PATENT CLAIM ANALYSIS

Application Number: 15770763
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-11
Patent Classification: ["514", "210160"]

Abstract:
The present invention relates to compounds of general formula (I), wherein D 1  to D 3 , -A-, n, R 1 , R 2 , Y 1 , L and  y2  are defined as in claim  1 , which have valuable pharmacological properties, in particular are inhibitors of plasma kallikrein. The compounds are suitable for treatment and prevention of diseases which can be influenced by inhibition of plasma kallikrein, such as diabetic complications, particularly in the treatment of retinal vascular permeability associated with diabetic retinopathy and diabetic macular edema.

Claim (Index 1):
A compound of formula (I) wherein of D 1  to D 3  (i) each denote N, or (ii) 2 denote N and 1 denotes CH, or (iii) 1 denotes N, 2 denote CH, or (iv) each denote CH and one or two H-atoms attached to C optionally are replaced by a substituent selected from the group consisting of C 1-4 -alkyl, \u2014CF 3 , \u2014CHF 2 , \u2014CN and \u2014OCH 3 ; n is 1, 2 or 3; denotes a 4-membered bridge composed of a \u2014C(NH 2 )\u2550N\u2014 unit and a second unit of \u2014CH\u2550CH\u2014, including both orientations for unsymmetric units, wherein a H-atom attached to a C-atom optionally is replaced by a substituent selected from the group consisting of F, Cl, CH 3 , CF 3  and CHF 2 ; R 1  denotes H, F, CN, C 1-3 -alkyl, CF 3 , OH, or \u2014OCH 3 ; R 2  denotes H, F, CN, CF 3 , CHF 2 , \u2014OCH 3  or a C 1-3 -alkyl group optionally substituted by \u2014OH; or R 1  and R 2  together denote \u2550O or together with the carbon atom they are attached to form a 3-7 membered saturated ring system wherein 1 \u2014CH 2 \u2014 group optionally is replaced by 0, S or NH; Y 1  denotes a divalent phenyl ring or a divalent 6-membered heteroaromatic ring containing for 2 \u2550N\u2014 ring members, wherein both ring systems are optionally substituted at one or two carbon atoms by a halogen atom, C 1-3 -alkyl, \u2014C 1-4 -cycloalkyl, \u2014CF 3 , \u2014CN, \u2014OH, HO\u2014C 1-3 -alkyl- or C 1-3 -alkyloxy-; L denotes a bond or a linker selected from \u2014C(R 3 R 4 )\u2014 and \u2014O\u2014, wherein\n R 3  denotes H, F, CN, C 1-3 -alkyl, CF 3 , CHF 2 , \u2014OH, \u2014CH 2 \u2014OH or \u2014OCH 3 , \n R 4  denotes H, F, CN, C 1-3 -alkyl, CF 3 , CHF 2 , \u2014CH 2 \u2014OH or \u2014OCH 3 ; and \n Y 2  denotes a fused or spiro polycyclic ring system attached to L via a C-atom or, where applicable, via a N-atom, containing 6 to 12 ring members in total, wherein\n 0 to 3 ring members are heteroatoms selected from \u2014N<, \u2014NH\u2014, \u2014N\u2550, \u2014O\u2014, \u2014S\u2014 with the proviso that one ring does not contain more than one heteroatom selected from \u2014O\u2014 and \u2014S\u2014, \n the polycyclic ring system is saturated, or \n one ring is saturated and a second ring is partially unsaturated, or \n one ring is saturated and a second ring is aromatic or heteroaromatic, or \n one ring is partially unsaturated and a second ring is aromatic or heteroaromatic, or \n a first and a second ring of the polycyclic ring system are partially unsaturated \n one \u2014CH 2 \u2014 ring member linked to a N-atom optionally is replaced by \u2014C(O)\u2014, \n and wherein the polycyclic ring system is optionally substituted at one or two carbon atoms by one or two groups independently selected from halogen atoms, C 1-3 -alkyl, \u2014CF 3 , \u2014CN, \u2014OH, HO\u2014C 1-3 -alkyl- and C 1-3 -alkyloxy-, with the proviso that two substituents containing an O-atom cannot be attached to the same carbon atom, and wherein the H atom in one or more NH groups present in Y 2  optionally is replaced by C 1-4 -alkyl or \u2014CH 2 \u2014C 1-4 -cycloalkyl; \n wherein in any definition mentioned hereinbefore and if not specified otherwise, any alkyl group or sub-group may be straight-chained or branched, or a salt thereof.

Metadata:
- Claim Count in Document: 2.0
- Percentile: 91.0
- Lexical Diversity: 1.57143
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15770762', '15953523', '15946837', '15508122', '15747818']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7882066214017031
- 35 USC 102 Novelty (BERT): 0.5822028162499892
- Combined Prediction Score: 0.7676062408865317
- Mean Citation Score: 333.686524
- Max Citation Score: 456.89117000000016
- Similarity Product: 454.7599282633377

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