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 T06273 Target Info
Target Name Poly [ADP-ribose] polymerase 1 (PARP1)
Synonyms Protein poly-ADP-ribosyltransferase PARP1; Poly[ADP-ribose] synthetase-1; Poly[ADP-ribose] synthase 1; Poly(ADP-ribose)polymerase-1; PPOL; PARP-1; NAD(+)Poly [ADP-ribose] polymerase-1 ADP-ribosyltransferase-1; NAD(+) ADP-ribosyltransferase-1; NAD(+) ADP-ribosyltransferase 1; DNA ADP-ribosyltransferase PARP1; ARTD1; ADPRT 1; ADPRT; ADP-ribosyltransferase diphtheria toxin-like 1
Target Type Successful Target
Gene Name PARP1
Biochemical Class Glycosyltransferases
UniProt ID
PARP1_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2013078771
Title Poly (Adp-Ribose) Polymerase Inhibitor.
Abstract Disclosed are a phthalic hydrazide (phthalazine ketone) compound, and a pharmaceutical composition comprising the same. As a DNA repair enzyme poly (ADP-ribozyme) polymerase inhibitor, the compound and the pharmaceutical composition can effectively treat diseases involving PARP enzymatic activity, including cancer, neural degenerative diseases, inflammation and the like.
Applicant(s) Chengdu Di Ao Pharmaceutical Group Co Ltd
Representative Drug(s) D05ZBB Drug Info IC50 = 6000 nM Click to Show More [1]
2 D0B4FV Drug Info IC50 = 8000 nM [1]
3 D0AN7Z Drug Info IC50 = 9000 nM [1]
Patent ID WO2014064149
Title 4-Carboxamido-Isoindolinone Derivatives As Selective Parp-1 Inhibitors.
Abstract There are provided substituted 4-carboxamido-isoindolinone derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
Applicant(s) Nerviano Medical Sciences S.R.L
Representative Drug(s) D08YPU Drug Info IC50 = 11 nM Click to Show More [1]
2 D0O9FC Drug Info IC50 = 20 nM [1]
3 D0R0PO Drug Info IC50 = 100 nM [1]
4 D0GH4V Drug Info N.A. [1]
Patent ID WO2013076090
Title 3-Phenyl-Isoquinolin-1(2H)-One Derivatives As Parp-1 Inhibitors.
Abstract There are provided substituted 3-phenyl-isoquinolin-1(2H)-one derivatives which selectively inhibit the activity of poly(ADP-ribose) polymerase PARP-1 with respect to poly(ADP-ribose) polymerase PARP-2. The compounds of the present invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
Applicant(s) Nerviano Medical Sciences S.R.L
Representative Drug(s) D0TD8R Drug Info IC50 < 10 nM Click to Show More [1]
2 D0G8HX Drug Info N.A. [1]
Patent ID WO2015011008
Title 7-Azaindole Derivatives As Parp Inhibitors.
Abstract The present invention relates to 7-azaindole derivatives of Formula (I), pharmaceutical compositions containing such derivatives. The invention further relates to said pharmaceutical compositions for use in medicine, and more particularly in the treatment of cancer diseases where an inhibition of PARP is responsive.
Applicant(s) Sigma-Tau Industrie Farmaceutiche Riunite Spa
Representative Drug(s) D09WUA Drug Info IC50 < 100 nM [1]
Patent ID WO2014009872
Title Tetrahydroquinazolinone Derivatives As Parp Inhibitors.
Abstract Disclosed are compounds of formula (I), their tautomeric forms, stereoisomers, and pharmaceutically acceptable salts thereof, wherein R1-R6, R7a-d, R8a-d, A, M, n, and p are as defined in the specification, pharmaceutical compositions including a compound, tautomer, stereoisomer, or salt thereof, and methods of treating or preventing diseases or disorders, for example, cancer, that are amenable to treatment or prevention by inhibiting the PARP enzyme of a subject.
Applicant(s) Lupin Limited
Representative Drug(s) D0MP4W Drug Info IC50 = 1 to 500 nM [1]
Patent ID WO2012019427
Title Phthalazinone Ketone Derivative, Preparation Method Thereof, and Pharmaceutical Use Thereof.
Abstract A phthalazinone ketone derivative as represented by formula (I), a preparation method thereof, a pharmaceutical composition containing the derivative, a use thereof as a poly (ADP-ribose) polymerase (PARP) inhibitor, and a cancer treatment method thereof.
Applicant(s) Shanghai Hengrui Pharm Co Ltd
Representative Drug(s) D02KMI Drug Info IC50 = 10 nM [1]
Patent ID WO2009046205
Title Parp Inhibitor Compounds, Compositions and Methods of Use.
Abstract The present invention relates to tetraaza phenalen-3-one compounds which inhibit poly (ADP-ribose) polymerase (PARP) and are useful in the chemosensitization of cancer therapeutics. The induction of peripheral neuropathy is a common side-effect of many of the conventional and newer chemotherapies. The present invention further provides means to reliably prevent or cure chemotherapy- induced neuropathy. The invention also relates to the use of the disclosed PARP inhibitor compounds in enhancing the efficacy of chemotherapeutic agents such as temozolomide. The invention also relates to the use of the disclosed PARP inhibitor compounds to radiosensitize tumor cells to ionizing radiation. The invention also relates to the use of the disclosed PARP inhibitor compounds for treatment of cancers with DNA repair defects.
Applicant(s) Eisai Inc
Representative Drug(s) D0F5TD Drug Info N.A. [1]
United States Patent and Trademark Office (USPTO)
Patent ID US2014023642
Title 1-(Arylmethyl)Quinazoline-2,4(1H,3H)-Diones As Parp Inhibitors and The Use Thereof.
Applicant(s) Impact Therapeutics, Inc
Representative Drug(s) D0J2SR Drug Info IC50 = 0.21 nM Click to Show More [1]
2 D0IX2C Drug Info IC50 = 0.37 nM [1]
Patent ID US2013053365
Title Dihydropyridophthalazinone Inhibitors of Poly(Adp-Ribose)Polymerase (Parp).
Representative Drug(s) D0B3QI Drug Info IC50 < 800 nM Click to Show More [1]
2 D0J4GY Drug Info IC50 < 800 nM [1]
Patent ID US2014235675
Title 3-Oxo-2,3-Dihydro-1H-Indazole-4-Carboxamide Derivatives As Parp-1 Inhibitors.
Applicant(s) Nerviano Medical Sciences S.R.L
Representative Drug(s) D0M0WS Drug Info IC50 = 26 nM; Kd < 10 nM Click to Show More [1]
2 D09HUV Drug Info IC50 = 15 nM; Kd < 10 nM [1]
3 D02QFM Drug Info IC50 = 44 nM [1]
4 D01KFW Drug Info IC50 = 230 nM [1]
5 D09ZIM Drug Info N.A. [1]
Patent ID US2015166544
Title Piperazinotriazole Compound, Preparation Method Therefor, and Use Thereof In Drug Preparation.
Applicant(s) Shanghai Institute of Materia Medica
Representative Drug(s) D0M9TG Drug Info IC50 = 10 nM [1]
Patent ID US2014100239
Title Quinazolinedione Derivatives As Parp Inhibitors.
Applicant(s) Janssen Pharmaceutica Nv
Representative Drug(s) D08KAH Drug Info IC50 = 140 nM [1]
Patent ID US2013303567
Title Small Molecule Inhibitors of Parp Activity.
Applicant(s) Angion Biomedica Corp
Representative Drug(s) D01PYO Drug Info IC50 < 1 nM [1]
China National Intellectual Property Administration (CNIPA)
Patent ID CN103772395
Title Tricyclic Indole Compound (I) with Parp (Poly-Adp-Ribose Polymerase) Inhibiting Activity, Preparation Method and Application Thereof.
Applicant(s) China Pharmaceutical University
Representative Drug(s) D0E9JI Drug Info IC50 = 10 to 270 nM [1]
Taiwan Intellectual Property Office (TIPO)
Patent ID TW201444842
Title Fused Tetra or Penta-Cyclic Dihydrodiazepinocarbazolones As Parp Inhibitors.
Applicant(s) Beigene Ltd
Representative Drug(s) D0P3YA Drug Info IC50 = 2.9 nM [1]
Patent ID TW201444839
Title Fused Tetra or Penta-Cyclic Pyridophthalazinones As Parp Inhibitors.
Applicant(s) Beigene Ltd
References  Top
REF 1 PARP inhibitors as antitumor agents: a patent update (2013-2015).Expert Opin Ther Pat. 2017 Mar;27(3):363-382.

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