PATENT CLAIM ANALYSIS

Application Number: 16320723
Application Type: Utility
Filing Date: 2019-01
Publication Date: 2019-05
Patent Classification: ["514", "263200"]

Abstract:
The invention relates to a xanthine derivative defined by chemical formula I or a salt thereof, its use as a medicament, especially for use in the treatment of serotonin-related diseases or disorders, and a pharmaceutical preparation comprising the xanthine derivative. The novel xanthine compounds are capable of inhibiting tryptophan hydroxylases (TPH) involved in the biosynthesis of serotonin and are effective in influencing the serotonin level in the body.

Claim (Index 1):
Xanthine derivative defined by chemical Formula I or a salt thereof: wherein R 1  and R 2  are each an optionally substituted group independently selected from hydrogen (\u2014H), (C1-C10)-alkyl, (C2-C10)-alkenyl, (C2-C10)-alkynyl, (C5-C14)-aryl, (C5-C14)-heteroaryl, (C6-C15)-alkyl-arylene, (C6-C15)-alkyl-heteroarylene, (C6-C15)-alkenyl-arylene, (C6-C15)-alkenyl-heteroarylene, (C6-C15)-alkynyl-arylene, (C6-C15)-alkynyl-heteroarylene, (C6-C15)-aryl-alkylene, (C6-C15)-heteroaryl-alkylene, (C6-C15)-aryl-alkenylene, (C6-C15)-heteroaryl-alkenylene, (C6-C15)-aryl-alkynylene and (C6-C15)-heteroaryl-alkynylene, wherein the alkyl, alkenyl, alkynyl, alkylene, alkenylene, and alkynylene groups optionally comprise one or more bivalent groups substituting a carbon moiety in their hydrocarbon chain and selected from \u2014O\u2014, \u2014S\u2014, \u2014S(O)\u2014, \u2014SO 2 \u2014, \u2014N\u2550, \u2014N(R)\u2014, \u2014C(O)\u2014, \u2014C(O)O\u2014, \u2014OC(O)\u2014, \u2014C(O)N(R)\u2014, \u2014N(R)C(O)\u2014, \u2014OC(O)N(R)\u2014, \u2014N(R)C(O)O\u2014, \u2014N(R)C(O)N(R)\u2014, (C3-C12)-heterocyclic alkylene and (C3-C12)-heterocyclic alkenylene;\n R 3  is a group selected from hydrogen (\u2014H), fluoro (\u2014F), bromo (\u2014Br), chloro (\u2014Cl), hydroxyl (\u2014OH), carbonyl (\u2014C(O)R), carboxyl (\u2014C(O)OH), carboxy ester (\u2014CO 2 R), alkoxy \n (\u2014OR), aldehyde (\u2014C(O)H), trihalide methyl ester (\u2014OCX 3 ), primary, secondary and tertiary amine (\u2014NR(R\u2032)), amide (\u2014N(R)\u2014C(O)\u2014R), imide (\u2014C(O)\u2014N(R)\u2014C(O)\u2014R\u2032), carbamate (\u2014N(R)\u2014C(O)\u2014OR\u2032), carboxamide (\u2014C(O)N(R)R\u2032), carbimide (\u2014N(R)\u2014C(O)\u2014N(R\u2032)R\u2033), primary and secondary ketimine (\u2014(R)\u2550NR\u2032), secondary ketimine (\u2014(R)\u2550NH), nitrile (\u2014CN), isonitrile (\u2014NC), nitroxy (\u2014ONO), nitro (\u2014NO 2 ), nitrate (\u2014ONO 2 ), nitroso (\u2014NO), cyanate (\u2014OCN), isocyanate (\u2014NCO), sulfhydryl (\u2014SH), sulfide (\u2014SR), sulfurtrihalide (\u2014SX 3 ), sulfurpentahalide (\u2014SX 5 ), sulfinyl (\u2014S(O)R), sulfonyl (\u2014SO 2 R), sulfino (\u2014SO 2 H), and sulfo (\u2014SO 3 H), and an optionally substituted and optionally linked group selected from (C1-C10)-alkyl, (C2-C10)-alkenyl, (C2-C10)-alkynyl, (C5-C14)-aryl, (C5-C14)-heteroaryl, (C6-C15)-alkyl-arylene, (C6-C15)-alkyl-heteroarylene, (C6-C15)-alkenyl-arylene, (C6-C15)-alkenyl-heteroarylene, (C6-C15)-alkynyl-arylene, (C6-C15)-alkynyl-heteroarylene, (C6-C15)-aryl-alkylene, (C6-C15)-heteroaryl-alkylene, (C6-C15)-aryl-alkenylene, (C6-C15)-heteroaryl-alkenylene, (C6-C15)-aryl-alkynylene and (C6-C15)-heteroaryl-alkynylene, wherein the alkyl, alkenyl, alkynyl, alkylene, alkenylene and alkynylene groups optionally comprise one or more bivalent groups substituting a carbon moiety in their hydrocarbon chain and selected from \u2014O\u2014, \u2014S\u2014, \u2014S(O)\u2014, \u2014SO 2 \u2014, \u2014N\u2550, \u2014N(R)\u2014, \u2014C(O)\u2014, \u2014C(O)O\u2014, \u2014OC(O)\u2014, \u2014C(O)N(R)\u2014, \u2014N(R)C(O)\u2014, \u2014OC(O)N(R)\u2014, \u2014N(R)C(O)O\u2014, \u2014N(R)C(O)N(R)\u2014, (C3-C12)-heterocyclic alkylene or (C3-C12)-heterocyclic alkenylene;\n Q is selected from carbon, nitrogen, oxygen, \n sulfur, \u2014*CH 2 \u2014CH(R x )\u2014, \u2014*CH\u2550C(R x )\u2014, \u2014*CH 2 \u2014O\u2014, \u2014*CH 2 \u2014N(R x )\u2014, wherein R x  represents hydrogen, methyl, ethyl, cyclopropyl, \u2014CH 2 -cyclopropyl, or halogen, and wherein the carbon marked with an asterisk is covalently linked to the imidazole;\n Z is selected from carbon, nitrogen, oxygen and sulfur; \n the ring member A is an saturated, unsaturated or aromatic ring; and \n wherein in the aforementioned definitions R, R\u2032 and R\u2033 independently mean hydrogen, \n (C1-C3)-alkyl or (C2-C3)-alkenyl.

Metadata:
- Claim Count in Document: 29.0
- Percentile: 99.0
- Lexical Diversity: 1.47059
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['15552556', '13389993', '12474838', '09738376', '11542166']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8018462858309706
- 35 USC 102 Novelty (BERT): 0.6345724055289645
- Combined Prediction Score: 0.78511889780077
- Mean Citation Score: 385.525688
- Max Citation Score: 580.3537
- Similarity Product: 569.6737312614978

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