Patent(s) and the Corresponding Patented Drug(s) |
Top |
United States Patent and Trademark Office (USPTO) |
Patent ID |
US9663511 |
Title |
Sphingosine 1-phosphate receptor antagonists |
Abstract |
The present invention relates to sphingosine-1-phosphate (S1P) receptors and compounds of the general formula: that are useful in the treatment and prevention of conditions associated with such receptors. More specifically, the present invention relates to the synthesis and use of sphingosine 1-phosphate receptor 2 (S1P2) antagonists that are useful in the treatment of cancer, atherosclerosis, diabetic retinopathy, and other inflammatory diseases. Among these inflammatory diseases that could be treated with these S1P2 antagonist are those characterized by fibrosis including chronic lung disease, chronic kidney and liver disease, chronic heart disease, and skin diseases such as sclerosis/scleroderma. The S1P2 antagonists can also be used in the treatment of glioblastoma multiforme (brain cancer), pediatric neuroblastoma, and other cancers. |
Applicant(s) |
Arroyo BioSciences, LLC |
Representative Drug(s) |
D0QU9I |
Drug Info
|
IC50 = 10 nM |
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[1] |
2
|
D0K4BI
|
Drug Info
|
IC50 = 11 nM
|
[1] |
3
|
D0J5YV
|
Drug Info
|
IC50 = 52 nM
|
[1] |
Patent ID |
US9663511 |
Title |
Sphingosine 1-phosphate receptor antagonists |
Abstract |
The present invention relates to sphingosine-1-phosphate (S1P) receptors and compounds of the general formula: that are useful in the treatment and prevention of conditions associated with such receptors. More specifically, the present invention relates to the synthesis and use of sphingosine 1-phosphate receptor 2 (S1P2) antagonists that are useful in the treatment of cancer, atherosclerosis, diabetic retinopathy, and other inflammatory diseases. Among these inflammatory diseases that could be treated with these S1P2 antagonist are those characterized by fibrosis including chronic lung disease, chronic kidney and liver disease, chronic heart disease, and skin diseases such as sclerosis/scleroderma. The S1P2 antagonists can also be used in the treatment of glioblastoma multiforme (brain cancer), pediatric neuroblastoma, and other cancers. |
Applicant(s) |
Arroyo BioSciences, LLC |
Representative Drug(s) |
D0QU9I |
Drug Info
|
IC50 = 10 nM |
Click to Show More |
[1] |
2
|
D0K4BI
|
Drug Info
|
IC50 = 11 nM
|
[1] |
3
|
D0J5YV
|
Drug Info
|
IC50 = 52 nM
|
[1] |
Patent ID |
US9663511 |
Title |
Sphingosine 1-phosphate receptor antagonists |
Abstract |
The present invention relates to sphingosine-1-phosphate (S1P) receptors and compounds of the general formula: that are useful in the treatment and prevention of conditions associated with such receptors. More specifically, the present invention relates to the synthesis and use of sphingosine 1-phosphate receptor 2 (S1P2) antagonists that are useful in the treatment of cancer, atherosclerosis, diabetic retinopathy, and other inflammatory diseases. Among these inflammatory diseases that could be treated with these S1P2 antagonist are those characterized by fibrosis including chronic lung disease, chronic kidney and liver disease, chronic heart disease, and skin diseases such as sclerosis/scleroderma. The S1P2 antagonists can also be used in the treatment of glioblastoma multiforme (brain cancer), pediatric neuroblastoma, and other cancers. |
Applicant(s) |
Arroyo BioSciences, LLC |
Representative Drug(s) |
D0QU9I |
Drug Info
|
IC50 = 10 nM |
Click to Show More |
[1] |
2
|
D0K4BI
|
Drug Info
|
IC50 = 11 nM
|
[1] |
3
|
D0J5YV
|
Drug Info
|
IC50 = 52 nM
|
[1] |
Patent ID |
US8975409 |
Title |
Phenyl derivative |
Abstract |
The compound represented by the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P2-mediated diseases such as diseases resulting from vascular constriction, fibrosis and respiratory diseases. |
Applicant(s) |
ONO Pharmaceutical Co., Ltd. |
Representative Drug(s) |
D0C4AW |
Drug Info
|
IC50 = 3 nM |
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[2] |
2
|
D0PW0R
|
Drug Info
|
IC50 = 6.2 nM
|
[2] |
3
|
D0T8FV
|
Drug Info
|
IC50 = 1200 nM
|
[2] |
Patent ID |
US8975409 |
Title |
Phenyl derivative |
Abstract |
The compound represented by the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P2-mediated diseases such as diseases resulting from vascular constriction, fibrosis and respiratory diseases. |
Applicant(s) |
ONO Pharmaceutical Co., Ltd. |
Representative Drug(s) |
D0C4AW |
Drug Info
|
IC50 = 3 nM |
Click to Show More |
[2] |
2
|
D0PW0R
|
Drug Info
|
IC50 = 6.2 nM
|
[2] |
3
|
D0T8FV
|
Drug Info
|
IC50 = 1200 nM
|
[2] |
Patent ID |
US8975409 |
Title |
Phenyl derivative |
Abstract |
The compound represented by the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P2-mediated diseases such as diseases resulting from vascular constriction, fibrosis and respiratory diseases. |
Applicant(s) |
ONO Pharmaceutical Co., Ltd. |
Representative Drug(s) |
D0C4AW |
Drug Info
|
IC50 = 3 nM |
Click to Show More |
[2] |
2
|
D0PW0R
|
Drug Info
|
IC50 = 6.2 nM
|
[2] |
3
|
D0T8FV
|
Drug Info
|
IC50 = 1200 nM
|
[2] |