PATENT CLAIM ANALYSIS

Application Number: 15981849
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2019-01
Patent Classification: ["514", "360000"]

Abstract:
This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors, R-isomers, and non-hydroxylated and/or non-chiral propanamides, and pharmaceutical compositions and uses thereof in treating 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 1):
A method of treating prostate cancer in a subject in need thereof, wherein said subject has AR overexpressing prostate cancer, castration-resistant prostate cancer, castration-sensitive prostate cancer, AR-V7 expressing prostate cancer, or d567ES expressing prostate 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 T is H, OH, OR, OCOR, CH 3 , \u2014NHCOCH 3 , or NHCOR; \n R 1  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , CH 2 CH 3 , or CF 2 CF 3 ;\n or T and R 1  form a 3-8 carbocyclic or heterocyclic ring; \n \n Y is H, CF 3 , F, I, Br, Cl, CN, or C(R) 3 ; \n Z is H, NO 2 , CN, halide, COOH, COR, NHCOR, CONHR, \n or Y and Z form a 5 to 8 membered fused ring; \n X is CH or N; \n R is H, alkyl, alkenyl, haloalkyl, alcohol, CH 2 CH 2 OH, CF 3 , CH 2 Cl, CH 2 CH 2 Cl, aryl, F, Cl, Br, I, or OH; \n A is R 2  or R 3 ; \n R 2  is a five or six-membered saturated or unsaturated ring having at least one nitrogen atom and 0, 1, or 2 double bonds, optionally substituted with at least one of Q 1 , Q 2 , Q 3  and Q 4 , each independently selected from hydrogen, keto, substituted or unsubstituted linear or branched alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, haloalkyl, CF 3 , substituted or unsubstituted aryl, substituted or unsubstituted phenyl, F, Cl, Br, I, CN, NO 2 , hydroxyl, alkoxy, OR, benzyl, NCS, maleimide, NHCOOR, N(R) 2 , NHCOR, CONHR, COOR or COR; \n R 3  is NHR 2 , halide, N 3 , OR 4 , CF 3 , COR 4 , COCl, COOCOR 4 , COOR 4 , OCOR 4 , OCONHR 4 , NHCOOR 4 , NHCONHR 4 , OCOOR 4 , CN, CONH 2 , CONH(R 4 ), CON(R 4 ) 2 , SR 4 , SO 2 R 4 , SOR 4  SO 3 H, SO 2 NH 2 , SO 2 NH(R 4 ), SO 2 N(R 4 ) 2 , NH 2 , NH(R 4 ), N(R 4 ) 2 , CO(N-heterocycle), NO 2 , cyanate, isocyanate, thiocyanate, isothiocyanate, mesylate, tosylate, triflate, PO(OH) 2  or OPO(OH) 2 ; and \n R 4  is H, alkyl, haloalkyl, cycloalkyl, aryl or heteroaryl, wherein said alkyl, haloalkyl, cycloalkyl, aryl or heteroaryl groups are optionally substituted; \n or its optical isomer, isomer, pharmaceutically acceptable salt, pharmaceutical product, hydrate or any combination thereof; \n wherein if A is Br or I, R 1  is CH 3 , and T is OH, then X is N or the aniline ring forms a fused heterocyclic ring.

Metadata:
- Claim Count in Document: 68.0
- Percentile: 93.0
- Lexical Diversity: 1.56044
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15923668', '15620761', '15981636', '15222734', '15331777']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8640238466012747
- 35 USC 102 Novelty (BERT): 0.740751649359886
- Combined Prediction Score: 0.8516966268771359
- Mean Citation Score: 746.166328
- Max Citation Score: 856.6156
- Similarity Product: 822.2859604431628

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