C07K7/645

METHOD FOR PRODUCING CYCLIC ORGANIC COMPOUND
20210147475 · 2021-05-20 ·

An objective of the present invention is to provide methods of producing a cyclic organic compound using a continuous stirred tank reactor(s) (CSTR), the methods being capable of achieving excellent impurity-suppressing effects (quality improvement), reduction in reaction-tank size, continuous production, and such. The present inventors conducted studies on cyclization reactions using a CSTR(s), which had not been conventionally used for cyclization reactions for cyclic compounds. As a result, the inventors have found that the present methods can achieve excellent impurity-suppressing effects (quality improvement), reduction in reaction-tank size, continuous production, and such, as compared with conventional cyclization methods. Furthermore, the present inventors have also found that the above-mentioned improvement effects can efficiently be achieved even in the production of cyclic peptides and heterocyclic compounds by applying simulation methods that had been conventionally used mainly at the fine chemicals plant level to the cyclization reactions of the present invention, thereby experimentally predicting the reaction rate of a cyclization reaction, and setting the flow volume (residence time), the concentrations of precursor and cyclic organic compound, and the temperature for the cyclization reaction and such which affect these conditions, in the cyclization reaction using a CSTR(s).

Maleate of SCY-635 and uses thereof in medicine

The present invention relates to a salt of a compound of formula (I) and uses thereof in medicine. Specifically, it relates to maleate of compound of formula (I) and pharmaceutically compositions thereof. Furthermore, the invention relates to the uses of maleate herein and pharmaceutically compositions thereof disclosed herein in the manufacture of a medicament, especially in the manufacture of a medicament for preventing, managing, treating or lessening hepatitis C virus (HCV) infection. ##STR00001##

Hybrid cyclic libraries and screens thereof

Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.

NTCP Inhibitors

The invention provides cyclosporin A analogues that are NTCP inhibitors and useful for treating HBV and/or HDV infection(s), hepatoprotection and amelioration of hypercholesterolemia, diabetes and inhibiting cancer.

NTCP inhibitors

The invention provides cyclosporin A analogues that are NTCP inhibitors and useful for treating HBV and/or HDV infection(s), hepatoprotection and amelioration of hypercholesterolemia, diabetes and inhibiting cancer.

Cyclosporine analogue mixtures and their use as immunomodulating agents

The invention is directed to isomeric mixtures of cyclosporine analogues that are structurally similar to cyclosporine A. The mixtures possess enhanced efficacy and reduced toxicity over the individual isomers and over naturally occurring and other presently known cyclosporines and cyclosporine derivatives. Embodiments of the present invention are directed toward cis and trans-isomers of cyclosporin A analogs referred to as ISA.sub.TX247, and derivatives thereof. Mixtures of ISA.sub.TX247 isomers exhibit a combination of enhanced potency and reduced toxicity over the naturally occurring and presently known cyclosporins. ISA.sub.TX247 isomers and alkylated, arylated, and deuterated derivatives are synthesized by stereoselective pathways where the particular conditions of a reaction determine the degree of stereoselectivity. The ratio of isomers in a mixture may range from about 10 to 90 percent by weight of the (E)-isomer to about 90 to 10 percent by weight of the (Z)-isomer, based on the total weight of the mixture.

Macrocycles

The invention relates to cyclic compounds of general formula (I): wherein R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, and their use as pharmaceuticals. ##STR00001##

Gene Therapy
20200237962 · 2020-07-30 ·

Use of cyclosporin A (CsA) or a derivative thereof for increasing the efficiency of transduction of an isolated population of human haematopoietic stem and/or progenitor cells by a vector derived from HIV-1, HIV-2, FIV, BIV, EIAV, CAEV or visna lentivirus.

CYCLOSPORIN ANALOGUES AND USES THEREOF
20200171122 · 2020-06-04 ·

A compound for use in the treatment or prevention of acute or chronic inflammatory disorders wherein the compound is a compound of Formula 1: or a salt thereof, wherein n is 2-5, and R.sub.1 and R.sub.2 are independently selected from H or C.sub.1-C.sub.4 alkyl, wherein R.sub.1 and R.sub.2 may be joined together to form a C.sub.3-C.sub.5 heteroalkyl ring.

NOVEL PHARMACEUTICAL FORMULATIONS AND THEIR USE IN THE TREATMENT OF PERIODONTAL DISEASE
20200085825 · 2020-03-19 ·

The present invention relates to novel treatments of periodontal disease by administering a suitable formulation of a cyclophilin inhibitor. The present invention further relates to novel pharmaceutical compositions containing said cyclophilin inhibitor compounds.