C07D473/40

METHOD FOR SYNTHESIZING DIVERSELY SUBSTITUTED PURINES

The present invention relates to a method for synthesizing diversely substituted purines starting from a pyrimidine. Formula (I). The method comprises the formation of an amidine group on the pyrimidine by implementing a Vilsmeier type reagent, the functionalization of the pyrimidine with an amine and the cyclization to form the purine nucleus. Optional steps can also be performed in order to further functionalize the molecule. The invention also relates to new purines and new intermediate product.

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HETEROCYCLIC COMPOUNDS AND USES AS ANTICANCER AGENTS
20210100802 · 2021-04-08 · ·

The present disclosure provides pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.

HETEROCYCLIC COMPOUNDS AND USES AS ANTICANCER AGENTS
20210100802 · 2021-04-08 · ·

The present disclosure provides pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.

Substituted quinoxaline DNA-PK inhibitors

The present invention relates to Provided are compounds of Formula (I): ##STR00001##
wherein R.sup.1, R.sup.2, X, Ring A, Ring B, and Ring C are as defined herein. Compounds of Formula (I) are useful as inhibitors of DNA-PK. Also provided are pharmaceutical compositions comprising said compounds and methods of using the compounds and compositions in the treatment of various diseases, conditions, and disorders.

Substituted quinoxaline DNA-PK inhibitors

The present invention relates to Provided are compounds of Formula (I): ##STR00001##
wherein R.sup.1, R.sup.2, X, Ring A, Ring B, and Ring C are as defined herein. Compounds of Formula (I) are useful as inhibitors of DNA-PK. Also provided are pharmaceutical compositions comprising said compounds and methods of using the compounds and compositions in the treatment of various diseases, conditions, and disorders.

Plant growth regulation

The present invention relates to a new plant growth regulation composition comprising a compound of Formula (Ia) and trinexapac-ethyl. (Ia). It also relates to a method for enhancing or regulating the growth of plants comprising applying said composition. ##STR00001##

Plant growth regulation

The present invention relates to a new plant growth regulation composition comprising a compound of Formula (Ia) and trinexapac-ethyl. (Ia). It also relates to a method for enhancing or regulating the growth of plants comprising applying said composition. ##STR00001##

Synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) and 2′-fluoro-6′methylene-carbocyclic guanosine (FMCG)

The invention provides a new convergent approach for the synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) and 2′-fluoro-6′-methylene-carbocyclic guanosine (FMCG) from a readily available starting material in eight steps. An efficient and practical methodology for stereospecific preparation of a versatile carbocyclic key intermediate, (1S,3R, 4R)-3-tert-butoxy-4-(tert-butoxymethyl)-2-fluoro-5-methylenecyclopentanol (compound 8 of scheme 1A or a) in only six (6) steps is also provided. Prodrugs of these compounds are also prepared.

Synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) and 2′-fluoro-6′methylene-carbocyclic guanosine (FMCG)

The invention provides a new convergent approach for the synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) and 2′-fluoro-6′-methylene-carbocyclic guanosine (FMCG) from a readily available starting material in eight steps. An efficient and practical methodology for stereospecific preparation of a versatile carbocyclic key intermediate, (1S,3R, 4R)-3-tert-butoxy-4-(tert-butoxymethyl)-2-fluoro-5-methylenecyclopentanol (compound 8 of scheme 1A or a) in only six (6) steps is also provided. Prodrugs of these compounds are also prepared.

BENZOIMIDAZOLES AS PROLYL HYDROXYLASE INHIBITORS

The present invention is directed to benzoimidazole compounds of the formula:

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and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.