PATENT CLAIM ANALYSIS

Application Number: 16416418
Application Type: Utility
Filing Date: 2019-05
Publication Date: 2019-09
Patent Classification: ["514", "243000"]

Abstract:
Pyrazolopyrimidone derivatives and methods of use thereof are described. Specifically, pharmaceutical uses of pyrazolopyrimidone derivatives represented by the general formula (II) and pharmaceutically acceptable salts thereof are described, wherein the definitions of substituents in the general formula (II) are the same as the definitions in the specification. The pyrazolopyrimidone derivatives are useful as gonadotropin releasing hormone (GnRH) antagonists, such as for therapeutic agents for endometriosis.

Claim (Index 1):
A method for treating a gonadal hormone-related disease, or for treating or preventing sex hormone-dependent cancers, bone metastasis of a sex hormone-dependent cancer, prostatic hyperplasia, uterine leiomyoma, endometriosis, uterine fibroids, precocious puberty, amenorrhea, premenstrual syndrome, dysmenorrhea, multilocular ovary syndrome, polycystic ovary syndrome, acne, alopecia, Alzheimer's disease, infertility, irritable bowel syndrome, benign or malignant tumors which are hormone-independent and LH-RH sensitive, or flush; or for regulating reproduction, contraception or stimulation ovulation; or for the prevention of postoperative recurrence of a sex hormone-dependent cancer in a subject in need thereof, wherein the sex hormone-dependent cancer is selected from the group consisting of prostate cancer, uterine cancer, breast cancer, and pituitary cancer, the method comprising administering to the subject a pharmaceutical composition comprising an effective amount of a compound of formula (II), or a tautomer, mesomer, racemate, enantiomer, or diastereomer thereof, or mixture thereof, or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable carriers, diluents, or excipients: wherein\n R 1  is selected from the group consisting of alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, and \u2014OR 6 , wherein the alkyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl are each independently and optionally further substituted with one or more groups selected from the group consisting of halogen, cyano, nitro, alkyl, haloalkyl, hydroxyalkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, \u2014OR 6 , \u2014C(O)OR 6 , \u2014OC(O)R 6 , \u2014NHS(O) m R 6 , \u2014C(O)R 6 , \u2014NHC(O)R 6 , \u2014NHC(O)OR 6 , \u2014NR 7 R 8 , \u2014OC(O)NR 7 R 8 , \u2014C(O)NR 7 R 8 , \u2014NHC(O)NHR 6 , and \u2014NHC(O)NHOR 6 ; \n R 2  is alkyl, wherein the alkyl is further substituted with one or more groups selected from the group consisting of aryl and heteroaryl, wherein the aryl and heteroaryl are each independently and optionally further substituted with one or more groups selected from the group consisting of halogen, alkyl, haloalkyl, cyano, nitro, \u2014C(O)OR 6 , \u2014C(O)NR 7 R 8 , \u2014OC(O)NR 7 R 8 , \u2014OR 6 , \u2014NHS(O) m R 6 , \u2014NHC(O)R 6 , and \u2014NR 7 R 8 ; \n R 3  is selected from the group consisting of aryl and heteroaryl, wherein the aryl and heteroaryl are each independently and optionally further substituted with one or more groups selected from the group consisting of halogen, alkyl, haloalkyl, \u2014OR 6 , \u2014C(O)OR 6 , \u2014OC(O)R 6 , \u2014C(O)R 6 , \u2014NR 7 R 8 , \u2014OC(O)NR 7 R 8 , \u2014C(O)NR 7 R 8 , \u2014NHS(O) m R 6 , \u2014NHC(O)R 6 , \u2014NHC(O)OR 6 , \u2014NHC(O)NHR 6 , and \u2014NHC(O)NHOR 6 ; \n R 4  is alkyl; \n R 5  is selected from the group consisting of hydrogen, cycloalkyl, heterocyclyl, aryl, heteroaryl, \u2014OR 5 , \u2014NR 7 R 8 , and \u2014NR 7 S(O) m R 6 , wherein the alkyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl are each independently and optionally further substituted with one or more groups selected from the group consisting of halogen, oxo, alkyl, haloalkyl, hydroxyalkyl, \u2014OR 6 , \u2014C(O)OR 6 , \u2014OC(O)R 6 , \u2014NR 7 S(O) m R 6 , \u2014S(O) m R 6 , \u2014C(O)R 6 , and \u2014NHC(O)R 6 ; \n R 6  is selected from the group consisting of hydrogen, alkyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl are each independently and optionally further substituted with one or more groups selected from the group consisting of alkyl, halogen, hydroxy, alkoxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, carboxylic acid, and carboxylic ester; \n R 7  and R 8  are each independently selected from the group consisting of hydrogen, alkyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl are each independently and optionally further substituted with one or more groups selected from the group consisting of alkyl, halogen, hydroxy, alkoxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, carboxylic acid, and carboxylic ester; \n or, R 7  and R 8  are taken together with the attached N atom to form a heterocyclyl, wherein the heterocyclyl contains one or more heteroatoms selected from the group consisting of N, O, and S(O) m , and the heterocyclyl is optionally further substituted with one or more groups selected from the group consisting of alkyl, halogen, hydroxyl, alkoxyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, carboxylic acid, and carboxylic ester;\n m is 0, 1, or 2; \n n is 1, 2, 3, or 4; and \n p is 0, 1, or 2.

Metadata:
- Claim Count in Document: 11.0
- Percentile: 100.0
- Lexical Diversity: 1.71111
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15031410', '15969098', '15030125', '15303704', '16012958']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8427048799207153
- 35 USC 102 Novelty (BERT): 0.6162983443478544
- Combined Prediction Score: 0.8200642263634292
- Mean Citation Score: 564.359462
- Max Citation Score: 711.75287
- Similarity Product: 485.68861080378304

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

Dataset: test