CETP inhibitors

1. A compound having Formula Ia, or a pharmaceutically acceptable salt thereof,

wherein R X and R Z are each H;

R W is selected from the group consisting of (a) C 1 -C 5 alkyl which is optionally substituted with 1-9 substituents independently selected from 1-7 halogens and 1-2 groups independently selected from —CN, —OH, —OCH 3 , —OCF 3 and —N(R 9 ) 2 , (b) C 2-5 alkenyl optionally substituted with 1-5 halogens; (c) —C(═O)OC 1-3 alkyl optionally substituted with 1-5 halogens; (d) —C(═O)C 1 -C 3 alkyl which is optionally substituted with 1-7 halogens, (e) —C(═O)H, (f) —NO 2 , (g) —OC 1 -C 3 alkyl which is optionally substituted with 1-7 halogens, (h) C 3 -C 6 cycloalkyl, (i) phenyl, (j) a 5-6 membered saturated or partly unsaturated heterocyclic ring having 1-3 heteroatoms independently selected from N, S and O, and (k) a 5-7 membered heteroaromatic ring having 1-3 heteroatoms independently selected from N, S, and O, wherein said C 3 -C 6 cycloalkyl, phenyl, 5-6 membered saturated or partly unsaturated heterocyclic ring, and 5-7 membered heteroaromatic ring are optionally substituted with 1-5 substituents independently selected from halogen, CH 3 , CF 3 , —OCH 3 , and —OCF 3 ;

R Y is selected from the group consisting of Br, —OCH 3 , —CN, and pyridyl;

x is an integer from 0-2;

B is selected from the group consisting of:

—N(R 9 )(C(═O))DR 3 ,

—N(R 9 )(C(═O))DR 7 ,

—N(R 9 )(C(═O))R 3 ,

—N(R 9 )(C(═O))R 7 ,

—N(R 9 )(C(═O))OCH 2 R 3 ,

—N(R 9 )D(C(═O))R 7 ,

—N(R 9 )DR 3 ,

—N(R 9 )D 2 R 7 ,

—OD 2 R 3 ,

—SD 2 R 3 ,

—C(═O)CH 2 CH 2 R 4 ,

-D 2 (C(═O))R 7 ,

-D 2 R 3 , and

D 2 R 7 ;

D is a difunctional group selected from C 1 -C 7 alkylene, C 2 -C 5 alkenylene, and C 2 -C 5 alkynylene, wherein said alkylene group optionally has one difunctional group O, S, —NH— or —N(C 1 -C 3 alkyl)-between two carbon atoms of D, and said alkylene, alkenylene, and alkynylene groups are optionally substituted with 1-9 substituents independently selected from 1-7 halogens and optionally 1-2-OH groups;

D 2 is a difunctional group selected from C 2 -C 7 alkylene and C 2 -C 5 alkynylene, wherein said alkylene group optionally has one difunctional group O, S, —NH— or —N(C 1 -C 3 alkyl)-between two carbon atoms of the alkylene group other than carbonyl, and said alkylene and alkynylene groups are optionally substituted with 1-9 substituents independently selected from (a) 1-7 halogens, (b) 1-2 substituents independently selected from —N(R 9 ) 2 , —CN, —NO 2 , —OC 1 -C 3 alkyl optionally substituted with 1-3 halogens, —C(═O)OH, —C(═O)H, —C(═O)OC 1 -C 5 alkyl optionally substituted with 1-7 halogens, —C(═O)C 1 -C 5 alkyl optionally substituted with 1-7 halogens, —C(═O)N(R 9 ) 2 , (c) 1-2-OH groups, and (d) an oxo group on a carbon atom between two other carbon atoms of the alkylene group;

R 3 is selected from the group consisting of R 4 , -T-R 4 , and —R 5 ;

R 7 is selected from the group consisting of —OC 1 -C 7 alkyl, —CH 2 S(O) 2 C 1 -C 7 alkyl, C 5 -C 10 alkyl, —NR 9 C 1 -C 7 alkyl, —NR 9 C(═O)OC 1 -C 7 alkyl, —OC(═O)OC 1 -C 7 alkyl and —OSi(R 8 ) 3 , wherein the C 5 -C 10 alkyl and C 1 -C 7 alkyl groups of R 7 are optionally substituted with 1-9 halogens and are optionally substituted with one group selected from —N(R 9 ) 2 , —N(R 9 )C(═O)OC 1 -C 7 alkyl, —N(R 9 )C(═O)C 1 -C 7 alkyl, and —OH, wherein the C 1 -C 7 alkyl groups of the —N(R 9 )C(═O)OC 1 -C 7 alkyl and —N(R 9 )C(═O)C 1 -C 7 alkyl substituents on R 7 are optionally substituted with 1-9 halogens;

T is selected from —O—, —N(R 9 )—, and —S—;

Each R 8 group is independently selected from C 1 -C 5 alkyl, which is optionally substituted with 1-7 halogens;

R 4 is a cyclic group selected from the group consisting of

(a) C 3 -C 8 Cycloalkyl which optionally comprises 1-2 double bonds;

(b) Bicyclic C 6 -C 12 Cycloalkyl optionally comprising 1-2 double bonds;

(c) A 4-8 membered saturated or partly unsaturated heterocyclic ring having 1-2 ring members independently selected from —O— and —N(R 6 )—, said heterocyclic ring being connected to the left hand part of Formula I through a carbon atom of the heterocyclic ring, wherein said heterocyclic ring is optionally fused to an aromatic ring selected from phenyl and naphthyl or to a C 5 -C 7 Cycloalkyl;

(d) An aromatic ring selected from phenyl and naphthyl; and

(e) A 5-7 membered heteroaromatic ring having 1-3 heteroatoms independently selected from N, S, and O, and optionally having one —C(═O)— group as a ring member, said heteroaromatic ring being connected to the left hand part of formula I through a carbon atom of the heteroaromatic ring, wherein said heteroromatic group is optionally fused to an aromatic ring selected from phenyl and naphthyl;

Wherein said cyclic groups R 4 defined in (a)-(e), including optional fused rings, are optionally substituted with 1-7 substitutents independently selected from halogen, C 1 -C 5 alkyl, —OC 1 -C 5 alkyl, phenyl, —NO 2 , —C(═O)C 1 -C 5 alkyl, —C(═O)OC 1 -C 5 alkyl, —C(═O)OH, and —NR 9 C(═O)C 1 -C 5 alkyl, wherein C 1 -C 5 alkyl and OC 1 -C 5 alkyl in all uses are optionally substituted with 1-9 halogens, and said phenyl is optionally substituted with 1-5 substituents independently selected from halogen, CH 3 , CF 3 , —OCH 3 , and —OCF 3 ;

R 5 is a saturated or partly unsaturated 5-8 membered monocyclic heterocyclic group or a saturated or partly unsaturated 6-10 membered bicyclic heterocyclic group, wherein said heterocyclic group has a heteroatom N connected to the left hand side of Formula I and optionally has a second heteroatom selected from O, S, and —N(R 6 )—, wherein said heterocyclic group optionally has 1-2 double bonds and an optional carbonyl group and is optionally fused to a cyclic group selected from phenyl and a 5-7 membered heteroaromatic ring having 1-3 heteroatoms independently selected from O, N, and S, or is optionally connected through a spiro linkage of a carbon atom to a 5-6 membered cycloalkyl ring or to a 5-7 membered heterocyclic ring having one heteroatom selected from 0, N and S(O) x , said cycloalkyl and heterocyclic ring optionally having one double bond and optionally being fused to a phenyl ring; wherein R 5 including the rings optionally fused to R 5 or connected to R 5 through a spiro linkage is optionally substituted with 1-9 halogen atoms and is optionally substituted with 1-3 substituents independently selected from C 1 -C 5 alkyl; —OC 1 -C 5 alkyl; —NO 2 ; —N(R 9 )C(═O)OCH 2 -phenyl; —S(O) 2 C 1 -C 3 alkyl; C 3 -C 6 cycloalkyl; —CO 2 H; —C(═O)C 1 -C 3 alkyl; —C(═O)OC 1 -C 3 alkyl; —C(═O)N(R 9 ) 2 ; —C 1 -C 3 alkyleneN(R 9 ) 2 ; C 1 -C 3 alkyleneC(═O)N(R 9 ) 2 ; phenyl; —C 1 -C 3 alkylenePhenyl; a 5-10 membered heteroaromatic monocyclic or fused bicyclic group having 1-3 heteroatoms independently selected from N, O, and S; a 5-6 membered saturated or partly unsaturated heterocyclic ring having 1-3 heteroatoms independently selected from N, O, and S, optionally having a carbonyl group, optionally having one double bond, and optionally being fused to a phenyl ring; and a 5-6-membered heteroaromatic ring having 1-2 heteroatoms independently selected from N, S, and O, said heteroaromatic ring being fused to a 5-7 membered cycloalkyl or to a saturated or partly unsaturated heterocycle having 1-2 heteroatoms independently selected from N, S, and O; wherein all of said alkyl groups that are included in substituent groups on R 5 are optionally substituted with 1-9 halogens, and all of said phenyl groups that are substituents on R 5 or that are included in substituents on R 5 are optionally substituted with 1-5 substituents independently selected from halogen, —CN, —NO 2 , CH 3 , CF 3 , —OCH 3 , and —OCF 3 ;

R 6 is selected from the group consisting of C 1 -C 7 alkyl, —C(═O)OC 1 -C 7 alkyl, —C(═O)C 1 -C 7 alkyl, —S(O) x phenyl, —S(O) x C 1 -C 7 alkyl, —C(═O)N(R 9 ) 2 , —C(═O)Phenyl, —C(═O)OPhenyl, —C 1 -C 3 alkylene —C(═O)OC 1 -C 6 alkyl, —C 1 -C 5 alkylene-OC 1 -C 5 alkyl, —C(═O)C 3 -C 7 cycloalkyl, —C(═O)OC 3 -C 7 cycloalkyl, and a cyclic group selected from (a) phenyl, (b) naphthyl, (c) biphenyl, (d) C 3 -C 8 cycloalkyl, (e) a saturated or partially unsaturated monocyclic or bicyclic 5-10 membered heterocycle having 1-2 heteroatoms independently selected from N, O, and S, said heterocycle optionally having 1-2 double bonds, and (f) a monocyclic or bicyclic 5-12 membered heteroaromatic group having 1-4 heteroatoms independently selected from N, S, and O and optionally having 1-2 carbonyl groups, wherein in all instances, each alkyl, alkenyl and alkynyl group included in R 6 is optionally substituted with 1-10 halogens and is also optionally substituted with 1-2 groups independently selected from phenyl, OH, biphenyl, —Ophenyl, and —OC 1 -C 3 alkylene-phenyl, wherein said phenyl substituents on the alkyl, alkenyl and alkynyl groups of R 6 are optionally substituted with 1-5 substituent groups independently selected from halogen, CH 3 , CF 3 , —OCF 3 , —NO 2 and —OCH 3 , and when R 6 is a cyclic group selected from (a) phenyl, (b) naphthyl, (c) biphenyl, (d) C 3 -C 8 cycloalkyl, (e) a saturated or partially unsaturated monocyclic or bicyclic 5-10 membered heterocycle having 1-2 heteroatoms independently selected from N, O, and S, said heterocycle optionally having 1-2 double bonds, and (f) a cyclic or bicyclic 5-12 membered heteroaromatic group having 1-4 heteroatoms independently selected from N, S, and O and optionally having 1-2 carbonyl groups, said cyclic group R 6 is optionally substituted with 1-3 groups independently selected from C 1 -C 5 alkyl, —OC 1 -C 5 alkyl, —C(═O)C 1 -C 3 alkyl, —S(O) x C 1 -C 3 alkyl, phenyl, halogen, —CN, and —NO 2 , said C 1 -C 5 alkyl and —OC 1- C 5 alkyl being optionally substituted with 1-7 halogens; and

R 9 is selected from the group consisting of H, C 1 -C 5 alkyl, C 2 -C 5 alkenyl, and C 2 -C 5 alkynyl, wherein said C 1 -C 5 alkyl, C 2 -C 5 alkenyl, and C 2 -C 5 alkynyl are optionally substituted with 1-9 halogens;

With the proviso (I) that when the group R W or R Y is —OCH 3 ; then B is not —N(H)C(═O)(CH 2 ) 5 NH(C(═O))CF 3 or —N(H)C(═O)CH(NH 2 )(C 4 alkyl);

And with the further proviso (II) that when the group R W is —OCH 3 , halogen, C 1 -C 4 alkyl, or —NH 2 , or R Y is —OCH 3 or Br, then B is not —NHC(═O)phenyl, —NHC(═O)cyclobutyl, —NHC(═O)(CH═CH)(1,4-furyl)phenyl, —NHC(═O)(1,4-furyl)phenyl, —NHC(═O)(CH 2 )(CH 2 ) 1,2,4-oxadiazolyl)phenyl, —NHC(═O)(cyclopentyl)phenyl, or NHC(═O)biphenyl, wherein phenyl in all instances is optionally substituted with 1-2 substituents independently selected from halogen, methoxy, and C1-4alkyl.

2. The compound of claim 1 having formula Ib, or a pharmaceutically acceptable salt thereof:

wherein R W is selected from the group consisting of (a) (b) C 1 -C 5 alkyl which is optionally substituted with 1-9 substituents independently selected from 1-7 halogens and 1-2 groups independently selected from —CN, —OH, —OCH 3 , —OCF 3 and —N(R 9 ) 2 , (c) C 2-5 alkenyl optionally substituted with 1-5 halogens; (d) —C(═O)OC 1-3 alkyl optionally substituted with 1-5 halogens; (e) —C(═O)C 1 -C 3 alkyl which is optionally substituted with 1-7 halogens, (f) —C(═O)H, (g) —NO 2 , (h) —OC 1 -C 3 alkyl which is optionally substituted with 1-7 halogens, (i) C 3 -C 6 cycloalkyl, (j) phenyl, (k) a 5-6 membered saturated or partly unsaturated heterocyclic ring having 1-3 heteroatoms independently selected from N, S and O, and (1) a 5-7 membered heteroaromatic ring having 1-3 heteroatoms independently selected from N, S, and O, wherein said C 3 -C 6 cycloalkyl, phenyl, 5-6 membered saturated or partly unsaturated heterocyclic ring, and 5-7 membered heteroaromatic ring are optionally substituted with 1-5 substituents independently selected from halogen, CH 3 , CF 3 , —OCH 3 , and —OCF 3 ; and

R 9 is independently selected from H and CH 3 .

3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

B is selected from the group consisting of:

—(NH)(C(═O))CH 2 R 3 ,

—(NH)(C(═O))CH 2 CH 2 R 3 ,

—(NH)(C(═O))CH 2 —O—(CH 2 ) 3 R 7 ,

—(NH)(C(═O))OCH 2 R 4 ,

—C 2 -C 4 alkyleneR 3 , wherein —C 2 -C 4 alkylene optionally has one difunctional group O, S, —NH—, or —N(CH 3 )— between two carbon atoms and is optionally substituted with 1-8 substituents independently selected from (a) 1-7 halogens, (b) 1-2 substituents independently selected from —N(R 9 ) 2 , —CN, —OC 1 -C 3 alkyl optionally substituted with 1-3 halogens, —C(═O)OH, —C(═O)H, —C(═O)OC 1 -C 5 alkyl optionally substituted with 1-7 halogens, —C(═O)C 1 -C 5 alkyl optionally substituted with 1-7 halogens, —C(═O)N(R 9 ) 2 , (c) 1-2-OH groups, and (d) an oxo group on a carbon atom between two other carbon atoms of the alkylene group;

—C 2 -C 4 alkyleneR 7 , wherein —C 2 -C 4 alkylene optimally has one difunctional group O, S, —NH—, or —N(CH 3 )— between two carbon atoms and is optionally substituted with 1-8 substituents independently selected from (a) 1-7 halogens, (b) 1-2 substituents independently selected from —N(R 9 ) 2 , —CN, —C(═O)OH, —C(═O)H, —C(═O)OC 1 -C 5 alkyl optionally substituted with 1-7 halogens, —C(═O)C 1 -C 5 alkyl optionally substituted with 1-7 halogens, —C(═O)N(R 9 ) 2 , (c) 1-2-OH groups, and (d) an oxo group on a carbon atom between two other carbon atoms of the alkylene group;

—C≡CH 2 R 3 ,

—C≡CH 2 R 7 ,

—NHCH 2 CH 2 R 3 ,

—NHCH(CF 3 )CH 2 R 7 ,

—NHCH 2 C(═O)R 5 ,

—CH(OH)CH(OH)C(═O)OC 1 -C 4 alkyl; and

Each R 9 is independently selected from H and CH 3 .

4. The compound of claim 3 , or a pharmaceutically acceptable salt thereof, wherein:

R 3 is selected from the group consisting of R 4 , —OR 4 , and —R 5 ;

R 4 is a cyclic group selected from the group consisting of:

(a) Cyclohexyl,

(b) 2-quinolyl,

(c) 1-isoquinolyl,

(d) phenyl,

(e) 2-tetrahydropyranyl,

wherein R 4 is optionally substituted with 1-3 substituents independently selected from —CH 3 , —CF 3 , —OCH 3 , —OCF 3 , and halogen;

R 5 is selected from the group consisting of:

wherein R 10 is selected from the group consisting of —SO 2 CF 3 , —SO 2 CH 3 , and —C(═O)CH 3 ;

R 11 is selected from the group consisting of H, C 1 -C 5 alkyl, phenyl, and benzyl, wherein C 1 -C 5 alkyl is optionally substituted with 1-3 halogens, and wherein phenyl and benzyl are optionally substituted with 1-3 groups independently selected from halogen, —CH 3 , —CF 3 , —OCH 3 , and —OCF 3 ;

R 12 is selected from the group consisting of H, C 1 -C 3 alkyl which is optionally substituted with 1-3 halogens, and —CH 2 C(═O)N(R 9 ) 2 ;

wherein when R 5 is (a) or (d)-(g), then R 5 is optionally substituted with 1-3 substituent groups independently selected from halogen, —CH 3 , —CF 3 , —OCH 3 , and —OCF 3 ; and when R 5 is (b) or (c), then R 5 is optionally substituted with 1-2 substituents independently selected from halogen, cyclohexyl, phenyl, —C(═O)N(R 9 )C 2 -C 5 alkyl, —C(═O)OC 1 -C 4 alkyl, benzotriazole, pyrazolotetrahydropyridine, and —N(C 2 -C 3 alkenyl)(C(═O))O-benzyl, wherein alkyl and alkenyl are optionally substitued with 1-3 halogens, and phenyl and the phenyl of benzyl are optionally substituted with 1-3 halogens and 1 group selected from —CH 3 , —CF 3 , —OCH 3 , —OCF 3 , and —NO 2 ;

x is an integer from 0-2;

R 6 is selected from the group consisting of:

(a) phenyl,

(b) pyrimidinyl,

(c) pyrazinyl,

(d) pyridyl,

(e) naphthyl,

(f) C 3 -C 6 cycloalkyl,

(g) CH(phenyl) 2 ,

(h) —C(═O)OC 1 -C 5 alkyl,

(i) —C(═O)C 1 -C 5 alkyl,

(j) —SO 2 C 1 -C 3 alkylene-phenyl,

(k) —SO 2 C 1 -C 5 alkyl,

(l) —C(═O)OC 3 -C 5 alkylene-OH,

(m) —C(═O)OC 3 -C 5 alkylene-Obenzyl,

(n) —C(═O)O-phenyl,

(o) —C(═O)O-benzyl,

(p) —C(═O)N(R 9 )C 1 -C 5 alkyl,

(q) —C(═O)OC 5 -C 6 cycloalkyl,

(r) —CH 2 C(═O)OC 1 -C 5 alkyl,

(s) C 1 -C 3 alkylene-phenyl, and

(t) C 4 -C 6 alkyl,

wherein alkyl, alkylene, and cycloalkyl groups are optionally substituted with 1-3 halogens; phenyl, the phenyl groups of benzyl, and naphthyl are optionally substituted with 1-3 substituents independently selected from (i) halogen, (ii) C 1 -C 3 alkyl optionally substituted with 1-3 halogens, (iii) —OCF 3 , (iv) —OCH 3 , (v) —NO 2 , (vii) phenyl, (viii) —CN, (ix) —C(═O)CH 3 and (x) —SO 2 CH 3 ; and pyridyl, pyrimidinyl and pyrazinyl are optionally substituted with 1-3 substituents independently selected from halogen, —CH 3 , —CF 3 , —OCH 3 , —OCF 3 , —NO 2 , —CN, and phenyl; and

R 7 is selected from the group consisting of —OC 3 -C 5 alkyl and —N(R 9 )C(═O)OC 3 -C 5 alkyl, wherein each alkyl group is optionally substituted with 1-3 halogens.

5. The compound of claim 2 , or a pharmaceutically acceptable salt thereof, wherein B is selected from the group consisting of:

(a) —NHC(═O)CH2OR 4 ,

(b) —NHC(═O)CH2R 3 ,

(c) —NHCH2CH2R 3 ,

(d) —SCH2CH2R 3 ,

(e) —C(═O)CH2CH2R 4 ,

(f) —CH2CH2CH2R 3 , wherein the propylene chain is optionally substituted with 1-2 halogens, one —OH group, or a methylene group (═CH 2 ),

(g) —CH2TCH2R 3 ,

(h) —CH2C(═O)CH2R 3 , and

(i) —CH2CH2TR 4 ;

T is selected from the group consisting of 0, —NH—, and S;

R 3 is selected from R 4 and R 5 ;

R 4 is selected from the group consisting of 4-piperidinyl having an R 6 substitutent on the N, cyclohexyl, and phenyl, wherein 4-piperidinyl is optionally substituted with 1-2 substitutents independently selected from F, CH3, and CF3, and phenyl and cyclohexyl are optionally substituted with 1-3 substitutents independently selected from halogen, CH3, CF3, OCH3, and OCF3;

R 5 is selected from the group consisting of 1-pyrrolidinyl, 1-piperidinyl, and 1-piperazinyl, wherein the N at the 4-position of 1-piperazinyl is substituted with R 6 , and the pyrrolidinyl, piperidinyl, and piperazinyl groups are optionally substituted with 1-2 substituents independently selected from F, CH 3 , and CF 3 ; and

R 6 is selected from the group consisting of (a) —C(═O)OC1-C5alkyl, (b) —C(═O)C1-C3alkyl optionally substituted with 1-3F, (c) phenyl, (d) pyridyl, and (e) pyrimidinyl, wherein pyridyl, pyrimidinyl, and phenyl are optionally substituted with 1-3 groups independently selected from halogen, CH3, CF3, OCH3, and OCF3, and optionally one phenyl.

6. The compound of claim 5 , wherein R W is selected from the group consisting of —OCH 3 , —OCF 3 , —C(═O)OCH 3 , C1-C3alkyl, and C2-C3alkenyl, wherein C1-C3alkyl and C2-C3alkenyl are each optionally substituted with 1-3 halogens and one —OH.

7. The compound of claim 1 or a pharmaceutically acceptable salt thereof, selected from the structures below:

8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, selected from the structures below:

TABLE 1

EX

R 1

R 2

R 3

157

CH 3

CN

158

CH 3

CN

159

CH 3

CN

160

CH 3

CN

161

CH 3

CN

162

CH 3

CN

163

CH 3

CN

TABLE 2

EX

R 1

R 2

R 3

184

CH 3

CN

185

CH 3

CN

187

CH 3

Br

188

CH 3

Br

TABLE 3

Ex

R

189

190

191

192

193

194

195

196

197

198

199

200

201

TABLE 5

Ex

R 4

R 5

R 6

R 7

258

H

Br

H

COCH3

262

H

H

CH3

270

H

Br

H

271

H

Br

H

272

H

Br

H

276

H

CN

H

CH3

282

H

CN

H

COCH3

283

H

CN

H

284

H

CN

H

285

H

CN

H

286

H

CN

H

287

H

CN

H

TABLE 12

Ex

R 6

366

367

368

369

370

371

372

373

374

375

376

377

378

379

380

381

382

383

384

385

386

387

388

389

390

391

392

393

394

395

396

397

398

399

400

401

402

403

404

405

406

407

408

409

410

411

412

413

414

415

416

417

418

419

420

421

422

423

424

425

426

427

428

429

430

431

432

433

434

435

436

437

438

439

440

441

TABLE 13

Ex

R

442

443

444

445

446

447

448

449

450

451

452

453

454

455

456

457

458

459

460

461

462

463

464

465

466

467

468

469

470

TABLE 14

Ex

R 6

472

473

TABLE 15

Ex

R 1

R 2

483

CN

484

CN

485

CN

486

Me

487

CN

488

CN

489

CN

TABLE 16

EXAMPLE

R 1

R 2

495

CN

496

CN

497

CN

498

CN

499

CN

TABLE 17

EXAMPLE

R

525

526

527

9. A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

10. A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable carrier, and one or more active ingredients selected from the group consisting of:

(a) PPAR gamma agonists and partial agonists;

(b) biguanides;

(c) protein tyrosine phosphatase-1B (PTP-1B) inhibitors,

(d) dipeptidyl peptidase IV (DP-IV) inhibitors;

(e insulin;

(f) sulfonylureas;

(g) α-glucosidase inhibitors;

(h) one or more compounds selected from the group consisting of (a) HMG-CoA reductase inhibitors; (b) bile acid sequestrants; (c) niacin, nicotinyl alcohol, nicotinamide, and nicotinic acid or a salt thereof; (d) PPARα agonists; (e) cholesterol absorption inhibitors; (f) acyl CoA:cholesterol acyltransferase (ACAT) inhibitors; (g) phenolic anti-oxidants, and (h) a microsomal triglyceride transfer protein (MTP)/ApoB secretion inhibitor;

(i) PPARα/γdual agonists;

(j) PPARδ agonists;

(k) antiobesity compounds

(l) ileal bile acid transporter inhibitors;

(m) anti-inflammatory agents;

(n) glucagon receptor antagonists;

(o) GLP-1,

(p) and GIP-1.

11. A method of treating atherosclerosis or raising HDL in a patient in need of treatment comprising the administration of a therapeutically effective amount of the compound of claim 1 or a pharmaceutically acceptable salt thereof.

12. A method of treating atherosclerosis or raising HDL in a patient in need of treatment comprising the administration of a therapeutically effective amount of the compound of claim 2 , or a pharmaceutically acceptable salt thereof.