PATENT CLAIM ANALYSIS

Application Number: 16028730
Application Type: Utility
Filing Date: 2018-07
Publication Date: 2018-12
Patent Classification: ["514", "235200"]

Abstract:
The invention provides methods of treatment of a progressive bone disease, such as osteoporosis, Paget's Disease, multiple myeloma, or hyperparathyroidism, comprising administration of an effective amount of a non-agonist PPARG modulator to a patient afflicted with the disease.

Claim (Index 17):
Use of a compound of formula (I) for treatment of a progressive bone disease, wherein the compound of formula (I) is: wherein: R is H, (C 1 -C 6 )alkyl, (C 3 -C 9 )cycloalkyl, or (C 3 -C 9 )cycloalkyl(C 1 -C 6 )alkyl; Y 1  or Y 2  are each independently C or N, provided that when Y 1  or Y 2  is N, R 1  or R 2 , respectively, is absent; R 1  and R 2  are independently H, (C 1 -C 6 )alkyl, (C 3 -C 9 )cycloalkyl, or (C 1 -C 6 )haloalkyl; or R 1  and R 2  together with the atoms to which they are bonded form a 5- to 9-membered ring, comprising 0-3 heteroatoms selected from the group consisting of O, NR, and SO q  wherein q is 0, 1, or 2, and optionally mono- or multi-substituted with independently selected (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, (C 6 -C 10 )aryl, (C 3 -C 9 )cycloalkyl, halo, oxo, (C 1 -C 6 )haloalkyl, nitro, cyano-(C 0 -C 6 )alkyl, R\u2032O 2 C\u2014(C 0 -C 6 )alkyl, methylenedioxy, R\u2032O\u2014(C 0 -C 6 )alkyl, (R\u2032) 2 N\u2014(C 0 -C 6 )alkyl, (R\u2032) 2 NC(\u2550O)\u2014(C 0 -C 6 )alkyl, R\u2032C(\u2550O)N(R\u2032)\u2014(C 0 -C 6 )alkyl, (C 1 -C 6 )alkyl-S(O) q (C 0 -C 6 )alkyl, aryl, aroyl, or SO 2 NR\u2032 2 ; R 3  is optionally mono- or multi-substituted (C 1 -C 6 )alkyl, (C 1 -C 6 )alkenyl, (C 1 -C 6 )alkynyl, (C6-C10)aryl, (C6-C10)aryl(C 1 -C 6 )alkyl, (3-9 membered)heterocyclyl, (3-9 membered)heterocyclyl(C 1 -C 6 )alkyl, (3-9 membered)heteroaryl, or (3-9 membered)heteroaryl(C 1 -C 6 )alkyl; wherein if present each substituent on R 3  is independently selected from the group consisting of (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, (C 6 -C 10 )aryl, (C 3 -C 9 )cycloalkyl, 3-9 membered mono- and bicyclic heterocyclyl, 3-9 membered mono- and bicyclic heteroaryl, halo, oxo, haloalkyl, haloalkoxy, nitro, cyano, CO 2 R\u2032, methylenedioxy, OR\u2032, N(R\u2032) 2 , C(O)N(R\u2032) 2 , (C 1 -C 6 )alkyl-S(O) q , SO 2 NR\u2032 2 , and (C 1 -C 6 )alkoxyl; and provided that group R 3 N(R\u2032)C(\u2550O)\u2014 can be bonded to any one of the four carbon atoms of the phenyl ring not bonded to N 1  or Y 1 ; wherein each R\u2032 is independently H, (C 1 -C 6 ) alkyl, (C 3 -C 9 )cycloalkyl, (C 3 -C 9 )cycloalkyl(C 1 -C 6 )alkyl, (C 6 -C 10 )aryl, or (C 6 -C 10 )aryl(C 1 -C 6 ) alkyl, or wherein two R\u2032 bonded to an atom together with the atom form a 3-9 membered ring optionally further comprising a heteroatom selected from the group consisting of O, NR\u2032, and S(O) q ; wherein any alkyl, alkenyl, alkynyl, aryl, arylalkyl, or cycloalkyl is optionally mono- or independently multi-substituted with (C 1 -C 6 )alkyl, (C 1 -C 6 )haloalkyl, (C 1 -C 6 )alkoxy, (C 1 -C 6 )haloalkoxy, halo, oxo, aryl, or aroyl; each of X 1 -X 5  is independently N or CH, or is C substituted with an independently selected R 4  or is C substituted with Z, provided that no more than two of X 1 -X 5  are N, and provided that there is no more than one Z group bonded to the ring comprising X 1 -X 5 ; each R 4  is independently halo, nitro, (C 1 -C 6 )fluoroalkyl, R\u2032\u2014(C 0 -C 6 )alkyl, R\u2032O 2 C\u2014(C 0 -C 6 )alkyl, NC\u2014(C 0 -C 6 )alkyl, R\u2032O\u2014(C 0 -C 6 )alkyl, (R\u2032) 2 N\u2014(C 0 -C 6 )alkyl, (R\u2032) 2 NC(\u2550O)\u2014(C 0 -C 6 )alkyl, R\u2032C(\u2550O)N(R\u2032)\u2014(C 0 -C 6 )alkyl, C-bonded tetrazolyl, 3-hydroxypyrrolidin-1-carbonyl, 2-hydroxyethylaminocarbonyl, cyclohexylaminocarbonyl, 2-(N,N-dimethylaminocarbonyl)-2-hydroxyethylaminocarbonyl, N,N-dimethylaminoethylcarbonyl, N-methylaminocarbonyl, N-hydroxylaminocarbonyl, (1,3,4-oxadiazol-2(3H)-on)-yl, (1,2,4-oxadiazol-5(4H)-on)-3-yl, (C 1 -C 6 )alkyl-S(O) q (C 0 -C 6 )alkyl, R'S(O) 2 NHC(O), R\u2032C(O)NHS(O) 2 , an unsubstituted or substituted aryl, an unsubstituted or substituted heteroaryl, (C 1 -C 6 )alkyl or (C 3 -C 9 )cycloalkyl-(C 0 -C 6 )alkyl, wherein any alkyl or cycloalkyl is optionally mono- or independently multi-substituted with R\u2032, OR\u2032, N(R\u2032) 2 , C-bonded tetrazolyl, (C 1 -C 6 )alkyl-S(O) q (C 0 -C 6 )alkyl, an unsubstituted or substituted aryl, or an unsubstituted or substituted heteroaryl; or R 4  is \u2014(C(R\u2033) 2 ) m CO 2 R\u2032, \u2014(C(R\u2033) 2 ) m CON(R\u2032) 2 , \u2014(C(R\u2033) 2 ) m CN, \u2014O(C(R\u2033) 2 ) m CO 2 R\u2032, \u2014O(C(R\u2033) 2 ) m CON(R\u2032) 2 , or \u2014O(C(R\u2033) 2 ) m CN, wherein m is 1, 2, or 3; R\u2033 is H, halo, (C 1 -C 6 ) alkyl, (C 1 -C 6 ) haloalkyl, (C 3 -C 9 )cycloalkyl, (C 3 -C 9 )cycloalkyl(C 1 -C 6 )alkyl, (C 6 -C 10 )aryl, or (C 6 -C 10 )aryl(C 1 -C 6 ) alkyl, or two R\u2033 together with an atom to which they are bonded form a 3- to 9-membered ring; Z is a group of formula wherein a wavy line indicates a point of bonding, each of Z 1 -Z 5  is independently N or is C substituted with an independently selected H or R 4 ; provided that no more than two of Z 1 -Z 5  are N;\n Y is (C 1 -C 2 )alkyl, or sulfur; \n when Y is (C 1 -C 2 )alkyl, R 5  and R 6  are independently H or (C 1 -C 4 )alkyl or independently each R 5  and R 6  together with the carbon atom to which they are bonded form a carbonyl, or, one R 5  group can further be bonded to X 5  to form a 4- to 8-membered ring; and, \n when Y is sulfur, R 5  and R 6  are both oxygen; \n or a pharmaceutically acceptable salt thereof; \n wherein the effective dose of the compound acts to inhibit bone resorption, improve bone formation, or both, in the patient.

Metadata:
- Claim Count in Document: 11.0
- Percentile: 95.0
- Lexical Diversity: 1.28571
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15302862', '13490324', '13490342', '13811965', '14060563']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7336423948082816
- 35 USC 102 Novelty (BERT): 0.5851460540466209
- Combined Prediction Score: 0.7187927607321156
- Mean Citation Score: 348.215824
- Max Citation Score: 526.92584
- Similarity Product: 380.00053695172784

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

Dataset: test