PATENT CLAIM ANALYSIS

Application Number: 15891585
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-08
Patent Classification: ["514", "248000"]

Abstract:
This invention is directed to compounds of formula (I): where r, q, R, R 2 , R 3 , R 4 , R 5a , R 5b , R 5c , R 6a , R 6b , R 6c , R 7 , R 8 , and R 9  are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A 4  hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

Claim (Index 1):
A compound having Formula (I): wherein: R is i) the group \u2003or\n ii) the group \n \u2003or\n iii) an optionally substituted heteroaryl; \n n 1 , n 2 , and n 3  are each independently 0 to 2; \n r is 0 to 4; q is 0 to 2; R 1a , R 1b , R 1c , R 1d  and R 1e  are each independently hydrogen, \u2014R 13 \u2014OR 10 , \u2014R 13 \u2014C(\u2550O)OR 10 , \u2014R 13 \u2014C(\u2550O)R 10 , alkyl, halo, haloalkyl, cyano, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted heterocyclyl, or optionally substituted heterocyclylalkyl; R 1v , R 1w , R 1x , R 1y  and R 1z  are each independently hydrogen or fluoro; R 2  is hydrogen, alkyl, haloalkyl, haloalkenyl, haloalkynyl, hydroxyalkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted heterocyclyl, or optionally substituted heterocyclyalkyl; or R 2  and R 7 , together with the nitrogens to which they are attached, form an optionally substituted 5- to 7-membered N-heterocyclyl; or R 2  and R 7 , together with the nitrogens to which they are attached and one of R 5a , R 5b  and R 5c , form an optionally substituted 6- to 10-membered bridged N-heterocyclyl; or R 2  and R 5a , together with the nitrogen and carbon to which they are attached, form an optionally substituted 5- to 7-membered N-heterocyclyl or an optionally substituted 6- to 10-membered bridged N-heterocyclyl; or R 2  and R 5a , together with the nitrogen and carbon to which they are attached, form an optionally substituted 5- to 7-membered N-heterocyclyl; or R 2  and R 8 , together with the nitrogen and carbon to which they are attached, form an optionally substituted N-heterocyclyl or an optionally substituted N-heteroaryl; R 3  is a direct bond, \u2014O\u2014, \u2014R 12 \u2014O\u2014, \u2014O\u2014R 12 \u2014, \u2014O\u2014R 12 \u2014O\u2014, an optionally substituted straight or branched alkylene chain, an optionally substituted straight or branched alkenylene chain, or an optionally substituted straight or branched alkynylene chain; R 4  is a direct bond, \u2014O\u2014R 12a \u2014, an optionally substituted straight or branched alkylene chain, an optionally substituted straight or branched alkenylene chain, or an optionally substituted straight or branched alkynylene chain; each R 5a , R 5b , R 5c , R 6a , R 6b  and R 6c  are each independently hydrogen, alkyl, haloalkyl or hydroxyalkyl; or any one of R 5a  and R 6a  together, R 5b  and R 6b  together, and R 5c  and R 6c  together can be an oxo group; or R 5a  and R 5b , together with the carbons to which they are attached, form an optionally substituted 3- to 7-membered cycloalkyl; or R 5a  and R 5c , together with the carbons to which they are attached, form an optionally substituted 4- to 7-membered cycloalkyl; or R 5b  and R 6b , together with the carbon to which they are attached, form an optionally substituted 3- to 7-membered cycloalkyl; R 7  is hydrogen, \u2014R 13 \u2014OR 10 , \u2014R 13 \u2014C(\u2550O)R 10 , \u2014R 13 \u2014C(\u2550O)OR 10 , \u2014R 13 \u2014C(\u2550O)\u2014R 13 \u2014N(R 10 )R 11 , \u2014R 13 \u2014N(R 10 )C(\u2550O)N(R 10 )R 11 , alkyl, haloalkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroarylalkyl, or optionally substituted heterocyclylalkyl; or R 7  and R 5a , together with the nitrogen and carbon to which they are attached, form an optionally substituted 5- to 7-membered N-heterocyclyl; or R 7  and R 5a , together with the nitrogen and carbon to which they are attached, form an optionally substituted 5- to 7-membered N-heterocyclyl and R 2  and R 5c , together with the nitrogen and carbon to which are they are attached, form an optionally substituted 5- to 7-membered N-heterocyclyl; or R 7  and R 5a , together with the nitrogen and carbon to which they are attached, form an optionally substituted 5- to 7-membered N-heterocyclyl; or R 7  and R 5c , together with the nitrogen and carbon to which they are attached, form an optionally substituted 5- to 7-membered N-heterocyclyl or an optionally substituted 6- to 10-membered bridged N-heterocyclyl; R 8  is hydrogen, alkyl, haloalkyl, haloalkenyl, haloalkynyl, hydroxyalkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted heterocyclyl, optionally substituted heterocyclylalkyl, \u2014R 13 \u2014OR 10 , \u2014R 13 \u2014O\u2014R 14 \u2014C(\u2550O)OR 10 , \u2014R 13 \u2014C(\u2550O)R 10 , \u2014R 13 \u2014C(\u2550O)OR 10 , \u2014R 13 \u2014C(\u2550O)\u2014R 14 \u2014C(\u2550O)OR 10 , \u2014R 13 \u2014C(\u2550O)\u2014R 13 \u2014N(R 10 )R u , \u2014R 13 \u2014C(\u2550O)\u2014R 14 \u2014S(\u2550O) t N(R 10 )R 11  (where t is 1 or 2), or \u2014R 14 \u2014S(\u2550O) p R 10  (where p is 0, 1 or 2); or R 8  is aralkyl optionally substituted with one or more substituents selected from the group consisting of halo, nitro, cyano, optionally substituted heteroaryl, hydroxyiminoalkyl, \u2014R 13 \u2014OR 10 , \u2014R 13 \u2014C(\u2550O)R 10 , \u2014R 13 \u2014C(\u2550O)OR 10 , \u2014R 13 \u2014C(\u2550O)\u2014R 13 \u2014N(R 10 )R 11 , \u2014R 13 \u2014C(\u2550O)N(R 10 )\u2014R 14 \u2014N(R 10 )R 11 , \u2014R 13 \u2014S(\u2550O) t N(R 10 )R 11  (where t is 1 or 2), \u2014R 13 \u2014N(R 10 )R u , \u2014R 13 \u2014N(R 10 )C(\u2550O)R 10 , \u2014R 13 \u2014N(R 10 )C(\u2550O)\u2014R 13 \u2014N(R 10 )R 11 , \u2014R 13 \u2014N(R 10 )\u2014R 13 \u2014C(\u2550O)OR 10 , \u2014R 13 \u2014N(R 10 )C(\u2550O)\u2014R 14 \u2014S(\u2550O) t N(R 10 )R 11  (where t is 1 or 2), \u2014R 13 \u2014N(R 10 )C(\u2550O)\u2014R 13 \u2014N(R 10 )C(\u2550O)R 10 , \u2014R 13 \u2014N(R 10 )C(\u2550O)\u2014R 13 \u2014N(R 10 )\u2014R 14 \u2014N(R 10 )R 11 , \u2014R 13 \u2014N(R 10 )S(\u2550O) t N(R 10 )R 11  (where t is 1 or 2), and \u2014R 13 \u2014O\u2014R 14 \u2014C(\u2550O)OR 10 ; each R 9  is independently \u2014O\u2014R 10 , alkyl, hydroxyalkyl, halo, haloalkyl, aryl or aralkyl; each R 10  and R 11  is independently hydrogen, alkyl, haloalkyl, hydroxyalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted heterocyclyl, or optionally substituted heterocyclylalkyl; or R 10  and R 11 , together with the nitrogen to which they are attached, form an optionally substituted N-heterocyclyl or an optionally substituted N-heteroaryl; R 12  is an optionally substituted straight or branched alkylene chain, an optionally substituted straight or branched alkenylene chain, or an optionally substituted straight or branched alkynylene chain; R 12a  is an optionally substituted straight or branched alkylene chain, an optionally substituted straight or branched alkenylene chain, or an optionally substituted straight or branched alkynylene chain; each R 13  is independently a direct bond, an optionally substituted straight or branched alkylene chain, an optionally substituted straight or branched alkenylene chain, or an optionally substituted straight or branched alkynylene chain; and each R 14  is independently an optionally substituted straight or branched alkylene chain, an optionally substituted straight or branched alkenylene chain, or an optionally substituted straight or branched alkynylene chain; as a single stereoisomer or as a mixture of stereoisomers; or a pharmaceutically acceptable salt, solvate, polymorph, clathrate, ammonium ion, N-oxide or prodrug thereof.

Metadata:
- Claim Count in Document: 76.0
- Percentile: 88.0
- Lexical Diversity: 1.75714
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14313672', '11644244', '14849810', '12771659', '15840097']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7988741845067256
- 35 USC 102 Novelty (BERT): 0.5961574799809007
- Combined Prediction Score: 0.7786025140541432
- Mean Citation Score: 393.50533800000005
- Max Citation Score: 528.1824
- Similarity Product: 436.0010084489823

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

Dataset: test