HRP20120621T1 - Sna“ni analozi kompstatina - Google Patents
Sna“ni analozi kompstatina Download PDFInfo
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- HRP20120621T1 HRP20120621T1 HRP20120621TT HRP20120621T HRP20120621T1 HR P20120621 T1 HRP20120621 T1 HR P20120621T1 HR P20120621T T HRP20120621T T HR P20120621TT HR P20120621 T HRP20120621 T HR P20120621T HR P20120621 T1 HRP20120621 T1 HR P20120621T1
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- Prior art keywords
- trp
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- analog
- compound according
- val
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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 1
- 230000003389 potentiating effect Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 22
- 108090000765 processed proteins & peptides Proteins 0.000 claims abstract 9
- AYFVYJQAPQTCCC-STHAYSLISA-N D-threonine Chemical compound C[C@H](O)[C@@H](N)C(O)=O AYFVYJQAPQTCCC-STHAYSLISA-N 0.000 claims abstract 6
- 108010016626 Dipeptides Proteins 0.000 claims abstract 6
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims abstract 6
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 6
- 239000001257 hydrogen Substances 0.000 claims abstract 6
- -1 Val Chemical compound 0.000 claims abstract 5
- 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 claims abstract 4
- QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical class C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 claims abstract 4
- 230000024203 complement activation Effects 0.000 claims abstract 4
- 125000001041 indolyl group Chemical group 0.000 claims abstract 4
- ZADWXFSZEAPBJS-UHFFFAOYSA-N racemic N-methyl tryptophan Natural products C1=CC=C2N(C)C=C(CC(N)C(O)=O)C2=C1 ZADWXFSZEAPBJS-UHFFFAOYSA-N 0.000 claims abstract 4
- KVNPSKDDJARYKK-JTQLQIEISA-N 5-methoxytryptophan Chemical compound COC1=CC=C2NC=C(C[C@H](N)C(O)=O)C2=C1 KVNPSKDDJARYKK-JTQLQIEISA-N 0.000 claims abstract 3
- HUNCSWANZMJLPM-UHFFFAOYSA-N 5-methyltryptophan Chemical compound CC1=CC=C2NC=C(CC(N)C(O)=O)C2=C1 HUNCSWANZMJLPM-UHFFFAOYSA-N 0.000 claims abstract 3
- KGVHCTWYMPWEGN-FSPLSTOPSA-N Gly-Ile Chemical compound CC[C@H](C)[C@@H](C(O)=O)NC(=O)CN KGVHCTWYMPWEGN-FSPLSTOPSA-N 0.000 claims abstract 3
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 3
- VPZKQTYZIVOJDV-LMVFSUKVSA-N Thr-Ala Chemical compound C[C@@H](O)[C@H](N)C(=O)N[C@@H](C)C(O)=O VPZKQTYZIVOJDV-LMVFSUKVSA-N 0.000 claims abstract 3
- DFTCYYILCSQGIZ-GCJQMDKQSA-N Thr-Ala-Asn Chemical compound [H]N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(O)=O DFTCYYILCSQGIZ-GCJQMDKQSA-N 0.000 claims abstract 3
- UQTNIFUCMBFWEJ-IWGUZYHVSA-N Thr-Asn Chemical compound C[C@@H](O)[C@H](N)C(=O)N[C@H](C(O)=O)CC(N)=O UQTNIFUCMBFWEJ-IWGUZYHVSA-N 0.000 claims abstract 3
- 229910052731 fluorine Inorganic materials 0.000 claims abstract 3
- 125000001153 fluoro group Chemical group F* 0.000 claims abstract 3
- 230000002209 hydrophobic effect Effects 0.000 claims abstract 3
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims abstract 3
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims abstract 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- KRUDZOGZZBVSHD-JTQLQIEISA-N (2s)-2-azaniumyl-3-(1-formylindol-3-yl)propanoate Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CN(C=O)C2=C1 KRUDZOGZZBVSHD-JTQLQIEISA-N 0.000 claims 1
- 102000009027 Albumins Human genes 0.000 claims 1
- 108010088751 Albumins Proteins 0.000 claims 1
- QIVBCDIJIAJPQS-UHFFFAOYSA-N Tryptophan Natural products C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 claims 1
- 238000007385 chemical modification Methods 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 230000014759 maintenance of location Effects 0.000 claims 1
- 238000010647 peptide synthesis reaction Methods 0.000 claims 1
- 102000040430 polynucleotide Human genes 0.000 claims 1
- 108091033319 polynucleotide Proteins 0.000 claims 1
- 239000002157 polynucleotide Substances 0.000 claims 1
- 210000004899 c-terminal region Anatomy 0.000 abstract 1
- 230000002708 enhancing effect Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/64—Cyclic peptides containing only normal peptide links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/10—Peptides having 12 to 20 amino acids
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
-
- 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
Abstract
Spoj koji inhibira aktivaciju komplementa, sadr·i peptid sa sekvencom: Xaa1 - Cys - Val - Xaa2 - Gln - Asp - Xaa3 - Gly - Xaa4 - His - Arg - Cys - Xaa5 (SEQ ID NO:26); gdje: Xaa1 je Ile, Val, Leu, Ac-Ile, Ac-Val, Ac-Leu ili dipeptid Gly-Ile; Xaa2 je Trp ili njegov analog, gdje analog od Trp ima pojačan hidrofobni karakter u odnosu na Trp i odabire se između halogeniranog triptofana, 5-metoksitriptofana, 5-metiltriptofan i 1-metiltriptofana, uz uvjet da ako Xaa3 je Trp, Xaa2 je analog od Trp; Xaa3 je Trp ili njegov analog gdje je vodik u indolu zamijenjen atomom fluora čime je pojačan potencijal vodikove veze indolnog prstena; Xaa4 je His, Ala, Phe ili Trp; Xaa5 je L-Thr, D-Thr, Ile, Val, Gly, dipeptid Thr-Asn ili Thr-Ala ili tripeptid Thr-Ala-Asn, gdje je na karboksi krajnjem -OH bilo koji od L-Thr, D-Thr, Ile, Val, Gly ili Asn po izboru zamijenjen s -NH2; idva ostatka Cys povezana su disulfidnom vezom. Patent sadr·i jo® 17 patentnih zahtjeva.
Claims (18)
1. Spoj koji inhibira aktivaciju komplementa, sadrži peptid sa sekvencom:
Xaa1 - Cys - Val - Xaa2 - Gln - Asp - Xaa3 - Gly - Xaa4 - His - Arg - Cys - Xaa5 (SEQ ID NO:26);
gdje:
Xaa1 je Ile, Val, Leu, Ac-Ile, Ac-Val, Ac-Leu ili dipeptid Gly-Ile;
Xaa2 je Trp ili njegov analog, gdje analog od Trp ima pojačan hidrofobni karakter u odnosu na Trp i odabire se između halogeniranog triptofana, 5-metoksitriptofana, 5-metiltriptofan i 1-metiltriptofana, uz uvjet da ako Xaa3 je Trp, Xaa2 je analog od Trp;
Xaa3 je Trp ili njegov analog gdje je vodik u indolu zamijenjen atomom fluora čime je pojačan potencijal vodikove veze indolnog prstena;
Xaa4 je His, Ala, Phe ili Trp;
Xaa5 je L-Thr, D-Thr, Ile, Val, Gly, dipeptid Thr-Asn ili Thr-Ala ili tripeptid Thr-Ala-Asn, gdje je na karboksi krajnjem -OH bilo koji od L-Thr, D-Thr, Ile, Val, Gly ili Asn po izboru zamijenjen s -NH2; i
dva ostatka Cys povezana su disulfidnom vezom.
2. Spoj prema zahtjevu 1, gdje analog od Trp kao Xaa2 je 5-fluoro-1-triptofan, ili 6-fluoro-1-triptofan.
3. Spoj prema zahtjevu 1, gdje analog od Trp kao Xaa2 je 5-metoksitriptofan ili 5-metiltriptofan.
4. Spoj prema zahtjevu 1, gdje analog od Trp kao Xaa2 je 1-metiltriptofan.
5. Spoj prema bilo kojem od prethodnih zahtjeva, gdje Xaa4 je Ala.
6. Spoj prema zahtjevu 1, gdje Xaa2 je 1-metil triptofan, Xaa3 je po izboru analog od Trp gdje je vodik u indolu zamijenjen atomom fluora i Xaa4 je Ala.
7. Spoj prema zahtjevu 6, gdje izborni Trp analog kao Xaa3 je 5-fluoro-1-triptofan.
8. Spoj prema zahtjevu 1, sadrži bilo koju od sekvenci SEQ ID NOS: 16-24.
9. Spoj koji inhibira aktivaciju komplementa, sadrži peptid sa sekvencom:
Xaa1 - Cys - Val - Xaa2 - Gln - Asp - Xaa3 - Gly - Xaa4 - His - Arg - Cys - Xaa5 (SEQ ID NO:26);
gdje:
Xaa1 je Ile, Val, Leu, Ac-Ile, Ac-Val, Ac-Leu ili dipeptid Gly-Ile;
Xaa2 je Trp ili njegov analog, gdje analog od Trp ima niži alkanoilni supstituent na položaju 1 triptofana ima pojačan hidrofobni karakter u odnosu na Trp, uz uvjet da ako Xaa3 je Trp, Xaa2 je analog od Trp;
Xaa3 je Trp ili njegov analog koji je halogenirani triptofan, što je kemijska modifikacija njegovog indolnog prstena čime je pojačan potencijal vodikove veze indolnog prstena;
Xaa4 je His, Ala, Phe ili Trp;
Xaa5 je L-Thr, D-Thr, Ile, Val, Gly, dipeptid Thr-Asn ili Thr-Ala ili tripeptid Thr-Ala-Asn, gdje je na karboksi krajnjem -OH bilo koji od L-Thr, D-Thr, Ile, Val, Gly ili Asn po izboru zamijenjen s -NH2; i
dva ostatka Cys povezana su disulfidnom vezom.
10. Spoj prema zahtjevu 10, gdje analog od Trp kao Xaa2 je 1-formiltriptofan i Xaa4 je po izboru Ala.
11. Spoj prema zahtjevu 10, sadrži sekvencu SEQ ID NO:25.
12. Spoj prema zahtjevu 9, 10 ili 11, dalje sadrži dodatnu peptidnu komponentu koja produžuje in vivo retenciju spoja; po izboru je dodatna peptidna komponenta peptid koji veže albumin; po izboru sadrži SEQ ID NO:39.
13. Spoj prema bilo kojem od prethodnih zahtjeva, koji sadrži peptid proizveden ekspresijom polinukleotida koji kodira peptid.
14. Spoj prema bilo kojem od prethodnih zahtjeva, gdje se spoj dobiva barem djelomično sintezom peptida.
15. Spoj prema bilo kojem od prethodnih zahtjeva, gdje je spoj PEGiliran; po izboru sadrži SEQ ID NO:36.
16. Spoj prema bilo kojem od prethodnih zahtjeva, koji inhibira aktivaciju komplementa s barem 100 puta jačom aktivnosti od peptida koji sadrži sekvencu SEQ ID NO:1 pod jednakim uvjetima ispitivanja.
17. Spoj prema zahtjevu 1, koji sadrži SEQ ID NO:23.
18. Spoj prema zahtjevu 1, koji sadrži SEQ ID NO:24.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US74020505P | 2005-11-28 | 2005-11-28 | |
| PCT/US2006/045539 WO2007062249A2 (en) | 2005-11-28 | 2006-11-28 | Potent compstatin analogs |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20120621T1 true HRP20120621T1 (hr) | 2012-09-30 |
Family
ID=37964706
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20120621TT HRP20120621T1 (hr) | 2005-11-28 | 2012-07-30 | Sna“ni analozi kompstatina |
Country Status (16)
| Country | Link |
|---|---|
| US (5) | US7888323B2 (hr) |
| EP (4) | EP3363810A1 (hr) |
| JP (2) | JP5302004B2 (hr) |
| CN (3) | CN101400692B (hr) |
| BR (1) | BRPI0619023B1 (hr) |
| CA (2) | CA2971349C (hr) |
| DK (1) | DK1960422T3 (hr) |
| ES (3) | ES2677619T3 (hr) |
| HK (1) | HK1124621A1 (hr) |
| HR (1) | HRP20120621T1 (hr) |
| IL (2) | IL191674A (hr) |
| PL (1) | PL1960422T3 (hr) |
| PT (1) | PT1960422E (hr) |
| RS (1) | RS52429B (hr) |
| RU (2) | RU2474586C2 (hr) |
| WO (1) | WO2007062249A2 (hr) |
Families Citing this family (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI1549333T1 (sl) * | 2002-09-20 | 2012-02-29 | Univ Pennsylvania | Analogi kompstatina z izboljĺ ano aktivnostjo |
| US8168584B2 (en) | 2005-10-08 | 2012-05-01 | Potentia Pharmaceuticals, Inc. | Methods of treating age-related macular degeneration by compstatin and analogs thereof |
| PL1960422T3 (pl) * | 2005-11-28 | 2012-11-30 | Univ Pennsylvania | Silne analogi kampstatyny |
| US8637325B2 (en) * | 2009-02-16 | 2014-01-28 | University Of Wyoming | Method and apparatus for pyrolysis-induced cleavage in peptides and proteins |
| CA2666843C (en) * | 2006-10-20 | 2015-06-16 | Celldex Therapeutics, Inc. | Treatment of age-related macular degeneration and other diseases of the eye |
| ES2545775T3 (es) * | 2007-02-05 | 2015-09-15 | Apellis Pharmaceuticals, Inc. | Análogos de compstatina para uso en el tratamiento de afecciones inflamatorias del sistema respiratorio |
| JP2009003429A (ja) * | 2007-05-18 | 2009-01-08 | Panasonic Corp | アクチュエータ |
| WO2008153963A1 (en) * | 2007-06-08 | 2008-12-18 | The Trustees Of The University Of Pennsylvania | Structure of compstatin-c3 complex and use for rational drug design |
| WO2009005651A2 (en) | 2007-06-29 | 2009-01-08 | The Trustees Of The University Of Pennsylvania | Complement-mediated thrombophilic assay |
| CA2701470A1 (en) * | 2007-10-02 | 2009-04-09 | Potentia Pharmaceuticals, Inc. | Sustained delivery of compstatin analogs from gels |
| EP2278987A4 (en) * | 2008-03-28 | 2012-08-22 | Apellis Ag | MODULATION AND REPLY / IMPROVEMENT OF THE COMPLEMENTARY SYSTEM IN THE TREATMENT OF TRAUMATISM |
| AU2009298684B2 (en) * | 2008-09-30 | 2015-11-19 | Konstantinos Ritis | Method of inhibiting biomaterial-induced procoagulant activity using complement inhibitors |
| ES2655389T3 (es) * | 2009-05-01 | 2018-02-19 | The Trustees Of The University Of Pennsylvania | Compstatina modificada con esqueleto peptídico y modificaciones c-terminales |
| US20110104154A1 (en) | 2009-10-30 | 2011-05-05 | Alcon Research, Ltd. | Single nucleotide polymorphisms and genes associated with age-related macular degeneration |
| US9358266B2 (en) | 2010-02-25 | 2016-06-07 | The Trustees Of The University Of Pennsylvania | Treatment of sepsis using complement inhibitors |
| US9421240B2 (en) | 2010-06-22 | 2016-08-23 | Apellis Pharmaceuticals, Inc. | Compstatin analogs for treatment of neuropathic pain |
| US20140113874A1 (en) * | 2010-09-23 | 2014-04-24 | The Trustees Of The University Of Pennsylvania | Modified Compstatin With Improved Stability And Binding Properties |
| JP6121330B2 (ja) * | 2010-09-28 | 2017-04-26 | アミリン・ファーマシューティカルズ, リミテッド・ライアビリティ・カンパニーAmylin Pharmaceuticals, Llc | 作用持続時間が増した改変ポリペプチド |
| WO2012095519A1 (en) | 2011-01-13 | 2012-07-19 | Leibniz-Institut Für Naturstoff-Forschung Und Infektionsbiologie | Potent inhibitors of complement activation |
| US20140219999A1 (en) | 2011-04-01 | 2014-08-07 | The Trustees Of The University Of Pennsylvania | Treatment of colon cancer using complement inhibitors |
| CA2835627C (en) * | 2011-05-11 | 2023-01-10 | Apellis Pharmaceuticals, Inc. | Cell-reactive, long-acting, or targeted compstatin analogs and uses thereof |
| WO2012162215A1 (en) | 2011-05-20 | 2012-11-29 | The Trustees Of The University Of Pennsylvania | Promotion of fracture healing using complement inhibitors |
| WO2012174055A1 (en) | 2011-06-13 | 2012-12-20 | The Trustees Of The University Of Pennsylvania | Wound healing using complement inhibitors |
| MX363606B (es) | 2011-06-22 | 2019-03-28 | Apellis Pharmaceuticals Inc | Uso de inhibidores del complemento en trastornos crónicos. |
| DK2753636T3 (da) * | 2011-09-07 | 2020-02-03 | Univ Pennsylvania | Compstatinanaloger med forbedret farmakokinetiske egenskaber |
| US20160067357A1 (en) * | 2012-08-17 | 2016-03-10 | Apellis Pharmaceuticals, Inc. | Detection of high risk drusen |
| LT3660033T (lt) | 2012-11-15 | 2021-07-12 | Apellis Pharmaceuticals, Inc. | Ilgo veikimo kompstatino analogai ir susijusios kompozicijos bei būdai |
| WO2014078734A2 (en) * | 2012-11-15 | 2014-05-22 | Apellis Pharmaceuticals, Inc. | Cell-reactive, long-acting, or targeted compstatin analogs and related compositions and methods |
| US9512180B2 (en) | 2012-12-19 | 2016-12-06 | The Regents Of The University Of California | Compstatin analogs |
| US10308687B2 (en) * | 2013-03-15 | 2019-06-04 | Apellis Pharmaceuticals, Inc. | Cell-penetrating compstatin analogs and uses thereof |
| CN105814205B (zh) | 2013-12-12 | 2019-11-19 | 阿尔尼拉姆医药品有限公司 | 补体成分iRNA组合物及其使用方法 |
| WO2015142701A1 (en) | 2014-03-17 | 2015-09-24 | The Trustees Of The University Of Pennsylvania | Compstatin analogs with improved potency and pharmacokinetic properties |
| CA2964620C (en) | 2014-12-23 | 2020-03-31 | Multi-Chem Group, Llc | Acrylate-based sulfur scavenging agents for use in oilfield operations |
| WO2017035401A1 (en) | 2015-08-26 | 2017-03-02 | Achillion Pharmaceuticals, Inc. | Amide compounds for treatment of immune and inflammatory disorders |
| WO2017035405A1 (en) | 2015-08-26 | 2017-03-02 | Achillion Pharmaceuticals, Inc. | Amino compounds for treatment of immune and inflammatory disorders |
| CN108431019A (zh) | 2015-10-07 | 2018-08-21 | 阿佩利斯制药有限公司 | 给药方案 |
| JP2020500157A (ja) | 2016-10-17 | 2020-01-09 | アペリス・ファーマシューティカルズ・インコーポレイテッドＡｐｅｌｌｉｓ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． | Ｃ３阻害のための組み合わせ治療 |
| EP3589628A4 (en) | 2017-03-01 | 2021-03-31 | Achillion Pharmaceuticals, Inc. | ARYL, HETEROARYL AND HETEROCYCLIC COMPOUNDS FOR TREATMENT OF MEDICAL DISEASES |
| WO2018160891A1 (en) | 2017-03-01 | 2018-09-07 | Achillion Pharmaceutical, Inc. | Pharmaceutical compounds for treatment of medical disorders |
| JP2020516607A (ja) | 2017-04-07 | 2020-06-11 | アペリス・ファーマシューティカルズ・インコーポレイテッドＡｐｅｌｌｉｓ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． | 投与レジメンならびに関連組成物および方法 |
| SG11202002940QA (en) | 2017-11-01 | 2020-04-29 | Alnylam Pharmaceuticals Inc | Complement component c3 irna compositions and methods of use thereof |
| EP3759120A1 (en) * | 2018-02-27 | 2021-01-06 | Zp Spv 3 K/S | Compstatin analogues and their medical uses |
| BR112020020369A2 (pt) * | 2018-04-06 | 2021-01-19 | The Trustees Of The University Of Pennsylvania | Análogos de compstatina com aumento de solubilidade e propriedades farmacocinéticas melhoradas |
| US11814391B2 (en) | 2018-09-06 | 2023-11-14 | Achillion Pharmaceuticals, Inc. | Macrocyclic compounds for the treatment of medical disorders |
| AU2019336238A1 (en) | 2018-09-06 | 2021-04-08 | Achillion Pharmaceuticals, Inc. | Morphic forms of Complement factor D inhibitors |
| US11807627B2 (en) | 2018-09-25 | 2023-11-07 | Achillon Pharmaceuticals, Inc. | Morphic forms of complement factor D inhibitors |
| US11510939B1 (en) | 2019-04-19 | 2022-11-29 | Apellis Pharmaceuticals, Inc. | RNAs for complement inhibition |
| BR112022003760A2 (pt) | 2019-08-27 | 2022-05-31 | Zp Spv 3 K/S | Análogos de compstatina e seus usos médicos |
| AR120267A1 (es) | 2019-10-22 | 2022-02-09 | Alnylam Pharmaceuticals Inc | COMPOSICIONES DE ARNi CONTRA EL COMPONENTE C3 DEL COMPLEMENTO Y SUS MÉTODOS DE USO |
| WO2021178607A1 (en) | 2020-03-05 | 2021-09-10 | Alnylam Pharmaceuticals, Inc. | Complement component c3 irna compositions and methods of use thereof for treating or preventing complement component c3-associated diseases |
| IL297680A (en) | 2020-04-30 | 2022-12-01 | Alnylam Pharmaceuticals Inc | IRNA compounds complement factor b (cfb) and methods of using them |
| KR20230009431A (ko) | 2020-05-12 | 2023-01-17 | 알렉시온 파마슈티칼스, 인코포레이티드 | 발작성 야간 혈색소뇨증의 치료를 위한 보체 인자 d 저해제를 단독으로 또는 항-c5 항체와 조합한 용도 |
| US20230287051A1 (en) | 2020-07-16 | 2023-09-14 | Zp Spv 3 K/S | Inhibitors of complement factor c3 and their medical uses |
| WO2022150260A1 (en) | 2021-01-05 | 2022-07-14 | Alnylam Pharmaceuticals, Inc. | COMPLEMENT COMPONENT 9 (C9) iRNA COMPOSITIONS AND METHODS OF USE THEREOF |
| WO2023044370A2 (en) | 2021-09-17 | 2023-03-23 | Alnylam Pharmaceuticals, Inc. | Irna compositions and methods for silencing complement component 3 (c3) |
| AR127477A1 (es) | 2021-10-29 | 2024-01-31 | Alnylam Pharmaceuticals Inc | COMPOSICIONES DE ARNi CONTRA EL FACTOR B DEL COMPLEMENTO (CFB) Y MÉTODOS DE USO DE LAS MISMAS |
| CN114605495A (zh) * | 2022-04-20 | 2022-06-10 | 广州市乾相生物科技有限公司 | 一种乳四肽的合成方法 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2295746A1 (fr) * | 1974-12-23 | 1976-07-23 | Francaise Coop Pharma | Nouveaux derives du tryptophane a activite nerveuse centrale renforcee |
| IT1179866B (it) * | 1984-12-12 | 1987-09-16 | Rotta Research Lab | Derivati del triptofano farmaceuticamente attivi e composizioni farmaceutiche che li contengono |
| US4576750A (en) | 1985-04-22 | 1986-03-18 | Merck & Co., Inc. | Tryptophan derivative |
| US5256642A (en) * | 1988-04-01 | 1993-10-26 | The Johns Hopkins University | Compositions of soluble complement receptor 1 (CR1) and a thrombolytic agent, and the methods of use thereof |
| US5167960A (en) * | 1988-08-03 | 1992-12-01 | New England Deaconess Hospital Corporation | Hirudin-coated biocompatible substance |
| JPH05508391A (ja) | 1990-04-23 | 1993-11-25 | リュクサニベルシテイト テ ユトレヒト | 環状ペプチドおよびそれらの使用 |
| JPH09510088A (ja) | 1994-03-03 | 1997-10-14 | アレクション・ファーマシューティカル・インク | 最終補体インヒビター融合遺伝子およびタンパク質 |
| 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 |
| CA2248772C (en) * | 1996-03-13 | 2007-06-12 | John D. Lambris | Novel peptides which inhibit complement activation |
| US6221621B1 (en) * | 1997-03-06 | 2001-04-24 | Bard Diagnostic Sciences, Inc. | Methods of screening for colorectal cancers in which a complement Factor I or related protein is associated |
| 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 |
| WO1999052539A1 (en) | 1998-04-10 | 1999-10-21 | Mayo Foundation For Medical Education And Research | Neo-tryptophan |
| SI1549333T1 (sl) * | 2002-09-20 | 2012-02-29 | Univ Pennsylvania | Analogi kompstatina z izboljĺ ano aktivnostjo |
| US7541032B2 (en) | 2002-09-20 | 2009-06-02 | Stichting Katholieke Universiteit | Antigen uptake receptor for Candida albicans on dendritic cells |
| EP1951279B1 (en) * | 2005-10-08 | 2017-04-12 | Apellis Pharmaceuticals, Inc. | Compstatin and analogs thereof for eye disorders |
| PL1960422T3 (pl) | 2005-11-28 | 2012-11-30 | Univ Pennsylvania | Silne analogi kampstatyny |
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