PATENT CLAIM ANALYSIS

Application Number: 15908571
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-07
Patent Classification: ["562", "466000"]

Abstract:
Pentacyclic triterpene weight loss agents are provided herein. Also provided are pharmaceutical formulations containing a therapeutically effective amount of one or more of the weight loss agents, or pharmaceutically acceptable salts or prodrugs thereof, in combination with one or more pharmaceutically acceptable excipients. The pharmaceutical formulations can be administered to a pre-obese, obese, or morbidly obese patient to induce weight loss, reduce body fat, reduce food intake, improve glucose homeostasis, prevent obesity, or a combination thereof. The weight loss agents can also be co-administered with leptin or a leptin analog.

Claim (Index 2):
The formulation of  claim 1 , wherein the compound is defined by Formula II wherein\n the dotted lines between A and C 2 , C 1  and C 2 , C 1  and C 7 , C 7  and C 5 , C 5  and C 6 , and C 8  and C 9  indicate that a single or double bond may be present, as valence permits; \n X is \u2014O\u2014, \u2014NR 7 \u2014, \u2014S\u2014, \u2014SO\u2014, or \u2014SO 2 \u2014; \n R 1  is hydrogen, or an alkyl, cycloalkyl, heterocycloalkyl, alkylaryl, alkenyl, alkynyl, aryl, or heteroaryl group, optionally substituted with between one and five substituents individually selected from alkyl, cyclopropyl, cyclobutyl ether, amine, halogen, hydroxyl, ether, nitrile, CF 3 , ester, amide, urea, carbamate, thioether, and aryl; \n R 2  is hydrogen; hydroxy (\u2014OH), thiol (\u2014SH), ether (e.g., \u2014OR 7 ), thioether (e.g., \u2014SR 7 ), primary amine (\u2014NH 2 ), secondary amine (e.g., \u2014NHR 7 ), tertiary amine (e.g., \u2014NR 7 R 7 ), primary amide (e.g., \u2014CONH 2 ), secondary amide (e.g., \n \u2014NHCOR 7 ), tertiary amide (e.g., \u2014NR 7 COR 7 ), secondary carbamate (e.g., \u2014OCONHR 7 ; \u2014NHCOOR 7 ), tertiary carbamate (e.g., \u2014OCONR 7 R 7 ; \u2014NR 7 COOR 7 ), urea (e.g., \u2014NHCONHR 7 ; \u2014NR 7 CONHR 7 ; \u2014NHCONR 7 R 7 , \u2014NR 7 CONR 7 R 7 ), sulfinyl group (e.g., \u2014SOR 7 ), sulfonyl group (e.g., \u2014SOOR 7 ) sulfino group, halogen, nitrile, or CF 3 ; or an alkyl, cycloalkyl, heterocycloalkyl, alkylaryl, alkenyl, alkynyl, aryl, or heteroaryl group optionally substituted with between one and five substituents individually selected from alkyl, cyclopropyl, cyclobutyl ether, amine, halogen, hydroxyl, ether, nitrile, CF 3 , ester, amide, urea, carbamate, thioether, carboxylic acid, and aryl; A is nitrogen or oxygen when a double bond is present between A and C 2 , or oxygen when a single bond is present between A and C 2 ;\n R 3  is hydrogen, a carbonyl group (e.g., \u2014COR 7 ), or an alkyl, cycloalkyl, heterocycloalkyl, alkylaryl, alkenyl, alkynyl, aryl, or heteroaryl group optionally substituted with between one and five substituents individually selected from alkyl, cyclopropyl, cyclobutyl ether, amine, halogen, hydroxyl, ether, nitrile, CF 3 , ester, amide, urea, carbamate, thioether, carboxylic acid, and aryl; \n R 4  is absent when A is oxygen and a double bond is present between A and C 2 , a hydroxy (\u2014OH) group when A is nitrogen and a double bond is present between A and C 2 , or is hydrogen, a carbonyl group (e.g., \u2014COR 7 ), or an alkyl, cycloalkyl, heterocycloalkyl, alkylaryl, alkenyl, alkynyl, aryl, or heteroaryl group optionally substituted with between one and five substituents individually selected from alkyl, cyclopropyl, cyclobutyl ether, amine, halogen, hydroxyl, ether, nitrile, CF 3 , ester, amide, urea, carbamate, thioether, carboxylic acid, and aryl when A is oxygen and a single bond is present between A and C 2 ; or \n A is oxygen, a single bond is present between A and C 2 , and R 3  and R 4 , taken together with A, C 2 , C 3 , and O 1 , form a 5- to 7-membered ring optionally substituted with between one and four substituents individually selected from alkyl, cyclopropyl, cyclobutyl ether, amine, halogen, hydroxyl, ether, nitrile, CF 3 , ester, amide, urea, carbamate, thioether, and carboxylic acid; \n R 5  is hydrogen; hydroxy (\u2014OH), thiol (\u2014SH), ether (e.g., \u2014OR 7 ), thioether (e.g., \u2014SR 7 ), primary amine (\u2014NH 2 ), secondary amine (e.g., \u2014NHR 7 ), tertiary amine (e.g., \u2014NR 7 R 7 ), primary amide (e.g., \u2014CONH 2 ), secondary amide (e.g., \n \u2014NHCOR 7 ), tertiary amide (e.g., \u2014NR 7 COR 7 ), secondary carbamate (e.g., \u2014OCONHR 7 ; \u2014NHCOOR 7 ), tertiary carbamate (e.g., \u2014OCONR 7 R 7 ; \u2014NR 7 COOR 7 ), urea (e.g., \u2014NHCONHR 7 ; \u2014NR 7 CONHR 7 ; \u2014NHCONR 7 R 7 , \u2014NR 7 CONR 7 R 7 ), sulfinyl group (e.g., \u2014SOR 7 ), sulfonyl group (e.g., \u2014SOOR 7 ) sulfino group, halogen, nitrile, or CF 3 ; or an alkyl, cycloalkyl, heterocycloalkyl, alkylaryl, alkenyl, alkynyl, aryl, or heteroaryl group optionally substituted with between one and five substituents individually selected from alkyl, cyclopropyl, cyclobutyl ether, amine, halogen, hydroxyl, ether, nitrile, CF 3 , ester, amide, urea, carbamate, thioether, carboxylic acid, and aryl;\n R 6  is absent when a double bond is present between C 8  and C 9 , is hydrogen; hydroxy (\u2014OH), thiol (\u2014SH), ether (e.g., \u2014OR 7 ), thioether (e.g., \u2014SR 7 ), primary amine (\u2014NH 2 ), secondary amine (e.g., \u2014NHR 7 ), tertiary amine (e.g., \u2014NR 7 R 7 ), primary amide (e.g., \u2014CONH 2 ), secondary amide (e.g., \n \u2014NHCOR 7 ), tertiary amide (e.g., \u2014NR 7 COR 7 ), secondary carbamate (e.g., \u2014OCONHR 7 ; \u2014NHCOOR 7 ), tertiary carbamate (e.g., \u2014OCONR 7 R 7 ; \u2014NR 7 COOR 7 ), urea (e.g., \u2014NHCONHR 7 ; \u2014NR 7 CONHR 7 ; \u2014NHCONR 7 R 7 , \u2014NR 7 CONR 7 R 7 ), sulfinyl group (e.g., \u2014SOR 7 ), sulfonyl group (e.g., \u2014SOOR 7 ) sulfino group, halogen, nitrile, or CF 3 ; or an alkyl, cycloalkyl, heterocycloalkyl, alkylaryl, alkenyl, alkynyl, aryl, or heteroaryl group optionally substituted with between one and five substituents individually selected from alkyl, cyclopropyl, cyclobutyl ether, amine, halogen, hydroxyl, ether, nitrile, CF 3 , ester, amide, urea, carbamate, thioether, carboxylic acid, and aryl when a single bond is present between C 8  and C 9 ; or\n a single bond is present between C 8  and C 9 , and R 5  and R 6 , taken together with C 8  and C 9 , form a cyclopropyl or epoxide ring; and \n R 7 , when present, is individually for each occurrence an alkyl, cycloalkyl, heterocycloalkyl, alkylaryl, alkenyl, alkynyl, aryl, or heteroaryl group, optionally substituted with between one and five substituents individually selected from alkyl, cyclopropyl, cyclobutyl ether, amine, halogen, hydroxyl, ether, nitrile, CF 3 , ester, amide, urea, carbamate, thioether, carboxylic acid, and aryl; \n or a pharmaceutically acceptable salt or prodrug thereof.

Metadata:
- Claim Count in Document: 31.0
- Percentile: 88.0
- Lexical Diversity: 1.83929
- Patent Class: 562.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['14431412', '15644247', '15771077', '14413137', '13596211']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7853297429859772
- 35 USC 102 Novelty (BERT): 0.6155662435991833
- Combined Prediction Score: 0.7683533930472979
- Mean Citation Score: 466.072956
- Max Citation Score: 639.6395
- Similarity Product: 468.23536309996246

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

Dataset: test