C07C233/07

Carbonic acid adducts

The present invention relates to a carbonic acid adduct (CAA) comprising carbonic acid, at least one amine, and optionally at least one salt, said adduct being producible by a method comprising the following steps: a) providing a solution (A) comprising dissolved CO.sub.2; optionally b) dissolving a base (BA) not corresponding to the amine (AM) in the solution (A) so as to obtain the solution (A1); c) dissolving the at least one amine (AM) in the solution (A) or (A1) so as to obtain the solution (B); d) freezing the solution obtained after completion of step c); and e) storing the solution frozen in step d) at −100 to 0° C. for no longer than 4 days. The content of CO.sub.2 in the solution that is subjected to step c) is at least 6 g/l. The invention also relates to a method for producing the carbonic acid adduct (CAA), a pharmaceutical preparation (PP) comprising the carbonic acid adduct (CAA), and methods for the production thereof and use of the carbonic acid adduct (CAA) or the pharmaceutical preparation (PP) in therapy for a range of indications.

Compositions for the treatment of pulmonary fibrosis
11401245 · 2022-08-02 · ·

The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related conditions.

Compositions for the treatment of pulmonary fibrosis
11401245 · 2022-08-02 · ·

The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related conditions.

MODULATORS OF TMEM16A FOR TREATING RESPIRATORY DISEASE

Compounds of general formula (I):

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wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, A, Z.sup.1, Z.sup.2 and Y are as defined herein are useful for treating respiratory disease and other diseases and conditions modulated by TMEM16A.

MODULATORS OF TMEM16A FOR TREATING RESPIRATORY DISEASE

Compounds of general formula (I):

##STR00001##

wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, A, Z.sup.1, Z.sup.2 and Y are as defined herein are useful for treating respiratory disease and other diseases and conditions modulated by TMEM16A.

Substituted benzenecarboxamides as IL-17A modulators

The disclosure herein provides compounds and pharmaceutical compositions for the modulation of IL-17A useful for the treatment of inflammatory conditions, such as psoriasis.

VASCULAR ADHESION PROTEIN-1 (VAP-1) MODULATORS AND THERAPEUTIC USES THEREOF

Disclosed herein are small molecule Vascular Adhesion Protein-1 (VAP-1) modulator compositions, pharmaceutical compositions, the use and preparation thereof.

Synthetic nicotine composition

A synthetic nicotine composition comprising synthetic nicotine, a synthetic nicotine salt and a synthetic nicotine derivative, wherein the synthetic nicotine, the synthetic nicotine salt, and the synthetic nicotine derivative are in mass percentage; the synthetic nicotine accounts for 1-20%, the synthetic nicotine salt accounts for 30-70%, and the synthetic nicotine derivative accounts for 20-50%; and the synthetic nicotine is one or more of S-nicotine and a mixture of R-nicotine containing a racemate and S-nicotine. The synthetic nicotine, synthetic nicotine salt and synthetic nicotine derivative according to the present invention are proportionally mixed to prepare an existing synthetic nicotine product, which relieves the problem of the impact of impurities in natural extracted nicotine products causing an unpleasant smell, a bitter taste and a strong volatility, and can be used in the fields of low temperature heat-not-burn products, snuff, electronic cigarettes, nicotine release patches, insecticides, herbicides, microbicides, drug synthesis, etc.

Synthetic nicotine composition

A synthetic nicotine composition comprising synthetic nicotine, a synthetic nicotine salt and a synthetic nicotine derivative, wherein the synthetic nicotine, the synthetic nicotine salt, and the synthetic nicotine derivative are in mass percentage; the synthetic nicotine accounts for 1-20%, the synthetic nicotine salt accounts for 30-70%, and the synthetic nicotine derivative accounts for 20-50%; and the synthetic nicotine is one or more of S-nicotine and a mixture of R-nicotine containing a racemate and S-nicotine. The synthetic nicotine, synthetic nicotine salt and synthetic nicotine derivative according to the present invention are proportionally mixed to prepare an existing synthetic nicotine product, which relieves the problem of the impact of impurities in natural extracted nicotine products causing an unpleasant smell, a bitter taste and a strong volatility, and can be used in the fields of low temperature heat-not-burn products, snuff, electronic cigarettes, nicotine release patches, insecticides, herbicides, microbicides, drug synthesis, etc.

Method For Preparing Hexahydrofuro-Furanol Derivative, Intermediate Thereof And Preparation Method Thereof

The invention relates to the field of pharmaceutical synthesis, in particular to the preparation method of hexahydrofuro-furanol derivative, intermediates thereof and preparation methods thereof. The preparation methods comprises the steps of halogenation reaction, acylation reaction, enzymatic reduction reaction, reaction with amine compounds, reduction ring closure reaction (A1, A2, B, Cp1, C.sub.L, Cf)

##STR00001##

wherein, R.sub.1, R.sub.2, R.sub.3 are hydrogen or hydroxy protecting groups; R.sub.4 and R.sub.5 are the same or different and are phenyl, alkyl or substituted phenyl. In the preparation process of hexahydrofuro-furanol derivatives, the chirality is constructed by enzymatic method, and the product can be prepared with very high optical purity by adopting such technical means. The preparation method can be used to prepare the key intermediate, (3R, 3aS, 6aR)-hexahydrofuro[2,3-b]-3-ol, of Darunavir, in commercial production, which is a very economical route suitable for industrial production.