PATENT CLAIM ANALYSIS

Application Number: 15774130
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-11
Patent Classification: ["544", "182000"]

Abstract:
The present invention relates to compounds of formula I or pharmaceutically acceptable salt, solvate or hydrate thereof, whereinR 1  is C 1 -C 3 alkyl optionally substituted with F, C 3 -C 6 cycloalkyl, C 1 -C 3 alkoxy; X represents a bond or C 1 -C 3 alkylene optionally substituted with OH, ONO, ONO 2 ; R 2  is H, OH, ONO, ONO 2 , C(O)OH, C(O)OC 1 -C 3 alkyl, CHO, CN, C 1 -C 3 alkoxy, OC(O)H, OC(O)—C 1 -C 3 alkyl, C(O)N(R 6 )OR 7 , OC 1 -C 3 alkylene-C(O)OH, OC 1 -C 3 alkylene-C(O)OC 1 -C 3 alkyl, OC 1 -C 3 alkylene-C(O)N(R 6 )OR 7 , S(O 0-2 )C 1 -C 3 alkyl, CR 8 ═N—OR 9 , CR 8 ═N—NR 10 R 11 , CR 8 ═NR 12  or CR 8 ═N—ONO 2 ; R 3  is C 1 -C 6 alkyl optionally substituted with F, OH, ONO, ONO 2 , C 1 -C 3 alkoxy, C 3 -C 6 cycloalkyl; C 3 -C 6 cycloalkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl; R 4  is C 1 -C 6 alkyl optionally substituted with C 3 -C 6 cycloalkyl, C 1 -C 6 alkoxy, F, ONO, ONO 2 ; C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl; R 5  is H, SO 2 NR 13 R 14 , NHSO 2 NR 13 R 14 ; R 6  is H or C 1 -C 3 alkyl; R 7  is H, C 1 -C 3 alkyl, C 1 -C 3 alkoxy, C 1 -C 3 alkyl substituted with phenyl, benzyl or a heterocyclic ring, wherein said phenyl, benzyl or said heterocyclic ring are independently optionally substituted by C 1 -C 3 alkyl, F; R 8  is H, CH 3  or C 2 H 5 ; R 9 : H, C 1 -C 3 alkyl optionally substituted with OH, ONO, ONO 2 , CN, COOH, COOC 1 -C 3 alkyl, C 1 -C 3 alkoxy, OC(O)H, OC(O)—C 1 -C 3 alkyl, C(O)N(R 6 )OR 7 , OC 1 -C 3 alkylene-C(O)OH, OC 1 -C 3 alkylene-C(O)OC 1 -C 3 alkyl, OC 1 -C 3 alkylene-C(O)N(R 6 )OR 7 , S(O 0-2 )C 1 -C 3 alkyl; R 10  and R 11  are each independently H, C 1 -C 3 alkyl optionally substituted with OH, ONO, ONO 2 , CN, COOH, COOC 1 -C 3 , C 1 -C 3 alkoxy, OC(O)H, OC(O)—C 1 -C 3 alkyl, C(O)N(R 6 )OR 7 , OC 1 -C 3 alkylene-C(O)OH, OC 1 -C 3 alkylene-C(O)OC 1 -C 3 alkyl, OC 1 -C 3 alkylene-C(O)N(R 6 )OR 7 , S(O 0-2 )C 1 -C 3 alkyl; or together with the nitrogen atom to which they are attached form a heterocyclic ring, wherein preferably said heterocyclic ring is selected from aziridine, azetidine, pyrollidine, piperidine, morpholine, piperazine and homopiperazine, wherein said heterocyclic ring is optionally substituted with C 1 -C 3  alkyl; R 12  is C 1 -C 3  alkyl optionally substituted with OH, ONO, ONO 2 , CN, COOH, COOC 1 -C 3 alkyl, C 1 -C 3 alkoxy, OC(O)H, OC(O)—C 1 -C 3 alkyl, C(O)N(R 6 )OR 7 , OC 1 -C 3 alkylene-C(O)OH, OC 1 -C 3 alkylene-C(O)OC 1 -C 3 alkyl, OC 1 -C 3 alkylene-C(O)N(R 6 )OR 7 , S(O 0-2 )C 1 -C 3 alkyl; R 13  and R 14  are each independently H or C 1 -C 6 alkyl optionally substituted with F, OH, ONO, ONO 2 , COOH, C 1 -C 3 alkoxy, C 3 -C 6 cycloalkyl; or together with the nitrogen atom to which they are attached form a heterocyclic ring, wherein preferably said heterocyclic ring is selected from aziridine, azetidine, pyrollidine, piperidine, morpholine, piperazine, homopiperazine, 2,5-diazabicyclo[2,2,1]heptane and 3,7-diazabicyclo[3,3,0]octane, wherein said heterocyclic ring is optionally substituted with R 15 ; R 15  is C 1 -C 6 alkyl optionally substituted with halogen, OH, ONO, ONO 2 , C 1 -C 3 alkoxy, C 1 -C 3 haloalkoxy, COOR 16 , NR 17 R 18 , C═NR 19 , or with a tetrazole group which is optionally substituted with C 1 -C 3 alkyl; or a heteroaryl ring which is optionally substituted with F, wherein the at least one heteroatom of said heteroaryl ring is nitrogen; R 16  is H, or C 1 -C 4 alkyl optionally substituted with F, OH, ONO, ONO 2 , NR 17 R 18 , or with a heteroaryl ring, wherein the at least one heteroatom of said heteroaryl ring is nitrogen, and wherein preferably said heteroaryl ring is selected from pyrrolidine, piperidine, piperazine, morpholine, pyrrole, and imidazole, wherein nitrogen atom is directly bound to C 1 -C 4  alkyl; R 17  and R 18  are each independently H or C 1 -C 4 alkyl optionally substituted with ONO, ONO 2 ; R 19  is C 1 -C 4 alkyl optionally substituted with F, ONO, ONO 2 ; C 3 -C 6 cycloalkyl; and their use in methods of treating or preventing a disease alleviated by inhibition of PDE-5 in a human or in a non-human mammal.

Claim (Index 13):
A process for the preparation of a compound of formula I of any one of the  claims 1  to  8 , wherein said process comprises:\n (a) reaction of a compound of formula II with a benzoic acid derivative of formula III in an aprotic or a protic solvent to generate a compound of formula IV \n (b) cyclization of said compound of formula IV to yield compound of formula I, wherein X, R 1 , R 2 , R 3 , R 4 , and R 5  are defined as for the compound of formula I in any one of the  claims 1  to  8 .

Metadata:
- Claim Count in Document: 23.0
- Percentile: 93.0
- Lexical Diversity: 7.57333
- Patent Class: 544.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['10536119', '14982131', '14912479', '11665428', '12083534']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7817895430295112
- 35 USC 102 Novelty (BERT): 0.5363318899260952
- Combined Prediction Score: 0.7572437777191696
- Mean Citation Score: 386.294384
- Max Citation Score: 391.60666
- Similarity Product: 250.01103550753

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