PATENT CLAIM ANALYSIS

Application Number: 16130801
Application Type: Utility
Filing Date: 2018-09
Publication Date: 2019-04
Patent Classification: ["544", "350000"]

Abstract:
The present invention is directed to imidazo[1,2-a]pyrazine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

Claim (Index 61):
The method of  claim 59 , wherein:\n Ring A is phenyl optionally substituted by 1, 2, or 3 substituents independently selected from R A ; Ring B is phenyl, pyridyl, or pyrimidinyl, each optionally substituted by 1 or 2 substituents independently selected from R B ; R 1  is halo, C 1-3  alkyl, Cy 1 , OR a1 , SR a1 , C(O)NR c1 R d1 , NR c1 R d1 , NR c1 C(O)R b1 , or NR c1 C(O)NR c1 R d1 ; wherein said C 1-3  alkyl is optionally substituted with 1, 2, or 3 substituents independently selected from Cy 1 , halo, CN, OH, OR a1 , C(O)NR c1 R d1 , NR c1 R d1 , and NR c1 C(O)R b1 ; R 2  is H, halo, C 1-3  alkyl, C 1-3  haloalkyl, Cy 2 , C(O)NR c2 R d2 , NR c2 R d2 , or NR c2 C(O)R b2 ; wherein said C 1-3  alkyl is optionally substituted with 1, 2, or 3 substituents independently selected from Cy 2 , halo, CN, OR a2 , C(O)NR c2 R d2 , NR c2 R d2 , and NR c2 C(O)R b2 ; R 3  is H; each R A  is independently selected from halo, C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  haloalkyl, CN, OR a4 , SR a4 , C(O)R b4 , C(O)NR c4 R d4 , NR c4 R d4 , NR c4 C(O)R b4 , NR c4 S(O) 2 R b4 , S(O)R b4 , S(O)NR c4 R d4 , S(O) 2 R b4 , and S(O) 2 NR c4 R d4 , wherein said C 1-6  alkyl, C 2-6  alkenyl, and C 2-6  alkynyl are each optionally substituted by 1, 2, or 3, substituents independently selected from halo, C 1-6  haloalkyl, CN, OR a4 , SR a4 , C(O)R b4 , C(O)NR c4 R d4 , NR c4 R d4 , NR c4 C(O)R b4 , NR c4 S(O) 2 R b4 , S(O)R b4 , S(O)NR c4 R d4 , S(O) 2 R b4 , and S(O) 2 NR c4 R d4 ; each R B  is independently selected from Cy 3 , halo, C 1-6  alkyl, C 1-6  haloalkyl, CN, OR a5 , C(O)NR c5 R d5 , NR c5 R d5 , NR c5 C(O)R b5 , NR c5 C(O)OR a5 , NR c5 C(O)NR c5 R d5 , NR c5 S(O)R b5 , NR c5 S(O) 2 R b5 , and NR c5 S(O) 2 NR c5 R d5 , wherein said C 1-6  alkyl is optionally substituted by 1, 2, or 3 substituents independently selected from Cy 3 , halo, C 1-6  haloalkyl, CN, OR a5 , C(O)NR c5 R d5 , NR c5 R d5 , and NR c5 C(O)R b5 ; each Cy 1 , Cy 2 , Cy 3 , and Cy 4  is independently selected from phenyl, cyclopropyl, azetidinyl, piperidinyl, pyrrolidinyl, diazapanyl, and diazaspirononanyl, each of which is optionally substituted with 1 or 2 substituents independently selected from R Cy ; each R Cy  is independently selected from halo, C 1-4  alkyl, C 1-4  haloalkyl, C 1-4  cyanoalkyl, CN, OR 36 , and NR c6 R d6 ; each R a1  is independently selected from C 1-3  alkyl and Cy 4 ; wherein said C 1-3  alkyl is optionally substituted with 1, 2, or 3 substituents independently selected from Cy 4 , halo, CN, and OR a3 , and NR c3 R d3 ; each R b1 , R c1 , and R d1  is independently selected from H, C 1-3  alkyl, C 1-3  haloalkyl, phenyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, pyridinyl, pyrimidinyl, azetidinyl, piperidinyl, pyrrolidinyl, thiazolyl, phenyl-C 1-2  alkyl-, cyclopropyl-C 1-2  alkyl-, cyclobutyl-C 1-2  alkyl-, cyclopentyl-C 1-2  alkyl-, cyclohexyl-C 1-2  alkyl-, pyridinyl-C 1-2  alkyl-, pyrimidinyl-C 1-2  alkyl-, azetidinyl-C 1-2  alkyl-, piperidinyl-C 1-2  alkyl-, pyrrolidinyl-C 1-2  alkyl-, and thiazolyl-C 1-2  alkyl-, wherein said C 1-3  alkyl, C 1-3  haloalkyl, phenyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, pyridinyl, pyrimidinyl, azetidinyl, piperidinyl, pyrrolidinyl, thiazolyl, phenyl-C 1-2  alkyl-, cyclopropyl-C 1-2  alkyl-, cyclobutyl-C 1-2  alkyl-, cyclopentyl-C 1-2  alkyl-, cyclohexyl-C 1-2  alkyl-, pyridinyl-C 1-2  alkyl-, pyrimidinyl-C 1-2  alkyl-, azetidinyl-C 1-2  alkyl-, piperidinyl-C 1-2  alkyl-, pyrrolidinyl-C 1-2  alkyl-, and thiazolyl-C 1-2  alkyl- are each optionally substituted with 1, 2, or 3 substituents independently selected from C 1-3  alkyl, C 1-3  haloalkyl, halo, CN, OR a7 , and NR c7 R d7 ; or any R c1  and R d1  together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with NR c7 R d7 ; each R a2 , R b2 , R c2 , and R d2  is independently selected from H, C 1-3  alkyl, C 1-3  haloalkyl, phenyl, cyclopropyl, cyclobutyl, cyclopropyl-C 1-2  alkyl-, cyclobutyl-C 1-2  alkyl-, pyridinyl, pyrimidinyl, isoxazolyl, azetidinyl, piperidinyl, and pyrrolidinyl, wherein said C 1-3  alkyl, C 1-3  haloalkyl, phenyl, cyclopropyl, cyclobutyl, cyclopropyl-C 1-2  alkyl-, cyclobutyl-C 1-2  alkyl-, pyridinyl, pyrimidinyl, isoxazolyl, azetidinyl, piperidinyl, and pyrrolidinyl are each optionally substituted with 1 or 2 substituents independently selected from C 1-4  alkyl, C 1-4  haloalkyl, C 1-4  cyanoalkyl, halo, CN, OR a7 , and NR c7 R d7 ; each R a3 , R b3 , R c3 , and R d3  is independently selected from H, C 1-3  alkyl, C 1-3  haloalkyl, phenyl, cyclopropyl, cyclobutyl, cyclopropyl-C 1-2  alkyl-, cyclobutyl-C 1-2  alkyl-, pyridinyl, pyrimidinyl, isoxazolyl, azetidinyl, piperidinyl, and pyrrolidinyl, wherein said C 1-3  alkyl, C 1-3  haloalkyl, phenyl, cyclopropyl, cyclobutyl, cyclopropyl-C 1-2  alkyl-, cyclobutyl-C 1-2  alkyl-, pyridinyl, pyrimidinyl, isoxazolyl, azetidinyl, piperidinyl, and pyrrolidinyl are each optionally substituted with 1 or 2 substituents independently selected from C 1-4  alkyl, C 1-4  haloalkyl, C 1-4  cyanoalkyl, halo, CN, OR a7 , and NR c7 R d7 ; each R a4 , R b4 , R c4 , and R d4  is independently selected from H and C 1-3  alkyl; each R a5 , R b5 , R c5 , and R d5  is independently selected from H or C 1-3  alkyl; each R a6 , R b6 , R c6 , and R d6  is independently selected from H or C 1-3  alkyl; and each R a7 , R b7 , R c7 , and R d7  is independently selected from H or C 1-3  alkyl.

Metadata:
- Claim Count in Document: 2.0
- Percentile: 97.0
- Lexical Diversity: 1.0
- Patent Class: 544.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['14795466', '15613361', '15610015', '14795536', '16038924']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8300349565846337
- 35 USC 102 Novelty (BERT): 0.6583760921030372
- Combined Prediction Score: 0.812869070136474
- Mean Citation Score: 619.088486
- Max Citation Score: 655.64526
- Similarity Product: 614.443662016847

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

Dataset: test