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 T66505 Target Info
Target Name Smoothened homolog (SMO)
Synonyms Smo-D473H; SMOH; Protein Gx
Target Type Successful Target
Gene Name SMO
Biochemical Class GPCR frizzled
UniProt ID
SMO_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2014071298
Title Cyclic Sulfonamide Containing Derivatives As Inhibitors of Hedgehog Signaling Pathway.
Abstract The invention relates generally to the creation and use of cyclic sulfonamide containing derivatives to inhibit the hedgehog signaling pathway and to the use of those compounds for the treatment of hyperproliferative diseases and angiogenesis mediated diseases.
Applicant(s) Nant Holdings Ip, Llc
Representative Drug(s) D0V9AB Drug Info EC50 = 0.005 nM Click to Show More [1]
2 D0B3XW Drug Info IC50 < 10 nM [1]
3 D0IW7A Drug Info IC50 < 10 nM [1]
4 D0K2FK Drug Info IC50 < 10 nM [1]
Patent ID WO2014012511
Title N-(3-Heteroarylaryl)-4-Arylarylcarboxamtdes and Analogs As Hedgehog Pathway Inhibitors and Use Thereof.
Abstract Disclosed are novel N-(3-heteroarylaryl)-4-arylarylcarboxamides and analogs thereof, represented by the Formula I: wherein C cyclic group, D1-D4, Q1, Q2, R5 are defined herein. Compounds having Formula (I) are hedgehog pathway inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of hedgehog activity, such as cancer.
Applicant(s) Impact Therapeutics, Inc
Representative Drug(s) D07ZUO Drug Info IC50 < 10 nM Click to Show More [1]
2 D0DH0O Drug Info IC50 < 10 nM [1]
3 D0J0AT Drug Info IC50 < 10 nM [1]
4 D0K6XL Drug Info IC50 < 10 nM [1]
5 D0R8UO Drug Info IC50 < 10 nM [1]
6 D0RH3O Drug Info IC50 < 10 nM [1]
Patent ID WO2013192301
Title Imidazo Bicyclic Imminium Compounds As Antitumor Agents.
Abstract Imidazobicycles having a quaternary nitrogen, i.e. imminium salts, are disclosed. Examples include derivatives of 6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepinium and 2,3-dihydroimidazo[2,1-b]thiazolium salts. The compounds are inhibitors of the Hedgehog pathway and therefore useful as antitumor agents and as probes of the function of Hedgehog-dependent systems.
Applicant(s) The Board of Trustes of the Leland Stanford Junior University
Representative Drug(s) D0XH5O Drug Info IC50 = 30 nM Click to Show More [1]
2 D0LH6R Drug Info IC50 = 80 nM [1]
3 D01AJO Drug Info IC50 = 140 nM [1]
4 D0AB3D Drug Info IC50 = 190 nM [1]
5 D0FS1J Drug Info IC50 = 340 nM [1]
6 D0KX5G Drug Info IC50 = 960 nM [1]
7 D0VR8N Drug Info IC50 = 1420 nM [1]
Patent ID WO2013142253
Title Treatment of Pancreatic and Related Cancers with 5-Acyl-6,7-Dihydrothieno[3,2-C]Pyridines.
Abstract Methods for inhibiting the growth of pancreatic cancer cells or other cancer cells driven by Sonic hedgehog are disclosed. The method involves exposing the cells to 5-acyl-6,7-dihydrothieno[3,2-c]pyridines of formula (I).
Applicant(s) Memorial Sloan-Kettering Cancer Center
Representative Drug(s) D0O7BH Drug Info IC50 = 680 nM Click to Show More [1]
2 D01AWH Drug Info IC50 = 2050 nM [1]
3 D00ITT Drug Info 98.90% inhibition = 12500 nM [1]
4 D03QAU Drug Info 100.80% inhibition = 12500 nM [1]
5 D0SO6T Drug Info 97.80% inhibition = 12500 nM [1]
Patent ID WO2013013614
Title 4-(3-Heteroarylarylamino)Quinazoline and 1-(3-Heteroarylarylamino)Isoquinoline As Hedgehog Pathway Inhibitor and Use Thereof.
Abstract Provided is novel 4-(3-heteroarylarylamino)quinazoline and 1-(3-heteroarylarylamino)isoquinoline of formula I, wherein ring C, A, R, and R2-R10 are defined in the text. The compound of formula I is a.
Applicant(s) Impact Therapeutics, Inc
Representative Drug(s) D0KC6Y Drug Info IC50 = 42 nM Click to Show More [1]
2 D06NBL Drug Info IC50 = 45 nM [1]
3 D0CD8G Drug Info IC50 = 46 nM [1]
4 D0B9ML Drug Info IC50 = 47 nM [1]
5 D0QO1Y Drug Info IC50 = 52 nM [1]
6 D0RV9D Drug Info IC50 = 52 nM [1]
Patent ID WO2014043608
Title Smoothened Modulators and Methods of Use Thereof.
Abstract Compounds of general Formulas (I), (IA), (IB) are described, along with compositions containing the same and methods of use thereof, inhibiting the hedgehog pathway in a cell or inhibiting unwanted proliferation of a cell.
Applicant(s) Duke University
Representative Drug(s) D07BIQ Drug Info IC50 = 2.6 nM Click to Show More [1]
2 D0Y6EY Drug Info N.A. [1]
Patent ID WO2014207069
Title Multitarget Hedgehog Pathway Inhibitors and Uses Thereof.
Abstract The present invention concerns compounds that selectively inhibit the activity of the Hedgehog (Hh) pathway, their preparation and uses thereof. The compounds of the present invention are useful in treating Hh-dependent tumors, such as medulloblastoma (MB).
Applicant(s) Universita 'Degli Studi Di Siena
Representative Drug(s) D00RRB Drug Info N.A. Click to Show More [2]
2 D01BGG Drug Info N.A. [2]
3 D04IFL Drug Info N.A. [2]
4 D05NRG Drug Info N.A. [2]
5 D09VIE Drug Info N.A. [2]
6 D0J1RB Drug Info N.A. [2]
7 D0TP0S Drug Info N.A. [2]
8 D0WI1G Drug Info N.A. [2]
9 D0Z6IS Drug Info N.A. [2]
Patent ID WO2013042082
Title Novel Compounds Modulating The Hedgehog Protein Signaling Pathway, Marked forms Thereof, and Applications.
Abstract The present invention relates to novel compounds having the following formula (I), and the use thereof as a drug, particularly for the treatment of tumors associated with hyperactivation of the hedgeh.
Applicant(s) Centre National De La Recherche Scientifique
Representative Drug(s) D05CWM Drug Info N.A. Click to Show More [1]
2 D05QYN Drug Info N.A. [1]
3 D0C4VR Drug Info N.A. [1]
4 D0E4TO Drug Info N.A. [1]
5 D0QA9Q Drug Info N.A. [1]
6 D0TK2O Drug Info N.A. [1]
7 D0ZF1N Drug Info N.A. [1]
Patent ID WO2014113191
Title Hedgehog Pathway Signaling Inhibitors and Therapeutic Applications Thereof.
Abstract The hedgehog (Hh) signaling pathway is a pathway which regulates patterning, growth and cell migration during embryonic development, but in adulthood is limited to tissue maintenance and repair. Mutational inactivation of the inhibitory pathway components leads to constitutive ligand-independent activation of the Hh signaling pathway, results in cancers such as basal cell carcinoma and medulloblastoma. Ligand-dependent activation of Hh signaling is involved in prostate cancer, pancreatic cancer, breast cancer and blood cancers. Therefore, inhibition of the aberrant Hh signaling represents a promising approach toward novel anticancer therapy. The invention provides novel molecules of formula I that inhibit hedgehog pathway signaling and provides therapeutic applications for the treatment of malignancies (basal cell carcinoma, medulloblastoma, glioblastoma, non-small cell lung cancer, prostate cancer, pancreatic cancer, blood cancers, mesenchymal cancers, etc.), prevention of tumor regrowth, sensitization of radio-chemo therapies, and other diseases (inflammation, fibrosis and immune disorders).
Applicant(s) Zhang, Xiaohu
Representative Drug(s) D0J9JS Drug Info IC50 = 21 nM [1]
United States Patent and Trademark Office (USPTO)
Patent ID US20130274233
Title Modulators of Hedgehog Signaling Pathway.
Representative Drug(s) D02JSW Drug Info IC50 < 10 nM Click to Show More [1]
2 D05QCM Drug Info IC50 < 10 nM [1]
3 D08LBZ Drug Info IC50 < 10 nM [1]
4 D0FT1X Drug Info IC50 < 10 nM [1]
5 D0PG1G Drug Info IC50 = 1460 nM [1]
6 D03SCM Drug Info IC50 = 1900 nM [1]
7 D0R3UI Drug Info IC50 = 1940 nM [1]
China National Intellectual Property Administration (CNIPA)
Patent ID CN103877562
Title Application of Rubia Alata Cyclopeptides As Hedgehog Signaling Path Inhibitor, and Their Preparation Methods and Application.
Abstract The invention provides a rubiaceae-type cyclopeptide taken as a novel Hedgehog signal channel inhibitor as well as a preparation method and an application of the rubiaceae-type cyclopeptide in preparation of a medicine for treating and preventing relevant cancers activated by the abnormity of Hedgehog signal channels. The rubiaceae-type cyclopeptide is prepared by the condensation of one D-alpha-alanine, one L-alpha-alanine, three substituted N-methyl-L-alpha-tyrosines and one L-alpha-amino acid of another type via peptide bonds, wherein six amino acids are condensed into an eighteen-membered rings; and benzene rings between two adjacent tyrosines are connected via an oxygen bridge so as to form a fourteen-membered ring.
Applicant(s) Kunming Institute of Botany, Chinese Academy of Sciences
Representative Drug(s) D0P8IR Drug Info IC50 = 1.24 nM Click to Show More [1]
2 D0I8RK Drug Info IC50 = 1.68 nM [1]
Patent ID CN104003990
Title Preparation of Heterocyclic Compounds As Hedgehog Signaling Path Inhibitors.
Representative Drug(s) D05MIG Drug Info IC50 = 1.3 nM Click to Show More [1]
2 D06ELK Drug Info IC50 = 1.3 nM [1]
3 D00GMI Drug Info IC50 < 2 nM [1]
4 D0B3FN Drug Info IC50 < 2 nM [1]
5 D0B6GA Drug Info IC50 < 2 nM [1]
6 D0C4PD Drug Info IC50 < 2 nM [1]
7 D0K8HU Drug Info IC50 < 2 nM [1]
8 D0Y8SC Drug Info IC50 < 2 nM [1]
9 D0IS8B Drug Info IC50 = 5 nM [1]
Patent ID CN103923066
Title Preparation of Multiple-Target Antitumor Compounds and Useful In The Treatment of Cancer.
Representative Drug(s) D0Y8JF Drug Info IC50 = 3.49 nM Click to Show More [1]
2 D0WJ3W Drug Info IC50 = 5.18 nM [1]
3 D07TVO Drug Info IC50 = 6.59 nM [1]
4 D0KH7Q Drug Info IC50 = 8.28 nM [1]
5 D0X5VI Drug Info IC50 = 9.24 nM [1]
Patent ID CN103910736
Title Preparation of Dihydropyranopyrimidine Derivatives As Hedgehog Signaling Inhibitor.
Representative Drug(s) D05MIG Drug Info IC50 = 1.3 nM Click to Show More [1]
2 D06ELK Drug Info IC50 = 1.3 nM [1]
3 D00GMI Drug Info IC50 < 2 nM [1]
4 D0B3FN Drug Info IC50 < 2 nM [1]
5 D0B6GA Drug Info IC50 < 2 nM [1]
6 D0C4PD Drug Info IC50 < 2 nM [1]
7 D0K8HU Drug Info IC50 < 2 nM [1]
8 D0Y8SC Drug Info IC50 < 2 nM [1]
9 D0IS8B Drug Info IC50 = 5 nM [1]
Patent ID CN103864770
Title Pyrimidinamines and Pyridylamines As Inhibitors for Hedgehog Signaling Conduction and Their Preparation, Pharmaceutical Compositions and Use In The Treatment of Cancer.
Representative Drug(s) D05MIG Drug Info IC50 = 1.3 nM Click to Show More [1]
2 D06ELK Drug Info IC50 = 1.3 nM [1]
3 D00GMI Drug Info IC50 < 2 nM [1]
4 D0B3FN Drug Info IC50 < 2 nM [1]
5 D0B6GA Drug Info IC50 < 2 nM [1]
6 D0C4PD Drug Info IC50 < 2 nM [1]
7 D0K8HU Drug Info IC50 < 2 nM [1]
8 D0Y8SC Drug Info IC50 < 2 nM [1]
9 D0IS8B Drug Info IC50 = 5 nM [1]
Patent ID CN103040824
Title Preparation of Signaling Pathway Inhibitors for Treating Tumors and Osteoporosis.
Abstract The present invention belongs to the technical field of medicine, particularly to a compound of one thienopyrimidine nucleus or a salt thereof, their preparation, compositions and compounds such as dipeptidyl peptidase (DPP-IV) inhibitors in the prevention or treatment of diseases benefiting from DPP-IV inhibition is. A compound of the present invention is simple preparation process, raw materials, suitable for industrial mass production, and in vitro experiments, which have very good selectivity for inhibition of DPP-, while effectively inhibiting DPP- activity of DPP- DPP- activity and almost no effect can be expected after the very low toxicity of the compound medicine developed the present invention has outstanding advantages.
Representative Drug(s) D0KS3J Drug Info IC50 = 40 nM Click to Show More [1]
2 D06MXI Drug Info IC50 = 100 nM [1]
Patent ID CN103923085
Title Preparation of Pyridine Heterocyclic Compounds with Hedgehog Pathway Antagonist Activity.
Representative Drug(s) D0K0IO Drug Info IC50 = 58 nM [1]
Patent ID CN103588771
Title Pyrimidine Derivatives As Hedgehog Pathway Antagonists and Their Preparation, Pharmaceutical Compositions and Use In The Treatment of Cancer.
Representative Drug(s) D03HMW Drug Info IC50 = 80 nM [1]
Patent ID CN103524535
Title Aminothiazole-Pyridine Heterocyclic Compounds As Hedgehog Pathway Antagonists and Their Preparation, Pharmaceutical Compositions and Use In The Treatment of Cancer.
Representative Drug(s) D0WB2S Drug Info IC50 = 87 nM [1]
References  Top
REF 1 Hedgehog inhibitors: a patent review (2013 - present).Expert Opin Ther Pat. 2015 May;25(5):549-65.
REF 2 Evaluation of WO2014207069 A1: Multitarget Hedgehog pathway inhibitors and uses thereof.Expert Opin Ther Pat. 2016;26(4):529-35.

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