| Patent(s) and the Corresponding Patented Drug(s) |
Top |
| World Intellectual Property Organization (WIPO) |
| Patent ID |
WO2014170914 |
| Title |
Rohitukine Analogs As Cyclin-Dependent Kinase Inhibitors and A Process for The Preparation Thereof. |
| Abstract |
The present invention relates to the rohitukine (5,7-dihydroxy-8-(3-hydroxy-1-methylpiperidin-4-yl)-4H-chromen-4-ones) analogs of formula A and pharmaceutically acceptable salts thereof. In addition, the invention relates to pharmaceutically acceptable compositions comprising at least one such compound, and methods of using the compounds for treating or preventing various proliferative disorders such as melanoma, leukemia, breast cancer and prostate cancer etc. [insert Formula A here] wherein, n=0 or 1, when n=1, the dotted line indicates the double bond. |
| Applicant(s) |
Council of Scientific and Industrial Research |
| Representative Drug(s) |
D0P9WR |
Drug Info
|
IC50 = nM range |
[1] |
| 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 |
WO2014076111 |
| Title |
N-(Pyridin-2-Yl)Pyrimidin-4-Amine Derivatives Containing A Sulfoximine Group. |
| Abstract |
The present invention relates to disubstituted N-(pyridin-2-yl)pyrimidin-4-amine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/ or prophylaxis of disorders, in particular of hyper- proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I). |
| Applicant(s) |
Bayer Pharma Aktiengesellschaft |
| Representative Drug(s) |
D0QS2B |
Drug Info
|
IC50 = 5 nM |
[1] |
| Patent ID |
WO2014076091 |
| Title |
5-Fluoro-N-(Pyridin-2-Yl)Pyridin-2-Amine Derivatives Containing A Sulfoximine Group. |
| Abstract |
The present invention relates to 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I). |
| Applicant(s) |
Bayer Pharma Aktiengesellschaft |
| Representative Drug(s) |
D0V7RP |
Drug Info
|
IC50 = 2 nM |
[1] |
| Patent ID |
WO2014076028 |
| Title |
4-(ortho)-Fluorophenyl-5-Fluoropyrimidin-2-Yl Amines Containing A Sulfoximine Group. |
| Abstract |
The present invention relates to 4-(ortho)-fluorophenyl-5-fluoropyrimidin-2-yl amine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I). |
| Applicant(s) |
Bayer Pharma Aktiengesellschaft |
| Representative Drug(s) |
D0AY5G |
Drug Info
|
IC50 = 6 nM |
[1] |
| Patent ID |
WO2014060493 |
| Title |
N-(Pyridin-2-Yl)Pyrimidin-4-Amine Derivatives Containing A Sulfone Group. |
| Abstract |
The present invention relates to N-(pyridin-2-yl)pyrimidin-4-amine derivatives containing a sulfone group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I). |
| Applicant(s) |
Bayer Pharma Aktiengesellschaft |
| Representative Drug(s) |
D00DDX |
Drug Info
|
IC50 = 4 nM |
[1] |
| Patent ID |
WO2014060375 |
| Title |
5-Fluoro-N-(Pyridin-2-Yl)Pyridin-2-Amine Derivatives Containing A Sulfone Group. |
| Abstract |
The present invention relates to 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfone group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I). |
| Applicant(s) |
Bayer Pharma Aktiengesellschaft |
| Representative Drug(s) |
D03EYT |
Drug Info
|
IC50 = 2 nM |
[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 |
WO2013037896 |
| Title |
Disubstituted 5-Fluoro-Pyrimidines. |
| Abstract |
The present invention relates to disubstituted 5-fluoro-pyrimidines of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I). |
| Applicant(s) |
Bayer Intellectual Property Gmbh |
| Representative Drug(s) |
D0P4NP |
Drug Info
|
IC50 = 70 to 300 nM |
[1] |
| Patent ID |
WO2013037894 |
| Title |
Disubstituted 5-Fluoro Pyrimidine Derivatives Containing A Sulfoximine Group. |
| Abstract |
The present invention relates to disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I). |
| Applicant(s) |
Bayer Ip Gmbh |
| Representative Drug(s) |
D0P4NP |
Drug Info
|
IC50 = 70 to 300 nM |
[1] |
| Patent ID |
WO2013026874 |
| Title |
Cdk9 Inhibitors In The Treatment of Midline Carcinoma. |
| Abstract |
The present invention relates to a CDK9 inhibitor, especially a selective CDK9 inhibitor, for use in treating, ameliorating and/or preventing midline carcinoma. Also corresponding methods for treating, preventing or ameliorating midline carcinoma are subject of the present invention. Preferably, NUT midline carcinoma is treated with the CDK9 inhibitors in accordance with the present invention. |
| Applicant(s) |
Lead Discovery Center Gmbh |
| Representative Drug(s) |
D0SV2E |
Drug Info
|
IC50 = 1 nM |
[1] |
| Patent ID |
WO2012160034 |
| Title |
4-Aryl-N-Phenyl-1,3,5-Triazin-2-Amines Containing A Sulfoximine Group. |
| Abstract |
The present invention relates to 4-aryl-N-phenyl-1,3,5-triazin-2-amines containing a sulfoximine group of general formula (I) or (Ia) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I) or (Ia). |
| Applicant(s) |
Bayer Intellectual Property Gmbh |
| Representative Drug(s) |
D0GQ7L |
Drug Info
|
IC50 = 2 nM |
[1] |
| Patent ID |
WO2012117059 |
| Title |
Pharmaceutically Active Disubstituted Pyridine Derivatives. |
| Abstract |
The present invention relates to disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted pyridine derivatives as inhibitors for a protein kinase. |
| Applicant(s) |
Lead Discovery Center Gmbh |
| Representative Drug(s) |
D0UU0V |
Drug Info
|
Kd < 100 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 = 38 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 |
WO2009118567 |
| Title |
Pyrimidines, Triazines and Their Use As Kinase Inhibitors. |
| Abstract |
A compound of formula (I) and its pharmaceutically acceptable salts or solvates and physiologically hydrolysable, solubilising or immobilisable derivatives wherein: Ar is a 5-membered heteroaryl ring wherein X1 and X2 are one or two heteroatoms or Ar is a 6-membered aromatic ring, wherein heteroatoms are selected from S, O, N, Se; Z is NH, NHCO, NHSO2, N-alkyl, CH2NH, CH2N-alkyl, CH2, CH2CH2, CH=CH, CH2CONH, SO2, or SO; Y is N or CR3; R1, R2, R5, R6, R7, R8 and R9 are each independently H, or a substituent; R3, when present, is selected from alkyl and a substituent, with the proviso that when Y is CR3, Ar is a 5- membered heterocycle comprising one or two N heteroatoms and Z is NH, then R3 is selected from C3+ alkyl and a substituent; R4 is selected from H, alkyl and R13 as hereinbefore defined, with the proviso that when R3 is absent, R4 is selected from alkyl and a substituent; processes for the preparation thereof, intermediates and precursors therefore and the use thereof as a medicament, and therapeutic compositions comprising the compound. |
| Applicant(s) |
The University of Nottingham |
| Representative Drug(s) |
D07QIP |
Drug Info
|
IC50 = 19 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 |
WO2003029248 |
| Title |
N-(4-(4-Methylthiazol-5-Yl) Pyrimidin-2-Yl) -N-Phenylamines As Antiproliferative Compounds. |
| Abstract |
The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders such as cancer, leukaemia, psoriasis and the like. |
| Applicant(s) |
Cyclacel Limited |
| Representative Drug(s) |
D07QIP |
Drug Info
|
IC50 = 19 nM |
[1] |
| Patent ID |
WO2002079193 |
| Title |
Inhibitors of Cyclin Dependent Kinases As Anti-Cancer Agent. |
| Abstract |
The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferation disorders such as cancer, leukaemia, psoriasis and the like. |
| Applicant(s) |
Cyclacel Limited |
| Representative Drug(s) |
D07QIP |
Drug Info
|
IC50 = 19 nM |
[1] |
| Patent ID |
WO2014060376 |
| Title |
4-(ortho)-Fluorophenyl-5-Fluoropyrimidin-2-Yl Amines Containing A Sulfone Group. |
| Abstract |
The present invention relates to 4-(ortho)-fluorophenyl-5-fluoropyrimidin-2-yl amine derivatives of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I). |
| Applicant(s) |
Bayer Pharma Aktiengesellschaft |
| Representative Drug(s) |
D05UJQ |
Drug Info
|
N.A. |
[1] |
| Patent ID |
WO2013049279 |
| Title |
Nitrogen Mustard Derivatives. |
| Abstract |
The disclosure includes compounds of Formula (1): wherein X1, X2, Q, Z, R1, and R2 are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds. |
| Applicant(s) |
Euro-Celtique Sa |
| Representative Drug(s) |
D0LK4L |
Drug Info
|
N.A. |
[1] |
| Patent ID |
WO2012066070 |
| Title |
3-(Aminoaryl)-Pyridine Compounds. |
| Abstract |
The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided are pharmaceutical compositions containing these compounds and methods of treating a disease or condition mediated by CDK9 using these compounds and compositions. |
| Applicant(s) |
Novartis Ag |
| Representative Drug(s) |
D0FR3Z |
Drug Info
|
N.A. |
[1] |
| Patent ID |
WO2012066065 |
| Title |
Phenyl-Heteroaryl Amine Compounds and Their Uses. |
| Abstract |
The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I, and pharmaceutical compositions comprising such compounds. |
| Applicant(s) |
Novartis Ag |
| Representative Drug(s) |
D09PGP |
Drug Info
|
N.A. |
[1] |
| Patent ID |
WO2011026917 |
| Title |
Heteroaryl Compounds As Kinase Inhibitors. |
| Abstract |
The present invention provides a compound of Formula (I): and pharmaceutically acceptable salts thereof. Also provided is a method of using a compound of Formula I for treating a disease or condition mediated by a CDK inhibitor. |
| Applicant(s) |
Novartis Ag |
| Representative Drug(s) |
D08DWG |
Drug Info
|
N.A. |
[1] |
| Patent ID |
WO2011026911 |
| Title |
Bipyridines Useful for The Treatment of Proliferative Diseases. |
| Abstract |
The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof. Also provided is a method of using a compound of Formula I for treating a disease or condition mediated by a CDK inhibitor. |
| Applicant(s) |
Novartis Ag |
| Representative Drug(s) |
D0TH7T |
Drug Info
|
N.A. |
[1] |
| Patent ID |
WO2011026904 |
| Title |
Pyrazinylpyridines Useful for The Treatment of Proliferative Diseases. |
| Abstract |
The present invention provides a compound of Formula (I) and pharmaceutically acceptable salts thereof. Also provided is a method of using a compound of Formula I for treating a disease or condition mediated by a CDK inhibitor. |
| Applicant(s) |
Novartis Ag |
| Representative Drug(s) |
D07VPQ |
Drug Info
|
N.A. |
[1] |
| Patent ID |
WO2009047359 |
| Title |
Inhibitors of Protein Kinases. |
| Abstract |
Compounds of general Formula I, wherein R1, R2, R3, x, A and Ra are as defined herein are inhibitors of cyclin-dependent kinases and are useful for preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases. |
| Applicant(s) |
Ingenium Pharmaceuticals Gmbh |
| Representative Drug(s) |
D03YMA |
Drug Info
|
N.A. |
[1] |
| United States Patent and Trademark Office (USPTO) |
| Patent ID |
US20140086941 |
| Title |
Substituted 2-Benzylidene-2H-Benzo[B][1,4]Thiazin-3(4H)-Ones, Derivatives Thereof, and Therapeutic Uses Thereof. |
| Representative Drug(s) |
D00BFF |
Drug Info
|
IC50 = 94 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 = 38 nM |
[1] |
| Canadian Intellectual Property Office (CIPO) |
| Patent ID |
CA2597193 |
| Title |
Compounds and Uses. |
| Representative Drug(s) |
D0LX6X |
Drug Info
|
N.A. |
[1] |
