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09/11/08 - USPTO Class 514 | 216 views | #20080221128 | Prev - Next | About this Page

Metalloprotease inhibitors containing a squaramide moiety

Title: Metalloprotease inhibitors containing a squaramide moiety

Brief Patent Description - Full Patent Description - Patent Claims

The Patent Description & Claims data below is from USPTO Patent Application 20080221128, Metalloprotease inhibitors containing a squaramide moiety.

1. A compound having Formula (I): wherein: R3 is R10; or R3 and R12 when taken together with the fragment N-Le and the two adjacent atoms of Q1 to which they are attached complete a 5- to 8-membered saturated or partially unsaturated heterocycle optionally containing additional heteroatoms selected from O, S(O)x, N or NR50 and which is optionally substituted one or more times; R4 in each occurrence is independently selected from R10, hydrogen, alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, halo, haloalkyl, CF3, (C0-C6)-alkyl-COR10, (C0-C6)-alkyl-OR10, (C0-C6)-alkyl-NR10R11, (C0-C6)-alkyl-NO2, (C0-C6)-alkyl-CN, (C0-C6)-alkyl-S(O)yOR10, (C0-C6)-alkyl-S(O)yNR10R11, (C0-C6)-alkyl-NR10CONR11SO2R30, (C0-C6)-alkyl-S(O)xR10, (C0-C6)-alkyl-OC(O)R10, (C0-C6)-alkyl-OC(O)NR10R11, (C0-C6)-alkyl-C(═NR10)NR10R11, (C0-C6)-alkyl-NR10C(═NR11)NR10R11, (C0-C6)-alkyl-C(O)OR10, (C0-C6)-alkyl-C(O)NR10R11, (C0-C6)-alkyl-C(O)NR10SO2R11, (C0-C6)-alkyl-C(O)—NR11—CN, O—(C0-C6)-alkyl-C(O)NR10R11, S(O), —(C0-C6)-alkyl-C(O)OR10, S(O), —(C0-C6)-alkyl-C(O)NR10R11, (C0-C6)-alkyl-C(O)NR10—(C0-C6)-alkyl-NR10R11, (C0-C6)-alkyl-NR10—C(O)R10, (C0-C6)-alkyl-NR10—C(O)OR10, (C0-C6)-alkyl-NR10—C(O)—NR10R11, (C0-C6)-alkyl-NR10—S(O)yNR10R11, (C0-C6)-alkyl-NR10—S(O)yR10, O—(C0-C6)-alkyl-aryl and O—(C0-C6)-alkyl-heteroaryl, wherein each R4 group is optionally substituted one or more times, or wherein each R4 group is optionally substituted by one or more R14 groups; R9 in each occurrence is independently selected from R10, hydrogen, alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, halo, CHF2, CF3, OR10, SR10, COOR10, CH(CH3)CO2H, (C0-C6)-alkyl-COR10, (C0-C6)-alkyl-OR10, (C0-C6)-alkyl-NR10R11, (C0-C6)-alkyl-NO2, (C0-C6)-alkyl-CN, (C0-C6)-alkyl-S(O)yOR10, (C0-C6)-alkyl-P(O)2OH, (C0-C6)-alkyl-S(O)yNR10R11, (C0-C6)-alkyl-NR10CONR11SO2R30, (C0-C6)-alkyl-S(O)xR11, (C0-C6)-alkyl-OC(O)R10, (C0-C6)-alkyl-OC(O)NR10R11, (C0-C6)-alkyl-C(═NR10)NR10R11, (C0-C6)-alkyl-NR10C(═NR11)NR10R11, (C0-C6)-alkyl-NR10C(═N—CN)NR10R11, (C0-C6)-alkyl-C(═N—CN)NR11R11, (C0-C6)-alkyl-NR10C(═N—NO2)NR10R11, (C0-C6)-alkyl-C(═N—NO2)NR10R11, (C0-C6)-alkyl-C(O)OR10, (C0-C6)-alkyl-C(O)NR10R11, (C0-C6)-alkyl-C(O)NR10SO2R11, C(O)NR10—(C0-C6)-alkyl-heteroaryl, C(O)NR10—(C0-C6)-alkyl-aryl, S(O)2NR10—(C0-C6)-alkyl-aryl, S(O)2NR10—(C0-C6)-alkyl-heteroaryl, S(O)2NR10-alkyl, S(O)2—(C0-C6)-alkyl-aryl, S(O)2—(C0-C6)-alkyl-heteroaryl, (C0-C6)-alkyl-C(O)—NR11—CN, O—(C0-C6)-alkyl-C(O)NR10R11, S(O), —(C0-C6)-alkyl-C(O)OR10, S(O), —(C0-C6)-alkyl-C(O)NR10R11, (C0-C6)-alkyl-C(O)NR10—(C0-C6)-alkyl-NR10R11, (C0-C6)-alkyl-NR10—C(O)R10, (C0-C6)-alkyl-NR10—C(O)OR10, (C0-C6)-alkyl-NR10—C(O)—NR10R11, (C0-C6)-alkyl-NR10—S(O)yNR10R11, (C0-C6)-alkyl-NR10—S(O)yR11, O—(C0-C6)-alkyl-aryl and O—(C0-C6)-alkyl-heteroaryl, wherein each R9 group is optionally one or more times substituted; R10 and R11 in each occurrence are independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, fluoroalkyl, heterocycloalkylalkyl, haloalkyl, alkenyl, alkynyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl and aminoalkyl, wherein alkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, fluoroalkyl, heterocycloalkylalkyl, alkenyl, alkynyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl and aminoalkyl are optionally substituted one or more times, or R10 and R11 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S(O)x, or NR50 and which is optionally substituted one or more times; R12 is selected from R9 or optionally R12 and R3 when taken together with the fragment N-Lc and the two adjacent atoms of Q1 to which they are attached complete a 5- to 8-membered saturated or partially unsaturated heterocycle optionally containing additional heteroatoms selected from O, S(O)x, N or NR50 and which is optionally substituted one or more times; R14 is independently selected from hydrogen, alkyl, arylalkyl, cycloalkylalkyl, heteroarylalkyl, heterocyclylalkyl and halo, wherein alkyl, arylalkyl, cycloalkylalkyl, heteroarylalkyl and heterocyclylalkyl are optionally substituted one or more times; R17 is selected from R9, alkenyl, alkynyl, bicycloalkyl, heterobicycloalkyl, spiroalkyl, spiroheteroalkyl, cycloalkyl fused aryl, heterocycloalkyl fused aryl, cycloalkyl fused heteroaryl, heterocycloalkyl fused heteroaryl or a bicyclic or tricyclic fused ring system, wherein at least one ring is partially saturated, and wherein each R17 group is optionally substituted one or more times, or wherein each R17 group is optionally substituted one or more R9 groups; R30 is selected from alkyl and (C0-C6)-alkyl-aryl, wherein alkyl and aryl are optionally substituted; R50 in each occurrence is independently selected from hydrogen, alkyl, aryl, heteroaryl, C(O)R80, C(O)NR80R81, SO2R80 and SO2NR80R81, wherein alkyl, aryl, and heteroaryl are optionally substituted one or more times; R80 and R81 in each occurrence are independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, fluoroalkyl, heterocycloalkylalkyl, haloalkyl, alkenyl, alkynyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl and aminoalkyl, wherein alkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, fluoroalkyl, heterocycloalkylalkyl, alkenyl, alkynyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl and aminoalkyl are optionally substituted, or R80 and R81 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally a heteroatom selected from O, S(O)x, NH, and N(alkyl) and which is optionally substituted one or more times; Lc is selected from a single bond or an acyclic, straight or branched, saturated or unsaturated hydrocarbon chain having 1 to 10 carbon atoms, optionally containing 1 to 3 groups independently selected from —S—, —O—, NR10—, —NR10CO—, —CONR10—, —S(O)x—, —SO2NR10—, —NR10SO2—, NR10SO2NR10—, —NR10CONR10—, —OC(O)NR10—, —NR10C(O)O—, which replace single carbon atoms, which in case that more than two carbon atoms are replaced are not adjacent, and wherein the hydrocarbon chain is optionally substituted one or more times; Ld is selected from a single bond or a straight or branched, saturated or unsaturated hydrocarbon chain having 1 to 10 carbon atoms, optionally containing 1 to 3 groups independently selected from —O—, —NR10—, —S(O)x—, —NR10C(X1)—, —C(X1)NR10—, —SO2NR10—, —NR10SO2—, —O—SO2—, —SO2—O—, —NR10SO2NR10—, —NR10C(X1)NR10—, —OC(X1)NR10—, —NR10C(X1)O—, —OC(X1)—, —C(X1)O—, -Q2-, —NR10-Q2-, -Q2-NR10—, —C(X1)-Q2-, -Q2-C(X1)—, —O-Q2-S(O)x-Q2-, -Q2-S(O)x— which replace single carbon atoms, which in case that more than two carbon atoms are replaced are not adjacent, and wherein the hydrocarbon chain is optionally substituted one or more times; Le is selected from a single bond or a (C1-C3)-alkyl chain, which is optionally substituted one or more times; Q1 is a 4- to 8-membered ring selected from cycloalkyl, heterocycloalkyl, bicycloalkyl, heterobicycloalkyl or a 5- or 6-membered ring selected from aryl and heteroaryl, wherein cycloalkyl, heterocycloalkyl, bicycloalkyl, heterobicycloalkyl, aryl and heteroaryl are optionally substituted one or more times by R4 and optionally a substituent of Q1 is linked with Ld to complete a 3- to 8-membered ring containing carbon atoms and optionally heteroatoms selected from O, S(O)x, —NH, and —N(alkyl) wherein this new ring is optionally substituted one or more times; Q2 is independently selected from an aromatic, partially aromatic or non-aromatic cyclic, bicyclic or multicyclic system containing 0 to 8 heteroatoms selected from N, O and S(O)x, which is optionally substituted one or more times with R4 and wherein the cycles are optionally spiro fused and optionally a substituent of Q2 is linked with Ld to complete a 3- to 8-membered ring containing carbon atoms and optionally heteroatoms selected from O, S(O)x, —NH, and —N(alkyl) wherein this new ring is optionally substituted one or more times; X1 is independently selected from O, S, NR10, NOR10, N—CN, NCOR10, N—NO2, and N—SO2R10; x is independently selected from 0 to 2; y is selected from 1 and 2; and N-oxides, pharmaceutically acceptable salts, prodrugs, formulations, polymorphs, racemic mixtures and stereoisomers thereof.

2. The compound of claim 1, wherein the group Q2-Lc-R17 is selected from: wherein: R5 in each occurrence is independently selected from hydrogen, alkyl, C(O)NR10R11, aryl, arylalkyl, SO2NR10R11 and C(O)OR10, wherein alkyl, aryl and arylalkyl are optionally substituted one or more times; E is independently selected from a bond, CR10R11, O, NR5, S, S═O, S(═O)2, C(═O), N(R10)(C═O), (C═O)N(R10), N(R10)S(═O)2, S(═O)2N(R10), C═N—OR11, —C(R10R11)C(R10R11)—, —CH2—W1— and Q3 is selected from an aromatic, partially aromatic or non-aromatic cyclic, bicyclic or multicyclic system containing 0 to 8 heteroatoms selected from N, O and S(O)x, which is optionally substituted one or more times with R4; Q4 is selected from an aromatic, partially aromatic or non-aromatic cyclic, bicyclic or multicyclic system containing 0 to 8 heteroatoms selected from N, O and S(O)x, which is optionally substituted one or more times with R4; U is independently selected from C(R5R10), NR5, O, S, S═O and S(═O)2; W1 is independently selected from O, NR5, S, S═O, S(═O)2, N(R10)(C═O), N(R10)S(═O)2 and S(═O)2N(R10); and g and h are independently selected from 0-2.

3. The compound of claim 2, wherein Q4 is selected from an aromatic, partially aromatic or non-aromatic bicyclic or multicyclic system containing 0 to 8 heteroatoms selected from N, O and S(O)x, which is optionally substituted one or more times with R4.

4. The compound of claim 3 selected from wherein L, M and T are independently selected from CR9 and N.

5. The compound of claim 4 selected from

6. A pharmaceutical composition comprising an effective amount of a compound according to claim 1; and a pharmaceutically-acceptable carrier.

7. A method of treating rheumatoid arthritis, osteoarthritis or inflammation comprising administering a therapeutically-effective amount of a compound according to claim 1.

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