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 T14912 Target Info
Target Name Induced myeloid leukemia cell differentiation protein Mcl-1 (MCL1)
Synonyms mcl1/EAT; Bcl2-L-3; Bcl-2-related protein EAT/mcl1; Bcl-2-like protein 3; BCL2L3
Target Type Clinical trial Target
Gene Name MCL1
Biochemical Class B-cell lymphoma Bcl-2
UniProt ID
MCL1_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2012122370
Title Compositions and Methods Useful for Treating Diseases.
Abstract The present invention relates to a compositions for and methods of cancer treatment in which compounds of Formula I or Formula II. In some aspects, the treatment of B-cell Lymphoma or other hematopoietic cancers is encompassed. In other aspects, the invention provides methods for treating particular types of hematopoietic cancers, such as B-cell lymphoma, using a combination of one or more compounds of Formula I or Formula II. Combination therapy with, for example, a class of therapeutics known as 26S proteasome inhibitors, for example, Bortezomib, are also included. In another aspect the present invention relates to autoimmune treatment with compounds of Formula I or Formula II. In another aspect, this invention relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have unique in vitrio properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease.
Applicant(s) Eutropics Pharmaceuticals, Inc
Patent ID WO2015031608
Title Substituted Indole Mcl-1 Inhibitors.
Abstract The present application, among other things, provides compounds that are capable of inhibiting the activity of anti-apoptotic Bcl-2 family proteins, for example, myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides pharmaceutical compositions as well as methods for using provided compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein. In some embodiments, a provided compound has the structure of formula I. In some embodiments, a provided compound has the structure of formula II.
Applicant(s) Vanderbilt University
Representative Drug(s) D0C2DV Drug Info Ki = 7 nM Click to Show More [1]
2 D0F8LE Drug Info Ki = 100 to 50000 nM [1]
Patent ID WO2016033486
Title Tetrahydronaphthalene Derivatives That Inhibit Mcl-1 Protein.
Abstract Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, (I) and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
Applicant(s) Amgen Inc
Representative Drug(s) D0JZ4W Drug Info IC50 = 31 nM [1]
Patent ID WO2015097123
Title New Thienopyrimidine Derivatives, A Process for Their Preparation and Pharmaceutical Compositions Containing Them.
Abstract Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R12, X, A and n are as defined in the description.
Applicant(s) Servier Lab
Representative Drug(s) D0M6MP Drug Info IC50 = 3.3 nM [1]
Patent ID WO2014047427
Title Substituted Benzofuran, Benzothiophene and Indole Mcl-1 Inhibitors.
Abstract The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.
Applicant(s) Vanderbilt University
Representative Drug(s) D0IS8R Drug Info Ki = 370 nM Click to Show More [1]
2 D0I9PC Drug Info N.A. [1]
Patent ID WO2013149124
Title Small Molecule Inhibitors of Mcl-1 and Uses Thereof.
Abstract This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a [(1-Piperazinyl)-4-pyridinylmethyl]-Naphtho[1,2-b]furan structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.
Applicant(s) The Regents of the University of Michigan
Representative Drug(s) D0NT2S Drug Info IC50 = 75 nM [1]
Patent ID WO2013142281
Title Inhibition of Mcl-1 and/or Bfl-1/A1.
Abstract This disclosure features compounds and pharmaceutically acceptable salts thereof that inhibit MCL-1 and/or BFL-1/A1 and compositions containing the same. This disclosure also features combinations that include one or more of the MCL-1/BFL-1/A1 inhibitor compounds described herein, or a pharmaceutically acceptable salt thereof; and one or more additional therapeutic agents (e.g., one or more chemotherapeutic agents (including small molecule and/or anti-body based chemotherapy and/or radiation); e.g., one or more therapeutic agents that modulate apoptosis; e.g., one or more therapeutic agents that bind to and inhibit anti-apoptotic proteins or modulate them indirectly; e.g., one or more therapeutic agents that bind to and inhibit, or indirectly modulate, anti-apoptotic BCL-2, BCL-XL, BCL-w, MCL-1, and/or BFL-1/A1; e.g., one or more therapeutic agents that directly bind to and inhibit anti-apoptotic BCL-2 / BCL-XL; e.g., agents such as ABT-199, ABT-263 and ABT-737; e.g., ABT-737), or (where applicable) a pharmaceutically acceptable salt of the one or more therapeutic agents (as well as compositions containing the same). Also featured are methods of using such compounds, salts, combinations, and compositions, e.g., for the treatment or prevention of diseases, disorders, and conditions associated with deregulated apoptosis of cells (e.g., diseased or damaged cells; e.g., insufficient apoptosis of diseased or damaged cells or reduced apoptosis of diseased or damaged cells).
Applicant(s) Dana Farber Cancer Institute, Inc
Representative Drug(s) D0QE9E Drug Info IC50 = 14 nM Click to Show More [1]
2 D0LO7X Drug Info IC50 = 1200 nM [1]
Patent ID WO2013052943
Title Small Molecule Inhibitors of Mcl-1 and Uses Thereof.
Abstract This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having sulfonamido-1-hydroxynaphthalene structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.
Applicant(s) The Regents of the University of Michigan
Representative Drug(s) D0TU3N Drug Info Ki = 5300 nM Click to Show More [1]
2 D00BEJ Drug Info N.A. [1]
Patent ID WO2011094708
Title Small Molecules for The Modulation of Mcl-1 and Methods of Modulatiing Cell Death, Cell Division, Cell Differentiation and Methods of Treating Disorders.
Abstract This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients.
Applicant(s) Dana-Farber Cancer Institute, Inc
Representative Drug(s) D0QE9E Drug Info IC50 = 14 nM Click to Show More [1]
2 D0LO7X Drug Info IC50 = 1200 nM [1]
Patent ID WO2010024783
Title Biarylrhodanine and Pyridylrhodanine Compounds and Their Use.
Abstract The present invention pertains generally to the field of therapeutic compounds, and more specifically to compounds related to rhodanine, which compounds are inter alia inhibitors and/or binders of antiapoptotic/pro-survival Bcl-2 proteins such as Bcl-XL and/or Mcl-1. More specifically, the present invention is concerned with Rhodanine- based Pan-Bcl-2 inhibitors and Mcl-1 -specific inhibitors as anti-cancer compounds. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit and/or bind Bcl-2 proteins such as Bcl-XL and/or Mcl-1, and in the treatment of diseases and conditions that are mediated by Bcl-2 proteins, that are ameliorated by the inhibition of Bcl-2 protein function (such as Bcl-XL and/or Mcl-1 ) including proliferative conditions such as cancer, optionally in combination with another agent.
Applicant(s) Agency for Science, Technology and Research
Representative Drug(s) D09XWR Drug Info Ki = 22000 nM Click to Show More [1]
2 D0F9QC Drug Info Ki = 78000 nM [1]
Patent ID WO2008131000
Title 7-Substituted Indole Mcl-1 Inhibitors.
Abstract Compounds of formula (I) which inhibit the activity of anti-apoptotic McI-I protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated McI-I protein are disclosed.
Applicant(s) Abbott Laboratories
Representative Drug(s) D0IV8T Drug Info N.A. Click to Show More [1]
2 D0RJ1U Drug Info N.A. [1]
Patent ID WO2008130970
Title 7-Nonsubstituted Indole Mcl-1 Inhibitors.
Abstract Compounds of formula (I) which inhibit the activity of anti-apoptotic Mcl-1 protein, compositins containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.
Applicant(s) Abbott Laboratories
Representative Drug(s) D0DG0F Drug Info N.A. Click to Show More [1]
2 D0H3NO Drug Info N.A. [1]
3 D0JA5B Drug Info N.A. [1]
Patent ID WO2007008627
Title Apoptosis Promoters.
Abstract Compounds which inhibit the activity of anti-apoptotic Mcl-I protein, compositions containing the compounds and methods of treating diseases during which are expressed the Mcl- 1 protein are disclosed.
Applicant(s) Abbott Laboratories
Representative Drug(s) D03FZI Drug Info N.A. Click to Show More [1]
2 D09SGU Drug Info N.A. [1]
Patent ID WO2015153959
Title Small Molecule Inhibitors of Mcl-1 and Uses Thereof.
Abstract This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having pyrazolopyridine structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.
Applicant(s) The Regents of the University of Michigan
Representative Drug(s) D0J9FN Drug Info Ki = 130 nM [1]
Patent ID WO2015148854
Title Substituted Indole Mcl-1 Inhibitors.
Abstract The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.
Applicant(s) Vanderbilt University
Representative Drug(s) D0MZ7I Drug Info Ki < 7 nM [1]
References  Top
REF 1 Mcl-1 inhibitors: a patent review.Expert Opin Ther Pat. 2017 Feb;27(2):163-178.

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