PATENT CLAIM ANALYSIS

Application Number: 16076813
Application Type: Utility
Filing Date: 2018-08
Publication Date: 2019-01
Patent Classification: ["514", "228200"]

Abstract:
In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminothiazine dioxide compounds bearing an ether linker, including compounds Formula (I) or a tautomer thereof and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R 1 , R 2 , R 3 , R A , ring A, m, n, -L 1 -, ring B, R B , and p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.

Claim (Index 1):
A compound, or a pharmaceutically acceptable salt thereof, said compound having the structural Formula (I): or a tautomer thereof having the structural Formula (r): or pharmaceutically acceptable salt thereof, wherein: ring C is selected from the group consisting of tetrahydrofuranyl and tetrahydropyranyl, wherein 1 or 2 of the ring carbon atoms having two available substitutable hydrogen atoms of said tetrahydrofuranyl and tetrahydropyranyl rings are optionally independently replaced with a \u2014C(R C1 R C2 )\u2014 group, wherein R C1  and R C2  are each independently selected from the group consisting of H, halogen, \u2014CO 2 \u2014(C 1 -C 6 -alkyl), alkyl, cycloalkyl, -alkyl-cycloalkyl, heterocycloalkyl, -alkyl-heterocycloalkyl, aryl, -alkyl-aryl, heteroaryl, and -alkyl-heteroaryl,\n wherein each said alkyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl of R C1  and R C2  are optionally substituted with one or more R 3 , and \n wherein 1 to 2 non-adjacent, non-terminal carbon atoms in each said alkyl of R C1  and R C2  are optionally independently replaced with \u2014O\u2014, \u2014NH\u2014, \u2014N(C 1 -C 6 -alkyl)-, \u2014S\u2014, \u2014S(O)\u2014, or \u2014S(O) 2 \u2014, \n or, alternatively, wherein said R C1  and R C2  of one said \u2014C(R C1 R C2 )\u2014 group are taken together with the carbon to which they are attached form a spirocyclic ring consisting of from 3 to 6 carbon atoms, wherein 1 of said carbon atoms may be replaced with \u2014O\u2014, \u2014NH\u2014, \u2014N(C 1 -C 6 -alkyl)-, \u2014N(C 1 -C 6 -haloalkyl)-, \u2014S\u2014, \u2014S(O)\u2014, or \u2014S(O) 2 \u2014, and wherein 1 to 2 of the carbon atoms of said spirocyclic ring may be optionally independently substituted with 1 to 2 fluorine, C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, or \u2014CH 2 O\u2014(C 1 -C 6 -alkyl); R 1  is selected from the group consisting of H, halogen, and alkyl, wherein said alkyl is optionally substituted with one or more fluorine, and wherein 1 to 2 non-adjacent, non-terminal carbon atoms in said alkyl are optionally independently replaced with \u2014O\u2014, \u2014NH\u2014, \u2014N(alkyl)-, \u2014S\u2014, \u2014S(O)\u2014, or \u2014S(O) 2 \u2014; R 2  and R 3  are each independently selected from the group consisting of H, halogen, alkyl, cycloalkyl, -alkyl-cycloalkyl, heterocycloalkyl, -alkyl-heterocycloalkyl, aryl, -alkyl-aryl, heteroaryl, and -alkyl-heteroaryl, wherein each said alkyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl of R 2  and R 3  are optionally substituted with one or more R 4 , and wherein 1 to 2 non-adjacent, non-terminal carbon atoms in each said alkyl of R 2  and R 3  are optionally independently replaced with \u2014O\u2014, \u2014NH\u2014, \u2014N(C 1 -C 3 -alkyl)-, \u2014S\u2014, \u2014S(O)\u2014, or \u2014S(O) 2 \u2014, or, alternatively, R 2  and R 3  are taken together with the carbon to which they are attached form a spirocyclic ring consisting of from 3 to 6 carbon atoms, wherein 1 of said carbon atoms may be replaced with \u2014O\u2014, \u2014NH\u2014, \u2014N(C 1 -C 3 -alkyl)-, \u2014N(C 1 -C 3 -haloalkyl)-, \u2014S\u2014, \u2014S(O)\u2014, or \u2014S(O) 2 \u2014, and wherein 1 to 2 of the carbon atoms of said spirocyclic ring may be optionally independently substituted with 1 to 2 fluorine, C 1 -C 3 -alkyl, C 1 -C 3 -haloalkyl, or \u2014CH 2 O\u2014(C 1 -C 3 -alkyl); ring A is selected from the group consisting of aryl and heteroaryl; m is 0 or more, with the proviso that the value of m does not exceed the number of available substitutable hydrogen atoms on ring A; each R A  (when present) is independently selected from the group consisting of halogen, oxo, \u2014OH, \u2014CN, alkyl, \u2014O-alkyl, and cycloalkyl, wherein said alkyl, \u2014O-alkyl, and cycloalkyl of R A  are each optionally independently unsubstituted or substituted with one or more fluorine, and wherein 1 to 2 non-adjacent, non-terminal carbon atoms in said alkyl and \u2014O-alkyl are optionally independently replaced with \u2014O\u2014, \u2014NH\u2014, \u2014N(C 1 -C 3 -alkyl)-, \u2014S\u2014, \u2014S(O)\u2014, or \u2014S(O) 2 \u2014; n is 0 or 1; -L 1 - (when present) independently represents a bond or a divalent moiety selected from the group consisting of \u2014O\u2014, \u2014CH 2 O\u2014, \u2014CH(CH 3 )O\u2014, \u2014CH(CF 3 )O\u2014, and \u2014CH(CHF 2 )O\u2014; ring B is selected from the group consisting of aryl, heteroaryl, cycloalkyl, and heterocycloalkyl; p is 0 or more, with the proviso that the value of p does not exceed the number of available substitutable hydrogen atoms on ring B; and each R B  (when present) is independently selected from the group consisting of halogen, oxo, \u2014OH, \u2014CN, \u2014SF 5 , \u2014OSF 5 , \u2014OR B1 , \u2014SR B1 , alkyl, alkenyl, alkynyl, cycloalkyl, -alkyl-cycloalkyl, heterocycloalkyl, -alkyl-heterocycloalkyl, aryl, and heteroaryl, wherein said each alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl of R B  are each optionally independently unsubstituted or substituted with one or more groups independently selected from R 4 , and wherein 1 to 2 non-adjacent, non-terminal carbon atoms in said alkyl are optionally independently replaced with \u2014O\u2014, \u2014NH\u2014, \u2014N(alkyl)-, \u2014S\u2014, \u2014S(O)\u2014, or \u2014S(O) 2 \u2014; each R B1  is independently selected from the group consisting of H, alkyl, alkenyl, alkynyl, cycloalkyl, -alkyl-cycloalkyl, heterocycloalkyl, and -alkyl-heterocycloalkyl, wherein each said alkyl, alkenyl, alkynyl, cycloalkyl, and heterocycloalkyl, of R B1  is unsubstituted or optionally substituted with one or more fluorine, and wherein 1 to 2 non-adjacent, non-terminal carbon atoms in said alkyl are optionally independently replaced with \u2014O\u2014, \u2014NH\u2014, \u2014N(C 1 -C 6 -alkyl)-, \u2014S\u2014, \u2014S(O)\u2014, or \u2014S(O) 2 \u2014; each R 4  (when present) is independently selected from the group consisting of halogen, \u2014OH, \u2014CN, C 1 -C 6 -alkyl, \u2014(C 1 -C 6 -alkyl)-OH, \u2014O\u2014(C 1 -C 6 -alkyl), cycloalkyl, \u2014(C 1 -C 6 -alkyl)-cycloalkyl, \u2014O-cycloalkyl, \u2014O\u2014(C 1 -C 6 -alkyl)-cycloalkyl, heterocycloalkyl, \u2014(C 1 -C 6 -alkyl)-heterocycloalkyl, \u2014O-heterocycloalkyl and \u2014O\u2014(C 1 -C 6 -alkyl)-heterocycloalkyl, wherein each said C 1 -C 6 -alkyl, cycloalkyl, and heterocycloalkyl are optionally substituted with one or more halogen, and wherein 1 to 2 non-adjacent, non-terminal carbon atoms in each said C 1 -C 6 -alkyl is optionally independently replaced with \u2014O\u2014, \u2014NH\u2014, \u2014N(C 1 -C 3 -alkyl)-, \u2014S\u2014, \u2014S(O)\u2014, or \u2014S(O) 2 \u2014.

Metadata:
- Claim Count in Document: 6.0
- Percentile: 96.0
- Lexical Diversity: 1.62921
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15527975', '16076441', '15780651', '15104257', '14240215']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8604829251752228
- 35 USC 102 Novelty (BERT): 0.6466615365264929
- Combined Prediction Score: 0.8391007863103499
- Mean Citation Score: 523.9988719999999
- Max Citation Score: 615.5891
- Similarity Product: 608.51367741974

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