PATENT CLAIM ANALYSIS

Application Number: 15751163
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-08
Patent Classification: ["546", "115000"]

Abstract:
The invention relates to capthepsin K inhibitors and uses thereof, specifically relates to a class of compounds having the formula (I) which are used for treating or preventing cathepsin dependent diseases or conditions, specifically, wherein the cathepsin is capthepsin K. The compounds and compositions thereof can be used as bone resorption inhibitors for the treatment of associated diseases.

Claim (Index 1):
A compound having Formula (I) or a stereoisomer, a tautomer, a geometric isomer, an N-oxide, a prodrug or a pharmaceutically acceptable salt thereof, wherein, R 4a  is H, C 1-6  alkyl or C 2-6  alkenyl, wherein each of the C 1-6  alkyl and C 2-6  alkenyl is independently and optionally substituted with 1, 2, 3, 4, 5 or 6 substituents selected from halogen, C 3-6  cycloalkyl, cyano, C 6-10  aryl, C 1-9  heteroaryl and C 2-9  heterocyclyl; R 4  is C 1-6  alkyl, \u2014C(R 7 )(R 7a )\u2014R 8 , C 3-9  heterocyclyl or C 2-6  alkenyl, wherein each of the C 1-6  alkyl and C 2-6  alkenyl is independently and optionally substituted with 1, 2, 3, 4, 5 or 6 substituents selected from halogen, C 3-6  cycloalkyl, cyano, C 6-10  aryl, C 1-9  heteroaryl or C 3-9  heterocyclyl; or, R 4  and R 4a , together with the nitrogen atom to which they are attached, form a C 3-9  heterocyclyl group containing nitrogen, wherein the C 3-9  heterocyclyl is optionally substituted with 1, 2, 3, 4 or 5 substituents selected from C 1-6  alkyl, C 1-6  hydroxyalkyl, cyano, \u2014C(R 10 )(R 10a )\u2014C(\u2550O)\u2014N(R 12 )(R 12a ), \u2014C(\u2550O)\u2014OR 8a , oxo (\u2550O), C 1 , haloalkyl and halogen; each of R 7  and R 7a  is independently H, C 1-6  alkyl, \u2014C(R 10 )(R 10a )\u2014C(\u2550O)\u2014N(R 12 )(R 12a ), \u2014C(\u2550O)\u2014OR 8a , C 2-9  heterocyclyl or C 2-6  alkenyl; or, R 7  and R 7a , together with the carbon atom to which they are attached, form a C 3-6  carbocyclic ring or C 2-6  heterocyclic ring, wherein each of the C 3-6  carbocyclic ring and C 2-6  heterocyclic ring is independently and optionally substituted with 1, 2, 3, 4, 5 or 6 substituents selected from C 1-6  alkyl, C 1-6  hydroxyalkyl, C 1-6  haloalkyl, oxo (\u2550O), cyano, \u2014C(\u2550O)\u2014OR 8a  and halogen; R 8  is H, C 1-6  alkyl, cyano, \u2014N(R 12 )(R 12 ), \u2014C(\u2550O)\u2014C(\u2550O)\u2014N(R 12 )(R 12a ), \u2014C(\u2550O)\u2014N(R 12 )(R 12a ), \u2014C(\u2550O)\u2014OR 8a , C 3-6  heterocyclyl or C 2-6  alkenyl; each R 6 , R 6a , R 3 , R 3a , R 2 , R 2a , R 8a , R 10 , R 10a , R 12  and R 12a  is independently H or C 1-6  alkyl, wherein the C 1-6  alkyl is optionally substituted with 1, 2, 3, 4, 5 or 6 substituents selected from halogen, hydroxy, amino, carboxy, cyano, C 3-6  cycloalkyl, C 6-10  aryl, C 1-9  heteroaryl and C 2-9  heterocyclyl; or, R 2  and R 2a , together with the carbon atom to which they are attached, form a C 3-9  carbocyclic ring or C 2-9  heterocyclic ring, wherein each of the C 3-9  carbocyclic ring and C 2-9  heterocyclic ring is independently and optionally substituted with 1, 2, 3, 4, 5 or 6 substituents selected from C 1-6  alkyl, C 2-6  alkenyl, C 1-6  hydroxyalkyl, C 1-6  haloalkyl, hydroxy, amino, carboxy, cyano and halogen; or, R 3  and R 3a , together with the carbon atom to which they are attached, form a >C(\u2550O), C 3-9  carbocyclic ring or C 2-9  heterocyclic ring, wherein each of the C 3-9  carbocyclic ring and C 2-9  heterocyclic ring is independently and optionally substituted with 1, 2, 3, 4, 5 or 6 substituents selected from C 1-6  alkyl, C 2-6  alkenyl, C 1-6  hydroxyalkyl, C 1-6  haloalkyl, hydroxy, amino, carboxy, cyano and halogen; X is \u2014O\u2014, \u2014S\u2014, or \u2014NH\u2014; each of V, Z and Y is independently C(R 9 ) or N; each R 9  is independently H, halogen, cyano, hydroxy, C 1-4  alkoxy, \u2014N(R 6 )(R 6a ), C 1-4  haloalkyl or C 1-4  alkyl, wherein each of the C 1-4  alkyl is optionally substituted with 1, 2, 3, 4, 5 or 6 substituents selected from halogen, C 3-6  cycloalkyl, C 6-10  aryl, C 1-9  heteroaryl and C 2-9  heterocyclyl; R 5  is H, C 1-4  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  alkoxy, F, Cl, Br, nitro, cyano, \u2014N(R 6 )(R 6a ) or C 1-4  haloalkyl; R 1  is C 6-10  aryl, C 1-9  heteroaryl, C 3-12  cycloalkyl or C 2-12  heterocyclyl, wherein each of the R 1  is independently and optionally substituted with 1, 2, 3, 4 or 5 R 1a  which are the same or different; each R 1a  is independently H, C 1-6  alkyl, C 1-6  haloalkyl, halogen, cyano, oxo (\u2550O), C 1-6  alkoxy, C 6-10  aryl, C 1-9  heteroaryl, C 3-12  cycloalkyl, C 2-12  heterocyclyl, \u2014SR 14 , \u2014OR 14 , \u2014SO 2 \u2014N(R 13 )(R 13a ), \u2014N(R 13a )\u2014SO 2 \u2014R 14 , \u2014N(R 13 )(R 13a ), \u2014C(\u2550O)\u2014C(\u2550O)\u2014N(R 13 )(R 13a ), \u2014C(\u2550O)\u2014N(R 13 )(R 13a ), \u2014C(\u2550N\u2014OH)(R 14a ), \u2014N(R 13 )\u2014C(\u2550O)R 14a , \u2014C(\u2550O)\u2014OR 14 , \u2014C(\u2550O)\u2014R 14a  or \u2014SO 2 R 14 , wherein each of the R 1a  is independently and optionally substituted with 1, 2, 3, 4 or 5 R 1b  which are the same or different; each R 1b  is independently H, C 1-6  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  alkoxy, halogen, nitro, cyano, hydroxy, oxo (\u2550O), \u2014OR 15 , \u2014SO 2 R 15 , \u2014N(R 16 )(R 16a ), \u2014C(\u2550O)\u2014N(R 16 )(R 16a ), C 6-10  aryl, C 1-9  heteroaryl, C 3-12  cycloalkyl or C 2-12  heterocyclyl, wherein each of the R 1b  is independently and optionally substituted with 1, 2, 3, 4 or 5 substituents selected from hydroxy, nitro, cyano, C 1-6  alkyl, C 1-6  haloalkyl, halogen, oxo (\u2550O), C 1-6  alkoxy, C 6-10  aryl, C 1-9  heteroaryl, C 3-12  cycloalkyl, C 2-12  heterocyclyl and amino; each R 16  and R 16a  is independently H, C 1-4  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 6-10  aryl, C 1-9  heteroaryl, C 3-6  cycloalkyl, \u2014SO 2 R 17 , \u2014N(R 18 )(R 18a ), C 1-4  haloalkyl or C 2-9  heterocyclyl; each R 15 , R 13 , R 13a , R 14 , R 14a , R 17 , R 18  and R 18a  is independently H, C 1-4  alkyl, C 1-4  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, phenyl, 5- to 6-membered heteroaryl, C 3-6  cycloalkyl or 4- to 7-membered heterocyclyl, wherein each of the phenyl, 5- to 6-membered heteroaryl, C 3-6  cycloalkyl and 4- to 7-membered heterocyclyl is independently and optionally substituted with 1, 2, 3, 4 or 5 substituents selected from F, Cl, Br, cyano, hydroxy, trifluoromethyl, C 1-4  alkyl, C 1-4  alkoxy and 2,2-difluoroethyl.

Metadata:
- Claim Count in Document: 8.0
- Percentile: 88.0
- Lexical Diversity: 1.42222
- Patent Class: 546.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['12734224', '14647445', '14397200', '15580978', '14894817']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8212696152789446
- 35 USC 102 Novelty (BERT): 0.5303389131848002
- Combined Prediction Score: 0.7921765450695302
- Mean Citation Score: 341.089354
- Max Citation Score: 366.94565
- Similarity Product: 275.9553237405777

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