PATENT CLAIM ANALYSIS

Application Number: 15775487
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-11
Patent Classification: ["514", "370000"]

Abstract:
The present invention relates to biaryl monobactam compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, Z, A 1 , Q, M, W, R X  and R z  are as defined herein. The present invention also relates to compositions which comprise a biaryl monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic.

Claim (Index 1):
A compound of Formula I or a pharmaceutically acceptable salt thereof, wherein: W is a bond or O; R X  and R Z  are independently hydrogen, \u2014SC 1 -C 3 alkyl, C 1 -C 3  alkyl, \u2014(C 1 -C 3 alkylene) n OC 1 -C 3 alkyl, or \u2014(C 1 -C 3 alkylene) n NC 1 -C 3 alkyl, wherein the \u2014SC 1 -C 3 alkyl, the C 1 -C 3  alkyl, the \u2014(C 1 -C 3 alkylene) n OC 1 -C 3 alkyl and the \u2014(C 1 -C 3 alkylene) n NC 1 -C 3 alkyl are optionally substituted with one to seven fluorines; or, alternatively, R X  and R Z , together with the carbon to which they are attached, form a monocyclic C 4 -C 7  cycloalkyl or a monocyclic C 4 -C 7  heterocycloalkyl with 1, 2, or 3 heteroatom ring atoms independently selected from N, O and S, wherein said C 4 -C 7  cycloalkyl and said C 4 -C 7  heterocycloalkyl are optionally substituted with one to three substituents independently selected from \u2014F, \u2014OH and \u2014OC 1 -C 3 alkyl; X is N or CR 1 ; R 1  is hydrogen, C 1 -C 3  alkyl, or halogen; wherein said C 1 -C 3  alkyl is optionally substituted with one to three R a ; each occurrence of R a  is independently hydrogen, halogen, C 1 -C 3 alkyl, \u2014NR c R d  or \u2014OR e ; Z is C 1 -C 3  alkylene, optionally substituted with one to three R b ; each occurrence of R b  is independently \u2014C 1 -C 8  alkyl, \u2014C 3 -C 7  cycloalkyl, \u2014C(O)OR e , \u2014C(O)NR c R d , tetrazolyl, oxadiazolonyl, HetA, AryA, \u2014S(O) m R e , \u2014S(O) m NR c R d , or \u2014P(O)(R e ) p  wherein said \u2014C 1 -C 5  alkyl and said \u2014C 3 -C 7  cycloalkyl are optionally substituted with one to three R a ; HetA is a 4- to 6-membered saturated or monounsaturated monocyclic ring with 1, 2, or 3 heteroatom ring atoms independently selected from N, N as a quaternary salt, O and S, optionally substituted with one to four R 4 ; AryA is a 5- to 6-membered monocyclic aromatic ring with 0, 1, 2, or 3 ring atoms independently selected from N, N as a quaternary salt, O and S, optionally substituted with one to four R 4 ; Y is a bond, O, NR 2 , S, or CH 2 ; R 2  is hydrogen, \u2014C 1 -C 3  alkyl, \u2014C(O)R e , \u2014C(O)NR c R d , \u2014S(O) m R e , or \u2014S(O) m NR c R d , wherein said \u2014C 1 -C 3  alkyl is optionally substituted with one to three R a ; A 1  is AryA; A 2  is \u2014(CH 2 ) n N(R 3 ) 2 \u2014, C 3 -C 7  cycloalkyl, AryC or HetC, wherein said C 3 -C 7  cycloalkyl is optionally substituted with one to four R 4 ; AryC is a 5- to 6-membered monocyclic aromatic ring with 0, 1, 2, or 3 ring atoms independently selected from N, N as a quaternary salt, O and S, optionally substituted with one to four R 4 ; HetC is a 4- to 7-membered saturated or monounsaturated monocyclic ring with 1, 2, or 3 heteroatom ring atoms independently selected from N, N as a quaternary salt, O and S, optionally substituted with one to four R 4 ; each occurrence of R 4  is independently: \u2014C 1 -C 8  alkyl, \u2014C 2 -C 8  alkenyl, \u2014C 2 -C 8  alkynyl, halogen, \u2014OR e , \u2014S(O) m R e , \u2014S(O) m NR c R d , \u2014C(O)R e , \u2014OC(O)R e , \u2014C(O)OR e , \u2014CN, \u2014C(O)NR c R d , \u2014NR c R d , \u2014(CH 2 ) n NR c R d ; \u2014NR c C(O)R e , \u2014NR c C(O)OR e , \u2014NR c C(O)NR c R d , \u2014NR c S(O) m R e , \u2550NH, \u2014CF 3 , \u2014OCF 3 , \u2014OCHF 2 , \u2014C 3 -C 6  cycloalkyl, \u2014O\u2014C 3 -C 6 cycloalkyl, \u2014C 1 -C 10 alkylene-C 3 -C 6 cycloalkyl, \u2014O\u2014C 1 -C 10  alkylene-C 3 -C 6 cycloalkyl, HetB, \u2014O-HetB, \u2014C 1 -C 10 alkylene-HetB, \u2014O\u2014C 1 -C 10  alkylene-HetB, AryA, \u2014O-AryA, \u2014C 1 -C 10  alkylene-AryA, or \u2014O\u2014C 1 -C 10 alkylene-AryA, wherein each R 4  is unsubstituted or substituted with one to four substituents selected from halogen, \u2014C 1 -C 6  alkyl and \u2014(CH 2 ) n NR c R d , or wherein R 4  and M, together with the atoms to which they are attached, form a 4- to 7-membered cycloheteroalkyl optionally containing one to two additional heteroatoms independently selected from O, S and \u2014NR g ; HetB is a 3- to 6-membered saturated or monounsaturated monocyclic ring with 1, 2, or 3 heteroatom ring atoms independently selected from N, N as a quaternary salt, O and S, optionally substituted with one to three R a ; Q is a bond, CH 2 , O, S, \u2014(CH 2 ) n NR 3 \u2014, or \u2014NR 3 (CH 2 ) n \u2014, wherein each CH 2  is unsubstituted or substituted with one to two substituents selected from halogen, \u2014C 1 -C 6  alkyl, OR e  and \u2014(CH 2 ) n NR c R d ; R 3  is hydrogen or \u2014C 1 -C 3  alkyl, wherein said \u2014C 1 -C 3  alkyl is optionally substituted with one to three R a ; M is R 5 , \u2014NHR 5 , \u2014N(R 5 )2, \u2014OR 5 , \u2014(CH 2 ) n R 5 , \u2014C(O)R 5 , \u2014C(NH)R 5 , or \u2014S(O) m R 5 ; R 5  is H, C 2 -C 10  alkyl, C 3 -C 7  cycloalkyl, C 1 -C 6  alkyl-C 3 -C 7  cycloalkyl, HetB, AryB, or \u2014NH(C 1 -C 6  alkyl), wherein said C 1 -C 6  alkyl, said C 2 -C 10  alkyl and said C 3 -C 7  cycloalkyl are optionally substituted with one to four R 6 ; AryB is a 5- to 6-membered monocyclic aromatic ring with 0, 1, 2, or 3 ring atoms independently selected from N, O and S, optionally substituted with one to four R 4 ; each occurrence of R 6  is independently selected from the group consisting of: halogen, \u2014OR e , \u2014S(O) m R e , \u2014S(O) m NR c R d , \u2014C(O)R e , \u2014OC(O)R e , \u2014C(O)OR e , \u2014CN, \u2014C(O)NR c R d , \u2014C(NH)NR c R d , \u2014NR c R d , \u2014(CH 2 ) n NR c R d , \u2014N(R c )(C(O)R e ), \u2014N(R c )(C(O)OR e ), \u2014N(R c )(C(O)NR c R d ), \u2014N(R c )(S(O) m R e ), and HetB; each occurrence of R c  and R d  is independently: hydrogen, \u2014C 1 -C 10  alkyl, \u2014C 2 -C 10  alkenyl, \u2014C 3 -C 6  cycloalkyl, \u2014C 1 -C 10  alkylene-C 3 -C 6  cycloalkyl, HetA, \u2014C 1 -C 10 alkylene-HetB, AryB, \u2014C 1 -C 10  alkylene-AryB, and \u2014C 1 -C 10  alkylene-HetB, or, alternatively, R c  and R d  together with the nitrogen atom to which they are attached, form a 4- to 7-membered cycloheteroalkyl optionally containing one to two additional heteroatoms independently selected from O, S and \u2014NR g , and wherein each R c  and R d  is optionally substituted with one to three R f ; each occurrence of R e  is independently: hydrogen, \u2014C 1 -C 10 alkyl, \u2014C 2 -C 10  alkenyl, \u2014OH, \u2014OC 1 -C 4  alkyl, \u2014C 3 -C 6  cycloalkyl, \u2014C 1 -C 10  alkylene-C 3 -C 6  cycloalkyl, HetB, \u2014C 1 -C 10  alkylene-HetB, AryB, \u2014C 1 -C 10  alkylene-AryB, or \u2014C 1 -C 10  alkylene-HetB; wherein each R e  is optionally substituted with one to three R h ; each occurrence of R f  is independently: halogen, \u2014C 1 -C 10  alkyl, \u2014OH, \u2014OC 1 -C 4  alkyl, \u2014S(O) m C 1 -C 4  alkyl, \u2014CN, \u2014CF 3 , \u2014OCHF 2 , \u2014OCF 3 , or NH 2 , wherein said \u2014C 1 -C 10  alkyl is optionally substituted with one to three substituents independently selected from: \u2014OH, halogen, cyano, and \u2014S(O) 2 CH 3 ; each occurrence of R g  is independently: hydrogen, \u2014C(O)R e , and \u2014C 1 -C 10  alkyl, wherein said \u2014C 1 -C 10 alkyl is optionally substituted with one to five fluorines; each occurrence of R h  is independently: halogen, \u2014C 1 -C 10 alkyl, \u2014OH, \u2014OC 1 -C 4  alkyl, \u2014S(O) m C 1 -C 4  alkyl, \u2014CN, \u2014CF 3 , \u2014OCHF 2 , or \u2014OCF 3 ; wherein said \u2014C 1 -C 10  alkyl is optionally substituted with one to three substituents independently selected from: \u2014OH, halogen, cyano, or \u2014S(O) 2 CH 3 ; each n is independently 0, 1, 2, 3 or 4; each m is independently 0, 1 or 2, and each p is independently 1 or 2.

Metadata:
- Claim Count in Document: 10.0
- Percentile: 93.0
- Lexical Diversity: 1.8125
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['16076781', '15110431', '15517570', '15910571', '15309533']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8470240756472874
- 35 USC 102 Novelty (BERT): 0.588193529706164
- Combined Prediction Score: 0.8211410210531751
- Mean Citation Score: 436.3704159999999
- Max Citation Score: 490.50583
- Similarity Product: 477.46559472870047

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