5317 results about "Stereochemistry" patented technology

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

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).

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 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.

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.

The invention discloses a low-water-solubility medicine crystal as well as a preparation method and application thereof. The compound Z pamoate crystal form I has large characteristic diffraction peaks at one or more positions with diffraction angles 2 theta of 9.9 + / -0.2 degrees, 10.7 + / -0.2 degrees, 12.1 + / -0.2 degrees, 14.9 + / -0.2 degrees, 17.3 + / -0.2 degrees, 19.4 + / -0.2 degrees, 20.7 + / -0.2 degrees and 23.1 + / -0.2 degrees. Compared with an amorphous compound Z pamoate, the crystal provided by the invention has the advantages of good stability, no crystal transformation phenomenon, no obvious increase of related substances and low solubility; the production process is simple, only water is used as a solvent in the whole process, and no organic solvent is used; when the long-acting slow-release anti-Parkinson medicine composition is prepared from the compound Z pamoate crystal form I, the medicine encapsulation efficiency is high, the burst release is low, the composition continuously releases the medicine in vivo for more than 2 weeks, the administration frequency of a patient can be reduced, and the medication compliance is improved.

The present application relates to a crystal form of 4-[3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenethyl]pyridine-2(1H)-one, a preparation method therefor, a composition containing the crystal form and the use thereof in the treatment of phosphodiesterase-related diseases.

Disclosed in the present invention is a novel substituted heterocyclic compound having VAV1 target degradation activity. Specifically disclosed is a compound serving as a VAV1 target degradation agent and having the structure of formula (I), or a pharmaceutically acceptable salt, solvate, hydrate, isotopic substituent or isomer of the compound. The compound can be used for preventing or treating diseases related to VAV1 targets or signaling pathways.

The present invention relates to a process for producing a chiral aromatic amine, said process comprising the steps of: a) providing an aromatic imine, and b) contacting said aromatic imine from step a) with an imine reductase, thereby stereoselectively reducing said aromatic imine to a chiral aromatic amine with said imine reductase; and to novel imine reductases capable of catalytic reactions.

This disclosure relates to bivalent compounds (e.g., bi-functional small molecule compounds), compositions comprising one or more of the bivalent compounds, and to methods of use the bivalent compounds for the treatment of certain disease in a subject in need thereof. The disclosure also relates to methods for identifying such bivalent compounds.

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.