PATENT CLAIM ANALYSIS

Application Number: 15992813
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2019-01
Patent Classification: ["514", "364000"]

Abstract:
Use of phospho-Akt as a biomarker for predicting the response, such as resistance, to a compound, wherein phospho-Akt is Akt that has been phosphorylated on one or more residues, with the proviso that fir Akt1, Akt2, and Akt3 the designation phospho-Akt is used to indicate phosphorylation at a site other than T308, T309 or T305 respectively, wherein the compound is a compound of general formula (I) wherein R represents phenyl, thienyl or pyridinyl wherein phenyl is optionally substituted by one or two substituents independently selected from alkyl, halo-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, acyloxy-lower alkyl, phenyl, hydroxy, lower alkoxy, hydroxy-lower alkoxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy, lower alkylcarbonyloxy, amino, monoalkylamino, dialkylamino, lower alkoxycarbonylamino, lower alkylcarbonylamino, substituted amino wherein the two substituents on nitrogen form together with the nitrogen heterocyclyl, lower alkylcarbonyl, carboxy, lower alkoxycarbonyl, cyano, halogen, and nitro; and wherein two adjacent substituents are methylenedioxy; and wherein pyridinyl is optionally substituted by lower alkoxy, amino or halogen; X represents a group C═Y, wherein Y stands for oxygen or nitrogen substituted by hydroxy or lower alkoxy; R 1  represents hydrogen, lower alkylcarbonyl, hydroxy-lower alkyl or cyano-lower alkyl; R 2 , R 3  and R 6  represent hydrogen; R 4  and R 5 , independently of each other, represent hydrogen, lower alkyl or lower alkoxy, or R 4  and R 5  together represent methylenedioxy, and pharmaceutically acceptable derivatives thereof; or wherein R represents phenyl or pyridinyl wherein phenyl is optionally substituted by one or two substituents independently selected from alkyl, halo-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, acyloxy-lower alkyl, phenyl, hydroxy, lower alkoxy, hydroxy-lower alkoxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy, lower alkylcarbonyloxy, amino, monoalkylamino, dialkylamino, lower alkoxycarbonylamino, lower alkoxycarbonylamino, substituted amino wherein the two substituents on nitrogen form together with the nitrogen heterocyclyl, lower alkylcarbonyl, carboxy, lower alkoxycarbonyl, formyl, cyano, halogen, and nitro; and wherein two adjacent substituents are methylenedioxy; and wherein pyridinyl is optionally substituted by lower alkoxy, amino or halogen; X represents oxygen; R 1  represents hydrogen, lower alkylcarbonyl, hydroxy-lower alkyl or cyano-lower alkyl; R 2 , R 3  and R 6  represent hydrogen; R 4  and R 5 , independently of each other, represent hydrogen, lower alkyl or lower alkoxy, or R 4  and R 5  together represent methylenedioxy; and pharmaceutically acceptable derivatives thereof. Methods of treatment of neoplastic and autoimmune diseases with these compounds we also disclosed.

Claim (Index 26):
A method of treating a neoplastic disease in a subject in need thereof, said method comprising the steps of:\n a) determining the level of phospho-Akt proteins in a sample of biologic material obtained from the body of said subject, said phospho-Akt proteins being selected from the group consisting of phospho-Akt1, phospho-Akt2; and phospho-Akt3, wherein the phospho-Akt proteins contain at least one phosphorylation at a site other than T308 of phospho-Akt1, T309 of phospho-Akt2 and T305 of phospho-Akt3 respectively; and b) administering to said subject a compound of formula I: wherein: R represents phenyl, thienyl or pyridinyl, wherein phenyl is optionally substituted by one or two substituents independently selected from alkyl, halo-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, acyloxy-lower alkyl, phenyl, hydroxy, lower alkoxy, hydroxy-lower alkoxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy, lower alkylcarbonyloxy, amino, monoalkylamino, dialkylamino, lower alkoxycarbonylamino, lower alkylcarbonylamino, substituted amino wherein the two substituents on nitrogen form together with the nitrogen heterocyclyl, lower alkylcarbonyl, carboxy, lower alkoxycarbonyl, cyano, halogen, and nitro; and wherein two adjacent substituents are methylenedioxy; and wherein pyridinyl is optionally substituted by lower alkoxy, amino or halogen; X-represents a group C\u2550Y, wherein Y is oxygen or nitrogen substituted by hydroxy or lower alkoxy; or when R is optionally substituted phenyl or optionally substituted pyridinyl, X is alternatively oxygen; R 1  represents hydrogen, lower alkylcarbonyl, hydroxy-lower alkyl or cyano-lower alkyl; R 2 , R 3  and R 6  represent hydrogen; R 4  and R 5 , independently of each other, represent hydrogen, lower alkyl or lower alkoxy; or R 4  and R 5  together represent methylenedioxy; wherein the term \u201clower\u201d denotes a radical having up to 7 carbon atoms; or pharmaceutically acceptable salts, esters and amides of naturally occurring amino acids, small peptides or pegylated hydroxy acids; salts of such esters and amides; and isomers of the compound of formula I;\n if the level of phospho-Akt proteins in said sample is not higher than a standard value or set of standard values for the level of phospho-Akt proteins; \n wherein said neoplastic disease is selected from the group consisting of epithelial neoplasms, squamous cell neoplasms, basal cell neoplasms, transitional cell papillomas and carcinomas, adenomas and adenocarcinomas, adnexal and skin appendage neoplasms, mucoepidermoid neoplasms, cystic neoplasms, mucinous and serous neoplasms, ducal-, lobular and medullary neoplasms, acinar cell neoplasms, complex epithelial neoplasms, specialized gonadal neoplasms, paragangliomas and glomus tumours, naevi and melanomas, soft tissue tumours and sarcomas, fibromatous neoplasms, myxomatous neoplasms, lipomatous neoplasms, myomatous neoplasms, complex mixed and stromal neoplasms, fibroepithelial neoplasms, synovial like neoplasms, mesothelial neoplasms, germ cell neoplasms, trophoblastic neoplasms, mesonephromas, blood vessel tumours, lymphatic vessel tumours, osseous and chondromatous neoplasms, giant cell tumours, miscellaneous bone turnouts, odontogenic tumours, gliomas, neuroepitheliomatous neoplasms, meningiomas, nerve sheath tumours, granular cell tumours and alveolar soft part sarcomas, Hodgkin's and non-Hodgkin's lymphomas, other lymphoreticular neoplasms, plasma cell tumours, mast cell tumours, immunoproliferative diseases, leukemias, miscellaneous myeloproliferative disorders, lymphoproliferative disorders and myelodysplastic syndromes.

Metadata:
- Claim Count in Document: 197.0
- Percentile: 93.0
- Lexical Diversity: 3.824
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['14005680', '15060998', '15294157', '13983887', '13979955']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8397641350208792
- 35 USC 102 Novelty (BERT): 0.6953952001560323
- Combined Prediction Score: 0.8253272415343945
- Mean Citation Score: 686.2725800000002
- Max Citation Score: 900.06415
- Similarity Product: 688.8517439126849

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

Dataset: test