Chemokine receptor modulators, production and use
First Claim
1. A chemokine receptor modulator comprising a chemokine polypeptide chain modified at its N-terminus with an aliphatic chain and one or more amino acid derivatives.
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Abstract
Chemokine receptor modulators comprising a chemically modified carboxyl-terminus (C-terminus) and/or amino-terminus (N-terminus) for modulating potency and pharmacokinetic properties, and methods of production and use are disclosed. The compounds and methods of the invention are exemplified by novel N-terminal, C-terminal and N/C-terminal analogs of CC and CXC chemokines. The chemokine receptor modulator analogs of the invention are useful for the treatment of disorders involving the naturally occurring chemokine that the analogs of the invention antagonize, such as for the treatment of HIV and AIDS related disorders and for the treatment of asthma, allergic rhinitis, atopic dermatitis, atheroma/atherosclerosis, organ transplant rejection, and rheumatoid arthritis.
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Citations
23 Claims
- 1. A chemokine receptor modulator comprising a chemokine polypeptide chain modified at its N-terminus with an aliphatic chain and one or more amino acid derivatives.
- 8. A chemokine receptor modulator comprising a chemokine polypeptide chain modified at its C-terminus with an aliphatic chain or polycyclic.
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12. A chemokine receptor modulator comprising a chemokine polypeptide chain modified at its N-terminus with an aliphatic chain and one or more amino acid derivatives, and at its C-terminus with an aliphatic chain or polycyclic.
- 13. A pharmaceutical composition comprising a chemokine receptor modulator, wherein said chemokine receptor modulator comprises a chemokine polypeptide chain modified at its N-terminus with an aliphatic chain and one or more amino acid derivatives, or a pharmaceutically acceptable salt thereof.
- 15. A pharmaceutical composition comprising a chemokine receptor modulator, wherein said chemokine receptor modulator comprises a chemokine polypeptide chain modified at its C-terminus with an aliphatic chain or polycyclic, or a pharmaceutically acceptable salt thereof.
- 18. A pharmaceutical composition comprising a chemokine receptor modulator comprising a chemokine polypeptide chain modified at its N-terminus with an aliphatic chain and one or more amino acid derivatives, and at its C-terminus with an aliphatic chain or polycyclic, or a pharmaceutically acceptable salt thereof.
- 20. A method of treating a disease state in mammals that is alleviated by treatment with a chemokine receptor modulator, which method comprises administering to a mammal in need of such a treatment a therapeutically effective amount of a chemokine receptor modulator, wherein said chemokine receptor modulator comprises a chemokine polypeptide chain (A) modified at its N-terminus with an aliphatic chain and one or more amino acid derivatives, (B) modified at its C-terminus with an aliphatic chain or polycyclic, or (C) modified at its N-terminus with an aliphatic chain and one or more amino acid derivatives, and at its C-terminus with an aliphatic chain or polycyclic.
Specification