PATENT CLAIM ANALYSIS

Application Number: 15861399
Application Type: Utility
Filing Date: 2018-01
Publication Date: 2018-05
Patent Classification: ["514", "233200"]

Abstract:
The present invention relates to novel fused Imidazobenzothiazole derivatives, their pharmaceutically acceptable salts, and their isomers, steroisomers, atropisomers, conformers, tautomers, polymorphs, hydrates, solvates and N-oxide. The present invention also encompasses pharmaceutically acceptable compositions of said compounds and process for preparing novel compounds. The invention further relates to the use of the above-mentioned compounds for the preparation of medicament for use as pharmaceuticals.

Claim (Index 9):
A method of treating allergic and non-allergic airway diseases comprising administering to a mammal in need thereof a pharmaceutical composition comprising a therapeutically effective amount of a compound of formula (I) their pharmaceutically acceptable salts and their stereoisomers, atropisomers, conformers, tautomers, polymorphs, hydrates, solvates and N-oxide;\n wherein, \n X is selected from O, S(O) n , NH and N(C 1 -C 3 )alkyl; \n R 1  and R 2  are independently selected from hydrogen, A, CHO, C\u2550N\u2014OH, C\u2550N\u2014O\u2014(C 1 -C 6 )alkyl, CH 2 OH, CH 2 R 3 , N(R 5 )CO 2 R 4 , CH 2 -halogen, NR 5 R 6 , N(R 5 )C(O)-A, N(R 5 )S(O) m -A, N(R 5 )C(O)N(R 5 )-A, N(R 5 )C(S)N(R 5 )-A, C(O)NR 5 R 6 , CO 2 R 7 , C(O)-A, CH(OH)-A C(CH 3 )\u2550N\u2014OH, C(CH 3 )\u2550N\u2014O\u2014(C 1 -C 6 )alkyl, C(O)CH 2 -halogen and C(O)CH 2 R 3 ; \n R is independently selected from hydrogen, (C 1 -C 6 )alkyl, (C 3 -C 10 )carbocycle, CN, CHO, C(O)-A, C(CH 3 )\u2550N\u2014OH, C(CH 3 )\u2550N\u2014O\u2014(C 1 -C 6 )alkyl, C(O)CH 2 -halogen, C(O)CH 2 R 3 , NR 5 R 6 , N(R 5 )C(O)-A, N(R 5 )S(O) m -A, N(R 5 )C(O)O-A, N(R 5 )C(O)N(R 5 )-A, N(R 5 )C(S)N(R 5 )-A, CO 2 R 7 , C(O)N(R 5 )-A, (C 1 -C 6 )alkyl-OR 7 , (C 1 -C 6 )alkyl-halogen, (C 1 -C 6 )alkyl-N 3 , (C 1 -C 6 )alkyl-NR 5 R 6 , (C 1 -C 6 )alkyl-N(R 5 )C(O)-A, (C 1 -C 6 )alkyl-N(R 5 )S(O) m -A, (C 1 -C 6 )alkyl-N(R 5 )C(O)O-A, (C 1 -C 6 )alkyl-N(R 5 )C(O)N(R 5 )-A, (C 1 -C 6 )alkyl-N(R 5 )C(S)N(R 5 )-A and (C 1 -C 6 )alkyl-OC(O)N(R 5 )-A; \n A is independently selected from (C 1 -C 6 )alkyl, (C 3 -C 10 )carbocycle, aryl, heteroaryl and heterocyclic, the said (C 1 -C 6 )alkyl, (C 3 -C 10 )carbocycle, aryl, heteroaryl or heterocyclic may be optionally substituted with 1-3 substituents independently selected from halogen, (C 1 -C 6 )alkyl, (C 3 -C 10 )carbocycle, aryl, heteroaryl, heterocyclic, hydroxyl, CF 3 , OCF 3 , O(C 1 -C 6 )alkyl, O\u2014(C 3 -C 10 )carbocycle, NO 2 , C(O)\u2014(C 1 -C 6 )alkyl, C(O)CH 2 -halogen, NR 5 R 6 , COOH, C(O)N(R 5 )\u2014(C 1 -C 6 )alkyl, C(O)N(R 5 )\u2014(C 3 -C 10 )carbocycle, C(O)N(R 5 )-aryl, C(O)N(R 5 )-heteroaryl, C(O)N(R 5 )-heterocyclic, N(R 5 )S(O) m \u2014(C 1 -C 6 )alkyl, N(R 5 )S(O) m \u2014(C 3 -C 10 )carbocycle, N(R 5 )S(O) m -aryl, N(R 5 )S(O) m -heteroaryl, N(R 5 )S(O) m -heterocyclic, SH, S(O) n (C 1 -C 6 )alkyl, S(O) m N(R 5 )\u2014(C 1 -C 6 )alkyl, S(O) m N(R 5 )\u2014(C 3 -C 10 )carbocycle, S(O) m N(R 5 )-aryl, S(O) m N(R 5 )-heteroaryl, S(O) m N(R 5 )-heterocyclic, CN, CHO, (C 1 -C 6 )alkyl-OH, (C 1 -C 6 )alkyl-O(C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl-O(C 3 -C 10 )carbocycle, (C 1 -C 6 )alkyl-O-aryl, (C 1 -C 6 )alkyl-O-heteroaryl, (C 1 -C 6 )alkyl-O-heterocyclic, (C 1 -C 6 )alkyl-halogen and (C 1 -C 6 )alkyl-NR 5 R 6  \n wherein each aryl or heteroaryl may be further optionally substituted with 1-3 substituents independently selected from halogen, (C 1 -C 6 )alkyl, (C 3 -C 10 )carbocycle, aryl, heteroaryl, heterocyclic, hydroxyl, CF 3 , OCF 3 , O(C 1 -C 6 )alkyl, O\u2014(C 3 -C 10 )carbocycle, NO 2 , C(O)\u2014(C 1 -C 6 )alkyl, C(O)CH 2 -halogen, NR 5 R 6 , COOH, C(O)N(R 5 )\u2014(C 1 -C 6 )alkyl, C(O)N(R 5 )\u2014(C 3 -C 10 )carbocycle, C(O)N(R 5 )-aryl, C(O)N(R 5 )-heteroaryl, C(O)N(R 5 )-heterocyclic, N(R 5 )S(O) m \u2014(C 1 -C 6 )alkyl, N(R 5 )S(O) m \u2014(C 3 -C 10 )carbocycle, N(R 5 )S(O) m -aryl, N(R 5 )S(O) m -heteroaryl, N(R 5 )S(O) m -heterocyclic, SH, S(O) n (C 1 -C 6 )alkyl, S(O) m N(R 5 )\u2014(C 1 -C 6 )alkyl, S(O) m N(R 5 )\u2014(C 3 -C 10 )carbocycle, S(O) m N(R 5 )-aryl, S(O) m N(R 5 )-heteroaryl, S(O) m N(R 5 )-heterocyclic, CN, OSO 3 H, CHO, (C 1 -C 6 )alkyl-OH, (C 1 -C 6 )alkyl-O(C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl-O(C 3 -C 10 )carbocycle, (C 1 -C 6 )alkyl-O-aryl, (C 1 -C 6 )alkyl-O-heteroaryl, (C 1 -C 6 )alkyl-O-heterocyclic, (C 1 -C 6 )alkyl-halogen, (C 1 -C 6 )alkyl-NR 5 R 6  and \n R 3  is independently selected from O-A, NR 5 R 6 , S(O) n -A, S(O) n \u2014(C 1 -C 6 )alkyl-CO 2 (C 1 -C 6 )alkyl, S(O) n \u2014(C 1 -C 6 )alkyl-OH, S(O) n \u2014(C 1 -C 6 )alkyl-CO 2 H, N(R 5 )C(O)-A, N(R 5 )C(O)O-A, N(R 5 )C(O)N(R 5 )-A, N(R 5 )S(O) m -A, N(R 5 )C(O)-heterocyclic and N(R 5 )C(S)N(R 5 )-A; R 4  is hydrogen or A; R 5  and R 5 \u2032 are independently selected from hydrogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl-(C 3 -C 10 )carbocycle and (C 3 -C 10 )carbocycle; R 6  is independently selected from hydrogen, (C 1 -C 6 )alkyl-OH, (C 1 -C 6 )alkyl-NR 5 \u2032R 6 \u2032, CH(CH 2 OH)-aryl, CH(CH 2 OH) 2 , (C 1 -C 6 )alkyl-aryl, (C 1 -C 6 )alkyl-heterocyclic and (C 1 -C 6 )alkyl-heteroaryl; R 6 \u2032 is independently selected from hydrogen, (C 1 -C 6 )alkyl-OH, CH(CH 2 OH)-aryl, CH(CH 2 OH) 2 , (C 1 -C 6 )alkyl-aryl, (C 1 -C 6 )alkyl-heterocyclic and (C 1 -C 6 )alkyl-heteroaryl; or R 5  and R 6  or R 5 \u2032 and R 6 \u2032 together with the nitrogen to which they are attached may form a 3 to 8 membered monocyclic or 8 to 12 membered bicyclic heterocycle ring, which ring optionally contains an additional heteroatom selected from 0, S or N and the said ring is optionally substituted by one or more R 9  or R 10  substituent; the nitrogen of said ring may also form N-oxide; in bicyclic heterocyclic system, the rings can be attached to each other in a spiro or fused manner; R 7  is hydrogen or A; each R 8  is independently 1-2 substituents and each selected from hydrogen, halogen, A, CN, CHO, C(O)-A, C(O)CH 2 -halogen, C(O)CH 2 R 3 , hydroxyl, CF 3 , OCF 3 , NR 5 R 6 , N(R 5 )C(O)-A, N(R 5 )S(O) m -A, C(O)N(R 5 )-A, O\u2014(C 1 -C 6 )alkyl, O\u2014(C 3 -C 10 )carbocycle, S(O) n -A and S(O) m N(R 5 )-A, wherein R and R 8  are simultaneously not hydrogen; R 9  is independently selected from hydrogen, halogen, A, hydroxyl, CF 3 , OCF 3 , O(C 1 -C 6 )alkyl, O\u2014(C 3 -C 10 )carbocycle, NO 2 , C(O)-A, C(O)CH 2 -halogen, C(O)CH 2 R 3 , N(R 5 )C(O)O-A, N(R 5 )C(O)N(R 5 )-A, N(R 5 )C(S)N(R 5 )-A, CO 2 R 7 , C(O)N(R 5 )-A, CN, CHO, (C 1 -C 6 )alkyl-OR 7 , (C 1 -C 6 )alkyl-halogen, (C 1 -C 6 )alkyl-aryl, (C 1 -C 6 )alkyl-N(R 5 )C(O)O-A, (C 1 -C 6 )alkyl-N(R 5 )C(O)N(R 5 )-A, (C 1 -C 6 )alkyl-N(R 5 )C(S)N(R 5 )-A, (C 1 -C 6 )alkyl-OC(O)N(R 5 )-A and N(R 5 )S(O) m -A; R 10  is selected from hydrogen, halogen, A, hydroxyl, (C 1 -C 6 )alkyl-(C 3 -C 10 )carbocycle, (C 1 -C 6 )alkyl-aryl, C(O)-A, CO 2 R 7 , C(O)N(R 5 )-A, C(O)(C 1 -C 6 )alkyl-A, oxo, thio, \u2550N\u2014OH, \u2550N\u2014O\u2014(C 1 -C 6 )alkyl, O\u2014(C 1 -C 6 )alkyl, O\u2014(C 3 -C 10 )carbocycle, O-aryl, O-heteroaryl, S(O) n -A, N(R 5 )C(O)-A, N(R 5 )C(O)O-A, N(R 5 )C(O)N(R 5 )-A, N(R 5 )S(O) m -A, N(R 5 )C(O)-heterocyclic and N(R 5 )C(S)N(R 5 )-A; m is 1 or 2; and n is 0, 1 or 2, in admixture with a pharmaceutically acceptable adjuvant or carrier.

Metadata:
- Claim Count in Document: 38.0
- Percentile: 86.0
- Lexical Diversity: 1.7619
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15128886', '15505902', '13639959', '15689075', '14424361']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7580999681455977
- 35 USC 102 Novelty (BERT): 0.6141708144273813
- Combined Prediction Score: 0.743707052773776
- Mean Citation Score: 399.13778
- Max Citation Score: 583.3345
- Similarity Product: 474.0239524189233

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