| Patent(s) and the Corresponding Patented Drug(s) |
Top |
| World Intellectual Property Organization (WIPO) |
| Patent ID |
WO2014121764 |
| Title |
2-Substituted-6-Biarylmethylamino-9-Cyclopentyl-9H-Purine Derivatives, Use Thereof As Medicaments, and Pharmaceutical Compositions. |
| Abstract |
This invention relates to novel 2-substituted-6-biarylmethylamino-9-cyclopentyl-9H-purine derivatives, showing activity as specific inhibitors of growth and angiogenesis of hepatocellular carcinoma. The invention further includes pharmaceutical compositions containing the 2-substituted-6-biarylmethylamino-9-cyclopentylpurines. |
| Applicant(s) |
Univerzita Palackeho V Olomouci et al |
| Representative Drug(s) |
D07DUX |
Drug Info
|
IC50 = nM range |
[1] |
| Patent ID |
WO2013156780 |
| Title |
Therapeutic Compounds. |
| Abstract |
The present invention relates to compounds of formula (I): wherein R1 is NH2 or NHMe; R2 is halo; and one of R3 or R4 is hydrogen and the other is selected from ...O2NH2, -SO2NHMe or ...O2NMe2, -SO2NHEt, or -SO2NEt2; or a pharmaceutically acceptable salt or solvate thereof. The compounds of formula (I) are inhibitors of protein kinases, especially cyclic dependent kinases (CDKs) such as CDK9. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which protein kinase/CDK activity is implicated. |
| Applicant(s) |
Changzhou Le Sun Pharmaceuticals Limited |
| Representative Drug(s) |
D01CJE |
Drug Info
|
Ki = single digit nM |
[1] |
| Patent ID |
WO2010103486 |
| Title |
Pyrazolo[1,5-A]-1,3,5-Triazine Derivatives, Preparation Thereof, and Therapeutic Use Thereof. |
| Abstract |
The present invention relates to a compound of the following formula (I), where R1 is a (C1-C6)alkyl group or a (C3-C6)cycloalkyl group; R2 and R3 are, independently, a (C1-C6)alkyl group, a (C3-C6)cycloalkyl group, a (C1-C6)alkenyl group, a (C1-C6)fluoroalkyl group, a (C1-C3)fluoroalkoxy group, or a (C1-C6)alkoxy(C1-C6)alkyl group substituted (i) by one to three hydroxyl groups or (ii) by an NRaRb, or R2 is a pyrrolidinylmethyl group substituted by one to three hydroxyl groups, assuming that R9 can be a hydrogen atom, or alternatively R2 and R3 are a heterocyclic compound with the nitrogen atom thereof; X and Y are, independently, a phenyl group or heteroaryl group, said heteroaryl and phenyl groups being substitutable, said heteroaryl group being selected from among a thienyl group, a pyridyl group, a pyrimidinyl group, a thiazolyl group, a pyrrolyl group, and furanyl group, as well as to the pharmaceutically acceptable salts thereof. The present invention also relates to the composition containing same, as well as to the therapeutic use thereof. |
| Applicant(s) |
Center Nat Rech Scient |
| Representative Drug(s) |
D0NB7Y |
Drug Info
|
IC50 = 19 nM |
[1] |
| Patent ID |
WO2010075542 |
| Title |
Cdk Inhibitors. |
| Abstract |
The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer. |
| Applicant(s) |
Curis, Inc |
| Representative Drug(s) |
D0M5DX |
Drug Info
|
IC50 < 100 nM |
[1] |
| Patent ID |
WO2010069833 |
| Title |
Pyrimidin- 2 -Ylamino Derivatives and Their Use To Treat Inflammation. |
| Abstract |
Compounds of formula (I) modulate JNK wherein X1 and X2 are each simultaneously N or CH; X3 is CH-R2 or N-SO2R, where R is lower alkyl; R1 is aryl or heteroaryl, substituted with 0-3 lower alkyl radicals; R2 is formula (II), where R3 is H, lower acyl, or an amino acid, or a pharmaceutically acceptable salt thereof. |
| Applicant(s) |
F. Hoffmann-La Roche Ag |
| Representative Drug(s) |
D0H4HD |
Drug Info
|
IC50 = 1520 nM |
[2] |
| Patent ID |
WO2010020675 |
| Title |
Pyrrolopyrimidine Compounds As Cdk Inhibitors. |
| Abstract |
The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein. |
| Applicant(s) |
Novartis Ag |
| Representative Drug(s) |
D08KKC |
Drug Info
|
IC50 < 1 nM |
[1] |
| Patent ID |
WO2009036016 |
| Title |
Cdk Inhibitors Containing A Zinc Binding Moiety. |
| Abstract |
The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The compounds of the invention may further act as HDAC inhibitors. |
| Applicant(s) |
Curis, Inc |
| Representative Drug(s) |
D0M5DX |
Drug Info
|
IC50 < 100 nM |
[1] |
| Patent ID |
WO2008028860 |
| Title |
Benzotriazole Kinase Modulators. |
| Abstract |
The invention is concerned with novel benzotriazole derivatives of Formula (I) Wherein R, R1, R2, R3, and m are as defined in the description and the claims, as well as physiologically acceptable salts thereof. These compounds are JNK and CDK modulators. |
| Applicant(s) |
F. Hoffmann-La Roche Ag |
| Representative Drug(s) |
D0H4HD |
Drug Info
|
IC50 = 1520 nM |
[2] |
| United States Patent and Trademark Office (USPTO) |
| Patent ID |
US20107713994 |
| Title |
Anticancer Activity of Cyclin Dependent Kinase Inhibitors. |
| Representative Drug(s) |
D0W4MN |
Drug Info
|
IC50 = 9700 nM |
[1] |
| Intellectual Property Office in India (IP India) |
| Patent ID |
INKO201101289 |
| Title |
Preparation of Naphthyridine and Isoquinoline Derivatives As Cdk Inhibitors. |
| Representative Drug(s) |
D08WJG |
Drug Info
|
IC50 = 66 nM |
[1] |
| French National Institute of Industrial Property (FINPI) |
| Patent ID |
FR2943058 |
| Title |
Preparation of Pyrazolo[1,5-A]-1,3,5-Triazine Derivatives As Inhibitors of Cyclin-Dependent Kinases, Casein Kinase 1 and Dyrk1A Kinase for Treating B-Cell Chronic Lymphoid Leukemia. |
| Representative Drug(s) |
D0NB7Y |
Drug Info
|
IC50 = 19 nM |
[1] |
| Canadian Intellectual Property Office (CIPO) |
| Patent ID |
CA2597193 |
| Title |
Compounds and Uses. |
| Representative Drug(s) |
D0LX6X |
Drug Info
|
N.A. |
[1] |
