PATENT CLAIM ANALYSIS

Application Number: 16030729
Application Type: Utility
Filing Date: 2018-07
Publication Date: 2019-02
Patent Classification: ["514", "330000"]

Abstract:
Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activtation of C5a receptors.

Claim (Index 29):
A method of inhibiting C5a receptor-mediated cellular chemotaxis comprising contacting mammalian white blood cells with a C5a receptor modulatory amount of a compound having formula and pharmaceutically acceptable salts, hydrates and rotomers thereof; wherein\n C 1  is selected from the group consisting of aryl and heteroaryl, wherein the heteroaryl group has from 1-3 heteroatoms as ring members selected from N, O and S; and wherein said aryl and heteroaryl groups are optionally substituted with from 1 to 3 R 1  substituents; \n C 2  is selected from the group consisting of aryl and heteroaryl, wherein the heteroaryl group has from 1-3 heteroatoms as ring members selected from N, O and S; and wherein said aryl and heteroaryl groups are optionally substituted with from 1 to 3 R 2  substituents; \n C 3  is selected from the group consisting of C 1-8  alkyl, C 3-8  cycloalkyl, C 3-8  cycloalkyl-C 1-4  alkyl, aryl, aryl-C 1-4  alkyl, heteroaryl, heteroaryl-C 1-4  alkyl, heterocycloalkyl or heterocycloalkyl-C 1-4  alkyl, wherein the heterocycloalkyl group or portion has from 1-3 heteroatoms selected from N, O and S, and wherein the heteroaryl group has from 1-3 heteroatoms as ring members selected from N, O and S, and each C 3  is optionally substituted with from 1-3 R 3  substituents; \n each R 1  is independently selected from the group consisting of halogen, \u2014CN, \u2014CO 2 R a , 'CO 2 R a R b , \u2014C(O)R a , \u2014OC(O)NR a R b , \u2014NR b C(O)R a , \u2014NR b C(O) 2 R c , \u2014NR a \u2014C(O)NR a R b , \u2014NR a C(O)NR a R b , \u2014NR a R b , \u2014OR a , and \u2014S(O) 2 NR a R b ; wherein each R a  and R b  is independently selected from hydrogen, C 1-8  alkyl, and C 1-8  haloalkyl, or when attached to the same nitrogen atom can be combined with the nitrogen atom to form a five or six-membered ring having from 0 to 2 additional heteroatoms as ring members selected from N, O or S; each R c  is independently selected from the group consisting of C 1-8  alkyl, C 1-8  haloalkyl, C 3-6  cycloalkyl, heterocycloalkyl, aryl and heteroaryl, and wherein the aliphatic and cyclic portions of R a , R b  and R c  are optionally further substituted with from one to three halogen, hydroxy, methyl, amino, alkylamino and dialkylamino groups; and optionally when two R 1  substituents are on adjacent atoms, are combined to form a fused five or six-membered carbocyclic ring; \n each R 2  is independently selected from the group consisting of halogen, \u2014CN, \u2014R f , \u2014CO 2 R d , \u2014CONR d R e , \u2014C(O)R d , \u2014OC(O)NR d R e , \u2014NR e C(O)R d , \u2014NR e C(O) 2 R e , \u2014NR d C(O)NR d R e , \u2014NR d C(O)NR d R e , \u2014NR d R e , \u2014OR d , and \u2014S(O) 2 NR d R e ; wherein each R d  and R e  is independently selected from hydrogen, C 1-8  alkyl, and C 1-8  haloalkyl, or when attached to the same nitrogen atom can be combined with the nitrogen atom to form a five or six-membered ring having from 0 to 2 additional heteroatoms as ring members selected from N, O or S; each R f  is independently selected from the group consisting of C 1-8  alkyl, C 1-8  haloalkyl, C 3-6  cycloalkyl, heterocycloalkyl, aryl and heteroaryl, and wherein the aliphatic and cyclic portions of R d , R e  and R f  are optionally further substituted with from one to three halogen, hydroxy, methyl, amino, alkylamino and dialkylamino groups; \n each R 3  is independently selected from the group consisting of \n halogen, \u2014CN, \u2014R i ,  13  CO 2 R g , \u2014CONR g R h , \u2014C(O )R g , \u2014OC(O)NR g R h , \u2014NR h C(O)R g , \u2014NR h C(O) 2 R i , \u2014NR g C(O)NR g R h , -NR g R h , \u2014OR g , \u2014S(O) 2 NR g R h , \u2014X 4 \u2014NR g R h , \u2014X 4 \u2014CONR  g R h , \u2014X 4 \u2014NR h C(O)R g , \u2014NHR j  and \u2014NHCH 2 R j  , wherein X 4  is a C 1-4  alkylene; each R g  and R h  is independently selected from hydrogen, C 1-8  alkyl, C 3-6  cycloalkyl and C 1-8 haloalkyl, or when attached to the same nitrogen atom can be combined with the nitrogen atom to form a five or six-membered ring having from 0 to 2 additional heteroatoms as ring members selected from N, O or S and is optionally substituted with one or two oxo; each R i  is independently selected from the group consisting of C 1-8  alkyl, C 1-8  haloalkyl, C 3-6  cycloalkyl, heterocycloalkyl, aryl and heteroaryl; and each is selected from the group consisting of C 3-6  cycloalkyl, pyrrolinyl, piperidinyl, morpholinyl, tetrahydrofuranyl, and tetrahydropyranyl, and wherein the aliphatic and cyclic portions of R g , R h , R j  are optionally further substituted with from one to three halogen, methyl, CF 3 , hydroxy, amino, alkylamino and dialkylamino groups; and \n X is hydrogen or CH 3 .

Metadata:
- Claim Count in Document: 14.0
- Percentile: 95.0
- Lexical Diversity: 1.34483
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['12643229', '15991747', '15991703', '13806339', '15908508']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.753339780232947
- 35 USC 102 Novelty (BERT): 0.5530227135441437
- Combined Prediction Score: 0.7333080735640667
- Mean Citation Score: 345.740594
- Max Citation Score: 404.33044
- Similarity Product: 343.3556063145566

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