PATENT CLAIM ANALYSIS

Application Number: 15946355
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2019-02
Patent Classification: ["514", "305000"]

Abstract:
The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy.

Claim (Index 9):
A method for reducing globotriaosylceramide (GL-3) in the heart of a subject having or at risk of having Fabry disease, wherein the method comprises administering to the subject an effective amount of a compound represented by the following structural formula, or a pharmaceutically acceptable salt or prodrug thereof, wherein: n is 1, 2 or 3; m is 0 or 1; p is O or 1; t is 0, 1 or 2; y is 1 or 2; z is 0, 1 or 2; E is S, O, NH, NOH, NNO 2 , NCN, NR, NOR or NSO 2 R; X 1  is CR 1  when m is 1 or N when m is 0; X 2  is O, \u2014NH, \u2014CH 2 \u2014, SO 2 , NH\u2014SO 2 ; CH(C 1 -C 6 ) alkyl or \u2014NR 2 ; X 3  is O, \u2014NH, \u2014CH 2 \u2014, CO, \u2014CH(C 1 -C 6 ) alkyl, SO 2 NH, \u2014CO\u2014NH\u2014 or \u2014NR 3 ; X 4  is CR 4 R 5 , CH 2 CR 4 R 5  or CH 2 \u2014(C 1 -C 6 ) alkyl-CR 4 R; X 5  is a direct bond, O, S, SO 2 , CR 4 R 5 ; (C 1 -C 6 )alkyl, (C 1 -C 6 )alkyloxy, (C 1 -C 6 )alkenyl, (C 1 -C 6 )alkenyloxy; R is (C 6 -C 12 )aryl, (C 2 -C 9 )heteroaryl, (C 1 -C 6 )alkyl, (C 2 -C 9 )heteroaryl(C 1 -C 6 )alkyl; R 1  is H, CN, (C 1 -C 6 )alkylcarbonyl, or (C 1 -C 6 )alkyl; R 2  and R 3  are each independently \u2014H, (C 1 -C 6 )alkyl optionally substituted by one or more substituents selected from the group consisting of halogen, (C 1 -C 6 )alkyl, (C 6 -C 12 )aryl, (C 2 -C 9 )heteroaryl, (C 1 -C 6 )alkyl(C 6 -C 12 )aryl, halo(C 6 -C 12 )aryl, and halo(C 2 -C 9 )heteroaryl, or optionally when X 2  is \u2014NR 2  and X 3  is \u2014NR 3 , R 2  and R 3  may be taken together with the nitrogen atoms to which they are attached form a non-aromatic heterocyclic ring optionally substituted by with one or more substituents selected from halogen, (C 1 -C 6 )alkyl, (C 6 -C 12 )aryl, (C 2 -C 9 )heteroaryl, (C 1 -C 6 )alkyl(C 6 -C 12 )aryl, halo(C 6 -C 12 )aryl, and halo(C 2 -C 9 )heteroaryl; R 4  and R 5  are independently selected from H, (C 1 -C 6 )alkyl, or taken together with the carbon to which they are attached to form a spiro (C 3 -C 10 )cycloalkyl ring or spiro (C 3 -C 10 )cycloalkoxy ring; R 6  is \u2014H, halogen, \u2014CN, (C 6 -C 12 )aryl, (C 6 -C 12 )aryloxy, (C 1 -C 6 )alkyloxy; (C 1 -C 6 )alkyl optionally substituted by one to four halo or (C 1 -C 6 )alkyl; A 1  is (C 2 -C 6 )alkynyl; (C 3 -C 10 )cycloalkyl, (C 6 -C 12 )aryl, (C 2 -C 9 )heteroaryl, (C 2 -C 9 )heterocycloalkyl or benzo(C 2 -C 9 )heterocycloalkyl optionally substituted with one or more substituents selected from the group consisting of halo, (C 1 -C 6 )alkyl optionally substituted by one to three halo; (C 1 -C 6 )alkenyl, amino, (C 1 -C 6 )alkylamino, (C 1 -C 6 )dialkylamino, (C 1 -C 6 )alkoxy, nitro, CN, \u2014OH, (C 1 -C 6 )alkyloxy optionally substituted by one to three halo; (C 1 -C 6 )alkoxycarbonyl, and (C 1 -C 6 ) alkylcarbonyl; A 2  is H, (C 3 -C 10 )cycloalkyl, (C 6 -C 12 )aryl, (C 2 -C 9 )heteroaryl, (C 2 -C 9 )heterocycloalkyl or benzo(C 2 -C 9 )heterocycloalkyl optionally substituted with one or more substituents selected from the group consisting of halo, (C 1 -C 6 )alkyl optionally substituted by one to three halo; (C 1 -C 6 )alkylenyl, amino, (C 1 -C 6 ) alkylamino, (C 1 -C 6 )dialkylamino, (C 1 -C 6 )alkoxy, O(C 3 -C 6  cycloalkyl), (C 3 -C 6 ) cycloalkoxy, nitro, CN, OH, (C 1 -C 6 )alkyloxy optionally substituted by one to three halo; (C 3 -C 6 ) cycloalkyl, (C 1 -C 6 ) alkoxycarbonyl, (C 1 -C 6 ) alkylcarbonyl, (C 1 -C 6 ) haloalkyl; with the proviso that the sum of n+t+y+z is not greater than 6; with the proviso that when p is 0; X 2  is NH\u2014SO 2  and X 3  is NH; with the proviso that when n is 1; t is 0; y is 1; z is 1; X 2  is NH; E is O; X 3  is NH; A 2  is H and X 5  is a direct bond; A 1  is not unsubstituted phenyl, halophenyl or isopropenyl phenyl; with the proviso that when n is 1; t is 0; y is 1; z is 1; X 2  is O; E is O; X 3  is NH; A 1  is (C 6 -C 12 )aryl and X 5  is a direct bond; A 2  is H and R 4  is H then R 5  is not cyclohexyl; and with the proviso that when n is 1; t is 0; y is 1; z is 1; X 2  is NH; E is O; X 3  is CH 2 ; R 4  and R 5  are both hydrogen; A 2  is H and X 5  is a direct bond; then A 1  is not unsubstituted phenyl.

Metadata:
- Claim Count in Document: 2.0
- Percentile: 91.0
- Lexical Diversity: 1.0625
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14030725', '14471958', '14776443', '15593440', '15630068']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8416046767757734
- 35 USC 102 Novelty (BERT): 0.5598743815648688
- Combined Prediction Score: 0.813431647254683
- Mean Citation Score: 395.667856
- Max Citation Score: 544.67175
- Similarity Product: 302.510502744019

Labels:
- Claim Label 101: 1
- Claim Label 102: 1
- Claim Label 103: 1
- Claim Label 112: 1
- Combined Label: 1
- Label 101 Adjusted: 1

Dataset: test