IP Library Granted Patent US 9,382,246
Granted Patent B2
US 9,382,246 · App. 14/559,889 · Granted Jul 5, 2016

Inhibitors of Bruton's tyrosine kinase

View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 9,382,246
App. No.
14/559,889
Granted
Jul 5, 2016
Kind
B2
Abstract

Disclosed herein are reversible and irreversible inhibitors of Bruton's tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are described, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

Claims (280)

1. A compound of Formula (IA) having the structure:

wherein:

ring A is substituted or unsubstituted C 3 -C 6 cycloalkyl, substituted or unsubstituted C 2 -C 7 heterocycloalkyl, substituted or unsubstituted C 6 -C 12 aryl, or substituted or unsubstituted C 1 -C 12 heteroaryl;

Y is optionally present and when present is —CH 2 O—, —OCH 2 —, —OCH 2 CH 2 O—, —O—, —N(R 3 )—, —C(O)—, —N(R 3 )C(O)—, —C(O)N(R 3 )—, —N(R 3 )C(O)N(R 3 )—, —S(O)—, —S(O) 2 —, —N(R 3 )S(O) 2 —, —S(O) 2 N(R 3 )—, —C(═NH)—, —C(═NH)N(R 3 )—, —C(═NH)N(R 3 )—, or substituted or unsubstituted C 1 -C 4 alkylene;

Z is optionally present and when present is substituted or unsubstituted C 1 -C 3 alkyl, substituted or unsubstituted C 3 -C 6 cycloalkyl, substituted or unsubstituted C 2 -C 7 heterocycloalkyl, substituted or unsubstituted C 6 -C 12 aryl, or substituted or unsubstituted C 1 -C 12 heteroaryl;

R 1 is —C(O)R 4 , —C(O)C(O)R 4 , —C(O)N(R 3 )(R 4 ), or —S(O) 2 R 4 ;

each R 2 is independently H, substituted or unsubstituted C 1 -C 4 alkyl, —CN, or halogen;

each R 3 is independently is H, or substituted or unsubstituted C 1 -C 4 alkyl;

each R 4 is independently H, substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted C 3 -C 6 cycloalkyl, substituted or unsubstituted C 2 -C 7 heterocycloalkyl, substituted or unsubstituted C 6 -C 12 aryl, or substituted or unsubstituted C 1 -C 12 heteroaryl;

R 5 is H, substituted or unsubstituted C 1 -C 4 alkyl, substituted or unsubstituted C 3 -C 6 cycloalkyl, substituted or unsubstituted C 2 -C 7 heterocycloalkyl, substituted or unsubstituted C 6 -C 12 aryl, or substituted or unsubstituted C 1 -C 12 heteroaryl; or R 1 and R 5 together with the nitrogen atom to which they are attached are combined to form a substituted or unsubstituted C 2 -C 9 heterocycloalkyl ring;

each R 6 is independently halogen, —CN, —OH, —NH 2 , substituted or unsubstituted C 1 -C 4 alkoxy, substituted or unsubstituted C 1 -C 4 alkyl, substituted or unsubstituted C 3 -C 6 cycloalkyl, substituted or unsubstituted C 2 -C 6 heterocycloalkyl, or —N(R 3 ) 2 ; or R 1 and R 6 are combined to form a substituted or unsubstituted C 2 -C 9 heterocycloalkyl ring;

each R 7 is independently halogen, —CN, —OH, —NH 2 , substituted or unsubstituted C 1 -C 4 alkoxy, substituted or unsubstituted C 1 -C 4 alkyl, substituted or unsubstituted C 3 -C 6 cycloalkyl, substituted or unsubstituted C 2 -C 6 heterocycloalkyl, or —N(R 3 ) 2 ;

n is 0-3;

p is 0-3; and

q is 0-3;

or a pharmaceutically acceptable solvate, or pharmaceutically acceptable salt thereof;

provided that

when n is 0; then each of p and q is independently 0, 1, or 2.

2. A compound of Formula (I) having the structure:

wherein:

ring A is substituted or unsubstituted C 3 -C 6 cycloalkyl, substituted or unsubstituted C 2 -C 7 heterocycloalkyl, substituted or unsubstituted C 6 -C 12 aryl, or substituted or unsubstituted C 1 -C 12 heteroaryl;

Y is optionally present and when present is —CH 2 O—, —OCH 2 —, —OCH 2 CH 2 O—, —O—, —N(R 3 )—, —C(O)—, —N(R 3 )C(O)—, —C(O)N(R 3 )—, —N(R 3 )C(O)N(R 3 )—, —S(O)—, —S(O) 2 —, —N(R 3 )S(O) 2 —, —S(O) 2 N(R 3 )—, —C(═NH)—, —C(═NH)N(R 3 )—, —C(═NH)N(R 3 )—, or substituted or unsubstituted C 1 -C 4 alkylene;

Z is optionally present and when present is substituted or unsubstituted C 1 -C 3 alkyl, substituted or unsubstituted C 3 -C 6 cycloalkyl, substituted or unsubstituted C 2 -C 7 heterocycloalkyl, substituted or unsubstituted C 6 -C 12 aryl, or substituted or unsubstituted C 1 -C 12 heteroaryl;

G is

R 1 is —C(O)(R 4 ), —C(O)N(R 3 )(R 4 ), or —S(O) 2 R 4 ;

each R 2 is independently H, —CN, or halogen;

each R 3 is independently is H, or substituted or unsubstituted C 1 -C 4 alkyl;

each R 4 is independently H, substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted C 3 -C 6 cycloalkyl, substituted or unsubstituted C 2 -C 7 heterocycloalkyl, substituted or unsubstituted C 6 -C 12 aryl, or substituted or unsubstituted C 1 -C 12 heteroaryl;

R 5 is H, substituted or unsubstituted C 1 -C 4 alkyl, substituted or unsubstituted C 3 -C 6 cycloalkyl, substituted or unsubstituted C 2 -C 7 heterocycloalkyl, substituted or unsubstituted C 6 -C 12 aryl, or substituted or unsubstituted C 1 -C 12 heteroaryl; or R 1 and R 5 together with the nitrogen atom to which they are attached are combined to form a substituted or unsubstituted C 2 -C 9 heterocycloalkyl ring;

each R 6 is independently halogen, —CN, —OH, —NH 2 , substituted or unsubstituted C 1 -C 4 alkoxy, substituted or unsubstituted C 1 -C 4 alkyl, substituted or unsubstituted C 3 -C 6 cycloalkyl, substituted or unsubstituted C 2 -C 6 heterocycloalkyl, or —N(R 3 ) 2 ; or R 1 and R 6 are combined to form a substituted or unsubstituted C 2 -C 9 heterocycloalkyl ring;

each R 7 is independently halogen, —CN, —OH, —NH 2 , substituted or unsubstituted C 1 -C 4 alkoxy, substituted or unsubstituted C 1 -C 4 alkyl, substituted or unsubstituted C 3 -C 6 cycloalkyl, substituted or unsubstituted C 2 -C 6 heterocycloalkyl, or —N(R 3 ) 2 ;

p is 0-3; and

q is 0-3;

or a pharmaceutically acceptable solvate, or pharmaceutically acceptable salt thereof.

3. The compound of claim 1 , wherein the compound is of the structure

or a pharmaceutically acceptable solvate, or pharmaceutically acceptable salt thereof.

4. The compound of claim 3 , wherein the compound is of the structure:

or a pharmaceutically acceptable solvate, or pharmaceutically acceptable salt thereof.

5. The compound according to claim 2 , wherein the compound is of Formula (IV) having the structure:

or a pharmaceutically acceptable solvate, or pharmaceutically acceptable salt thereof.

6. The compound of claim 5 , wherein R 6 is Me.

7. The compound of claim 5 , wherein ring A is phenyl.

8. The compound of claim 5 , wherein Y is absent, —CH 2 O—, —OCH 2 —, —O—, —N(R 3 )—, —C(O)—, —N(R 3 )C(O)—, —C(O)N(R 3 )—, or substituted or unsubstituted C 1 -C 4 alkylene.

9. The compound of claim 5 , wherein Z is substituted or unsubstituted C 2 -C 7 heterocycloalkyl, substituted or unsubstituted C 6 -C 12 aryl, or substituted or unsubstituted C 1 -C 12 heteroaryl.

10. The compound of claim 5 , wherein R 1 is —C(O)R 4 .

11. The compound of claim 10 , wherein R 4 is substituted or unsubstituted C 6 -C 12 aryl, or substituted or unsubstituted C 1 -C 12 heteroaryl.

12. The compound of claim 5 , wherein ring A is substituted or unsubstituted C 1 -C 12 heteroaryl.

13. The compound of claim 12 , wherein ring A is pyridyl, pyrazolyl, thiazolyl, isothiazolyl, oxazolyl, or isoxazolyl.

14. The compound of claim 5 , wherein R 1 is —C(O)N(R 3 )(R 4 ).

15. The compound of claim 5 , wherein R 1 is —C(O)N(R 3 )(R 4 ) and R 4 is H, or substituted or unsubstituted C 1 -C 6 alkyl.

16. The compound of claim 5 , wherein R 1 and R 5 together with the nitrogen atom to which they are attached are combined to form a substituted or unsubstituted C 2 -C 9 heterocycloalkyl ring.

17. A compound selected from the group consisting of

5-[(3R)-3-(4-tert-butylbenzamido)piperidin-1-yl]-3-{[4-(morpholine-4-carbonyl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-(4-tert-butylbenzamido)piperidin-1-yl]-3-{[4-(1-methylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-(4-tert-butylbenzamido)piperidin-1-yl]-3-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1-methylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-[(piperidine-1-carbonyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-5-[(3R)-3-[(piperidine-1-carbonyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]-3-{[4-(1-propanoylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-({4-[1-(cyanomethyl)piperidin-4-yl]phenyl}amino)-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]-3-({4-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]phenyl}amino)pyrazine-2-carboxamide;

3-{[3-fluoro-4-(morpholin-4-yl)phenyl]amino}-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]-3-{[4-(3-oxomorpholin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]-3-[(3-methyl-1,2-thiazol-5-yl)amino]pyrazine-2-carboxamide;

3-({4-[2-(dimethylamino)ethoxy]phenyl}amino)-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

(R)-2-(4-(3-carbamoyl-6-(3-(4-methoxybenzamido)piperidin-1-yl)pyrazin-2-ylamino)phenoxy)-N,N-dimethylethanamine oxide;

3-{[4-(dimethylcarbamoyl)phenyl]amino}-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

3-({4-[4-(dimethylcarbamoyl)piperidin-1-yl]phenyl}amino)-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]-3-({4-[1-(propan-2-yl)piperidin-4-yl]phenyl}amino)pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-formylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]-3-{[4-(morpholin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-[(6-ethoxypyridin-3-yl)amino]-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

3-[(4-methanesulfonylphenyl)amino]-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]-3-{[4-(2-oxo-1,2-dihydropyridin-1-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1-methanesulfonylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

3-({4-[1-(2-cyanoacetyl)piperidin-4-yl]phenyl}amino)-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

3-[(4-methanesulfonylphenyl)amino]-5-[(3R)-3-[(piperidine-1-carbonyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(2-ethoxyethoxy)phenyl]amino}-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

3-[(4-ethoxyphenyl)amino]-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]-3-{[4-(oxan-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]-3-{[4-(2-oxopiperidin-1-yl)phenyl]amino}pyrazine-2-carboxamide;

3-({4-[1-(dimethylcarbamoyl)piperidin-4-yl]phenyl}amino)-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[(piperidine-1-carbonyl)amino]piperidin-1-yl]-3-{[4-(1-propanoylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1-acetylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-formylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-[(piperidine-1-carbonyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]-3-{[4-(1-methylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]-3-{[6-(morpholin-4-yl)pyridin-3-yl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]-3-[(quinolin-6-yl)amino]pyrazine-2-carboxamide;

3-[(1,3-benzothiazol-6-yl)amino]-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]-3-[(4-methoxyphenyl)amino]pyrazine-2-carboxamide;

5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]-3-{[4-(2-methoxyethoxy)phenyl]amino}pyrazine-2-carboxamide;

3-({4-[1-(2-cyanoacetyl)piperidin-4-yl]phenyl}amino)-5-[(3R)-3-[(piperidine-1-carbonyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-[(4-methanesulfonylphenyl)amino]pyrazine-2-carboxamide;

3-({4-[1-(2-cyanoacetyl)piperidin-4-yl]phenyl}amino)-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-{[4-(piperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-{[4-(1-propanoylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1-ethylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopropylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-{[4-(1-methylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-{[ethyl(methyl)carbamoyl]amino}piperidin-1-yl]-3-{[4-(1-methylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-[(diethylcarbamoyl)amino]piperidin-1-yl]-3-{[4-(1-methylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-(4-fluorobenzamido)piperidin-1-yl]-3-{[4-(1-methylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-(4-ethoxybenzamido)piperidin-1-yl]-3-{[4-(1-methylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]-3-{[4-(propan-2-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1,1-dioxo-1λ 6 -thiomorpholin-4-yl)phenyl]amino}-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)(methyl)amino]piperidin-1-yl]-3-{[4-(1,1-dioxo-1λ 6 -thiomorpholin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[2-fluoro-4-(piperidin-4-yl)phenyl]amino}-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[3-fluoro-4-(piperidin-4-yl)phenyl]amino}-5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)(methyl)amino]piperidin-1-yl]-3-{[4-(1-propanoylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)(methyl)amino]piperidin-1-yl]-3-({4-[1-(dimethylcarbamoyl)piperidin-4-yl]phenyl}amino)pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)(methyl)amino]piperidin-1-yl]-3-{[4-(1-methanesulfonylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-[(dimethylcarbamoyl)(methyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1,1-dioxo-1λ 6 -thiomorpholin-4-yl)phenyl]amino}-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-{imidazo[1,2-a]pyridine-6-amido}piperidin-1-yl]-3-{[4-(oxan-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-{5-hydroxyimidazo[1,2-a]pyridine-6-amido}piperidin-1-yl]-3-{[4-(oxan-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-(4-methoxybenzamido)piperidin-1-yl]-3-{[4-(piperidin-1-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1-cyclopropylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-{[4-(1,1-dioxo-1λ 6 -thiomorpholin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-ethylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-{[ethyl(methyl)carbamoyl]amino}piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-propanamidopiperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(4-fluorobenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-(phenylamino)pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-{[4-(4-methylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-{[4-(1-ethylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1-cyclopropylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

3-[(4-chlorophenyl)amino]-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-({4-[1-(propan-2-yl)piperidin-4-yl]phenyl}amino)pyrazine-2-carboxamide;

4-[4-({3-carbamoyl-6-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazin-2-yl}amino)phenyl]-1-(propan-2-yl)piperidin-1-ium-1-olate;

3-[(4-chloro-3-methoxyphenyl)amino]-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-[(3-methoxy-4-methylphenyl)amino]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-{[4-(4-methyl-1-propanoylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-({4-[1-(dimethylcarbamoyl)-4-methylpiperidin-4-yl]phenyl}amino)-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentyl-4-methylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(4-cyclopropylpiperazin-1-yl)phenyl]amino}-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-[(4-fluorophenyl)amino]pyrazine-2-carboxamide;

3-{[4-(4-cyclopentylpiperazin-1-yl)phenyl]amino}-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-({4-[(pyridin-2-yl)carbamoyl]phenyl}amino)pyrazine-2-carboxamide;

5-[(3R)-3-{[methyl(phenyl)carbamoyl]amino}piperidin-1-yl]-3-(phenylamino)pyrazine-2-carboxamide;

3-{[2-chloro-4-(piperidin-4-yl)phenyl]amino}-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-({4-[1-(dimethylcarbamoyl)piperidin-4-yl]phenyl}amino)pyrazine-2-carboxamide;

3-{[4-(1-cyclobutylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-({4-[1-(oxan-4-yl)piperidin-4-yl]phenyl}amino)pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-[(4-{1-[2-(2-hydroxyethoxy)ethyl]piperidin-4-yl}phenyl)amino]pyrazine-2-carboxamide;

3-{[4-(1-cyclopropanecarbonylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-{[4-(1-methanesulfonylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

ethyl N-[(3R)-1-(5-carbamoyl-6-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}pyrazin-2-yl)piperidin-3-yl]carbamate;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-[(5-fluoro-6-methylpyridin-2-yl)amino]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-({4-[1-(pyridin-2-yl)piperidin-4-yl]phenyl}amino)pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-{[4-(dimethylcarbamoyl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-{[4-(pyrrolidine-1-carbonyl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-{[4-(1-phenylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1-cyclohexylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-aminopiperidin-1-yl]-3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-formamidopiperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-methanesulfonamidopiperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-ethanesulfonamidopiperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-benzamidopiperidin-1-yl]-3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(pyridine-3-amido)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(5-fluoropyridine-3-amido)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(1-oxo-2,3-dihydro-1H-isoindol-2-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(2-oxopyrrolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-cyclopropaneamidopiperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-({4-[1-(oxetan-3-yl)piperidin-4-yl]phenyl}amino)pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-ethyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(2R,3R)-3-[(dimethylcarbamoyl)amino]-2-methylpiperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(2S,3R)-3-[(dimethylcarbamoyl)amino]-2-methylpiperidin-1-yl]pyrazine-2-carboxamide;

3-({4-[4-methyl-1-(propan-2-yl)piperidin-4-yl]phenyl}amino)-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopropyl-4-methylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-({4-[4-methyl-1-(oxetan-3-yl)piperidin-4-yl]phenyl}amino)-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclobutyl-4-methylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentyl-4-methylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-formyl-4-methylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(4-methyl-1-propanoylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopropanecarbonyl-4-methylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-[(dimethylsulfamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-({4-[1-(dimethylsulfamoyl)piperidin-4-yl]phenyl}amino)pyrazine-2-carboxamide;

5-[(2R,3R)-3-amino-2-methylpiperidin-1-yl]-3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(2S,3R)-3-amino-2-methylpiperidin-1-yl]-3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-aminopiperidin-1-yl]-3-{[4-(1-cyclopropylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-[(4-cyclohexylphenyl)amino]-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyanocyclopentyl)phenyl]amino}-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopropylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-{spiro[3.3]heptane-2-amido}piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopropylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(4-phenylbenzamido)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopropylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(6-phenylpyridine-3-amido)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(2R,3R)-3-benzamido-2-methylpiperidin-1-yl]-3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(2S,3R)-3-benzamido-2-methylpiperidin-1-yl]-3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-(1-benzothiophene-2-amido)piperidin-1-yl]-3-{[4-(1-cyclopropylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-(3-chlorobenzamido)piperidin-1-yl]-3-{[4-(1-cyclopropylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-(4-chlorobenzamido)piperidin-1-yl]-3-{[4-(1-cyclopropylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-(5-chlorothiophene-2-amido)piperidin-1-yl]-3-{[4-(1-cyclopropylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-cyclopentaneamidopiperidin-1-yl]-3-{[4-(1-cyclopropylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1-cyclopropylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(4,5,6,7-tetrahydro-1-benzothiophene-2-amido)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-(5-chloropyridine-3-amido)piperidin-1-yl]-3-{[4-(1-cyclopropylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1-cyclopropylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(naphthalene-2-amido)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopropylpiperidin-4-yl)phenyl]amino}-5-[(2R,3R)-3-[(dimethylcarbamoyl)amino]-2-methylpiperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclobutyl-4-methylpiperidin-4-yl)phenyl]amino}-5-[(2R,3R)-3-[(dimethylcarbamoyl)amino]-2-methylpiperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentyl-4-methylpiperidin-4-yl)phenyl]amino}-5-[(2R,3R)-3-[(dimethylcarbamoyl)amino]-2-methylpiperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyano-1-methylethyl)phenyl]amino}-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-carbamoyl-1-methylethyl)phenyl]amino}-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyanocyclopentyl)phenyl]amino}-5-[(2R,3R)-3-[(dimethylcarbamoyl)amino]-2-methylpiperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-carbamoylcyclopentyl)phenyl]amino}-5-[(2R,3R)-3-[(dimethylcarbamoyl)amino]-2-methylpiperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(4-cyano-1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(4-carbamoyl-1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3 aR,7aR)-1-(dimethylcarbamoyl)-octahydro-1H-pyrrolo[3,2-b]pyridin-4-yl]-3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3 aR,7aR)-1-cyclopropanecarbonyl-octahydro-1H-pyrrolo[3,2-b]pyridin-4-yl]-3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1-cyanocyclopropyl)phenyl]amino}-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-carbamoylcyclopropyl)phenyl]amino}-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(4-cyano-1-cyclobutylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3aR,7aR)-octahydro-1H-pyrrolo[3,2-b]pyridin-4-yl]-3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1-cyclobutylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[3-(3-chlorophenyl)-2-oxoimidazolidin-1-yl]piperidin-1-yl]-3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(2R,3R)-2-methyl-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]-3-{[4-(4-methylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1-cyclobutyl-4-methylpiperidin-4-yl)phenyl]amino}-5-[(2R,3R)-2-methyl-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentyl-4-methylpiperidin-4-yl)phenyl]amino}-5-[(2R,3R)-2-methyl-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]-3-(phenylamino)pyrazine-2-carboxamide;

5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]-3-({4-[1-(trifluoromethyl)cyclopropyl]phenyl}amino)pyrazine-2-carboxamide;

5-[(3aR,7aR)-octahydro-1H-pyrrolo[2,3-c]pyridin-6-yl]-3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-methyl-2-oxo-1,3-diazinan-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopropyl-4-methylpiperidin-4-yl)phenyl]amino}-5-[(2R,3R)-3-[(dimethylcarbamoyl)amino]-2-methylpiperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R,4R)-3-[(dimethylcarbamoyl)amino]-4-methylpiperidin-1-yl]pyrazine-2-carboxamide;

5-[(3 aS,7aR)-1-(dimethylcarbamoyl)-octahydro-1H-pyrrolo[2,3-c]pyridin-6-yl]-3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

5-[(3 aS,7aR)-1-cyclopropanecarbonyl-octahydro-1H-pyrrolo[2,3-c]pyridin-6-yl]-3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1-cyclobutylpiperidin-4-yl)phenyl]amino}-5-[(2R,3R)-3-[(dimethylcarbamoyl)amino]-2-methylpiperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(4-methyl-1-propanoylpiperidin-4-yl)phenyl]amino}-5-[(2R,3R)-2-methyl-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-cyclopropyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-(3-cyclopropyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]-3-{[4-(1-cyclopropyl-4-methylpiperidin-4-yl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1-cyclobutylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-cyclopropyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(4-cyano-1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(2R,3R)-3-[(dimethylcarbamoyl)amino]-2-methylpiperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(4-carbamoyl-1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(2R,3R)-3-[(dimethylcarbamoyl)amino]-2-methylpiperidin-1-yl]pyrazine-2-carboxamide;

5-[(2R,3R)-3-[(dimethylcarbamoyl)amino]-2-methylpiperidin-1-yl]-3-({4-[1-(trifluoromethyl)cyclopropyl]phenyl}amino)pyrazine-2-carboxamide;

3-{[4-(1-cyanocyclopropyl)phenyl]amino}-5-[(2R,3R)-3-[(dimethylcarbamoyl)amino]-2-methylpiperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-carbamoylcyclopropyl)phenyl]amino}-5-[(2R,3R)-3-[(dimethylcarbamoyl)amino]-2-methylpiperidin-1-yl]pyrazine-2-carboxamide;

3-({4-[1-(aminomethyl)cyclopentyl]phenyl}amino)-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-({4-[1-(dimethylcarbamoyl)cyclopropyl]phenyl}amino)pyrazine-2-carboxamide;

5-[(3R)-3-({[3-chloro-5-(trifluoromethyl)phenyl](methyl)carbamoyl}amino)piperidin-1-yl]-3-[(4-fluorophenyl)amino]pyrazine-2-carboxamide;

5-[(3R)-3-({[3-chloro-5-(trifluoromethyl)phenyl](methyl)carbamoyl}amino)piperidin-1-yl]-3-{[4-(1-cyanocyclopropyl)phenyl]amino}pyrazine-2-carboxamide;

3-{[4-(1-carbamoylcyclopropyl)phenyl]amino}-5-[(3R)-3-({[3-chloro-5-(trifluoromethyl)phenyl](methyl)carbamoyl}amino)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopropylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-methyl-2-oxo-1,3-diazinan-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopropyl-4-methylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-methyl-2-oxo-1,3-diazinan-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-[(1-cyclopropyl-1H-pyrazol-4-yl)amino]-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

3-[(1-cyclopentyl-1H-pyrazol-4-yl)amino]-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentyl-4-methylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-methyl-2-oxo-1,3-diazinan-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopropyl-4-methylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-ethyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(2R,3R)-2-methyl-3-(3-methyl-2-oxo-1,3-diazinan-1-yl)piperidin-1-yl]pyrazine-2-carboxamide;

3-({4-[1-(aminomethyl)cyclopropyl]phenyl}amino)-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

3-({4-[(dimethylamino)methyl]phenyl}amino)-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-[(1-methyl-2-oxo-1,2-dihydropyridin-4-yl)amino]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-[(dimethylcarbamoyl)amino]azepan-1-yl]pyrazine-2-carboxamide;

3-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-cyclopropaneamidoazepan-1-yl]pyrazine-2-carboxamide;

3-{[1-(1-cyclopentylazetidin-3-yl)-1H-pyrazol-4-yl]amino}-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

3-{[1-(1-cyclopentylpiperidin-4-yl)-1H-pyrazol-4-yl]amino}-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

3-{[1-(1-cyclopropanecarbonylpiperidin-4-yl)-1H-pyrazol-4-yl]amino}-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

(4aR,8aR)-5-(5-carbamoyl-6-{[4-(1-cyclopentylpiperidin-4-yl)phenyl]amino}pyrazin-2-yl)-N,N-dimethyl-decahydro-1,5-naphthyridine-1-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-[(3-methyl-1,2-thiazol-5-yl)amino]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-[(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)amino]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-{[4-(propan-2-yloxy)phenyl]amino}pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-{[4-(2-methoxyethoxy)phenyl]amino}pyrazine-2-carboxamide;

3-({4-[2-(dimethylamino)ethoxy]phenyl}amino)-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]-3-[(4-nitrophenyl)amino]pyrazine-2-carboxamide;

3-{[4-(1-cyclobutylpiperidin-4-yl)phenyl]amino}-5-[(2R,3R)-3-[(dimethylcarbamoyl)amino]-2-ethylpiperidin-1-yl]pyrazine-2-carboxamide;

3-{[4-(cyclopentyloxy)phenyl]amino}-5-[(3R)-3-[(dimethylcarbamoyl)amino]piperidin-1-yl]pyrazine-2-carboxamide;

5-[(2R,3R)-3-[(dimethylcarbamoyl)amino]-2-methylpiperidin-1-yl]-3-[(3-methyl-1,2-thiazol-5-yl)amino]pyrazine-2-carboxamide;

5-[(2R,3R)-3-[(dimethylcarbamoyl)amino]-2-methylpiperidin-1-yl]-3-{[4-(propan-2-yloxy)phenyl]amino}pyrazine-2-carboxamide;

5-[(2R,3R)-3-[(dimethylcarbamoyl)amino]-2-methylpiperidin-1-yl]-3-[(4-methanesulfonylphenyl)amino]pyrazine-2-carboxamide;

3-(4-(2-methoxyethoxy)phenylamino)-5-((R)-3-(3-((S)-1-phenylethyl)ureido)piperidin-1-yl)pyrazine-2-carboxamide;

3-(4-(2-methoxyethoxy)phenylamino)-5-((R)-3-(3-((R)-1-phenylethyl)ureido)piperidin-1-yl)pyrazine-2-carboxamide;

(R)-3-(4-(1-cyclopentylpiperidin-4-yl)phenylamino)-5-(3-(cyclopropanecarboxamido)-2-methylpiperidin-1-yl)pyrazine-2-carboxamide;

(R)-3-(cyclopropylamino)-5-(3-(3-methyl-3-phenylureido)piperidin-1-yl)pyrazine-2-carboxamide;

(R)-3-(cyclopentylamino)-5-(3-(3-methyl-3-phenylureido)piperidin-1-yl)pyrazine-2-carboxamide;

(R)-5-(3-(3-(3-chloro-5-(trifluoromethyl)phenyl)-3-methylureido)piperidin-1-yl)-3-(cyclopropylamino)pyrazine-2-carboxamide;

(R)-5-(3-(3-(3-chloro-5-(trifluoromethyl)phenyl)-3-methylureido)piperidin-1-yl)-3-(tetrahydro-2H-pyran-4-ylamino)pyrazine-2-carboxamide; and

(R)-5-(3-(3-(tetrahydro-2H-pyran-4-yl)ureido)piperidin-1-yl)-3-(tetrahydro-2H-pyran-4-ylamino)pyrazine-2-carboxamide;

or a pharmaceutically acceptable solvate or pharmaceutically acceptable salt thereof.

18. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 1 , and a pharmaceutically acceptable excipient.

19. The compound of claim 1 , wherein R 1 is —C(O)R 4 , —C(O)N(R 3 )(R 4 ), or —S(O) 2 R 4 .

20. The compound of claim 2 , wherein R 1 is —C(O)R 4 or —C(O)N(R 3 )(R 4 ).

Assignments (5)
CORRECTIVE ASSIGNMENT TO CORRECT THE CONVEYING PARTY DATA PREVIOUSLY RECORDED ON REEL 036126 FRAME 0368. ASSIGNOR(S) HEREBY CONFIRMS THE MERGER AND CHANGE OF NAME. Recorded May 18, 2016
From: PHARMACYCLICS, INC.; OXFORD AMHERST LLC
To: PHARMACYCLICS LLC
Reel/Frame 038742/0371 →
CORRECTIVE ASSIGNMENT TO CORRECT THE CONVEYING PARTY DATA PREVIOUSLY RECORDED ON REEL 036126 FRAME 0359. ASSIGNOR(S) HEREBY CONFIRMS THE MERGER. Recorded May 17, 2016
From: OXFORD AMHERST CORPORATION; PHARMACYCLICS, INC.
To: PHARMACYCLICS, INC.
Reel/Frame 038742/0064 →
MERGER Recorded Jul 16, 2015
From: OXFORD AMHERST CORPORATION
To: PHARMACYCLICS, INC.
Reel/Frame 036126/0359 →
MERGER AND CHANGE OF NAME Recorded Jul 16, 2015
From: PHARMACYCLICS, INC.; OXFORD AMHERST LLC
To: PHARMACYCLICS LLC
Reel/Frame 036126/0368 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 19, 2015
From: ZHAOZHONG, JIA J.; CHEN, WEI; THOMAS, WILLIAM D.
To: PHARMACYCLICS, INC.
Reel/Frame 034983/0734 →