PATENT CLAIM ANALYSIS

Application Number: 16175895
Application Type: Utility
Filing Date: 2018-10
Publication Date: 2019-05
Patent Classification: ["514", "318000"]

Abstract:
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

Claim (Index 6):
The compound according to  claim 1  having the structure: or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt or solvate thereof; wherein: R 1  is \u2014CH(CH 3 ) 2  or cyclopropyl; E 1 , E 2  and E 3  together form a moiety selected from a is zero; L 1  is a covalent bond, \u2014CH 2 \u2014, \u2014CH 2 CH 2 \u2014, \u2014CH\u2550CH\u2014, \u2014C\u2261C\u2014, \u2014CH(OH)\u2014, \u2014CH(OH)CH 2 \u2014 \u2014CH 2 O\u2014, \u2014CH 2 OCH 2 \u2014, \u2014CH 2 NH\u2014, \u2014C(O)\u2014, \u2014C(O)NH\u2014, \u2014C(O)NHCH 2 \u2014, \u2014C(O)N(CH 3 )CH 2 \u2014, \u2014C(S)NH\u2014, imidazolyl, oxadiazolyl, thiadiazolyl, thiazolyl, or triazolyl; Z is 1,5-naphthyridinyl, benzo[d]imidazolyl, benzo[d]oxazolyl, benzo[d]thiazolyl, cyclopropyl, cyclohexyl, imidazo[1,2-a]pyridinyl, imidazo[1,2-b]pyridazinyl, indazolyl, indolyl, isoquinolinyl, naphthalenyl, oxadiazolyl, oxazolyl, phenyl, piperidinyl, pyrazinyl, pyrazolo[1,5-a]pyridinyl, pyrazolo[3,4-b]pyridinyl, pyrazolyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrrolo[2,3-b]pyridinyl, quinazolinyl, quinolinyl, tetrahydroimidazo[1,2-a]pyrazinyl, tetrahydroisoquinolinyl, or thiazolyl, each substituted with zero to 3 R 10 ; R x  is \u2014CN, \u2014CH 2 OH, \u2014C(O)OH, \u2014C(CH 3 ) 2 C(O)CN, \u2014C(CH 3 ) 2 C(O)NH 2 , \u2014C(CH 3 ) 2 C(O)OH, \u2014C(CH 3 ) 2 CN, \u2014C(O)N(CH 3 ) 2 , \u2014C(O)NH 2 , \u2014C(O)NHS(O) 2 (cyclopropyl), \u2014C(O)NHS(O) 2 (phenyl), \u2014C(O)NHS(O) 2 CH 3 , \u2014CH 2 (tetrazolyl), \u2014CH 2 C(O)N(CH 3 ) 2 , \u2014CH 2 C(O)NH(CH 3 ), \u2014CH 2 C(O)OH, \u2014CH 2 CH 2 COOH, \u2014CH 2 OCH 2 COOH, \u2014C(O)OCH 3 , -carboxycyclopropyl, \u2014OCH(CH 3 )C(O)OH, \u2014OCH 2 COOH, tetrazolyl, or carboxythiazolyl; each R 10  is independently F, Cl, \u2014OH, \u2014CN, \u2014CH 3 , \u2014CH 2 CH 3 , \u2014CH 2 CH 2 CH 3 , \u2014CH(CH 3 ) 2 , C 1-3  alkyl, \u2014CHF 2 , \u2014CF 3 , \u2014CF 2 CH 3 , \u2014CH 2 OCH 3 , \u2014OCH 3 , \u2014OCH 2 CH 3 , \u2014OCH(CH 3 ) 2 , \u2014OCHF 2 , \u2014OCF 3 , \u2014OCH 2 CHF 2 , \u2014OCH 2 CF 3 , \u2014OCH 2 C(CH 3 ) 20 H, \u2014OCH 2 CH 2 OCH 3 , \u2014OCH 2 CH 2 CH 2 OCH 3 , \u2014OCH(CH 2 Cl)(CH 2 OH), \u2014OCH 2 CH(CH 2 Cl)(CH 2 OH), \u2014O(C 3-5  cycloalkyl), \u2014N(CH 3 ) 2 , \u2014S(O) 2 CH 3 , \u2014CH 2 (cyclopropyl), \u2014CH 2 (oxetanyl), \u2014OCH 2 (cyclopropyl), \u2014NH(cyclopropyl), \u2014NH(phenyl), \u2014O(oxetanyl), \u2014O(tetrahydrofuranyl), \u2014O(tetrahydropyranyl), \u2014OCH 2 (cyclopropyl), \u2014OCH 2 (cyclobutyl), \u2014OCH 2 (oxetanyl), \u2014OCH 2 CH 2 (pyrrolidinyl), cyclopropyl, azetidinyl, (hydroxymethyl)azetidinyl, fluoroazetidinyl, (dimethylamino)azetidinyl, methoxyazetidinyl, hydroxyazetidinyl, morpholinyl, piperazinyl, methylpiperazinyl, hydroxypiperidinyl, pyrrolidinyl, or hydroxypyrrolidinyl; L 2  is covalent bond or \u2014CH(cyclopropyl)-; R 2  is cyclopropyl, phenyl, pyridinyl, or pyrazolyl, each independently substituted with 0 to 3 R 16 ; and each R 16  is independently F, Cl, \u2014CH 3 , \u2014CF 3 , \u2014OCH 3 , or \u2014OCF 3 .

Metadata:
- Claim Count in Document: 5.0
- Percentile: 97.0
- Lexical Diversity: 1.5
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['14971875', '15541018', '14971825', '16322945', '12377307']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8048113233909084
- 35 USC 102 Novelty (BERT): 0.5331863370246905
- Combined Prediction Score: 0.7776488247542866
- Mean Citation Score: 329.48176399999994
- Max Citation Score: 338.1815
- Similarity Product: 269.01835749858617

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