Title:
MACROCYCLIC COMPOUNDS FOR INHIBITION OF TUMOR NECROSIS FACTOR ALPHA
Document Type and Number:
WIPO Patent Application WO/2010/022249
Kind Code:
A3
Abstract:
The invention provides macrocyclic compounds of formula (I) and methods for their synthesis and use. In particular, the invention provides macrocyclic compounds that modulate the activity of tumor necrosis factor alpha and/or are useful in the treatment of medical conditions, such as, rheumatoid arthritis, psoriasis, and asthma.
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Inventors:
LEE JINBO (US)
BOND JULIAN F (US)
TERRETT NICHOLAS (US)
FAVALORO FRANK G (US)
WANG DANIEL (US)
BRIGGS TIMOTHY F (US)
SEIGAL BENJAMIN ADAM (US)
SUN WEI-CHUAN (US)
HALE STEPHEN P (US)
BOND JULIAN F (US)
TERRETT NICHOLAS (US)
FAVALORO FRANK G (US)
WANG DANIEL (US)
BRIGGS TIMOTHY F (US)
SEIGAL BENJAMIN ADAM (US)
SUN WEI-CHUAN (US)
HALE STEPHEN P (US)
Application Number:
PCT/US2009/054487
Publication Date:
April 15, 2010
Filing Date:
August 20, 2009
Export Citation:
Assignee:
ENSEMBLE DISCOVERY CORP (US)
LEE JINBO (US)
BOND JULIAN F (US)
TERRETT NICHOLAS (US)
FAVALORO FRANK G (US)
WANG DANIEL (US)
BRIGGS TIMOTHY F (US)
SEIGAL BENJAMIN ADAM (US)
SUN WEI-CHUAN (US)
HALE STEPHEN P (US)
LEE JINBO (US)
BOND JULIAN F (US)
TERRETT NICHOLAS (US)
FAVALORO FRANK G (US)
WANG DANIEL (US)
BRIGGS TIMOTHY F (US)
SEIGAL BENJAMIN ADAM (US)
SUN WEI-CHUAN (US)
HALE STEPHEN P (US)
International Classes:
C07D257/02; A61K31/395; A61P19/02; A61P25/28; A61P35/00; C07D273/00
Domestic Patent References:
| WO2003057722A2 | 2003-07-17 | |||
| WO2009047523A1 | 2009-04-16 |
Foreign References:
| US5952320A | 1999-09-14 |
Other References:
MIYAZAKI A ET AL: "Design and synthesis of novel type somatostatin analogs with antiproliferative activities on A431 tumor cells", TETRAHEDRON LETTERS, ELSEVIER, AMSTERDAM, vol. 45, no. 33, 9 August 2004 (2004-08-09), pages 6323 - 6327, XP004817751, ISSN: 0040-4039
R. SCHWYZER, B. ISELIN, W. RITTEL, P. SIEBER: "Synthesen zyklischer Polypeptide. c-Tetraglycyl und c-Hexaglycyl. Über aktivierte Ester VII", HELVETICA CHIMICA ACTA, vol. 39, no. 3, 1956, Zurich CH, pages 872 - 883, XP002555697
SHEH L ET AL: "CYCLIZATION STUDIES OF TETRAPEPTIDE HOMOLOGS", TETRAHEDRON LETTERS, vol. 26, no. 47, 1985, pages 5755 - 5758, XP002555698, ISSN: 0040-4039
GIOLITTI ALESSANDRO ET AL: "Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.", JOURNAL OF MEDICINAL CHEMISTRY 1 AUG 2002, vol. 45, no. 16, 1 August 2002 (2002-08-01), pages 3418 - 3429, XP002555699, ISSN: 0022-2623
ROTHE M ET AL: "MAKROCYCLISCHE PEPTIDE IN ANIONISCHEN POLYMERISATEN VON AMINOSAEURE-N-CARBONSAEUREANHYDRIDEN", ANGEWANDTE CHEMIE, WILEY - V C H VERLAG GMBH & CO. KGAA, WEINHEIM, DE, vol. 88, no. 10, 1 January 1976 (1976-01-01), pages 338/339, XP009033462, ISSN: 0044-8249
BEDNAREK MARIA A ET AL: "Selective, high affinity peptide antagonists of alpha-melanotropin action at human melanocortin receptor 4: Their synthesis and biological evaluation in vitro", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, WASHINGTON, US, vol. 44, no. 22, 3 October 2001 (2001-10-03), pages 3665 - 3672, XP009109532, ISSN: 0022-2623
R. SCHWYZER, B. ISELIN, W. RITTEL, P. SIEBER: "Synthesen zyklischer Polypeptide. c-Tetraglycyl und c-Hexaglycyl. Über aktivierte Ester VII", HELVETICA CHIMICA ACTA, vol. 39, no. 3, 1956, Zurich CH, pages 872 - 883, XP002555697
SHEH L ET AL: "CYCLIZATION STUDIES OF TETRAPEPTIDE HOMOLOGS", TETRAHEDRON LETTERS, vol. 26, no. 47, 1985, pages 5755 - 5758, XP002555698, ISSN: 0040-4039
GIOLITTI ALESSANDRO ET AL: "Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.", JOURNAL OF MEDICINAL CHEMISTRY 1 AUG 2002, vol. 45, no. 16, 1 August 2002 (2002-08-01), pages 3418 - 3429, XP002555699, ISSN: 0022-2623
ROTHE M ET AL: "MAKROCYCLISCHE PEPTIDE IN ANIONISCHEN POLYMERISATEN VON AMINOSAEURE-N-CARBONSAEUREANHYDRIDEN", ANGEWANDTE CHEMIE, WILEY - V C H VERLAG GMBH & CO. KGAA, WEINHEIM, DE, vol. 88, no. 10, 1 January 1976 (1976-01-01), pages 338/339, XP009033462, ISSN: 0044-8249
BEDNAREK MARIA A ET AL: "Selective, high affinity peptide antagonists of alpha-melanotropin action at human melanocortin receptor 4: Their synthesis and biological evaluation in vitro", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, WASHINGTON, US, vol. 44, no. 22, 3 October 2001 (2001-10-03), pages 3665 - 3672, XP009109532, ISSN: 0022-2623
Attorney, Agent or Firm:
DAVIS, Chad, E. et al. (Exchange PlaceBoston, MA, US)
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