Selective inhibitors and allosteric activators of sphingosine kinase

Robert Bittman (Inventor), Nigel Pyne (Inventor), Susan Pyne (Inventor), Dong Jae Baek (Inventor), Zheng Liu (Inventor), Hoe-Sup Byun (Inventor)

Research output: Patent

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Abstract

Sphingosine 1-phosphate (S1P) is involved in hyper-proliferative diseases, such as cancer and vascular remodeling in pulmonary arterial hypertension. Inhibitors of sphingosine kinase 1 and 2 (SK1 and SK2), which catalyze the synthesis of S1P, may be useful anti- proliferative agents. We have synthesized a series of sphingosine-based inhibitors of SK and SK2. Also provided in this invention are compounds that activate SK1 which can be used in diseases such as fibrosis, where intracellular S1P is anti-fibrotic.
Original languageEnglish
Patent numberPCT/GB2014/050264
IPCC07D401/04
Priority date31/01/13
Publication statusPublished - 7 Aug 2014

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Sphingosine
Pulmonary Hypertension
Fibrosis
sphingosine kinase
sphingosine 1-phosphate
Neoplasms
Vascular Remodeling

Keywords

  • inhibitors
  • synthesis
  • anti-proliferative agents

Cite this

Bittman, R., Pyne, N., Pyne, S., Baek, D. J., Liu, Z., & Byun, H-S. (2014). IPC No. C07D401/04. Selective inhibitors and allosteric activators of sphingosine kinase. (Patent No. PCT/GB2014/050264).
Bittman, Robert (Inventor) ; Pyne, Nigel (Inventor) ; Pyne, Susan (Inventor) ; Baek, Dong Jae (Inventor) ; Liu, Zheng (Inventor) ; Byun, Hoe-Sup (Inventor). / Selective inhibitors and allosteric activators of sphingosine kinase. IPC No.: C07D401/04. Patent No.: PCT/GB2014/050264.
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abstract = "Sphingosine 1-phosphate (S1P) is involved in hyper-proliferative diseases, such as cancer and vascular remodeling in pulmonary arterial hypertension. Inhibitors of sphingosine kinase 1 and 2 (SK1 and SK2), which catalyze the synthesis of S1P, may be useful anti- proliferative agents. We have synthesized a series of sphingosine-based inhibitors of SK and SK2. Also provided in this invention are compounds that activate SK1 which can be used in diseases such as fibrosis, where intracellular S1P is anti-fibrotic.",
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Bittman, R, Pyne, N, Pyne, S, Baek, DJ, Liu, Z & Byun, H-S 2014, Selective inhibitors and allosteric activators of sphingosine kinase, Patent No. PCT/GB2014/050264, IPC No. C07D401/04.

Selective inhibitors and allosteric activators of sphingosine kinase. / Bittman, Robert (Inventor); Pyne, Nigel (Inventor); Pyne, Susan (Inventor); Baek, Dong Jae (Inventor); Liu, Zheng (Inventor); Byun, Hoe-Sup (Inventor).

IPC No.: C07D401/04. Patent No.: PCT/GB2014/050264.

Research output: Patent

TY - PAT

T1 - Selective inhibitors and allosteric activators of sphingosine kinase

AU - Bittman, Robert

AU - Pyne, Nigel

AU - Pyne, Susan

AU - Baek, Dong Jae

AU - Liu, Zheng

AU - Byun, Hoe-Sup

PY - 2014/8/7

Y1 - 2014/8/7

N2 - Sphingosine 1-phosphate (S1P) is involved in hyper-proliferative diseases, such as cancer and vascular remodeling in pulmonary arterial hypertension. Inhibitors of sphingosine kinase 1 and 2 (SK1 and SK2), which catalyze the synthesis of S1P, may be useful anti- proliferative agents. We have synthesized a series of sphingosine-based inhibitors of SK and SK2. Also provided in this invention are compounds that activate SK1 which can be used in diseases such as fibrosis, where intracellular S1P is anti-fibrotic.

AB - Sphingosine 1-phosphate (S1P) is involved in hyper-proliferative diseases, such as cancer and vascular remodeling in pulmonary arterial hypertension. Inhibitors of sphingosine kinase 1 and 2 (SK1 and SK2), which catalyze the synthesis of S1P, may be useful anti- proliferative agents. We have synthesized a series of sphingosine-based inhibitors of SK and SK2. Also provided in this invention are compounds that activate SK1 which can be used in diseases such as fibrosis, where intracellular S1P is anti-fibrotic.

KW - inhibitors

KW - synthesis

KW - anti-proliferative agents

UR - http://patentscope.wipo.int/search/en/WO2014118556

M3 - Patent

M1 - PCT/GB2014/050264

ER -

Bittman R, Pyne N, Pyne S, Baek DJ, Liu Z, Byun H-S, inventors. Selective inhibitors and allosteric activators of sphingosine kinase. C07D401/04. 2014 Aug 7.