PATENT CLAIM ANALYSIS

Application Number: 16045427
Application Type: Utility
Filing Date: 2018-07
Publication Date: 2019-01
Patent Classification: ["544", "113000"]

Abstract:
The invention relates to a method of manufacturing triazine, pyrimidine and pyridine derivatives of formula (I) wherein U, V, W and Z are nitrogen or carbon atoms, whereby at least one of U, V and W is nitrogen, and the other substituents are defined as in the specification, by condensing a corresponding halo-triazine, pyrimidine or pyridine in a type of Suzuki coupling with a pyridyl- or pyrimidinyl-borane, wherein the amino function is protected as a formamidine. The invention further relates to suitable intermediates and methods of manufacturing of such intermediates. Furthermore the invention relates to pure 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine in solid form.

Claim (Index 10):
A method of manufacture of an acid addition salt of formula (Ia) or a stereomer or tautomer, wherein, U is CR U  or N, wherein R U  is selected from the group consisting of hydrogen, cyano, halogen, methyl and trifluoromethyl; V is CR V  or N, wherein R V  is selected from the group consisting of hydrogen, cyano, halogen, methyl and trifluoromethyl; W is CR W  or N, wherein R W  is selected from the group consisting of hydrogen, cyano, halogen, methyl and trifluoromethyl; provided that at least one of U, V and W is N; Z is CR Z  or N, wherein R Z  is selected from the group consisting of hydrogen, cyano, halogen, methyl and trifluoromethyl; R 1  is selected from the group consisting of hydrogen, halogen and \u2014N(R T )R S , wherein R T  and R S  are hydrogen or C 1 -C 7 -alkyl, or wherein R T  and R S  together with the nitrogen to which they are attached form a C 3 -C 8  mono- or bicyclic heterocyclic ring optionally containing one or more additional ring atoms selected from N, O or S, wherein said heterocyclic ring is optionally substituted with one or more groups independently selected from C 1 -C 7 -alkyl or C 3 -C 7 -cycloalkyl; R 2  is selected from the group consisting of hydrogen, cyano, halogen, methyl and trifluoromethyl; R 3  is hydrogen or halogen; and HX is a protonic acid; comprising treating a free base of formula (I) wherein said free base of formula (I) is manufactured according to the method of  claim 1 ; and wherein the substituents are defined as indicated for formula (Ia), with protonic acid HX, optionally in a suitable solvent, and the resulting acid additional salt is purified by precipitation from a solvent or recrystallization.

Metadata:
- Claim Count in Document: 8.0
- Percentile: 95.0
- Lexical Diversity: 1.76812
- Patent Class: 544.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15304595', '14620721', '12936451', '13617035', '12016897']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7349143117358511
- 35 USC 102 Novelty (BERT): 0.5263745594445092
- Combined Prediction Score: 0.7140603365067169
- Mean Citation Score: 282.585952
- Max Citation Score: 348.9181
- Similarity Product: 338.9265511122168

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

Dataset: test