C07D501/57

Crystal of cephalosporin intermediate 7α-methoxy cephalothin and method for preparing same

The present invention relates to a crystal of cephalosporin intermediate 7-methoxy cephalothin (I) and a method for preparing same. The crystal of 7-methoxy cephalothin (I) undergoes Cu-Ka radiation and X-ray powder diffraction expressed in terms of angle 2; the crystal of 7-methoxy cephalothin (I) has characteristic absorption peaks at positions of 7.340.20, 12.710.20, 14.250.20, 14.680.20, 16.520.20, 17.990.20, 19.980.20, and 22.690.20. The crystal of 7-methoxy cephalothin provided by the present invention is easy to prepare. Related test data shows that the crystal of 7-methoxy cephalothin has high purity, low impurity content, and good stability. The preparation cost is low, the preparation method is simple to operate, conditions are mild and easy to control, and crystals of 7-methoxy cephalothin can be obtained stably. The invention is applicable to industrial production.

APPLICATIONS OF SPERMINE AND DERIVATIVES THEREOF
20200297660 · 2020-09-24 ·

This disclosure relates to a method for treating a disease which can be alleviated by inhibiting PAICS activity. The method includes administering a therapeutically effective amount of spermine or a pharmaceutically acceptable salt or C.sub.1-C.sub.6 amide thereof to a patient in need thereof.

APPLICATIONS OF SPERMINE AND DERIVATIVES THEREOF
20200297660 · 2020-09-24 ·

This disclosure relates to a method for treating a disease which can be alleviated by inhibiting PAICS activity. The method includes administering a therapeutically effective amount of spermine or a pharmaceutically acceptable salt or C.sub.1-C.sub.6 amide thereof to a patient in need thereof.

Applications of spermine and derivatives thereof
10709676 · 2020-07-14 · ·

Provided are applications of spermine and derivatives thereof. On the basis of existing protein structure data and small molecule structure data, calculations and analysis are performed using software to screen and obtain compounds capable of effectively interfering with PAICS activity, reducing SAICAR synthesis, and ultimately reducing SAICAR accumulation, in order to achieve the goal of treating or reducing ADSL deficiency. A better effect in the treatment or improvement of ADSL deficiency is expected from the joint use of at least two of the described compounds.

Applications of spermine and derivatives thereof
10709676 · 2020-07-14 · ·

Provided are applications of spermine and derivatives thereof. On the basis of existing protein structure data and small molecule structure data, calculations and analysis are performed using software to screen and obtain compounds capable of effectively interfering with PAICS activity, reducing SAICAR synthesis, and ultimately reducing SAICAR accumulation, in order to achieve the goal of treating or reducing ADSL deficiency. A better effect in the treatment or improvement of ADSL deficiency is expected from the joint use of at least two of the described compounds.

CRYSTAL OF CEPHALOSPORIN INTERMEDIATE 7alpha-METHOXY CEPHALOTHIN AND METHOD FOR PREPARING SAME

The present invention relates to a crystal of cephalosporin intermediate 7-methoxy cephalothin (I) and a method for preparing same. The crystal of 7-methoxy cephalothin (I) undergoes Cu-Ka radiation and X-ray powder diffraction expressed in terms of angle 2; the crystal of 7-methoxy cephalothin (I) has characteristic absorption peaks at positions of 7.340.20, 12.710.20, 14.250.20, 14.680.20, 16.520.20, 17.990.20, 19.980.20, and 22.690.20. The crystal of 7-methoxy cephalothin provided by the present invention is easy to prepare. Related test data shows that the crystal of 7-methoxy cephalothin has high purity, low impurity content, and good stability. The preparation cost is low, the preparation method is simple to operate, conditions are mild and easy to control, and crystals of 7-methoxy cephalothin can be obtained stably. The invention is applicable to industrial production.

NOVEL APPLICATIONS OF SPERMINE AND DERIVATIVES THEREOF
20190209493 · 2019-07-11 ·

Provided are applications of spermine and derivatives thereof. On the basis of existing protein structure data and small molecule structure data, calculations and analysis are performed using software to screen and obtain compounds capable of effectively interfering with PAICS activity, reducing SAICAR synthesis, and ultimately reducing SAICAR accumulation, in order to achieve the goal of treating or reducing ADSL deficiency. A better effect in the treatment or improvement of ADSL deficiency is expected from the joint use of at least two of the described compounds.

Cephem Compounds with Latent Reactive Groups

Cephem and penem compounds having a styrylmethylene moiety at the 3-position in the cephem or penem ring to which a positively charged leaving group is bonded and wherein the leaving group contains a vicinal diol or is bonded to a unsubstituted or substituted catechol. The leaving group can be a positively charge nitrogen leaving group. Cephems include cephalosporins, cephamycins, carbacephems, and oxacephems. Penems include penems, carbapenems and oxapenems. Preferred cephems are cephalosporins. Preferred penems are carbapenems. Compounds exhibit antibiotic activity against Gram-negative bacteria and/or Gram-positive bacteria. Compounds exhibit antibiotic activity against bacteria which exhibit multi-drug resistance. Compounds of the invention exhibit antibiotic activity against bacterial strains which produce extended spectrum beta-lactamases (ESBL), which produce AmpC beta-lactamases or which produce a carbapenemase. Pharmaceutical compositions comprising one or more cephems or penems or methods of treatment of bacterial infections with such compounds and compositions.

Cephem Compounds with Latent Reactive Groups

Cephem and penem compounds having a styrylmethylene moiety at the 3-position in the cephem or penem ring to which a positively charged leaving group is bonded and wherein the leaving group contains a vicinal diol or is bonded to a unsubstituted or substituted catechol. The leaving group can be a positively charge nitrogen leaving group. Cephems include cephalosporins, cephamycins, carbacephems, and oxacephems. Penems include penems, carbapenems and oxapenems. Preferred cephems are cephalosporins. Preferred penems are carbapenems. Compounds exhibit antibiotic activity against Gram-negative bacteria and/or Gram-positive bacteria. Compounds exhibit antibiotic activity against bacteria which exhibit multi-drug resistance. Compounds of the invention exhibit antibiotic activity against bacterial strains which produce extended spectrum beta-lactamases (ESBL), which produce AmpC beta-lactamases or which produce a carbapenemase. Pharmaceutical compositions comprising one or more cephems or penems or methods of treatment of bacterial infections with such compounds and compositions.