C07C59/70

Compounds and methods for delivery of prostacyclin analogs
11292758 · 2022-04-05 · ·

This invention pertains generally to prostacyclin formulations and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis.

Compounds and methods for delivery of prostacyclin analogs
11292758 · 2022-04-05 · ·

This invention pertains generally to prostacyclin formulations and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis.

Single phase liquids of alkanolamine salts of dicamba

The invention is a herbicidal composition containing an alkanolamine salt of an dicamba capable of remaining as a single phase liquid over a period of at least 1 week and containing low amounts of water and high loadings of the salt. Such herbicidal compositions are capable of remaining liquid in the absence of high amounts of water, thereby enhancing their capacity to remain liquid over an extended period of time when exposed to environmental conditions to improve their effectiveness to transport the active salt through a leafy substrate and can reduce transportation costs by increasing the salt loading without compromising the stability of the composition.

Single phase liquids of alkanolamine salts of dicamba

The invention is a herbicidal composition containing an alkanolamine salt of an dicamba capable of remaining as a single phase liquid over a period of at least 1 week and containing low amounts of water and high loadings of the salt. Such herbicidal compositions are capable of remaining liquid in the absence of high amounts of water, thereby enhancing their capacity to remain liquid over an extended period of time when exposed to environmental conditions to improve their effectiveness to transport the active salt through a leafy substrate and can reduce transportation costs by increasing the salt loading without compromising the stability of the composition.

Process for the preparation of treprostinil

Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anhydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable. Also disclosed are treprostinil intermediates and the preparation of the intermediates. ##STR00001##

Process for the preparation of treprostinil

Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anhydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable. Also disclosed are treprostinil intermediates and the preparation of the intermediates. ##STR00001##

Binaphthyl compounds

The present invention relates to binaphthyl compounds of the formula (I), which are suitable as monomers for preparing polycarbonate resins having beneficial optical properties and which can be used for producing optical lenses: Formula (I) where X is C.sub.2-C.sub.4-alkandiyl or C.sub.1-C.sub.4-alkandiyl-C(O)—, where C(O) is bound to the oxygen atom of the hydroxyl group and where C.sub.2-C.sub.4-alkandiyl or C.sub.1-C.sub.4-alkandiyl, respectively, are unsubstituted or carry a phenyl ring; R and R′ are identical or different and selected from mono or polycyclic aryl having from 6 to 36 carbon atoms and mono- or polycyclic hetaryl having a total of 5 to 36 atoms, which are ring members, where 1, 2, 3 or 4 of these atoms are selected from nitrogen, sulfur and oxygen, while the remainder of these atoms are carbon atoms, where mono- or polycyclic aryl and mono- or polycyclic hetaryl are unsubstituted or carry 1 or 2 radicals R.sup.a, which are selected from the group consisting of CN, CH.sub.3, OCH.sub.3, O-phenyl, O-naphthyl, S-phenyl, S-naphthyl, CI or F; and, if X is C.sub.1-C.sub.4-alkandiyl-C(O)—, the esters thereof, in particular the C.sub.1-C.sub.4-alkylesters thereof. ##STR00001##

PHENOXY ACETIC ACIDS AND PHENYL PROPIONIC ACIDS AS PPAR DELTA AGONISTS

Phenoxy acetic acids and phenyl propionic acids and their use in improving mitochondrial energy output in a subject are provided herein. The present compounds are activators of PPARδ and may be useful for treating conditions mediated by the same.

PHENOXY ACETIC ACIDS AND PHENYL PROPIONIC ACIDS AS PPAR DELTA AGONISTS

Phenoxy acetic acids and phenyl propionic acids and their use in improving mitochondrial energy output in a subject are provided herein. The present compounds are activators of PPARδ and may be useful for treating conditions mediated by the same.

Preparation method of phenoxycarboxylic acid herbicides

Disclosed is a preparation method of phenoxycarboxylic acid herbicides. The preparation method comprises the following steps. S1: mixing an anhydrous phenol and a basic substance with a chloro-substituted carboxylic acid ester and performing a one-pot condensation reaction in an anhydrous system to obtain a phenoxycarboxylic acid ester. The chloro-substituted carboxylic acid ester is represented by the formula ClR.sub.1COOR, in which R.sub.1 is a C1-3 alkanediyl or alkylidene group, R is a C1-10 alkyl group or a C3-10 cycloalkyl group; S2: the phenoxycarboxylic acid ester undergoes selective chlorination with a chlorinating agent in the presence of a first catalyst and a second catalyst to obtain a chloro-substituted phenoxycarboxylic acid ester; and S3: the chloro-substituted phenoxycarboxylic acid ester undergoes an acid hydrolysis reaction to obtain a phenoxycarboxylic acid herbicide represented by formula I, in which R.sub.3 is H, Cl or CH.sub.3. ##STR00001##