CN102977191B - 有效的c3补体抑制素类似物 - Google Patents
有效的c3补体抑制素类似物 Download PDFInfo
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- CN102977191B CN102977191B CN201210455683.0A CN201210455683A CN102977191B CN 102977191 B CN102977191 B CN 102977191B CN 201210455683 A CN201210455683 A CN 201210455683A CN 102977191 B CN102977191 B CN 102977191B
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- Prior art keywords
- trp
- peptide
- tryptophan
- analog
- cys
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- RDTRHBCZFDCUPW-KWICJJCGSA-N 2-[(4r,7s,10s,13s,19s,22s,25s,28s,31s,34r)-4-[[(2s,3r)-1-amino-3-hydroxy-1-oxobutan-2-yl]carbamoyl]-34-[[(2s,3s)-2-amino-3-methylpentanoyl]amino]-25-(3-amino-3-oxopropyl)-7-[3-(diaminomethylideneamino)propyl]-10,13-bis(1h-imidazol-5-ylmethyl)-19-(1h-indol Chemical class C([C@H]1C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CSSC[C@@H](C(N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=2C3=CC=CC=C3NC=2)C(=O)NCC(=O)N[C@@H](CC=2NC=NC=2)C(=O)N1)C(C)C)C(C)C)=O)NC(=O)[C@@H](N)[C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(N)=O)C1=CN=CN1 RDTRHBCZFDCUPW-KWICJJCGSA-N 0.000 title description 130
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- 238000000034 method Methods 0.000 claims description 34
- -1 Val Chemical compound 0.000 claims description 29
- QIVBCDIJIAJPQS-UHFFFAOYSA-N Tryptophan Natural products C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 claims description 27
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- FEZASNVQLJQBHW-CABZTGNLSA-N Trp-Gly-Ala Chemical compound C1=CC=C2C(C[C@H](N)C(=O)NCC(=O)N[C@@H](C)C(O)=O)=CNC2=C1 FEZASNVQLJQBHW-CABZTGNLSA-N 0.000 claims 9
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- 125000002707 L-tryptophyl group Chemical group [H]C1=C([H])C([H])=C2C(C([C@](N([H])[H])(C(=O)[*])[H])([H])[H])=C([H])N([H])C2=C1[H] 0.000 description 18
- 125000004432 carbon atom Chemical group C* 0.000 description 17
- ZADWXFSZEAPBJS-JTQLQIEISA-N 1-methyl-L-tryptophan Chemical compound C1=CC=C2N(C)C=C(C[C@H](N)C(O)=O)C2=C1 ZADWXFSZEAPBJS-JTQLQIEISA-N 0.000 description 16
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- C—CHEMISTRY; METALLURGY
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- 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
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| ES2677619T3 (es) | 2005-11-28 | 2018-08-03 | The Trustees Of The University Of Pennsylvania | Análogos potentes de la compstatina |
| US8637325B2 (en) * | 2009-02-16 | 2014-01-28 | University Of Wyoming | Method and apparatus for pyrolysis-induced cleavage in peptides and proteins |
| WO2008048675A2 (en) * | 2006-10-20 | 2008-04-24 | Celldex Therapeutics, Inc. | Treatment for age-related macular degeneration and other diseases of the eye |
| PL2148691T3 (pl) * | 2007-02-05 | 2015-12-31 | Apellis Pharmaceuticals Inc | Analogi kompstatyny do stosowania w leczeniu stanów zapalnych układu oddechowego |
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| US8442776B2 (en) | 2007-06-08 | 2013-05-14 | The Trustees Of The University Of Pennsylvania | Structure of compstatin-C3 complex and use for rational drug design |
| US8563259B2 (en) | 2007-06-29 | 2013-10-22 | The Trustees Of The University Of Pennsylvania | Complement-mediated thrombophilic assay |
| RU2505311C2 (ru) * | 2007-10-02 | 2014-01-27 | Потентия Фармасьютикалз, Инк. | Пролонгированная доставка аналогов компстатина из гелей |
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| DK2424557T3 (en) * | 2009-05-01 | 2018-01-22 | Univ Pennsylvania | MODIFIED COMPSTATIN WITH PEPTID BACKBONE AND C-TERMINAL MODIFICATIONS |
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| FR2295746A1 (fr) | 1974-12-23 | 1976-07-23 | Francaise Coop Pharma | Nouveaux derives du tryptophane a activite nerveuse centrale renforcee |
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| US5167960A (en) * | 1988-08-03 | 1992-12-01 | New England Deaconess Hospital Corporation | Hirudin-coated biocompatible substance |
| AU7749491A (en) | 1990-04-23 | 1991-11-11 | Rijksuniversiteit Te Utrecht | Cyclic peptides and their use |
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| US5776970A (en) | 1994-04-28 | 1998-07-07 | Yeda Research And Development Co. Ltd. | Tryptophan derivatives as protein tyrosine kinase blockers and their use in the treatment of neoplastic diseases |
| GB9604865D0 (en) * | 1996-03-07 | 1996-05-08 | Imutran Ltd | Modified proteins |
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| US6169057B1 (en) | 1997-09-04 | 2001-01-02 | The Regents Of The University Of California | Use of tryptophan and analogs as plant growth regulators |
| AU4648197A (en) | 1997-09-17 | 1999-04-05 | Burnham Institute, The | Peptides and peptidomimetics for inhibiting complement activation |
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| PT1549333E (pt) * | 2002-09-20 | 2012-01-03 | Univ Pennsylvania | Análogos de compstatina com actividade melhorada |
| US7541032B2 (en) | 2002-09-20 | 2009-06-02 | Stichting Katholieke Universiteit | Antigen uptake receptor for Candida albicans on dendritic cells |
| PL1951279T3 (pl) * | 2005-10-08 | 2017-12-29 | Apellis Pharmaceuticals, Inc. | Kompstatyna i jej analogi w zaburzeniach oczu |
| ES2677619T3 (es) * | 2005-11-28 | 2018-08-03 | The Trustees Of The University Of Pennsylvania | Análogos potentes de la compstatina |
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| Hydrophobic effect and hydrogen bonds account for the improved activity of a complement inhibitor, compstatin;Madan Katragadda et al;《J. Med. Chem.》;20060727;第49卷;4616-4622 * |
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