PATENT CLAIM ANALYSIS

Application Number: 16331579
Application Type: Utility
Filing Date: 2019-03
Publication Date: 2019-07
Patent Classification: ["514", "260100"]

Abstract:
The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to fused bicyclic compounds, pharmaceutical composition comprising such compounds, and their use as menin/MLL protein/protein interaction inhibitors, useful for treating diseases such as cancer, myelodysplastic syndrome (MDS) and diabetes.

Claim (Index 1):
A compound of Formula (I) or a tautomer or a stereoisomeric form thereof, wherein R 1  is selected from the group consisting of CH 3 , CH 2 F, CHF 2  and CF 3 ; R 2  is selected from the group consisting of hydrogen and CH 3 ; L 1  is a 7- to 9-membered fused heterocycle of Formula (a) wherein a represents the position of linkage to the thienopyrimidinyl heterocycle; m is equal to 0 or 1; n is equal to 0 or 1; p is equal to 0, 1 or 2; q is equal to 0 or 1; R is selected from the group consisting of hydrogen and oxo; and\n L 2 -R 3  is selected from (a), (b), (c), (d) or (e), wherein\n (a) L 2  is selected from the group consisting of >SO 2 , >CR 4a R 4b , and \u2014CHR 4a CHR 5 \u2014; \n \u2003wherein\n R 4a  is selected from the group consisting of hydrogen; \u2014C(\u2550O)NR 7a R 7b ; C 1-4 alkyl optionally substituted with a substituent selected from the group consisting of fluoro, \u2014CN, \u2014OR 8 , and \u2014NR 9a R 9b ; and C-linked 4- to 7-membered non-aromatic heterocyclyl containing at least one nitrogen, oxygen or sulfur atom; \n R 4b  is selected from the group consisting of hydrogen and methyl; or \n R 4a  and R 4b  together with the carbon atom to which they are attached form a C 3-5 cycloalkyl or a C-linked 4- to 6-membered heterocyclyl containing an oxygen atom; \n R 5  is selected from the group consisting of hydrogen; \u2014OR 6 ; \u2014NR 7a R 7b ; \u2014C(\u2550O)NR 7a R 7b ; C 1-4 alkyl optionally substituted with a substituent selected from the group consisting of fluoro, \u2014CN, \u2014OR 8 , and \u2014NR 9a R 9b ; and C-linked 4- to 7-membered non-aromatic heterocyclyl containing at least one nitrogen, oxygen or sulfur atom; wherein \n R 6 , R 7a , R 7b , R 8 , R 9a  and R 9b  are each independently selected from the group consisting of hydrogen; C 1-4 alkyl optionally substituted with a substituent selected from the group consisting of fluoro, \u2014CN and \u2014C(\u2550O)NR 10a R 10b ; and C 2-4 alkyl substituted with a substituent selected from the group consisting of \u2014OR 11  and \u2014NR 10a R 10b ; wherein \n R 10a , R 10b  and R 11  are each independently selected from the group consisting of hydrogen; C 1-4 alkyl; and C-linked 4- to 7-membered non-aromatic heterocyclyl containing at least one nitrogen, oxygen or sulfur atom; and \n R 3  is selected from the group consisting of Ar; Het 1 ; Het 2 ; and a 7- to 10-membered saturated spirocarbobicyclic system; or \n \n (b) L 2  is selected from >CR 4c R 4d  and \u2014CHR 4c CHR 5a \u2014; wherein R 4c , R 4d  and R 5a  are each independently selected from the group consisting of hydrogen and C 1-4 alkyl; and\n R 3  is selected from the group consisting of \n \n \n \u2003wherein R 12a , R 12b , and R 12c  are each independently selected from the group consisting of C 1-6 alkyl optionally substituted with a \u2014OH or a \u2014NH 2  substituent; and \u2014OC 1-6 alkyl; or (c) -L 2 -R 3  is C 1-6 alkyl optionally substituted with one, two or three fluoro or \u2014OH substituents; or (d) -L 2 -R 3  is \u2003wherein\n R 13  is selected from the group consisting of hydrogen; C 1-4 alkyl optionally substituted with a fluoro or a \u2014CN substituent; and C 2-4 alkyl substituted with a substituent selected from the group consisting of \u2014OR 14  and \u2014NR 15a R 15b ; wherein \n R 14 , R 15a  and R 15b  are each independently selected from the group consisting of hydrogen; C 1-4 alkyl optionally substituted with a substituent selected from the group consisting of fluoro, \u2014CN, and \u2014C(\u2550O)NR 16a R 16b ; C 2-4 alkyl substituted with a substituent selected from the group consisting of \u2014OR 17  and \u2014NR 16a R 16b ; and C-linked 4- to 7-membered non-aromatic heterocyclyl containing at least one nitrogen, oxygen or sulfur atom; wherein \n R 16a , R 16b  and R 17  are each independently selected from the group consisting of hydrogen and C 1-4 alkyl; and \n R 13a  is selected from the group consisting of hydrogen, fluoro and C 1-4 alkyl; \n R 13b  is selected from the group consisting of hydrogen, fluoro, \u2014OC 1-4 alkyl, and C 1-4 alkyl optionally substituted with 1, 2 or 3 fluoro substituents; or \n R 13a  and R 13b  are bound to the same carbon atom and together form a C 3-5 cycloalkyl or a C-linked 4- to 6-membered heterocyclyl containing an oxygen atom; or \n (e) -L 2 -R 3  is \u2003and wherein Ar is phenyl or naphthyl, each of which may be optionally substituted with one, two, or three substituents each independently selected from the group consisting of halo, \u2014CN, \u2014OR 18 , \u2014NR 19a R 19b , and C 1-4 alkyl optionally substituted with a substituent selected from the group consisting of fluoro, \u2014CN, \u2014OR 20 , \u2014NR 21a R 21b , and \u2014C(\u2550O)NR 21a R 21b ; Het 1  is a monocyclic heteroaryl selected from the group consisting of pyridyl, 4-, 5- or 6-pyrimidinyl, pyrazinyl, pyridazinyl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, 4- or 5-thiazolyl, isothiazolyl, and isoxazolyl; or a bicyclic heteroaryl selected from the group consisting of imidazothiazolyl, imidazoimidazolyl, benzofuranyl, benzothiophenyl, benzimidazolyl, benzoxazolyl, isobenzoxazolyl, benzisoxazolyl, benzothiazolyl, benzisothiazolyl, isobenzofuranyl, indolyl, isoindolyl, indolizinyl, indolinyl, isoindolinyl, indazolyl, pyrazolopyridinyl, pyrazolopyrimidinyl, imidazopyridinyl, imidazopyrazinyl, imidazopyridazinyl; each of which may be optionally substituted with one, two, or three substituents each independently selected from the group consisting of halo, \u2014CN, \u2014OR 18 , \u2014NR 19a R 19b , C 3-6 cycloalkyl, and C 1-4 alkyl optionally substituted with a substituent selected from the group consisting of fluoro, \u2014CN, \u2014OR 20 , \u2014NR 21a R 21b , and \u2014C(\u2550O)NR 21a R 21b , and Het 2  is a non-aromatic heterocyclyl optionally substituted with one, two, or three substituents each independently selected from the group consisting of halo, \u2014CN, \u2014OR 18 , \u2014NR 19a R 19b , \u2014C(\u2550O)C 1-6 alkyl, \u2014C(\u2550O)\u2014O\u2014C 1-6 alkyl, \u2014C(\u2550O)\u2014C 3-6 cycloalkyl, \u2014C(\u2550O)\u2014Ar 2 , \u2014C(\u2550O)\u2014Het 3 , \u2014C(\u2550O)\u2014Het 4 , and C 1-4 alkyl optionally substituted with a substituent selected from the group consisting of fluoro, \u2014CN, \u2014OR 20 , \u2014NR 21a R 21b , and \u2014C(\u2550O)NR 21a R 21b ; Ar 2  is phenyl; Het 3  is pyridyl; Het 4  is oxetanyl, tetrahydrofuranyl, or tetrahydropyranyl; wherein R 18 , R 19a , R 19b , R 20 , R 21a  and R 21b  are each independently selected from the group consisting of hydrogen; C 1-4 alkyl optionally substituted with a substituent selected from the group consisting of fluoro and \u2014C(\u2550O)NR 22a R 22b ; and C 2-4 alkyl substituted with a substituent selected from the group consisting of \u2014OR 23  and \u2014NR 22a R 22b , wherein R 22a , R 22b  and R 23  are each independently selected from the group consisting of hydrogen; C 1-4 alkyl; and C-linked 4- to 7-membered non-aromatic heterocyclyl containing at least one nitrogen, oxygen or sulfur atom; or a pharmaceutically acceptable salt or a solvate thereof.

Metadata:
- Claim Count in Document: 11.0
- Percentile: 99.0
- Lexical Diversity: 1.34146
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15766887', '15537619', '15976037', '15537551', '15976223']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7906852934181355
- 35 USC 102 Novelty (BERT): 0.5208708840121246
- Combined Prediction Score: 0.7637038524775345
- Mean Citation Score: 294.28313799999995
- Max Citation Score: 308.84235
- Similarity Product: 233.0628713307917

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