e de receptores acoplados à proteína g | |
| ES2663916T3 (es) | Ligandos de los receptores de la melanocortina | |
| JP6084207B2 (ja) | 虚血性脳損傷及び疼痛治療用の効率的な神経保護剤としてのｐｓｄ−９５の高親和性二量体阻害剤 | |
| DE69623254T2 (de) | Lhrh antagonistische peptide | |
| BRPI0613984A2 (pt) | peptìdios para uso no tratamento da obesidade, seu uso e composição farmacêutica compreendendo os mesmos | |
| PT97992B (pt) | Processo de preparacao de analogos de um patrimonio peptoide com resistencia a protease, e processo para a sintese de uma mistura de polimeros com eles relacionados | |
| JP2005515973A (ja) | Ｇタンパク質結合受容体アンタゴニストとしての環状ペプチド | |
| PT2132221E (pt) | Peptidomiméticos fixados num molde | |
| BR122019016211B1 (pt) | Composto, composição farmacêutica, uso do composto e processo para a fabricação do mesmo | |
| CN116209671A (zh) | 补体因子c3的抑制剂及其医学用途 | |
| DE69703032T2 (de) | Peptidderivate | |
| IL322205A (en) | GIP/GLP1/GCG trireceptor agonists and their uses | |
| EP1809666A2 (en) | Peptides for use in the treating obesity | |
| EP1812471A2 (en) | Peptides for use in treating of obesity | |
| PT87857B (pt) | Processo para a preparacao de novos peptidos com propriedades imunossupressoras | |
| CN102223898A (zh) | 治疗肥胖的肽 | |
| DE69725338T2 (de) | Inhibitore der peptidbindung an mhc class ii proteine | |
| CN108676074A (zh) | 一种促肝细胞生长的活性多肽 | |
| US20180148474A1 (en) | Peptide derivative for regulating thymic stromal lymphoid protein-mediated signaling and pharmaceutical composition for preventing and treating allergy and asthma diseases comprising same | |
| HK1029595B (en) | Cyclic antagonists of c5a receptors and g protein-coupled receptors | |
| Maji | Amyloid: a natural nanomaterial | |
| Jaishankar | Synthesis and biological evaluation of α-MSH peptide-peptoid hybrids |