Chemokine CCR5 antagonists incorporating a 4-aminopiperidine scaffold

Expert Opinion on Therapeutic Patents

Volumn 13, Issue 9, 2003, Pages 1469-1473

[No Author Info available]

Author keywords

CCR5 antagonists; Chemokine; HIV 1; Inflammation; Macrophage inflammatory protein (MIP) 1 ; RANTES

Indexed keywords

4 AMINOPIPERIDINE DERIVATIVE; 4 [(4 BROMOPHENYL)(ETHOXYIMINO)METHYL] 1' [(2,4 DIMETHYL 3 PYRIDINYL)CARBONYL] 4' METHYL 1,4' BIPIPERIDINE; AZD 0275; AZD 0475; AZD 7140; AZD 8309; CHEMOKINE RECEPTOR CCR5; MARAVIROC; N [4 [[[6,7 DIHYDRO 2 (4 METHYLPHENYL) 5H BENZOCYCLOHEPTEN 8 YL]CARBONYL]AMINO]BENZYL] N,N DIMETHYL 2H TETRAHYDROPYRAN 4 AMINIUM CHLORIDE; PIPERAZINE DERIVATIVE; PIPERIDINE DERIVATIVE; TROPANE DERIVATIVE; UNCLASSIFIED DRUG; VICRIVIROC;

ARTICLE; AUTOIMMUNE DISEASE; CLINICAL TRIAL; DRUG ACTIVITY; DRUG DESIGN; DRUG POTENCY; DRUG STRUCTURE; HAMSTER; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; INFLAMMATORY DISEASE; NONHUMAN; RHEUMATOID ARTHRITIS; STRUCTURE ACTIVITY RELATION;

EID: 0141740276     PISSN: 13543776     EISSN: None     Source Type: Journal    
DOI: 10.1517/eotp.13.9.1469.22939     Document Type: Article

References (11)

1. SIMMONS G, CLAPHAM PR, PICARD L et al.: Potent inhibition of HIV-1 infectivity in macrophages and lymphocytes by a novel CCR5 antagonist. Science (1997) 276(5310):276-279.
2. LE Y, SHEN W, LI B, GONG W et al.: A new insight into the role of 'old' chemotactic peptide receptors FPR and FPRL1: down-regulation of chemokine receptors CCR5 and CXCR4. Forum (Genova) (1999) 9(4):299-314.
3. GABUZDA D, WANG J: Chemokine receptors and mechanisms of cell death in HIV neuropathogenesis. J. Neurovirol. (2000) 6(suppl.1):S24-32.
4. AGRAWAL L, ALKHATIB G: Chemokine receptors: emerging opportunities for new anti-HIV therapies. Expert Opin. Ther. Targets (2001) 5(3):303-326.
5. FUJII N, NAKASHIMA H, TAMAMURA H: The therapeutic potential of CXCR4 antagonists in the treatment of HIV. Expert Opin. Investig. Drugs (2003) 12(2):185-195.
6. SHIRAISHI M, ARAMAKI Y, SETO M et al.: Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety. J. Med. Chem. (2000) 43(10):2049-2063.
7. DORR P, MACARTNEY M, RICKETT G et al.: UK-427857, a novel small molecule HIV entry inhibitor is a specific antagonist of the chemokine receptor CCR5. 10th Conference on Retroviruses and Opportunistic Infections, Boston, MA, USA (February 2003).
8. PALANI A, SHAPIRO S, CLADER JW et al.: Discovery of 4-[(Z)-(4-bromophenyl)- (ethoxyimino)methyl]-1′-[(2,4-dimethyl-3-pyridinyl)carbonyll- 4′-methyl-1,4′-bipiperidine N-oxide (Sch-351125): an orally bioavailable human CCR5 antagonist for the treatment of HIV infection. J. Med. Chem. (2001) 44(21):3339-3342.
9. ESTE JA: Sch-351125 and Sch-350634. Schering-Plough. Curr. Opin. Investig. Drugs (2002) 3(3):379-383.
10. FINKE PE, OATES B, MILLS SG et al.: Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: synthesis and structure-activity relationships for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)- N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes. Bioorg. Med. Chem. Lett. (2001) 11(18):2475-2479.
11. YANG YF, MUKAI T, GAO P et al.: A non-peptide CCR5 antagonist inhibits collagen-induced arthritis by modulating T cell migration without affecting anti-collagen T cell responses. Eur. J. Immunol. (2002) 32(8):2124-2132.