1460761834-78896878-6c3d-4480-9a96-8ce6a649918c

1. A pharmaceutical composition comprising a compound of the Formula:
or a salt thereof; wherein:
(a) R is 2-butyl or isopropyl;
(b) each of R1 and R2 is independently methyl;
(c) R3 is \u2014CH2CH2CH2CH2R9;
(d) R4 is methoxy;
(e) R5 is carboxyamino;
(f) R6 is hydrido or methyl;
(g) each of R7 and R9 is independently amino, monosubstituted amino, disubstituted amino, acylamino, ureido, guanidino, carbamoyl, sulfonamino, thioacylamino, thioureido, iminoamino, or phosphonamino;
(h) provided that R7 is other than
wherein each of R11 and R12 is hydrido, C6-C18 unsubstituted alkanoyl, C8-C18 unsubstituted alkenoyl, C8-C18 unsubstituted alkyl, or C8-C18 select substituted alkyl; or alternatively, R11 and R12 together are C8-C18 alkylidenyl.
2. The composition of claim 1 wherein R7 is
wherein each of Raa, Raa2 and Raa3 is independently an amino acid side chain and wherein R13 is amino, monosubstituted amino, disubstituted amino, acylamino, ureido, guanidino, carbamoyl, sulfonamino, thioacylamino, thioureido, iminoamino, or phosphonamino.
3. A composition comprising a compound of the Formula
or a salt thereof; wherein:
(a) R is 2-butyl, isopropyl or 2-(2\u2032-aminophenacyl);
(b) each of R1 and R6 is independently hydrido or methyl;
(c) R4 is hydrido or methoxy;
(d) R5 hydroxyl or carboxyamino;
(e) R15 is hydrido,
wherein: R18 is amino or hydroxyl; R19 is hydrido or hydroxyl; and R20 is carboxyamino or carboxymethyl;

(f) R16 is methyl or \u2014CH2CH2CH2R21;
(g) R17 is methyl or \u2014CH2CH2CH2CH2R22;
wherein each of R21 and R22 is independently amino, monosubstituted amino, disubstituted amino, acylamino, ureido, guanidino, carbamoyl, sulfonamino, thioacylamino, thioureido, iminoamino, or phosphonamino.
4. The composition of claim 3 wherein each of R21 and R22 is independently \u2014NHR23, wherein R23 is an amino protecting group.
5. The composition of claim 4 wherein the compound of Formula I is
wherein each of R6 and R14 is independently hydrido or methyl.
6. A method of treating a bacterial infection in a subject, comprising administering to the subject a therapeutically-effective amount of a composition comprising a compound of the Formula:
or a salt thereof; wherein:
(a) R is 2-butyl, isopropyl or 2-(2\u2032-aminophenacyl);
(b) each of R1 and R6 is independently hydrido or methyl;
(c) R2 is methyl or \u2014CH2CH2CH2R8;
(d) R3 is methyl or \u2014CH2CH2CH2CH2R9;
(e) R4 is hydrido or methoxy;
(f) R5 is hydroxyl or carboxyamino;
(g) each of R7, R8 and R9 is independently amino, monosubstituted amino, disubstituted amino, acylamino, ureido, guanidino, carbamoyl, sulfonamino, thioacylamino, thioureido, iminoamino, or phosphonamino;
(h) provided that
(1) when R2 is \u2014CH2CH2CH2R8, R7 is other than
wherein R10 is amino, monosubstituted amino, disubstituted amino, acylamino, ureido, guanidino, carbamoyl, sulfonamino, thioacylamino, iminoamino, or phosphonamino;

(2) when R2 is methyl, R7 is other than
wherein each of R11 and R12 is hydrido, C6-C18 unsubstituted alkanoyl, C8-C18 unsubstituted alkenoyl, C8-C18 unsubstituted alkyl, or C8-C18 select substituted alkyl; or alternatively, R11 and R12 together are C8-C18 alkylidenyl;
comprising removing an amino protecting group from a compound of Formula XVII,
or a salt thereof,
wherein R28 is methyl or \u2014CH2CH2CH2NHP; R29 is methyl or \u2014CH2CH2CH2CH2NHP; and P is an amino protecting group; provided that at least one of R28 or R29 is other than methyl.
8. The process of claim 7 further comprising treating a compound of the Formula XVI,
or a salt thereof,
with a modifying agent to obtain the compound of Formula XVII, or a salt thereof.
9. The process of claim 8 further comprising removing the terminal amino acid residue from a compound of Formula XV,
or a salt thereof,
wherein R18 is amino or hydroxy; R19 is hydrido or hydroxy;
to obtain the compound of Formula XVI, or a salt thereof.
10. The process of claim 9 further comprising removing the terminal amino acid residue from a compound of Formula XIV
or a salt thereof,
wherein R20 is carboxyamino or carboxymethyl;
to obtain the compound of Formula XV, or a salt thereof.
11. The process of claim 10 further comprising removing the tryptophan amino acid residue from a compound of Formula XIII
or a salt thereof,
to obtain the compound of Formula XIV, or a salt thereof.
12. The process of claim 11 further comprising deacylating a compound of Formula XII
or a salt thereof;
wherein R25 is an alkyl group;
to obtain the compound of Formula XIII, or a salt thereof.
13. The process of claim 12 further comprising protecting the free amine group(s) of a compound of Formula XI
or a salt thereof;
wherein R26 methyl or \u2014CH2CH2CH2NH2; and R27 is methyl or \u2014CH2CH2CH2CH2NH2;
to obtain the compound of Formula XII, or a salt thereof.
14. A process for preparing a compound of Formula I:
or a salt thereof; wherein:
(a) R is 2-butyl, isopropyl or 2-(2\u2032-aminophenacyl);
(b) each of R1 and R6 is independently hydrido or methyl;
(c) R2 is methyl or \u2014CH2CH2CH2R8;
(d) R3 is methyl or \u2014CH2CH2CH2CH2R9;
(e) R4 is hydrido or methoxy;
(f) R5 is hydroxyl or carboxyamino;
(g) each of R7, R8 and R9 is independently amino, monosubstituted amino, disubstituted amino, acylamino, ureido, guanidino, carbamoyl, sulfonamino, thioacylamino, thioureido, iminoamino, or phosphonamino;
(h) provided that
(1) when R2 is \u2014CH2CH2CH2R8, R7 is other than
wherein R10 is amino, monosubstituted amino, disubstituted amino, acylamino, ureido, guanidino, carbamoyl, sulfonamino, thioacylamino, iminoamino, or phosphonamino;

wherein R2a is methyl or \u2014CH2CH2CH2NH2; and R3a is methyl or \u2014CH2CH2CH2CH2NH2; provided at least one of R2a and R3a is other than methyl; with a modifying agent.
15. A process for preparing a compound of Formula I:
or a salt thereof; wherein:
(a) R is 2-butyl, isopropyl or 2-(2\u2032-aminophenacyl);
(b) each of R1 and R6 is independently hydrido or methyl;
(c) R2 is methyl or \u2014CH2CH2CH2R8;
(d) R3 is methyl or \u2014CH2CH2CH2CH2R9;
(e) R4 is hydrido or methoxy;
(f) R5 is hydroxyl or carboxyamino;
(g) each of R7, R8 and R9 is independently amino, monosubstituted amino, disubstituted amino, acylamino, ureido, guanidino, carbamoyl, sulfonamino, thioacylamino, thioureido, iminoamino, or phosphonamino;
(h) provided that
(1) when R2 is \u2014CH2CH2CH2R8, R7 is other than
wherein R10 is amino, monosubstituted amino, disubstituted amino, acylamino, ureido, guanidino, carbamoyl, sulfonamino, thioacylamino, iminoamino, or phosphonamino;

(2) when R2 is methyl, R7 is other than
wherein each of R11 and R12 is hydrido, C6-C18 unsubstituted alkanoyl, C8-C18 unsubstituted alkenoyl, C8-C18 unsubstituted alkyl, or C8-C18 select substituted alkyl; or alternatively, R11 and R12 together are C8-C18 alkylidenyl;
comprising treating a compound of Formula XXVIII
or a salt thereof;
wherein R37 is methyl or \u2014CH2CH2CH2R8; and R38 is methyl or \u2014CH2CH2CH2CH2R9; provided that at least one of R37 and R38 is other than methyl and further provided that each of R8 and R9 is other than amino;
with a modifying agent.
16. The process of claim 15 further comprising removing the terminal amino acid residue from a compound of Formula XXVII
or a salt thereof;
wherein R18 is amino or hydroxyl; and R19 is hydrido or hydroxyl;
to obtain the compound of Formula XXVIII, or a salt thereof.
17. The process of claim 16 further comprising removing the terminal amino acid residue from a compound of Formula XXVI
or a salt thereof;
wherein R20 is carboxyamino or carboxymethyl;
to obtain the compound of Formula XXVII, or a salt thereof.
18. The process of claim 17 further comprising removing the tryptophan amino acid residue from a compound of Formula XXV
or a salt thereof,
to obtain the compound of Formula XXVI, or a salt thereof.
19. The process of claim 18 further comprising deacylating a compound of Formula XXIV
or a salt thereof;
wherein R25 is an alkyl group;
to obtain the compound of Formula XXV, or a salt thereof.
20. The process of claim 19 further comprising treating the free amine group(s) of a compound of Formula XI,
or a salt thereof;
wherein R26 methyl or \u2014CH2CH2CH2NH2; and R27 is methyl or \u2014CH2CH2CH2CH2NR2;
with a modifying agent to obtain the compound of Formula XXV, or a salt thereof.
21. A process for preparing a compound of the Formula XXXII
or a salt thereof; wherein:
(a) R is 2-butyl, isopropyl or 2-(2\u2032-aminophenacyl);
(b) each of R1 and R6 is independently hydrido or methyl;
(c) R4 is hydrido or methoxy;
(d) R5 is hydroxyl or carboxyamino;
(e) R18 is amino or hydroxyl;
(f) R19 is hydrido or hydroxyl;
(g) R20 is carboxyamino or carboxymethyl;
(h) R28 is methyl or \u2014CH2CH2CH2NHP;
(i) R29 is methyl or CH2CH2CH2CH2NHP;
(j) P is an amino protecting group;
(k) R39 is independently amino, monosubstituted amino, disubstituted amino, acylamino, ureido, guanidino, carbamoyl, sulfonamino, thioacylamino, thioureido, iminoamino, or phosphonamino;
(l) provided that
(1) when R2 is \u2014CH2CH2CH2R8, R7 is other than
wherein R10 is amino, monosubstituted amino, disubstituted amino, acylamino, ureido, guanidino, carbamoyl, sulfonamino, thioacylamino, iminoamino, or phosphonamino;

R7
R9
NH2

NH2

NH2
a) wherein R14 is hydrido or methyl;
b) wherein R7** is an amino, monosubstituted amino, disubstituted amino, acylamino, ureido, guanidino, carbamoyl, sulfonamino, thioacylamino, thioureido, iminoamino, or phosphonamino and
c) each of Raa4, Raa5, and Raa6 is independently an amino acid side chain.
24. A composition comprising a compound of the Formula:
;
wherein R6 is H or CH3 and each of R7* and R9 is independently amino, monosubstituted amino, disubstituted amino, acylamino, ureido, guanidino, carbamoyl, sulfonamino, thioacylamino, thioureido, iminoamino, or phosphonamino.
25. A compound of the Formula 33:

The claims below are in addition to those above.
All refrences to claim(s) which appear below refer to the numbering after this setence.

1. A power semiconductor device, comprising:
a semiconductor layer;
polysilicon-containing gates;
a first semiconductor region formed in said semiconductor layer at one surface of said semiconductor layer and operative to serve as at least one of a source region and an emitter region;
a second semiconductor region formed in said semiconductor layer at the other surface of said semiconductor layer and operative to serve as at least one of a drain region and a collector region;
a gate routing wire commonly connected to a plurality of said gates and including a polysilicon portion and a metal portion formed adjacent to it in the direction of plane of said semiconductor layer;
an interlayer insulator film formed to cover said first semiconductor region, said gate routing wire and a plurality of said gates;
electrode portions formed in said interlayer insulator film and connected to said first semiconductor region; and
a strap electrode plate located to cover said interlayer insulator on said gate routing wire and cover a plurality of said electrode portions and commonly connected to a plurality of said electrode portions.
2. The power semiconductor device according to claim 1, wherein said gate is formed on a gate insulator film in a gate trench, said gate trench extending from one surface of said semiconductor layer into said semiconductor layer.
3. The power semiconductor device according to claim 2, further comprising a buried metal portion formed on and connected to said gate in said gate trench, wherein the bottom of said buried metal portion is located higher than the bottom of said first semiconductor region.
4. The power semiconductor device according to claim 2, further comprising:
an Intermediate insulator film formed between one surface of said semiconductor layer and said interlayer insulator film and having a larger thickness than said gate insulator film: and
a buried metal portion formed on and connected to said gate in said intermediate insulator film, wherein the bottom of said buried metal portion is located higher than the bottom of said first semiconductor region.
5. The power semiconductor device according to claim 4, wherein said intermediate insulator film is removed from below said gate routing wire.
6. The power semiconductor device according to claim 2, wherein said electrode portion extends into said semiconductor layer down to a location deeper than said first semiconductor region.
7. The power semiconductor device according to claim 1, wherein said metal portion extends along the direction of extension of said gate routing wire.
8. The power semiconductor device according to claim 1, wherein said metal portions and said polysilicon portions are arranged alternately.
9. The power semiconductor device according to claim 1, wherein said metal portion configures a side of said gate routing wire and having a sidewall shape.
10. The power semiconductor device according to claim 1, wherein said metal portion and said polysilicon portion are formed to have substantially the same height.
11. The power semiconductor device according to claim 1, wherein the bottom of said metal portion and the bottom of said polysilicon portion are located at substantially the same height.
12. The power semiconductor device according to claim 1, wherein the bottom of said metal portion is located higher than the bottom of said polysilicon portion.
13. The power semiconductor device according to claim 1, wherein said gate routing wire has a portion extending in a direction intersecting the direction of extension of said gate, said portion being commonly connected to said plurality of gates.
14. The power semiconductor device according to claim 1, wherein said gate is formed on said gate insulator film on one surface of said semiconductor layer.
15. The power semiconductor device according to claim 1, wherein said device is a MISFET, in which said first semiconductor region serves as said source region and said second semiconductor region serves as said drain region.
16. The power semiconductor device according to claim 1, wherein said device is an IGBT, in which said first semiconductor region serves as said emitter region and said second semiconductor region serves as said collector region.
17. A power semiconductor device, comprising:
a semiconductor layer;
a first semiconductor region formed in said semiconductor layer at one surface of said semiconductor layer and operative to serve as at least one of a source region and an emitter region;
a second semiconductor region formed in said semiconductor layer at the other surface of said semiconductor layer and operative to serve as at least one of a drain region and a collector region;
an insulator film formed on said first semiconductor region;
a gate formed on gate insulator film in a gate trench, said gate trench extending through said insulator film into said semiconductor layer; and
a buried metal portion formed in said gate trench and stacked on said gate, wherein the bottom of said buried metal portion is located higher than the bottom of said first semiconductor region.
18. The power semiconductor device according to claim 17, wherein said insulator film is an intermediate insulator film having a larger thickness than said gate insulator film.
19. The power semiconductor device according to claim 18, further comprising an electrode portion connected to said first semiconductor region,
wherein the lower part of said electrode portion is formed in a current path trench provided in said intermediate insulator film isolated from said trench.
20. The power semiconductor device according to claim 19, wherein the upper surface of said lower part of said electrode portion and the upper surface of said buried metal portion are located at substantially the same height.