PATENT CLAIM ANALYSIS

Application Number: 16172197
Application Type: Utility
Filing Date: 2018-10
Publication Date: 2019-05
Patent Classification: ["548", "356100"]

Abstract:
The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R 1 -R 4 , n, p, A, B, D, E, L and AR 1  are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).

Claim (Index 76):
A method for treatment of an inflammatory or immune related disorder in a subject comprising topically administering to said subject in need thereof a formulation comprising an LFA-1 antagonist and a pharmaceutically acceptable excipient, wherein the LFA-1 antagonist comprises a compound of Formula I or its pharmaceutically acceptable salt or ester, wherein wherein R 1  and R 2  are each independently hydrogen, \u2014(CH 2 ) m OH, \u2014(CH 2 ) m aryl, \u2014(CH 2 ) m heteroaryl, wherein m is 0-6, \u2014CH(R 1A )(OR 1B ), \u2014CH(R 1A )(NHR 1B ), U-T-Q, or an aliphatic, alicyclic, heteroaliphatic or heteroalicyclic moiety optionally substituted with U-T-Q, wherein U is absent, \u2014O\u2014, \u2014-S(O) 0-2 \u2014, \u2014SO 2 N(R 1A ), \u2014N(R 1A )\u2014, \u2014N(R 1A )C(\u2550O)\u2014, \u2014N(R 1A )C(\u2550O)\u2014O\u2014, \u2014N(R 1A )C(\u2550O)\u2014N(R 1B )\u2014, \u2014N(R 1A )\u2014SO 2 \u2014, \u2014C(\u2550O)\u2014, \u2014C(\u2550O)\u2014O\u2014, \u2014O\u2014C(\u2550O)\u2014, aryl, heteroaryl, alkylaryl, alkylheteroaryl, \u2014C(\u2550O)\u2014N(R 1A )\u2014, \u2014O\u2014C(\u2550O)\u2014N(R 1A )\u2014, \u2014C(\u2550N\u2014R 1E )\u2014, \u2014C(\u2550N\u2014R 1E )\u2014O\u2014, \u2014C(\u2550N\u2014R 1E )\u2014N(R 1A )\u2014, \u2014O\u2014C(\u2550N\u2014R 1E )\u2014N(R 1A )\u2014, \u2014N(R 1A )C(\u2550N\u2014R 1E )\u2014, \u2014N(R 1A )C(\u2550N\u2014R 1E )\u2014O\u2014, N(R 1A )C(\u2550N\u2014R 1E )\u2014N(R 1B )\u2014, -P(\u2550O)(OR 1A )\u2014O\u2014, or -P(\u2550O)(R 1A )\u2014O\u2014; T is absent, an aliphatic, heteroaliphatic, aryl, heteroaryl, alkylaryl or alkylheteroaryl moiety; and Q is hydrogen, halogen, cyano, isocyanate, \u2014OR 1B , \u2014SR 1B ; \u2014N(R 1B ) 2 , \u2014NHC(\u2550O)OR 1B , \u2014NHC(\u2550O)N(R 1B ) 2 , \u2014NHC(\u2550O)R 1B , \u2014NHSO 2 R 1B , \u2014NHSO 2 N(R 1B ) 2 , \u2014NHSO 2 NHC(\u2550O)OR 1B , \u2014NHC(\u2550O)NHSO 2 R 1B , \u2014C(\u2550O)NHC(\u2550O)OR 1B , \u2014C(\u2550O)NHC(\u2550O)R 1B , \u2014C(\u2550O)NHC(\u2550O)N(R 1B ) 2 , \u2014C(\u2550O)NHSO 2 R 1B , \u2014C(\u2550O)NHSO 2 N(R 1B ) 2 , \u2014C(\u2550S)N(R 1B ) 2 , \u2014SO 2 R 1B , \u2014SO 2 \u2014O\u2014R 1B , \u2014SO 2 \u2014N(R 1B ) 2 , \u2014SO 2 \u2014NHC(\u2550 0 )OR 1B , \u2014SO 2 \u2014NHC(\u2550O)\u2014N(R 1B ) 2 , \u2014SO 2 \u2014NHC(\u2550O)R 1B , \u2014O\u2014C(\u2550O)N(R 1B ) 2 , \u2014O\u2014C(\u2550O)R 1B , \u2014O\u2014C(\u2550O)NHC(\u2550O)R 1B , \u2014O\u2014C(\u2550O)NH\u2014SO 2 R 1B , \u2014O\u2014SO 2 R 1B , or an aliphatic heteroaliphatic, aryl or heteroaryl moiety, or wherein R 1  and R 2  taken together are an alicyclic or heterocyclic moiety; wherein each occurrence of R 1A  and R 1B  is independently hydrogen, an aliphatic, alicyclic, heteroaliphatic, heterocyclic, aryl, heteroaryl, alkylaryl or alkylheteroaryl moiety, \u2014COR 1C , or \u2014CONR 1C R 1D ; wherein each occurrence of R 1C  and R 1D  is independently hydrogen, hydroxyl, or an aliphatic, heteroaliphatic, aryl, heteroaryl, alkylaryl or alkylheteroaryl moiety; and R 1E  is hydrogen, an aliphatic, alicyclic, heteroaliphatic, heterocyclic, aryl, heteroaryl, alkylaryl or alkylheteroaryl moiety, \u2014CN, \u2014OR 1C , \u2014NR 1C R 1D  or \u2014SO 2 R 1C ; R 3  is \u2014C(\u2550O)OR 3A , \u2014C(\u2550O)H, \u2014CH 2 OR 3A , \u2014CH 2 O\u2014C(\u2550O)-alkyl, \u2014C(\u2550O)NH(R 3A ), \u2014CH 2 X 0 ; wherein each occurrence of R 3A  is independently hydrogen, a protecting group, an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl, heteroaryl, alkylaryl, alkylheteroaryl, heteroalkylaryl or heteroalkylheteroaryl moiety, or R 3A , taken together with R 1  or R 2 , forms a heterocyclic moiety; wherein X 0  is a halogen selected from F, Cl, Br or I; R 4 , for each occurrence, is independently hydrogen, halogen, \u2014CN, \u2014NO 2 , an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl, heteroaryl, alkylaryl or alkylheteroaryl moiety, or is -GR G1  wherein G is \u2014O\u2014, \u2014S\u2014, \u2014NR G2 \u2014, \u2014CO\u2014, \u2014SO\u2014, \u2014SO 2 \u2014, \u2014C(\u2550O)O\u2014, \u2014C(\u2550O)NR G2 \u2014, \u2014OC(\u2550O)\u2014, \u2014NR G2 C(\u2550O)\u2014 or \u2014SO 2 NR G2 \u2014, and R G1  and R G2  are independently hydrogen, an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl, heteroaryl, alkylaryl or alkylheteroaryl moiety; n is an integer from 0-4; AR 1  is a monocyclic or polycyclic aryl, heteroaryl, alkylaryl, alkylheteroaryl, alicyclic or heterocyclic moiety; A, B, D and E are connected by single bonds; wherein D is N and each occurrence of A, B, and E is independently CHR i  wherein each occurrence of R i  is independently hydrogen, halogen, \u2014CN, \u2014NO 2 , an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl, heteroaryl, alkylaryl or alkylheteroaryl moiety, or is -GR G1  wherein G is \u2014O\u2014, \u2014S\u2014, \u2014NR G2 \u2014, \u2014CO\u2014, \u2014SO\u2014, \u2014SO 2 \u2014, \u2014C(\u2550O)O\u2014, \u2014C(\u2550O)NR G2 \u2014, \u2014OC(\u2550O)\u2014, \u2014NR G2 C(\u2550O)\u2014 or \u2014SO 2 NR G2 \u2014, and R G1  and R G2  are independently hydrogen, an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl, heteroaryl, alkylaryl or alkylheteroaryl moiety, or any two adjacent occurrences of R i , taken together, represent an alicyclic, heteroalicyclic, aryl, or heteroaryl moiety; p is an integer from 0-4; and L is C\u2550O or a substituted or unsubstituted C 1-6 alkylidene or C 2-6 alkenylidene chain wherein up to two non-adjacent methylene units are independently optionally replaced by \u2014C(\u2550O)\u2014.

Metadata:
- Claim Count in Document: 41.0
- Percentile: 97.0
- Lexical Diversity: 1.43103
- Patent Class: 548.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['13969915', '14939600', '13969968', '11934049', '11978388']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7862540329144648
- 35 USC 102 Novelty (BERT): 0.6285357613257428
- Combined Prediction Score: 0.7704822057555926
- Mean Citation Score: 558.435568
- Max Citation Score: 566.11993
- Similarity Product: 562.0547303597963

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

Dataset: test