# US 10,766,903 B2 · Piperidine derivatives as inhibitors of ubiquitin specific protease 7

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- Number: US 10,766,903 B2
- Document ID: US10766903B2
- Status: Granted
- Kind: B2
- Application number: 16/343,917
- Filed: 2017-10-20
- Published: 2019-08-22
- Granted: 2020-09-08
- Earliest claimed: 2016-10-20
- Assignees: Almac Discovery Limited
- Applicants: Almac Discovery Limited
- Inventors: Colin O'Dowd; Tim Harrison; Peter Hewitt; Shane Rountree; Miel Hugues; Frank Burkamp; Linda Duncan Jordan; Matthew Helm; Fabio Broccatelli; James John Crawford; Lewis Gazzard; Ingrid Wertz; Wendy Lee
- Web page: https://patentgrep.com/patent/US10766903B2

## CPC

- C07D 487/04: Ortho-condensed systems
- A61K 31/506: not condensed and containing further heterocyclic rings
- A61P 35/00: Antineoplastic agents
- C07D 401/04: directly linked by a ring-member-to-ring-member bond
- C07D 401/06: linked by a carbon chain containing only aliphatic carbon atoms
- C07D 401/14: containing three or more hetero rings
- C07D 403/04: directly linked by a ring-member-to-ring-member bond
- C07D 405/14: containing three or more hetero rings
- C07D 413/14: containing three or more hetero rings
- C07D 471/04: Ortho-condensed systems
- C07D 471/10: Spiro-condensed systems
- C07D 473/00: Heterocyclic compounds containing purine ring systems
- C07D 487/08: Bridged systems
- C07D 491/04: Ortho-condensed systems
- C07D 491/107: with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D 493/04: Ortho-condensed systems
- C07D 513/04: Ortho-condensed systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention concerns the identification of inhibitors of ubiquitin specific protease 7 (USP7), and methods of use thereof.

## Claims

### Claim 1

A compound of formula (I):
or a pharmaceutically acceptable salt, tautomer, stereoisomer or N-oxide derivative thereof, wherein:
R1 is H, OH or an optionally substituted alkyl group;
R2 is an optionally substituted C1-C6 alkyl, optionally substituted C2-C6 alkenyl, optionally substituted C2-C6 alkynyl, optionally substituted C3-C6 cycloalkyl, optionally substituted C4-C6 alkylcycloalkyl, optionally substituted C4-C6 aryl, optionally substituted C3-C6 heteroaryl, optionally substituted C4-C8 aryloxy, optionally substituted C7-C10 arylalkyl or optionally substituted C5-C10 heteroarylalkyl group; and
Q is selected from the group consisting of:
wherein:
R5a is H, halo, optionally substituted C1-C6 alkyl, or optionally substituted amino;
R5b is H, halo, optionally substituted C1-C6 alkyl, optionally substituted C2-C6 alkynyl, benzyl, optionally monosubstituted C3-C6 heteroaryl, optionally substituted C3-C6 heterocycloalkyl, optionally substituted C1-C6 alkoxy, NR′R″, or RaNR′R″,
wherein Ra is C1-C6 alkyl or C2-C6 alkenyl; and
wherein R′ and R″ are each independently selected from H, oxo-substituted C1-C6 alkyl, hydroxy-substituted C1-C6 alkyl, optionally substituted C1-C6 alkoxy, optionally substituted C3-C6 cycloalkyl, optionally substituted C1-C7 alkylamine, optionally substituted C2-C7 alkenylamine, optionally substituted C3-C10 heterocycloalkyl, optionally substituted C4-C10 aryl, optionally substituted C3-C10 heteroaryl, optionally substituted C5-C10 alkylaryl, optionally substituted C4-C10 alkylheterocycloalkyl, and C4-C6 alkylheteroaryl, or wherein R′ and R″ together form an optionally substituted C3-C8 heterocycloalkyl including the N to which they are attached;
R6a is H, optionally substituted C1-C6 alkyl, optionally substituted amino, optionally substituted C4-C6 aryl, optionally substituted C1-C6 sulfide, optionally substituted C1-C6 sulfonyl, or optionally substituted amino;
R6b is H, cyano, halo, optionally substituted C1-C6 alkyl, optionally substituted C2-C6 alkenyl, optionally substituted C2-C6 alkynyl, optionally substituted C3-C6 cycloalkyl, optionally substituted C4-C6 cycloalkenyl, optionally substituted C2-C6 ynol, optionally substituted C4-C6 aryl, optionally substituted C3-C6 heteroaryl, optionally substituted amino;
R7a is H;
R7b is H or optionally substituted C4-C6 aryl;
or wherein R7a and R7b together form an optionally substituted C1-C6 aryl group together with the carbons to which they are attached;
R8a is H or is optionally substituted C4-C6 aryl;
R9a is Cl, F, Br, I, or cyano; and
R9b is H, optionally substituted C1-C6 alkyl, optionally substituted C4-C6 aryl, optionally substituted C3-C8 heteroaryl, C1-C6 alkoxy.

### Claim 2 (depends on 1)

The compound according to claim 1 wherein the optional substituents are independently selected from OH, F, Cl, Br, I, CN, C1-C6 alkyl, CF3, CHF2, CH2F, CH2OH, COOH, C(O)CH3, CH2NHC(O)OCH2CH3, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C1-C6 alkoxy, amino, C1-C6 alkylamine, C5-C6 aryl, C3-C6 heteroaryl, benzyl, oxo and amide, or two adjacent substituents may together constitute a ring.

### Claim 3 (depends on 1)

The compound according to claim 1 wherein Q is:
and:
R5a is H,
R5b is selected from optionally methyl- or ethylamine-substituted pyrazole, and NR′R″, wherein R′ and R″ are each independently selected from H, methyl, cyclohexylamine, optionally methyl-, fluoro-, or fluorophenyl-substituted C2-C7 ethylamine, optionally substituted phenyl or wherein R′ and R″ together form an optionally substituted C3-C8 heterocycloalkyl including the N to which they are attached.

### Claim 4 (depends on 3)

The compound of claim 3 wherein R′ is H and R″ is ethylpyrollidine optionally substituted with methyl, fluoro, or fluorophenyl.

### Claim 5 (depends on 1)

The compound according to claim 1 wherein Q is:
and
R9a Cl, F, Br, I, or cyano;
R9b is H, optionally substituted C1-C6 alkyl, optionally substituted C4-C6 aryl;
wherein the optional substituents are selected from F, Cl, Br, methoxy, OH, CH2OH, C1-C6 alkylamine, cyclopropane, dioxolane, methylpyrazole optionally substituted with fluoro, and morpholine.

### Claim 6 (depends on 5)

The compound according to claim 5, wherein R9a is Cl, Br, I, or cyano and R9b is phenyl optionally substituted with F, Cl, Br, methoxy, OH, C1-C6 alkylamine, cyclopropane, dioxolane, methylpyrazole.

### Claim 7 (depends on 1)

The compound according to claim 1 wherein Q is:
and
R8a is H or phenyl; and optionally wherein R1 is OH.

### Claim 8 (depends on 1)

The compound according to claim 1 wherein Q is:
and
R6a is H, or C1-C6 alkyl;
R6b is H, or optionally substituted C4-C6 aryl;
wherein the optional substituent is selected from C1-C6 alkylamine.

### Claim 9 (depends on 8)

The compound according to claim 8 wherein R6a is H, or methyl and R6b is H, or phenyl optionally substituted with CH2NH2 or CH(CH3)NH2.

### Claim 10 (depends on 1)

The compound according to claim 1 wherein Q is:
and
R6b is H, or C4-C6 aryl, optionally wherein R6b is phenyl.

### Claim 11 (depends on 1)

The compound according to claim 1 wherein Q is:
and
R6a is H or C1-C6 alkyl, optionally wherein R6a is methyl;
R6b is H, or C1-C6 alkyl, optionally wherein R6b is propyl.

### Claim 12 (depends on 1)

The compound according to claim 1 wherein Q is:
and
R6a is H or C1-C6 alkyl;
R6b is H, halo, optionally substituted C2-C6 alkenyl, optionally substituted C2-C6 alkynyl, optionally substituted C3-C6 cycloalkyl, optionally substituted C4-C6 aryl, optionally substituted C3-C6 heteroaryl;
wherein the optional substituents are independently selected from F, CN, OH, CH2OH, amide, NH2, C1-C6 alkylamine, C3-C6 cycloalkylamine, CF3, COOH, methylmorpholine, CH(CF3)NH2, CH(CHF2)NH2, CH2NHC(O)OCH2CH3.

### Claim 13 (depends on 12)

The compound according to claim 12, wherein R6a is H, methyl or ethyl; R6b is H, Br, optionally substituted propenyl, ethynyl, optionally substituted propynyl, optionally substituted pentynyl, optionally substituted cyclohexane, optionally substituted phenyl, pyrazole, pyridine;
wherein the optional substituents are independently selected from F, CN, OH, CH2OH, amide, NH2, C1-C6 alkylamine, C3-C6 cycloalkylamine, CF3, CH(CF3)NH2, CH(CHF2)NH2.

### Claim 14 (depends on 12)

The compound according to claim 12, wherein R6a is methyl and R6b is phenyl optionally substituted with one or more of F, CN, OH, CH2OH, NH2, CH2NH2, CH2CH2NH2, CH(CH3)NH2, amide, cyclopropylamine, and cyclobutylamine.

### Claim 15 (depends on 1)

The compound according to claim 1, wherein Q is:
and
R6a is H or C1-C6 alkyl;
R6b is C4-C6 aryl, optionally phenyl.

### Claim 16 (depends on 1)

The compound according to claim 1 wherein R2 is CH2CRbRcRd and wherein no more than one of Rb, Rc and Rd are hydrogen.

### Claim 17 (depends on 1)

The compound according to claim 1 wherein R2 is optionally substituted C3-C5 heteroaryl, optionally substituted C3-C6 cycloalkyl, optionally substituted C4-C6 alkylcycloalkyl, optionally substituted C5-C10 arylalkyl or optionally substituted C5-C10 heteroarylalkyl group, wherein each optional substituent is independently selected from OH, F, methyl, CF3, CHF2, CH2F, CH2OH, C1-C4 alkoxy, and C3-C4 cycloalkyl.

### Claim 18 (depends on 17)

The compound according to claim 17, wherein R2 is optionally substituted ethylphenyl, wherein the ethyl group is optionally substituted with methyl, methyl, CF3, CHF2, or CH2F and the phenyl group is optionally substituted with F.

### Claim 19 (depends on 17)

The compound according to claim 17, wherein when R2 has the structure CH2CRbRcRd, no more than one of Rb, Rc and Rd is hydrogen.

### Claim 20 (depends on 17)

The compound according to claim 17, wherein the R2 is oxazole optionally substituted with cyclopropane, or pyrazole optionally substituted with methyl.

### Claim 21 (depends on 1)

The compound of claim 1 selected from the group consisting of:
(R)-6-Chloro-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(pyridin-4-yl)pyrimidin-4(3H)-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(1H-pyrazol-5-yl)pyrimidin-4(3H)-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(phenylamino)pyrimidin-4(3H)-one
(R)-6-Amino-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-6-((2-(Dimethylamino)ethyl)amino)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-6-((2-(Dimethylamino)ethyl)(methyl)amino)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(4-methylpiperazin-1-yl)pyrimidin-4(3H)-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-methoxypyrimidin-4(3H)-one
(R)-6-(2-(Dimethylamino)ethoxy)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((2-(pyrrolidin-1-yl)ethyl)amino)pyrimidin-4(3H)-one
6-((S)-3-Aminopyrrolidin-1-yl)-3-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-6-(3-Aminoazetidin-1-yl)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-5-Amino-6-chloro-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-1-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-9-methyl-1H-purin-6(9H)-one
(R)-1-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-9-methyl-8-phenyl-1H-purin-6(9H)-one
(R)-1-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-9-phenyl-1H-purin-6(9H)-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-4H-pyrido[1,2-a]pyrimidin-4-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-9-phenyl-4H-pyrido[1,2-a]pyrimidin-4-one
(R)-6-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-3-Bromo-6-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-3-Ethynyl-6-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-6-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-3-(trifluoromethyl)-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-6-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-3-(3-hydroxy-3-methyl but-1-yn-1-yl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-6-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-3-(1H-pyrazol-5-yl)-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-6-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-3-(pyridin-4-yl)-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-6-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-3-phenyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-3-(6-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-7-oxo-6,7-dihydro-2H-pyrazolo[4,3-d]pyrimidin-3-yl)benzamide
(R)-3-(3-Aminophenyl)-6-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-3-(4-(Aminomethyl)phenyl)-6-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-6-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-3-(3-hydroxyprop-1-yn-1-yl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-6-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-3-(prop-1-en-2-yl)-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-6-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-3-isopropyl-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-6-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-3-isopropyl-2-methyl-5,6-dihydro-2H-pyrazolo[4,3-d]pyrimidin-7(4H)-one
(R)-6-((1-(3,4-Dimethylpent-4-enoyl)-4-hydroxypiperidin-4-yl)methyl)-2-methyl-3-phenyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-6-((4-Hydroxy-1-(4-methyl-3-(trifluoromethyl) pent-4-enoyl)piperidin-4-yl)methyl)-2-methyl-3-phenyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-6-((4-Hydroxy-1-(4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-3-phenyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
6-((4-Hydroxy-1-(3-phenylpropanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
6-((4-Hydroxy-1-(3-phenylpropanoyl)piperidin-4-yl)methyl)-2-methyl-3-(trifluoromethyl)-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(1-methyl-1H-pyrazol-4-yl)pyrimidin-4(3H)-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(1-isobutyl-1H-pyrazol-4-yl)pyrimidin-4(3H)-one
3-((4-Hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((1,2,3,4-tetrahydro-1,4-epiminonaphthalen-6-yl)amino)pyrimidin-4(3H)-one
(R)-6-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-3-(phenylamino)-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-6-Chloro-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-5-methylpyrimidin-4(3H)-one
(R)-5-Bromo-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((2-(pyrrolidin-1-yl)ethyl)amino)pyrimidin-4(3H)-one
(R)-3-(4-(Aminomethyl)phenyl)-6-((4-hydroxy-1-(4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
6-((S)-3-Aminopiperidin-1-yl)-3-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-6-(4-Aminopiperidin-1-yl)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(2,8-diazaspiro[4.5]decan-8-yl)pyrimidin-4(3H)-one
6-((S)-3-(Dimethylamino)piperidin-1-yl)-3-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R,E)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(3-(pyrrolidin-1-yl) prop-1-en-1-yl)pyrimidin-4(3H)-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((2-(piperidin-1-yl)ethyl)amino)pyrimidin-4(3H)-one
(R,S)-3-(4-(Aminomethyl)phenyl)-6-((4-hydroxy-1-(4-methoxy-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-6-(1-(2-(Dimethylamino)ethyl)-1H-pyrazol-4-yl)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
6-((E)-3-((R)-3-Aminopyrrolidin-1-yl)prop-1-en-1-yl)-3-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
6-((E)-3-((S)-3-Aminopyrrolidin-1-yl)prop-1-en-1-yl)-3-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
3-((4-Hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(((S)-1-phenyl-3-(pyrrolidin-1-yl) propan-2-yl)amino)pyrimidin-4(3H)-one
3-((4-Hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(((R)-2-(pyrrolidin-1-yl)propyl)amino)pyrimidin-4(3H)-one
3-((4-Hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(((S)-2-(pyrrolidin-1-yl)propyl)amino)pyrimidin-4(3H)-one
3-((4-Hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(((R)-1-(pyrrolidin-1-yl)propan-2-yl)amino)pyrimidin-4(3H)-one
3-((4-Hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(((S)-1-(pyrrolidin-1-yl)propan-2-yl)amino)pyrimidin-4(3H)-one
6-((S)-3-(Dimethylamino)pyrrolidin-1-yl)-3-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
rac-6-(((±-trans-1,2)-2-Aminocyclohexyl)amino)-3-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
6-(((±-cis-1,2)-2-Aminocyclohexyl)amino)-3-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
3-((4-Hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((((R)-1-methylpyrrolidin-2-yl)methyl)amino)pyrimidin-4(3H)-one
3-((4-Hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((((S)-1-methylpyrrolidin-2-yl)methyl)amino)pyrimidin-4(3H)-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-9-(4-(Aminomethyl)phenyl)-1-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-1H-purin-6(9H)-one
3-((4-Hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((2-((S)-2-methylpyrrolidin-1-yl)ethyl)amino)pyrimidin-4(3H)-one
3-((4-Hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((2-((R)-2-(methoxymethyl)pyrrolidin-1-yl)ethyl)amino)pyrimidin-4(3H)-one
3-((4-Hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((2-((S)-3-methylpyrrolidin-1-yl)ethyl)amino)pyrimidin-4(3H)-one
(R)-9-(4-(Aminomethyl)phenyl)-1-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-8-methyl-1H-purin-6(9H)-one
6-((2-((R)-3-Fluoropyrrolidin-1-yl)ethyl)amino)-3-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
6-((2-((S)-3-Fluoropyrrolidin-1-yl)ethyl)amino)-3-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
3-(4-((R)-1-Aminoethyl)phenyl)-6-((4-hydroxy-1-((R)-4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
3-(4-((S)-1-Aminoethyl)phenyl)-6-((4-hydroxy-1-((R)-4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-9-(4-(Aminomethyl)phenyl)-1-((4-hydroxy-1-(4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-1H-purin-6(9H)-one
(R)-9-(4-(Aminomethyl)phenyl)-1-((4-hydroxy-1-(4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-8-methyl-1H-purin-6(9H)-one
(R)-3-(4-((Dimethylamino)methyl)phenyl)-6-((4-hydroxy-1-(4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazlo[4,3-d]pyrimidin-7(6H)-one
(R)-3-(4-(Aminomethyl)phenyl)-6-((1-(4,4-difluoro-3-phenylbutanoyl)-4-hydroxypiperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-isopropylpyrimidin-4(3H)-one
(R)-3-(4-(Aminomethyl)-3-fluorophenyl)-6-((4-hydroxy-1-(4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazlo[4,3-d]pyrimidin-7(6H)-one
(R)-6-((4-Hydroxy-1-(4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-3-(4-((methylamino)methyl)phenyl)-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-3-(4-(Aminomethyl)phenyl)-6-((1-(3-(3,5-difluorophenyl)-4,4,4-trifluorobutanoyl)-4-hydroxypiperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-3-(4-(Aminomethyl)phenyl)-6-((4-hydroxy-1-(4,4,4-trifluoro-3-(4-fluorophenyl) butanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-6-((2-(4-Fluoroisoindolin-2-yl)ethyl)amino)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-3-(4-(2-Aminoethyl)phenyl)-6-((4-hydroxy-1-(4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-3-(4-(1-Aminocyclobutyl)phenyl)-6-((4-hydroxy-1-(4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-3-((1-(4,4-Difluoro-3-phenylbutanoyl)-4-hydroxypiperidin-4-yl)methyl)-6-((2-(pyrrolidin-1-yl)ethyl)amino)pyrimidin-4(3H)-one
6-((4-Hydroxy-1-(3-phenylpropanoyl)piperidin-4-yl)methyl)-2-(methylthio)thiazolo[4,5-d]pyrimidin-7(6H)-one
3-((4-Hydroxy-1-(3-phenylpropanoyl)piperidin-4-yl)methyl)furo[3,2-d]pyrimidin-4(3H)-one
6-((4-Hydroxy-1-(3-phenylpropanoyl)piperidin-4-yl)methyl)-2-(methylsulfonyl)thiazolo[4,5-d]pyrimidin-7(6H)-one
6-((4-Hydroxy-1-(3-phenylpropanoyl)piperidin-4-yl)methyl)-2-(methylamino)thiazolo[4,5-d]pyrimidin-7(6H)-one
3-((4-Hydroxy-1-(3-phenylpropanoyl)piperidin-4-yl)methyl)furo[2,3-d]pyrimidin-4(3H)-one
6-((4-Hydroxy-1-(3-phenylpropanoyl)piperidin-4-yl)methyl)-2-methyl-3-(trifluoromethyl)-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-1-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-9-methyl-8-(trifluoromethyl)-1H-purin-6(9H)-one
3-(2-Fluorophenyl)-6-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-3-(6-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-7-oxo-6,7-dihydro-2H-pyrazolo[4,3-d]pyrimidin-3-yl)benzonitrile
3-(2-Aminophenyl)-6-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-morpholinopyrimidin-4(3H)-one
3-(Hydroxy(4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-4H-pyrido[1,2-a]pyrimidin-4-one
(R)-1-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-[4,5′-bipyrimidin]-6(1H)-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((2-hydroxyethyl)amino)pyrimidin-4(3H)-one
(R)-6-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-3-(3-hydroxyphenyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
3-(Hydroxy(4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-9-phenyl-4H-pyrido[1,2-a]pyrimidin-4-one
(R)-4-(6-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-7-oxo-6,7-dihydro-2H-pyrazolo[4,3-d]pyrimidin-3-yl)benzamide
(R)-6-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-3-(4-(hydroxymethyl)phenyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-6-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-3-(3-(morpholinomethyl)phenyl)-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((2-methoxyethyl)amino)pyrimidin-4(3H)-one
3-((4-Hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(((R)-pyrrolidin-3-yl)amino)pyrimidin-4(3H)-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-5-methyl-6-((2-(pyrrolidin-1-yl)ethyl)amino)pyrimidin-4(3H)-one
Benzyl 4-((3-(4-(aminomethyl)phenyl)-2-methyl-7-oxo-2,7-dihydro-6H-pyrazolo[4,3-d]pyrimidin-6-yl)methyl)-4-hydroxypiperidine-1-carboxylate
(R)—N-(1-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-oxo-1,6-dihydropyrimidin-4-yl)-N-(2-(pyrrolidin-1-yl)ethyl)acetamide
3-((4-Hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((2-((R)-2-methylpyrrolidin-1-yl)ethyl)amino)pyrimidin-4(3H)-one
(R)-1-(4-Hydroxy-4-((5-phenylpyrazin-2-yl)methyl)piperidin-1-yl)-3-phenylbutan-1-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(phenylethynyl)pyrimidin-4(3H)-one
(R)-6-Benzyl-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
3-(4-((R)-1-Amino-2,2,2-trifluoroethyl)phenyl)-6-((4-hydroxy-1-((R)-4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
3-(4-((S)-1-Amino-2,2,2-trifluoroethyl)phenyl)-6-((4-hydroxy-1-((R)-4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-3-(4-(Aminomethyl)phenyl)-2-ethyl-6-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(phenyl(2-(pyrrolidin-1-yl)ethyl)amino)pyrimidin-4(3H)-one
3-(4-((S)-1-Amino-2,2-difluoroethyl)phenyl)-6-((4-hydroxy-1-((R)-4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-3-(4-(Aminomethyl)-3-(trifluoromethyl)phenyl)-6-((4-hydroxy-1-(4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazlo[4,3-d]pyrimidin-7(6H)-one
(R)-3-(4-(1-Aminocyclopropyl)phenyl)-6-((4-hydroxy-1-(4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazlo[4,3-d]pyrimidin-7(6H)-one
(S)-3-(4-(Aminomethyl)phenyl)-6-((4-hydroxy-1-(4,4,4-trifluoro-3-(5-methylthiophen-2-yl) butanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-1-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)indolin-2-one
3-(4-(Aminomethyl)phenyl)-6-((1-(3,3-dicyclopropylpropanoyl)-4-hydroxypiperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-1-((4-Hydroxy-1-(4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-9-phenyl-1H-purin-6(9H)-one
(R)-1-((1-(4,4-Difluoro-3-phenylbutanoyl)-4-hydroxypiperidin-4-yl)methyl)-9-phenyl-1H-purin-6(9H)-one
(R)-6-((4-Hydroxy-1-(4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-3-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
6-((1-Acetyl-4-hydroxypiperidin-4-yl)methyl)-2-methyl-3-phenyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
3-((1-Acetyl-4-hydroxypiperidin-4-yl)methyl)-6-((2-(pyrrolidin-1-yl)ethyl)amino)pyrimidin-4(3H)-one
3-((1-(3,3-Dicyclopropylpropanoyl)-4-hydroxypiperidin-4-yl)methyl)-6-((2-(pyrrolidin-1-yl)ethyl)amino)pyrimidin-4(3H)-one
(R)-3-(Cyclohex-1-en-1-yl)-6-((4-hydroxy-1-(4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-3-(3-(Dimethylamino)prop-1-yn-1-yl)-6-((4-hydroxy-1-(4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazlo[4,3-d]pyrimidin-7(6H)-one
(R)-3-Cyclohexyl-6-((4-hydroxy-1-(4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-6-((4-Hydroxy-1-(4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-3-(4-(morpholinomethyl)phenyl)-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
3-(4-(Aminomethyl)phenyl)-6-((1-(3-cyclobutylpropanoyl)-4-hydroxypiperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-3-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-8-phenylpyrazolo[1,5-a][1,3,5]triazin-4(3H)-one
3-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((R)-2-(hydroxymethyl)pyrrolidin-1-yl)pyrimidin-4(3H)-one
(R)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(3-(methoxymethyl)azetidin-1-yl)pyrimidin-4(3H)-one
(R)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((2-(isopropylamino)ethyl)amino)pyrimidin-4(3H)-one
(R)—N-(2-((1-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-oxo-1,6-dihydropyrimidin-4-yl)amino)ethyl)acetamide
(R)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(4-hydroxypiperidin-1-yl)pyrimidin-4(3H)-one
(R)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((2-((4-(trifluoromethyl)pyrimidin-2-yl)amino)ethyl)amino)pyrimidin-4(3H)-one
(R)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((2-(phenylamino)ethyl)amino)pyrimidin-4(3H)-one
tert-butyl ((1-(1-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-oxo-1,6-dihydropyrimidin-4-yl)pyrrolidin-2-yl)methyl)carbamate
4-(1-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-oxo-1,6-dihydropyrimidin-4-yl)-N,N,2-trimethylmorpholine-2-carboxamide
3-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(3-morpholinopyrrolidin-1-yl)pyrimidin-4(3H)-one
3-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(3-hydroxy-3-methylpyrrolidin-1-yl)pyrimidin-4(3H)-one
3-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((tetrahydrofuran-3-yl)amino)pyrimidin-4(3H)-one
3-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(2-oxa-7-azaspiro[4.4]nonan-7-yl)pyrimidin-4(3H)-one
3-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(tetrahydro-2H-furo[2,3-c]pyrrol-5(3H)-yl)pyrimidin-4(3H)-one
(R)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(((1-methyl-1H-pyrazol-5-yl)methyl)amino)pyrimidin-4(3H)-one
(R)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((3-methyloxetan-3-yl)amino)pyrimidin-4(3H)-one
(R)-6-(4-(1H-pyrazol-5-yl)piperidin-1-yl)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-6-((4-chlorobenzyl)amino)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(4-(pyridin-3-ylmethyl)piperazin-1-yl)pyrimidin-4(3H)-one
(R)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(4-(pyridin-2-ylmethyl)piperazin-1-yl)pyrimidin-4(3H)-one
(R)-6-(4,4-difluoropiperidin-1-yl)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-2-((1-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-oxo-1,6-dihydropyrimidin-4-yl)amino)-N,N-dimethylacetamide
(R)-6-(((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)methyl)amino)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(((tetrahydro-2H-pyran-4-yl)methyl)amino)pyrimidin-4(3H)-one
(R)—N-(cyclopropylmethyl)-1-(1-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-oxo-1,6-dihydropyrimidin-4-yl)azetidine-3-carboxamide
(R)-6-(3-fluoroazetidin-1-yl)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((2-hydroxyethyl)(methyl)amino)pyrimidin-4(3H)-one
(R)-6-(cyclopentylamino)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(4-methyl-3-oxopiperazin-1-yl)pyrimidin-4(3H)-one
(R)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(5-oxa-2-azaspiro[3.4]octan-2-yl)pyrimidin-4(3H)-one
(R)-6-((1,3-dimethyl-1H-pyrazol-4-yl)amino)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(8-methyl-5-oxa-2,8-diazaspiro[3.5]nonan-2-yl)pyrimidin-4(3H)-one
(R)-6-(6-acetyl-2,6-diazaspiro[3.3]heptan-2-yl)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-6-(5,5-difluoro-2-azaspiro[3.3]heptan-2-yl)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)pyrimidin-4(3H)-one
(R)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(7-oxa-2-azaspiro[3.5]nonan-2-yl)pyrimidin-4(3H)-one
(R)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(2-oxa-7-azaspiro[3.5]nonan-7-yl)pyrimidin-4(3H)-one
(R)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(6-oxa-2-azaspiro[3.4]octan-2-yl)pyrimidin-4(3H)-one
(R)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((2-hydroxyethyl)(pyridin-3-ylmethyl)amino)pyrimidin-4(3H)-one
(R)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(5-methyl-2,5-diazaspiro[3.4]octan-2-yl)pyrimidin-4(3H)-one
(R)-3-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-6-(2-oxa-6-azaspiro[3.4]octan-6-yl)pyrimidin-4(3H)-one
3-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((1R,5S)-3-methyl-3,6-diazabicyclo[3.2.1]octan-6-yl)pyrimidin-4(3H)-one
3-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-6-((1 S,5R)-3-methyl-3,6-diazabicyclo[3.2.1]octan-6-yl)pyrimidin-4(3H)-one
(R)-3-(4-(1-Aminocyclobutyl)phenyl)-6-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
3-((1-(3-Cyclobutylpropanoyl)-4-hydroxypiperidin-4-yl)methyl)-6-((2-(pyrrolidin-1-yl)ethyl)amino)pyrimidin-4(3H)-one
3-((1-(2,2-Dicyclobutylacetyl)-4-hydroxypiperidin-4-yl)methyl)-6-((2-(pyrrolidin-1-yl)ethyl)amino)pyrimidin-4(3H)-one
(R)-6-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-3-phenyl-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7(6H)-one
6-((1-(3-Cyclobutylpropanoyl)-4-hydroxypiperidin-4-yl)methyl)-3-phenyl-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7(6H)-one
6-((1-(3,3-Dicyclopropylpropanoyl)-4-hydroxypiperidin-4-yl)methyl)-3-phenyl-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7(6H)-one
(R)-1-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-8-methyl-9-phenyl-1H-purin-6(9H)-one
(R)-1-((4-Hydroxy-1-(4,4,4-trifluoro-3-phenylbutanoyl)piperidin-4-yl)methyl)-8-methyl-9-phenyl-1H-purin-6(9H)-one
1-((1-(3,3-Dicyclopropylpropanoyl)-4-hydroxypiperidin-4-yl)methyl)-8-methyl-9-phenyl-1H-purin-6(9H)-one
6-((4-Hydroxy-1-(1-methylcyclopropanecarbonyl)piperidin-4-yl)methyl)-2-methyl-3-phenyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
6-((4-Hydroxy-1-(oxazole-5-carbonyl)piperidin-4-yl)methyl)-2-methyl-3-phenyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
6-((1-(3,3-Dicyclopropylpropanoyl)-4-hydroxypiperidin-4-yl)methyl)-2-methyl-3-phenyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
(R)-Ethyl 4-(6-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-7-oxo-6,7-dihydro-2H-pyrazolo[4,3-d]pyrimidin-3-yl)benzylcarbamate
1-((1-(2-Cyclopropyloxazole-5-carbonyl)-4-hydroxypiperidin-4-yl)methyl)-8-methyl-9-phenyl-1H-purin-6(9H)-one
6-((1-(2-Cyclopropyloxazole-5-carbonyl)-4-hydroxypiperidin-4-yl)methyl)-2-methyl-3-phenyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
6-((4-Hydroxy-1-(1-methylcyclopropanecarbonyl)piperidin-4-yl)methyl)-3-phenyl-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7(6H)-one
6-((1-(2-Cyclopropyloxazole-5-carbonyl)-4-hydroxypiperidin-4-yl)methyl)-3-phenyl-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7(6H)-one
7-Cyclopropyl-3-((4-hydroxy-1-(3-phenylpropanoyl)piperidin-4-yl)methyl)thieno[3,2-d]pyrimidin-4(3H)-one
6-Chloro-3-((4-hydroxy-1-(1-methylcyclopropanecarbonyl)piperidin-4-yl)methyl)-7-phenyl-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
7-(Benzo[d][1,3]dioxol-5-yl)-6-chloro-3-((4-hydroxy-1-(1-methylcyclopropanecarbonyl)piperidin-4-yl)methyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-7-(4-chlorophenyl)-3-((4-hydroxy-1-(1-methylcyclopropanecarbonyl)piperidin-4-yl)methyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-7-(4-fluorophenyl)-3-((4-hydroxy-1-(1-methylcyclopropanecarbonyl)piperidin-4-yl)methyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-3-((1-(2-cyclopropyloxazole-5-carbonyl)-4-hydroxypiperidin-4-yl)methyl)-7-(4-fluorophenyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-3-((1-(2-cyclopropyloxazole-5-carbonyl)-4-hydroxypiperidin-4-yl)methyl)-7-(4-fluoro-3-methoxyphenyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-7-(4-fluoro-3-methoxyphenyl)-3-((4-hydroxy-1-(1-methylcyclopropanecarbonyl)piperidin-4-yl)methyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-3-((4-hydroxy-1-(1-methylcyclopropanecarbonyl)piperidin-4-yl)methyl)-7-(3-(1-methyl-1H-pyrazol-5-yl)phenyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-3-((4-hydroxy-1-(1-methylcyclopropanecarbonyl)piperidin-4-yl)methyl)-7-methyl-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-3-((1-(2-cyclopropyloxazole-5-carbonyl)-4-hydroxypiperidin-4-yl)methyl)-7-(3-(1-methyl-1H-pyrazol-5-yl)phenyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-3-((1-(2-cyclopropyloxazole-5-carbonyl)-4-hydroxypiperidin-4-yl)methyl)-7-(3-(1-methyl-1H-pyrazol-4-yl)phenyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-3-((4-hydroxy-1-(1-methylcyclopropanecarbonyl)piperidin-4-yl)methyl)-7-(3-(1-methyl-1H-pyrazol-4-yl)phenyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
7-(3-Bromophenyl)-6-chloro-3-((1-(2-cyclopropyloxazole-5-carbonyl)-4-hydroxypiperidin-4-yl)methyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
7-(3-Bromophenyl)-6-chloro-3-((4-hydroxy-1-(1-methylcyclopropanecarbonyl)piperidin-4-yl)methyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-3-((1-(2-cyclopropyloxazole-5-carbonyl)-4-hydroxypiperidin-4-yl)methyl)-7-phenyl-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-3-((4-hydroxy-1-(1-methyl-1H-pyrazole-4-carbonyl)piperidin-4-yl)methyl)-7-phenyl-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-3-((1-(2-cyclopropyloxazole-5-carbonyl)-4-hydroxypiperidin-4-yl)methyl)-7-(3-cyclopropylphenyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-7-(3-cyclopropylphenyl)-3-((4-hydroxy-1-(1-methylcyclopropanecarbonyl)piperidin-4-yl)methyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-7-(3-cyclopropylphenyl)-3-((4-hydroxy-1-(1-methyl-1H-pyrazole-4-carbonyl)piperidin-4-yl)methyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-7-(4-cyclopropylphenyl)-3-((4-hydroxy-1-(1-methylcyclopropanecarbonyl)piperidin-4-yl)methyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-3-((1-(2-cyclopropyloxazole-5-carbonyl)-4-hydroxypiperidin-4-yl)methyl)-7-(4-cyclopropylphenyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Bromo-3-((1-(2-cyclopropyloxazole-5-carbonyl)-4-hydroxypiperidin-4-yl)methyl)-7-phenyl-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Bromo-3-((4-hydroxy-1-(1-methylcyclopropanecarbonyl)piperidin-4-yl)methyl)-7-phenyl-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
3-((1-(2-Cyclopropyloxazole-5-carbonyl)-4-hydroxypiperidin-4-yl)methyl)-6-iodo-7-phenyl-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-3-((4-hydroxy-1-(1-methylcyclopropanecarbonyl)piperidin-4-yl)methyl)-7-(3-(4-(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-3-((4-hydroxy-1-(1-methylcyclopropanecarbonyl)piperidin-4-yl)methyl)-7-(3-morpholinophenyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-7-(3-(4-fluoro-1H-pyrazol-1-yl)phenyl)-3-((4-hydroxy-1-(1-methylcyclopropanecarbonyl)piperidin-4-yl)methyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-7-(4-chlorophenyl)-3-((1-(2-cyclopropyloxazole-5-carbonyl)-4-hydroxypiperidin-4-yl)methyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-7-(4-chlorophenyl)-3-((4-hydroxy-1-(1-methyl-1H-pyrazole-4-carbonyl)piperidin-4-yl)methyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
6-Chloro-3-((1-(2-cyclopropyloxazole-5-carbonyl)-4-hydroxypiperidin-4-yl)methyl)-7-(4-fluoro-3-(1-methyl-1H-pyrazol-5-yl)phenyl)-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
3-((4-Hydroxy-1-(1-methylcyclopropanecarbonyl)piperidin-4-yl)methyl)-4-oxo-7-phenyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-6-carbonitrile,
7-(Benzo[d][1,3]dioxol-5-yl-2,2-d2)-6-chloro-3-((4-hydroxy-1-(1-methylcyclopropane-1-carbonyl)piperidin-4-yl)methyl)-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one
7-(Benzo[d][1,3]dioxol-5-yl-2,2-d2)-6-chloro-3-((1-(2-cyclopropyloxazole-5-carbonyl)-4-hydroxypiperidin-4-yl)methyl)-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one
3-(4-(Aminomethyl)phenyl)-6-((4-hydroxy-1-(1-methylcyclopropane-1-carbonyl)piperidin-4-yl)methyl)-2-methyl-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
3-(4-(Aminomethyl)phenyl)-6-((1-(2-cyclopropyloxazole-5-carbonyl)-4-hydroxypiperidin-4-yl)methyl)-2-methyl-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
6-Chloro-7-(3,4-dimethoxyphenyl)-3-((4-hydroxy-1-(1-methylcyclopropane-1-carbonyl)piperidin-4-yl)methyl)-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one
6-Chloro-3-((1-(2-cyclopropyloxazole-5-carbonyl)-4-hydroxypiperidin-4-yl)methyl)-7-(3,4-dimethoxyphenyl)-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one
7-(4-(Aminomethyl)phenyl)-6-chloro-3-((4-hydroxy-1-(1-methylcyclopropane-1-carbonyl)piperidin-4-yl)methyl)-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one
7-(4-(Aminomethyl)phenyl)-6-chloro-3-((1-(2-cyclopropyloxazole-5-carbonyl)-4-hydroxypiperidin-4-yl)methyl)-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one
(R)-4-(6-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-7-oxo-6,7-dihydro-2H-pyrazolo[4,3-d]pyrimidin-3-yl)benzoic acid
(R)-3-(6-((4-Hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-7-oxo-6,7-dihydro-2H-pyrazolo[4,3-d]pyrimidin-3-yl)benzoic acid
4-(6-((4-Hydroxy-1-(1-methylcyclopropane-1-carbonyl)piperidin-4-yl)methyl)-2-methyl-7-oxo-6,7-dihydro-2H-pyrazolo[4,3-d]pyrimidin-3-yl)benzoic acid
or a pharmaceutically acceptable salt, tautomer, isomer, or N-oxide derivative thereof.

### Claim 22 (depends on 1)

A pharmaceutical composition comprising a compound according to claim 1 or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient.