Target and Its Patented Drug(s)

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Target General Information
Patent(s) and the Corresponding Patented Drug(s)
References
Target General Information  Top
Target ID T15776 Target Info
Target Name Pyruvate dehydrogenase kinase 1 (PDHK1)
Synonyms Pyruvate dehydrogenase kinase isoform 1; Pyruvate dehydrogenase (acetyl-transferring) kinase isozyme 1, mitochondrial; PDHK1; PDH kinase 1
Target Type Clinical trial Target
Gene Name PDK1
Biochemical Class Kinase
UniProt ID
PDK1_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2012135799
Title Substituted 3-(1H-Benzo{D}Imidazol-2-Yl)-1H-Indazole-Analogs As Inhibitors of The Pdk1 Kinase.
Abstract In one aspect, the invention relates to substituted 3-(lH-benzo[d]imidazol-2-yl)-lH- indazole analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the PDK1 kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions for treating disorders associated with dysfunction of the PDK1 kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Applicant(s) University of Utah Research Foundation
Representative Drug(s) D0DC2P Drug Info IC50 = 300 nM Click to Show More [1]
2 D0R0SJ Drug Info IC50 = 780 nM [1]
Patent ID WO2012058176
Title Novel Heteroaryl-Carboxamide Derivatives As Pdk1 Inhibitors.
Abstract This invention relates to certain Heteroaryl Carboxamide derivatives of Formula (I) as inhibitors of 3-phosphoinositide-dependent protein kinase (PDK-1). The compounds can be useful in inhibiting the proliferation of cancer cells, and other aberrant conditions where the PDK-1 signaling pathway is overstimulated.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D00LMA Drug Info IC50 <= 50 nM Click to Show More [1]
2 D00ZXR Drug Info IC50 <= 50 nM [1]
3 D03WFI Drug Info IC50 <= 50 nM [1]
4 D08SNT Drug Info IC50 <= 50 nM [1]
5 D0GH9W Drug Info IC50 <= 50 nM [1]
6 D0H7SO Drug Info IC50 <= 50 nM [1]
7 D0MG4D Drug Info IC50 <= 50 nM [1]
8 D0MW7L Drug Info IC50 <= 50 nM [1]
9 D0TB2H Drug Info IC50 <= 50 nM [1]
Patent ID WO2012058174
Title Novel Thiazole-Carboxamide Derivatives As Pdk1 Inhibitors.
Abstract This invention relates to certain thiazole carboxamide derivatives as inhibitors of 3-phosphoinositide-dependent protein kinase (PDK-1). The compounds can be useful in inhibiting the proliferation of cancer cells, and other aberrant conditions where the PDK-1 signaling pathway is overstimulated.
Applicant(s) Merck Sharp & Dohme Corp
Patent ID WO2012044157
Title Product Conveying Device for Lifting A Product From A Conveying Means.
Abstract A product conveying device, comprising a substantially horizontally disposed conveying means (101) for supplying a product, a movable support (112) and a lifting mechanism (102) mounted on the movable support for lifting the product from the conveying means. The conveying means is provided with a plurality of slots (106) arranged in one direction and the lifting mechanism comprises support elements (103) that can cooperate with the slots. The movable support is designed for displacing the lifting mechanism, such that the support elements can be moved into the slots from above, wherein the support elements can be moved under the product in the direction in which the slots extend and wherein the product being supplied can subsequently be lifted from the conveying means by means of the support elements.
Applicant(s) Beheersmaatschappij Gach.M. Jentjens Bv
Representative Drug(s) D02USE Drug Info IC50 = 100 to 5000 nM Click to Show More [1]
2 D04BBT Drug Info IC50 = 100 to 5000 nM [1]
3 D04MHV Drug Info IC50 = 100 to 5000 nM [1]
4 D0EH9Z Drug Info IC50 = 100 to 5000 nM [1]
5 D0FW3M Drug Info IC50 = 100 to 5000 nM [1]
6 D0HI8X Drug Info IC50 = 100 to 5000 nM [1]
7 D0RH6G Drug Info IC50 = 100 to 5000 nM [1]
Patent ID WO2012036974
Title Novel Thiazol-Carboximide Derivatives As Pdk1 Inhibitors.
Abstract This invention relates to certain thiazole carboxamide derivatives of Formula (I) as inhibitors of 3-phosphoinositide-dependent protein kinase (PDK-1). The compounds can be useful in inhibiting the proliferation of cancer cells, and other aberrant conditions where the PDK-1 signaling pathway is overstimulated.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0JR0F Drug Info IC50 < 50 nM Click to Show More [1]
2 D04BBA Drug Info IC50 < 250 nM [1]
3 D04QRX Drug Info IC50 < 250 nM [1]
4 D07ZMG Drug Info IC50 < 250 nM [1]
5 D0B2GM Drug Info IC50 < 250 nM [1]
6 D0D8PF Drug Info IC50 < 250 nM [1]
7 D0DO6K Drug Info IC50 < 250 nM [1]
8 D0FJ4A Drug Info IC50 < 250 nM [1]
9 D0GE6F Drug Info IC50 < 250 nM [1]
10 D0GY8G Drug Info IC50 < 250 nM [1]
11 D0KN7T Drug Info IC50 < 250 nM [1]
12 D0P6PT Drug Info IC50 < 250 nM [1]
13 D0QV1E Drug Info IC50 < 250 nM [1]
Patent ID WO2011137219
Title Inhibitors of Phosphoinositide Dependent Kinase 1 (Pdk1).
Abstract The instant invention provides for compounds that inhibit PDK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting PDK1 activity by administering the compound to a patient in need of treatment of cancer.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0P0WF Drug Info IC50 = 33 nM Click to Show More [1]
2 D0IO2X Drug Info IC50 = 85 nM [1]
3 D00SVK Drug Info IC50 = 110 nM [1]
4 D0B8OB Drug Info IC50 = 170 nM [1]
Patent ID WO2006106326
Title Substituted Heterocycles and Their Use As Chk1, Pdk1 and Pak Inhibitors.
Abstract This invention relates to novel compounds of Formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds possess CHK1 kinase inhibitory activity, PDK1 inhibitory activity and Pak kinase inhibitory activity and are accordingly useful in the treatment and/or prophylaxis of cancer.
Applicant(s) Astrazeneca Ab
Representative Drug(s) D03GFZ Drug Info IC50 = 160 nM Click to Show More [1]
2 D06BSG Drug Info IC50 = 350 nM [1]
Patent ID WO2012072200
Title 3-Hetaryl-Substituted Pyrrolo[2,3-B]Pyridine Derivatives As Pdk1 Inhibitors.
Abstract Compounds of the formula I in which Q, R1, R2, R3 and R4 are each as defined in claim 1 are PDK1 inhibitors and can be used for treatment of tumors.
Applicant(s) Merck Patent Gmbh
Patent ID WO2011076327
Title Pyrrolo[2,3-D]Pyrazin-7-Yl Pyrimidine Compounds.
Abstract The invention relates to pyrrolo[2,3-d]pyrazin-7-yl pyrimidine compounds that are cell proliferation/cell vitality inhibitors and can be used for the treatment of tumours.
Applicant(s) Merck Patent Gmbh
Representative Drug(s) D02MMG Drug Info IC50 = 120 nM [1]
Patent ID WO2011006567
Title Aminopyridine Derivatives for Treating Tumors and Inflammatory Diseases.
Abstract Compounds of the formula (I), wherein R1, R2, R3, R4, R7 and Y have the meanings specified in claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be used for treating tumors and for treating inflammatory diseases.
Applicant(s) Merck Patent Gmbh
Representative Drug(s) D06WAN Drug Info IC50 = 0.1 to 10 nM [1]
Patent ID WO2010127754
Title 3-([1,2,3]Triazole-4-Yl)-Pyrrolo[2,3-B]Pyridine Derivates.
Abstract The invention relates to compounds of the formula I, where R1, R2, and R3 have the meanings indicated in claim 1, wherein said compounds are inhibitors of PDK1 and cell proliferation/cell vitality, and can be used for treating tumors.
Applicant(s) Merck Patent Gmbh
Representative Drug(s) D0C6VX Drug Info IC50 = 0.5 to 1000 nM [1]
Patent ID WO2010120854
Title Chemical Compounds.
Abstract The invention is directed to to substituted indazole derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1 - R6 and X are defined herein. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of disorders characterized by constitutively activated ACG kinases such as cancer and more specifically leukemia and cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Applicant(s) Glaxosmithkline Llc
Representative Drug(s) D0PJ7M Drug Info IC50 = 7.6 nM [1]
Patent ID WO2010019637
Title Chemical Compounds.
Abstract The invention is directed to pyrido[4,3-d]pyrimidin-5(6H)-one derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R1, R2, R3, and R4 are defined below. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Applicant(s) Glaxosmithkline Llc
Patent ID WO2010017047
Title Therapeutic Compounds.
Abstract The present invention relates to pyrazolopyridines and imidazopyridines which are inhibitors of the kinase PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer. The compounds are also useful as inhibitors of other kinases such as FGFR3, NTRK3, RP-S6K and WEE1. Furthermore, the present compounds also selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0I1YQ Drug Info IC50 = 30000 nM [1]
Patent ID WO2010007116
Title Pyridons As Pdk1 Inhibitors.
Abstract The present invention encompasses compounds of general formula (1) while the groups R4 to R7 and the units W, L, Qa and QH are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use as medicaments having the above-mentioned properties.
Applicant(s) Boehringer Ingelheim International Gmbh
Representative Drug(s) D05GMT Drug Info IC50 <= 1000 nM [1]
Patent ID WO2010007114
Title Heterocyclyl Carbonic Acid Amides As Antiproliferative Agents, Pdkl Inhibitors.
Abstract The present invention encompasses compounds of general formula (1) wherein the units W, A, L, Qa and QH are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use as medicaments having the above-mentioned properties.
Applicant(s) Boehringer Ingelheim International Gmbh
Representative Drug(s) D0P1VT Drug Info IC50 <= 1000 nM [1]
Patent ID WO2009153313
Title 2 -Arylaminoquinazolines for Treating Proliferative Diseases.
Abstract The invention provides novel compounds that are inhibitors of PDKI. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or composition.
Applicant(s) Novartis Ag
Representative Drug(s) D06LLS Drug Info IC50 <= 50 nM [1]
Patent ID WO2008109613
Title Benzo[C][2,7]Naphthyridine Derivatives, and Their Use As Kinase Inhibitors.
Abstract The present invention relates to Benzo[c] [2,7] naph thy ri dine Derivatives of formula (I), compositions comprising an effective amount of a Benzo[c] [2,7]naphthyridine Derivative, methods for treating or preventing a proliferative disorder or an autoimmune disease, comprising administering to a subject in need thereof an effective amount of a Benzo[c] [2,7]naphthyridine Derivative, methods for modulating PDK-I activity, PKA activity, Akt activity, S6K activity, or PKC activity, comprising administering to a subject in need thereof an effective amount of a Benzo[c] [2,7] naphthyridine Derivative. The invention also relates to processes for preparing a Benzo[c] [2,7] naphthyridine Derivative.
Applicant(s) WISSNER, Allan et al
Representative Drug(s) D0IR8B Drug Info IC50 = 8 nM [1]
Patent ID WO2008109599
Title Pyrimido [5,4-C] Quinoline-2, 4-Diamine Derivatives and Methods of Use Thereof.
Abstract The present invention relates to Pyrimxdo [5,4-c]quinoline-2, 4 -diamine Derivatives, compositions comprising an effective amount of a Pyrimido [5, 4 -c] quinoline-2, 4 -diamine Derivative of formula (I), methods for treating or preventing a proliferative disorder, comprising administering to a subject in need thereof an effective amount of an Pyrimido [ 5, 4 - c] quinoline-2, 4 -diamine Derivative. Disclosed are also methods for modulating PDK-I activity, comprising administering to a subject in need thereof an effective amount of a Pyrimido [5,4- c] quinoline- 2,4-diamine Derivative. The invention also relates to a process for preparing a Pyrimido [5,4- c] quinoline-2, 4 -diamine Derivative or a pharmaceutically acceptable salt thereof,.
Applicant(s) WISSNER, Allan et al
Patent ID WO2008107444
Title 9H- Purine Derivatives and Their Use In The Treatment of Proliferative Diseases.
Abstract The present invention encompasses compounds of general formula (1) wherein R1, R2 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.
Applicant(s) Boehringer Ingelheim International Gmbh
Representative Drug(s) D0MI3E Drug Info IC50 <= 1000 nM [1]
Patent ID WO2008054238
Title Biologically Active Preparation (Variants) and A Method for The Production Thereof (Variants).
Abstract The invention relates to medicine. The inventive biologically active preparation is embodied in the form of a liquid which is extracted from a biological raw material by breaking down a cellular structure and is treated by constant and low-frequency variable or pulsed fields. According to the first variant, the inventive method consists in freezing and thawing a raw material, in rapidly sublimating it at a temperature of 30-45, in condensing said raw material and in treating the thus obtained condensate by means of a combined constant field within a magnetic induction range of 0.01-100 mTl and by a low-frequency variable or pulsed field within the magnetic induction range of 0.01-100 mTl. According to the second variant, the inventive method consists in drying a raw material in vacuum by heating and in simultaneously treating it by a combined constant field within a magnetic induction range of 0.01-100 mTl and by a low-frequency variable or pulsed field within the magnetic induction range of 0.01-100 mTl. Volatile components are condensed on the walls of a closed space, the temperature of which is maintained within the range of dew-point temperatures. The condensate is obtained in the form of a biologically active liquid preparation, the rest being a solid biologically active preparation.
Applicant(s) Kutushov Mikhail Vladimirovich
Representative Drug(s) D0D5YE Drug Info IC50 = 34 to 330 nM [1]
Patent ID WO2008005457
Title Pyridinonyl Pdk1 Inhibitors.
Abstract The present invention provides pyridinonyl PDKl inhibitors and methods of treating cancer using the same.
Applicant(s) Sunesis Pharmaceuticals Biogen Idec Ma Inc
Representative Drug(s) D08EGT Drug Info IC50 < 500 nM [1]
Patent ID WO2006015124
Title Fused Ring Heterocycle Kinase Modulators.
Abstract The present invention provides novel fused ring heterocycle kinase modulators and methods of using the novel fused ring heterocycle kinase modulators to treat diseases mediated by kinase activity.
Applicant(s) Sgx Pharmaceuticals, Inc
Representative Drug(s) D0RP4U Drug Info IC50 = 1000 to 5000 nM [1]
Patent ID WO2003064397
Title Indazole Compounds Useful As Protein Kinase Inhibitors.
Abstract The present invention provides compounds of formula (I), or a pharmaceutically acceptable derivative thereof, wherein R1, R2, V1, V2 and V3 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of AKT, PKA, PDK1, p70S6K, or ROCK kinase, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of utilizing those compositions in the treatment of various disorders.
Applicant(s) Vertex Pharmaceuticals Incorporated
Representative Drug(s) D0CK8H Drug Info IC50 = 10 to 140 nM [1]
Patent ID WO2011044157
Title Heterocyclic Compounds Useful As Pdk1 Inhibitors.
Applicant(s) Sunesis & Biogen
Representative Drug(s) D0CQ1M Drug Info IC50 = 100 to 1000 nM [1]
Patent ID WO2010065384
Title Drivs De 3-([1, 2, 3] Triazol-4-Yl)-Pyrrolo[2,3-B]Pyridine.
Applicant(s) Merck & Co., Inc
Representative Drug(s) D0RY6M Drug Info IC50 <= 30000 nM [1]
Patent ID WO2008079988
Title 2-Arylaminoquinazolines for Treating Proliferative Diseases.
Applicant(s) Novartis
Representative Drug(s) D04UHW Drug Info IC50 <= 50 nM [1]
United States Patent and Trademark Office (USPTO)
Patent ID US20130165450
Title Novel Thiazol-Carboximide Derivatives As Pdk1 Inhibitors.
Applicant(s) Schering Corp
Representative Drug(s) D0K8XT Drug Info IC50 < 50 nM Click to Show More [1]
2 D0Q8JK Drug Info IC50 = 100 nM [1]
3 D06LCB Drug Info IC50 < 250 nM [1]
4 D06PTW Drug Info IC50 < 250 nM [1]
5 D06WXJ Drug Info IC50 < 250 nM [1]
6 D07MSB Drug Info IC50 < 250 nM [1]
7 D08YPQ Drug Info IC50 < 250 nM [1]
8 D0H6AF Drug Info IC50 < 250 nM [1]
9 D0HP8K Drug Info IC50 < 250 nM [1]
10 D0PD2I Drug Info IC50 < 250 nM [1]
11 D0Q6RC Drug Info IC50 < 250 nM [1]
12 D0R3VG Drug Info IC50 < 250 nM [1]
Patent ID US20130053382
Title Inhibitors of Phosphoinositide Dependent Kinase 1 (Pdk1).
Representative Drug(s) D0SB4A Drug Info IC50 = 33 nM Click to Show More [1]
2 D07FMW Drug Info IC50 = 85 nM [1]
3 D07XBA Drug Info IC50 = 170 nM [1]
Patent ID US20120277229
Title Substituted 3-(1H-Benzo[D]Imidazol-2-Yl)-1H-Indazole Analogs As Inhibitors of The Pdk1 Kinase.
Representative Drug(s) D09FQP Drug Info IC50 = 140 nM Click to Show More [1]
2 D06LSZ Drug Info IC50 = 160 nM [1]
3 D04EDM Drug Info IC50 = 280 nM [1]
4 D0RE3R Drug Info IC50 = 300 nM [1]
5 D07ZKE Drug Info IC50 = 780 nM [1]
Patent ID US20120208819
Title Heterocyclic Compounds Useful As Pdk1 Inhibitors.
Representative Drug(s) D05OTD Drug Info IC50 = 100 to 5000 nM Click to Show More [1]
2 D07HOA Drug Info IC50 = 100 to 5000 nM [1]
3 D07IQE Drug Info IC50 = 100 to 5000 nM [1]
4 D09BNP Drug Info IC50 = 100 to 5000 nM [1]
5 D0AM2D Drug Info IC50 = 100 to 5000 nM [1]
6 D0D0ML Drug Info IC50 = 100 to 5000 nM [1]
7 D0J9DI Drug Info IC50 = 100 to 5000 nM [1]
Patent ID US20140017701
Title Chimeric Pdk1 Kinases.
Applicant(s) Biondi Rm, Laura Al, Lopez G, et Al
Patent ID US20130245355
Title 3-Hetaryl-Substituted Pyrrolo [2,3B] Pyridine Derivatives As Pdk1 Inhibitors.
Applicant(s) Merck Patent Gmbh
Patent ID US20090111799
Title Anti-Infective Agents Against Intracellular Pathogens.
Applicant(s) The Ohio State University Research Foundation
Representative Drug(s) D00MLJ Drug Info IC50 = 2000 nM [1]
Patent ID US20070135429
Title 10,11-Dimethoxydibenzo[C,F]-2,7-Naphthyridin-6-Amine; Inhibiting Pyruvate Dehydrogenase Kinase Pdk-1In A Cell; Antiproliferative Agent; Brain, Colon Cancer, Leukemia, Prostate and Breast Cancer.
Applicant(s) Wyeth
Representative Drug(s) D0I5KI Drug Info IC50 = 60 to 7500 nM [1]
Patent ID US200607105563
Title 5-Ureido-3-[(4-(3-Methoxyphenyl) Pyrrol-2-Yl)Methylene]Indolin-2-One and Derivatives; Inhibition of Phosphoinositide-Dependent Kinase-1 (Pdk-1).
Applicant(s) Schering Ag
Patent ID US20120003668
Title High Resolution Complex Structure and Allosteric Effects of Low Molecular Weight Activators On The Protein Kinase Pdk1.
Applicant(s) Universities Des Saarlandes
European Patent Office (EPO)
Patent ID EP20041486488
Title Use of A Compound of formula I for Making A Pharmaceutical Composition.
Applicant(s) Phosphosites Gmbh
References  Top
REF 1 PDK1 disruptors and modulators: a patent review.Expert Opin Ther Pat. 2015 May;25(5):513-37.

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