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Claims for Patent: 6,413,980

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Claims for Patent: 6,413,980

Title: Nitrogen containing heterobicycles as factor Xa inhibitors
Abstract:The present application describes nitrogen containing heterobicyclics and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
Inventor(s): Fevig; John M. (Lincoln University, PA), Cacciola; Joseph (Newark, DE), Clark; Charles G. (Cherry Hill, NJ), Han; Qi (Wilmington, DE), Lam; Patrick Yuk Sun (Chadds Ford, PA), Pinto; Donald J.P. (Kennett Square, PA), Pruitt; James R. (Landenberg, PA), Quan; Mimi L. (Newark, DE), Rossi; Karen A. (Newark, DE)
Assignee: Bristol-Myers Squibb Pharma Company (Princeton, NJ)
Application Number:09/470,326
Patent Claims: 1. A compound selected from the group: ##STR233##

or a stereoisomer or pharmaceutically acceptable salt thereof, wherein compounds of the above formulas are substituted with 0-2 R.sup.3 ;

G is a group of formula I or II: ##STR234##

ring D is selected from --(CH.sub.2).sub.3 --,--(CH.sub.2).sub.4 --,--CH.sub.2 N=CH--, --CH.sub.2 CH.sub.2 N=CH--, and a 5-6 membered aromatic system, containing from 0-2 heteroatoms selected from the group N, O, and S, provided that from 0-1 O and S atoms are present;

ring D, when present, is substituted with 0-2 R;

E is selected from phenyl, pyridyl, pyrimidyl, pyrazinyl, and pyridazinyl, substituted with 0-1 R;

R is selected from Cl, F, Br, I, OH, C.sub.1-3 alkoxy, NH.sub.2, NH(C.sub.1-3 alkyl), N(C.sub.1-3 alkyl).sub.2, CH.sub.2 NH.sub.2, CH.sub.2 NH (C.sub.1-3 alkyl), CH.sub.2 N(C.sub.1-3 alkyl).sub.2, CH.sub.2 CH.sub.2 NH.sub.2, CH.sub.2 CH.sub.2 NH(C.sub.1-3 alkyl), and CH.sub.2 CH.sub.2 N(C.sub.1-3 alkyl).sub.2 ;

alternatively, ring D is absent;

when ring D is absent, ring E is selected from phenyl, pyridyl, pyrimidyl, pyrazinyl, and pyridazinyl, and ring E is substituted with R" and R';

R" is selected from F, Cl, Br, I, OH, C.sub.1-3 alkoxy, CN, C(=NR.sup.8)NR.sup.7 R.sup.9, NHC(=NR.sup.8)NR.sup.7 R.sup.9, NR.sup.8 CH(=NR.sup.7), C(O)NR.sup.7 R.sup.8, (CR.sup.8 R.sup.9).sub.t NR.sup.7 R.sup.8, SH, C.sub.1-3 alkyl-S, S(O)R.sup.3b, S(O).sub.2 R.sup.3a, S(O).sub.2 NR.sup.2 R.sup.2a, and OCF.sub.3 ;

R' is selected from H, F, Cl, Br, I, SR.sup.3, CO.sub.2 R.sup.3, NO.sub.2, (CH.sub.2).sub.t OR.sup.3, C.sub.1-4 alkyl, OCF.sub.3, CF.sub.3, C(O)NR.sup.7 R.sup.8, and (CR.sup.8 R.sup.9).sub.t NR.sup.7 R.sup.8 ; alternatively, R" and R' combine to form methylenedioxy or ethylenedioxy;

Z is N or CR.sup.1a ;

Z.sup.1 is S, O, or NR.sup.3 ;

Z.sup.2 is selected from H, C.sub.1-4 alkyl, phenyl, benzyl, C(O)R.sup.3, and S(O).sub.p R.sup.3c ;

R.sup.1a is selected from H, --(CH.sub.2).sub.r --R.sup.1', --CH =CH--R.sup.1', NCH.sub.2 R.sup.1", OCH.sub.2 R.sup.1", SCH.sub.2 R.sup.1", NH(CH.sub.2).sub.2 (CH.sub.2).sub.t R.sup.1', O(CH.sub.2).sub.2 (CH.sub.2).sub.t R.sup.1', and S(CH.sub.2).sub.2 (CH.sub.2).sub.t R.sup.1' ;

R.sup.1' is selected from H, C.sub.1-3 alkyl, F, Cl, Br, I, --CN, --CHO, (CF.sub.2).sub.r CF.sub.3, (CH.sub.2).sub.r OR.sup.2, NR.sup.2 R.sup.2a, C(O)R.sup.2c, OC(O)R.sup.2, (CF.sub.2).sub.r CO.sub.2 R.sup.2c, S(O).sub.p R.sup.2b, NR.sup.2 (CH.sub.2).sub.r OR.sup.2, C(=NR .sup.2c)NR.sup.2 R.sup.2a, NR.sup.2 C(O)R.sup.2b, NR.sup.2 C(O)R.sup.3, NR.sup.2 C(O)NHR.sup.2b, NR.sup.2 C(O).sub.2 R.sup.2a, OC(O)NR.sup.2a R.sup.2b, C(O)NR.sup.2 R.sup.2a, C(O)NR.sup.2 (CH.sub.2).sub.r OR.sup.2, SO.sub.2 NR.sup.2 R.sup.2a, NR.sup.2 SO.sub.2 R.sup.2b, C.sub.3-6 carbocyclic residue substituted with 0-2 R.sup.4a, and 5-10 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R.sup.4a ;

R.sup.1" is selected from H, CH(CH.sub.2 OR.sup.2).sub.2, C(O)R.sup.2c, C(O)NR.sup.2 R.sup.2a, S(O)R.sup.2b, S(O).sub.2 R.sup.2b, and SO.sub.2 NR.sup.2 R.sup.2a ;

R.sup.2, at each occurrence, is selected from H, CF.sup.3, C.sub.1-6 alkyl, benzyl, C.sub.3-6 carbocyclic residue substituted with 0-2 R.sup.4b, a C.sub.3-6 carbocyclic--CH.sub.2 -- residue substituted with 0-2 R.sup.4b, and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R.sup.4b ;

R.sup.2a, at each occurrence, is selected from H, CF.sub.3, C.sub.1-6 alkyl, benzyl, C.sub.3-6 carbocyclic residue substituted with 0-2 R.sup.4b, and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R.sup.4b ;

R.sup.2b, at each occurrence, is selected from CF.sub.3, C.sub.1-4 alkoxy, C.sub.1-6 alkyl, benzyl, C.sub.3-6 carbocyclic residue substituted with 0-2 R.sup.4b, 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R.sup.4b ;

R.sup.2c, at each occurrence , is selected from CF.sub.3, OH, C.sub.1-4 alkoxy, C.sub.1-6 alkyl, benzyl, C.sub.3-6 carbocyclic residue substituted with 0-2 R.sup.4b, and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 014 3 R.sup.4b ;

alternatively, R.sup.2 and R.sup.2a, together with the atom to which they are attached, combine to form a 5 or 6 membered saturated, partially saturated or unsaturated ring substituted with 0-2 R.sup.4b and containing from 0-1 additional heteroatoms selected from the group consisting of N, O, and S;

R.sup.3, at each occurrence, is selected from H, C.sub.1-4 alkyl, and phenyl;

R.sup.3a, at each occurrence, is selected from H, C.sub.1-4 alkyl, and phenyl;

R.sup.3b, at each occurrence, is selected from H, C.sub.1-4 alkyl, and phenyl;

R.sup.3c, at each occurrence, is selected from C.sub.1-4 alkyl, and phenyl;

A is selected from: C.sub.3-10 carbocyclic residue substituted with 0-2 R.sup.4, and 5-10 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R.sup.4 ;

B is selected from: Y, X-Y, C(=NR.sup.2)NR .sup.2 R.sup.2a, and NR.sup.2 C(=NR.sup.2)NR.sup.2 R.sup.2a, provided that B is other than a cycloalkoxy group;

X is selected from C.sub.1-4 alkylene, --CR.sup.2 (CR.sup.2 R.sup.2b)(CH.sub.2).sub.t --, --C(O)--, --C(=NR.sup.1")--, --CR.sup.2 (NR.sup.1"R.sup.2)--, --CR.sup.2 (OR.sup.2)-, --CR.sup.2 (SR.sup.2)--, --C(O)CR.sup.2 R.sup.2a --, --CR.sup.2 R.sup.2a C(O), --S(O).sub.p --, --S(O).sub.p CR.sup.2 R.sup.2a --, --CR.sup.2 R.sup.2a S(O).sub.p --, --S(O).sub.2 NR.sup.2 --, --NR.sup.2 S(O).sub.2 --, --NR.sup.2 S(O).sub.2 CR.sup.2 R.sup.2a --, --CR.sup.2 R.sup.2a S(O).sub.2 NR.sup.2 --, --NR.sup.2 S(O).sub.2 NR.sup.2 --, --C(O)NR.sup.2 --, --NR.sup.2 C(O)--, --C(O)NR.sup.2 CR.sup.2 R.sup.2a --,--NR.sup.2 C(O)CR.sup.2 R.sup.2a --, --CR.sup.2 R.sup.2a C(O)NR.sup.2 --, --CR.sup.2 R.sup.2a NR.sup.2 C(O)--, --NR.sup.2 C(O)O--, --OC(O)NR.sup.2 --, --NR.sup.2 C(O)NR.sup.2 --, --NR.sup.2 --, --NR.sup.2 CR.sup.2 R.sup.2a --, --CR.sup.2 R.sup.2a NR.sup.2 --, O, --CR.sup.2 R.sup.2a O--, and --OCR.sup.2 R.sup.2a --;

Y is selected from: CH.sub.2 NR.sup.2 R.sup.2a ; CH.sub.2 CH.sub.2 NR.sup.2 R.sup.2a ; C.sub.3-10 carbocyclic residue substituted with 0-2 R.sup.4a, and 5-10 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R.sup.4a ;

R.sup.4, at each occurrence, is selected from H, =O, (CH.sub.2).sub.r OR.sup.2, F, Cl, Br, I, C.sub.1-4 alkyl, --CN, NO.sub.2, (CH.sub.2).sub.r NR.sup.2 R.sup.2a, (CH.sub.2).sub.r C(O)R.sup.2c, NR.sup.2 C(O)R.sup.2b, C(O)NR.sup.2 R.sup.2a, NR.sup.2 C(O)NR.sup.2 R.sup.2a, C(=NR.sup.2)NR.sup.2 R.sup.2a, C(=NS(O).sub.2 R.sup.5)NR.sup.2 R.sup.2a, NHC(=NR.sup.2)NR.sup.2 R.sup.2a, C(O)NHC(=NR.sup.2)NR.sup.2 R.sup.2a, SO.sub.2 NR.sup.2 R.sup.2a, NR.sup.2 SO.sub.2 NR.sup.2 R.sup.2a, NR.sup.2 SO.sub.2 --C.sub.1-4 alkyl, NR.sup.2 SO.sub.2 R.sup.5, S(O).sub.p R.sup.5, (CF.sub.2).sub.r CF.sub.3, NCH.sub.2 R.sup.1", OCH.sub.2 R.sup.", SCH.sub.2 R.sup.1", N(CH.sub.2).sub.2 (CH.sub.2).sub.t R.sup.1', O(CH.sub.2).sub.2 (CH.sub.2).sub.t R.sup.1', and S(CH.sub.2).sub.2 (CH.sub.2.sub.t R.sup.1' ;

alternatively, one R.sup.4 is a 5-6 membered aromatic heterocycle containing from 1-4 heteroatoms selected from the group consisting of N, O, and S;

R.sup.4a, at each occurrence, is selected from H, =O, (CH.sub.2).sub.r OR.sup.2, (CH.sub.2).sub.r --F, (CH.sub.2).sub.r --Br, (CH.sub.2).sub.r --Cl, Cl, Br, F, I, C.sub.1-4 alkyl, --CN, NO.sub.2, (CH.sub.2).sub.r NR.sup.2 R.sup.2a, (CH.sub.2).sub.r C(O)R.sup.2c, NR.sup.2 C(O)R.sup.2b, C(O)NR.sup.2 R.sup.2a, (CH.sub.2).sub.r N=CHOR.sup.3, C(O)NH(CH.sub.2).sub.2 NR.sup.2 R.sup.2a, NR.sup.2 C(O)NR.sup.2 R.sup.2a, C(=NR.sup.2)NR.sup.2 R.sup.2a, NHC(=NR.sup.2)NR.sup.2 R.sup.2a, SO.sub.2 NR.sup.2 R.sup.2a, NR.sup.2 SO.sub.2 NR.sup.2 R.sup.2a, NR.sup.2 SO.sub.2 --C.sub.1-4 alkyl, C(O)NHSO.sub.2 --C.sub.1-4 alkyl, NR.sup.2 SO.sub.2 R.sup.5, S(O).sub.p R.sup.5, and (CF.sub.2).sub.r CF.sub.3 ;

alternatively, one R.sup.4a is a 5-6 membered aromatic heterocycle containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-1 R.sup.5 ;

R.sup.4b, at each occurrence, is selected from H, =O, (CH.sub.2).sub.r OR.sup.3, F, Cl, Br, I, C.sub.1-4 alkyl, --CN, NO.sub.2, (CH.sub.2).sub.r NR.sup.3 R.sup.3a, (CH.sub.2).sub.r C(O)R.sup.3, (CH.sub.2).sub.r C(O)OR.sup.3c, NR.sup.3 C(O)R.sup.3a, C(O)NR.sup.3 R.sup.3a, NR.sup.3 C(O)NR.sup.3 R.sup.3a, C(=NR.sup.3 NR.sup.3 R.sup.3a, NR.sup.3 C(=NR.sup.3)NR.sup.3 R.sup.3a, SO.sub.2 NR.sup.3 R.sup.3a, NR.sup.3 SO.sub.2 NR.sup.3 R.sup.3a, NR.sup.3 SO.sub.2 --C.sub.1-4 alkyl, NR.sup.3 SO.sub.2 CF.sub.3, NR.sup.3 SO.sub.2 --phenyl, S(O).sub.p CF.sub.3, S(O).sub.p --C.sub.1-4 alkyl, S(O).sub.p --phenyl, and (CF.sub.2).sub.r CF.sub.3 ;

R.sup.5, at each occurrence, is selected from CF.sub.3, C.sub.1-6 alkyl, phenyl substituted with 0-2 R.sup.6, and benzyl substituted with 0-2 R.sup.6 ;

R.sup.6, at each occurrence, is selected from H, OH, (CH.sub.2).sub.r OR.sup.2, halo, C.sub.1-4 alkyl, CN, NO.sub.2, (CH.sub.2).sub.r NR.sup.2 R.sup.2a, (CH.sub.2).sub.r C(O)R.sup.2b, NR.sup.2 C(O)R.sup.2b, NR.sup.2 C(O)NR.sup.2 R.sup.2a, C(=NH)NH.sub.2, NHC(=NH)NH.sub.2, SO.sub.2 NR.sup.2 R.sup.2a, NR.sup.2 SO.sub.2 NR.sup.2 R.sup.2a, and NR.sup.2 SO.sub.2 C.sub.1-4 alkyl;

R.sup.7, at each occurrence, is selected from H, OH, C.sub.1-6 alkyl, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxy, C.sub.1-4 alkoxycarbonyl, (CH.sub.2).sub.n --phenyl, C.sub.6-10 aryloxy, C.sub.6-10 aryloxycarbonyl, C.sub.6-10 arylmethylcarbonyl, C.sub.1-4 alkylcarbonyloxy C.sub.1-4 alkoxycarbonyl, C.sub.6-10 arylcarbonyloxy C.sub.1-4 alkoxycarbonyl, C.sub.1-6 alkylaminocarbonyl, phenylaminocarbonyl, and phenyl C.sub.1-4 alkoxycarbonyl;

R.sup.8, at each occurrence, is selected from H, C.sub.1-6 alkyl and (CH.sub.2).sub.n --phenyl;

alternatively, R.sup.7 and R.sup.8 combine to form a 5 or 6 membered saturated, ring which contains from 0-1 additional heteroatoms selected from the group consisting of N, O, and S;

R.sup.9, at each occurrence, is selected from H, C.sub.1-6 alkyl and (CH.sub.2).sub.n --phenyl;

n, at each occurrence, is selected from 0, 1, 2, and 3;

m, at each occurrence, is selected from 0, 1, and 2;

p, at each occurrence, is selected from 0, 1, and 2;

r, at each occurrence, is selected from 0, 1, 2, and 3;

s, at each occurrence, is selected from 0, 1, and 2;

t, at each occurrence, is selected from 0, 1, 2, and 3; and,

provided that when the compound is a 1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one and Y is a nitrogen--containing non-aromatic heterocycle attached via a nitrogen atom, then either (a) B is X--Y or (b) Y is substituted with at least one R.sup.4a that is other than H and alkyl.

2. A compound of claim 1, wherein the compound is selected from the group: ##STR235##

wherein compounds of the above formulas are substituted with 0-2 R.sup.3 ;

G is selected from the group: ##STR236## ##STR237## ##STR238##

A is selected from one of the following carbocyclic and heterocyclic systems which are substituted with 0-2 R.sup.4 ; phenyl, piperidinyl, piperazinyl, pyridyl, pyrimidyl, furanyl, morpholinyl, thiophenyl, pyrrolyl, pyrrolidinyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, oxadiazolyl, thiadiazolyl, triazolyl, 1, 2, 3--oxadiazolyl, 1, 2, 4--oxadiazolyl, 1, 2, 5--oxadiazolyl, 1, 3, 4--oxadiazolyl, 1, 2, 3--thiadiazolyl, 1, 2, 4--thiadiazolyl, 1, 2, 5--thiadiazolyl, 1, 3, 4--thiadiazolyl, 1, 2, 3--triazolyl, 1, 2, 4--triazolyl, 1, 2, 5--triazolyl, 1, 3, 4--triazolyl, benzofuranyl, benzothiofuranyl, indolyl, benzimidazolyl, benzoxazolyl, benzthiazolyl, indazolyl, benzisoxazolyl, benzisothiazolyl, and isoindazolyl;

B is selected from: Y and X--Y, provided that B is other than a cycloalkoxy group;

X is selected from C.sub.1-4 alkylene, --C(O)--, --C(=NR.sup.1")--, --CR.sup.2 (NR.sup.1" R.sup.2)--, --C(O)CR.sup.2 R.sup.2a --, --CR.sup.2 R.sup.2a C(O), --C(O)NR.sup.2 --, --NR.sup.2 C(O)--, --C(O)NR.sup.2 CR.sup.2 R.sup.2a --, --NR.sup.2 C(O)CR.sup.2 R.sup.2a --, --CR.sup.2 R.sup.2a C(O)NR.sup.2 --, --CR.sup.2 R.sup.2a NR.sup.2 C(O)--, --NR.sup.2 C(O)NR.sup.2 --, --NR.sup.2 --, --NR.sup.2 CR.sup.2 R.sup.2a --, --CR.sup.2 R.sup.2a NR.sup.2 --, O, --CR.sup.2 R.sup.2a O--, and --OCR.sup.2 R.sup.2a --;

Y is CH.sub.2 NR.sup.2 R.sup.2a or CH.sub.2 CH.sub.2 NR.sup.2 R.sup.2a ;

alternatively, Y is selected from one of the following carbocyclic and heterocyclic systems that are substituted with 0-2 R.sup.4a ; cyclopropyl, cyclopentyl, cyclohexyl, phenyl, piperidinyl, piperazinyl, pyridyl, pyrimidyl, furanyl, morpholinyl, thiophenyl, pyrrolyl, pyrrolidinyl, oxazolyl, isoxazolyl, isoxazolinyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, oxadiazolyl, thiadiazolyl, triazolyl, 1, 2, 3--oxadiazolyl, 1, 2, 4--oxadiazolyl, 1, 2, 5--oxadiazolyl, 1, 3, 4--oxadiazolyl, 1, 2, 3--thiadiazolyl, 1, 2, 4--thiadiazolyl, 1, 2, 5--thiadiazolyl, 1, 3, 4--thiadiazolyl, 1, 2, 3--triazolyl, 1, 2, 4--triazolyl, 1, 2, 5--triazolyl, 1, 3, 4--triazolyl, benzofuranyl, benzothiofuranyl, indolyl, benzimidazolyl, benzoxazolyl, benzthiazolyl, indazolyl, benzisoxazolyl, benzisothiazolyl, and isoindazolyl;

alternatively, Y is selected from the following bicyclic heteroaryl ring systems: ##STR239##

K is selected from O, S, NH, and N;

s is 0; and,

provided that when the compound is a 1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin --7--one and Y is a nitrogen--containing non--aromatic heterocycle attached via a nitrogen atom, then either (a) B is X--Y or (b) Y is substituted with at least one R.sup.4a that is other than H and alkyl.

3. A compound of claim 2, wherein the compound is selected from the group: ##STR240##

wherein compounds of the above formulas are substituted with 0-2 R.sup.3 ;

G is selected from the group: ##STR241## ##STR242##

A is selected from phenyl, pyridyl, and pyrimidyl, and is substituted with 0-2 R.sup.4 ;

B is selected from X-Y, phenyl, pyrrolidino, morpholino, 1, 2, 3--triazolyl, and imidazolyl, and is substituted with 0-1 R.sup.4a ;

R.sup.2, at each occurrence, is selected from H, CH.sub.3, CH.sub.2 CH.sub.3, cyclopropylmethyl, cyclobutyl, and cyclopentyl;

R.sup.2a, at each occurrence, is H, or CH.sub.3 ;

alternatively, R.sup.2 and R.sup.2a, together with the atom to which they are attached, combine to form pyrrolidine substituted with 0-2 R.sup.4b ;

R.sup.4, at each occurrence, is selected from OH, (CH.sub.2).sub.r OR.sup.2, halo, C.sub.1-4 alkyl, (CH.sub.2).sub.r NR.sup.2 R.sup.2a, and (CF.sub.2).sub.r CF.sub.3 ;

R.sup.4a is selected from C.sub.1-4 alkyl, CF.sub.3, (CH.sub.2).sub.r OR.sup.2, (CH.sub.2).sub.r NR.sup.2 R.sup.2a, S(O).sub.p R.sup.5, SO.sub.2 NR.sup.2 R.sup.2a, and 1--CF.sub.3 --tetrazol--2--yl;

R.sup.4b, at each occurrence, is selected from H, CH.sub.3, and OH;

R.sup.5, at each occurrence, is selected from CF.sub.3, C.sub.1-6 alkyl, phenyl, and benzyl;

X is CH.sub.2 or C(O);

Y is selected from pyrrolidino and morpholino; and,

r, at each occurrence, is selected from 0, 1, and 2;

provided that when the compound is a 1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one and Y is a nitrogen--containing non--aromatic heterocycle attached via a nitrogen atom, then either (a) B is X--Y or (b) Y is substituted with at least one R.sup.4a that is other than H and alkyl.

4. A compound of claim 3, wherein:

G is selected from: ##STR243##

A is selected from the group: phenyl, 2--pyridyl, 3--pyridyl, 2--pyrimidyl, 2--Cl--phenyl, 3--Cl--phenyl, 2--F--phenyl, 3--F--phenyl, 2--methylphenyl, 2--aminophenyl, and 2--methoxyphenyl; and,

B is selected from the group: 2--(aminosulfonyl)phenyl, 2--(methylaminosulfonyl)phenyl, 1--pyrrolidinocarbonyl, 2--(methylsulfonyl)phenyl, 2--(N,N--dimethylaminomethyl)phenyl, 2--(N--pyrrolidinylmethyl)phenyl, 1--methyl--2--imidaolyl, 2--methyl--1--imidazolyl, 2--(dimethylaminomethyl)--1--imidazolyl, 2--(N--(cyclopropylmethyl)aminomethyl)phenyl, 2--(N--(cyclobutyl)aminomethyl)phenyl, 2--(N--(cyclopentyl)aminomethyl)phenyl, and 2--(N--(3--hydroxypyrrolidinyl)methyl)phenyl.

5. A compound of claim 2, wherein the compound is selected from the group: ##STR244##

wherein compounds of the above formulas are substituted with 0-2 R.sup.3 ;

G is selected from the group: ##STR245## ##STR246##

6. A compound of claim 2, wherein the compound is selected from the group: ##STR247##

wherein compounds of the above formulas are substituted with 0-2 R.sup.3.

7. A compound of claim 2, wherein:

G is selected from the group: ##STR248## ##STR249##

8. A compound of claim 7, wherein:

G is selected from: ##STR250##

9. A compound of claim 4, wherein:

A is selected from phenyl, pyridyl, and pyrimidyl, and is substituted with 0-2 R.sup.4 ;

B is selected from X--Y, phenyl, pyrrolidino, morpholino, 1, 2, 3--triazolyl, and imidazolyl, and is substituted with 0-1 R.sup.4a ;

R.sup.2, at each occurrence, is selected from H, CH.sub.3, CH.sub.2 CH.sub.3, cyclopropylmethyl, cyclobutyl, and cyclopentyl;

R.sup.2a, at each occurrence, is H or CH.sub.3 ;

alternatively, R.sup.2 and R.sup.2a, together with the atom to which they are attached, combine to form pyrrolidine substituted with 0-2 R.sup.4b ;

R.sup.4, at each occurrence, is selected from OH, (CH.sub.2).sub.r OR.sup.2, halo, C.sub.1-4 alkyl, (CH.sub.2).sub.r NR.sup.2 R.sup.2a, and (CF.sub.2).sub.r CF.sub.3 ;

R.sup.4a is selected from C.sub.1-4 alkyl, CF.sub.3, (CH.sub.2).sub.r OR.sup.2, (CH.sub.2).sub.r NR.sup.2 R.sup.2a, S(O).sub.p R.sup.5, SO.sub.2 NR.sup.2 R.sup.2a, and 1--CF.sub.3 --tetrazol--2--yl;

R.sup.4b, at each occurrence, is selected from H, CH.sub.3, and OH;

R.sup.5, at each occurrence, is selected from CF.sub.3, C.sub.1-6 alkyl, phenyl, and benzyl;

X is CH.sub.2 or C(O);

Y is selected from pyrrolidino and morpholino; and,

r, at each occurrence, is selected from 0, 1, and 2;

provided that the compound is a 1, 4, 5, 6,--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one and Y is a nitrogen--containing non--aromatic heterocycle attached via a nitrogen atom, then either (a) B is X--Y or (b) Y is substituted with at least one R.sup.4a that is other than H and alkyl.

10. A compound of claim 2, wherein:

A is selected from phenyl, pyridyl, and pyrimidyl, and is substituted with 0-2 R.sup.4.

11. A compound of claim 2, wherein:

B is selected from X-Y, phenyl, pyrrolidino, morpholino, 1, 2, 3--triazolyl, and imidazolyl, and is substituted with 0-1 R.sup.4a.

12. A compound of claim 2, wherein:

X is CH.sub.2 or C(O); and,

Y is selected from pyrrolidino and morpholine.

13. A compound of claim 2, wherein:

R.sup.4, at each occurrence, is selected from OH, (CH.sub.2).sub.r OR.sup.2, halo, C.sub.1-4 alkyl, (CH.sub.2).sub.r NR.sup.2 R.sup.2a, and (CF.sub.2).sub.r CF.sub.3.

14. A compound of claim 2, wherein: R.sup.4a is selected from C.sub.1-4 alkyl, CF.sub.3, (CH.sub.2).sub.r OR.sup.2, (CH.sub.2).sub.r NR.sup.2 R.sup.2a, S(O).sub.p R.sup.5, SO.sub.2 NR.sup.2 R.sup.2a, and 1--CF.sub.3 --tetrazol--2--yl.

15. A compound of claim 9, wherein:

A is selected from the group: phenyl, 2--pyridyl, 3--pyridyl, 2--pyrimidyl, 2--Cl--phenyl, 3--Cl--phenyl, 2--F--phenyl, 3--F--pheny, 2--methylphenyl, 2--aminophenyl, and 2--methoxyphenyl; and,

B is selected from the group: 2--(aminosulfonyl)phenyl, 2--(methylaminosulfonyl)phenyl, 1--pyrrolidinocarbonyl, 2--(methylsulfonyl)phenyl, 2--(N,N--dimethylaminomethyl)phenyl, 2--(N--pyrrolidinylmethyl)phenyl, 1--methyl--2--imidazolyl, 2--methyl--1--imidazolyl, 2--(dimethylaminomethyl)--1--imidazolyl, 2--(N--(cyclopropylmethyl)aminomethyl)phenyl, 2--(N--(cyclobutyl)aminomethyl)phenyl, 2--(N--(cyclopentyl)aminomethyl)phenyl, and 2--(N--(3--hydroxypyrrolidinyl)methyl)phenyl.

16. A compound of claim 10, wherein:

A is selected from the group: phenyl, 2--pyridyl, 3--pyridyl, 2--pyrimidyl, 2--Cl--phenyl, 2--F--phenyl, 3--F--phenyl, 2--methyphenyl, 2--aminophenyl, and 2--methoxyphenyl.

17. A compound of claim 11, wherein:

B is selected from the group: 2--(aminosulfonyl)phenyl, 2--(methylaminosulfonyl)phenyl, 1--pyrrolidinocarbonyl, 2--(methylsulfonyl)phenyl, 2--(N,N--dimethylaminomethyl)phenyl, 2--(N--pyrrolidinymethyl)phenyl, 1--methyl--2--imidazolyl, 2--methyl--1--imidazolyl, 2--(dimethylaminomethyl)--1--imidazolyl, 2--(N-(cyclopropylmethyl)aminomethyl)phenyl, 2--(N--(cyclobutyl)aminomethyl)phenyl, 2--(N--(cyclopentyl)aminomethyl)phenyl, and 2--(N--(3--hydroxypyrrolidinyl)methyl)phenyl.

18. A compound selected from:

1--[3--Aminoiminomethylphenyl]--3--methyl--6--[2'--aminosulfonyl--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

1--[2--Aminomethylphenyl]--3--methyl--6--[2'--aminosulfonyl--[1, 1'--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

1--[3--Aminobenzisoxazol--5'--yl]--3--methyl--6--[2'--aminsulfonyl--[1, 1']--biphen --4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin --7--one;

1--[3--Aminbenzisoxazol--5'--yl]--3--methyl--6--[`'--N--pyrrolidinylmethyl- -[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydrol--7H--pyrazolo--[3, 4--c]--pyridin--7--one;

1--[3--Aminobenzisoxazol--5'--ul]--3--methyl--6--[2'--(3--(S)--hydroxy--N-- pyrrolidinyl)methyl--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydro--7H--pyrazolo--[3, 4--c]--pyridin--7--one;

1--[3--Aminbenzisoxazol--5'--yl]--3--methyl--6--[2'--N--isopropylaminomethy l--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydro--7H--pyrazolo--[3, 4--c]--pyridin--7--one;

1--[3--Aminobenzisoxazol--5'--yl]--3--methyl--6--[2'--N,N--dimethylamiinome thyl--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydro--7H--pyrazolo--[3, 4--c]--pyridin--7--one; 1--[3--Aminobenzisoxazol--5'--yl]--3--methyl--6--[2'--methylsulfonyl--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydro--7H--pyrazolo--[3, 4--c]--pyridin--7--one;

1--[3--Aminobenzisoxazol--5'--methylsulfonyl--3--fluoro--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydro--7H--pyrazolo--[3, 4--c]--pyridin--7--one;

1--[2--Aminomethyphenyl]--3--trifluoromethyl--6--[2'--methylsulfonyl--3--fl uoro--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

1--[2--Aminomethylphenyl]--3--trifluoromethyl--6--[2'--aminosulfonyl--3--fl uoro--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetahyfropyrazolo--[3, 4--c]--pyridin--7--one;

1--[2--Aminomethylphenyl]--3--trifluoromethyl--6--[2'--methysulfonnyl--[1, 1]--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

1--[2--Aminomethylphenyl]--3--trifluoromethyl--6--[2'--N,N--dimethylaminome thyl--3--fluoro--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

1--[2--Aminomethylphenyl]--3--trigluoromethyl--6--[2'--(3--(R)--hydroxy--N- -pyrrolidinyl)methyl--3--fluoro--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

1--[3--Aminovenzisoxazol--5'--yl]--3--trifluoromethyl--6--[2'--dimethylamin omethyl--3--fluoro--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

1--[3--Aminobenzisoxazol--5'--yl]--3--trifluoromethyl--6--[2'--(3--(R)--hyd roxy--N--pyrrolidinylmethyl--3--fluoro--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--ppyridin--7-- one;

1--[--Aminobenzisoxazol--5'--yl]--3--trifluoromethyl--6--[2'--(3--(R)--hydr oxy--N--pyrrolidinyl)methyl--[1, 1']--biphen--4--1, 4, 4, 6--tetrahdropyraolo--[3, 4--c]--pyridin--7--one;

1--[3--Aminobenzisoxazol--5'--yl]--3--trifluoromethyl--6--[2'--isopropylami nomethyl--3--fluoro--[1, 1']--biphen --4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

1--[3--Aminobenzisoxazol--5'--yl]--3--trifluoromethyl--6--[2'--N--(2--methy limidazol--1--yl)methyl--3--fluoro--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c[--pyridin--7--one;

1--[3--Aminobenzisoxazol--5'--yl]--3--trifluoromethyl--6--[2'--N--pyrrolidi nomethyl--3--fluoro--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

1--[3--Aminobenzisoxazol--5'--yl--3--trifluoromethyl--6--[2'--oximinomethyl --3--fluoro--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

1--[4--Methoxyphenyl]--3--trifluoromethyl--6--[2'--(3--(R)--hydroxy--N--pyr rolidinyl)methyl--3--fluoro--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

1--[3--Aminomethylphenyl]--3--trifluoromethyl--6--[2'--methylsulfonyl--3--f luoro--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

1--[3--Aminobenzisoxazol--5'--yl]--3--trifluoromethyl--6--[2'--(3--(S)--hyd roxy--N--pyrrolidinyl)methyl--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

1--[3--Aminobenzisoxazol--5'--yl]--3--trifuoromethyl--6--[2'--N--(pyrrolind inyl)methyl--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

1--[3--Aminobenzisoxazol--5'--yl]--3--trifluoromethyl--6--[2'--N--(morpholi no)methyl--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

1--[3--Aminobenzisoxazol--5'--yl]--3--trifluoromethyl--6--[2'--N,N--dimethy laminomethyl--[1, ']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

1[4--Meethoxyphenyl]--3--trifluoromethyl--6--[(4--aminomethyl)phenyl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]pyridin--7--one;

1--[3--Aminomethylphenyl]--3--methyl--6--[(2'--N--((3--(S)--hydroxy)pyrroli dinyl)methyl--[1, 1']--biphen--4--yl)]--1, 4, 5, 6--tetrahydro--7H--pyrazolo--[3, 4--c]--pyridin--7--one;

1--[3--Aminomethylphenyl]--3--methyl--6--[(2'--methylsulfonyl--[1, 1']--biphen--4--yl)]--1, 4, 5, 6--tetrahydro--7H--pyrazolo[3, 4--c]pyridin--7--one;

1--[3--Aminobenzisoxazol--5'--yl]--3--methyl--6--[(3--fluoro--2'--N--(3(S)- -hydroxy)pyrrolidinylmethyl--[1, 1']--biphen--4--yl)[--1, 4, 5, 6--tetrahydro--7H--pyrazolo[3, 4--c pyridin--7--one;

1--[3--Aminobenisoxazol--5'--yl]--3--methyl--6--[(3--fluoro--2'--N--pyrroli dinylmethyl--[1, 1']--biphen--4--yl)]--1, 4, 5, 6--tetrahydro--7H--pyrazolo[3, 4--c]pyridin--7--one;

1--[1--Aminoisoquinolin--7'--yl]--3--trifluoromethyl--6--[4--(2--methylimid azol--1'--yl)phenyl]--1, 4, 5, 6--tetrahydroprazolo--[3, 4--c]--pyridin--7--one; and,

1--[3--Aminovenzisoxazol--5'--yl]--3--methyl--6--[4--(2--(dimethylaminometh yl)imidazol1'--yl)--2--flurohphenyl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

or a pharmaceuticlly acceptable salt form thereof.

19. A compound according to claim 18, wherein the compound is selected from the group:

1--[3--aminobenisoxazol--5'--yl]--3--methyl--6--[2'--aminosulfonyl--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

1--[3--aminobenzisoxazol--5'--yl]--3--trifluoromenthyl--6--[2'--(3--(R)--hy droxy--N--pyrrolidinyl)methyl--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c ]--pyridin--7--one;

1--[3--aminobenzisoxazol--5'--yl]--3--trufluoromethyl--6--['--N,N--dimethyl aminomethyl--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

1--[2--Aminomethylphenyl]--3--trifluoromethyl--6--[2'--methylsulfonyl--[1, 1]--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

1--[3--aminobenzisoxazol--5'--yl]--3--trifluoromethyl--6--[2'--dimethylamin omethyl--3--fluoro--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

1--[3--aminobenzisoxazol--5'--yl]--3--trifluoromethyl--6--[2'--(3--(R)--hyd roxy--N--pyrrolidinyl)methyl--3--fluoro--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one; and,

1--[1--aminoisoquinolin--7'--yl]--3--trifluoromethyl--6--[4--(2--methylimid azol--1'--yl)phenyl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one;

20. A compound according to claim 19, wherein the compound is:

1--[3--aminobenzisoxazol--5'--yl]--3--methyl--6--[2'--aminosulfonyl--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one or a pharmaceutically acceptable salt form thereof.

21. A compound according to claim 19, wherein the compound is:

1--[3--aminobenzisoxazol--5'--yl]--3--trifluoromethyl--6--[2'--(3--(R)--hyd roxy--N--pyrrolidinyl)methyl--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one or a pharmaceutically acceptable salt form thereof.

22. A compound according to claim 19, wherein the compound is:

1--[3--aminobenzisoxazol--5'--yl]--3--trifluoromethyl--6--[2'--N,N--dimethy laminomethyl--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one or a pharmaceutically acceptable salt form thereof.

23. A compound according to claim 19, wherein the compound is:

1--[2--aminomethylphenyl]--3--trifluoromethyl--6--[2'--methylsulfonyl--[1, 1]--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one or a pharmaceutically acceptable salt form thereof.

24. A compound according to claim 19, wherein the compound is:

1--[3--aminobenzisoxazol--5'--yl]--3--trifluoromethyl--6--[2 '--dimethylaminomethyl--3--fluoro--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one or a pharmaceutically acceptable salt form thereof.

25. A compound according to claim 19, wherein the compound is:

1--[--aminobenzisoxazol--5'--yl]--3--trifluoromethyl--6--[2'--(3--(R)--hydr oxy--N--pyrrolidinyl)methyl--3--fluoro--[1, 1']--biphen--4--yl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one or a pharmaceutically acceptable salt form thereof.

26. A compound according to claim 19, wherein the compound is:

1--[1--aminoisoquinolin--7'--yl]--3--trifluoromethyl--6--[4--(2--methylimid azol--1'--yl)phenyl]--1, 4, 5, 6--tetrahydropyrazolo--[3, 4--c]--pyridin--7--one or a pharmaceutically acceptable salt form thereof.

27. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt form thereof.

28. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 2 or a pharmaceutically acceptable salt form thereof.

29. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 3 or a pharmaceutically acceptable salt form thereof.

30. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 4 or a pharmaceutically acceptable salt form thereof.

31. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 5 or a pharmaceutically acceptable salt form thereof.

32. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 6 or a pharmaceutically acceptable salt form thereof.

33. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 7 or a pharmaceutically acceptable salt form thereof.

34. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 8 or a pharmaceutically acceptable salt form thereof.

35. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 9 or a pharmaceutically acceptable salt form thereof.

36. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 10 or a pharmaceutically acceptable salt form thereof.

37. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 11 or a pharmaceutically acceptable salt form thereof.

38. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 12 or a pharmaceutically acceptable salt form thereof.

39. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 13 or a pharmaceutically acceptable salt form thereof.

40. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 14 or a pharmaceutically acceptable salt form thereof.

41. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 15 or a pharmaceutically acceptable salt form thereof.

42. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 16 or a pharmaceutically acceptable salt form thereof.

43. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 17 or a pharmaceutically acceptable salt form thereof.

44. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 18 or a pharmaceutically acceptable salt form thereof.

45. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 19 or a pharmaceutically acceptable salt form thereof.

46. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 20 or a pharmaceutically acceptable salt form thereof.

47. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 21 or a pharmaceutically acceptable salt form thereof.

48. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 22, or a pharmaceutically acceptable salt form thereof.

49. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 23 or a pharmaceutically acceptable salt form thereof.

50. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 24 or a pharmaceutically acceptable salt form thereof.

51. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 25 or a pharmaceutically acceptable salt form thereof.

52. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 26 or a pharmaceutically acceptable salt form thereof.

53. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable acceptable salt form thereof.

54. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 2 or a pharmaceutically acceptable salt form thereof.

55. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 3 or a pharmaceutically acceptable salt form thereof.

56. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 4 or a pharmaceutically acceptable salt form thereof.

57. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 5 or a pharmaceutically acceptable salt form thereof.

58. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 6 or a pharmaceutically acceptable salt form thereof.

59. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 7 or pharmaceutically acceptable salt form thereof.

60. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 8 or a pharmaceutically acceptable salt form thereof.

61. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 9 or a pharmaceutically acceptable salt form thereof.

62. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 10 or a pharmaceutically acceptable salt form thereof.

63. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 11 or a pharmaceutically acceptable salt form thereof.

64. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 12 or a pharmaceutically acceptable salt form thereof.

65. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 13 or a pharmaceutically acceptable salt form thereof.

66. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 14 or a pharmaceutically acceptable salt form thereof.

67. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 15 or a pharmaceutically acceptable salt form thereof.

68. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 16 or a pharmaceutically acceptable salt form thereof.

69. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 17 or a pharmaceutically acceptable salt form thereof.

70. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 18 or a pharmaceutically acceptable salt form thereof.

71. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 19 or a pharmaceutically acceptable salt form thereof.

72. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 20 or a pharmaceutically acceptable salt form thereof.

73. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 21 or pharmaceutically acceptable salt form thereof.

74. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 22 or pharmaceutically acceptable salt form thereof.

75. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 23 or a pharmaceutically acceptable salt form thereof.

76. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 24 or a pharmaceutically acceptable salt form thereof.

77. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 25 or a pharmaceutically acceptable salt form thereof.

78. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 26 or a pharmaceutically acceptable salt form thereof.
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