PATENT CLAIM ANALYSIS

Application Number: 16201117
Application Type: Utility
Filing Date: 2018-11
Publication Date: 2019-08
Patent Classification: ["546", "200000"]

Abstract:
The invention provides novel asymmetric and symmetric bisaminoquinolmes and related compounds, methods of treatment and syntheses. The novel compounds exhibit effective anticancer activity and are useful in the treatment of a variety of autophagy-related disorders.

Claim (Index 5):
A compound of formula IE: Wherein R 1  and R 1\u2032  are each independently H, halo (F, Cl, Br or I), CN, NO 2 , optionally substituted C 1 -C 6  alkyl, optionally substituted O\u2014C 1 -C 6  alkyl, optionally substituted \u2014(NH)-acyl, optionally substituted C 2 -C 7  acyl or optionally substituted C 2 -C 7  ester (oxycarbonyl ester or carboxyester, preferably carboxyester); R M  is independently at each occurrence H, F, Cl, Br, I, an optionally substituted C 1 -C 12  (preferably C 1 -C 8 ) alkyl, alkene, alkynyl or alkoxy group; R and R\u2032 are each independently H, a C 1 -C 6  optionally substituted alkyl group, a C 1 -C 7  (preferably C 2 -C 7 ) optionally substituted acyl group, a C 2 -C 7  optionally substituted carboxy ester group (which forms a urethane group with the nitrogen atom to which R or R 1\u2032  is bonded); Linker group L 1E  is a \ue8a0CH 2 Y\ue8a0 n X\ue8a0Y\u2032CH 2 \ue8a0 n  group or a A\ue8a0CH 2 \u2014CH 2 \u2014Z\ue8a0 n A\u2032 group wherein at least one of the CH 2  groups in L 1E  is optionally substituted with an optionally substituted C 1 -C 6  alkyl group including a cyclic alkyl group, each of which alkyl groups is optionally substituted, or at least two methylene groups (preferably two adjacent methylene groups) are optionally substituted with alkylene groups to form an optionally substituted C 3 -C 8  cycloalkyl group, or linker group L 1E  is a (poly)ethylene glycol group having from 1 to 20 ethylene glycol units, each (poly)ethylene glycol group being optionally substituted at one or both of its distal ends with an A group, or L is a linear group containing from 1 to 5 non-contiguous amine groups N\u2014R\u2033, each amine group being separated from an adjacent amine group by an alkylene group containing from 1, 2, 3, 4, 5, 6, 7, or 8 (preferably 2, 3, 4, 5 or 6) methylene groups or an ethylene glycol containing group having from 1 to 6 (preferably 2 to 6, 3 to 6 or 4, 5 or 6) ethylene glycol units; X is absent, (CH 2 ) j  O, S or N\u2014R\u2033; Y is absent, CH 2 , O, CH 2 O or N\u2014R\u2033 and Y\u2032 is absent CH 2 , O, OCH 2  or N\u2014R\u2033, with the proviso that when one or more of X, Y and Y\u2032 is present, each of X and Y, X and Y\u2032 or Y and Y\u2032, when present, forms a stable bond; R\u2033 is H or an optionally substituted C 1 -C 6  alkyl group or an amine protecting group; each j is independently 1, 2, 3, 4, 5 or 6; each n is independently 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 with the proviso that when n is 0, X is (CH 2 ) j  where j is at least 1 and at least one CH 2  group is optionally substituted, preferably with a C 1 -C 3  alkyl group which itself is optionally substituted with one or two hydroxyl groups or one, two, or three halo groups; A is absent, C\u2550O or (CH 2 ) j  and A\u2032 is C\u2550O or (CH 2 ) j  wherein at least one CH 2  group in A or A\u2032 is optionally substituted, preferably with a C 1 -C 3  alkyl group which is itself optionally substituted; Z is O or N\u2014R Z ; R Z  is H or an optionally substituted C 1 -C 3  alkyl group, or a pharmaceutically acceptable salt, enantiomer, diastereomer, solvent or polymorph thereof.

Metadata:
- Claim Count in Document: 17.0
- Percentile: 98.0
- Lexical Diversity: 1.35714
- Patent Class: 546.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['15502330', '15384823', '15890040', '15580978', '14396956']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7830842873000349
- 35 USC 102 Novelty (BERT): 0.6493613653236274
- Combined Prediction Score: 0.7697119951023942
- Mean Citation Score: 356.153908
- Max Citation Score: 619.825
- Similarity Product: 606.7312961816788

Labels:
- Claim Label 101: 1
- Claim Label 102: 0
- Claim Label 103: 1
- Claim Label 112: 1
- Combined Label: 0
- Label 101 Adjusted: 1

Dataset: test