PATENT CLAIM ANALYSIS

Application Number: 15752000
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-08
Patent Classification: ["514", "210180"]

Abstract:
Disclosed herein, in part, are fumagillol compounds and methods of use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making fumagillol compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

Claim (Index 1):
A compound represented by Formula I: wherein: is a single or double bond;\n R 1  and R 2 , together with the nitrogen to which they are attached, form a 4-6 membered saturated heterocyclic ring A which may have an additional heteroatom selected from the group consisting of O, S(O) w  (wherein w is 0, 1, or 2), and NR a ; heterocyclic ring A is substituted on an available carbon by a substituent represented by L-B; and wherein heterocyclic ring A is additionally and optionally substituted by one or two substituents each independently selected from the group consisting of halogen, hydroxyl, C 1-3 alkyl and C 1-3 alkoxy; wherein C 1-3 alkyl and C 1-3 alkoxy may optionally be substituted by one or more fluorine atoms or a substituent selected from the group consisting of cyano, hydroxyl, and N(R a R b ); L is selected from the group consisting of C 1-6 alkylene and C 1-6 alkenylene; wherein C 1-6 alkylene and C 1-6 alkenylene may optionally be substituted by one or two substituents each independently selected from the group consisting of halogen and hydroxyl; and wherein one or two methylene units of L may optionally and independently be replaced by a moiety selected from the group consisting of a bond, \u2014O\u2014, \u2014C(O)\u2014, \u2014O\u2014C(O)\u2014, \u2014C(O)\u2014O\u2014, \u2014NR a \u2014, \u2014C(O)\u2014NR a \u2014, \u2014NR a \u2014C(O)\u2014, \u2014O\u2014C(O)\u2014NR a \u2014, \u2014NR a \u2014C(O)\u2014O\u2014, \u2014S(O) w \u2014 (wherein w is 0, 1, or 2), \u2014S(O) w \u2014NR a \u2014, and \u2014NR a \u2014S(O) w \u2014; B is selected from the group consisting of R i R j N\u2014, heterocyclyl, heterocyclyloxy, heteroaryl, heterocyclyl-(NR a )\u2014, and hydrogen; wherein said heteroaryl may optionally be substituted with one or more substituents selected from R f ; and wherein said heterocyclyl is bound to L through a ring carbon and may optionally be substituted by one or more substituents selected from R g ; and wherein if said heterocyclyl contains a \u2014NH moiety that nitrogen may optionally be substituted by R h ; R i  and R j  are selected independently for each occurrence from the group consisting of hydrogen, C 1-6 alkyl, C 2-6 alkenyl, C 3-6 cycloalkyl, heterocyclyl and heterocyclylcarbonyl; wherein C 1-6 alkyl, C 2-6 alkenyl and C 3-6 cycloalkyl may be optionally substituted by one or more substituents independently selected from the group consisting of fluorine, hydroxyl, cyano, R a R b N\u2014, R a R b N-carbonyl- and C 1-3 alkoxy; and wherein heterocyclyl and heterocyclylcarbonyl may be optionally substituted by one or more substituents independently selected from the group consisting of C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, C 1-6 alkoxy, halo-C 1-6 -alkyl, hydroxyl-C 1-6 -alkyl, R a R b N\u2014C 1-6 alkyl- and C 1-6 -alkoxy-C 1-6 -alkyl group; and wherein if said heterocyclyl or heterocyclylcarbonyl contains a \u2014NH moiety that nitrogen may optionally be substituted by one or more groups independently selected from the group consisting of C 1-6 alkyl, C 3-6 alkenyl, C 3-6 alkynyl, C 3-6 cycloalkyl, C 1-6 alkyl-S(O) 2 \u2014 and C 1-6 -alkylcarbonyl; or R i  and R j  taken together with the nitrogen to which they are attached form a 4-9 membered monocyclic, bridged bicyclic, fused bicyclic or spirocyclic heterocyclic ring, which may have an additional heteroatom selected from the group consisting of 0, N, and S(O) w  (wherein w is 0, 1 or 2); wherein the 4-9 membered monocyclic, bridged bicyclic, fused bicyclic or spirocyclic heterocyclic ring may be optionally substituted on carbon by one, two, or more substituents selected from the group consisting of halogen, hydroxyl, oxo, cyano, C 1-6 alkyl, C 1-6 alkoxy, R a R b N\u2014, R a R b N\u2014SO 2 \u2014 and R a R b N-carbonyl-; wherein said C 1-6 alkyl or C 1-6 alkoxy may optionally be substituted the group consisting of fluorine, hydroxyl, and cyano; and wherein if said 4-9 membered monocyclic, bridged bicyclic, fused bicyclic or spirocyclic heterocyclic ring contains a \u2014NH moiety that nitrogen may be optionally substituted by a substituent selected from the group consisting of hydrogen, C 1-6 alkyl, C 3-6 alkenyl, C 3-6 alkynyl, C 3-6 cycloalkyl, C 1-6  alkyl-S(O) 2 \u2014, C 1-6 alkylcarbonyl-, C 1-6 alkoxycarbonyl-, R i R j N-carbonyl- and R i R j N\u2014SO 2 \u2014; wherein C 1-6 alkyl, C 3-6 alkenyl, C 3-6 alkynyl, C 3-6 cycloalkyl, C 1-6 alkyl-S(O) 2 \u2014, C 1-6 alkylcarbonyl-, and C 1-6 alkoxycarbonyl- may optionally be substituted by one or more substituents selected from the group consisting of fluorine, hydroxyl, and cyano; R a  and R b  are independently selected, for each occurrence, from the group consisting of hydrogen and C 1-3 alkyl; wherein C 1-3 alkyl may optionally be substituted by one or more substituents selected from halogen, cyano, oxo and hydroxyl; R f  is independently selected, for each occurrence, from the group consisting of R P , hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 alkoxy, C 1-6 alkyl-S(O) w \u2014, (wherein wherein w is 0, 1 or 2), C 1-6 alkylcarbonyl-N(R a )\u2014 and C 1-6 alkoxycarbonyl-N(R a )\u2014; wherein C 1-6 alkyl, C 3-6 cycloalkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 alkoxy, C 1-6 alkylcarbonyl-N(R a )\u2014, C 1-6 alkoxycarbonyl-N(R a )\u2014 may be optionally substituted by one or more substituents selected from R P ; R g  is independently selected for each occurrence from the group consisting of R P , hydrogen, oxo, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, C 1-6 alkoxy, C 1-6 alkyl-S(O) w \u2014 (wherein w is 0, 1 or 2), C 1-6 alkylcarbonyl-N(R a )\u2014 and C 1-6 alkoxycarbonyl-N(R a )\u2014; wherein C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, C 1-6 alkoxy, C 1-6 alkyl-S(O) w \u2014, C 1-6 alkylcarbonyl-N(R a )\u2014, and C 1-6 alkoxycarbonyl-N(R a )\u2014 may be optionally substituted by one or more substituents selected from R P ; R h  is independently selected for each occurrence from the group consisting of hydrogen, C 1-6 alkyl, C 3-6 alkenyl, C 3-6 alkynyl, C 3-6 cycloalkyl, C 1-6 alkyl-S(O) 2 \u2014, C 1-6 alkylcarbonyl-, C 1-6 alkoxycarbonyl-, R i R j N-carbonyl- and R i R j N\u2014SO 2 \u2014; wherein C 1-6 alkyl, C 3-6 alkenyl, C 3-6 alkynyl, C 3-6 cycloalkyl, C 1-6 alkyl-S(O) 2 \u2014, C 1-6 alkylcarbonyl-, and C 1-6 alkoxycarbonyl- may optionally be substituted by one or more substituents selected from R P ; and R P  is independently selected, for each occurrence, from the group consisting of halogen, hydroxyl, cyano, C 1-6 alkoxy, R i R j N\u2014, R i R j N-carbonyl-, R i R j N\u2014SO 2 \u2014, and R i R j N-carbonyl-N(R a )\u2014; and pharmaceutically acceptable salts, stereoisomers, esters and prodrugs thereof.

Metadata:
- Claim Count in Document: 14.0
- Percentile: 88.0
- Lexical Diversity: 1.40625
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15827074', '15354834', '15796519', '14974033', '14851909']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.848571170998708
- 35 USC 102 Novelty (BERT): 0.581855656959793
- Combined Prediction Score: 0.8218996195948166
- Mean Citation Score: 464.616548
- Max Citation Score: 551.8046
- Similarity Product: 443.7484944287181

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

Dataset: test