5550 results about "Stereochemistry" patented technology

The invention relates to compounds of formula (I), a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable salt of the stereoisomer thereof, a prodrug thereof, a deuterated molecule thereof or a PROTAC molecule thereof that selectively inhibit the activity of K-Ras G12D protein, compositions comprising the same, the methods of using the same and related intermediates.

The present invention relates to a bifunctional Kras modulator (K-T or K-L-T) and the use thereof, wherein K represents a targeting group and is a modulator of a Kras protein (target protein), T is a ligand group of an E3 ubiquitin ligase, and L is a divalent linking group that chemically links the targeting group (K) to the ligand group (T). The bifunctional modulator or compound and a composition thereof disclosed in the present invention have pharmacological activity of degrading or inhibiting the target protein, and can be used for treating, inhibiting or preventing Kras-related diseases or disorders.

To provide a compound which is a novel proline derivative, and to provide a pharmaceutical composition comprising the compound for the treatment of, for example, systemic sclerosis (SSc) and non-alcoholic steatohepatitis (NASH).SOLUTION: A pharmaceutical composition comprises, as a cGAS inhibitor, a compound which is a novel proline derivative encompassed by formula (I), or a prodrug, a pharmaceutically acceptable salt, or a stereoisomer of the compound.SELECTED DRAWING: None

The present application relates to a GLP-1 receptor agonist, which is a compound of formula (II) or a pharmaceutically acceptable salt thereof, and a method for treating or preventing a GLP-1 receptor-mediated disease or disorder or regulating a GLP-1 receptor.

The invention provides a solid-liquid combined synthesis method of semeglutide, which belongs to the technical field of semeglutide synthesis, and specifically comprises the following steps: segmenting a main chain of the semeglutide into three shorter polypeptide fragments, namely a fragment 4, a fragment 5 and a fragment 2 at sites 7-14, 15-22 and 23-37, and respectively synthesizing at the same time; performing solid-phase assembly on the fragment 4 and the fragment 5 to form 7-22 peptide fragments, namely a fragment 1, and after the fragment 1 is cut off from the resin, forming NHS ester at a C end; after the fragment 2 is assembled, selectively removing a protecting group A11oc on the Lys26, then connecting with a side chain for fatty acid treatment to form a fragment 3, and cutting off the fragment 3 from the resin; and connecting the NHS ester of the fragment 1 with the fragment 3 in a liquid phase reaction system. The crude semeglutide prepared by the synthetic method is relatively high in yield and purity. The refined semeglutide of which the purity is more than 99.3% and the content of single impurity is less than 0.1% can be obtained at high yield through a conventional purification means.

The invention relates to a vitamin E derivative as well as a carrier compound and application thereof. The vitamin E derivative has a structure as shown in a formula (1) and can be connected and combined with different linkers to obtain a carrier for synthesizing polypeptide, the preparation process is simple, and the obtained carrier is good in solubility, stability and recoverability and can be used for efficiently synthesizing high-purity polypeptide with high yield. # imgabs0 #

This invention provides a tetrahedral antibody comprising a first, second, third, and fourth domain, wherein the first and second domains are Fab or Fc domains; wherein each of the first and second domains comprise a first polypeptide chain comprising a first N-terminus of the domain, and a second polypeptide chain comprising a second N-terminus of the domain; wherein the first N-terminus of the first domain and the first N-terminus of the second domain are joined to each other by a non-peptidyl linkage, which can be a covalent linkage or a non-covalent linkage between first and second dimerizing polypeptides attached to the first N-termini of the first and second domains, respectively; and wherein the third and fourth domains are attached at their respective C-termini to the second N-termini of the first and second domains, respectively, or the N-termini of the first and second dimerizing polypeptides.

The invention discloses a cyclic nonapeptide with repairing and anti-oxidation effects and application of the cyclic nonapeptide, the amino acid sequence of the cyclic nonapeptide is cyclic (arginine-glycine-aspartic acid-serine-arginine-lysine-valine-lysine-serine), the prepared cyclic nonapeptide has the repairing and anti-oxidation effects, and the cyclic nonapeptide has the repairing and anti-oxidation effects. The composition can be applied to preparation of cosmetics with repairing and / or anti-oxidation effects.

The invention discloses a cyclic peptide compound as well as a preparation method and application thereof, belongs to the field of polypeptide synthesis and application, and particularly relates to full-protection peptide resin prepared by solid-phase synthesis. Carrying out cutting and monocyclization on the full-protection peptide resin to obtain monocyclic peptide; the monocyclic peptide is subjected to binary cyclization treatment to obtain a cyclic peptide compound Cyclo (His-Lys-Cys-Gly-His-Lys-Cys-Gly-, and a disulfide bond is in bridge connection with Cysamp; and the binary cyclization is cyclized under the action of iodine methanol and ascorbic acid. The cyclopeptide compound prepared by the invention has the advantages of low toxicity, good stability, good antioxidant effect and good anti-inflammatory effect, and the expression of type I collagen can be improved. Therefore, the invention has the advantages of low toxicity, good stability, good antioxidant effect and good anti-inflammatory effect, and can improve the expression of the type I collagen.

The invention provides a compound of a GLP-1R agonist or modulator with a structure as shown in a formula (I).

Crystalline forms of peptide fragments, methods for their preparation and their use in the preparation of peptides are provided. The crystalline compound of the present invention can be used as an intermediate having improved purity and physical properties for peptide synthesis.

Provided herein are compounds of formulae (I) - (IX), or pharmaceutically acceptable salts or deuterated forms thereof as defined herein. Also provided herein are pharmaceutical compositions comprising a compound of formula (I) - (IX) or pharmaceutically acceptable salt or deuterated form thereof, and methods of using a compound of formula (I) - (IX) or pharmaceutically acceptable salt or deuterated form thereof, e.g., in the treatment of a disease that is treatable by administration of a DPP1 inhibitor.

The invention belongs to the technical field of organic synthesis, and particularly discloses an ammonia aromatic alkene modified near-infrared BODIPY fluorescent probe as well as a preparation method and application thereof.The near-infrared BODIPY fluorescent probe is obtained by adopting 6-(dimethylamino) nicotinic aldehyde to directionally modify the alpha position of BODIPY and constructing an expanded conjugated system through Knoevenagel condensation. Wherein dimethylamino provides a strong electron donating effect, a molecular structure is twisted into a non-planar configuration due to steric hindrance of a pyridine ring, pi-pi accumulation is reduced, and an ACQ effect is inhibited. According to the structural modification strategy, significant red shift of absorption / emission wavelength is realized by expanding a molecular pi-conjugated skeleton, and meanwhile, the stability of the BODIPY core and the quantum yield are effectively enhanced. The probe molecule can specifically recognize the diphenylalanine dipeptide structural unit by utilizing the synergistic coordination effect of the 2-aminopyridine derivative and the BODIPY mother nucleus, so that the selective detection of the Alzheimer's disease biomarker Abeta42 is realized, and a novel optical detection tool is provided for the early molecular diagnosis and targeted therapy of AD (Alzheimer's disease).

The present invention relates to crystalline forms of the compound represented by Structural Formula I, and compositions comprising crystalline forms of the compound represented by Structural Formula I described herein. The crystalline forms of the compound of Structural Formula I and compositions comprising the crystalline forms of the compound of Structural Formula I provided herein, in particular, single crystalline Form A, can be incorporated into pharmaceutical compositions, which can be used to treat various disorders associated with CRM1 activity, including cancer. Also described herein are methods for preparing the compound of Structural Formula I and its single crystalline forms.

The present application provides compounds that may be used as a glucagon-like peptide-1 receptors (GLP-1R) agonist, or pharmaceutically acceptable salts thereof. Also provided are pharmaceutical compositions containing such compounds, or pharmaceutically acceptable salts thereof. Methods of preparing these compounds and compositions, and methods of using these compounds and compositions to treat or prevent a disease or a condition mediated by GLP-1R, are also provided.

To provide a compound which is a novel proline derivative, and to provide a pharmaceutical composition comprising the compound for the treatment of diseases, for example, systemic lupus erythematosus.SOLUTION: A pharmaceutical composition comprises, as a cGAS inhibitor, a compound which is a novel proline derivative of formula (I) (where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and G are as defined in claim 1), or a prodrug, a pharmaceutically acceptable salt, or a stereoisomer of the compound.SELECTED DRAWING: None

The present invention relates to a compound having a structure represented by formula (I) and having GLP-1 receptor agonistic activity; and the use of said compound and a pharmaceutically acceptable salt, stereoisomer, solvate, or hydrate thereof in the preparation of a GLP-1 receptor agonist and in the preparation of a drug for treating and / or preventing metabolic diseases.

The invention provides a novel chiral ferrocene bridged binaphthyl skeleton phosphine ligand and application thereof. The ligand has the advantages of low cost, simplicity in synthesis, air stability and the like. The ligands have good catalytic activity and enantioselectivity in the asymmetric hydrogenation reaction of ketone, and have certain industrial application prospects in the synthesis of pharmaceutical molecules.

The invention relates to a compound, a composition, an organic optoelectronic device, and a display device. The compound is represented by Chemical Formula 1, where X1 and X2 are each independently NRa, O, S, Se, or Te, any one of R1 to R10 is a group represented by Chemical Formula A, the remaining ones of R1 to R10 and Ra are each independently hydrogen, deuterium, a substituted or unsubstituted C1 to C20 alkyl group, a substituted or unsubstituted C6 to C30 aryl group, a substituted or unsubstituted C2 to C30 heterocyclic group, a substituted or unsubstituted amine group, a substituted or unsubstituted silyl group, a cyano group, or a halogen, and R1 to R10 and Ra are each independently present, or adjacent two of R1 to R10 and Ra are linked to form a ring.

The present disclosure relates to compositions including 2,4-bis-{[4-(2-ethyl hexyloxy)-2-hydroxy]-phenyl}-6-(4-methoxyphenyl)-1,3,5-triazine, avobenzone, and additional organic UV filter(s), as well as to methods of making and using such compositions.

The invention relates to the technical field of antibacterial drugs, in particular to an antibacterial peptide which has an amino acid sequence X1KRFKKFFX2KLKKWV-NH2, in which X1 is selected from any one or deletion of amino acids A, C, D, E, F, G, H, K, L, N, M, P, Q, R, S, I, V, W, Y and T; and X2 represents an amino acid having an aromatic side chain or an amino acid having a basic side chain. Aiming at the defects of poor gastrointestinal fluid stability and the like of the antibacterial peptide in the prior art, the invention provides a brand new antibacterial peptide sequence design scheme and a preparation method thereof, and the peptide sequence is subjected to full D-type amino acid or partial D-type amino acid replacement or structure derivation; compared with the prior art, a series of antibacterial peptides with higher antibacterial activity and gastrointestinal fluid stability are obtained, so that the antibacterial peptides have wider application range and higher potential development value.

Provided are an antibacterial peptide and the use thereof. The antibacterial peptide has a structure represented by formula (I), wherein Z1 is selected from tetrapeptides, the tetrapeptides being optionally modified by -OH, -CHO, -COOH, -NH2, -SO3H or -C=O; S1 and S2 are each independently selected from amino acids having the structure of (I); Q1 and Q2 are each independently selected from dipeptides or tripeptides; and n is independently selected from any integer between 1 and 6. (Q2)4-(S2-Q1)2-S1-Z1

The present application provides compounds that may be used as a glucagon-like peptide-1 receptors (GLP-1R) agonist, or pharmaceutically acceptable salts thereof. Also provided are pharmaceutical compositions containing such compounds, or pharmaceutically acceptable salts thereof. Methods of preparing these compounds and compositions, and methods of using these compounds and compositions to treat or prevent a disease or a condition mediated by GLP-1R, are also provided.

The present disclosure relates to compositions including 2,4-bis-{[4-(2-ethyl hexyloxy)-2-hydroxy]-phenyl}-6-(4-methoxyphenyl)-1,3,5-triazine and an antioxidant system, as well as to methods of making and using such compositions.

Compositions for delivering ketone bodies to a subject include one or more beta-hydroxybutyrate salts, one or more acetoacetate salts, beta-hydroxybutyric acid, and optionally acetoacetic acid. The compositions may optionally include one or more ketone body esters, such as one or more beta-hydroxybutyrate esters and / or one or more acetoacetate esters. An example composition contains about 2% to about 98% on a molar basis of the one or more beta-hydroxybutyrate salts and the one or more acetoacetate salts, about 2% to about 98% on a molar basis of the beta-hydroxybutyrate free acid and optionally the acetoacetate free acid, and optionally about 2% to about 98% on a molar basis of one or more ketone body esters.