http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RS-51950-B
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_2ca2e4410855da087e11bf3eea8933fa |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K38-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K7-54 |
| filingDate | 2008-05-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cf1dc3a8608dab0078c1553550572dd9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_391c4604da4f3577be62e0ef4ebf564e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f53c91c8c2f747d74da70479773dee1d |
| publicationDate | 2012-02-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | RS-51950-B |
| titleOfInvention | CYCLIC PEPTIDE ANTAGONISTS CXCR4 |
| abstract | CYCLIC PEPTIDE ANTAGONISTS CXCR4. A lactam-cyclized peptide of formula I: R1 - cyclopd - Tyr - X3 - DArg - 2Nal - Gly - X7] - X8 - X9 - X10 - R2 (SEQ ID (I) NO: 1), characterized in that: a) lactam is given is formed by forming an amide bond between the side chain of the amino group in Xi and the side chain of the carboxyl group X7, wherein X1 and X7, the pair are selected from the group consisting of (D / L) Ag1 / Glu, Dab / Glu, and Dap / Glu, and R1 is Ac or n-hexanoyl; orb) the lactam given is formed by forming an amide bond between the side chain of the carboxyl group Xt and the side chain of the amino group X7, where X1 and X7, a pair selected from the group consisting of Asp / (D / L) Agl, Asp / Dab, Asp / Dap , Glu / (D / L) Agl, Glu / Dab, Glu / Dap, Glu / DDap, and Glu / Lys, and R1 is Ac or Bz, or where Xi and X7 are a pair selected from the group consisting of succinyl / ( D / L) Agl, succinyl / Dab, succinyl / Dap, succinyl / Lys, and succinyl / Orn, and Ri is absent; ilic) the lactam given is formed by forming an amide bond between the α-amino group in Xi and the side chain of the carboxyl group X7, where X1 and X7, a pair selected from the group consisting of Ala / Glu, Ala / DGlu, DAla / Glu, DAla / DGlu, Dap (Ac) / Glu, Gly / Asp, Gly / Glu, Gly / DGIu, Leu / Glu, Leu / DGlu, Lys / DGIu, Lys (Ac) / Glu, 2Nal / Glu, Phe / Glu, Phe / DGlu, DPhe / Glu, and DPhe / DGlu, and R1 is absent; ilid) the lactam given is formed by forming an amide bond between the non-amino group of the non-side chain on X1 and the side chain of the carboxyl group X7, where X1 and X7, a pair selected from the group consisting of (3-Ala / Asp, (3- Ala / Glu, 5-amino-valeryl / Asp, 5-aminovaleryl / Glu, 4-AMB / Glu, 4-AMPA / Asp, and 4-AMPA / Glu, and R, is absent; or e) lactam is formed by formation amide bonds between the α-amino group X2 and the side chain of the carboxyl group X7, wherein X2 and X7, a pair selected from the group consisting of Tyr / Asp, Tyr / Glu, and Tyr / DGIu, and each of R1 and X1 is absent; R1 is a substituent on the a-amino group in X1 when X1 contains an n a-amino group and the a-amino group provided is not a component of the lactam amide bond, selected from the group consisting of Ac, Bz, and n-hexanoyl, or is absent, where X1 is selected from the group consisting of (D / L) Agl, Asp, Dab, Dap, and Glu; X1 is selected from the group consisting of (D / L) Agl, Ala, (3-Ala, DAla, 5-aminovaleryl, 4 -AMB, 4-AMPA, Asp, Dab, Dap, Dap (Ac), Glu, Gly, Leu, Lys, Lys (Ac), 2Nal, Phe, DPhe, and succinyl, or absent; X3 is from selected from the group consisting of Arg, Lys, Lys (iPr), and Lys (Me2); X7 is selected from the group consisting of (D / L) Agl, Asp, Dab, Dap, DDap, Glu, DGIu, Lys, and Om; X8 is selected from the group consisting of (3-Ala, Arg, DArg, Gly, Lys , Lys (iPr), and Om, or absent; X9 is selected from the group consisting of Gly, 2Nal, D2Nal, and DPhe, or absent; X10 is 2Nal, or absent; whereby, when X8 is absent, then each of X9 and X10 is absent, and when X9 is absent, then X10 is absent, iR2 is selected from the group consisting of NH2 and NHEt, Ilinjeg's pharmaceutically acceptable salt. The application contains 12 more claims. |
| priorityDate | 2007-05-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 48.