The present disclosure describes compounds of the general Formula (I) or its stereoisomers, pharmaceutically acceptable salts, poly morphs, sols ales, hydrates, thereof. These compounds or small molecular adjuvants in combination with antibiotics are effective against resistant bacterial infections. The present disclosure also discloses a process of preparation of small-molecular adjuvants, its stereoisomers, pharmaceutically acceptable salts, polymorphs, solvates and hydrates thereof, and to pharmaceutical compositions containing them

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The present invention provides a process for preparing 2-methyl-N-(2′-methylbutyl) butanamide of the following formula (1):the process comprising: subjecting an α-arylethyl-2-methylbutylamine compound of the following general formula (2): wherein Ar represents a substituted or unsubstituted aryl group having 6 to 20 carbon atoms, to N-2-methylbutyrylation to form an N-α-arylethyl-2-methyl-N-(2′-methylbutyl)butanamide compound of the following general formula (3): wherein Ar is as defined above, and removing the α-arylethyl group of the resulting compound (3) to form 2-methyl-N-(2′ -methylbutyl)butanamide (1). ##STR00001##

The present invention provides a process for preparing 2-methyl-N-(2′-methylbutyl) butanamide of the following formula (1):the process comprising: subjecting an α-arylethyl-2-methylbutylamine compound of the following general formula (2): wherein Ar represents a substituted or unsubstituted aryl group having 6 to 20 carbon atoms, to N-2-methylbutyrylation to form an N-α-arylethyl-2-methyl-N-(2′-methylbutyl)butanamide compound of the following general formula (3): wherein Ar is as defined above, and removing the α-arylethyl group of the resulting compound (3) to form 2-methyl-N-(2′ -methylbutyl)butanamide (1). ##STR00001##

This invention provides a method of synthesizing new active compounds for pharmaceutical uses including cancer treatment, wherein the cancers comprise breast, leukocytic, liver, ovarian, bladder, prostatic, skin, bone, brain, leukemia, lung, colon, CNS, melanoma, renal, cervical, esophageal, testicular, splenic, kidney, lymphatic, pancreatic, stomach, eye and thyroid cancers. The active compounds are amine, sulfonamides, amide, and urea analogs of triterpene.

This invention provides a method of synthesizing new active compounds for pharmaceutical uses including cancer treatment, wherein the cancers comprise breast, leukocytic, liver, ovarian, bladder, prostatic, skin, bone, brain, leukemia, lung, colon, CNS, melanoma, renal, cervical, esophageal, testicular, splenic, kidney, lymphatic, pancreatic, stomach, eye and thyroid cancers. The active compounds are amine, sulfonamides, amide, and urea analogs of triterpene.

Certain disclosed embodiments concern a crosslinker having a Formula I

(Polymerizing Group 1).sub.s-(Amino Acid).sub.u-(Polymerizing Group 2).sub.y   Formula I,

where polymerizing group 1 and polymerizing group 2 independently are selected from an acrylate, alkyl acrylate, acrylamide, alkyl acrylamide, acrylonitrile, alkyl acrylonitrile or a (hydroxyalkyl) acrylate; s and y are from 1 to 10, with s and y each typically being 1; the amino acid is any naturally occurring amino acid, any non-naturally occurring amino acid, and any and all combinations thereof; and u is 2 to 100. Crosslinkers may include a naturally occurring amino acid or acids that are selected to provide amino-acid defining functional groups that are zwitterionic at a pH of from 2.5 to 10. Disclosed crosslinkers can also include “internal spacers”, “external spacers,” or both. Crosslinkers according to the present invention are used to make zwitterionic hydrogels that address fouling and bacteria adhesion issues associated with previously known hydrogels. Accordingly, such products are particularly suitable for biomedical applications, such as contact lenses, drug delivery vehicles, tissue engineering platforms, tissue regeneration platforms, catheters, implants and sensors.

Certain disclosed embodiments concern a crosslinker having a Formula I

(Polymerizing Group 1).sub.s-(Amino Acid).sub.u-(Polymerizing Group 2).sub.y   Formula I,

where polymerizing group 1 and polymerizing group 2 independently are selected from an acrylate, alkyl acrylate, acrylamide, alkyl acrylamide, acrylonitrile, alkyl acrylonitrile or a (hydroxyalkyl) acrylate; s and y are from 1 to 10, with s and y each typically being 1; the amino acid is any naturally occurring amino acid, any non-naturally occurring amino acid, and any and all combinations thereof; and u is 2 to 100. Crosslinkers may include a naturally occurring amino acid or acids that are selected to provide amino-acid defining functional groups that are zwitterionic at a pH of from 2.5 to 10. Disclosed crosslinkers can also include “internal spacers”, “external spacers,” or both. Crosslinkers according to the present invention are used to make zwitterionic hydrogels that address fouling and bacteria adhesion issues associated with previously known hydrogels. Accordingly, such products are particularly suitable for biomedical applications, such as contact lenses, drug delivery vehicles, tissue engineering platforms, tissue regeneration platforms, catheters, implants and sensors.

The invention provides synthetic processes and synthetic intermediate compounds that can be used to prepare therapeutic conjugates. The invention also provides methods for treating HBV and/or HDV infection in a human by administering a therapeutic conjugate prepared by the synthetic methods of the invention.

The invention provides synthetic processes and synthetic intermediate compounds that can be used to prepare therapeutic conjugates. The invention also provides methods for treating HBV and/or HDV infection in a human by administering a therapeutic conjugate prepared by the synthetic methods of the invention.

The present invention provides a method of industrially and safely producing lacosamide high in diastereomeric excess at a high yield and a low cost. Adopting a particular isomerization-crystallization condition makes it possible to a method of industrially and safely producing lacosamide high in diastereomeric excess at a high yield and a low cost. Additionally, an intermediate efficacious for producing lacosamide is provided.