C07F9/6524

Nucleoside phosphate compound and preparation method and use thereof

Provided in the present invention are a compound of Formula (I), a pharmaceutical composition comprising the same, a method for preparing the same, and use thereof as a NS5B polymerase inhibitor, a DNA polymerase inhibitor or a reverse transcriptase inhibitor for the prevention or treatment of viral diseases or cancers.

Long-Lived Gadolinium Based Tumor Targeted Imaging and Therapy Agents
20210008203 · 2021-01-14 ·

Alkylphosphocholine analogs incorporating a chelating moiety that is chelated to gadolinium are disclosed herein. The alkylphophocholine analogs are compounds having the formula:

##STR00001##

or a salt therof. R.sub.1 includes a chelating agent that is chelated to a gadolinium atom; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is H, OH, COOH, COOX, OCOX, or OX, wherein X is an alkyl or an arylalkyl; R.sub.2 is N.sup.+H.sub.3, N.sup.+H.sub.2Z, N.sup.+HZ.sub.2, or N.sup.+Z.sub.3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2. The compounds can be used to detect solid tumors or to treat solid tumors. In detection/imaging applications, the gadolinium emits signals that are detectable using magnetic resonance imaging. In therapeutic treatment, the gadolinium emits tumor-targeting charged particles when exposed to epithermal neutrons.

Long-Lived Gadolinium Based Tumor Targeted Imaging and Therapy Agents
20210008203 · 2021-01-14 ·

Alkylphosphocholine analogs incorporating a chelating moiety that is chelated to gadolinium are disclosed herein. The alkylphophocholine analogs are compounds having the formula:

##STR00001##

or a salt therof. R.sub.1 includes a chelating agent that is chelated to a gadolinium atom; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is H, OH, COOH, COOX, OCOX, or OX, wherein X is an alkyl or an arylalkyl; R.sub.2 is N.sup.+H.sub.3, N.sup.+H.sub.2Z, N.sup.+HZ.sub.2, or N.sup.+Z.sub.3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2. The compounds can be used to detect solid tumors or to treat solid tumors. In detection/imaging applications, the gadolinium emits signals that are detectable using magnetic resonance imaging. In therapeutic treatment, the gadolinium emits tumor-targeting charged particles when exposed to epithermal neutrons.

Long-lived gadolinium based tumor targeting imaging and therapy agents

Alkylphosphocholine analogs incorporating a chelating moiety that is chelated to gadolinium are disclosed herein. The alkylphophocholine analogs are compounds having the formula: ##STR00001##
or a salt thereof. R.sub.1 includes a chelating agent that is chelated to a gadolinium atom; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is H, OH, COOH, COOX, OCOX, or OX, wherein X is an alkyl or an arylalkyl; R.sub.2 is N.sup.+H.sub.3, N.sup.+H.sub.2Z, N.sup.+HZ.sub.2, or N.sup.+Z.sub.3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2. The compounds can be used to detect solid tumors or to treat solid tumors. In detection/imaging applications, the gadolinium emits signals that are detectable using magnetic resonance imaging. In therapeutic treatment, the gadolinium emits tumor-targeting charged particles when exposed to epithermal neutrons.

Long-lived gadolinium based tumor targeting imaging and therapy agents

Alkylphosphocholine analogs incorporating a chelating moiety that is chelated to gadolinium are disclosed herein. The alkylphophocholine analogs are compounds having the formula: ##STR00001##
or a salt thereof. R.sub.1 includes a chelating agent that is chelated to a gadolinium atom; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is H, OH, COOH, COOX, OCOX, or OX, wherein X is an alkyl or an arylalkyl; R.sub.2 is N.sup.+H.sub.3, N.sup.+H.sub.2Z, N.sup.+HZ.sub.2, or N.sup.+Z.sub.3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2. The compounds can be used to detect solid tumors or to treat solid tumors. In detection/imaging applications, the gadolinium emits signals that are detectable using magnetic resonance imaging. In therapeutic treatment, the gadolinium emits tumor-targeting charged particles when exposed to epithermal neutrons.

DEUTERATED AZOLE COMPOUNDS AND PREPARATION METHOD THEREFOR AND USES THEREOF
20200317636 · 2020-10-08 ·

Disclosed are a deuterated azole compound of formula (I) and a preparation method and an application of a pharmaceutically acceptable salt and prodrug of the compound. The deuterated azole compound disclosed by the invention has good antifungal activity and metabolic stability, and can be used for preparing antifungal drugs.

##STR00001##

DEUTERATED AZOLE COMPOUNDS AND PREPARATION METHOD THEREFOR AND USES THEREOF
20200317636 · 2020-10-08 ·

Disclosed are a deuterated azole compound of formula (I) and a preparation method and an application of a pharmaceutically acceptable salt and prodrug of the compound. The deuterated azole compound disclosed by the invention has good antifungal activity and metabolic stability, and can be used for preparing antifungal drugs.

##STR00001##

NUCLEOSIDE PHOSPHATE COMPOUND AND PREPARATION METHOD AND USE THEREOF

Provided in the present invention are a compound of Formula (I), a pharmaceutical composition comprising the same, a method for preparing the same, and use thereof as a NS5B polymerase inhibitor, a DNA polymerase inhibitor or a reverse transcriptase inhibitor for the prevention or treatment of viral diseases or cancers.

Radioactive Phospholipid Metal Chelates for Cancer Imaging and Therapy
20200291049 · 2020-09-17 ·

Alkylphosphocholine analogs incorporating a chelating moiety that chelates a radioactive metal isotope are disclosed herein. The alkylphophocholine analogs, which can be used to treat or detect solid tumors, have the formula:

##STR00001##

R.sub.1 includes a chelating agent that is chelated to a metal atom, wherein the metal atom is a positron or single photon emitting metal isotope with a half life of greater than or equal to 4 hours, or an alpha, beta or Auger emitting metal isotope with a half life of greater than 6 hours and less than 30 days; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is H, OH, COOH, COOX, OCOX, or OX, wherein X is an alkyl or an arylalkyl; R.sub.2 is N.sup.+H.sub.3, N.sup.+H.sub.2Z, N.sup.+HZ.sub.2, or N.sup.+Z.sub.3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2.

Radioactive Phospholipid Metal Chelates for Cancer Imaging and Therapy
20200291049 · 2020-09-17 ·

Alkylphosphocholine analogs incorporating a chelating moiety that chelates a radioactive metal isotope are disclosed herein. The alkylphophocholine analogs, which can be used to treat or detect solid tumors, have the formula:

##STR00001##

R.sub.1 includes a chelating agent that is chelated to a metal atom, wherein the metal atom is a positron or single photon emitting metal isotope with a half life of greater than or equal to 4 hours, or an alpha, beta or Auger emitting metal isotope with a half life of greater than 6 hours and less than 30 days; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is H, OH, COOH, COOX, OCOX, or OX, wherein X is an alkyl or an arylalkyl; R.sub.2 is N.sup.+H.sub.3, N.sup.+H.sub.2Z, N.sup.+HZ.sub.2, or N.sup.+Z.sub.3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2.