The disclosure is directed to new crystalline tebipenem pivoxil salt forms, including a crystalline tebipenem pivoxil ethane sulfonate salt form (Form A), a crystalline tebipenem pivoxil ketoglutarate salt form (Form A), tebipenem pivoxil maleate salt forms (Form A and Form B), a tebipenem pivoxil malate salt form (Form A), a tebipenem pivoxil methane sulfonate salt form (Form B), a tebipenem pivoxil hydrobromide salt form (Form B), and a tebipenem pivoxil edisylate salt form (Form A). The disclosure also includes a composition, comprising a crystalline tebipenem pivoxil salt and a pharmaceutically acceptable carrier and further includes a method for treating an antibiotic resistant bacterial infection, comprising administering to a patient in need of such treatment a therapeutically effective amount of a crystalline tebipenem pivoxil salt.

The disclosure is directed to new crystalline tebipenem pivoxil salt forms, including a crystalline tebipenem pivoxil ethane sulfonate salt form (Form A), a crystalline tebipenem pivoxil ketoglutarate salt form (Form A), tebipenem pivoxil maleate salt forms (Form A and Form B), a tebipenem pivoxil malate salt form (Form A), a tebipenem pivoxil methane sulfonate salt form (Form B), a tebipenem pivoxil hydrobromide salt form (Form B), and a tebipenem pivoxil edisylate salt form (Form A). The disclosure also includes a composition, comprising a crystalline tebipenem pivoxil salt and a pharmaceutically acceptable carrier and further includes a method for treating an antibiotic resistant bacterial infection, comprising administering to a patient in need of such treatment a therapeutically effective amount of a crystalline tebipenem pivoxil salt.

The present disclosure provides broad-spectrum carbapenem derivatives and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such derivatives and/or compositions.

The present disclosure provides broad-spectrum carbapenem derivatives and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such derivatives and/or compositions.

A process for the preparation of a carbapenem, includes the step of treating a solution of a protected carbapenem with hydrogen gas in the presence of a heterogeneous catalyst to form the carbapenem, wherein the heterogeneous catalyst includes at least two platinum group metals.

This invention describes an ICE inhibitor prodrug (I) having good bioavailability. ##STR00001##
Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.

This invention describes an ICE inhibitor prodrug (I) having good bioavailability. ##STR00001##
Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.

Provided herein are the design, preparation, evaluation, and use of structurally modified carbapenem antibiotics with improved activity, relative to current commercially available carbapenem antibiotics, against infections involving multidrug-resistant, carbapenemase-producing Enterobacterales strains. In particular, the new carbapenem antibiotics are demonstrated to produce improved activity, relative to current commercial carbapenem antibiotics, against bacterial strains producing a KPC carbapenemase. This invention includes their use as standalone antibiotics, as well as synergistic mixtures of the structurally modified carbapenems with carbapenemase inhibitors as well as synergistic mixtures of the newly modified carbapenems with other carbapenem antibiotics.

Provided herein are the design, preparation, evaluation, and use of structurally modified carbapenem antibiotics with improved activity, relative to current commercially available carbapenem antibiotics, against infections involving multidrug-resistant, carbapenemase-producing Enterobacterales strains. In particular, the new carbapenem antibiotics are demonstrated to produce improved activity, relative to current commercial carbapenem antibiotics, against bacterial strains producing a KPC carbapenemase. This invention includes their use as standalone antibiotics, as well as synergistic mixtures of the structurally modified carbapenems with carbapenemase inhibitors as well as synergistic mixtures of the newly modified carbapenems with other carbapenem antibiotics.

The disclosure provides a new crystal form of ertapenem sodium and preparation method therefor. The new crystal form of ertapenem sodium has 27 principal characteristic peaks in an X-ray powder diffraction diagram. The crystal form of ertapenem sodium of the disclosure has a rod-like crystal habit, which has a large particle size, is not prone to aggregation and is easier to dry, and a product with high crystallinity and high purity may be obtained by simple drying treatment. Meanwhile, the crystal form of the disclosure has better stability, and the crystal form may remain unchanged to a maximum extent in subsequent washing and drying processes, thereby further improving the purity of the product.