Renin inhibitors

A compound represented by the following structural formula:

• wherein:
• X1 is a covalent bond, —O—, —S—, —S(O)—, —S(O)2—;
• Y1 is a covalent bond or C1-C10 alkylene, C1-C10 alkenylene or C1-C10 alkynylene, each optionally substituted at one or more substitutable carbon atom with halogen, cyano, nitro, hydroxy, (C1-C3)alkyl, (C1-C3)alkoxy or halo(C1-C3)alkoxy, provided that Y1 is a covalent bond only when X1 is a covalent bond;
• A is a saturated or unsaturated 4-, 5-, 6-, or 7-membered ring which is optionally bridged by (CH2)p via bonds to two members of said ring, wherein said ring is composed of carbon atoms and 0-2 hetero atoms selected from the group consisting of 0, 1, or 2 nitrogen atoms, 0 or 1 oxygen atoms, and 0 or 1 sulfur atoms, said ring being optionally and independently substituted with zero to four halogen atoms, (C1-C6)alkyl groups, halo(C1-C6)alkyl groups or oxo groups such that when there is substitution with one oxo group on a carbon atom it forms a carbonyl group, and when there is substitution of one or two oxo groups on sulfur it forms sulfoxide or sulfone groups, respectively;
• p is 1 to 3;
• R1 is (C3-C7) cycloalkyl, phenyl, heteroaryl, or bicyclic heteroaryl each optionally substituted with 1 to 3 groups independently selected from:
• fluorine, chlorine, bromine, cyano, nitro, hydroxy, (C1-C6)alkyl. (C3-C6)cycloalkyl, (C4-C7)cycloalkylalkyl, (C2-C6)alkenyl, (C5-C7)cycloalkylalkenyl, (C2-C6)alkynyl, (C3-C6)cycloalkyl(C2-C4)alkynyl, halo(C1-C6)alkyl, halo(C3-C6)cycloalkyl, halo(C4-C7)cycloalkylalkyl, halo(C2-C6)alkenyl, halo(C3-C6)alkynyl, halo(C5-C7)-cycloalkylalkynyl, (C1-C6)alkoxy, (C3-C6)cycloalkoxy, (C4-C7)cycloalkylalkoxy, halo(C1-C6)alkoxy, halo(C3-C6)cycloalkoxy, halo(C4-C7)cycloalkylalkoxy and (C1-C6)alkanesulfonyl:
• and phenyl, heteroaryl, phenoxy, heteroaryloxy, phenylthio, heteroarylthio, benzyl, heteroarylmethyl, benzyloxy and heteroarylmethoxy, each optionally substituted with 1 to 3 groups independently selected from:
• fluorine, chlorine, bromine, cyano, nitro, hydroxy, (C1-C3)alkyl, halo(C1-C3)alkyl, (C1-C3)-alkoxy, and halo(C1-C3)alkoxy, and aminocarbonyl;
• R2 is —NHC(═NR12)(NH2), —NHC(═NR12)(NHR9),
• —OC(O)(NH2), —OC(S)(NH2), —SC(S)(NH2), —SC(O)(NH2), —OC(O)(NHR9), —OC(S)(NHR9), —SC(S)(NHR9), —SC(O)(NHR9), —NHC(O)OR9, —NHC(S)SR9, —NHC(S)OR9, —NHC(O)SR9, —C(O)R9, —C(S)R9, —C(O)(NH2), —C(S)(NH2), —C(O)(NHR9), —C(S)(NHR9) or —NHC(O)H, wherein R9 is a straight or branched C1-C5 alkyl, straight or branched C1-C5haloalkyl, (C3-C4)cycloalkyl or straight or branched C1-C5 alkoxyalkyl and R12 is H, (C1-C6)alkyl, phenyl, heteroaryl, cyano, nitro, —S(O)R9, —S(O2)R9, —S(O2)NHR9, —S(O2)NR9R9, —C(O)R9, —C(S)R9, —C(O)OR9, —C(S)OR9, —C(O)(NH2), —C(O)(NHR9);
• R3 is —H, —F, C1-C5 alkyl, —NHC(O)R10, —OH or —OR10, wherein R10 is C1-C3 alkyl, provided that when R3 is —F or —OH, then X1 is not —O—, —S—, —S(O)—, —S(O)2— and R2—Y1—X1 is not —OC(O)(NH2), —OC(S)(NH2), —SC(S)(NH2), —SC(O)(NH2), —OC(O)(NHR9), —OC(S)(NHR9), —SC(S)(NHR9), —SC(O)(NHR9), —NHC(O)OR9, —NHC(S)OR9, —NHC(S)SR9, —NHC(O)SR9 or —NHC(O)H;
• Q is Q1, Q2, Q3, Q4, Q5, or Q6:
• R4 is H, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C3)alkoxy(CI-C3)alkyl, or cyano(C1-C6)alkyl;
• G is OH, ORe, NH2, NHRe, NReRf, C(=NH)NH2, C(═NH)NHRe, NHC(═NH)NH2, or NHC(═NH)NHRe;
• L is 1) a linear (C2-C4)alkyl chain when G is OH, ORe, NH2, NHRe, NReRf, NHC(═NH)NH2, or NHC(═NH)NHRe, or 2) a linear (C1-C3)alkyl chain when G is C(═NH)NH2 or C(═NH)NHRe;
• L is optionally substituted by 1-4 groups independently selected from R5, R5a, R6, and R6a;
• one or more of the carbon atoms of L may be part of a 3-, 4-, 5-, 6-, or 7-membered saturated ring composed of carbon atoms, and 0-2 hetero atoms selected from 0 or 1 nitrogen atoms, 0 or 1 oxygen atoms, and 0 or 1 sulfur atoms;
• said saturated ring being optionally substituted with up to four groups selected from halogen, (C1-C6)alkyl, halo(C3-C6)alkyl, (C3-C6)cycloalkyl, halo(C3-C6)cycloalkyl, (C4-C7)cycloalkylalkyl, halo(C4-C7)cycloalkylalkyl, and oxo, such that when there is substitution with one oxo group on a carbon atom it forms a carbonyl group and when there is substitution of one or two oxo groups on sulfur it forms sulfoxide or sulfone groups, respectively;
• R5, R5a, R6, and R6a is each independently selected from 1) H, (C1-C12)alkyl, halo(C1-C12)alkyl, hydroxy(C -C12)alkyl, (C3-C10)cycloalkyl, (C3-C10)cycloalkyl, (C3-C10)cycloalkylalkyl, halo(C3-C10)cycloalkylalkyl, hydroxy(C3-C10)cycloalkylalkyl, (C1-C2)alkyl (C3-C10)cycloalkylalkyl, halo(C1-C2)alkyl (C3-C10)cycloalkylalkyl, di (C1-C2)alkyl (C3-C10)cycloalkylalkyl, hydroxy(C1-C2)alkyl (C3-C10)cycloalkylalkyl, hydroxy di (C1-C2)alkyl (C3-C10)cycloalkylalkyl, (C2-C12)alkenyl, (C5-C8)cycloalkyl(C1-C3)alkenyl, (C2-C12)alkynyl, (C3-C8)cycloalkyl(C1-C3)alkynyl, (C4-C12)bicycloalkyl(C1-C3)alkyl, (C8-C14)tricycloalkyl(C1-C3)alkyl, (C1-C6)alkoxy(C1-C6)alkyl, halo(C1-C6)alkoxy(C1-C6)alkyl, (C3-C8)cycloalkoxy(C1-C3)alkyl, (C1-C6)alkylthio(C1-C6)alkyl, halo(C1-C6)alkylthio(C1-C6)alkyl, (C3-C8)cycloalkylthio(C1-C3)alkyl, saturated heterocyclyl, and saturated heterocyclyl(C1-C3)alkyl wherein (a) hydrogen atoms in these groups are optionally substituted by 1 to 6 groups independently selected from halogen, cyano, nitro, hydroxy, (C1-C6)alkyl, (C1-C6)alkoxy, (C3-C6)cycloalkyl, (C3-C7)cycloalkylalkyl, halo(C3-C7)cycloalkylalkyl, (C2-C6)alkenyl, halo(C2-C6)alkenyl, (C3-C7)cycloalkylalkenyl, (C2-C6)alkynyl, halo(C2-C6)alkynyl, (C3-C7)cycloalkylalkoxy, halo(C3-C7)cycloalkylalkoxy, (C3-C7)cycloalkoxy, halo(C1-C6)alkyl, (C3-C7)cycloalkylalkynyl, halo(C3-C7)cycloalkylalkynyl, halo(C1-C6)alkoxy, halo(C3-C7)cycloalkyl, halo(C3-C7)cycloalkoxy, (C1-C6)alkylsulfonyl, aminocarbonyl and wherein (b) divalent sulfur atoms are optionally oxidized to sulfoxide or sulfone;
• or 2) phenyl, naphthyl, heteroaryl, phenyl(C1-C3)alkyl, phenoxymethyl, naphthyl(C1-C3)alkyl, and heteroaryl(C1-C3)alkyl, each optionally substituted with 1 to 3 groups independently selected from:
• halogen, cyano, nitro, amino, hydroxy, carboxy, (C1-C6)alkyl, (C3-C6)cycloalkyl, (C4-C7)cycloalkylalkyl, (C2-C6)alkenyl, halo(C2-C6)alkenyl, (C3-C6)cycloalkylalkenyl, (C2-C6)alkynyl, halo(C2-C6)alkynyl, (C3-C6)cycloalkyl-(C2-C4)alkynyl, halo(C3-C7)cycloalkylalkynyl, halo(C1-C6)alkyl, halo(C3-C6)cycloalkyl, halo(C4-C7)cycloalkylalkyl, (C1-C6)alkoxy, (C3-C6)cycloalkoxy, (C4-C7)cycloalkylalkoxy, halo(C1-C6)alkoxy, halo(C3-C6)cyeloalkoxy, halo(C4-C7)cycloalkylalkoxy, (C1-C6)alkylthio, (C3-C6)cycloalkythio, (C4-C7)cycloalkylalkylthio, halo(C1-C6)alkylthio, halo(C3-C6)cycloalkythio, halo(C4-C7)cycloalkylalkylthio, (C1-C6)alkanesulfinyl, (C3-C6)cycloalkanesulfinyl, (C4-C7)cycloalkylalkanesulfinyl, halo(C1-C6)alkanesulfinyl, halo(C3-C6)cycloalkanesulfinyl, halo(C4-C7)cycloalkylalkanesulfinyl, (C1-C6)alkanesulfonyl, (C3-C6)cycloalkanesulfonyl, (C4-C7)cycloalkylalkanesulfonyl, halo(C1-C6)alkanesulfonyl, halo(C3-C6)cycloalkanesulfonyl, halo(C4-C7)-cycloalkylalkanesulfonyl, (C1-C6)alkylamino, di(C1-C6)alkylamino, (C1-C6)-alkoxy(C1-C6)alkoxy, halo(C1-C6)alkoxy(C1-C6)alkoxy, (C1-C6)alkoxycarbonyl, aminocarbonyl, (C1-C6)alkylaminocarbonyl, di(C1-C6)alkylaminocarbonyl, cyano(C1-C6)alkyl, hydroxy(C1-C6)alkyl, carboxy(C1-C6)alkyl, (C1-C6)alkoxy(C1-C6)alkyl, (C3-C8)cycloalkoxy(C1-C6)alkyl, (C4-C8)cycloalkylalkoxy(C1-C6)alkyl, halo(C1-C6)alkoxy(C1-C6)alkyl, halo(C3-C6)cycloalkoxy(C1-C6)alkyl, halo(C4-C8)-cycloalkylalkoxy(C1-C6)alkyl, (C1-C8)alkylthio(C1-C6)alkyl, (C3-C8)cycloalkythio(C1-C6)alkyl, (C4-C8)cycloalkylalkylthio(C1-C6)alkyl, halo(C1-C8)alkylthio(C1-C6)alkyl, halo(C3-C8)cycloalkythio(C1-C6)alkyl, halo(C4-C8)-cycloalkylalkylthio(C1-C6)alkyl, (C1-C8)alkanesulfinyl(C1-C6)alkyl, (C3-C8)-cycloalkanesulfinyl(C1-C6)alkyl, (C4-C8)cycloalkyl-alkanesulfinyl(C1-C6)alkyl, halo(C1-C8)alkanesulfinyl(C1-C6)alkyl, halo(C3-C8)cycloalkanesulfinyl(C1-C6)alkyl, halo(C4-C8)cycloalkylalkanesulfinyl(C1-C6)alkyl, (C1-C8)alkane-sulfonyl(C1-C6)alkyl, (C3-C8)cycloalkanesulfonyl(C1-C6)alkyl, (C4-C8) cycloalkylalkanesulfonyl(C1-C6)alkyl, halo(C1-C8)alkanesulfonyl(C1-C6)alkyl, halo(C3-C8)cycloalkanesulfonyl(C1-C6)alkyl, halo(C4-C8)cycloalkylalkane-sulfonyl(C1-C6)alkyl, (C1-C8)alkylamino(C1-C6)alkyl, di(C1-C8)alkylamino(C1-C6)alkyl, (C1-C8)alkoxycarbonyl(C1-C6)alkyl, (C1-C8)acyloxy(C1-C6)alkyl, aminocarbonyl(C1-C6)alkyl, (C1-C8)alkylamino-carbonyl(C1-C6)alkyl, di(C1-C8)alkylaminocarbonyl(C1-C6)alkyl and (C1-C8)acylamino(C1-C6)alkyl, (C1-C8)alkoxycarbonylamino, (C1-C8)alkoxycarbonylamino(C1-C6)alkyl, aminocarboxy(C1-C6)alkyl, (C1-C8)alkylamino-carboxy(C1-C6)alkyl and di(C1-C8)alkylaminocarboxy(C1-C6)alkyl, phenyl, naphthyl, heteroaryl, bicyclic heteroaryl, phenoxy, naphthyloxy, heteroaryloxy, bicyclic heteroaryloxy, phenylthio, naphthylthio, heteroarylthio, bicyclic heteroarylthio, phenylsulfinyl, naphthylsulfinyl, heteroarylsulfinyl, bicyclic heteroarylsulfinyl, phenylsulfonyl, naphthylsulfonyl, heteroarylsulfonyl, bicyclic heteroarylsulfonyl, phenyl(C1-C3)alkyl, naphthyl(C1-C3)alkyl, heteroaryl(C1-C3)alkyl, and bicyclic heteroaryl(C1-C3)alkyl, wherein the aromatic and heteroaromatic groups are optionally substituted with 1 to 3 groups independently selected from fluorine, chlorine, cyano, (C1-C3)alkyl, halo(C1-C3)alkyl, (C1-C3)alkoxy, halo(C1-C3)-alkoxy, (C1-C3)alkanesulfonyl, and (C1-C3)alkoxycarbonyl;
• Re is a) (C1-C12)alkyl, (C4-C12)cycloalkylalkyl, halo(C1-C12)alkyl, halo(C4-C12)cycloalkylalkyl, (C2-C12)alkenyl, (C5-C12)cycloalkylalkenyl, halo(C2-C12)alkenyl, halo(C5-C12)cycloalkylalkenyl, (C2-C12)alkynyl, (C5-C12)cycloalkylalkynyl, halo(C2-C12)alkynyl, halo(C5-C12)cycloalkylalkynyl, (C1-C6)alkoxy(C1-C6)alkyl, halo(C1-C6)alkoxy(C1-C6)alkyl, (C1-C6)alkylthio(C1-C6)alkyl, halo(C1-C6)alkylthio(C1-C6)alkyl, (C1-C6)alkanesulfinyl(C1-C6)alkyl, halo(C1-C6)alkane-sulfinyl(C1-C6)alkyl, (C1-C6)alkanesulfonyl(C1-C6)alkyl, halo(C1-C6)alkanesulfonyl(C1-C6)alkyl, aminocarbonyl(C1-C6)alkyl, (C1-C6)alkylaminocarbonyl(C1-C6)alkyl, di(C1-C6)alkylamino-carbonyl(C1-C6)alkyl, cyano(C1-C6)alkyl, carboxy(C1-C6)alkyl, (C1-C6)alkoxycarbonyl(C1-C6)alkyl, saturated heterocyclyl, or saturated heterocyclyl(C1-C6)alkyl or b) phenyl, naphthyl, heteroaryl, phenyl(C1-C3)alkyl, naphthyl(C1-C3)alkyl, or heteroaryl(C1-C3)alkyl, each of a) and b) are optionally substituted by 1 to 3 groups independently selected from:
• 1) fluorine, chlorine, bromine, iodine, cyano, nitro, amino, hydroxy, carboxy, (C1-C6)alkyl, (C3-C6)cycloalkyl, (C4-C7)cycloalkylalkyl, (C2-C6)alkynyl, (C3-C6)cycloalkyl-(C2-C4)alkynyl, halo(C1-C6)alkyl, halo(C3-C6)cycloalkyl, halo(C4-C7)cycloalkylalkyl, (C1-C6)alkoxy, (C3-C6)cycloalkoxy, (C4-C7)cycloalkylalkoxy, halo(C1-C6)alkoxy, halo(C3-C6)cycloalkoxy, halo(C4-C7)cycloalkylalkoxy, (C1-C6)alkylthio, (C3-C6)cycloalkythio, (C4-C7)cycloalkylalkylthio, halo(C1-C6)alkylthio, halo(C3-C6)cycloalkythio, halo(C4-C7)cycloalkylalkylthio, (C1-C6)alkanesulfinyl, (C3-C6)cycloalkanesulfinyl, (C4-C7)cycloalkylalkanesulfinyl, halo(C1-C6)alkanesulfinyl, halo(C3-C6)cycloalkanesulfinyl, halo(C4-C7)cycloalkylalkanesulfinyl, (C1-C6)alkanesulfonyl, (C3-C6)cycloalkanesulfonyl, (C4-C7)cycloalkylalkanesulfonyl, halo(C1-C6)alkanesulfonyl, halo(C3-C6)cycloalkanesulfonyl, halo(C4-C7)-cycloalkylalkanesulfonyl, (C1-C6)alkylamino, di(C1-C6)alkylamino, (C1-C6)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkoxy(C1-C6)alkoxy, (C1-C6)alkoxycarbonyl, aminocarbonyl, (C1-C6)alkylaminocarbonyl, di(C1-C6)alkylaminocarbonyl, cyano(C1-C6)alkyl, hydroxy(C1-C6)alkyl, carboxy(C1-C6)alkyl, (C1-C6)alkoxy(C1-C6)alkyl, (C3-C8)cycloalkoxy(C1-C6)alkyl, (C4-C8)cycloalkylalkoxy(C1-C6)alkyl, halo(C1-C6)alkoxy(C1-C6)alkyl, halo(C3-C6)cycloalkoxy(C1-C6)alkyl, halo(C4-C8)-cycloalkylalkoxy(C1-C6)alkyl, (C1-C8)alkylthio(C1-C6)alkyl, (C3-C8)cycloalkythio(C1-C6)alkyl, (C4-C8)cycloalkylalkylthio(C1-C6)alkyl, halo(C1-C8)alkylthio(C1-C6)alkyl, halo(C3-C8)cycloalkythio(C1-C6)alkyl, halo(C4-C8)-cycloalkylalkylthio(C1-C6)alkyl, (C1-C8)alkanesulfinyl(C1-C6)alkyl, (C3-C8)-cycloalkanesulfinyl(C1-C6)alkyl, (C4-C8)cycloalkyl-alkanesulfinyl(C1-C6)alkyl halo(C1-C8)alkanesulfinyl(C1-C6)alkyl, halo(C3-C8)cycloalkanesulfinyl(C1-C6)alkyl, halo(C4-C8)cycloalkylalkanesulfinyl(C1-C6)alkyl, (C1-C8)alkane-sulfonyl(C1-C6)alkyl, (C3-Cg)cycloalkanesulfonyl(C1-C6)alkyl, (C4-C8) cycloalkylalkanesulfonyl(C1-C6)alkyl, halo(C1-C8)alkanesulfonyl(C1-C6)alkyl, halo(C3-C8)cycloalkanesulfonyl(C1-C6)alkyl, halo(C4-C8)cycloalkylalkane-sulfonyl (C1-C6)alkyl, (C1-C8)alkylamino(C1-C6)alkyl, di(C1-C8)alkylamino(C1-C6)alkyl, (C1-C8)alkoxycarbonyl(C1-C6)alkyl, (C1-C8)acyloxy(C1-C6)alkyl, aminocarbonyl (C1-C6)alkyl, (C1-C8)alkylamino-carbonyl(C1-C6)alkyl, di(C1-C8)alkylaminocarbonyl(C1-C6)alkyl (C1-C8)acylamino(C1-C6)alkyl, (C1-C8)alkoxycarbonylamino, (C1-C8)alkoxycarbonylamino(C1-C6)alkyl, aminocarboxy(C1-C6)alkyl, (C1-C8)alkylamino-carboxy(C1-C6)alkyl and di(C1-C8)alkylaminocarboxy(C1-C6)alkyl;
• or 2) phenyl, naphthyl, heteroaryl, bicyclic heteroaryl, phenoxy, naphthyloxy, heteroaryloxy, bicyclic heteroaryloxy, phenylthio, naphthylthio, heteroarylthio, bicyclic heteroarylthio, phenylsulfinyl, naphthylsulfinyl, heteroarylsulfinyl, bicyclic heteroarylsulfinyl, phenyl sulfonyl, naphthylsulfonyl, heteroarylsulfonyl, bicyclic heteroarylsulfonyl, phenyl (C1-C3)alkyl, naphthyl(C1-C3)alkyl, heteroaryl(C1-C3)alkyl, and bicyclic heteroaryl(C1-C3)alkyl, each optionally substituted with 1 to 3 groups independently selected from fluorine, chlorine, cyano, (C1-C3)alkyl, halo(C1-C3)alkyl, (C1-C3)alkoxy, halo(C1-C3)alkoxy, (C1-C3)alkanesulfonyl, and (C1-C3)-alkoxycarbonyl;
• or
• b) Re is a saturated divalent radical composed of carbon atoms, and 0, 1 or 2 hetero atoms selected from 0 or 1 nitrogen atoms, 0 or 1 oxygen atoms, and 0 or 1 sulfur atoms that is attached to any core carbon atom on L to form a saturated 3-, 4-, 5-, 6-, or 7-membered L-G ring;
• said L-G ring being optionally substituted with 1 to 4 groups selected from halogen, fluorine, (C1-C8)alkyl, halo(C1-C8)alkyl, (C3-C8)cycloalkyl, halo(C3-C8)cycloalkyl, hydroxy(C3-C8)cycloalkyl, (C3-C8)cycloalkyl(C1-C3)alkyl, halo(C3-C8)cycloalkyl(C1-C3)alkyl, hydroxy (C3-C8)cycloalkyl(C1-C3)alkyl, (C1-C8)alkoxy, halo(C1-C8)alkoxy, (C3-C8)cycloalkoxy, halo(C3-C8)cycloalkoxy, hydroxy(C3-C8)cycloalkoxy, (C1-C8)alkoxy(C1-C3)alkyl, halo(C1-C8)alkoxy(C1-C3)alkyl, (C3-C8)cycloalkoxy(C1-C3)alkyl, halo(C3-C8)cycloalkoxy(C1-C3)alkyl, hydroxy(C3-C8)cycloalkoxy(C1-C3)alkyl, (C3-C8)cycloalkyl(C1-C3)alkoxy(C1-C3)alkyl, halo(C3-C8)cycloalkyl(C1-C3)alkoxy(C1-C3)alkyl, hydroxy(C3-C8)cycloalkyl(C1-C3)alkoxy(C1-C3)alkyl, (C1-C8)alkylthio, halo(C1-C8)alkylthio, (C3-C8)cycloalkylthio, halo(C3-C8)cycloalkylthio, hydroxy(C3-C8)cycloalkylthio, (C3-C8)cycloalkyl(C1-C3)alkylthio, halo(C3-C8)cycloalkyl(C1-C3)alkylthio, hydroxy(C3-C8)cycloalkyl(C1-C3)alkylthio, (C1-C8)alkylthio(C1-C3)alkyl, halo(C1-C8)alkylthio(C1-C3)alkyl, (C3-C8)cycloalkylthio(C1-C3)alkyl, halo(C3-C8)cycloalkylthio(C1-C3)alkyl, hydroxy(C3-C8)cycloalkylthio(C1-C3)alkyl, (C3-C8)cycloalkyl(C1-C3)alkylthio(C1-C3)alkyl, halo(C3-C8)cycloalkyl (C1-C3)alkylthio(C1-C3)alkyl, hydroxy(C3-C8)cycloalkyl(C1-C3)alkylthio(C1-C3)alkyl, heterocyclyl, and oxo;
• Rf is (C1-C6)alkyl or halo(C1-C6)alkyl;
• or an enantiomer, diastereomer, or a pharmaceutically acceptable salt thereof;
• provided that
• A is not 2,4-morpholine or 1,3-piperidine
• R2 is —NHC(═NR12)(NH2), —NHC(═NR12)(NHR9),
• —OC(O)(NH2), —OC(S)(NH2), —SC(S)(NH2), —SC(O)(NH2), —OC(O)(NHR9), —OC(S)(NHR9), —SC(S)(NHR9), —SC(O)(NHR9), —NHC(O)OR9, —NHC(S)SR9, —NHC(S)OR9, —NHC(O)SR9, —C(O)R9, —C(S)R9, —C(O)(NH2), —C(S)(NH2), —C(O)(NHR9), —C(S)(NHR9) or —NHC(O)H, wherein R9 is a straight or branched C1-C5 alkyl, straight or branched C1-C5haloalkyl, (C3-C4)cycloalkyl or straight or branched C1-C5 alkoxyalkyl and R12 is H, (C1-C6)alkyl, phenyl, heteroaryl, cyano, nitro, —S(O)R9, —S(O2)R9, —S(O2)NHR9, —S(O2)NR9R9, —C(O)R9, —C(S)R9, —C(O)OR9, —C(S)OR9, —C(O)(NH2), —C(O)(NHR9).