PATENT CLAIM ANALYSIS

Application Number: 15981892
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2019-02
Patent Classification: ["514", "300000"]

Abstract:
This invention is directed to selective androgen receptor degrader (SARD) compounds pharmaceutical compositions and uses thereof in treating early prostate cancer, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

Claim (Index 36):
A method of adjuvant therapy of prostate cancer (PCa), and/or of neoadjuvant therapy of prostate cancer (PCa), and/or of treatment of early disease prostate cancer (PCa), and/or of treatment of prostate cancer (PCa) in intact males, and/or of treatment of prostate cancer (PCa) prior to androgen deprivation therapy (ADT) or castration, and/or of first line therapy of PCa, comprising administering to a subject in need thereof, a therapeutically effective amount of a selective androgen receptor degrader (SARD) compound represented by the structure of formula XIV: wherein\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;\n 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; \n 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;\n R 4  is hydrogen, F, Cl, Br, I, CF 3 , CN, NO 2 , NH 2 , SH, COOH, COOR, keto (\u2550O), 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 n is an integer between 1-3; \n m is an integer between 1-3; \n l is 0 or 1; and \n k is 0, 1 or 2; or its isomer, pharmaceutically acceptable salt, pharmaceutical product, polymorph, hydrate or any combination thereof.

Metadata:
- Claim Count in Document: 11.0
- Percentile: 93.0
- Lexical Diversity: 1.56
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15222734', '15135334', '15331777', '15981636', '15923668']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8977555415417812
- 35 USC 102 Novelty (BERT): 0.7233527192177254
- Combined Prediction Score: 0.8803152593093756
- Mean Citation Score: 942.740778
- Max Citation Score: 977.20337
- Similarity Product: 776.0549046237386

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