PATENT CLAIM ANALYSIS

Application Number: 16153193
Application Type: Utility
Filing Date: 2018-10
Publication Date: 2019-02
Patent Classification: ["514", "619000"]

Abstract:
This invention provides novel 3-amino propanamide selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, androgenic alopecia or other 5 hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), 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, suppressing, reducing the incidence, reducing the severity, or inhibiting the progression of a hormonal condition in a male in need thereof, comprising administering to the subject a therapeutically effective amount of a selective androgen receptor degrader (SARD) compound represented by the structure of formula IA: wherein\n T is OH, OR, \u2014NHCOCH 3 , or NHCOR; \n Z is NO 2 , CN, COOH, COR, NHCOR or CONHR; \n Y is CF 3 , F, I, Br, Cl, CN, C(R) 3  or Sn(R) 3 ; \n 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; \n R 1  is CH 3 , CH 2 F, CHF 2 , CF 3 , CH 2 CH 3 , or CF 2 CF 3 ; \n R 2  is hydrogen, C 1 -C 12 -alkyl, \u2014SO 2 -aryl, \u2014SO 2 -phenyl, \u2014CO-aryl, arylalkyl, benzyl, aryl, or C 3 -C 7 -cycloalkyl; \n Q 1 , Q 4 , and Q 5  are each independently selected from hydrogen, substituted or unsubstituted linear or branched alkyl, substituted aryl, F, Cl, Br, I, CF 3 , CN, NO 2 , substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted 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 Q 2  and Q 3  are each independently selected from hydrogen, substituted or unsubstituted linear or branched alkyl, substituted aryl, F, Cl, Br, I, CF 3 , CN, NO 2 , substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted 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 wherein at least two of Q 1 , Q 2 , Q 3 , Q 4 , and Q 5  are not hydrogens; or \n Q 1  and Q 2  are joined together to form a substituted or unsubstituted C 5 -C 8  carbocyclic or heterocyclic ring, and Q 3 , Q 4 , and Q 5  are as defined above; or \n Q 2  and Q 3  are joined together to form a substituted or unsubstituted C 5 -C 8  carbocyclic or heterocyclic ring, and Q 1 , Q 4 , and Q 5  are as defined above; and \n wherein said formed carbocyclic or heterocyclic ring is not dihydropyridin-2(1H)-one, pyridin-2(1H)-one or 1H-pyrrole; \n or its optical isomer, its racemic mixture, pharmaceutically acceptable salt, pharmaceutical product, polymorph, hydrate, or any combination thereof.

Metadata:
- Claim Count in Document: 5.0
- Percentile: 97.0
- Lexical Diversity: 1.42647
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15135151', '15331751', '15981636', '15135334', '15222734']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8942401069713637
- 35 USC 102 Novelty (BERT): 0.6710514425971049
- Combined Prediction Score: 0.8719212405339378
- Mean Citation Score: 793.601892
- Max Citation Score: 854.0647
- Similarity Product: 644.564618749547

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

Dataset: test