PATENT CLAIM ANALYSIS

Application Number: 15981636
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-12
Patent Classification: ["514", "300000"]

Abstract:
This invention provides novel indole, indazole, benzimidazole, benzotriazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, other AR-expressing cancers, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels (through degradation) and/or activity (through inhibition) of any androgen receptor including androgen receptor-full length (AR-FL) including pathogenic and/or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

Claim (Index 27):
A method of treating breast cancer in a subject in need thereof, wherein said subject has AR expressing breast cancer, AR-SV expressing breast cancer, and/or AR-V7 expressing breast cancer, comprising administering to the subject a therapeutically effective amount of a selective androgen receptor degrader (SARD) compound represented by the structure of formula I: wherein\n W 1  and W 2  are each independently selected from N or CH; \n W 3 , W 4 , W 5  and W 6  are each independently selected from CH or N; \n wherein if any one of W 1 , W 2 , W 3 , W 4 , W 5 , and W 6  is CH, then the H is optionally replaced with R 4 , Q or R 3  in the respective position, and if any one of W 1 , W 2 , W 3 , W 4 , W 5 , and W 6  is not CH, then the respective position is unsubstituted;\n T is OH, OR, \u2014NHCOCH 3 , NHCOR or \n Z is NO 2 , CN, COOH, COR, NHCOR or CONHR; Y is CF 3 , F, I, Br, Cl, CN or C(R) 3 ; R is alkyl, haloalkyl, dihaloalkyl, trihaloalkyl, CH 2 F, CHF 2 , CF 3 , CF 2 CF 3 , aryl, phenyl, F, Cl, Br, I, alkenyl or OH; R 1  is CH 3 , CH 2 F, CHF 2 , CF 3 , CH 2 CH 3 , or CF 2 CF 3 ; R 2  is hydrogen, halogen, CN, NO 2 , COOH, COOR, COR, NHCOR, CONHR, OH, OR, SH, SR, NH 2 , NHR, NR 2 , C 1 -C 12 -alkyl, C 1 -C 12 -haloalkyl, O\u2014C 1 -C 12 -alkyl, O\u2014C 1 -C 12 -haloalkyl, \u2014SO 2 -aryl, \u2014SO 2 -phenyl, \u2014CO-aryl, arylalkyl, benzyl, aryl, or C 3 -C 7 -cycloalkyl; Q is hydrogen, F, Cl, Br, I, CF 3 , CN, NO 2 , COOH, COOR, alkoxy, haloalkyl, optionally substituted linear or branched alkyl, optionally substituted linear or branched heteroalkyl, optionally substituted aryl, optionally substituted phenyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted arylalkyl, C(R) 3 , N(R) 2 , NHCOCH 3 , NHCOCF 3 , NHCOR, NHCONHR, NHCOOR, OCONHR, CONHR, NHCSCH 3 , NHCSCF 3 , NHCSR, NHSO 2 CH 3 , NHSO 2 R, OR, COR, OCOR, OSO 2 R, SO 2 R, SR, NCS, SCN, NCO or OCN; R 3  is hydrogen, F, Cl, Br, I, CF 3 , CN, NO 2 , NH 2 , SH, COOH, COOR, alkoxy, haloalkyl, optionally substituted linear or branched alkyl, optionally substituted linear or branched heteroalkyl, optionally substituted aryl, optionally substituted phenyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted arylalkyl, C(R) 3 , N(R) 2 , NHCOCH 3 , NHCOCF 3 , NHCOR, NHCONHR, NHCOOR, OCONHR, CONHR, NHCSCH 3 , NHCSCF 3 , NHCSR, NHSO 2 CH 3 , NHSO 2 R, OR, COR, OCOR, OSO 2 R, SO 2 R, SR, NCS, SCN, NCO or OCN; R 4  is hydrogen, F, Cl, Br, I, CF 3 , CN, NO 2 , NH 2 , SH, COOH, COOR, alkoxy, haloalkyl, optionally substituted linear or branched alkyl, optionally substituted linear or branched heteroalkyl, optionally substituted aryl, optionally substituted phenyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted arylalkyl, C(R) 3 , N(R) 2 , NHCOCH 3 , NHCOCF 3 , NHCOR, NHCONHR, NHCOOR, OCONHR, CONHR, NHCSCH 3 , NHCSCF 3 , NHCSR, NHSO 2 CH 3 , NHSO 2 R, OR, COR, OCOR, OSO 2 R, SO 2 R, SR, NCS, SCN, NCO or OCN; n is an integer between 1-3; and m is an integer between 1-3; or its isomer, pharmaceutically acceptable salt, pharmaceutical product, polymorph, hydrate or any combination thereof.

Metadata:
- Claim Count in Document: 197.0
- Percentile: 93.0
- Lexical Diversity: 1.63333
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15222734', '15135334', '15331777', '15331751', '15135151']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8913146676289845
- 35 USC 102 Novelty (BERT): 0.6542921728049852
- Combined Prediction Score: 0.8676124181465846
- Mean Citation Score: 847.607848
- Max Citation Score: 927.6335
- Similarity Product: 596.646108110398

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