PATENT CLAIM ANALYSIS

Application Number: 16163259
Application Type: Utility
Filing Date: 2018-10
Publication Date: 2019-03
Patent Classification: ["552", "513000"]

Abstract:
The invention relates to compounds of formula (I), wherein R 1 , R 2 , Y, R 4  and R 5b  are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids.

Claim (Index 11):
A process for the preparation of a compound of general formula (XXI): wherein: R 1  is C 1-4  alkyl optionally substituted with one or more substituents selected from halo, OR 6  and NR 6 R 7 ;\n where each of R 6  and R 7  is independently selected from H and C 1-4  alkyl; \n Y 1  is a bond or an alkylene linker group having from 1 to 20 carbon atoms and optionally substituted with one or more R 3  groups; each R 3  is independently halo, OR 8  or NR 8 R 9 ;\n where each of R 8  and R 9  is independently selected from H and C 1-14  alkyl; \n and R 4  is C(O)OR 10 , OC(O)R 10 , C(O)NR 10 R 11 , OR 10 , OSi(R 13 ) 3 , S(O)R 10 , SO 2 R 10 , OSO 2 R 10 , SO 3 R 10 , or OSO 3 R 10\u2212 ;\n where each R 10  and R 11  is independently: \n a. hydrogen or \n b. C 1-20  alkyl, C 2-20  alkenyl, C 2-20  alkynyl, \u2014O\u2014C 1-20  alkyl, \u2014O\u2014C 2-20  alkenyl or \u2014O\u2014C 2-20  alkynyl, any of which is optionally substituted with one or more substituents selected from halo, NO 2 , CN, OR 19 , SR 19 , SO 2 R 19 , SO 3 R 19 , N(R 19 ) 2 , and a 6- to 14-membered aryl or 5 to 14-membered heteroaryl group, either of which is optionally substituted with C 1-6  alkyl, C 1-6  haloalkyl, halo, NO 2 , CN, OR 19 , SR 19 , SO 2 R 19 , SO 3 R 19  or N(R 19 )2; or \n c. a 6- to 14-membered aryl or 5 to 14-membered heteroaryl group optionally substituted with one or more substituents selected from C 1-6  alkyl, C 1-6  haloalkyl, halo, NO 2 , CN, OR 19 , SR 19 , SO 2 R 19 , SO 3 R 19  and N(R 19 ) 2 ; \n d. a polyethylene glycol residue;\n each R 19  is independently selected from H, C 1-6  alkyl, C 1-6  haloalkyl, and a 6- to 14-membered aryl or 5 to 14-membered heteroaryl group optionally substituted with halo, C 1-6  alkyl or C 1-6  haloalkyl; \n \n each R 13  is independently \n a. C 1-20  alkyl, C 2-20  alkenyl or C 2-20  alkynyl optionally substituted with one or more substituents selected from halo, NO 2 , CN, OR 19 , SR 19 , SO 2 R 19 , SO 3 R 19 , N(R 19 ) 2 , a 6- to 14-membered aryl or 5 to 14-membered heteroaryl group, either of which is optionally substituted with C 1-6  alkyl, C 1-6  haloalkyl, halo, NO 2 , CN, OR 19 , SO 2 R 19 , SO 3 R 19  or N(R 19 ) 2 ; or \n b. a 6- to 14-membered aryl or 5 to 14-membered heteroaryl group optionally substituted with one or more substituents selected from C 1-6  alkyl, C 1-6  haloalkyl, halo, NO 2 , CN, OR 19 , SR 19 , SO 2 R 19 , SO 3 R 19  and N(R 19 ) 2 ;\n each R 19  is independently selected from H, C 1-6  alkyl and C 1-6  haloalkyl; \n \n R 2  is H, halo or OH; and R 5a  is H or OH; the process comprising: i. reduction of a compound of general formula (I): wherein: R 1  is C 1-4  alkyl optionally substituted with one or more substituents selected from halo, OR 6  and NR 6 R 7 ;\n where each of R 6  and R 7  is independently selected from H or C 1-4  alkyl; \n R 2  is H, halo or OH or a protected OH, which is stable under basic conditions; Y 1  is a bond or an alkylene linker group having from 1 to 20 carbon atoms and optionally substituted with one or more R 3  groups; each R 3  is independently halo, OR 8  or NR 8 R 9 ;\n where each of R 8  and R 9  is independently selected from H and C 1-4  alkyl; \n and R 4  is C(O)OR 10 , OC(O)R 10 , C(O)NR 10 R 11 , OR 10 , OSi(R 13 ) 3 , S(O)R 10 , SO 2 R 10 , OSO 2 R 10 , SO 3 R 10 , or OSO 3 R 10\u2212 ;\n where each R 10  and R 11  is independently: \n a. hydrogen or \n b. C 1-20  alkyl, C 2-20  alkenyl, C 2-20  alkynyl, \u2014O\u2014C 1-20  alkyl, \u2014O\u2014C 2-20  alkenyl or \u2014O\u2014C 2-20  alkynyl, any of which is optionally substituted with one or more substituents selected from halo, NO 2 , CN, OR 19 , SR 19 , SO 2 R 19 , SO 3 R 19 , N(R 19 ) 2 , and a 6- to 14-membered aryl or 5 to 14-membered heteroaryl group, either of which is optionally substituted with C 1-6  alkyl, C 1-6  haloalkyl, halo, NO 2 , CN, OR 19 , SR 19 , SO 2 R 19 , SO 3 R 19  or N(R 19 ) 2 ; or \n c. a 6- to 14-membered aryl or 5 to 14-membered heteroaryl group optionally substituted with one or more substituents selected from C 1-6  alkyl, C 1-6  haloalkyl, halo, NO 2 , CN, OR 19 , SR 19 , SO 2 R 19 , SO 3 R 19  and N(R 19 ) 2 ; \n d. a polyethylene glycol residue;\n each R 19  is independently selected from H, C 1-6  alkyl, C 1-6  haloalkyl, and a 6- to 14-membered aryl or 5 to 14-membered heteroaryl group optionally substituted with halo, C 1-6  alkyl or C 1-6  haloalkyl; \n \n each R 13  is independently \n a. C 1-20  alkyl, C 2-20  alkenyl or C 2-20  alkynyl optionally substituted with one or more substituents selected from halo, NO 2 , CN, OR 19 , SR 19 , SO 2 R 19 , SO 3 R 19 , N(R 19 ) 2 , a 6- to 14-membered aryl or 5 to 14-membered heteroaryl group, either of which is optionally substituted with C 1-6  alkyl, C 1-6  haloalkyl, halo, NO 2 , CN, OR 19 , SO 2 R 19 , SO 3 R 19  or N(R 19 ) 2 ; or \n b. a 6- to 14-membered aryl or 5 to 14-membered heteroaryl group optionally substituted with one or more substituents selected from C 1-6  alkyl, C 1-6  haloalkyl, halo, NO 2 , CN, OR 19 , SR 19 , SO 2 R 19 , SO 3 R 19  and N(R 19 ) 2 ;\n each R 19  is independently selected from H, C 1-6  alkyl and C 1-6  haloalkyl; \n \n R 5b  is H or OH or a protected OH; or a salt or an isotopic variant thereof using a reducing agent and, where R 2  and/or R 5b  is a protected OH, removal of the protecting group(s), to give the compound of general formula (XXI), wherein removal of the protecting group can take place before or after the reduction; and optionally ii. conversion of a compound of general formula (XXI) to another compound of general formula (XXI).

Metadata:
- Claim Count in Document: 8.0
- Percentile: 97.0
- Lexical Diversity: 1.35484
- Patent Class: 552.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15528331', '15528214', '15528220', '14127159', '14132567']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7066907028473114
- 35 USC 102 Novelty (BERT): 0.6727392281107085
- Combined Prediction Score: 0.7032955553736511
- Mean Citation Score: 426.947016
- Max Citation Score: 518.72705
- Similarity Product: 509.47495470784594

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

Dataset: test