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 T60631 Target Info
Target Name Proto-oncogene c-Ret (RET)
Synonyms RET51; RET receptor tyrosine kinase; RET mutant Y791F; RET mutant V804M; RET mutant V804L; RET mutant S891A; RET mutant M918T; RET mutant G691S; Proto-oncogene tyrosine-protein kinase receptor Ret; PTC; Cadherin family member 12; CDHR16; CDHF12; C-ret
Target Type Successful Target
Gene Name RET
Biochemical Class Kinase
UniProt ID
RET_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2015079251
Title Quinazoline Compounds.
Abstract The present invention relates to quinazoline compounds of formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity: (Formula (I)) wherein X, R1, R2, R3, R4, R5, R6 and R7 are each as defined herein. 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 RET kinase activity is implicated.
Applicant(s) Cancer Research Technology Limited
Representative Drug(s) D05PRG Drug Info IC50 = 3.9 nM Click to Show More [1]
2 D0DV4X Drug Info IC50 = 11 nM [1]
3 D0B3GX Drug Info N.A. [1]
Patent ID WO2014050781
Title Ret Inhibitor.
Abstract A compound represented by general formula (I) (the symbols in the formula are as defined in the description), a salt thereof, or the like is a RET inhibitor or RET tyrosine kinase inhibitor that can be used as an agent for the prevention or treatment of disorders including cancers and cancer metastases having mutations in RET.
Applicant(s) Chugai Pharmaceutical Co., Ltd
Representative Drug(s) D0O9JD Drug Info IC50 = 4.8 nM Click to Show More [1]
2 D08LCQ Drug Info N.A. [1]
Patent ID WO2014184069
Title Pyrrolo[2,3-D]Pyrimidine Derivatives, Process for Their Preparation and Their Use As Kinase Inhibitors.
Abstract The present invention relates to 6-amino-7-deaza-purine derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular RET family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions containing these compounds.
Applicant(s) Nerviano Medical Sciences S.R.L
Representative Drug(s) D07OLQ Drug Info N.A. Click to Show More [1]
2 D09FBJ Drug Info N.A. [1]
3 D0FU0I Drug Info N.A. [1]
4 D0NH2H Drug Info N.A. [1]
5 D0P1AH Drug Info N.A. [1]
Patent ID WO2014141187
Title Pyridine Derivatives As Rearranged During Transfection (Ret) Kinase Inhibitors.
Abstract This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, medullary thyroid cancer, follicular thyroid cancer, anaplastic thyroid cancer, papillary thyroid cancer, brain tumors, peritoneal cavity cancer, solid tumors, other lung cancer, head and neck cancer, gliomas, neuroblastomas, Von Hippel-Lindau Syndrome and kidney tumors, breast cancer, fallopian tube cancer, ovarian cancer, transitional cell cancer, prostate cancer, cancer of the esophagus and gastroesophageal junction, biliary cancer, adenocarcinoma, and any malignancy with increased RET kinase activity.
Applicant(s) Glaxosmithkline Intellectual Property Development Limited
Representative Drug(s) D03JZP Drug Info N.A. Click to Show More [1]
2 D03ORX Drug Info N.A. [1]
3 D0A6RR Drug Info N.A. [1]
4 D0JY9S Drug Info N.A. [1]
5 D0X7IS Drug Info N.A. [1]
6 D0YC7C Drug Info N.A. [1]
Patent ID WO2014072220
Title Substituted Pyrimidinyl and Pyridinyl-Pyrrolopyridinones, Process for Their Preparation and Their Use As Kinase Inhibitors.
Abstract The present invention relates to substituted pyrimidinyl- and pyridinylpyrrolopyridinone compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular RET family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions containing these compounds.
Applicant(s) Nerviano Medical Sciences S.R.L
Representative Drug(s) D05NBB Drug Info N.A. Click to Show More [1]
2 D07QKP Drug Info N.A. [1]
3 D0QY6M Drug Info N.A. [1]
4 D0XR9O Drug Info N.A. [1]
Patent ID WO2013077921
Title Substituted Pyrazolo[3,4-D]Pyrimidines and Uses Thereof.
Abstract Presented herein are novel therapeutic compounds and methods of using the same for the treatment of cancers.
Applicant(s) The Regents of the University of California
Representative Drug(s) D01BMX Drug Info N.A. Click to Show More [1]
2 D03MMZ Drug Info N.A. [1]
3 D05HYJ Drug Info N.A. [1]
4 D06BNK Drug Info N.A. [1]
Patent ID WO2012053606
Title Arylaminoheterocyclic Carboxamide Compound.
Applicant(s) Astellas Pharma Inc
Representative Drug(s) D0MX7B Drug Info N.A. [1]
Patent ID WO2014039971
Title Inhibitors of Met, Vegfr and Ret for Use In The Treatment of Lung Adenocarcinoma.
Abstract This invention is directed to the treatment of cancer in a patient, particularly a patient with lung adenocarcinoma, and more particularly a patient with KIF5B-RET fusion-positive non-small cell lung cancer, with an inhibitor of MET, VEGF, and RET which is a compound of Formula (I) or a pharmaceutically acceptable salt thereof.
Applicant(s) Exelixis, Inc
Patent ID WO2007049624
Title Preventives/Remedies for Cancer.
Abstract It is intended to provide a medicine containing a substance which inhibits the function of RET, for example, an antibody to RET. It is also intended to provide a medicine containing a substance which inhibits the function of GDNF, for example, an antibody to GDNF. Furthermore, it is intended to provide a medicine containing a substance which inhibits the function of GFRalpha1, for example, an antibody to GFRalpha1. These drugs are useful as preventives/remedies for cancer such as breast cancer, cancer cell growth inhibitors and so on.
Applicant(s) Takeda Pharmaceutical Co., Ltd
United States Patent and Trademark Office (USPTO)
Patent ID US20140272958
Title Ret Inhibitor.
Applicant(s) Chugai Pharmaceutical
Representative Drug(s) D0O9JD Drug Info IC50 = 4.8 nM Click to Show More [1]
2 D08LCQ Drug Info N.A. [1]
Patent ID US9382238
Title Pyridine Derivatives As Rearranged During Transfection (Ret) Kinase Inhibitors.
Applicant(s) Glaxosmithkline
Representative Drug(s) D03JZP Drug Info N.A. Click to Show More [1]
2 D03ORX Drug Info N.A. [1]
3 D0A6RR Drug Info N.A. [1]
4 D0JY9S Drug Info N.A. [1]
5 D0X7IS Drug Info N.A. [1]
6 D0YC7C Drug Info N.A. [1]
Patent ID US9321772
Title Substituted Pyrazolo[3,4-D]Pyrimidines and Uses Thereof.
Applicant(s) The Regents of the University of California
Representative Drug(s) D01BMX Drug Info N.A. Click to Show More [1]
2 D03MMZ Drug Info N.A. [1]
3 D05HYJ Drug Info N.A. [1]
4 D06BNK Drug Info N.A. [1]
Patent ID US9029386
Title Inhibitors of Kinase Activity.
Applicant(s) Ym Biosciences Australia Pty
Representative Drug(s) D0AK1F Drug Info N.A. Click to Show More [1]
2 D0NB1V Drug Info N.A. [1]
3 D0O0AW Drug Info N.A. [1]
4 D0O4TA Drug Info N.A. [1]
5 D0T7BE Drug Info N.A. [1]
Patent ID US20130137660
Title Inhibitors of Kinase Activity.
Applicant(s) Ym Biosciences Australia Pty
Representative Drug(s) D0AK1F Drug Info N.A. Click to Show More [1]
2 D0NB1V Drug Info N.A. [1]
3 D0O0AW Drug Info N.A. [1]
4 D0O4TA Drug Info N.A. [1]
5 D0T7BE Drug Info N.A. [1]
Patent ID US20120231001
Title Preventives/Remedies for Cancer.
Applicant(s) Takeda Pharmaceutical
References  Top
REF 1 RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.

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