# US 8,404,677 B2 · Kinase inhibitors

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- Number: US 8,404,677 B2
- Document ID: US8404677B2
- Status: Granted
- Kind: B2
- Application number: 12/916,368
- Filed: 2010-10-29
- Published: 2011-11-03
- Granted: 2013-03-26
- Earliest claimed: 2009-10-29
- Assignees: Genosco; Oscotec Inc.
- Applicants: Hong Woo Kim; Jong Sung Koh; Jaekyoo Lee; Ho-Juhn Song; Youngsam Kim; Hee Kyu Lee; Jang-Sik Choi; Sun-Hee Lim; Sunhwa Chang
- Inventors: Hong Woo Kim; Jong Sung Koh; Jaekyoo Lee; Ho-Juhn Song; Youngsam Kim; Hee Kyu Lee; Jang-Sik Choi; Sun-Hee Lim; Sunhwa Chang
- Web page: https://patentgrep.com/patent/US8404677B2

## CPC

- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/04: Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- A61P 9/06: Antiarrhythmics
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 9/12: Antihypertensives
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/02: Nasal agents, e.g. decongestants
- A61P 11/06: Antiasthmatics
- A61P 11/08: Bronchodilators
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/06: Antipsoriatics
- A61P 19/00: Drugs for skeletal disorders
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 19/10: for osteoporosis
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 27/02: Ophthalmic agents
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 31/04: Antibacterial agents
- A61P 31/10: Antimycotics
- A61P 31/12: Antivirals
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 471/04: Ortho-condensed systems
- 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
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The present invention provides a new group of protein kinase inhibitors, pyrido[4,3,-d]pyrimidin-5-one derivatives, and pharmaceutically acceptable salts thereof that are useful for intreating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrido[4,3,-d]pyrimidin-5-one derivatives.

## Claims

### Claim 1

A compound of Formula (I):
wherein:(a) when R1 is H and X is NR2R3 or NR4R5, then
Y is NHR6 and Z is selected from H, halogen, C1-C3 alkyl, C2-C4 alkynyl, aryl, heteroaryl, or C3-C8 cycloalkyl, wherein the alkyl, cycloalkyl, aryl, alkynyl or heteroaryl is optionally substituted with halo, alkyl, or cyano; wherein:
R2 and R3, taken together with the nitrogen atom to which they are bonded form:
i) a 3-8 membered saturated or partially saturated monocyclic group having no heteroatom other than the nitrogen atom to which R2 and R3 are bonded, wherein said 3-8 membered saturated or partially saturated monocyclic group is independently substituted at one or more carbon atoms with 1-2 R7 and optionally substituted at one or more carbon atoms with 0-4 R8, wherein R7 is hydroxy, heterocycloalkyl, or NR9R9 and R8 is hydroxy(C1-C6)alkyl, aryl, COOR9, (CH2)nNR9R9, or (CH2)nNR9R10, wherein each n is independently 1, 2, or 3 and the aryl is optionally substituted with halo; or
ii) an 8-10 membered bicyclic aryl group having 0-5 heteroatoms independently selected from nitrogen, oxygen, sulfur, sulfoxide, or sulfone;
each R9 is independently selected from H, C1-C6 alkyl, C3-C6 alkynyl, C2-C6 alkyl cyano, C2-C6 alkyl sulfone, C3-C6 cycloalkyl sulfone, C2-C6 sulfonamide, C3-C6 cycloalkyl, C3-C8 heterocycloalkyl, aryl, aryl(C1-C6)alkyl, or heteroaryl, wherein the alkyl, alkynyl, alkylcyano, alkylsulfone, sulfonamide, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, or heteroaryl is optionally substituted with R25;
R10 is C(O)R9, COOR9, C(O)NR9R9, or S(O)nR9, wherein n is 1 or 2;
R4 is selected from H, C1-C6 alkyl, or hydroxy(C1-C6)alkyl;
R5 is aryl(C1-C3)alkyl, wherein the aryl group is independently substituted at one or more carbon atoms with 1-3 R11, wherein R11 is independently selected from OR9, NR9R9, NR9COR9, or NR9S(O)nR9, wherein n is 1 or 2;
R6 is selected from C1-C6 alkyl, C2-C6 alkenyl, C3-C6 alkynyl, C3-C6 cycloalkyl, C3-C8 heterocycloalkyl, C4-C6 cycloalkenyl, aryl, aryl(C1-C6)alkyl, or heteroaryl, wherein the heterocycloalkyl, aryl, or heteroaryl is optionally substituted, wherein the heterocycloalkyl, aryl, or heteroaryl of R6 is optionally substituted with an aryl selected from the group consisting of:
i) a 5-6 membered monocyclic aryl group;
ii) an 8-10 membered bicyclic aryl group having 0-5 heteroatoms independently selected from nitrogen, oxygen, sulfur, sulfoxide, or sulfone;
iii) an 8-10 membered unsaturated or partially unsaturated bicyclic aryl group having 0-5 heteroatoms independently selected from nitrogen, oxygen, sulfur, sulfoxide, or sulfone; and
iv) an 8-10 membered unsaturated or partially unsaturated bicyclic aryl group having a carbonyl, carboxamide, or sulfoxamide; or
the heterocycloalkyl, aryl, or heteroaryl of R6 is optionally substituted at one or more carbon atoms with R12, wherein each R12 is independently selected from C1-C6 alkyl, CF3, OCF3, S(O)n(C1-C4)alkyl, halo(C1-C4)alkyl, C2-C6 alkenyl, C3-C6 alkynyl, C3-C6 cycloalkyl, C3-C8 heterocycloalkyl, C4-C6 cycloalkenyl, aryl, aryl (C1-C6)alkyl, heteroaryl, halo, haloalkyl, SR13, OR13, OC(O)R13, NR13R13, NR13R14, COOR13, NO2, CN, C(O)R13, C(O)C(O)R13, C(O)NR13R13, S(O)nR13, S(O)nNR13R13, or NR15R16, wherein each n is independently 1 or 2 and the alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, arylalkyl, haloalkyl, or heteroaryl is optionally substituted with R25, wherein the aryl and heteroaryl of R12 is independently selected from:
i) a 5-6 membered monocyclic aryl group;
ii) an 8-10 membered bicyclic aryl group having 0-5 heteroatoms independently selected from nitrogen, oxygen, sulfur, sulfoxide or sulfone;
iii) an 8-10 membered unsaturated or partially unsaturated bicyclic aryl group having 0-5 heteroatoms independently nitrogen, oxygen, sulfur, sulfoxide or sulfone; or
iv) an 8-10 membered unsaturated or partially unsaturated bicyclic aryl group having a carbonyl, carboxamide, or sulfoxamide;
each R13 is independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C3-C6 alkynyl, C2-C6 alkyl cyano, C2-C6 alkyl sulfone, C2-C6 sulfonamide, C3-C6 cycloalkyl, C3-C8 heterocycloalkyl, C4-C6 cycloalkenyl, aryl, aryl(C1-C6)alkyl, haloalkyl or heteroaryl, wherein the alkyl, alkenyl, alkynyl, alkyl cyano, alkyl sulfone, alkyl sulfonamide, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, arylalkyl, haloalkyl, or heteroaryl is optionally substituted with R25;
R14 is C(O)R13, COOR13, C(O)NR13R13, SO2NR13R13, or S(O)nR13, wherein n is 1 or 2;
R15 and R16, taken together with the nitrogen atom to which they are bonded, form:
i) a 3-8 membered saturated or partially saturated monocyclic group, wherein the 3-8 membered saturated or partially saturated monocyclic group is optionally substituted with R25;
ii) an 8-12 membered saturated or partially saturated bicyclic group, wherein the 8-12 membered saturated or partially saturated bicyclic group is optionally substituted with R25;
iii) a 3-8 membered saturated or partially saturated monocyclic group having 1-3 heteroatoms selected from nitrogen, oxygen, sulfur, sulfone or sulfoxide, wherein the 3-8 membered saturated or partially saturated monocyclic group having 1-2 heteroatoms is optionally substituted with R13 or R14; or
iv) a 8-12 membered saturated or partially saturated bicyclic group having 1-3 heteroatoms selected from nitrogen, oxygen, sulfur, sulfone, sulfoxide, wherein the 8-12 membered saturated or partially saturated bicyclic group having 1-3 heteroatoms is optionally substituted with R13 or R14;
(b) when R1 is H and Y is NHR17 or R17, then X is OR18, NHR18, NR15R16, NR18R19, or NR19R20; and
Z is H, halogen, C1-C3 alkyl, C2-C4 alkynyl, aryl, heteroaryl, or C3-C8 cycloalkyl, wherein the alkyl, alkynyl, cycloalkyl, aryl, or heteroaryl is optionally substituted with halo, alkyl, or cyano, wherein:
R17 is selected from aryl(C1-C6)alkyl, aryl, or heteroaryl, wherein the aryl, or the heteroaryl is substituted at one or more carbon atoms with at least one R21 and 0-2 R22 and the aryl group of said aryl(C1-C6)alkyl is optionally substituted with halo;
R21 is independently selected from OH, CF3, OCF3, O-aryl, or NR15R16;
R22 is independently H, C1-C6 alkyl, CF3, OCF3, S(O)n(C1-C4)alkyl, halo(C1-C4)alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C8 heterocycloalkyl, C4-C6 cycloalkenyl, aryl, aryl(C1-C6)alkyl, heteroaryl, halo, SR13, OR13, OC(O)R13, NR13R13, NR13R14, COOR13, NO2, CN, C(O)R13, C(O)C(O)R13, C(O)NR13R13, S(O)nR13, S(O)nNR13R13, NR13C(O)NR13R13, NR13C(O)R13, NR13(COOR13), NR13S(O)nR13, or NR15R16, wherein each n is independently 1 or 2 and wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, arylalkyl, haloalkyl, or heteroaryl is optionally substituted with R25;
R18 is selected from C1-C6 alkyl, C2-C6 alkenyl, C3-C6 alkynyl, C3-C6 cycloalkyl, C3-C8 heterocycloalkyl, C4-C6 cycloalkenyl, aryl, aryl(C1-C6)alkyl, hydroxy(C2-C6)alkyl, amino(C2-C6)alkyl, haloalkyl, or heteroaryl, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, arylalkyl, haloalkyl, or heteroaryl is optionally substituted with R25;
each R19 is independently selected from C1-C6 alkyl, C2-C6 alkenyl, C3-C6 alkynyl, hydroxy(C2-C6)alkyl, amino(C2-C6)alkyl, C2-C6 alkyl cyano, C2-C6 alkyl sulfone, C2-C6 sulfonamide, C3-C6 cycloalkyl, C3-C8 heterocycloalkyl, C4-C6 cycloalkenyl, aryl, aryl(C1-C6)alkyl, haloalkyl, or heteroaryl, wherein the alkyl, alkenyl, alkynyl, alkyl cyano, alkylsulfone, sulfonamide, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, arylalkyl, haloalkyl, or heteroaryl is optionally substituted with R25;
R20 is C(O)R19COOR19, C(O)NR19R19 or S(O)nR19, wherein n is 1 or 2;
each R25 is independently selected from hydroxy, hydroxy(C1-C6)alkyl, C1-C6 alkyl, C2-C6 alkenyl, C3-C6 alkynyl, C3-C6cycloalkyl, C3-C8 heterocycloalkyl, C4-C6 cycloalkenyl, aryl(C1-C6)alkyl, aryl, halo, haloalkyl, oxo, oxime, CF3, SR13, OCF3, OR13, OC(O)CH2R13, NR13R13, NR13R14, NHC(O)R13, (CH2)nNR13R13, COOR13, CN, C(O)R13, C(O)CF3, CONR15R16, CONH2, S(O)nR13, S(O)nNR13R13, or NR15R16, wherein each n is independently 1 or 2 and the heterocycloalkyl is optionally substituted with C1-C3 alkyl; and
(c) when R1 is CH3, then
X is NH2 or NHR6,
Y is NHR6 or R6, and
Z is H, halogen, C1-C3 alkyl, C2-C4 alkynyl, aryl, heteroaryl, or C3-C8 cycloalkyl, wherein the alkyl, cycloalkyl, aryl, alkynyl, or heteroaryl is optionally substituted with halo, alkyl, or cyano, or
a pharmaceutically acceptable salt thereof;
wherein each heterocycloalkyl is independently a 3 to 8 membered ring haying 1 to 3 heteroatoms in the ring selected from N, O, S, sulfone or sulfoxide.

### Claim 2 (depends on 1)

The compound of claim 1, wherein R1 is H and X is NR2R3.

### Claim 3 (depends on 1)

The compound of claim 1, wherein R1 is H and X is NR4R5.

### Claim 4 (depends on 2)

The compound of claim 2, wherein NR2R3 is a 3-8 membered saturated or partially saturated monocyclic group having no heteroatom other than the nitrogen atom to which R2 and R3 are bonded, wherein said 3-8 membered saturated or partially saturated monocyclic group is independently substituted at one or more carbon atoms with 1-2 R7 and optionally substituted at one or more carbon atoms with 0-4 R8, wherein R7 is hydroxy, heterocycloalkyl, or NR9R9 and R8 is hydroxy(C1-C6)alkyl, aryl, COOR9, (CH2)nNR9R9, or (CH2)nNR9R10, wherein each n is independently 1, 2, or 3 and the aryl is optionally substituted with halo.

### Claim 5 (depends on 2)

The compound of claim 2, wherein NR2R3 is selected from an 8-10 membered bicyclic aryl group having 0-5 heteroatoms independently selected from nitrogen, oxygen, sulfur, sulfoxide, or sulfone.

### Claim 6 (depends on 4)

The compound of claim 4, wherein the 3-8 membered saturated or partially saturated monocyclic group is substituted with hydroxy or amine.

### Claim 7 (depends on 6)

The compound of claim 6, wherein the 3-8 membered saturated or partially saturated monocyclic group is azetidine, piperidine or pyrrolidine, wherein the azetidine, piperidine or pyrrolidine is independently substituted with 1-3 hydroxy or amino group and optionally and independently substituted with hydroxymethyl at the one or more carbon atoms.

### Claim 8 (depends on 3)

The compound of claim 3, wherein R4 is selected from H, C1-C6 alkyl, or hydroxy(C1-C6)alkyl and R5 is aryl(C1-C3)alkyl, wherein the aryl group of aryl(C1-C3)alkyl of R5 is independently substituted at the one or more carbon atoms with 1-3 R11, wherein R11 is independently selected from OR9, NR9R9, NR9COR9, or NR9S(O)nR9, wherein n is 1 or 2.

### Claim 9 (depends on 4)

The compound of claim 4, wherein R9 is independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C3-C6 alkynyl, C2-C6 alkyl cyano, C2-C6 alkyl sulfone, C3-C6 alkyl sulfone, C3-C6 cycloalkyl sulfone, C2-C6 sulfonamide, C3-C6 cycloalkyl, C3-C8 heterocycloalkyl, C4-C6 cycloalkenyl, aryl, aryl(C1-C6)alkyl, haloalkyl, or heteroaryl, wherein the alkyl, alkenyl, alkynyl, alkyl cyano, alkyl sulfone, sulfonamide, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, arylalkyl, haloalkyl, or heteroaryl is optionally substituted with R25.

### Claim 10 (depends on 2)

The compound of claim 2, wherein Y is NHR6.

### Claim 11 (depends on 10)

The compound of claim 10, wherein R6 is selected from C1-C6 alkyl, C2-C6 alkenyl, C3-C6 alkynyl, C3-C6 cycloalkyl, C3-C8 heterocycloalkyl, C4-C6 cycloalkenyl, aryl, aryl(C1-C6)alkyl, or heteroaryl, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, arylalkyl, haloalkyl, or heteroaryl is optionally substituted with R25.

### Claim 12 (depends on 11)

The compound of claim 11, wherein the aryl of R6 is an optionally substituted aryl selected from the group consisting of:
i) a 5-6 membered monocyclic aryl group;
ii) an 8-10 membered bicyclic aryl group having 0-5 heteroatoms independently selected from nitrogen, oxygen, sulfur, sulfoxide, or sulfone;
iii) an 8-10 membered unsaturated or partially unsaturated bicyclic aryl group having 0-5 heteroatoms independently selected from nitrogen, oxygen, sulfur, sulfoxide or sulfone; and
iv) an 8-10 membered unsaturated or partially unsaturated bicyclic aryl group having a carbonyl, carboxamide, or sulfoxamide.

### Claim 13 (depends on 12)

The compound of claim 12, wherein the aryl of R6 is optionally substituted at one or more carbon atoms with R12, wherein each R12 is independently selected from C1-C6 alkyl, OCF3, CF3, S(O)n(C1-C4)alkyl, halo(C1-C4)alkyl, C2-C6 alkenyl, C3-C6 alkynyl, C3-C6 cycloalkyl, C3-C8 heterocycloalkyl, C4-C6 cycloalkenyl, aryl, aryl C1-C6 alkyl, heteroaryl, halo, haloalkyl, SR13, OR13, OC(O)R13, NR13R13, NR13R14, COOR13, NO2, CN, C(O)R13, C(O)C(O)R13, C(O)NR13R13, S(O)nR13, S(O)nNR13R13, or NR15R16, wherein each n is independently 1 or 2; and wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, arylalkyl, haloalkyl, or heteroaryl is optionally substituted with R25.

### Claim 14 (depends on 13)

The compound of claim 13, wherein R12 is independently selected from C1-C6 alkyl, CF3, OCF3, S(O)n(C1-C4)alkyl, halo(C1-C4)alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C8 heterocycloalkyl, C4-C6 cycloalkenyl, aryl, aryl(C1-C6)alkyl, heteroaryl, halo, SR13, OR13, OC(O)R13, NR13R13, NR13R14, COOR13, NO2, CN, C(O)R13, C(O)NR13R13, S(O)nR13, S(O)nNR13R13, or NR15R16, wherein each n is independently 1 or 2.

### Claim 15 (depends on 14)

The compound of claim 14, wherein R12 is an aryl and the aryl is independently selected from:
i) a 5-6 membered monocyclic aryl group;
ii) an 8-10 membered bicyclic aryl group having 0-5 heteroatoms independently selected from nitrogen, oxygen, sulfur, sulfoxide, or sulfone;
iii) an 8-10 membered unsaturated or partially unsaturated bicyclic aryl group having 0-5 heteroatoms independently nitrogen, oxygen, sulfur, sulfoxide, or sulfone; or
iv) an 8-10 membered unsaturated or partially unsaturated bicyclic aryl group having a carboxamide, or sulfoxamide.

### Claim 16 (depends on 14)

The compound of claim 14, wherein R12 is SR13, OR13, OC(O)R13, NR13R13, NR13R14, COOR13, CN, C(O)R13, C(O)NR13R13, S(O)nR13, S(O)nNR13R13, or NR15R16, wherein each R13 is independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C2-C6 alkylcyano, C2-C6 alkyl sulfone, C2-C6 sulfonamide, C3-C6 cycloalkyl, C3-C8 heterocycloalkyl, C4-C6 cycloalkenyl, aryl, alkoxy, aryl(C1-C6)alkyl, haloalkyl, or heteroaryl and R14 is C(O)R13, COOR13, C(O)NR13R13, SO2NR13R13, or S(O)nR13, wherein n is 1 or 2 and the alkyl, alkenyl, alkynyl, alkyl cyano, alkyl sulfone, alkyl sulfonamide, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, alkoxy, arylalkyl, haloalkyl, or heteroaryl is optionally substituted with R25.

### Claim 17 (depends on 16)

The compound claim 16, wherein R12 is NR15R16.

### Claim 18 (depends on 17)

The compound claim 17, wherein R15 and R16, taken together with the nitrogen atom to which they are bonded, form:
i) a 3-8 membered saturated or partially saturated monocyclic group, wherein the 3-8 membered saturated or partially saturated monocyclic group is optionally substituted with R25;
ii) an 8-12 membered saturated or partially saturated bicyclic group, wherein the 8-12 membered saturated or partially saturated bicyclic group is optionally substituted with R25;
iii) a 3-8 membered saturated or partially saturated monocyclic group having 1-3 heteroatoms selected from nitrogen, oxygen, sulfur, sulfone or sulfoxide, wherein the 3-8 membered saturated or partially saturated monocyclic group having 1-2 heteroatoms is optionally substituted with R13 or R14; or
iv) an 8-12 membered saturated or partially saturated bicyclic group having 1-3 heteroatoms selected from nitrogen, oxygen, sulfur, sulfone, sulfoxide, wherein the 8-12 membered saturated or partially saturated bicyclic group having 1-3 heteroatoms is optionally substituted with R13 or R14.

### Claim 19 (depends on 11)

The compound of claim 11, wherein R6 is the optionally substituted 5-6 membered monocyclic aryl group or 9-10 membered bicyclic aryl group.

### Claim 20 (depends on 19)

The compound of claim 19, wherein the optionally substituted 5-6 membered monocyclic aryl group is phenyl and 9-10 membered bicyclic aryl group is naphtyl, quinolinyl, indazoyl, indolyl, or dihydrobenzodioxynyl.

### Claim 21 (depends on 20)

The compound of claim 20, wherein the phenyl group is optionally substituted with 1-4 groups selected from the group consisting of methyl, methoxy, methylsulfone, amino, hydroxy, CF3, OCF3, halo, phenyl, phenoxy, piperazinyl, and morpholino.

### Claim 22 (depends on 1)

The compound of claim 1, wherein Z is H, halo, C1-C3 alkyl, alkynyl or phenyl.

### Claim 23 (depends on 1)

The compound of claim 1, wherein R1 is H and Y is NHR17 or R17.

### Claim 24 (depends on 23)

The compound of claim 23, wherein X is NHR18 or OR18.

### Claim 25 (depends on 23)

The compound of claim 23, wherein X is NR18R19.

### Claim 26 (depends on 23)

The compound of claim 23, wherein X is NR19R20.

### Claim 27 (depends on 23)

The compound of claim 23, wherein X is NR15R16.

### Claim 28 (depends on 23)

The compound of claim 23, wherein R17 is aryl(C1-C6)alkyl, aryl or heteroaryl, wherein the aryl or the heteroaryl of R17 is substituted at two or more carbon atoms with at least one R21 and 0-2 R22, wherein R21 is independently selected from OH, CF3, OCF3, O-aryl, or NR15R16 and R22 is independently selected from H, C1-C6 alkyl, CF3, OCF3, S(O)n(C1-C4)alkyl, halo(C1-C4)alkyl, C2-C6 alkenyl, C3-C6 alkynyl, C3-C6 cycloalkyl, C3-C8 heterocycloalkyl, C4-C6 cycloalkenyl, aryl, aryl C1-C6 alkyl, heteroaryl, halo, haloalkyl, SR13, OR13, OC(O)R13, NR13R13, NR13R14, COOR13, NO2, CN, C(O)R13, C(O)C(O)R13, C(O)NR13R13, S(O)nR13, S(O)nNR13R13, or NR15R16, wherein each n is independently 1 or 2; and wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, arylalkyl, haloalkyl, heteroarylalkyl, or heteroaryl is optionally substituted with R25; and wherein the aryl group of said aryl(C1-C6)alkyl is optionally substituted with halo.

### Claim 29 (depends on 28)

The compound of claim 28, wherein the aryl of O-aryl is independently selected from:
i) a 5-6 membered monocyclic aryl group;
ii) an 8-10 membered bicyclic aryl group having 0-5 heteroatoms independently selected from nitrogen, oxygen, sulfur, sulfoxide or sulfone;
iii) an 8-10 membered unsaturated or partially unsaturated bicyclic aryl group having 0-5 heteroatoms independently nitrogen, oxygen, sulfur, sulfoxide or sulfone; or
iv) an 8-10 membered unsaturated or partially unsaturated bicyclic aryl group having a carboxamide or sulfoxamide.

### Claim 30 (depends on 28)

The compound of claim 28, wherein the aryl of R17 is a 5-6 membered monocyclic aryl group substituted with at least one group selected from CF3, OCF3, O-aryl, or NR15R16 at the one or more carbon atoms.

### Claim 31 (depends on 30)

The compound of claim 30, wherein the monocyclic aryl group is phenyl substituted with at least one group selected from CF3, OCF3, O-aryl, or NR15R16 at the one or more carbon atoms.

### Claim 32 (depends on 27)

The compound of claim 27, wherein NR15R16 is morpholino, piperazinyl, homopiperazinyl, thiomorpholino, piperidinyl, or pyrrolidinyl, wherein the piperazinyl, homopiperazinyl, piperidinyl, or pyrrolidinyl is optionally substituted at one or more carbon atoms with 1, 2 or 3 R25 or at one nitrogen atom with R13 or R14.

### Claim 33 (depends on 24)

The compound of claim 24, wherein R18 is selected from C1-C6 alkyl, C3-C6 alkenyl, C3-C6 alkynyl, C3-C6 cycloalkyl, C3-C8 heterocycloalkyl, C4-C6 cycloalkenyl, aryl, aryl(C1-C6)alkyl, haloalkyl or heteroaryl, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, arylalkyl, haloalkyl, or heteroaryl is optionally substituted with R25.

### Claim 34 (depends on 33)

The compound of claim 33, wherein R18 is C1-C6 alkyl optionally substituted with one or more aryl, alkyl, halo, R23 or R24, wherein each R23 is independently CF3, OCF3, SR13, OR13, NR13R13, S(O)nNR13R13, S(O)nR13, or NR15R16, each of n being independently 1 or 2 and wherein each R24 is selected from a 5-8 membered monocyclic group having 1-3 heteroatoms, an 8-12 membered bicyclic group having 1-5 heteroatoms, or an 11-14 membered tricyclic group having 1-8 heteroatoms, wherein said heteroatoms of R24 are independently oxygen, nitrogen, or sulfur, wherein R24 is optionally substituted with R13 or R14.

### Claim 35 (depends on 34)

The compound of claim 34, wherein zero, one, two, three or four atoms of R24 are optionally and independently substituted with R13.

### Claim 36 (depends on 34)

The compound of claim 34, wherein the aryl is optionally and independently substituted at one or more carbon atoms with 1-3 R11, wherein R11 is independently selected from OR9, NR9R9, NR9COR9, or NR9S(O)nR9, wherein n is 1 or 2.

### Claim 37 (depends on 34)

The compound of claim 34, wherein the C1-C6 alkyl is C2-C4 alkyl optionally substituted with 1-3 groups selected from the group consisting of amino, hydroxy, phenyl, benzyl, and morpholino.

### Claim 38 (depends on 33)

The compound of claim 33, wherein R18 is C3-C6 alkenyl optionally substituted with one or more, aryl, alkyl, halo, R23, or R24, wherein each R23 is independently selected from CF3, OCF3, SR13, OR13, NR13R13, S(O)nNR13R13, S(O)nR13, or NR15R16, wherein each n is independently 1 or 2, and wherein each R24 is independently selected from: a 5-8 membered monocyclic group having 1-3 heteroatoms; an 8-12 membered bicyclic having 1-5 heteroatoms; or an 11-14 membered tricyclic group having 1-8 heteroatoms, wherein said heteroatoms of R24 is independently selected from oxygen, nitrogen or sulfur, and wherein R24 is optionally substituted with R13 or R14.

### Claim 39 (depends on 38)

The compound of claim 38, wherein zero, one, two, three or four atoms of R24 are optionally and independently substituted with R13.

### Claim 40 (depends on 33)

The compound of claim 33, wherein R18 is C3-C6 cycloalkyl optionally substituted with one or more, aryl, alkyl, halo, R23 or R24; wherein each R23 is independently selected from CF3, OCF3, SR13, OR13, NR13R13, (CH2)nNR13R13, S(O)nNR13R13, S(O)nR13, or NR15R16, wherein each n is independently 1 or 2; and wherein each R24 is independently selected from a 5-8 membered monocyclic group having 1-3 heteroatoms, an 8-12 membered bicyclic group having 1-5 heteroatoms, or an 11-14 membered tricyclic group having 1-8 heteroatoms, wherein said heteroatoms of R24 is independently selected from oxygen, nitrogen or sulfur, and wherein R24 is optionally substituted with R13 or R14.

### Claim 41 (depends on 40)

The compound of claim 40, wherein zero, one, two, three or four atoms of R24 are optionally and independently substituted with R13.

### Claim 42 (depends on 25)

The compound of claim 25, wherein R18 is C3-C6 cycloalkyl optionally substituted with one or more aryl, alkyl, halo, R23, or R24.

### Claim 43 (depends on 33)

The compound of claim 33, wherein R18 is C3-C8 heterocycloalkyl, wherein the C3-C8 heterocycloalkyl is a 5-7 membered monocycle having a heteroatom, wherein said heteroatom is independently selected from oxygen, nitrogen, sulfur, or sulfone; wherein the nitrogen atom is optionally substituted with R19.

### Claim 44 (depends on 43)

The compound of claim 43, wherein the monocycle is optionally substituted morpholine, tetrahydrofuran, thiomorpholine, piperazine or homopiperazine.

### Claim 45 (depends on 25)

The compound of claim 25, wherein R19 is independently selected from C1-C6 alkyl, C2-C6 alkenyl, C3-C6 alkynyl, hydroxy(C2-C6)alkyl, amino(C2-C6)alkyl, C2-C6 alkyl cyano, C2-C6 alkyl sulfone, C2-C6 sulfonamide, C3-C6 cycloalkyl, C4-C6 heterocycloalkyl, C4-C6 cycloalkenyl, aryl, aryl(C1-C6)alkyl, haloalkyl, or heteroaryl.

### Claim 46 (depends on 26)

The compound of claim 26, wherein R19 is independently selected from hydroxy(C2-C6)alkyl, amino(C2-C6)alkyl, C2-C6 alkyl cyano, C2-C6 alkyl sulfone, C2-C6 sulfonamide, C3-C6 cycloalkyl, or C4-C8 heterocycloalkyl.

### Claim 47 (depends on 26)

The compound of claim 26, wherein R20 is selected from C(O)R19, COOR19, C(O)NR19R19, or S(O)nR19, wherein n is 1 or 2.

### Claim 48 (depends on 27)

The compound of claim 27, wherein R15 and R16 of NR15R16, taken together with the nitrogen atom to which they are bonded, form:
i) a 3-8 membered saturated or partially saturated monocyclic group, wherein the 3-8 membered saturated or partially saturated monocyclic group is optionally substituted with R25;
ii) an 8-12 membered saturated or partially saturated bicyclic group, wherein the 8-12 membered saturated or partially saturated bicyclic group is optionally substituted with R25;
iii) a 3-8 membered saturated or partially saturated monocyclic group having 1-3 heteroatoms selected from nitrogen, oxygen, sulfur, sulfone or sulfoxide, wherein the 3-8 membered saturated or partially saturated monocyclic group having 1-2 heteroatoms is optionally substituted with R13 or R14; or
iv) an 8-12 membered saturated or partially saturated bicyclic group having 1-3 heteroatoms selected from nitrogen, oxygen, sulfur, sulfone, sulfoxide, wherein the 8-12 membered saturated or partially saturated bicyclic group having 1-3 heteroatoms is optionally substituted with R13 or R14.

### Claim 49 (depends on 48)

The compound of claim 48, wherein NR15R16 is the 4-6 membered saturated monocyclic group optionally and independently substituted at one or more carbon atoms with 1-4 R25.

### Claim 50 (depends on 49)

The compound of claim 49, wherein the aryl group of R25 is selected from:
i) a 5-6 membered monocyclic aryl group;
ii) an 8-10 membered bicyclic aryl group having 0-5 heteroatoms independently selected from nitrogen, oxygen, sulfur, sulfoxide or sulfone;
iii) an 8-10 membered unsaturated or partially unsaturated bicyclic aryl group having 0-5 heteroatoms independently selected from nitrogen, oxygen, sulfur, sulfoxide, or sulfone; or
iv) an 8-10 membered unsaturated or partially unsaturated bicyclic aryl group having a carbonyl, carboxamide, or sulfoxamide.

### Claim 51 (depends on 48)

The compound of claim 48, wherein NR15R16 is a 5-8 membered saturated heterocyclic group having 1-2 heteroatoms selected from nitrogen, oxygen, sulfur, sulfone, or sulfoxide, wherein said 5-8 membered saturated heterocyclic group is optionally substituted with hydroxy, amino, C1-C6 alkyl, or phenyl at one or more carbon atoms or nitrogen atoms.

### Claim 52 (depends on 49)

The compound of claim 49, wherein the 4-6 membered saturated monocyclic group is selected from piperidine or pyrrolidine optionally substituted with 1-4 groups selected from hydroxy, amino, C1-C6 alkyl, hydroxy(C1-C6)alkyl, amino(C1-C6)alkyl, or phenyl.

### Claim 53 (depends on 51)

The compound of claim 51, wherein the 5-8 membered saturated heterocyclic group is selected from morpholine, thiomorpholine, piperazine or homopiperazine optionally substituted with 1-4 groups selected from hydroxy, amino, C1-C6 alkyl and phenyl, wherein each C1-C6 alkyl is optionally substituted with one or more amino, or hydroxy.

### Claim 54 (depends on 51)

The compound of claim 51, wherein the 1-2 heteroatoms are nitrogen and nitrogen atoms are independently substituted with C1-C6 alkyl, C(O)C1-C3 alkyl, or S(O)2C1-C3 alkyl, wherein the alkyl is optionally and independently substituted with amino or hydroxy.

### Claim 55 (depends on 1)

The compound of claim 1, wherein R1 is methyl, X is selected from NH2 or NHR6, and Y is selected from R6 or NHR6.

### Claim 56 (depends on 1)

A compound or salt of claim 1, wherein the compound or salt is selected from the group consisting of:
4-(3,5-dimethoxyphenylamino)-2-(4-hydroxypiperidin-1-yl)pyrido[4,3-d]pyrimidin-6(6H)-one;
4-(3,5-dimethoxyphenylamino)-2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)pyrido[4,3d]pyrimidin-5(6H)-one;
2-(4-aminopiperidin-1-yl)-4-(3,5-dimethoxyphenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
4-(3,5-dimethoxyphenylamino)-2-(4-morpholinopiperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
methyl 1-(4-(3,5-dimethoxyphenyl amino)-5-oxo-5,6-dihydropyrido[4,3-d]pyrimidin-2-yl)-4-hydroxy piperidine-4-carboxylate;
2-(4-hydroxypiperidin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidine-5(6H)-one;
(R)-2-(3-aminopyrrolidin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
(S)-2-(pyrrolidin-3-ylamino)-4-(4-trifluoromethylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-((1R,4R)-4-aminocyclohexyl amino)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(2-morpholinoethoxy)-4-(3-(trifluoro methyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-aminopiperidin-1-yl)-4-(3-(trifluoro methyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
2-(4-methylpiperazin-1-yl)-4-(3-(trifluoro methyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(3,4-dihydroisoquinolin-2(1H)-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
(R)-2-(3-hydroxypyrrolidin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(piperidin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-aminopiperidin-1-yl)-4-(3-(trifluoro methyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
2-(4-hydroxypiperidin-1-yl)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-(2-hydroxyethyl)piperazin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
N-(2-((5-oxo-4-(3-(trifluoromethyl)phenylamino)-5,6-dihydropyrido[4,3-d]pyrimidin-2-ylamino)methyl)phenyl)methanesulfonamide;
(S)-2-(3-hydroxypyrrolidin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-aminopiperidin-1-yl)-4-(4-(trifluoro methyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
N-(1-(5-oxo-4-(4-(trifluoromethyl)phenylamino)-5,6-dihydropyrido[4,3-d]pyrimidin-2-yl)piperidin-4-yl)cyclopropanesulfonamide;
2-(piperidin-4-ylamino)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
(S)-2-(3-aminopyrrolidin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
2-morpholino-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-a]pyrimidin-5(6H)-one;
2-((1R,4R)-4-hydroxycyclohexylamino)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-oxopiperidin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(3,4-dihydroisoquinolin-2(1H)-yl)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(3-(3-(trifluoromethyl)phenyl)-6,7-dihydro-[1,2,3]triazolo[1,5-a]pyrazin-5(4H)-yl)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(cyclopropylamino)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(cyclopentylamino)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
(R)-2-(pyrrolidin-3-ylamino)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
2-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(benzylamino)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(benzyl(methyl)amino)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
(S)-2-(1-(4-fluorophenyl)ethylamino)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-((tetrahydro-2H-pyran-4-yl)methylamino)-4-(4-(trifluoromethyl)phenyl amino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-fluorobenzylamino)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(piperidin-4-ylmethylamino)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
2-(tetrahydro-2H-pyran-4-ylamino)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(1,4-diazepan-1-yl)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
2-(thiazolidin-3-yl)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
N-(2-((5-oxo-4-(4-(trifluoromethyl)phenylamino)-5,6-dihydropyrido[4,3-d]pyrimidin-2-ylamino)methyl)phenyl)methanesulfonamide;
(S)-2-(1-cyclohexylethylamino)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(cyclohexylamino)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
(R)-2-(1-methylpyrrolidin-3-ylamino)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
(R)-2-(1-isopropylpyrrolidin-3-ylamino)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-((1-methylpiperidin-4-yl)methylamino)-4-(4-(trifluoromethyl)phenylamino) pyrido[4,3-d]pyrimidin-5(6H)-one;
2-((1-isopropylpiperidin-4-yl)methylamino)-4-(4-(trifluoromethyl)phenyl amino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-((dimethylamino)methyl)piperidin-1-yl)-4-(4-(trifluoromethyl)phenylamino) pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-methylthiazol-2-ylamino)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
(S)-2-(1-(methylsulfonyl)pyrrolidin-3-ylamino)-4-(4-(trifluoromethyl)phenyl amino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-(2-hydroxyethyl)piperazin-1-yl)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-(hydroxymethyl)piperidin-1-yl)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
ethyl 1-(5-oxo-4-(4-(trifluoromethyl)phenylamino)-5,6-dihydropyrido[4,3-d]pyrimidin-2-yl)piperidine-4-carboxylate;
2-(4-(4-(2-hydroxyethyl)piperazine-1-carbonyl)piperidin-1-yl)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-(4-(hydroxymethyl)piperidine-1-carbonyl)piperidin-1-yl)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-((1S,2R)-2-aminocyclohexylamino)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-((1S,2S)-2-aminocyclohexylamino)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-((1R,2S)-2-aminocyclohexylamino)-4-(2-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-((1R,2R)-2-aminocyclohexylamino)-4-(2-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-((1R,4R)-4-aminocyclohexylamino)-4-(2-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-ethylpiperazin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(2-morpholinoethylamino)-4-(3(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(3-aminocyclohexylamino)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-(methylsulfonyl)piperazin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(morpholinoamino)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-acetylpiperazin-1-yl)-4-(3-(trifluoro methyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
(R)-2-(2-hydroxy-1-phenylethylamino)-4-(3-(trifluoromethyl)phenylaminopyrido[4,3-d]pyrimidin-5(6H)-one;
(S)-2-(2-hydroxy-1-phenylethylamino)-4-(3-(trifluoromethyl)phenylaminopyrido[4,3-d]pyrimidin-5(6H)-one;
(R)-2-(1-hydroxy-3-phenylpropan-2-ylamino)-4-(3-(trifluoromethyl)phenyl amino)pyrido[4,3-d]pyrimidin-5(6H)-one;
(S)-2-(1-hydroxy-3-phenylpropan-2-ylamino)-4-(3-(trifluoromethyl)phenyl amino)pyrido[4,3-d]pyrimidin-5(6H)-one;
1-(5-oxo-4-(3-(trifluoromethyl)phenyl amino)-5,6-dihydropyrido[4,3-d]pyrimidin-2-yl)piperidine-4-carboxamide;
(R)-2,2,2-trifluoro-N-(1-(5-oxo-4-(3-(trifluoromethyl)phenylamino)-5,6-dihydropyrido[4,3-d]pyrimidin-2-yl)pyrrolidin-3-yl)acetamide;
2-(4-(4-chlorophenyl)-4-hydroxy piperidin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-((1S,2S)-2-(phenylsulfonyl)cyclohexylamino)-4-(3-(trifluoromethyl)phenyl amino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-((1S,2R)-2-aminocyclohexylamino)-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-thiomorpholino-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-sulfonylpyrido)-4-(3-(trifluoro methyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-morpholinopiperidin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
N-((1R,2S)-2-(5-oxo-4-(3-(trifluoro methyl)phenylamino)-5,6-dihydropyrido[4,3-d]pyrimidin-2-ylamino)cyclohexyl)acetamide;
N-((1R,4R)-4-(5-oxo-4-(3-(trifluoro methyl)phenylamino)-5,6-dihydropyrido[4,3-d]pyrimidin-2-ylamino)cyclohexyl)acetamide;
2-((1R,2R)-2-(dimethylamino)cyclohexyl amino)-4-(3-(trifluoromethyl)phenyl amino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-aminopiperidin-1-yl)-4-(3-bromophenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
4-(3-bromophenylamino)-2-(4-hydroxypiperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-aminopiperidin-1-yl)-4-(3-bromophenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
4-(3-bromophenylamino)-2-(4-(dimethylamino)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
(S)-4-(3-bromophenylamino)-2-(4-(1-hydroxypropan-2-ylamino)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
(R)-2-(4-(3-aminopyrrolidin-1-yl)piperidin-1-yl)-4-(3-bromophenyl amino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
(R)-2-(3-aminopyrrolidin-1-yl)-4-(3-bromophenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
4-(3-bromophenylamino)-2-(3-hydroxypiperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
(R)-2-(3-aminopyrrolidin-1-yl)-4-(4-bromophenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
(S)-2-(3-aminopyrrolidin-1-yl)-4-(4-bromophenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
4-(4-bromophenylamino)-2-(4-hydroxypiperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-aminopiperidin-1-yl)-4-(4-bromophenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
(S)-4-(3-bromophenylamino)-2-(4-(1-hydroxypropan-2-ylamino)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(3-bromophenylamino)-2-(4-(dimethylamino)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-aminopiperidin-1-yl)-4-(m-tolylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
2-(4-hydroxypiperidin-1-yl)-4-(m-tolyl amino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-((1R,2R)-2-aminocyclohexylamino)-4-(3,5-bis(trifluoromethyl)phenylamino) pyrido[4,3-d]pyrimidin-5(6H)-one;
(2-((1R,2S)-2-aminocyclohexylamino)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one with (2-((1S,2R)-2-aminocyclohexylamino)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(3,5-bis(trifluoromethyl)phenylamino)-2-(4-hydroxypiperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(3,5-bis(trifluoromethyl)phenylamino)-2-morpholinopyrido[4,3-d]pyrimidin-5(6H)-one;
4-(3,5bis(trifluoromethyl)phenyl amino)-2-((1r,4r)-4-hydroxycyclohexyl amino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(2-aminobenzylamino)-4-(3,5-bis(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(3,5-bis(trifluoromethyl)phenylamino)-2-(4-methylpiperazin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-aminopiperidin-1-yl)-4-(3,5-bis(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
(S)-4-(3,5-bis(trifluoromethyl)phenylamino)-2-(pyrrolidin-3-ylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
4-(3,5-bis(trifluoromethyl)phenylamino)-2-(piperidin-4-ylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
4-(3,5-bis(trifluoromethyl)phenylamino)-2-(1-methylpiperidin-4-ylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
(S)-4-(3,5-bis(trifluoromethyl)phenyl amino)-2-(1-methylpyrrolidin-3-ylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(3,5-bis(trifluoromethyl)phenylamino)-2-(4-(dimethylamino)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(3,5-bis(trifluoromethyl)phenylamino)-2-(4-(hydroxymethyl)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(3,5-bis(trifluoromethyl)phenylamino)-2-(4-(2-hydroxyethyl)piperazin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
(R)-4-(3,5-bis(trifluoromethyl)phenyl amino)-2-(3-hydroxypyrrolidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(3,5-bis(trifluoromethyl)phenylamino)-2-(3-hydroxyazetidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(3,5-bis(trifluoromethyl)phenylamino)-2-(4-(2-hydroxyethyl)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
N-((1r,4r)-4-(4-(3,5-bis(trifluoromethyl)phenylamino)-5-oxo-5,6-dihydropyrido[4,3-d]pyrimidin-2-ylamino)cyclohexyl)acetamide;
4-(3,5-bis(trifluoromethyl)phenylamino)-2-(3-oxopiperazin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(3,5-bis(trifluoromethyl)phenylamino)-2-(piperazin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
methyl 1-(4-(3,5-bis(trifluoromethyl)phenylamino)-5-oxo-5,6-dihydropyrido[4,3-d]pyrimidin-2-yl)-4-hydroxy piperidine-4-carboxylate;
4-(3,5-bis(trifluoromethyl)phenylamino)-2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-((1R,4R)-4-aminocyclohexylamino)-4-(3,5-bis(trifluoromethyl)phenylamino) pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(3,5-bis(trifluoromethyl)phenylamino)-2-(4-(hydroxyimino)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
(S)-4-(phenoxyphenylamino)-2-(pyrrolidin-3-ylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
2-(4-hydroxypiperidin-1-yl)-4(4-(methylsulfonyl)phenylamino)pyrido[4,3d]pyrimidin-5(6H)-one;
N-(2-((4-(4-(methylsulfonyl)phenylamino)-5-oxo-5,6-dihydropyrido[4,3-d]pyrimidin-2-ylamino)methyl)phenyl)methanesulfonamide;
2-(4-hydroxypiperidin-1-yl)-4-(4-(methyl sulfonyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(4-(methylsulfonyl)phenylamino)-2-(4-morpholinopiperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-hydroxypiperidin-1-yl)-4-(3-(methyl sulfonyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
N-(2-((4-(4-(methylsulfonyl)phenylamino)-5-oxo-5,6-dihydropyrido[4,3-d]pyrimidin-2-yl amino)methyl)phenyl)cyclopropane sulfonamide;
N-methyl-N-(2-((4-(4-(methylsulfonyl)phenylamino)-5-oxo-5,6-dihydropyrido[4,3-d]pyrimidin-2-ylamino)methyl)phenyl)cyclopropanesulfonamide;
(S)-2-(3-aminopyrrolidin-1-yl)-4-(4-(methylsulfonyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-hydroxypiperidin-1-yl)-4-(4-morpholinophenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(4-(4-acetylpiperazin-1-yl)phenylamino)-2-(4-(hydroxymethyl)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
(S)-4-(4-morpholinophenylamino)-2-(pyrrolidin-3-ylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
2-(4-(hydroxymethyl)piperidin-1-yl)-4-(4-sulfonylphenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(4-(4-acetylpiperazin-1-yl)phenylamino)-2-(4-(hydroxymethyl)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-(hydroxymethyl)piperidin-1-yl)-4-(4-morpholinophenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(4-(5-oxo-2-(piperidin-4-ylmethyl amino)-5,6-dihydropyrido[4,3-d]pyrimidin-4-ylamino)phenyl)morpholine 4-oxide hydrochloride;
4-(4-morpholinophenylamino)-2-(piperidin-4-ylmethylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
N-methyl-N-(2-((4-(4-morpholinophenylamino)-5-oxo-5,6-dihydropyrido[4,3-d]pyrimidin-2-ylamino)methyl)phenyl)cyclopropanesulfonamide;
N-(2-((4-(4-morpholinophenylamino)-5-oxo-5,6-dihydropyrido[4,3-d]pyrimidin-2-ylamino)methyl)phenyl)cyclopropanesulfonamide;
N-(2-((4-(4-morpholinophenylamino)-5-oxo-5,6-dihydropyrido[4,3-d]pyrimidin-2-ylamino)methyl)phenyl)methanesulfonamide;
2-(2-aminobenzylamino)-4-(4-morpholinophenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-((1R,2R)-2-aminocyclohexylamino)-4-(4-morpholinophenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-((1R,2S)-2-aminocyclohexylamino)-4-(4-morpholinophenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-((1R,2R)-2-aminocyclohexylamino)-4-(benzo[d][1,3]dioxol-5-ylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-hydroxypiperidin-1-yl)-4-(3,4,5-triemethoxyphenylamino)pyrido[4,3d]pyrimidin-5(6H)-one;
2-(4-hydroxypiperidin-1-yl)-4-(4-methoxy-3-(trifluoromethyl)phenylamino)pyrido[4,3d]pyrimidin-5(6H)-one;
2-(4-(hydroxymethyl)piperidin-1-yl)-4-(4-methoxy-3-(trifluoromethyl)phenylamino) pyrido[4,3d]pyrimidin-5(6H)-one;
2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)-4-(4-methoxy-3-(trifluoromethyl)phenylamino)pyrido[4,3d]pyrimidin-5(6H)-one;
2-(4-hydroxypiperidin-1-yl)-4-(3-methoxy-5-(trifluoromethyl)phenylamino)pyrido[4,3d]pyrimidin-5(6H)-one;
2-(4-(hydroxymethyl)piperidin-1-yl)-4-(3-methoxy-5-(trifluoromethyl)phenylamino) pyrido[4,3d]pyrimidin-5(6H)-one;
2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)-4-(3-methoxy-5-(trifluoromethyl)phenyl amino)pyrido[4,3d]pyrimidin-5(6H)-one;
2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)-4-(3,4,5-trimethoxyphenylamino)pyrido[4,3d]pyrimidin-5(6H)-one;
4-(3,5-dimethylphenylamino)-2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(4-chloro-3-methoxyphenylamino)-2-(4-hydroxypiperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-hydroxypiperidin-1-yl)-4-(3-methoxy-5-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-(hydroxymethyl)piperidin-1-yl)-4-(3-methoxy-5-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)-4-(3-methoxy-5-(trifluoromethyl)phenyl amino)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(4-chloro-3-(trifluoromethyl)phenylamino)-2-(4-hydroxypiperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(4-chloro-3-(trifluoromethyl)phenylamino)-2-(4-(hydroxymethyl)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(4-chloro-3-(trifluoromethyl)phenylamino)-2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one
4-(3-chloro-5-(trifluoromethyl)phenylamino)-2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(3-bromo-5-(trifluoromethyl)phenylamino)-2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(4-chloro-3-(trifluoromethoxy)phenylamino)-2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-hydroxypiperidine-1-yl)-6-methyl-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
6-methyl-4-(phenylamino)-2-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
methyl 4-(6-methyl-2-morpholino-5-oxo-5,6-dihydropyrido[4,3-d]pyrimidin-4-ylamino)benzoate;
6-methyl-2-(methylamino)-4-(4-(piperazine-1-carbonyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
methyl 4-(6-methyl-2-(methylamino)-5-oxo-5,6-dihydropyrido[4,3-d]pyrimidin-4-ylamino)benzoate;
2-amino-6-methyl-4-(phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(4-fluorobenzylamino)-6-methyl-2-(methylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
6-methyl-2-(methylamino)-4-(phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-methoxybenzylamino)-6-methyl-4-(phenyl amino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-hydroxycyclohexylamino)-6-methyl-4-(phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(4-methoxyphenyl)-6-methyl-2-(methylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-(hydroxymethyl)piperidin-1-yl)-4-(4-methoxyphenyl)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(4-methoxyphenyl)-6-methyl-2-(methylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(4-aminophenyl)-6-methyl-2-(methylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
1-(4-fluorophenyl)-3-(4-(6-methyl-2-(methylamino)-5-oxo-5,6-dihydropyrido[4,3-d]pyrimidin-4-yl)phenyl)urea;
8-bromo-2-(4-hydroxypiperidin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
8-bromo-2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)-4-(4-methoxy-3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
8-chloro-2-(4-hydroxypiperidin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
8-bromo-2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)-4-(3-(trifluoromethyl)phenyl amino)pyrido[4,3-d]pyrimidin-5(6H)-one;
(R)-2-(3-aminopyrrolidin-1-yl)-8-bromo-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
(R)-2-(3-aminopyrrolidin-1-yl)-8-bromo-4-(4-bromo-3-methylphenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
8-bromo-2-(4-hydroxypiperidin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
8-bromo-2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)-4-(4-methoxy-3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
8-chloro-2-(4-hydroxypiperidin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
8-bromo-2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)-4-(3-(trifluoromethyl)phenyl amino)pyrido[4,3-d]pyrimidin-5(6H)-one;
(R)-2-(3-aminopyrrolidin-1-yl)-8-bromo-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
(R)-2-(3-aminopyrrolidin-1-yl)-8-bromo-4-(4-bromo-3-methylphenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
8-bromo-2-(4-hydroxypiperidin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
8-bromo-2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)-4-(4-methoxy-3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
8-chloro-2-(4-hydroxypiperidin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-hydroxypiperidin-1-yl)-4-(3-methoxy-5-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-(hydroxymethyl)piperidin-1-yl)-4-(3-methoxy-5-(trifluoromethyl)phenylamino) pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(4-chloro-3-(trifluoromethyl)phenylamino)-2-(4-hydroxypiperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(4-chloro-3-(trifluoromethyl)phenylamino)-2-(4-(hydroxymethyl)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(4-chloro-3-methoxyphenylamino)-2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)-4-(3-methoxy-5-(trifluoromethyl)phenyl amino)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(4-chloro-3-(trifluoromethyl)phenylamino)-2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
8-bromo-2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)-4-(3-(trifluoromethyl)phenyl amino)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(3,4-dimethoxyphenylamino)-2-(4-hydroxypiperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(3-bromo-4-methoxyphenylamino)-2-(4-hydroxypiperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
(R)-2-(3-aminopyrrolidin-1-yl)-8-bromo-4-(4-phenoxyphenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
8-bromo-2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)-4-(4-phenoxyphenyl amino)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(3,4-dimethoxyphenylamino)-2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(3-bromo-4-methoxyphenylamino)-2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-aminopiperidin-1-yl)-8-bromo-4-(4-phenoxyphenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
(R)-2-(3-aminopyrrolidin-1-yl)-8-iodo-4-(4-phenoxyphenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
4-(4-chloro-3-(trifluoromethyl)phenylamino)-2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)-8-iodopyrido[4,3-d]pyrimidin-5(6H)-one;
4-(4-chloro-3-(trifluoromethyl)phenylamino)-2-(4-hydroxypiperidin-1-yl)-8-iodopyrido[4,3-d]pyrimidin-5(6H)-one;
(R)-2-(3-aminopyrrolidin-1-yl)-8-bromo-4-(4-chloro-3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
2-(4-hydroxypiperidin-1-yl)-8-iodo-4-(4-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-hydroxypiperidin-1-yl)-4-(4-morpholino-3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
(R)-2-(3-aminopyrrolidin-1-yl)-8-bromo-4-(4-methoxy-3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
(R)-2-(3-aminopyrrolidin-1-yl)-8-bromo-4-(4-chloro-3-(trifluoromethoxy)phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
4-(4-chloro-3-(trifluoromethoxy)phenylamino)-2-(4-hydroxypiperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(3-bromo-5-(trifluoromethyl)phenylamino)-2-(4-hydroxypiperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
(R)-6-(3-aminopyrrolidin-1-yl)-4-iodo-8-(4-(trifluoromethyl)phenylamino)isoquinolin-1(2H)-one hydrochloride;
(R)-6-(3-aminopyrrolidin-1-yl)-4-bromo-8-(4-(trifluoromethyl)phenylamino)isoquinolin-1(2H)-one hydrochloride;
(S)-6-(3-aminopyrrolidin-1-yl)-4-bromo-8-(4-(trifluoromethyl)phenylamino)isoquinolin-1(2H)-one hydrochloride;
4-(2,3-dihydrobenzo[b][1,4]dioxin-6-ylamino)-2-(4-hydroxypiperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-hydroxypiperidin-1-yl)-4-(naphthalen-2-ylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
2-(4-hydroxypiperidin-1-yl)-4-(quinolin-5-ylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
4-(3H-indol-2-ylamino)-2-(4-hydroxypiperidin-1-yl)pyrido[4,3-d]pyrimidin-5(6H)-one; and
2-(4-hydroxypiperidin-1-yl)-4-(4-phenoxyphenylamino)-8-phenylpyrido[4,3-d]pyrimidin-5(6H)-one;
or a pharmaceutically acceptable salt thereof.

### Claim 57 (depends on 1)

A pharmaceutical formulation comprising a compound of claim 1, or a pharmaceutically acceptable salt thereof, in combination with a pharmaceutically acceptable carrier, diluent or excipient.

### Claim 58 (depends on 1)

A method of treating a protein kinase-mediated disease in a subject in need thereof, comprising administering to said subject a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein said protein kinase-mediated disease is selected from the group of consisting of rheumatoid arthritis, lymphoma, osteosarcoma, melanoma, breast cancer, renal cancer, prostate cancer, colorectal cancer, thyroid cancer, ovarian cancer, pancreatic cancer, neuronal cancer, lung cancer, uterine cancer, and gastrointestinal cancer.

### Claim 59 (depends on 58)

The method of claim 58, wherein said compound or a pharmaceutically acceptable salt thereof is administered singly or in combination with one or more additional therapeutic agents.

### Claim 60 (depends on 59)

The method of claim 59, wherein said compound of or a pharmaceutically acceptable salt thereof is administered via intravenous administration, subcutaneous administration, inhalation, oral administration, rectal administration, parenteral, intravitreal administration, intramuscular administration, intranasal administration, dermal administration, topical administration, otic administration, ophthalmic administration, buccal administration, tracheal administration, bronchial administration, or sublingual administration.

### Claim 61 (depends on 1)

A method of inhibiting growth of cancer cells, comprising contacting the cancer cells with a compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein the cancer cells are cells from a cancer selected from acute lymphoblastic leukemia, acute promyelocytic leukemia, acute myeloid leukemia, chronic myelogenous leukemia, lung cancer, colon cancer, brain cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, or breast cancer.

### Claim 62 (depends on 1)

A method of treating cancer in a subject in need thereof, comprising administering to the subject an effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein said cancer is acute lymphoblastic leukemia, acute promyelocytic leukemia, chronic myelogenous leukemia, lung cancer, colon cancer, brain cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, or breast cancer.

### Claim 63 (depends on 62)

The method of claim 62, wherein said compound is selected from the group consisting of:
2-(4-hydroxypiperidin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d]pyrimidine-5(6H)-one;
(S)-2-(pyrrolidin-3-ylamino)-4-(4-trifluoromethylamino)pyrido[4,3-d]pyrimidin-5(6H)-one;
(S)-4-(4-morpholinophenylamino)-2-(pyrrolidin-3-ylamino)pyrido[4,3-d]pyrimidin-5(6H)-one hydrochloride;
2-(4-(hydroxymethyl)piperidin-1-yl)-4-(4-sulfonylphenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one; and
2-(4-(hydroxymethyl)piperidin-1-yl)-4-(4-morpholinophenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one.