- Synthesis of α-Helices Having a Positively Charged Random Coil-Block on Either N- or C-Terminal
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To study a charge-induced stabilization of α-helix, α-helical peptides having a positively charged random-coil block on either N- or C-terminal of the helix, and having a strictly defined length, (Ala)20(X)20Phe and (X)20(Ala)20Phe(X=Lys or Orn), were syn
- Takahashi, Sho,Hibino, Takeshi,Sawada, Seiji
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Read Online
- Photocatalytic continuous bromination method
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The invention provides a photocatalytic continuous bromination method. The method comprises the following steps: carrying out a first-stage photocatalytic continuous bromination reaction on a materialcontaining an aromatic substrate with a structural general formula I and a bromination reagent in a first continuous illumination reactor to form a first continuous system; overflowing the obtained first continuous system into a second continuous illumination reactor for a second-stage photocatalytic continuous bromination reaction to form a second continuous system; and purifying the second continuous system, wherein the structural general formula I is shown in the specification, R is selected from any one of carboxyl, ester group, NO2, CN, C1 to C8 alkyl and alkoxy, and R1 is C1 to C8 alkyl; n is 1 or 2; X is N or C, and the bromination reagent is Nbromo succinimide or dibromohydantoin. According to the bromination reagent, the selectivity of a product is improved, so the yield of the product is improved; the photocatalytic continuous bromination reaction of the two stages effectively relieves the reaction heat accumulation, and enhances the yield of the target product.
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Paragraph 0060-0061
(2021/04/03)
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- Preparation method of netarsudil mesylate
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The invention relates to a preparation method of netarsudil mesylate.Netarsudil mesylate is synthesized by utilizing chiral induction, and compared with an existing chiral HPLC method or SFC method, netarsudil mesylate prepared by adopting a chemical synt
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Paragraph 0021
(2021/07/17)
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- Nitroxide derivative of ROCK kinase inhibitor
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The invention provides a small molecular compound of a NO donor. The small molecular compound is characterized in that the small molecular compound is a compound shown represented by structural formula I shown in the description, or a stereoisomer, a geometrical isomer, a tautomer, a racemate, a deuterated isotope derivative, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof; and in the formula I, ring A is a substituted or unsubstituted heteroaromatic ring, X is selected from (CH2)n, n is selected from 0, 1, 2 and 3, R is a substituent group of terminal -O-NO2, R is selected from hydrogen, a hydroxyl group, halogen, an amino group, a cyano group, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group and a substituted or unsubstituted heteroalkyl group, and R and R are respectively and independently selected from hydrogen, a substituted or unsubstituted alkyl group, a substituted or unsubstituted naphthenic base or an amino protecting group, or R and R are connected to form a substituted or unsubstituted cyclic heteroalkyl group. The compound has a high-activity inhibition effect on ROCK kinase.
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Paragraph 0064-0070
(2020/06/17)
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- BIARYL UREA DERIVATIVE OR SALT THEREOF, AND MANUFACTURING AND APPLICATION OF SAME
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The present invention discloses a biaryl urea RORγt inhibitor, and specifically relates to a biaryl urea derivative, as represented by formula I, with an RORγt inhibiting activity, and a preparation process thereof, and a pharmaceutical composition comprising the compound. Further disclosed is use of the compound for treating an RORγt-related disease.
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Paragraph 0173
(2019/05/10)
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- p-bromomethyl phenylacetic acid preparation method
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The present invention provides a p-bromomethyl phenylacetic acid preparation method, which comprises: dissolving p-methyl phenylacetic acid in a high boiling point solvent, wherein the solvent is benzene, chlorobenzene or dichlorobenzene; adding a bromina
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Paragraph 0018; 0019; 0020; 0021
(2017/07/21)
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- Process for the preparation of kinase inhibitors and intermediates thereof
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Described are processes for the synthesis of certain compounds, useful for treating diseases, e.g. eye disease, such as glaucoma and ocular hypertension, in a subject.
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Page/Page column 33;34
(2017/05/31)
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- PROCESS FOR THE PREPARATION OF KINASE INHIBITORS AND INTERMEDIATES THEREOF
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Described are processes for the synthesis of certain compounds, useful for treating diseases, e.g. eye disease, such as glaucoma and ocular hypertension, in a subject.
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Paragraph 00104
(2017/06/12)
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- Preparation method of AR-13324
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The invention relates to a preparation method of AR-13324. According to the invention, a chiral ligand is used for chiral induced synthesis of AR-13324. In comparison with an existing chiral HPLC method or a SFC method, the method of the invention has the
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Paragraph 0055-0058
(2018/03/28)
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- 6-Membered heterocyclic compound and use thereof
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A compound represented by the general formula (I) or a salt thereof: [T represents oxygen atom and the like; V represents CH2 and the like; RO1 to RO4 represent hydrogen atom and the like; A represents a linear alkylene group or linear alkenylene group having 2 to 8 carbon atoms and the like; D represents carboxyl group and the like; X represents ethylene group, trimethylene group and the like; E represents —CH(OH)— group and the like; and W represent —U1—(RW1)(RW2)—U2—U3 group (U1 represents a single bond, an alkylene group having 1 to 4 carbon atoms and the like; RW1 and RW2 represent hydrogen atom and the like; U2 represents a single bond, an alkylene group having 1 to 4 carbon atoms and the like; and U3 represent an alkyl group having 1 to 8 carbon atoms and the like), or a residue of a carbon ring or heterocyclic compound], which can be utilized as an active ingredient of medicaments effective for prophylactic and/or therapeutic treatment of skeletal diseases such as osteoporosis and fracture, glaucoma, ulcerative colitis and the like.
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Page/Page column 218
(2008/06/13)
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- Solid-supported synthesis of highly functionalized tripodal peptides with flexible but preorganized geometry: Towards potential serine protease mimics
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Tripodal scaffold 1 has been used in the synthesis of a representative member of a library of serine protease mimics, possessing three independent functionalized peptide chains on a central core. Each peptide chain contains one residue of the classical ca
- Gea, An,Farcy, Nadia,Roque I Rossell, Nuria,Martins, Jose C.,De Clercq, Pierre J.,Madder, Annemieke
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p. 4135 - 4146
(2007/10/03)
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- PPAR agonists
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PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-c
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- Fluorescent maleimides and uses thereof
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The present invention relates to compounds of formula I provided that R1and R2not simultaneously stand for phenyl, the use thereof in, for example, electroluminescent devices and as void detection compounds.
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- Scavenger assisted combinatorial process for preparing libraries of tertiary amine compounds
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This invention relates to a novel solution phase process for the preparation of tertiary amine combinatorial libraries. These libraries have utility for drug discovery and are used to form wellplate components of novel assay kits.
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- A Novel Receptor for Dicarboxylic Acid Derivatives
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A novel receptor 4 has been prepared, which binds the monopotassium salts of various dicarboxylic acids in chloroform solution, using a combination of hydrogen bonding interactions and an electrostatic association between a carboxylate anion and a crown e
- Flack, Stephen S.,Chaumette, Jean-Louis,Kilburn, Jeremy D.,Langley, G. John,Webster, Michael
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p. 399 - 401
(2007/10/02)
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- Carbacyclin analogs
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Carbacyclin analogs that exhibit platelet aggregation inhibition activity and other biological activites common to structurally related prostacyclins are provided.
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- Antibacterial agents, and 4-thio azetidinone intermediates
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This invention relates to 2-substituted and 2,6-disubstituted penem compounds of the formula STR1 wherein Y is hydrogen, halo or certain organic substituents and X represents certain organic substituents. Also included in the invention are pharmaceutically acceptable salts of the above compounds and derivatives of the above compounds in which the carboxyl group at the 3-position is protected as by an easily removable ester protecting group. The compounds of the present invention are potent antibacterial agents or are of use as intermediates in the preparation of such agents.
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