# US 2018/0022753 A1 · Macrocycles as factor xia inhibitors

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- Number: US 2018/0022753 A1
- Document ID: US20180022753A1
- Status: Published application
- Kind: A1
- Application number: 15/718,431
- Filed: 2017-09-28
- Published: 2018-01-25
- Earliest claimed: 2010-02-11
- Assignees: Bristol-Myers Squibb Company
- Applicants: Bristol-Myers Squibb Company
- Inventors: James R. Corte; Tianan Fang; Carl P. Decicco; Donald J.P. Pinto; Karen A. Rossi; Zilun Hu; Yoon Jeon; Mimi L. Quan; Joanne M. Smallheer; Yufeng Wang; Wu Yang
- Web page: https://patentgrep.com/patent/US20180022753A1

## CPC

- C07D 471/08: Bridged systems
- C07D 487/04: Ortho-condensed systems
- C07D 225/08: condensed with two six-membered rings
- C07D 471/14: Ortho-condensed systems
- C07D 471/18: Bridged systems
- C07D 487/06: Peri-condensed systems
- C07D 487/08: Bridged systems
- C07D 487/14: Ortho-condensed systems
- C07D 487/16: Peri-condensed systems
- C07D 487/18: Bridged systems
- C07D 498/04: Ortho-condensed systems
- C07D 498/06: Peri-condensed systems
- C07D 498/08: Bridged systems
- C07D 513/08: Bridged systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective Factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

## Claims

### Claim 1

A compound of Formula (I):
or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, or a solvate thereof, wherein:
ring A is independently a C3-10 carbocycle or a 5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NH, N(C1-4 alkyl), O, and S(O)p;
ring B is independently a benzene ring or a 5- to 6-membered heteroaryl comprising: carbon atoms and 1-4 heteroatoms selected from N, O, and S(O)p;
ring C is independently a benzene ring or a 5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NH, N(C1-4 alkyl), O, and S(O)p;
L1 is independently selected from the group consisting of: a bond, —CHR5—, —CHR5CHR5—, —CR5═CR5—, —C≡C—, —OCH2—, —CHR5NH—, —CH2O—, —SCH2—, —SO2CH2—, —CH2NH—, and —CR5R5—;
L is independently selected from the group consisting of: C3-8 alkylene, C3-8 alkenylene, and C4-8 alkynylene; wherein said alkylene, alkenylene and alkynylene are substituted with 0-2 R7 and optionally one or more of the carbon atoms of said alkylene and alkenylene may be replaced by O, S, NH, N(C1-4 alkyl), CO, CONH, NHCO, OCONH, NHCO2, —NHCONH—, SO2NH, NHSO2, CON(C1-4 alkyl), or N(C1-4 alkyl)CO;
Y is independently selected from the group consisting of: CH2, CH(C1-4 alkyl), C(C1-4 alkyl)2, CO, O, S, NH, N(C1-4 alkyl), N(CO2(C1-4 alkyl)), —N(C1-4 alkyl)CH2—, —N(CO2(C1-4 alkyl))CH2—, —N(CH2CO2(C1-4 alkyl))CH2—, —CONH—, —NHCO—, —CONHCH2—, —CON(C1-4 alkyl)CH2—, —OCONH—, —OCON(C1-4 alkyl)-, —NHCONH—, —SO2NH—, —NHCO2—, and —NHSO2—;
alternatively, L-Y is —C3-6 alkylene-CH═N—;
R1 is, independently at each occurrence, selected from the group consisting of: halogen, C1-6 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 haloalkyl, OH, OCH2F, OCHF2, OCF3, CN, NH2, NH(C1-4 alkyl), N(C1-4 alkyl)2, CO2(C1-4 alkyl), CO(C1-4 alkyl), —CH2NH2, —CONH2, —CONH(C1-4 alkyl), —OCH2CO2H, —NHCO(C1-4 alkyl), —NHCO2(C1-4 alkyl), —NHSO2(C1-4 alkyl), —SO2NH2, —C(═NH)NH2, and phenyl substituted with 0-2 Ra;
R2 is independently a 5- to 7-membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NH, N(C1-4 alkyl), O, and S(O)p, wherein said heterocycle is substituted with 0-2 R2a;
R2a is, independently at each occurrence, selected from the group consisting of: halogen, C1-4 alkyl, —CH2OH, C1-4 alkoxy, OH, CF3, OCF3, CN, NH2, CO2H, CO2(C1-4 alkyl), COC1-4 alkyl, —CONH2, —CONH(C1-4 alkyl), —CON(C1-4 alkyl)2, —SO2(C1-4 alkyl), —SO2NH2, —SO2NH(C1-4 alkyl), and —SO2N(C1-4 alkyl)2;
R3 is independently selected from the group consisting of: H, ═O, halogen, OH, NH2, CN, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, —CH2OH, CO2H, CO2(C1-4 alkyl), —C(O)NH2, —C(O)NH(C1-4 alkyl), —C(O)N(C1-4 alkyl)2, —CH2CO2H, and C3-6 cycloalkyl;
R4 is independently selected from the group consisting of: H, and C1-4 alkyl;
R5 is, independently at each occurrence, selected from the group consisting of: H, halogen, OH, and C1-4 alkyl;
R6 is, independently at each occurrence, selected from the group consisting of: halogen, C1-4 alkyl, CN, OH, CF3, CO2H, CO2(C1-4 alkyl), —CH2CO2H, —(CH2)2CO2H, —CH2CO2(C1-4 alkyl), —(CH2)2CO2(C1-4 alkyl), NH2, —CH2NH2, —NHCO(C1-4 alkyl), —NHCOCF3, —NHCO2(C1-4 alkyl), —NHCO2(CH2)2O(C1-4 alkyl), —NHCO2(CH2)3O(C1-4 alkyl), —NHCO2CH2CH(C1-4 alkyl)O(C1-4 alkyl), —NHCO2(CH2)2OH, —NHCO2(CH2)2NH2, —NHCO2(CH2)2N(C1-4 alkyl)2, —NHCO2CH2CO2H, —CH2NHCO2(C1-4 alkyl), —NHC(O)NH(C1-4 alkyl), —NHC(O)N(C1-4 alkyl)2, —NHSO2(C1-4 alkyl), —SO2NH2, —SO2NH(C1-4 alkyl), —SO2NH(CH2)2OH, —SO2NH(CH2)2O(C1-4 alkyl), —CONH2, —CONH(C1-4 alkyl), —CON(C1-4 alkyl)2, —CH2CONH2, and —NHCO2(CH2)0-2R9;
R7 is, independently at each occurrence, selected from the group consisting of: halogen, OH, NH2, CH2NH2, C1-4 haloalkyl, OCH2F, OCHF2, OCF3, —NH(C1-4 alkyl), —N(C1-4 alkyl)2, C1-4 alkoxy, CH2OH, CH2O(C1-4 alkyl), CH2O(CH2)0-4O(C1-4 alkyl), CO2H, CO2(C1-4 alkyl), CO2(CH2)2O(C1-4 alkyl), CO2(C1-4 haloalkyl), CO2(CH2)2SO2(C1-4 alkyl), CH2CO2H, CH2CO2(C1-4 alkyl), CONH2, CONH(C1-4 alkyl), CON(C1-4 alkyl)2, —OCO(C1-4 alkyl), —CH2NH(CH2)2O(C1-4 alkyl), —CONH(C1-4 alkoxy), —CO2(CH2)2O(C1-4 alkyl), —CO2(CH2)2N(C1-4 alkyl)2, —CONH(CH2)2O(C1-4 alkyl), —CONH(CH2)2N(C1-4 alkyl)2, —CON(C1-4 alkyl)(CH2)2O(C1-4 alkyl), —CON(C1-4 alkyl)(CH2)2N(C1-4 alkyl)2, C1-4 alkyl, —CONHBn, —CONH(OBn), —(CO)0-1(CH2)0-3—C3-6 carbocycle, and —(CH2)0-1—(CO)0-1—(W)0-1-(CH2)0-2—(4- to 6-membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NH, N(C1-4 alkyl), O, and S(O)p); wherein said carbocycle and heterocycle are substituted with 0-2 R8;
R8 is, independently at each occurrence, selected from the group consisting of: halogen, OH, CHF2, CF3, C1-4 alkoxy, CH2OH, CO2H, CO2(C1-4 alkyl), CONH2, and C1-4 alkyl;
R9 is a 4- to 6-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NH, N(C1-4 alkyl), N(CO2(C1-4 alkyl)), O, and S(O)p;
Ra is, independently at each occurrence, selected from the group consisting of: halogen, OH, CF3, C1-4 alkoxy, and C1-4 alkyl;
W is independently selected from the group consisting of: O, NH and N(C1-4 alkyl); and
p is, independently at each occurrence, selected from the group consisting of: 0, 1, and 2.

### Claim 2 (depends on 1)

The compound of claim 1, wherein:
ring A is independently a 6-membered carbocycle, a 9- to 10-membered carbocycle, or a 5- to 10-membered heterocycle comprising: carbon atoms and 1-3 heteroatoms selected from N, NH, N(C1-4 alkyl), O, and S(O)p;
ring B is independently selected from the group consisting of: imidazole, oxazole, oxadiazole, triazole, pyridine, pyridazine, pyrimidine, and benzene; and
ring C is independently selected from the group consisting of: benzene, pyridine, indazole, indole, benzimidazole, quinoline, isoquinoline, tetrahydroquinoline, tetrahydroisoquinoline, and quinazoline.

### Claim 3 (depends on 2)

The compound of claim 2, wherein:
ring A is independently selected from the group consisting of: benzene, cyclohexane, indane, tetrahydronaphthalene, naphthalene, isoxazoline, isoxazole, pyrazole, imidazole, triazole, piperidine, pyridine, indazole, indole, benzimidazole, quinoline, isoquinoline, tetrahydroquinoline, and tetrahydroisoquinoline;
is independently selected from the group consisting of:
is independently selected from the group consisting of:

### Claim 4

A compound of Formula (II):
or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, or a solvate thereof, wherein:
is independently selected from the group consisting of:
L1 is independently selected from the group consisting of: a bond, —CHR5CHR5—, —CR5═CHR5—, —C≡C—, —OCH2—, —CHR5NH—, —CH2O—, —SCH2—, —SO2CH2—, —CH2NH—, and —CR5R5—;
L is independently selected from the group consisting of: C3-8 alkylene and C3-8 alkenylene; wherein said alkylene and alkenylene are substituted with 0-2 R7 and optionally one or two of the carbon atoms of said alkylene and alkenylene may be replaced by O, CO, S, NH, N(C1-4 alkyl), CONH—, NHCO, OCONH, SO2NH, or CON(C1-4 alkyl);
Y is independently selected from the group consisting of: CH2, CO, CH(C1-4 alkyl), C(C1-4 alkyl)2, O, S, NH, N(C1-4 alkyl), N(CO2(C1-4 alkyl)), —N(C1-4 alkyl)CH2—, —N(CO2(C1-4 alkyl))CH2—, —N(CH2CO2(C1-4 alkyl))CH2—, —CONH—, —NHCO—, —CONHCH2—, —CON(C1-4 alkyl)CH2—, —OCONH—, —OCON(C1-4 alkyl)-, —NHCONH—, and —SO2NH—;
alternatively, L-Y is —C3-6 alkylene-CH═N—;
R1 is, independently at each occurrence, selected from the group consisting of: halogen, C1-6 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 haloalkyl, OH, OCH2F, OCHF2, OCF3, CN, NH2, NH(C1-4 alkyl), N(C1-4 alkyl)2, CO2(C1-4 alkyl), CO(C1-4 alkyl), —OCH2CO2H, —CH2NH2, —CONH2, —CONH(C1-4 alkyl), —SO2NH2, and —C(═NH)NH2;
R2 is independently a 5- to 6-membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NH, O, and S(O)p, wherein said heterocycle is substituted with 0-2 R2a;
R2a is, independently at each occurrence, selected from the group consisting of: halogen, C1-4 alkyl, —CH2OH, C1-4 alkoxy, OH, CF3, CN, NH2, CO2H, CO2(C1-4 alkyl), COC1-4 alkyl, —CONH2, —CONH(C1-4 alkyl), and —CON(C1-4 alkyl)2;
R3 is independently selected from the group consisting of: H, halogen, OH, NH2, CN, CF3, C1-4 alkyl, C1-4 alkoxy, —CH2OH, CO2H, CO2(C1-4 alkyl), C(O)NH2, —C(O)NH(C1-4 alkyl), —C(O)N(C1-4 alkyl)2, —CH2CO2H, and C3-6 cycloalkyl;
R4 is independently selected from the group consisting of: H and C1-4 alkyl;
R5 is, independently at each occurrence, selected from the group consisting of: H, halogen, OH, and C1-4 alkyl;
R6 is, independently at each occurrence, selected from the group consisting of: halogen, C1-4 alkyl, CN, OH, CF3, CO2H, CO2(C1-4 alkyl), —CH2CO2H, —(CH2)2CO2H, —CH2CO2(C1-4 alkyl), —(CH2)2CO2(C1-4 alkyl), NH2, —CH2NH2, —NHCO(C1-4 alkyl), —NHCO2(C1-4 alkyl), —NHCO2(CH2)2O(C1-4 alkyl), —NHCO2(CH2)3O(C1-4 alkyl), —NHCO2CH2CH(C1-4 alkyl)O(C1-4 alkyl), —NHCO2(CH2)2OH, —NHCO2(CH2)2NH2, —NHCO2CH2CO2H, —CH2NHCO2(C1-4 alkyl), —NHC(O)NH(C1-4 alkyl), —NHC(O)N(C1-4 alkyl)2, —NHSO2(C1-4 alkyl), —SO2NH(CH2)2OH, —SO2NH(CH2)2O(C1-4 alkyl), —CONH(CH2)2O(C1-4 alkyl), CONH2, CONH(C1-4 alkyl), CON(C1-4 alkyl)2, —CH2CONH2, —NHCO2(CH2)2N(C1-4 alkyl)2, —NHCOCF3, and —NHCO2(CH2)0-1R9;
R7 is, independently at each occurrence, selected from the group consisting of: halogen, OH, C1-4 haloalkyl, C1-4 alkoxy, CH2OH, CH2O(C1-4 alkyl), CO2H, CO2(C1-4 alkyl), CO2(CH2)2O(C1-4 alkyl)), CO2CH2CF3, CO2(CH2)2SO2(C1-4 alkyl), CH2CO2H, CH2CO2(C1-4 alkyl), CONH2, CONH(C1-4 alkyl), CON(C1-4 alkyl)2, —OCO(C1-4 alkyl), —CH2NH(CH2)2O(C1-4 alkyl), —CO2(CH2)2N(C1-4 alkyl)2, —CONH(CH2)2O(C1-4 alkyl), —CONH(CH2)2N(C1-4 alkyl)2, —CON(C1-4 alkyl)(CH2)2O(C1-4 alkyl), —CONH(CH2)2N(C1-4 alkyl)2, —CON(C1-4 alkyl)(CH2)2N(C1-4 alkyl)2, —CONH(C1-4 alkoxy), —CONHBn, —CONH(OBn), —(CH2)1-3Ph, C1-4 alkyl, and —(CH2)0-1—(CO)0-1—(W)0-1—(CH2)0-2—(4- to 6-membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NH, N(C1-4 alkyl), O, and S(O)p); wherein said heterocycle is substituted with 0-2 R8;
R8 is, independently at each occurrence, selected from the group consisting of: halogen, OH, CHF2, CF3, C1-4 alkoxy, and C1-4 alkyl;
R9 is a 4- to 6-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NH, N(C1-4 alkyl), N(CO2(C1-4 alkyl)), O, and S(O)p;
W is independently selected from the group consisting of: O and NH; and
p is, independently at each occurrence, selected from the group consisting of: 0, 1, and 2.

### Claim 5 (depends on 4)

A compound of claim 4 having Formula (IIa) or Formula (IIb):
or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, or a solvate thereof.

### Claim 6 (depends on 4)

The compound of claim 4 having Formula (IIc) or Formula (IId):
or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, or a solvate thereof.

### Claim 7 (depends on 4)

The compound of claim 4 having Formula (IIe) or Formula (IIf):
or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, or a solvate.

### Claim 8 (depends on 1)

The compound of claim 1, wherein:
L1 is independently selected from the group consisting of: a bond, —CH2CH2—, —CH═CH—, —C(Me)=CH—, —C≡C—, and —CH2NH— in Formula (I), (II), (IIa), (IIb), (IIe) or (IIf);
L is independently selected from the group consisting of: C3-7 alkylene and C3-7 alkenylene; wherein said alkylene and alkenylene are substituted with 0-2 R7 and optionally one or two of the carbon atoms of said alkylene and alkenylene may be replaced by O, CO, NH, N(C1-4 alkyl), CONH, NHCO, or CON(C1-4 alkyl);
Y is independently selected from the group consisting of: CH2, CO, CH(C1-4 alkyl), C(C1-4 alkyl)2, O, S, NH, N(C1-4 alkyl), N(CO2(C1-4 alkyl)), —N(C1-4 alkyl)CH2—, —N(CO2(C1-4 alkyl))CH2—, —N(CH2CO2(C1-4 alkyl))CH2—, —CONH—, —NHCO—, —CONHCH2—, —CON(C1-4 alkyl)CH2—, —OCONH—, —NHCONH—, and —SO2NH—;
alternatively, L-Y is —(CH2)3-6—CH═N—;
R1 is, independently at each occurrence, selected from: halogen, CN, OH, OCH2F, OCHF2, OCF3, C1-4 haloalkyl, C1-4 alkyl, C1-4 alkoxy, CO(C1-4 alkyl), NH2, NH(C1-4 alkyl), N(C1-4 alkyl)2, —C(═NH)NH2, —C(O)NH2, —CH2NH2, and —SO2NH2;
R3 is independently selected from the group consisting of: H, halogen, OH, NH2, CN, CF3, C1-4 alkyl, C1-4 alkoxy, —CH2OH, CO2H, CO2(C1-4 alkyl), C(O)NH2, —C(O)NH(C1-4 alkyl), —C(O)N(C1-4 alkyl)2, —CH2CO2H, and C3-6 cycloalkyl; and
R6 is, independently at each occurrence, selected from the group consisting of: halogen, C1-4 alkyl, CN, OH, CF3, CO2H, CO2(C1-4 alkyl), —CH2CO2H, —(CH2)2CO2H, —CH2CO2(C1-4 alkyl), —(CH2)2CO2(C1-4 alkyl), NH2, —CH2NH2, —NHCO(C1-4 alkyl), —NHCO2(C1-4 alkyl), —NHCO2(CH2)2O(C1-4 alkyl), —NHCO2(CH2)3O(C1-4 alkyl), —NHCO2CH2CH(C1-4 alkyl)O(C1-4 alkyl), —NHCO2(CH2)2OH, —NHCO2(CH2)2NH2, —NHCO2CH2CO2H, —CH2NHCO2(C1-4 alkyl), —NHC(O)NH(C1-4 alkyl), —NHC(O)N(C1-4 alkyl)2, —NHSO2(C1-4 alkyl), —SO2NH(CH2)2OH, —SO2NH(CH2)2O(C1-4 alkyl), CONH2, CONH(C1-4 alkyl), CON(C1-4 alkyl)2, —NHCO2(CH2)2N(C1-4 alkyl)2, —NHCOCF3, and —NHCO2(CH2)0-1R9.

### Claim 9 (depends on 1)

The compound of claim 1, wherein:
L1 is independently selected from the group consisting of: a bond, —CH2CH2— and —CH═CH— in Formula (I), (II), (IIa), (IIb), (IIe) or (IIf);
R1 is, independently at each occurrence, selected from the group consisting of: halogen, CN, C1-4 alkyl, OH, C1-4 alkoxy, CH2F, CHF2, CF3, OCH2F, OCHF2, OCF3, CO(C1-4 alkyl), NH2, NH(C1-4 alkyl)2, N(C1-4 alkyl)2, —CH2NH2, and —C(═NH)NH2;
R3 is independently selected from the group consisting of: H, halogen, CN, CF3, CO2H, CO2(C1-4 alkyl), C1-4 alkyl, CONH2, CON(C1-4 alkyl)2, and C3-6 cycloalkyl; and
R6 is, independently at each occurrence, selected from the group consisting of: halogen, C1-4 alkyl, CN, OH, CF3, CO2H, CO2(C1-4 alkyl), —CH2CO2H, —CH2CO2(C1-4 alkyl), NH2, —CH2NH2, —NHCO(C1-4 alkyl), —NHCO2(C1-4 alkyl), —CH2NHCO2(C1-4 alkyl), —CONH2, CONH(C1-4 alkyl), CON(C1-4 alkyl)2, —NHCO2(CH2)2OH, —NHCO2(CH2)2O(C1-4 alkyl), —NHCO2CH2CO2H, —NHCO2CH2CH(C1-4 alkyl)O(C1-4 alkyl), —NHCO2(CH2)2N(C1-4 alkyl)2, —NHCOCF3,

### Claim 10 (depends on 1)

The compound of claim 1, wherein:
L1 is independently selected from the group consisting of: a bond and —CH═CH— in Formula (I), (II), (IIa), (IIb), (IIe) or (IIf);
L is independently selected from the group consisting of: —(CH2)3-6—, —(CH2)2-4CH(C1-4 alkyl)(CH2)0-2—, —(CH2)1-2—CH═CH—(CH2)O3—, —CH2—CH═C(C1-4 alkyl)-(CH2)1-2—, —CH2—C(C1-4 alkyl)=CH—(CH2)1-2—, —CH2—CH═CH—CH2CH(C1-4 alkyl)-, —CH2—CH═CH—CH(C1-4 alkyl)-(CH2)0-2—, —CH2—CH═CH—CH2C(halo)2-, —CH2—CH═CH—(CH2)1-2CH(CF3)—, —CH2—CH═CH—CH(OH)CH2—, —(CH2)3CH(halo)-, —(CH2)3-4C(halo)2-, —(CH2)4CH(CH2OH)—, —(CH2)3-4CH(C1-4 alkoxy)-, —(CH2)4CH(CH2(C1-4 alkoxy))-, —(CH2)4CH(CO2H)—, —(CH2)4CH(CH2CO2H)—, —(CH2)4-5CH(CO2(C1-4 alkyl))-, —(CH2)4CH(CH2CO2(C1-4 alkyl))-, —(CH2)4CH(CO2CH2CF3)—, —(CH2)4CH(CO2(CH2)2SO2(C1-4 alkyl))-, —(CH2)4C(C1-4 alkyl)(CO2(C1-4 alkyl))-, —(CH2)4C(CF3)(CO2(C1-4 alkyl))-, —(CH2)4CH(CONH2))—, —(CH2)4CH(CONH(C1-4 alkyl))-, —(CH2)4CH(CON(C1-4 alkyl)2)-, —(CH2)3CH(C1-4 alkyl)CH(CONH2)—, —(CH2)4CH(CO2(CH2)2O(C1-4 alkyl))-, —(CH2)4CH(CH2NH(CH2)2O(C1-4 alkyl))-, —(CH2)4CH(CONH(C1-4 alkoxy))-, —(CH2)4CH(CONH(OBn))-, —(CH2)4CH((CH2)3Ph)-, —(CH2)4CH(CO2(CH2)2N(C1-4 alkyl)2)-, —(CH2)4CH(CONH(CH2)2O(C1-4 alkyl))-, —(CH2)4CH(CONH(CH2)2N(C1-4 alkyl)2)-, —(CH2)4CH(CON(C1-4 alkyl)(CH2)2O(C1-4 alkyl))-, —(CH2)4CH(CON(C1-4 alkyl)(CH2)2N(C1-4 alkyl)2)-, —(CH2)4CH(CH(halo)2)-, —(CH2)4-5CH(CF3)—, —(CH2)3C(halo)2CH2—, —(CH2)—CH(OH)(CH2)1-2—, —CH2CH(OH)CH(OH)CH2—, —(CH2)3CH(OCO(C1-4 alkyl))CH2—, —(CH2)3C(O)CH2—, —CH2O(CH2)2-4—, —CH2NH(CH2)2-4—, (CH2)2-3NH(CH2)1-2—(CH2)2-4N(C1-4 alkyl)(CH2)0-2—, —CH2CONH(CH2)2-4, —CH2CON(C1-4 alkyl)(CH2)2-4—, —CH2NHCOC(halo)2CH2—, —(CH2)4CH(3-C1-4 alkyl-oxetan-3-yl)-, —(CH2)4CH(thiazol-4-yl)-, —(CH2)4CH(4-C1-4 alkyl-thiazol-2-yl)-, —(CH2)4CH(1-C1-4 alkyl-imidazol-2-yl)-, —(CH2)4CH(1-C1-4 alkyl-pyrazol-3-yl)-, —(CH2)4CH(1-C1-4 alkyl-pyrazol-5-yl)-, —CH2—CH═CH—CH2CH(1-C1-4 alkyl-pyrazol-5-yl)-, —(CH2)4CH(1-C1-4 alkyl-3-C1-4 alkyl-pyrazol-5-yl)-, —(CH2)4CH(1-C1-4 alkyl-4-halo-pyrazol-3-yl)-,
Y is independently selected from the group consisting of: CH2, CO, O, NH, N(C1-4 alkyl), N(CO2(C1-4 alkyl)), —N(C1-4 alkyl)CH2—, —N(CO2(C1-4 alkyl))CH2—, —N(CH2CO2(C1-4 alkyl))CH2—, —CONH—, —NHCO—, —CONHCH2—, —CON(C1-4 alkyl)CH2—, —OCONH—, —NHCONH—, and —SO2NH—; and
alternatively, L-Y is —(CH2)3-6—CH═N—;
R1 is, independently at each occurrence, selected from the group consisting of: halogen, C1-4 alkyl, OH, C1-4 alkoxy, CO(C1-4 alkyl), CN, CH2F, CHF2, CF3, OCHF2, NH2, N(C1-4 alkyl)2, —CH2NH2, and —C(═NH)NH2;
R3 is independently selected from the group consisting of: H, halogen, C1-4 alkyl, CN, CO2(C1-4 alkyl), CONH2, CON(C1-4 alkyl)2, and C3-6 cycloalkyl; and
R6 is, independently at each occurrence, selected from the group consisting of: halogen, NH2, CO2H, CO2(C1-4 alkyl), CONH2, CONH(C1-4 alkyl), CON(C1-4 alkyl)2, —NHCO2(C1-4 alkyl), —CH2NHCO2(C1-4 alkyl), —NHCO2CH2CO2H, —NHCO2(CH2)2OH, —NHCO2(CH2)2O(C1-4 alkyl), —NHCO2CH2CH(C1-4 alkyl)O(C1-4 alkyl), —NHCO2(CH2)2N(C1-4 alkyl)2, —NHCOCF3,

### Claim 11

A compound of Formula (III) or Formula (IIIa):
or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, or a solvate thereof, wherein:
L1 is independently selected from the group consisting of: a bond and —CH═CH— in Formula (IIIa);
L is independently selected from the group consisting of: —(CH2)3—, —(CH2)4—, —(CH2)5—, —(CH2)6—, —(CH2)3CH(C1-4 alkyl)-, —(CH2)4CH(C1-4 alkyl)-, —(CH2)2CH(C1-4 alkyl)CH2—, —(CH2)3CH(C1-4 alkyl)CH2—, —(CH2)2CH(C1-4 alkyl)(CH2)2—, —(CH2)3CH(C1-4 alkyl)(CH2)2—, —(CH2)4CH(C1-4 alkyl)CH2—, —(CH2)4CH(C1-4 alkyl)(CH2)2—, —(CH2)2—CH═CH—, —CH2—CH═CH—CH2—, —CH2—CH═CH—(CH2)2—, —CH2—CH═CH—(CH2)3—, —CH2—CH═C(C1-4 alkyl)-(CH2)2—, —CH2—CH═CH—CH2CH(C1-4 alkyl)-, —CH2—CH═CH—CH(C1-4 alkyl)CH2—, —CH2—CH═CH—CH2C(halo)2-, —CH2—CH═CH—CH2CH(CF3)—, —CH2—CH═CH—(CH2)2CH(CF3)—, —CH2—CH═CH—CH(OH)CH2—, —(CH2)3CH(halo)-, —(CH2)3C(halo)2-, —(CH2)4C(halo)2-, —(CH2)4CH(CH2OH)—, —(CH2)3CH(C1-4 alkoxy)-, —(CH2)4CH(CH2(C1-4 alkoxy))-, —(CH2)4CH(CO2H)—, —(CH2)4CH(CH2CO2H)—, —(CH2)4CH(CO2(C1-4 alkyl))-, —(CH2)4CH(CH2CO2(C1-4 alkyl))-, —(CH2)4CH(CO2CH2CF3)—, —(CH2)4CH(CO2(CH2)2SO2(C1-4 alkyl))-, —(CH2)5CH(CO2(C1-4 alkyl))-, —(CH2)4C(C1-4 alkyl)(CO2(C1-4 alkyl))-, —(CH2)4C(CF3)(CO2(C1-4 alkyl))-, —(CH2)4CH(CONH2)—, —(CH2)4CH(CONH(C1-4 alkyl))-, —(CH2)4CH(CON(C1-4 alkyl)2)-, —(CH2)3CH(C1-4 alkyl)CH(CONH2)—, —(CH2)4CH(CONH(C1-4 alkoxy))-, —(CH2)4CH(CONH(OBn))-, —(CH2)4CH((CH2)3Ph)-, —(CH2)4CH(CON(C1-4 alkyl)(CH2)2O(C1-4 alkyl))-, —(CH2)4CH(CON(C1-4 alkyl)(CH2)2N(C1-4 alkyl)2)-, —(CH2)4CH(CH(halo)2)-, —(CH2)4CH(CF3)—, —(CH2)5CH(CF3)—, —(CH2)3C(halo)2CH2—, —CH2CH(OH)(CH2)2—, —(CH2)2CH(OH)CH2—, —(CH2)3CH(OH)CH2—, —CH2CH(OH)CH(OH)CH2—, —(CH2)3CH(OCO(C1-4 alkyl))CH2—, —(CH2)3C(O)CH2—, —CH2O(CH2)3—, —CH2O(CH2)4—, —CH2NH(CH2)2—, —CH2NH(CH2)3—, —CH2NH(CH2)4—, —(CH2)2N(C1-4 alkyl)CH2—, —(CH2)2N(C1-4 alkyl)(CH2)2—, —CH2CONH(CH2)2—, —CH2CONH(CH2)3—, —CH2CONH(CH2)4—, —CH2CON(C1-4 alkyl)(CH2)2—, —CH2CON(C1-4 alkyl)(CH2)3—, —(CH2)4CH(thiazol-4-yl)-, —(CH2)4CH(4-C1-4 alkyl-thiazol-2-yl)-, —(CH2)4CH(1-C1-4 alkyl-imidazol-2-yl)-, —(CH2)4CH(1-C1-4 alkyl-pyrazol-3-yl)-, —(CH2)4CH(1-C1-4 alkyl-pyrazol-5-yl)-, —CH2—CH═CH—CH2CH(1-C1-4 alkyl-pyrazol-5-yl)-, —(CH2)4CH(1-C1-4 alkyl-3-C1-4 alkyl-pyrazol-5-yl)-,
Y is independently selected from the group consisting of: CH2, CO, O, NH, N(C1-4 alkyl), N(CO2(C1-4 alkyl)), —N(C1-4 alkyl)CH2—, —N(CO2(C1-4 alkyl))CH2—, —N(CH2CO2(C1-4 alkyl))CH2—, —CONH—, —NHCO—, —CONHCH2—, —CON(C1-4 alkyl)CH2—, —OCONH—, —NHCONH—, and —SO2NH—;
alternatively, L-Y is —(CH2)4—CH═N—;
R1 is, independently at each occurrence, selected from the group consisting of: halogen, C1-4 alkyl, OH, C1-4 alkoxy, CO(C1-4 alkyl), CN, CH2F, CHF2, CF3, OCHF2, NH2, N(C1-4 alkyl)2, —CH2NH2, and —C(═NH)NH2 in Formula (IIIa);
R1b is independently selected from the group consisting of: H and halogen in Formula (III);
R2 is independently a 5-membered heterocycle selected from: triazolyl and tetrazolyl in Formula (IIIa);
R3 is independently selected from the group consisting of: H, halogen, C1-4 alkyl, CN, CO2(C1-4 alkyl), CONH2, CON(C1-4 alkyl)2, and C3-6 cycloalkyl; and
R6 is independently selected from the group consisting of: halogen, NH2, CO2H, CONH2, CO2(C1-4 alkyl), —NHCO2(C1-4 alkyl), —NHCO2(CH2)2OH, —NHCO2(CH2)2O(C1-4 alkyl), —NHCO2CH2CO2H, —NHCO2CH2CH(C1-4 alkyl)O(C1-4 alkyl), —NHCO2(CH2)2N(C1-4 alkyl)2, —NHCOCF3,

### Claim 12 (depends on 11)

The compound of claim 11, wherein:
L is independently selected from the group consisting of: —(CH2)4—, —(CH2)5—, —(CH2)6—, —(CH2)3CH(C1-4 alkyl)-, —(CH2)4CH(C1-4 alkyl)-, —(CH2)2CH(C1-4 alkyl)CH2—, —(CH2)3CH(C1-4 alkyl)CH2—, —(CH2)2CH(C1-4 alkyl)(CH2)2—, —(CH2)3CH(C1-4 alkyl)(CH2)2—, —(CH2)4CH(C1-4 alkyl)CH2—, —(CH2)4CH(C1-4 alkyl)(CH2)2—, —(CH2)2—CH═CH—, —CH2—CH═CH—CH2—, —CH2CH═CH—(CH2)2—, —CH2—CH═CH—(CH2)3—, —CH2—CH═C(C1-4 alkyl)-(CH2)2—, —CH2—CH═CH—CH2CH(C1-4 alkyl)-, —CH2—CH═CH—CH(C1-4 alkyl)CH2—, —CH2—CH═CH—CH2C(halo)2-, —CH2—CH═CH—CH2CH(CF3)—, —CH2—CH═CH—(CH2)2CH(CF3)—, —CH2—CH═CH—CH(OH)CH2—, —(CH2)3CH(halo)-, —(CH2)3C(halo)2-, —(CH2)4C(halo)2-, —(CH2)4CH(CH2OH)—, —(CH2)4CH(CH2(C1-4 alkoxy))-, —(CH2)3CH(C1-4 alkoxy)-, —(CH2)4CH(C1-4 alkoxy)-, —(CH2)4CH(CO2H)—, —(CH2)4CH(CH2CO2H)—, —(CH2)4CH(CO2(C1-4 alkyl))-, —(CH2)4CH(CH2CO2(C1-4 alkyl))-, —(CH2)4CH(CO2CH2CF3)—, —(CH2)4CH(CO2(CH2)2SO2(C1-4 alkyl))-, —(CH2)5CH(CO2(C1-4 alkyl))-, —(CH2)4C(C1-4 alkyl)(CO2(C1-4 alkyl))-, —(CH2)4C(CF3)(CO2(C1-4 alkyl))-, —(CH2)4CH(CONH2)—, —(CH2)4CH(CONH(C1-4 alkyl))-, —(CH2)4CH(CON(C1-4 alkyl)2)-, —(CH2)3CH(C1-4 alkyl)CH(CONH2)—, —(CH2)4CH(CONH(C1-4 alkoxy))-, —(CH2)4CH(CONH(OBn))-, —(CH2)4CH(CON(C1-4 alkyl)(CH2)2O(C1-4 alkyl))-, —(CH2)4CH(CON(C1-4 alkyl)(CH2)2N(C1-4 alkyl)2)-, —(CH2)4CH(CH(halo)2)-, —(CH2)4CH(CF3)—, —(CH2)5CH(CF3)—, —(CH2)3C(halo)2CH2—, —CH2CH(OH)(CH2)2—, —(CH2)2CH(OH)CH2—, —(CH2)3CH(OH)CH2—, —CH2CH(OH)CH(OH)CH2—, —(CH2)3CH(OCO(C1-4 alkyl))CH2—, —(CH2)3C(O)CH2—, —CH2O(CH2)3—, —CH2O(CH2)4—, —CH2NH(CH2)2—, —CH2NH(CH2)3—, —CH2NH(CH2)4—, —(CH)2N(C1-4alkyl)CH2—, —(CH2)2N(C1-4 alkyl)(CH2)2—, —CH2CONH(CH2)2—, —CH2CONH(CH2)3—, —CH2CONH(CH2)4—, —CH2CON(C1-4alkyl)(CH2)2—, —CH2CON(C1-4 alkyl)(CH2)3—, —(CH2)4CH(thiazol-4-yl)-, —(CH2)4CH(4-C1-4 alkyl-thiazol-2-yl)-, —(CH2)4CH(1-C1-4 alkyl-imidazol-2-yl)-, —(CH2)4CH(1-C1-4 alkyl-pyrazol-3-yl)-, —(CH2)4CH(1-C1-4 alkyl-pyrazol-5-yl)-, —CH2—CH═CH—CH2CH(1-C1-4 alkyl-pyrazol-5-yl)-, —(CH2)4CH(1-C1-4 alkyl-3-C1-4 alkyl-pyrazol-5-yl)-, —(CH2)4CH(1-C1-4 alkyl-4-halo-pyrazol-3-yl)-,
Y is independently selected from the group consisting of: CH2, O, NH, —CONH—, —NHCO—, —CONHCH2—, —CON(C1-4 alkyl)CH2—, —N(C1-4 alkyl)CH2—, —N(CO2(C1-4 alkyl))CH2—, —N(CH2CO2(C1-4 alkyl))CH2—, —OCONH—, —NHCONH—, and —SO2NH—;
alternatively, L-Y is —(CH2)4—CH═N—; and
R6 is independently selected from the group consisting of: halogen, NH2, CO2H, CONH2, —NHCO2(C1-4 alkyl), —NHCO2(CH2)2OH, —NHCO2(CH2)2O(C1-4 alkyl), —NHCO2CH2CH(C1-4 alkyl)O(C1-4 alkyl), —NHCO2CH2CO2H,

### Claim 13 (depends on 11)

The compound of claim 11 having Formula (III), wherein:
L-Y is independently selected from the group consisting of: —(CH2)6—, —(CH2)7—, —(CH2)4CH(CO2H)CH2—, —(CH2)4CH(CO2(C1-4 alkyl))CH2—, —(CH2)4CH(CONH2)CH2—, —(CH2)4CH(CONH(C1-4 alkyl))CH2—, —(CH2)4CH(CON(C1-4 alkyl)2)CH2—, —(CH2)4CF2CO—, —CH2—CH═CH—(CH2)3—, —CH2—CH═CH—(CH2)4—, —CH2CON(C1-4 alkyl)(CH2)3—, —CH2CON(C1-4 alkyl)(CH2)4—, —(CH2)4N(C1-4 alkyl)CH2—, —(CH2)4N(CO2(C1-4 alkyl))CH2—, —(CH2)4N(CH2CO2(C1-4 alkyl))CH2—, —(CH2)5O—, —(CH2)6O—, —(CH2)3CH(C1-4 alkyl)(CH2)2O—, —(CH2)4CH(C1-4 alkyl)CH2O—, —CH2CONH(CH2)2O—, —CH2NH(CH2)4O—, —CH2—CH═CH—(CH2)2O—, —CH2—CH═CH—(CH2)3O—, —(CH2)5NH—, —(CH2)6NH—, —(CH2)3CH(C1-4 alkyl)CH2NH—, —(CH2)4CH(C1-4 alkyl)NH—, —(CH2)4CH(C1-4 alkyl)CH2NH—, —(CH2)4CH(CH2OH)NH—, —(CH2)4CH(CH2(C1-4alkoxy))NH—, —(CH2)4CH(CO2H)NH—, —(CH2)4CH((CH2)3Ph)NH—, —(CH2)4CH(CH2CO2H)NH—, —(CH2)4CH(CH2CO2(C1-4 alkyl))NH—, —(CH2)4CH(CO2(C1-4 alkyl))NH—, —(CH2)4CH(CO2CH2CF3)NH—, —(CH2)4CH(CO2(CH2)2SO2(C1-4 alkyl))NH—, —(CH2)5CH(CO2(C1-4 alkyl))NH—, —(CH2)4CH(CONH2)NH—, —(CH2)4CH(CONH(C1-4 alkyl))NH—, —(CH2)4CH(CON(C1-4 alkyl)2)NH—, —(CH2)4C(C1-4 alkyl)(CO2(C1-4 alkyl))NH—, —(CH2)4C(CF3)(CO2(C1-4 alkyl))NH—, —(CH2)3CH(C1-4 alkyl)CH(CONH2)NH—, —(CH2)4CH(CONH(C1-4 alkoxy))NH—, —(CH2)4CH(CONH(OBn))NH—, —(CH2)4CH(CON(C1-4 alkyl)(CH2)2O(C1-4 alkyl))NH—, —(CH2)4CH(CON(C1-4 alkyl)(CH2)2N(C1-4 alkyl)2)NH—, —CH2—CH═CH—(CH2)2NH—, —CH2—CH═CH—(CH2)3NH—, —(CH2)4CH(CHF2)NH—, —(CH2)4CH(CF3)NH—, —(CH2)5CH(CF3)NH—, —(CH2)3CF2CH2NH—, —CH2—CH═CH—CH2CH(CF3)NH—, —CH2—CH═CH—(CH2)2CH(CF3)NH—, —CH2CONH(CH2)2NH—, —CH2CONH(CH2)3NH—, —CH2NHCOCF2CH2NH—, —CH2CONH(CH2)4NH—, —(CH2)4CH(CO-pyrrolidin-1-yl)NH—, —(CH2)4CH(thiazol-4-yl)NH—, —(CH2)4CH(4-C1-4 alkyl-thiazol-2-yl)NH—, —(CH2)4CH(1-C1-4 alkyl-imidazol-2-yl)NH—, —(CH2)4CH(1-C1-4 alkyl-pyrazol-3-yl)NH—, —(CH2)4CH(1-C1-4 alkyl-pyrazol-5-yl)NH—, —(CH2)4CH(1-C1-4 alkyl-3-C1-4 alkyl-pyrazol-5-yl)NH—, —(CH2)4CH(1-C1-4 alkyl-4-halo-pyrazol-3-yl)NH—, —CH2—CH═CH—CH2CH(1-C1-4 alkyl-pyrazol-5-yl)NH—, —(CH2)6N(C1-4 alkyl)-, —(CH2)5N(CO2(C1-4 alkyl))-, —(CH2)4CONH—, —(CH2)5CONH—, —(CH2)6CONH—, —(CH2)3CH(C1-4 alkyl)CONH—, —(CH2)4CH(C1-4 alkyl)CONH—, —(CH2)2CH(C1-4 alkyl)CH2CONH—, —(CH2)3CH(C1-4 alkyl)CH2CONH—, —(CH2)2CH(C1-4 alkyl)(CH2)2CONH—, —(CH2)2—CH═CH—CONH—, —CH2—CH═CH—CH2CONH—, —CH2—CH═CH—(CH2)2CONH—, —CH2—CH═CH—(CH2)3CONH—, —CH2—CH═CH—CH2CH(C1-4 alkyl)CONH—, —CH2—CH═CH—CH(C1-4 alkyl)CH2CONH—, —CH2—CH═C(C1-4 alkyl)(CH2)2CONH—, —(CH2)3CH(C1-4 alkyl)CONH—, —(CH2)3CHFCONH—, —(CH2)3CF2CONH—, —(CH2)4CF2CONH—, —CH2—CH═CH—CH2CF2CONH—, —(CH2)3CH(CF3)CONH—, —CH2CH(OH)(CH2)2CONH—, —(CH2)2CH(OH)CH2CONH—, —(CH2)3CH(OH)CH2CONH—, —CH2CH(OH)CH(OH)CH2CONH—, —CH2—CH═CH—CH(OH)CH2CONH—, —(CH2)3CH(C1-4 alkoxy)CONH—, —(CH2)3CH(OCO(C1-4 alkyl))CH2CONH—, —(CH2)3C(O)CH2CONH—, —CH2O(CH2)3CONH—, —CH2O(CH2)4CONH—, —CH2NH(CH2)2CONH—, —CH2NH(CH2)3CONH—, —(CH2)2N(C1-4 alkyl)CH2CONH—, —(CH2)2N(C1-4 alkyl)(CH2)2CONH—, —(CH2)5NHCO—, —CH2—CH═CH—(CH2)2NHCO—, —(CH2)30CONH—, —(CH2)40CONH—, —CH2—CH═CH—CH2OCONH—, —CH2—CH═CH—CH2NHCONH—, —(CH2)4SO2NH—, —CH2—CH═CH—CH2SO2NH—, —(CH2)4—CH═N—,
R1b is independently selected from the group consisting of: H and halogen;
R3 is independently selected from the group consisting of: H, halogen, C1-4 alkyl, CN, CO2(C1-4 alkyl), CONH2, CON(C1-4 alkyl)2, and C3-6 cycloalkyl; and
R6 is independently selected from the group consisting of: halogen, NH2, CO2H, CONH2, —NHCO2(C1-4 alkyl), —NHCO2(CH2)2OH, —NHCO2(CH2)2O(C1-4 alkyl), —NHCO2CH2CH(C1-4 alkyl)O(C1-4 alkyl),

### Claim 14 (depends on 11)

The compound of claim 11 having Formula (III), wherein:
L-Y is independently selected from the group consisting of: —(CH2)6—, —(CH2)7—, —(CH2)4CH(CO2H)CH2—, —(CH2)4CH(CO2(C1-4 alkyl))CH2—, —(CH2)4CH(CONH2)CH2—, —(CH2)4CH(CONH(C1-4 alkyl))CH2—, —(CH2)4CH(CON(C1-4 alkyl)2)CH2—, —CH2—CH═CH—(CH2)3—, —CH2—CH═CH—(CH2)4—, —CH2CON(C1-4 alkyl)(CH2)3—, —(CH2)5O—, —(CH2)6O—, —(CH2)3CH(C1-4 alkyl)(CH2)2O—, —(CH2)4CH(C1-4 alkyl)CH2O—, —CH2NH(CH2)4O—, —CH2—CH═CH—(CH2)3O—, —(CH2)5NH—, —(CH2)6NH—, —(CH2)3CH(C1-4 alkyl)CH2NH—, —(CH2)4CH(C1-4 alkyl)NH—, —(CH2)4CH(C1-4 alkyl)CH2NH—, —(CH2)4CH(CH2OH)NH—, —(CH2)4CH(CH2(C1-4 alkoxy))NH—, —(CH2)4CH(CO2H)NH—, —(CH2)4CH(CH2CO2H)NH—, —(CH2)4CH(CH2CO2(C1-4 alkyl))NH—, —(CH2)4CH(CO2(C1-4 alkyl))NH—, —(CH2)4CH(CO2CH2CF3)NH—, —(CH2)4CH(CO2(CH2)2SO2(C1-4 alkyl))NH—, —(CH2)5CH(CO2(C1-4 alkyl))NH—, —(CH2)4CH(CONH2)NH—, —(CH2)4CH(CONH(C1-4 alkyl))NH—, —(CH2)4CH(CON(C1-4 alkyl)2)NH—, —(CH2)4C(C1-4 alkyl)(CO2(C1-4 alkyl))NH—, —(CH2)4C(CF3)(CO2(C1-4 alkyl))NH—, —(CH2)3CH(C1-4 alkyl)CH(CONH2)NH—, —(CH2)4CH(CONH(C1-4alkoxy))NH—, —(CH2)4CH(CONH(OBn))NH—, —(CH2)4CH(CON(C1-4 alkyl)(CH2)2O(C1-4 alkyl))NH—, —(CH2)4CH(CON(C1-4 alkyl)(CH2)2N(C1-4 alkyl)2)NH, —CH2—CH═CH—(CH2)2NH—, —CH2—CH═CH—(CH2)3NH—, —(CH2)4CH(CHF2)NH—, —(CH2)4CH(CF3)NH—, —(CH2)5CH(CF3)NH—, —(CH2)3CF2CH2NH—, —CH2—CH═CH—(CH2)2CH(CF3)NH—, —CH2CONH(CH2)2NH—, —CH2CONH(CH2)3NH—, —(CH2)4CH(3-C1-4 alkyl-oxetan-3-yl)NH—, —(CH2)4CH(CO-pyrrolidin-1-yl)NH—, —(CH2)4CH(thiazol-4-yl)NH—, —(CH2)4CH(4-C1-4 alkyl-thiazol-2-yl)NH—, —(CH2)4CH(1-C1-4 alkyl-imidazol-2-yl)NH—, —(CH2)4CH(1-C1-4 alkyl-pyrazol-3-yl)NH—, —(CH2)4CH(1-C1-4 alkyl-pyrazol-5-yl)NH—, —(CH2)4CH(1-C1-4 alkyl-3-C1-4 alkyl-pyrazol-5-yl)NH—, —(CH2)4CH(1-C1-4 alkyl-4-halo-pyrazol-3-yl)NH—, —CH2—CH═CH—CH2CH(1-C1-4 alkyl-pyrazol-5-yl)NH—, —(CH2)4N(CO2(C1-4 alkyl))CH2—, —(CH2)4N(CH2CO2(C1-4 alkyl))CH2—, —(CH2)4CONH—, —(CH2)5CONH—, —(CH2)6CONH—, —(CH2)3CH(C1-4 alkyl)CONH—, —(CH2)4CH(C1-4 alkyl)CONH—, —(CH2)2CH(C1-4 alkyl)CH2CONH—, —(CH2)3CH(C1-4 alkyl)CH2CONH—, —(CH2)2CH(C1-4 alkyl)(CH2)2CONH—, —(CH2)2—CH═CH—CONH—, —CH2—CH═CH—CH2CONH—, —CH2—CH═CH—(CH2)2CONH—, —CH2—CH═CH—(CH2)3CONH—, —CH2—CH═CH—CH2CH(C1-4 alkyl)CONH—, —CH2—CH═CH—CH(C1-4 alkyl)CH2CONH—, —CH2—CH═C(C1-4 alkyl)-(CH2)2CONH—, —(CH2)3CH(C1-14 alkyl)CONH—, —(CH2)3CHFCONH—, —(CH2)3CF2CONH—, —(CH2)4CF2CONH—, —CH2—CH═CH—CH2CF2CONH—, —(CH2)3CH(CF3)CONH—, —CH2CH(OH)(CH2)2CONH—, —(CH2)2CH(OH)CH2CONH—, —(CH2)3CH(OH)CH2CONH—, —CH2CH(OH)CH(OH)CH2CONH—, —CH2—CH═CH—CH(OH)CH2CONH—, —(CH2)3CH(C1-4 alkoxy)CONH—, —(CH2)3CH(OCO(C1-4 alkyl))CH2CONH—, —(CH2)3C(O)CH2CONH—, —CH2O(CH2)3CONH—, —CH2O(CH2)4CONH—, —CH2NH(CH2)2CONH—, —CH2NH(CH2)3CONH—, —(CH2)2N(C1-14 alkyl)CH2CONH—, —(CH2)2N(C1-4 alkyl)(CH2)2CONH—, —(CH2)5NHCO—, —CH2—CH═CH—(CH2)2NHCO—, —CH2—CH═CH—CH2OCONH—, —(CH2)40CONH—, —CH2—CH═CH—CH2NHCONH—, —(CH2)4SO2NH—, —CH2—CH═CH—CH2SO2NH—, —(CH2)4—CH═N—,
R1b is independently selected from the group consisting of: H and halogen;
R3 is independently selected from the group consisting of: H, halogen, C1-4 alkyl, CN, CO2(C1-4 alkyl), CONH2, CON(C1-4 alkyl)2, and cyclopropyl; and
R6 is independently selected from the group consisting of: halogen, NH2, CO2H, CONH2, —NHCO2(C1-4 alkyl), —NHCO2(CH2)2OH, —NHCO2(CH2)2O(C1-4 alkyl), —NHCO2CH2CH(C1-4 alkyl)O(C1-4 alkyl), and

### Claim 15 (depends on 11)

The compound of claim 11 having Formula (III), wherein:
L-Y is independently selected from the group consisting of: —(CH2)6—, —(CH2)7—, —(CH2)4CH(CO2H)CH2—, —(CH2)4CH(CO2Me)CH2—, —(CH2)4CH(CONH2)CH2—, —(CH2)4CH(CONHMe)CH2—, —(CH2)4CH(CON(Me)2)CH2—, —CH2—CH═CH—(CH2)3—, —CH2—CH═CH—(CH2)4—, —CH2CON(CH3)(CH2)3—, —(CH2)4N(CO2Me)CH2—, —(CH2)4N(CH2CO2Et)CH2—, —(CH2)5O—, —(CH2)6O—, —(CH2)3CH(Me)(CH2)2O—, —(CH2)4CH(Me)CH2O—, —CH2NH(CH2)4O—, —CH2—CH═CH—(CH2)3O—, —(CH2)5NH—, —(CH2)6NH—, —(CH2)3CH(Me)CH2NH—, —(CH2)4CH(Me)NH—, —(CH2)4CH(Me)CH2NH—, —(CH2)4CH(CH2OH)NH—, —(CH2)4CH(CH2OMe)NH—, —(CH2)4CH(CO2H)NH—, —(CH2)4CH(CO2Me)NH—, —(CH2)4CH(CO2Et)NH—, —CH2CONH(CH2)4NH—, —(CH2)4CH(CO2(i-Pr))NH—, —(CH2)4CH(CO2(t-Bu))NH—, —(CH2)4CH(CO2CH2CF3)NH—, —(CH2)4CH(CO2(CH2)2SO2Me)NH—, —(CH2)5CH(CO2Me)NH—, —(CH2)4CH(CH2CO2H)NH—, —(CH2)4CH(CH2CO2Me)NH—, —(CH2)4CH(CONH2)NH—, —(CH2)4CH(CONH(Me))NH—, —(CH2)4CH(CONH(t-Bu))NH—, —(CH2)4CH(CON(Me)2)NH—, —(CH2)4CH(CONH(OMe))NH—, —(CH2)4CH(CONH(OBn))NH—, —(CH2)4CH(CON(Me)(CH2)2OMe)NH—, —(CH2)4C(Me)(CO2Me)NH—, —(CH2)4C(CF3)(CO2Me)NH—, —(CH2)3CH(Me)CH(CONH2)NH—, —(CH2)4CH(CON(Me)(CH2)2N(Me)2)NH—, —CH2—CH═CH—(CH2)2NH—, —CH2—CH═CH—(CH2)3NH—, —(CH2)4CH(CHF2)NH—, —(CH2)4CH(CF3)NH—, —(CH2)5CH(CF3)NH—, —(CH2)3CF2CH2NH—, —CH2—CH═CH—(CH2)2CH(CF3)NH—, —CH2CONH(CH2)2NH—, —CH2CONH(CH2)3NH—, —(CH2)4CH(3-Me-oxetan-3-yl)NH—, —(CH2)4CH(CO-pyrrolidin-1-yl)NH—, —(CH2)4CH(thiazol-4-yl)NH—, —(CH2)4CH(4-Me-thiazol-2-yl)NH—, —(CH2)4CH(1-Me-imidazol-2-yl)NH—, —(CH2)4CH(1-Me-pyrazol-3-yl)NH—, —(CH2)4CH(1-(n-Pr)-pyrazol-3-yl)NH—, —(CH2)4CH(1-Me-pyrazol-5-yl)NH—, —(CH2)4CH(1,3-di-Me-pyrazol-5-yl)NH—, —(CH2)4CH(1-Me-4-Cl-pyrazol-3-yl)NH—, —CH2—CH═CH—CH2CH(1-Me-pyrazol-5-yl)NH—, —(CH2)4CONH—, —(CH2)5CONH—, —(CH2)6CONH—, —(CH2)3CH(Me)CONH—, —(CH2)4CH(Me)CONH—, —(CH2)2CH(Me)CH2CONH—, —(CH2)3CH(Me)CH2CONH—, —(CH2)2CH(Me)(CH2)2CONH—, —(CH2)2—CH═CH—CONH—, —CH2—CH═CH—CH2CONH—, —CH2—CH═CH—(CH2)2CONH—, —CH2—CH═CH—(CH2)3CONH—, —CH2—CH═CH—CH2CH(Me)CONH—, —CH2—CH═CHCH(Me)CH2CONH—, —CH2—CH═CHCH(Et)CH2CONH—, —CH2—CH═C (Me)-(CH2)2CONH—, —(CH2)3CH(Et)CONH—, —(CH2)3CH(i-Pr)CONH—, —(CH2)3CHFCONH—, —(CH2)3CF2CONH—, —(CH2)4CF2CONH—, —CH2—CH═CH—CH2CF2CONH—, —(CH2)3CH(CF3)CONH—, —CH2CH(OH)(CH2)2CONH—, —(CH2)2CH(OH)CH2CONH—, —(CH2)3CH(OH)CH2CONH—, —CH2CH(OH)CH(OH)CH2CONH—, —CH2—CH═CH—CH(OH)CH2CONH—, —(CH2)3CH(OMe)CONH—, —(CH2)3CH(OCOMe)CH2CONH—, —(CH2)3C(O)CH2CONH—, —CH2O(CH2)3CONH—, —CH2O(CH2)4CONH—, —CH2NH(CH2)2CONH—, —CH2NH(CH2)3CONH—, —(CH2)2N(Me)CH2CONH—, —(CH2)2N(Me)(CH2)2CONH—, —(CH2)5NHCO— —CH2—CH═CH—(CH2)2NHCO—, —CH2—CH═CH—CH2OCONH—, —(CH2)4OCONH—, —CH2—CH═CH—CH2NHCONH—, —(CH2)4SO2NH—, —CH2—CH═CH—CH2SO2NH—, —(CH2)4—CH═N—,
R1b is independently selected from the group consisting of: H and F;
R3 is independently selected from the group consisting of: H, F, Cl, Br, CH3, CN, CO2Me, CO2Et, CONH2, CONMe2, and cyclopropyl; and
R6 is independently selected from the group consisting of: F, NH2, CO2H, CONH2, —NHCO2Me, —NHCO2(CH2)2OH, —NHCO2(CH2)2OMe, —NHCO2(CH2)2OEt, —NHCO2CH2CH(Et)OMe, and

### Claim 16 (depends on 11)

The compound of claim 11 having Formula (III), wherein:
L-Y is independently selected from the group consisting of: —(CH2)6—, —(CH2)7—, —(CH2)4CH(CO2H)CH2—, —(CH2)4CH(CO2(C1-4 alkyl))CH2—, —(CH2)4CH(CONH2)CH2—, —(CH2)4CH(CONH(C1-4 alkyl))CH2—, —(CH2)4CH(CON(C1-4 alkyl)2)CH2—, —CH2—CH═CH—(CH2)4—, —(CH2)4N(CO2(C1-4 alkyl))CH2—, —(CH2)6O—, —(CH2)3CH(C1-4 alkyl)(CH2)2O—, —CH2NH(CH2)4O—, —(CH2)5NH—, —(CH2)6NH—, —(CH2)4CH(C1-4 alkyl)NH—, —(CH2)3CH(C1-4 alkyl)CH2NH—, —(CH2)4CH(C1-4 alkyl)CH2NH—, —(CH2)4CH(CH2OH)NH—, —(CH2)4CH(CH2(C1-4 alkoxy))NH—, —(CH2)4CH(CO2H)NH—, —(CH2)4CH(CH2CO2H)NH—, —(CH2)4CH(CH2CO2(C1-4 alkyl))NH—, —(CH2)4CH(CO2(C1-4 alkyl))NH—, —(CH2)4CH(CO2CH2CF3)NH—, —(CH2)4CH(CO2(CH2)2SO2(C1-4 alkyl))NH—, —(CH2)5CH(CO2(C1-4 alkyl))NH—, —(CH2)4CH(CONH2)NH—, —(CH2)4CH(CONH(C1-4 alkyl))NH—, —(CH2)4CH(CON(C1-4 alkyl)2)NH—, —(CH2)4CH(CONH(C1-4 alkoxy))NH—, —(CH2)4CH(CONH(OBn))NH—, —(CH2)4CH(CON(C1-4 alkyl)(CH2)2O(C1-4 alkyl))NH—, —(CH2)4CH(CON(C1-4 alkyl)(CH2)2N(C1-4 alkyl)2)NH—, —CH2—CH═CH—(CH2)2NH—, —CH2—CH═CH—(CH2)3NH—, —(CH2)4CH(CHF2)NH—, —(CH2)4CH(CF3)NH—, —(CH2)3CF2CH2NH—, —CH2—CH═CH—(CH2)2CH(CF3)NH—, —(CH2)4CH(3-C1-4 alkyl-oxetan-3-yl)NH—, —(CH2)4CH(CO-pyrrolidin-1-yl)NH—, —(CH2)4CH(thiazol-4-yl)NH—, —(CH2)4CH(4-C1-4 alkyl-thiazol-2-yl)NH—, —(CH2)4CH(1-C1-4 alkyl-imidazol-2-yl)NH—, —(CH2)4CH(1-C1-4 alkyl-pyrazol-3-yl)NH—, —(CH2)4CH(1-C1-4 alkyl-pyrazol-5-yl)NH—, —(CH2)4CH(1-C1-4 alkyl-3-C1-4 alkyl-pyrazol-5-yl)NH—, —(CH2)4CH(1-C1-4 alkyl-4-halo-pyrazol-3-yl)NH—, —(CH2)4CONH—, —(CH2)5CONH—, —(CH2)6CONH—, —(CH2)3CH(C1-4 alkyl)CONH—, —(CH2)4CH(C1-4 alkyl)CONH—, —(CH2)2CH(C1-4 alkyl)CH2CONH—, —(CH2)3CH(C1-4 alkyl)CH2CONH—, —(CH2)2CH(C1-4 alkyl)(CH2)2CONH—, —(CH2)2—CH═CH—CONH—, —CH2—CH═CH—CH2CONH—, —CH2—CH═CH—(CH2)2CONH—, —CH2—CH═CH—(CH2)3CONH—, —CH2—CH═CH—CH2CH(C1-4alkyl)CONH—, —CH2—CH═CH—CH(C1-4 alkyl)CH2CONH—, —CH2—CH═C(C1-4 alkyl)-(CH2)2CONH—, —(CH2)3CH(C1-4 alkyl)CONH—, —(CH2)3CHFCONH—, —(CH2)3CF2CONH—, —(CH2)4CF2CONH—, —CH2—CH═CH—CH2CF2CONH—, —(CH2)3CH(CF3)CONH—, —CH2CH(OH)(CH2)2CONH—, —(CH2)2CH(OH)CH2CONH—, —(CH2)3CH(OH)CH2CONH—, —CH2CH(OH)CH(OH)CH2CONH—, —CH2—CH═CH—CH(OH)CH2CONH—, —(CH2)3CH(C1-4 alkoxy)CONH—, —(CH2)3CH(OCO(C1-4 alkyl))CH2CONH—, —(CH2)3C(O)CH2CONH—, —CH2O(CH2)3CONH—, —CH2O(CH2)4CONH—, —CH2NH(CH2)2CONH—, —CH2NH(CH2)3CONH—, —(CH2)2N(C1-4 alkyl)CH2CONH—, —(CH2)2N(C1-4alkyl)(CH2)2CONH—, —(CH2)5NHCO—, —CH2—CH═CH—(CH2)2NHCO—, —CH2—CH═CH—CH2OCONH—, —(CH2)4OCONH—, —CH2—CH═CH—CH2NHCONH—, —(CH2)4SO2NH—, —CH2—CH═CH—CH2SO2NH—, —(CH2)4—CH═N—,
R1b is independently selected from the group consisting of: H and halogen;
R3 is independently selected from the group consisting of: H, halogen, C1-4 alkyl, CN, CO2(C1-4 alkyl), CONH2, CON(C1-4 alkyl)2, and cyclopropyl; and
R6 is independently selected from the group consisting of: F, NH2, CO2H, —NHCO2(C1-4 alkyl), —NHCO2(CH2)2OH, —NHCO2(CH2)2O(C1-4 alkyl), —NHCO2CH2CH(C1-4 alkyl)O(C1-4 alkyl), and

### Claim 17 (depends on 11)

The compound of claim 11 having Formula (III), wherein:
L-Y is independently selected from the group consisting of: —(CH2)6—, —(CH2)7—, —(CH2)4CH(CO2H)CH2—, —(CH2)4CH(CO2Me)CH2—, —(CH2)4CH(CONH2)CH2—, —(CH2)4CH(CONHMe)CH2—, —(CH2)4CH(CON(Me)2)CH2—, —CH2—CH═CH—(CH2)4—, —(CH2)4N(CO2Me)CH2—, —(CH2)6O—, —(CH2)3CH(Me)(CH2)2O—, —CH2NH(CH2)4O—, —(CH2)5NH—, —(CH2)6NH—, —(CH2)4CH(Me)NH—, —(CH2)3CH(Me)CH2NH—, —(CH2)4CH(Me)CH2NH—, —(CH2)4CH(CH2OH)NH—, —(CH2)4CH(CH2OMe)NH—, —(CH2)4CH(CO2H)NH—, —(CH2)4CH(CO2Me)NH—, —(CH2)4CH(CO2Et)NH—, —(CH2)4CH(CO2(i-Pr))NH—, —(CH2)4CH(CO2(t-Bu))NH—, —(CH2)4CH(CO2CH2CF3)NH—, —(CH2)4CH(CO2(CH2)2SO2Me)NH—, —(CH2)5CH(CO2Me)NH—, —(CH2)4CH(CH2CO2H)NH—, —(CH2)4CH(CH2CO2Me)NH—, —(CH2)4CH(CONH2)NH—, —(CH2)4CH(CONH(Me))NH—, —(CH2)4CH(CONH(t-Bu))NH—, —(CH2)4CH(CON(Me)2)NH—, —(CH2)4CH(CONH(OMe))NH—, —(CH2)4CH(CONH(OBn))NH—, —(CH2)4CH(CON(Me)(CH2)2OMe)NH—, —(CH2)4CH(CON(Me)(CH2)2N(Me)2)NH—, —CH2—CH═CH—(CH2)2NH—, —CH2—CH═CH—(CH2)3NH—, —(CH2)4CH(CHF2)NH—, —(CH2)4CH(CF3)NH—, —(CH2)3CF2CH2NH—, —CH2—CH═CH—(CH2)2CH(CF3)NH—, —(CH2)4CH(3-Me-oxetan-3-yl)NH—, —(CH2)4CH(CO-pyrrolidin-1-yl)NH—, —(CH2)4CH(thiazol-4-yl)NH—, —(CH2)4CH(4-Me-thiazol-2-yl)NH—, —(CH2)4CH(1-Me-imidazol-2-yl)NH—, —(CH2)4CH(1-Me-pyrazol-3-yl)NH—, —(CH2)4CH(1-(n-Pr)-pyrazol-3-yl)NH—, —(CH2)4CH(1-Me-pyrazol-5-yl)NH—, —(CH2)4CH(1,3-di-Me-pyrazol-5-yl)NH—, —(CH2)4CH(1-Me-4-Cl-pyrazol-3-yl)NH—, —(CH2)4N(CO2Me)CH2—, —(CH2)4CONH—, —(CH2)5CONH—, —(CH2)6CONH—, —(CH2)3CH(Me)CONH—, —(CH2)4CH(Me)CONH—, —(CH2)2CH(Me)CH2CONH—, —(CH2)3CH(Me)CH2CONH—, —(CH2)2CH(Me)(CH2)2CONH—, —(CH2)2—CH═CH—CONH—, —CH2—CH═CH—CH2CONH—, —CH2—CH═CH—(CH2)2CONH—, —CH2—CH═CH—(CH2)3CONH—, —CH2—CH═CH—CH2CH(Me)CONH—, —CH2—CH═CH—CH(Me)CH2CONH—, —CH2—CH═CHCH(Et)CH2CONH—, —CH2—CH═C (Me)-(CH2)2CONH—, —(CH2)3CH(Me)CONH—, —(CH2)3CH(Et)CONH—, —(CH2)3CH(i-Pr)CONH—, —(CH2)3CHFCONH—, —(CH2)3CF2CONH—, —(CH2)4CF2CONH—CH2—CH═CH—CH2CF2CONH—, —(CH2)3CH(CF3)CONH—, —CH2CH(OH)(CH2)2CONH—, —(CH2)2CH(OH)CH2CONH—, —(CH2)3CH(OH)CH2CONH—, —CH2CH(OH)CH(OH)CH2CONH—, —CH2—CH═CH—CH(OH)CH2CONH—, —(CH2)3CH(OMe)CONH—, —(CH2)3CH(OCOMe)CH2CONH—, —(CH2)3C(O)CH2CONH—, —CH2O(CH2)3CONH—, —CH2O(CH2)4CONH—, —CH2NH(CH2)2CONH—, —CH2NH(CH2)3CONH—, —(CH2)2N(Me)CH2CONH—, —(CH2)2N(Me)(CH2)2CONH—, —(CH2)5NHCO—, —CH2—CH═CH—(CH2)2NHCO—, —CH2—CH═CH—CH2OCONH—, —(CH2)4OCONH—, —CH2—CH═CH—CH2NHCONH—, —(CH2)4SO2NH—, —CH2—CH═CH—CH2SO2NH—, —(CH2)4—CH═N—,
R1b is independently selected from the group consisting of: H and F;
R3 is independently selected from the group consisting of: H, F, Cl, Br, CH3, CN, CO2Me, CO2Et, CONH2, CONMe2, and cyclopropyl; and
R6 is independently selected from the group consisting of: F, NH2, CO2H, —NHCO2Me, —NHCO2(CH2)2OH, —NHCO2(CH2)2OMe, —NHCO2(CH2)2OEt, —NHCO2CH2CH(Et)OMe, and

### Claim 18 (depends on 1)

A compound of claim 1 having Formula (IV):
or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, or a solvate thereof, wherein:
is independently selected from the group consisting of:
L1 is independently selected from the group consisting of: a bond, —CH2CH2— and —CH═CH—;
L is independently selected from the group consisting of: —CH2—CH═CH—CH2—, —CH2—CH═CH—(CH2)2—, —(CH2)4—, —(CH2)5—, —(CH2)3CH(C1-4 alkyl)-, —CH2—CH═CH—CH2CH(CF3)—, —(CH2)4CH(CF3)—, —(CH2)4CH(CH2OH)—, —(CH2)4CH(CO2H)—, —(CH2)4CH(CO2(C1-4 alkyl))-, —CH2CONH(CH2)2—, —(CH2)4CH(CO2(CH2)2O(C1-4 alkyl))-, —(CH2)4CH(CH2NH(CH2)2O(C1-4 alkyl))-, —(CH2)4CH(CO2(CH2)2N(C1-4 alkyl)2)-, —(CH2)4CH(CON(C1-4 alkyl)(CH2)2O(C1-4 alkyl))-, —(CH2)4CH(CON(C1-4 alkyl)(CH2)2N(C1-4 alkyl)2)-,
Y is independently —CONH—, O, or NH;
R1 is, independently at each occurrence, selected from: halogen, CN, OCF3, CHF2, CF3, C1-4 alkyl, C1-4 alkoxy, CO(C1-4 alkyl), NH2, —C(═NH)NH2, —C(O)NH2, and —CH2NH2;
R2 is independently a 5-membered heterocycle selected from: pyrazolyl, imidazolyl, triazolyl, and tetrazolyl;
R3 is independently selected from the group consisting of: H, halogen, and C1-4 alkyl; and
R6 is, independently at each occurrence, selected from the group consisting of: H, halogen, CN, —NHCO2(C1-4 alkyl), —CH2NHCO2(C1-4 alkyl), —NHCO2(CH2)2O(C1-4 alkyl), CO2H, and CONH2.

### Claim 19 (depends on 18)

The compound of claim 18 having Formula (IVa):
or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, or a solvate thereof, wherein:
is independently selected from the group consisting of:
Y is independently —CONH— or NH;
R3 is independently selected from the group consisting of: H, F, Cl, and C1-4 alkyl; and
R6 is independently selected from the group consisting of: F, —NHCO2(C1-4 alkyl), —CH2NHCO2(C1-4 alkyl), CO2H, CONH2, and —NHCO2(CH2)2O(C1-4 alkyl).

### Claim 20 (depends on 1)

The compound of claim 1 having Formula (V):
or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, or a solvate thereof, wherein:
ring B is independently selected from the group consisting of: imidazole and pyridine; and
R1 is independently selected from the group consisting of: C1-4 alkyl and CH2NH2.