Patent(s) and the Corresponding Patented Drug(s) |
Top |
United States Patent and Trademark Office (USPTO) |
Patent ID |
US9777010 |
Title |
Substituted 4-phenylpiperidines, their preparation and use |
Abstract |
The present invention provides a compound having the structure: whereinR1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl, wherein two or more of R1, R2, R3, R4, or R5 are other than H; R6 is H, OH, or halogen; andB is a substituted or unsubstituted heterobicycle,wherein when R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is H, R2 is CF3, R3 is H, R4 is CF3, and R5 is H, or R1 is Cl, R2 is H, R3 is H, R4 is F, and R5 is H, or R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is CF3, R2 is F, R3 is H, R4 is H, and R5 is H, or R1 is Cl, R2 is F, R3 is H, R4 is H, and R5 is H, then B is other than or a pharmaceutically acceptable salt thereof. |
Applicant(s) |
THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK |
Representative Drug(s) |
D05AIC |
Drug Info
|
IC50 = 3.45 nM |
[1] |
Patent ID |
US9434727 |
Title |
Substituted 4-phenylpiperidines, their preparation and use |
Abstract |
The present invention provides a compound having the structure: whereinR1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl, wherein two or more of R1, R2, R3, R4, or R5 are other than H; R6 is H, OH, or halogen; andB is a substituted or unsubstituted heterobicycle,wherein when R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is H, R2 is CF3, R3 is H, R4 is CF3, and R5 is H, or R1 is Cl, R2 is H, R3 is H, R4 is F, and R5 is H, or R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is CF3, R2 is F, R3 is H, R4 is H, and R5 is H, or R1 is Cl, R2 is F, R3 is H, R4 is H, and R5 is H, then B is other than or a pharmaceutically acceptable salt thereof. |
Applicant(s) |
THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK |
Representative Drug(s) |
D0YU9U |
Drug Info
|
IC50 = 16 nM |
Click to Show More |
[2] |
2
|
D0K0IZ
|
Drug Info
|
IC50 = 21 nM
|
[2] |
3
|
D04BAA
|
Drug Info
|
IC50 = 833 nM
|
[2] |
Patent ID |
US9434727 |
Title |
Substituted 4-phenylpiperidines, their preparation and use |
Abstract |
The present invention provides a compound having the structure: whereinR1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl, wherein two or more of R1, R2, R3, R4, or R5 are other than H; R6 is H, OH, or halogen; andB is a substituted or unsubstituted heterobicycle,wherein when R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is H, R2 is CF3, R3 is H, R4 is CF3, and R5 is H, or R1 is Cl, R2 is H, R3 is H, R4 is F, and R5 is H, or R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is CF3, R2 is F, R3 is H, R4 is H, and R5 is H, or R1 is Cl, R2 is F, R3 is H, R4 is H, and R5 is H, then B is other than or a pharmaceutically acceptable salt thereof. |
Applicant(s) |
THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK |
Representative Drug(s) |
D0YU9U |
Drug Info
|
IC50 = 16 nM |
Click to Show More |
[2] |
2
|
D0K0IZ
|
Drug Info
|
IC50 = 21 nM
|
[2] |
3
|
D04BAA
|
Drug Info
|
IC50 = 833 nM
|
[2] |
Patent ID |
US9434727 |
Title |
Substituted 4-phenylpiperidines, their preparation and use |
Abstract |
The present invention provides a compound having the structure: whereinR1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl, wherein two or more of R1, R2, R3, R4, or R5 are other than H; R6 is H, OH, or halogen; andB is a substituted or unsubstituted heterobicycle,wherein when R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is H, R2 is CF3, R3 is H, R4 is CF3, and R5 is H, or R1 is Cl, R2 is H, R3 is H, R4 is F, and R5 is H, or R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is CF3, R2 is F, R3 is H, R4 is H, and R5 is H, or R1 is Cl, R2 is F, R3 is H, R4 is H, and R5 is H, then B is other than or a pharmaceutically acceptable salt thereof. |
Applicant(s) |
THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK |
Representative Drug(s) |
D0YU9U |
Drug Info
|
IC50 = 16 nM |
Click to Show More |
[2] |
2
|
D0K0IZ
|
Drug Info
|
IC50 = 21 nM
|
[2] |
3
|
D04BAA
|
Drug Info
|
IC50 = 833 nM
|
[2] |
Patent ID |
US8853215 |
Title |
Derivatives of N-acyl-N-phenylpiperazine useful (inter alia) for the prophylaxis or treatment of diabetes |
Abstract |
The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specification, which has a superior RBP4-lowering action and is useful as a pharmaceutical composition for the prophylaxis or treatment of a disease or condition mediated by an increase in RBP4. |
Applicant(s) |
Takeda Pharmaceutical Company Limited |
Representative Drug(s) |
D0IV0E |
Drug Info
|
IC50 = 3.8 nM |
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[3] |
2
|
D0D5AI
|
Drug Info
|
IC50 = 54 nM
|
[3] |
3
|
D01KKC
|
Drug Info
|
IC50 = 540 nM
|
[3] |
Patent ID |
US8853215 |
Title |
Derivatives of N-acyl-N-phenylpiperazine useful (inter alia) for the prophylaxis or treatment of diabetes |
Abstract |
The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specification, which has a superior RBP4-lowering action and is useful as a pharmaceutical composition for the prophylaxis or treatment of a disease or condition mediated by an increase in RBP4. |
Applicant(s) |
Takeda Pharmaceutical Company Limited |
Representative Drug(s) |
D0IV0E |
Drug Info
|
IC50 = 3.8 nM |
Click to Show More |
[3] |
2
|
D0D5AI
|
Drug Info
|
IC50 = 54 nM
|
[3] |
3
|
D01KKC
|
Drug Info
|
IC50 = 540 nM
|
[3] |
Patent ID |
US8853215 |
Title |
Derivatives of N-acyl-N-phenylpiperazine useful (inter alia) for the prophylaxis or treatment of diabetes |
Abstract |
The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specification, which has a superior RBP4-lowering action and is useful as a pharmaceutical composition for the prophylaxis or treatment of a disease or condition mediated by an increase in RBP4. |
Applicant(s) |
Takeda Pharmaceutical Company Limited |
Representative Drug(s) |
D0IV0E |
Drug Info
|
IC50 = 3.8 nM |
Click to Show More |
[3] |
2
|
D0D5AI
|
Drug Info
|
IC50 = 54 nM
|
[3] |
3
|
D01KKC
|
Drug Info
|
IC50 = 540 nM
|
[3] |
Patent ID |
US8586571 |
Title |
Heterocyclic compound |
Abstract |
The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4. |
Applicant(s) |
Takeda Pharmaceutical Company Limited |
Representative Drug(s) |
D0J9YV |
Drug Info
|
IC50 = 20 nM |
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[4] |
2
|
D0I1LE
|
Drug Info
|
IC50 = 36 nM
|
[4] |
3
|
D08PYU
|
Drug Info
|
IC50 = 210 nM
|
[4] |
Patent ID |
US8586571 |
Title |
Heterocyclic compound |
Abstract |
The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4. |
Applicant(s) |
Takeda Pharmaceutical Company Limited |
Representative Drug(s) |
D0J9YV |
Drug Info
|
IC50 = 20 nM |
Click to Show More |
[4] |
2
|
D0I1LE
|
Drug Info
|
IC50 = 36 nM
|
[4] |
3
|
D08PYU
|
Drug Info
|
IC50 = 210 nM
|
[4] |
Patent ID |
US8586571 |
Title |
Heterocyclic compound |
Abstract |
The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4. |
Applicant(s) |
Takeda Pharmaceutical Company Limited |
Representative Drug(s) |
D0J9YV |
Drug Info
|
IC50 = 20 nM |
Click to Show More |
[4] |
2
|
D0I1LE
|
Drug Info
|
IC50 = 36 nM
|
[4] |
3
|
D08PYU
|
Drug Info
|
IC50 = 210 nM
|
[4] |
Patent ID |
US10072016 |
Title |
Substituted 4-phenylpiperidines, their preparation and use |
Abstract |
The present invention provides a compound having the structure: whereinR1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl, wherein two or more of R1, R2, R3, R4, or R5 are other than H; R6 is H, OH, or halogen; andB is a substituted or unsubstituted heterobicycle,wherein when R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is H, R2 is CF3, R3 is H, R4 is CF3, and R5 is H, or R1 is Cl, R2 is H, R3 is H, R4 is F, and R5 is H, or R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is CF3, R2 is F, R3 is H, R4 is H, and R5 is H, or R1 is Cl, R2 is F, R3 is H, R4 is H, and R5 is H, then B is other than or a pharmaceutically acceptable salt thereof. |
Applicant(s) |
THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK |
Representative Drug(s) |
D02TPQ |
Drug Info
|
IC50 = 8 nM |
[5] |