Disclosed herein are prodrugs of tapinarof and pharmaceutical formulations comprising tarpinarof, such as oral formulations. Further disclosed herein are methods for treating diseases and disorders of the gastrointestinal tract, skin, eye, lung, and bone joints via the tapinarof prodrugs.

Disclosed herein are prodrugs of tapinarof and pharmaceutical formulations comprising tarpinarof, such as oral formulations. Further disclosed herein are methods for treating diseases and disorders of the gastrointestinal tract, skin, eye, lung, and bone joints via the tapinarof prodrugs.

The present invention relates to a process for the preparation of the mono sodium salt of the derivative 3,5-diiodo-O-[3-iodo-4-(sulphooxy)phenyl]-L-tyrosine (T3S) by starting from the corresponding phenolic compound, in the presence of chlorosulfonic acid and dimethylacetamide as a solvent. The so obtained T3S compound may conveniently be isolated in a pure form as a solid in good yields.

The present invention further relates to the process for T3S preparation, wherein the starting reagent is T2 and further comprising the formulation of such compound in tablets.

Furthermore, the invention discloses non-radioactive immunoassays based on T3S derivatives.

The present invention relates to a process for the preparation of the mono sodium salt of the derivative 3,5-diiodo-O-[3-iodo-4-(sulphooxy)phenyl]-L-tyrosine (T3S) by starting from the corresponding phenolic compound, in the presence of chlorosulfonic acid and dimethylacetamide as a solvent. The so obtained T3S compound may conveniently be isolated in a pure form as a solid in good yields.

The present invention further relates to the process for T3S preparation, wherein the starting reagent is T2 and further comprising the formulation of such compound in tablets.

Furthermore, the invention discloses non-radioactive immunoassays based on T3S derivatives.

The present invention relates to a process for the preparation of the mono sodium salt of the derivative 3,5-diiodo-O-[3-iodo-4-(sulphooxy)phenyl]-L-tyrosine (T3S) by starting from the corresponding phenolic compound, in the presence of chlorosulfonic acid and dimethylacetamide as a solvent. The so obtained T3S compound may conveniently be isolated in a pure form as a solid in good yields.

The present invention further relates to the process for T3S preparation, wherein the starting reagent is T2 and further comprising the formulation of such compound in tablets.

Furthermore, the invention discloses non-radioactive immunoassays based on T3S derivatives.

The present invention relates to a process for the preparation of the mono sodium salt of the derivative 3,5-diiodo-O-[3-iodo-4-(sulphooxy)phenyl]-L-tyrosine (T3S) by starting from the corresponding phenolic compound, in the presence of chloro-sulfonic acid and dimethylacetamide as a solvent. The so obtained T3S compound may conveniently be isolated in a pure form as a solid in good yields. The present invention further relates to the process for T3S preparation, wherein the starting reagent is T2 and further comprising the formulation of such compound in tablets. Furthermore, the invention discloses non-radioactive immunoassays based on T3S derivatives.

The present invention relates to a process for the preparation of the mono sodium salt of the derivative 3,5-diiodo-O-[3-iodo-4-(sulphooxy)phenyl]-L-tyrosine (T3S) by starting from the corresponding phenolic compound, in the presence of chloro-sulfonic acid and dimethylacetamide as a solvent. The so obtained T3S compound may conveniently be isolated in a pure form as a solid in good yields. The present invention further relates to the process for T3S preparation, wherein the starting reagent is T2 and further comprising the formulation of such compound in tablets. Furthermore, the invention discloses non-radioactive immunoassays based on T3S derivatives.

Cannabinoid-gabapentinoid conjugates and their formulations possessing dual synergistic pharmacological effects to control neuropathic pain, multiple sclerosis, seizures and postherpetic neuralgia, restless leg syndrome, trigeminal neuralgia, fibromyalgia, diabetic neuropathy, anxiety and bipolar disorders, schizophrenia, sleep disorders, and other related pathological conditions. The conjugates improve the therapeutic potential for both component compounds, while reducing the addiction and substance abuse problems commonly observed with each component, when prescribed independently, thereby providing a solution for cannabinoid and gabapentinoid substance abuse disorders.

Cannabinoid-gabapentinoid conjugates and their formulations possessing dual synergistic pharmacological effects to control neuropathic pain, multiple sclerosis, seizures and postherpetic neuralgia, restless leg syndrome, trigeminal neuralgia, fibromyalgia, diabetic neuropathy, anxiety and bipolar disorders, schizophrenia, sleep disorders, and other related pathological conditions. The conjugates improve the therapeutic potential for both component compounds, while reducing the addiction and substance abuse problems commonly observed with each component, when prescribed independently, thereby providing a solution for cannabinoid and gabapentinoid substance abuse disorders.

A sulfonium salt of formula (0-1) is provided wherein W is alkylene or arylene, R.sup.01 is a monovalent hydrocarbon group, m is 0, 1 or 2, k is an integer: 0k5+4m, R.sup.101, R.sup.102 and R.sup.103 are a monovalent hydrocarbon group, or at least two of R.sup.101, R.sup.102 and R.sup.103 may bond together to form a ring with the sulfur atom, and L is a single bond, ester, sulfonic acid ester, carbonate or carbamate bond. A resist composition comprising the sulfonium salt as PAG exhibits a very high resolution when processed by EB and EUV lithography. A pattern with minimal LER is obtainable. ##STR00001##