| 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 = 63 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 = 4 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 = 1300 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 = 170 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 |
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
|
IC50 = 2.7 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 = 2 to 6 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 = 2 to 6 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 = 260 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 |
WO2011096676 |
| Title |
Indirubin-3'-Oxime Derivatives As Potent Cyclin Dependent Kinase Inhibitors. |
| Abstract |
The present invention relates to an indirubin-3'-oxime derivative as potent cyclin dependent kinase inhibitor with anti-cancer activity. More particularly, this invention relates to an indirubin-3'-oxime derivative as potent cyclin dependent kinase inhibitor having excellent anti-cancer activity against human lung cancer cell, human fibro sarcoma cell, human colon cancer cell, human leukemia cell, human stomach cancer cell, human nasopharyngeal cancer cell and/or human breast cancer cell. |
| Applicant(s) |
Anygen Co., Ltd |
| Representative Drug(s) |
D09ISI |
Drug Info
|
IC50 = 1.7 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 = 12 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 = 300 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 |
WO2010009166 |
| Title |
Oxindolyl Inhibitor Compounds. |
| Abstract |
A compound of general Formula (I) having histone deacetylase (HDAC) and/or CDK inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound. (Formula should be inserted here) Formula (I). |
| Applicant(s) |
Gilead Sciences, Inc |
| Representative Drug(s) |
D02KWX |
Drug Info
|
IC50 = 10 nM |
[1] |
| Patent ID |
WO2010009155 |
| Title |
Fused Heterocyclyc Inhibitors of Histone Deacetylase and/or Cyclin-Dependent Kinases. |
| Abstract |
The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) and/or Cyclin-dependent kinase (CDK) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound. Formula (I). |
| Applicant(s) |
Gilead Sciences, Inc |
| Representative Drug(s) |
D06QPW |
Drug Info
|
IC50 = 39 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 = 45 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 = 300 nM |
[2] |
| 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 = 45 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 = 45 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 |
WO2013128028 |
| Title |
Pyrazolo-Triazine Derivatives As Selective Cyclin- Dependent Kinase Inhibitors. |
| Abstract |
The present invention relates to pyrazolo[1,5-a][1,3,5]triazine 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 pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase. |
| Applicant(s) |
Lead Discovery Center Gmbh |
| Representative Drug(s) |
D0T6CM |
Drug Info
|
N.A. |
[1] |
| Patent ID |
WO2012061156 |
| Title |
Cdk Inhibitors. |
| Abstract |
Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors. |
| Applicant(s) |
G1 Therapeutics, Inc |
| Representative Drug(s) |
D03HED |
Drug Info
|
N.A. |
[1] |
| Patent ID |
WO2009058739 |
| Title |
Heterocyclic Urea and Thiourea Derivatives and Methods of Use Thereof. |
| Abstract |
The present invention relates to novel Heterocyclic Urea and Thiourea Derivatives of formula (I), compositions comprising the Heterocyclic Urea and Thiourea Derivatives, and methods for using the Heterocyclic Urea and Thiourea Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase. |
| Applicant(s) |
Schering Corp |
| Representative Drug(s) |
D0LR2Y |
Drug Info
|
N.A. |
[1] |
| Patent ID |
WO2009058730 |
| Title |
Diamido Thiazole Derivatives As Protein Kinase Inhibitors. |
| Abstract |
The present invention relates to novel Diamido Thiazole Derivatives of structure I, compositions comprising the Diamido Thiazole Derivatives, and methods for using the Diamido Thiazole Derivatives for treating or preventing a proliferative disorder, an anti -proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase. Formula (I) wherein: M is -C(O)-, -C(S)-. -S(O)-. -S(O)2-. -NHS(O)2-. -OC(O)- or -NHC(O)-; Q is:formula (II). |
| Applicant(s) |
Schering Corp |
| Representative Drug(s) |
D0LR2Y |
Drug Info
|
N.A. |
[1] |
| Patent ID |
WO2009058729 |
| Title |
Thiazole Carboxamide Derivatives and Their To Treat Cancer. |
| Abstract |
The present invention relates to novel Heterocyclic Ether or Thioether Derivatives, compositions comprising the Heterocyclic Ether or Thioether Derivatives, and methods for using the Heterocyclic Ether or Thioether Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase. |
| Applicant(s) |
Schering Corp |
| Representative Drug(s) |
D0LR2Y |
Drug Info
|
N.A. |
[1] |
| 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 = 3100 nM |
[1] |
| Patent ID |
US20100009990 |
| Title |
Imidazolyl Pyrimidine Inhibitor Compounds. |
| Representative Drug(s) |
D0QR1Z |
Drug Info
|
IC50 = 2 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 = 40 nM |
[1] |
| Patent ID |
INMU200901493 |
| Title |
Preparation of 4-Amino-3,5-Disubstituted-Thiazole-2(3H)-Thione/One Series As Novel Class of Cdk2 Inhibitors. |
| Representative Drug(s) |
D0JU4Z |
Drug Info
|
N.A. |
[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 = 12 nM |
[1] |
| Canadian Intellectual Property Office (CIPO) |
| Patent ID |
CA2597193 |
| Title |
Compounds and Uses. |
| Representative Drug(s) |
D0LX6X |
Drug Info
|
N.A. |
[1] |
