PATENT CLAIM ANALYSIS

Application Number: 15750471
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-08
Patent Classification: ["514", "043000"]

Abstract:
The present invention relates to mannose derivatives of formula (I): wherein R 1  represents H, CO—(C 1 -C 6 )-alkyl or CO-alkylaryl, Y represents a single bond, CH 2 , O, NR 3 , S, A represents O, NH or S, X represents H and X′ represents OH or X and X′ taken together with the carbon atom bearing them form a CO group, R 2  represents H, a linear or branched (C 1 -C 6 )-alkyl or CF 3 , R 3  represents H, a C 1 -C 6  alkyl, a CO—(C 1 -C 6 )-alkyl, CF 3  or COCF 3 , and R is as described in claim  1.    The mannose derivatives of formulae (I) are useful for treating pathologies associated with the presence of adherent  Escherichia coli  (AEC), in particular inflammatory bowel diseases (IBD), such as Crohn's disease and ulcerative colitis; a urinary tract infection, in particular painful bladder syndrome and cystitis, more particularly interstitial cystitis; irritable bowel syndrome; metabolic diseases such as metabolic obesity, diabetes, hypercholesterolemia; autoimmune inflammatory diseases; and colorectal cancer, in particular colon cancer.

Claim (Index 1):
A compound of formula (I): wherein\n R 1  represents H, CO\u2014(C 1 -C 6 )-alkyl or CO-alkylaryl, preferably H, COMe or COCH 2 Ph, \n Y represents a single bond, CH 2 , O, NR 3 , S, preferably a single bond, CH 2 , NR 3 , S, \n A represents O, NH or S, preferably O or S, \n X represents H and X\u2032 represents OH or X and X\u2032 taken together with the carbon atom bearing them form a CO group, \n R 2  represents H, a linear or branched (C 1 -C 6 )-alkyl or CF 3 , \n R 3  represents H, a C 1 -C 6  alkyl, a CO\u2014(C 1 -C 6 )-alkyl, CF 3  or COCF 3 , preferably H, CH 3 , COCH 3 , CF 3  or OCF 3 , and \n R represents: a (C 1 -C 6 )-alkyl, a (C 2 -C 6 )-alkenyl, a (C 2 -C 6 )-alkynyl, a (C 3 -C 10 )-cycloalkyl, a (C 5 -C 10 )-cycloalkenyl, a heterocycloalkyl, a heterocycloalkenyl, an arylan alkyl aryl, CF 3 , adamantyl, OR a , or NR b R c , \n wherein R a  represents H, a (C 1 -C 6 )-alkyl, a (C 2 -C 6 )-alkenyl, a (C 2 -C 6 )-alkynyl, a (C 3 -C 6 )-cycloalkyl, a (C 3 -C 6 )-cycloalkenyl, a heterocycloalkyl, a heterocycloalkenyl, an aryl, a alkylaryl, a CHO, a CO\u2014(C 1 -C 6 )-alkyl, or CO-aryl, a CO 2 H, a CO 2 \u2014(C 1 -C 6 )-alkyl, or a CONH\u2014(C 1 -C 6 )-alkyl, \n and wherein R b  and R c  represent independently from each other any of the groups defined for R a , R b  representing in particular H, \n said (C 1 -C 6 )-alkyl, (C 2 -C 6 )-alkenyl, (C 2 -C 6 )-alkynyl, (C 3 -C 10 )-cycloalkyl, (C 5 -C 10 )-cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, CO\u2014(C 1 -C 6 )-alkyl, CO 2 \u2014(C 1 -C 6 )-alkyl, CONH\u2014(C 1 -C 6 )-alkyl, aryl, alkylaryl, CO-aryl and CO-alkylaryl being optionally substituted by one or more, preferably 1 to 4, more preferably 1 or 2 substituent(s) R\u2032, each independently selected from:\n a (C 1 -C 6 )-alkyl optionally substituted by one or more, preferably one to three substituents selected from a halogen, NH 2 , OH, CF 3 , a C 1 -C 6  alkyl preferably substituted by a carbohydrate, CH 2 SO 3 T, CH 2 COOT or N(R g ) 3 T\u2032, wherein R g  represents independently H, a (C 1 -C 6 )-alkyl (preferably H or CH 3 ), T represents a monovalent cation such as a mineral monovalent cation, in particular an alkaline cation preferably selected from Li + , Na + , K + , and even more preferable Na + , and wherein T\u2032 is a monovalent anion, such as a halogenide, in particular chloride, bromide or iodide, preferably chloride, \n a (C 2 -C 6 )-alkenyl, \n a (C 2 -C 6 )-alkynyl, \n a (C 3 -C 10 )-cycloalkyl, \n a (C 5 -C 10 )-cycloalkenyl, \n a heterocycloalkyl, \n a heterocycloalkenyl, \n an aryl, optionally substituted by one or more, preferably one to three substituents selected from a halogen, NH 2 , OH, CF 3 , a C 1 -C 6  alkyl preferably substituted by a carbohydrate, CH 2 SO 3 T, CH 2 COOT or N(R g ) 3 T\u2032, wherein R g , T and T\u2032 are as defined above, \n an alkyl aryl optionally substituted by one or more, preferably one to three substituents selected from a halogen, NH 2 , OH, CF 3 , a C 1 -C 6  alkyl preferably substituted by a carbohydrate, CH 2 SO 3 T, CH 2 COOT or N(R g ) 3 T\u2032, wherein R 9 , T and T\u2032 are as defined above, \n a NH-alkyl aryl optionally substituted by one or more, preferably one to three substituents selected from a halogen, NH 2 , OH, CF 3 , a C 1 -C 6  alkyl preferably substituted by a carbohydrate, CH 2 SO 3 T, CH 2 COOT or N(R g ) 3 T\u2032, wherein R g , T and T\u2032 are as defined above, \n a CHO, \n a CO\u2014(C 1 -C 6 )-alkyl optionally substituted by a halogen such as fluorine or a carbohydrate, \n a CO-aryl optionally substituted by one or more, preferably one to three substituents selected from a halogen, NH 2 , OH, CF 3 , a C 1 -C 6  alkyl preferably substituted by a carbohydrate, CH 2 SO 3 T, CH 2 COOT or N(R g ) 3 T\u2032, wherein R g , T and T\u2032 are as defined above, \n a CO 2 H, \n a CO 2 \u2014(C 1 -C 6 )-alkyl, \n a CONH\u2014(C 1 -C 6 )-alkyl, \n a CONH-aryl or NHCO-aryl optionally substituted by one or more, preferably one to three substituents selected from a halogen, NH 2 , OH, CF 3 , a C 1 -C 6  alkyl preferably substituted by a carbohydrate, CH 2 SO 3 T, CH 2 COOT or N(R g ) 3 T\u2032, wherein R g , T and T\u2032 are as defined above, \n a halogen, \n CF 3 , \n OR d , wherein R d  represents: H, a (C 1 -C 6 )-alkyl, a (C 3 -C 10 )-cycloalkyl, CO\u2014(C 1 -C 6 )-alkyl, or CO-aryl optionally substituted by one or more, preferably one to three substituents selected from a halogen, CF 3 , a C 1 -C 6  alkyl preferably substituted by a carbohydrate, \n NR e R f , wherein R e  and R f  represent independently from each other: H, a (C 1 -C 6 )-alkyl, a (C 3 -C 10 )-cycloalkyl, CO\u2014(C 1 -C 6 )-alkyl, or CO-aryl optionally substituted by one or more, preferably one to three substituents selected from a halogen, CF 3 , a C 1 -C 6  alkyl preferably substituted by a carbohydrate, \n NHR b , wherein R b  is as defined above, \n NO 2 , \n CN, and \n CH 2 SO 3 T, CH 2 COOT or N(R g ) 3 T\u2032, wherein R g , T and T\u2032 are as defined above, \n or a pharmaceutically acceptable salt or solvate thereof.

Metadata:
- Claim Count in Document: 2.0
- Percentile: 88.0
- Lexical Diversity: 2.09346
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['14416529', '15113986', '13437491', '12594495', '13180144']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.772225179232548
- 35 USC 102 Novelty (BERT): 0.5474359901935765
- Combined Prediction Score: 0.7497462603286509
- Mean Citation Score: 334.753958
- Max Citation Score: 387.36984
- Similarity Product: 280.48346214385987

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