6993 results about "Stereochemistry" patented technology

Disclosed in the present invention is a novel fused heterocyclic compound having CDK target inhibitory activity. Specifically disclosed are a compound having a structure as shown in formula (I) and serving as a CDK target inhibitor, or a pharmaceutically acceptable salt, solvate, hydrate, isotopic substituent or isomer thereof.

The invention relates to a disubstituted nitrogenous five-membered heteroaryl compound serving as a kinase inhibitor and application of the disubstituted nitrogenous five-membered heteroaryl compound. The chemical structure of the disubstituted nitrogenous five-membered heteroaryl compound disclosed by the invention is shown as a formula A, the compounds of the invention are CHK1 inhibitors. Therefore, the compounds of the present invention can be used for the treatment of cancer. # imgabs0 #

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.

The present disclosure relates generally to GLP-1 agonists and pharmaceutical compositions comprising the same, as well as methods for treating a GLP-1 associated disease, disorder, or condition.

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 invention discloses an acyltransferase mutant and application of the acyltransferase mutant in synthesis of N-acetyl-trans-4-hydroxyproline, and belongs to the technical field of enzyme engineering. The acyltransferase mutant provided by the invention contains 10th and 95th mutations on the basis of a corresponding amino acid sequence, such as a sequence as shown in SEQ ID NO.1, or contains 62nd or 64th mutations while containing the 10th and 95th mutations. Compared with an original enzyme before mutation, the acyltransferase mutant obtained by the invention has higher acyltransferase activity, and the conversion rate of trans-4-hydroxy-L-proline is greatly improved, so that the yield of N-acetyl-trans-4-hydroxy proline is further improved, and the yield of N-acetyl-trans-4-hydroxy proline is improved. After the surfactant and the metal ions are added, the yield of the N-acetyl-trans-4-hydroxyproline synthesized by the mutant D62K / D10V / D95I under the catalysis is up to 18.7 g / L.

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 present disclosure provides crystalline forms, solvates and hydrates of (R)-5-fluoro-2-methyl-1-((R)-5-(pyridin-2-yl)-2,3-dihy dro-lH-indene-2-carbonyl)indoline-6- sulfonamide, and methods of making.

The invention relates to the technical field of preparation methods of polypeptide drugs, and provides a solid-phase preparation method of tirpotide, which comprises the following steps: by taking amino resin as initial resin, sequentially coupling amino acid and small-fragment peptide according to an amino acid sequence of the tirpotide by using a solid-phase synthesis method to synthesize tirpotide resin; and cracking and purifying the tilpotide resin to obtain a pure tilpotide product. Wherein the small fragment peptide is 1-4 tetrapeptide fragment Boc-Tyr (tBu)-Aib-Glu (OtBu)-G1y-OH, 5-6 dipeptide fragment Fmoc-Thr (tBu)-Phe-OH, 7-8 dipeptide fragment Fmoc-Thr (tBu)-Ser (tBu)-OH, 10-11 dipeptide fragment Fmoc-Tyr (tBu)-Ser (tBu)-OH, 12-13 dipeptide fragment Fmoc-Ile-Aib-OH, 17-18 dipeptide fragment Fmoc-Lys (AEEA-AEA-gamma-Glu (alpha-OtBu)-Ecosanoic acid (mon-tBu), 20 side chain peptide Fmoc The coupling agent coupling the amino acid and the small fragment peptide is selected from the group consisting of Oxyma and DIC, TPTU and TMP or COMU and DIEA. The crude product of the tirpotide prepared by the method disclosed by the invention is high in yield and high in purity.

The invention belongs to the technical field of medicines, and particularly relates to a disulfide cyclic peptide compound of a melanocortin receptor agonist based on polypeptide small molecules, and the disulfide cyclic peptide compound has the following structure: R2-R1-c (Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-R3-R4, wherein R2 and R4 are respectively and independently selected from an amino group, an acetyl group or a palmitoyl group; r1 and R3 are independently selected from Ile, Arg, D-Phe, Pro or deletion, R1 and R3 are not deleted at the same time, and when R1 or R3 is deleted, at least one of R2 and R4 is a palmitoyl group. The disulfide cyclopeptide compound provided by the invention has relatively good selectivity on melanocortin receptors (MCR1, MCR3, MCR4 and MCR5).

The invention discloses an alpha, omega-diiodo perfluoroalkane derivative, an alpha, omega-diiodo ethyl perfluoroalkane derivative as well as a preparation method and application of the alpha, omega-diiodo perfluoroalkane derivative and the alpha, omega-diiodo ethyl perfluoroalkane derivative. According to the method, alpha, omega-diiodo perfluoroalkane is taken as a raw material, and the alpha, omega-diiodo perfluoroalkane and ethylene are subjected to free radical addition reaction under the action of an initiator and a solvent to prepare the alpha, omega-diiodo ethyl perfluoroalkane. The alpha, omega-diiodoethyl perfluoroalkane and alkali are subjected to a one-molecule and / or two-molecule hydrogen iodide hydride elimination reaction, and alpha, omega-iodoethyl vinyl perfluoroalkane and / or alpha, omega-divinyl perfluoroalkane are / is generated. The method is simple and convenient to operate, the raw material utilization rate and the target product yield are high, the preparation cost is effectively reduced, and the industrial production requirement is met. The alpha, omega-diiodo perfluoroalkane derivative or alpha, omega-diiodo ethyl perfluoroalkane derivative prepared by the method disclosed by the invention can be used as a vulcanization point monomer for preparing peroxide vulcanized fluororubber, and compared with common rubber, the rubber has more excellent compression deformation performance, strength and medium resistance and has a wide application prospect.

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 present invention relates to novel (3,3-dimethyl-2-oxo-butoxy)phenyl derivatives and (2- aryl-2-oxo-ethoxy]phenyl derivatives and to their application in a process for the preparation of (3,3,3-trifluoro-2-oxo-propoxy)phenyl derivatives and their further transformation into [(2- trifluoromethyl-1,3-dioxolan-2-yl)methoxy]phenyl derivatives and (2-ethoxy-3,3,3-trifluoro- prop-1-enoxy)phenyl derivatives suitable for use, e.g., as active ingredients, which have microbiocidal activity, in particular, fungicidal activity.

Disclosed herein are (6-(4-(trifluoromethyl)pyridin-3-yl)pyridazin-3-yl)octahydrocyclopenta[c]pyrrol-5-amine, (6-(4-(difluoromethyl)pyridin-3-yl)pyridazin-3-yl)octahydrocyclopenta[c]pyrrol-5-amine, and (6-(2-(trifluoromethyl)pyridin-3-yl)pyridazin-3-yl)octahydrocyclopenta[c]pyrrol-5-amine compounds, useful as antagonists of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating disorders using the compounds and compositions.

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 #

The invention discloses a dimeric electron acceptor, which has one of the following structural formula: # imgabs0 #, in which R1 and R2 are respectively and independently selected from C1-C100 alkyl groups; x comprises H, F, Cl, I, NO2 or CN. According to the dimeric electron acceptor, a 3, 4-ethylenedioxythiophene or 3, 4-dimethoxythiophene unit serves as a connecting unit, an alkoxy side chain is connected to an outer side chain, the open-circuit voltage Voc of a solar cell device with the dimeric electron acceptor as an acceptor material can reach 1.02 V, the energy conversion efficiency PCE is 15.1%, and the dimeric electron acceptor is Vocgt reported at present; and the maximum value of PCE in a dimer acceptor system of 1V. The invention also provides a preparation method of the dimer electron acceptor and an organic photovoltaic device containing the dimer electron acceptor.

Provided herein are compounds of formula (I), or pharmaceutically acceptable salts or deuterated forms thereof, wherein ring A, R1, R2, R3, R4, and m are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of formula (I) or pharmaceutically acceptable salt or deuterated form thereof, and methods of using a compound of formula (I) 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.

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.