PATENT CLAIM ANALYSIS

Application Number: 15975296
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-09
Patent Classification: ["548", "255000"]

Abstract:
Compounds for targeting and agents for imaging, prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.

Claim (Index 1):
A method comprising:\n administering to a patient, a compound comprising Formula I: and pharmaceutically acceptable salts and stereoisomers thereof, wherein:\n X 1  is CH or N; \n X 2  is CH or N; \n X 3  is (CH 2 ) 1-6  wherein at least one CH 2  is optionally replaced by at least one of CONH or aryl;\n X 4  is selected from the group consisting of aryl, NH, CH 2 , and \n \n X 5  is selected from the group consisting of CONH, C(O), (CH 2 ) 1-2 \u2014C(O) and (CH 2 ) 1-2 \u2014CONH; X 6  is aryl or CH; X 7  is CH or N; X 8  is CH or N; X 13  is (CH 2 ) 1-5 , where at least one CH 2  of (CH 2 ) 1-5  is replaced by aryl, NH, CH 2 , and R 1  is selected from the group consisting of alkyne, N 3 , NO 2 , \u2014(CH 2 ) 1-20 \u2014R 3  where at least one CH 2  of \u2014(CH 2 ) 1-20 \u2014R 3  is optionally replaced by at least one of \u2014O\u2014, aryl, heteroaryl, NH or CONH and wherein at least one H of \u2014(CH 2 ) 1-20 \u2014R 3  is optionally substituted with COOH or NO 2 ; and (\u2014CH 2 \u2014CH 2 \u2014O\u2014) 1-5 \u2014NH 2  where at least one CH 2  of (\u2014CH 2 \u2014CH 2 \u2014O\u2014) 1-5 \u2014NH 2  is optionally replaced by aryl or heteroaryl; R 2  is selected from the group consisting of H, COOH or CH 2 \u2014COOH; and R 3  is selected from the group consisting of COOH, N 3 , alkyne, protecting group, halo and positron emitting isotope; or\n administering to a patient, a compound comprising Formula II: \n and pharmaceutically acceptable salts and stereoisomers thereof, wherein:\n X 1  is CH or N; \n X 2  is CH or N; \n X 9  is (CH 2 ) 1-5  where at least one CH 2  is optionally replaced by NH, \n X 10  is CH or N; \n X 11  is selected from the group consisting of (CH 2 ), aryl, or heteroaryl, wherein at least one H of the aryl or heteroaryl is optionally replaced by NO 2 , \n X 12  is selected from the group consisting of O, CONH and (CH 2 ) 1-2  wherein at least one CH 2  is optionally replaced by NH; \n R 2  is selected from the group consisting of H, COOH or CH 2 \u2014COOH; \n R 4  is selected from the group consisting of H, alkyne, N 3 , NO 2 , \u2014(CH 2 ) 1-20 \u2014R 8  where at least one CH 2  of \u2014(CH 2 ) 1-20 \u2014R 8  is optionally replaced by at least one of \u2014O\u2014, aryl, heteroaryl, NH or CONH and wherein at least one H of \u2014(CH 2 ) 1-20 \u2014R 8  is optionally substituted with COOH or NO 2 ; \n R 8  is selected from the group consisting of H and \u2014(CH 2 ) 1-10 \u2014R 8  where at least one CH 2  of \u2014(CH 2 ) 1-10 \u2014R 8  is optionally replaced by at least one of \u2014O\u2014, aryl, heteroaryl or CONH; \n R 6  is selected from the group consisting of H and \u2014(CH 2 ) 1-10 \u2014R 8  where at least one CH 2  of \u2014(CH 2 ) 1-10 \u2014R 9  is optionally replaced by at least one of \u2014O\u2014, aryl, heteroaryl or CONH; and \n R 8  is selected from the group consisting of COOH, N 3 , alkyne, protecting group, halo and positron emitting isotope; \n or\n administering to a patient, a compound comprising Formula III: \n and pharmaceutically acceptable salts and isomers thereof, wherein:\n X 1  is CH or N; \n X 13  is (CH 2 ) 1-5  wherein at least one CH 2  is optionally replaced by aryl; \n R 2  is selected from the group consisting of H, COOH or CH 2 \u2014COOH; \n R 11  is selected from the group consisting of alkyne, N 3 , NO 2 , (CH 2 ) 1-10 \u2014R 12  wherein at least one CH 2  is optionally replaced by at least one of CONH, aryl or heteroaryl; and \n R 12  is selected from the group consisting of N 3 , alkyne, protecting group, halo and radioisotope; \n or\n administering to a patient, a compound comprising Formula IV: \n and pharmaceutically acceptable salts and isomers thereof, wherein:\n X 1  is CH or N; \n X 14  is selected from the group consisting of: C(O) and heteroaryl, wherein at least one H of the heteroaryl is substituted with NO 2 ; \n X 15  is selected from the group consisting of: a bond, NH, CH 2 , aryl, heteroaryl, cycloalkyl and heterocycloalkyl; \n X 16  is at least one selected from the group consisting of: a bond, aryl, heteroaryl, (CH 2 ) 1-25 , wherein at least one CH 2  of (CH 2 ) 1-12  is optionally replaced with heteroaryl, aryl, CONH, and \u2014O\u2014; and \n R 13  is selected from the group consisting of H, NO 2 , N 3 , alkyne, protecting group, halo and radioisotope; \n or\n administering to a patient, a compound comprising Formula V: \n and pharmaceutically acceptable salts and isomers thereof, wherein:\n X 1  is CH or N; \n X 17  is selected from the group consisting of: N and CH; \n X 18  is selected from the group consisting of: (CH 2 ) 1-10  wherein at least one CH 2  of (CH 2 ) 1-10  is optionally replaced by NH, aryl, heteroaryl and wherein at least one H is optionally substituted with NO 2 ; and \n R 14  is selected from the group consisting of O and S; and \n R 15  is selected from the group consisting of N 3 , alkyne, protecting group, halo and radioisotope; \n or\n administering to a patient, a compound comprising Formula VI: \n and pharmaceutically acceptable salts and isomers thereof, wherein:\n X 1  is CH or N; \n X 19  is selected from the group consisting of: H, NO 2 , (CH 2 ) 1-10 \u2014R 16  wherein at least one CH 2  of (CH 2 ) 1-10  is optionally replaced by CONH, aryl, heteroaryl; \n X 20  is selected from the group consisting of: H, NO 2 , (CH 2 ) 1-10 \u2014R 16  wherein at least one CH 2  of (CH 2 ) 1-10  is optionally replaced by CONH, aryl, heteroaryl; \n X 21  is selected from the group consisting of (CH 2 ) 1-3  wherein at least one CH 2  of (CH 2 ) 1-3  is optionally replaced by heteroaryl, and \n R 16  is selected from the group consisting of N 3 , alkyne, protecting group, halo and radioisotope; \n or\n administering to a patient, a compound comprising Formula VII: \n and pharmaceutically acceptable salts and isomers thereof, wherein:\n X 1  is CH or N; \n X 2  is CH or N; \n X 22  is a protecting group; and \n X 23  is (CH 2 ) 1-10 \u2014NH 2  wherein at least one CH 2  of (CH 2 ) 1-10  is optionally replaced by at least one selected from the group consisting of S, O, NH, CONH, aryl, heteroaryl, cycloalkyl and heterocycloalkyl; \n or\n administering to a patient, a compound comprising Formula VIII: \n and pharmaceutically acceptable salts and isomers thereof, wherein:\n X 1  is CH or N; \n X 24  is selected from the group consisting of (CH 2 ) 1-6  wherein at least one CH 2  of (CH 2 ) 1-6  is optionally replaced by at least one selected from the group consisting of NH, O, S; \n X 25  is N or CH; \n X 26  is NH or CH 2 ; \n X 27  is selected from the group consisting of: H, NO 2 , (CH 2 ) 1-10 \u2014R 16  wherein at least one CH 2  of (CH 2 ) 1-10  is optionally replaced by O, CONH, aryl, heteroaryl; and \n R 16  is selected from the group consisting of N 3 , alkyne, protecting group, halo and radioisotope; \n scanning the patient using positron emission tomography or single photon emission computed tomography; and \n imaging a tissue in the patient.

Metadata:
- Claim Count in Document: 56.0
- Percentile: 93.0
- Lexical Diversity: 1.71429
- Patent Class: 548.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14917127', '12862955', '12099135', '14152864', '15492933']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.6995526017618674
- 35 USC 102 Novelty (BERT): 0.5999646970259712
- Combined Prediction Score: 0.6895938112882778
- Mean Citation Score: 364.583886
- Max Citation Score: 519.5915
- Similarity Product: 465.62814070999616

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