Patent classifications
C07K7/645
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.
SUSPENSIONS OF CYCLOSPORIN A FORM 2
Disclosed herein are methods of formulating cyclosporin A Form 2.
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 comprises from about 70 to about 80 percent by weight of the E-isomer and from about 20 to about 30 percent by weight of the Z-isomer, based on the total weight of the mixture.
Pharmaceutical formulations and their use in the treatment of periodontal disease
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.
Method for improving retroviral transduction and gene editing in hematopoietic stem cells using cyclosporine h (CsH)
Use of cyclosporin H (CsH) or a derivative thereof for increasing the efficiency of transduction of an isolated population of cells by a viral vector and/or increasing the efficiency of gene editing of an isolated population of cells when transduced by a viral vector.
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.
Gene therapy
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.
Crystalline form of compound and uses thereof in medicine
A crystalline form A of the compound having formula (I) and uses thereof in medicine are described. Specifically, it relates to crystalline form A and pharmaceutically compositions thereof. Furthermore, it relates to the uses of crystalline form A disclosed 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 vims (HCV) infection.
PRODRUGS AND COMPOSITIONS FOR OPHTHALMOLOGY APPLICATIONS
The present disclosure is directed to prodrugs, compositions including prodrugs, and methods for administering prodrugs and compositions thereof to a patient, including prodrugs represented by Formula (I):
##STR00001##
wherein: D is a drug moiety; Q is an oxygen atom, a sulfur atom, or a nitrogen atom; X is a chemical bond or
##STR00002##
each of G, G, and G is independently an oxygen atom or a sulfur atom; L is a polyether; T is a hydrogen atom, a hydroxyl group, a thiol group, a boronic acid group, or an amine group; R.sup.1 is selected from the group consisting of a substituted aryl group, unsubstituted aryl group, and a substituted carbonyl group; and each of R.sup.2, R.sup.3, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 is independently a hydrogen atom, a substituted C.sup.1-C.sup.20 alkyl group, or an unsubstituted C.sup.1 -C.sup.20 alkyl group. In at least one embodiment, a composition comprises a compound and a carrier material.
METHOD FOR CONTROLLING IMPURITY OF CYCLOSPORIN A EYE GEL
A method of controlling the impurities in a cyclosporin A eye gel. A high performance liquid chromatography is performed, and chromatographic conditions are as follows: the detection wavelength is 210-230 nm; the column temperature is 60-68? C.; the flow rate is 0.8-1 ml/min; and the mobile phase A is: THF-water-phosphoric acid. The method of controlling impurities solves the problem of excipients interference and separation of many impurities at the same time, it also provides an effective method for the formulation of quality standard of impurities in this kind of preparation.