PATENT CLAIM ANALYSIS

Application Number: 15761914
Application Type: Utility
Filing Date: 2018-03
Publication Date: 2018-12
Patent Classification: ["514", "369000"]

Abstract:
The present invention provides pharmaceutical compositions and methods for treating and/or preventing a metabolic condition.

Claim (Index 3):
The pharmaceutical composition of  claim 1 , wherein the inhibitor is a compound of formula I wherein R 5  is selected from: wherein:\n each G is independently selected from C, N, O, S and Se, and wherein only one G may be O, S, or Se; \n each G\u2032 is independently selected from C and N and wherein no more than two G\u2032 groups are N; \n A is selected from \u2014H, \u2014NR 4 2 , \u2014CONR 4 2 , \u2014CO 2 R 3 , halo, \u2014S(O)R 3 , \u2014SO 2 R 3 , alkyl, alkenyl, alkynyl, perhaloalkyl, haloalkyl, aryl, \u2014CH 2 OH, \u2014CH 2 NR 4 2 , \u2014CH 2 CN, \u2014CN, \u2014C(S)NH 2 , \u2014OR 3 , \u2014SR 3 , \u2014N 3 , \u2014NHC(S)NR 4 2 , \u2014NHAc, and a bond or A is absent; \n each B and D are independently selected from \u2014H, alkyl, alkenyl, alkynyl, aryl, alicyclic, aralkyl, alkoxyalkyl, \u2014C(O)R 11 , \u2014C(O)SR 3 , \u2014SO 2 R 11 , \u2014S(O)R 3 , \u2014CN, \u2014NR 9 2 , \u2014OR 3 , \u2014SR 3 , perhaloalkyl, halo, \u2014NO 2 , and a bond, all except \u2014H, \u2014CN, perhaloalkyl, \u2014NO 2 , and halo are optionally substituted or each B and D are independently absent; \n E is absent or is selected from \u2014H, alkyl, alkenyl, alkynyl, aryl, alicyclic, alkoxyalkyl, \u2014C(O)OR 3 , \u2014CONR 4 2 , \u2014CN, \u2014NR 9 2 , \u2014NO 2 , \u2014OR 3 , \u2014SR 3 , perhaloalkyl, halo, and a bond, all except \u2014H, \u2014CN, perhaloalkyl, and halo are optionally substituted; \n J is absent or is selected from \u2014H and a bond; \n X is an optionally substituted linking group that links R 5  to the phosphorus atom via 2-4 atoms, including 0-1 heteroatoms selected from N, O, and S, except that if X is urea or carbamate there is 2 heteroatoms, measured by the shortest path between R 5  and the phosphorus atom, and wherein the atom attached to the phosphorus is a carbon atom, and wherein there is no N in the linking group unless it is connected directly to a carbonyl or in the ring of a heterocycle; and wherein X is not a 2 carbon atom -alkyl- or -alkenyl- group; with the proviso that X is not substituted with \u2014COOR 2 , \u2014SO 3 R 1 , or \u2014PO 3 R 1 2 ; \n Y is independently selected from \u2014O\u2014, and \u2014NR 6 \u2014; \n when Y is \u2014O\u2014, then R 1  attached to \u2014O\u2014 is independently selected from \u2014H, alkyl, optionally substituted aryl, optionally substituted alicyclic where the cyclic moiety contains a carbonate or thiocarbonate, optionally substituted -alkylaryl, \u2014C(R 2 ) 2 OC(O)NR 2 2 , \u2014NR 2 \u2014C(O)\u2014R 3 , \u2014C(R 2 ) 2 \u2014OC(O)R 3 , \u2014C(R 2 ) 2 \u2014O\u2014C(O)OR 3 , \u2014C(R 2 ) 2 OC(O)SR 3 , -alkyl-S\u2014C(O)R 3 , -alkyl-S\u2014S-alkylhydroxy, and -alkyl-S\u2014S\u2014S-alkylhydroxy, \n when Y is \u2014NR 6 \u2014, then R 1  attached to \u2014NR 6 \u2014 is independently selected from \u2014H, \u2014[C(R 2 ) 2 ] q \u2014COOR 3 , \u2014C(R 4 ) 2 COOR 3 , \u2014[C(R 2 ) 2 ] q \u2014C(O)SR, and -cycloalkylene-COOR 3 ; \n or when either Y is independently selected from \u2014O\u2014 and \u2014NR 6 \u2014, then together R 1  and R 1  are -alkyl-S\u2014S-alkyl- to form a cyclic group, or together R 1  and R 1  are \n wherein\n V, W, and W\u2032 are independently selected from \u2014H, alkyl, aralkyl, alicyclic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, 1-alkenyl, and 1-alkynyl; or \n together V and Z are connected via an additional 3-5 atoms to form a cyclic group containing 5-7 atoms, optionally 1 heteroatom, substituted with hydroxy, acyloxy, alkoxycarbonyloxy, or aryloxycarbonyloxy attached to a carbon atom that is three atoms from both Y groups attached to the phosphorus; or \n together V and Z are connected via an additional 3-5 atoms to form a cyclic group, optionally containing 1 heteroatom, that is fused to an aryl group at the beta and gamma position to the Y attached to the phosphorus; \n together V and W are connected via an additional 3 carbon atoms to form an optionally substituted cyclic group containing 6 carbon atoms and substituted with one substituent selected from hydroxy, acyloxy, alkoxycarbonyloxy, alkylthiocarbonyloxy, and aryloxycarbonyloxy, attached to one of said carbon atoms that is three atoms from a Y attached to the phosphorus; \n together Z and W are connected via an additional 3-5 atoms to form a cyclic group, optionally containing one heteroatom, and V must be aryl, substituted aryl, heteroaryl, or substituted heteroaryl; \n together W and W\u2032 are connected via an additional 2-5 atoms to form a cyclic group, optionally containing 0-2 heteroatoms, and V must be aryl, substituted aryl, heteroaryl, or substituted heteroaryl; \n Z is selected from \u2014CHR 2 OH, \u2014CHR 2 OC(O)R 3 , \u2014CHR 2 OC(S)R 3 , \u2014CHR 2 OC(S)OR 3 , \u2014CHR 2 OC(O)SR 3 , \u2014CHR 2 OCO 2 R 3 , \u2014OR 2 , \u2014SR 2 , \u2014CHR 2 N 3 , \u2014CH 2 aryl, \u2014CH(aryl)OH, \u2014CH(CH\u2550CR 2 2 )OH, \u2014CH(C\u2261CR 2 )OH, \u2014R 2 , \u2014NR 2 2 , \u2014OCOR 3 , \u2014OCO 2 R 3 , \u2014SCOR 3 , \u2014SCO 2 R 3 , \u2014NHCOR 2 , \u2014NHCO 2 R 3 , \u2014CH 2 NHaryl, \u2014(CH 2 ) p \u2014OR 2 , and \u2014(CH 2 ) p \u2014SR 2 ; \n p is an integer 2 or 3; \n q is an integer 1 or 2; \n with the provisos that: \n a) V, Z, W, W\u2032 are not all \u2014H; and \n b) when Z is \u2014R 2 , then at least one of V, W, and W\u2032 is not \u2014H, alkyl, aralkyl, or alicyclic; \n R 2  is selected from R 3  and \u2014H; \n R 3  is selected from alkyl, aryl, alicyclic, and aralkyl; \n each R 4  is independently selected from \u2014H, and alkyl, or together R 4  and R 4  form a cyclic alkyl group; \n R 6  is selected from \u2014H, lower alkyl, acyloxyalkyl, alkoxycarbonyloxyalkyl, and lower acyl; \n each R 9  is independently selected from \u2014H, alkyl, aralkyl, and alicyclic, or together R 9  and R 9  form a cyclic alkyl group; \n R 11  is selected from alkyl, aryl, \u2014NR 2 2 , and \u2014OR 2 ; and \n with the provisos that: \n 1) when G\u2032 is N, then the respective A, B, D, or E is absent; \n 2) at least one of A and B, or A, B, D, and E is not \u2014H or is not absent; \n 3) when R 5  is a six-membered ring, then X is not any 2 atom linker, an optionally substituted -alkyl-, an optionally substituted -alkenyl-, an optionally substituted -alkyloxy-, or an optionally substituted -alkylthio-; \n 4) when G is N, then the respective A or B is not halogen or a group directly bonded to G via a heteroatom; \n 5) R 1  is not unsubstituted C1-C10 alkyl; \n 6) when X is not an -aryl- group, then R 5  is not substituted with two or more aryl groups; \n and pharmaceutically acceptable prodrugs and salts thereof.

Metadata:
- Claim Count in Document: 29.0
- Percentile: 90.0
- Lexical Diversity: 1.0
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['09900364', '10615563', '11043859', '09747182', '09801933']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7960868204376857
- 35 USC 102 Novelty (BERT): 0.5072876485863655
- Combined Prediction Score: 0.7672069032525537
- Mean Citation Score: 283.510686
- Max Citation Score: 290.39886
- Similarity Product: 232.85797632260085

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

Dataset: test