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 T05880 Target Info
Target Name Gamma-secretase subunit APH-1A/1B (APH-1)
Synonyms Anterior pharynx-defective 1
Target Type Patented-recorded Target
Gene Name APH1A-APH1B
UniProt ID
APH1A_HUMAN - APH1B_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2014084471
Title Novel N-Acetyl-L-Leucyl-L-Leucyl-L-Norleucinal (Alln) Derivative Compound, Composition for Preventing or Treating Malaria.
Abstract The present invention relates to an antimalarial composition containing an N-acetyl-L-Leucyl-L-leucyl-L-norleucinal (ALLN) derivative compound as an active ingredient. The ALLN derivative compound of.
Applicant(s) Wonkwang University Center for Industry-Academy Cooperation
Representative Drug(s) D08VTV Drug Info IC50 = 17 nM Click to Show More [1]
2 D0FV9R Drug Info IC50 = 50000 nM [1]
Patent ID WO2007034326
Title Imidazole Compounds for The Treatment of Neurological Disorders.
Abstract The present invention relates to compounds of Formula (I) wherein R1, R2, R3, R4, R6, R7 and A are as defined. Compounds of Formula (I) have activity inhibiting production of Agama-peptide. The invention also relates to pharmaceutical compositions and methods for treating diseases and disorders, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of Formula (I).
Applicant(s) Pfizer Products Inc
Representative Drug(s) D0PS0J Drug Info IC50 = 1.2 nM Click to Show More [1]
2 D09UJB Drug Info IC50 = 4 nM [1]
Patent ID WO2004092155
Title Fluoro-and Trifluoroalkyl-Containing Heterocyclic Sulfonamide Inhibitors of Beta Amyloid Production and Derivatives Thereof.
Abstract Compounds of Formula (I), are provided where T is CHO, COR8, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substitutedalkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substitutedphenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y=C, or substituted diene fused to Y when Y=C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.
Applicant(s) KREFT, Anthony, Frank et al
Representative Drug(s) D0C6OW Drug Info EC50 = 12.4 Nm Click to Show More [1]
2 D0D8IZ Drug Info IC50 = 16 nM [1]
3 D0OL7Q Drug Info IC50 = 25 nM [1]
Patent ID WO2014085211
Title Spirocyclic Sulfones As Gamma Secretase Inhibitors.
Abstract Disclosed herein are compounds of Formula (I), wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0A0UX Drug Info IC50 = 2 nM [1]
Patent ID WO2013036464
Title Gamma Secretase Inhibitors.
Abstract Disclosed herein are compounds of Formula (I) (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0HL6X Drug Info IC50 = 1.4 nM [1]
Patent ID WO2008145525
Title Process for The Preparation of Dibenzo [B,D]Azepin-6-One Derivative.
Abstract The invention relates to a process for the optical resolution of a dibenzo[b,d]azepinone derivative of the formula (II) wherein R1 is hydrogen or halogen and R2 has the meaning of C1-4-alkyl optionally substituted with C3-7-cycloalkyl or benzyl which is optionally substituted with C1-4-alkoxy to obtain a (S)-7-amino-5H,7H-dibenzo[b,d]azepin-6-one of the formula (I) wherein R1 is as above. The (S)-7-amino-5H,7H-dibenzo[b,d]azepin-6-ones of formula (I) can be used as chiral building blocks for the preparation of malonamide derivatives which have the potential to act as gama-secretase inhibitors and therefore may be useful in the treatment of Alzheimer's disease and cancer.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0D2BV Drug Info IC50 = 14 nM [1]
Patent ID WO2005118634
Title Helical Peptidomimetics with Enhanced Activity Against Beta-Amyloid Production.
Abstract Helical peptidomimetic compounds as inhibitors of beta-amyloid production are provided. These inhibitors have sequences with lengths from 11 to 16 amino acids, inclusive. These inhibitors potently inhibit intramembrane proteases, notably aspartyl secretases involved in the enzymatic cleavage of amyloid precursor protein (APP) to yield amyloid-gama-peptide. Methods are provided for making a medicament containing the compounds and for administering the compounds to treat gama-amyloid-associated diseases, notably Alzheimer's disease.
Applicant(s) The Brigham and Women'S Hospital, Inc
Representative Drug(s) D0PG2V Drug Info IC50 = 140 pM [1]
Patent ID WO2004031139
Title Cyclohexyl Sulphones As Gamma-Secretase Inhibitors.
Abstract Compounds of formula (I) inhibit the processing of APP by gamma-secretase, and hence are useful in treating or preventing Alzheimer's disease.
Applicant(s) Merck Sharp &Amp
Representative Drug(s) D0S5BD Drug Info IC50 = 15 nM [1]
Patent ID WO2003053912
Title Alpha-(N-Sulphonamido)Acetamide Derivatives As Beta -Amyloid Inhibitors.
Abstract There is provided a series of novel alpha-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of gama-amyloid peptide (gama-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D09SSG Drug Info IC50 = 16 nM [1]
Patent ID WO2002040451
Title Preparation of Lactam Derivative Useful for Inhibiting -Amyloid Peptide Release and/or Its Synthesis.
Representative Drug(s) D0J4PC Drug Info IC50 = 15 nM [1]
Patent ID WO02057252
Title Heterocyclic Sulfonamides Inhibitors of Beta Amyloid Production.
Representative Drug(s) D0OL7Q Drug Info IC50 = 25 nM [1]
United States Patent and Trademark Office (USPTO)
Patent ID US7105509
Title Benzodiazepine Derivatives As App Modulators.
Representative Drug(s) D0I9VU Drug Info IC50 = 0.06 nM Click to Show More [1]
2 D04NCC Drug Info IC50 = 1.2 nM [1]
3 D09UJB Drug Info IC50 = 4 nM [1]
Patent ID US8853274
Title Compositions Comprising Farnesyl Transferase Inhibitor (Fti) and A Gamma-Secretase Inhibitor (Gsi) for Targeting Glioblastomas Cells.
Representative Drug(s) D0E9IY Drug Info IC50 = 20 nM [1]
Patent ID US20140357620
Title Method for Administration of A Gamma Secretase Inhibitor for Treating Cancer.
Representative Drug(s) D0D2BV Drug Info IC50 = 14 nM [1]
Patent ID US20120183508
Title Gamma secretase inhibitor for treatment of herpesvirus infection.
Abstract This invention relates to methods and compositions for the treatment of malignancies associated with gamma-herpesvirus infection. Specifically, the invention s relates to the use of gamma-secretase inhibitors to prevent the production of intracellular Notch1 thereby arresting the growth of the infected cells.
Applicant(s) University of Pennsylvania
Representative Drug(s) D08VTV Drug Info IC50 = 17 nM [1]
Patent ID US2014227173
Title Cancer Treatment with Gamma-Secretase Inhibitors.
Representative Drug(s) D0K2YO Drug Info N.A. [2]
References  Top
REF 1 Gamma secretase inhibitors: a patent review (2013 - 2015).Expert Opin Ther Pat. 2017 Jul;27(7):851-866.
REF 2 Cancer stem cell (CSC) inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jul;27(7):753-761.

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