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 11):
The compound for use, or the pharmaceutical composition for use, according to  claim 10 , wherein said disease is selected from wound healing, chronic wound healing, diabetic foot, diabetic foot ulcer, leg ulcer, Raynaud's disease, male erectile dysfunction, female sexual dysfunction, hair loss, skin aging, vascular aging, pulmonary artery hypertension; stable, unstable and variant (Prinzmetal) angina; hypertension, pulmonary hypertension, chronic obstructive pulmonary disease, congestive heart failure, renal failure, atherosclerosis, conditions of reduced blood vessel patency, peripheral vascular disease, vascular disorders, systemic sclerosis (SSc), scleroderma, morphea, inflammatory diseases, stroke, bronchitis, chronic asthma, allergic asthma, allergic rhinitis, diabetic neuropathy, Idiopathic pulmonary fibrosis (IPF), peyronic's disease, glaucoma or a disease characterized by disorders of gut motility like irritable bowel syndrome, liver fibrosis, Alzheimer's disease and chronic heart failure, wherein preferably said disease is selected from wound healing, chronic wound healing, diabetic foot, diabetic foot ulcer, leg ulcer, diabetic neuropathy, peripheral vascular disease, vascular disorders such as Raynaud's disease, systemic sclerosis (SSc), scleroderma, pulmonary artery hypertension, male erectile dysfunction, and wherein again further preferably said disease is selected from wound healing, chronic wound healing, diabetic foot, diabetic foot ulcer, leg ulcer and diabetic neuropathy.

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): 0.7829572586688128
- 35 USC 102 Novelty (BERT): 0.5345672636760964
- Combined Prediction Score: 0.7581182591695412
- Mean Citation Score: 386.294384
- Max Citation Score: 391.60666
- Similarity Product: 204.6197233016014

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