30results about How to "Good pharmacological properties" patented technology

This invention relates to compounds of the formula wherein one of R5, R6 and R7 is and X1, X2, Y1 to Y4, R1 to R13 and m and n are defined in the description, and to all enantiomers and pharmaceutically acceptable salts and / or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and / or prevention of diseases which are modulated by PPARδ and / or PPARα agonists.

The present invention relates to polypeptide compound optimized for subcutaneous administration, exemplified by growth hormone conjugates having a linker providing non-covalent binding to albumin.

The present invention relates to using a versatile synthetic approach to generate a new class of ester, amido, or carbamate prodrugs of highly potent, but systemically too toxic, platinum-acridine anticancer agents. The new hybrids contain a hydroxyl group, which has been masked with a cleavable lipophilic acyl moiety. Both butanoic (butyric) and bulkier 2-propanepentanoic (valproic) esters were introduced to these compounds. The goal of this design was to improve the drug-like properties of the pharmacophore (e. g., log D) without compromising its DNA-mediated cell kill potential. Two distinct pathways by which the target compounds undergo effective ester hydrolysis, the proposed activating step, have been confirmed: platinum-mediated, self-immolative ester cleavage in a low-chloride environment (LC-ESMS, NMR spectroscopy) and enzymatic cleavage by human carboxylesterase-2 (hCES-2) (LC-ESMS). Several of the new compounds show excellent stability, reduced systemic toxicity, and favorable activation profiles while maintaining submicromolar cytotoxicity in various cancers, such as lung adenocarcinoma cell lines (A549, NCI-H1435). The results suggest that the novel dual-mode prodrug concept may have the potential to hasten the preclinical development of platinum-acridines.

The invention discloses a freeze-dried preparation and a preparation method and applications thereof. The mass percentage of triterpenoid saponin in the freeze-dried preparation is 0.004-95%, and themass percentage of a binder in the freeze-dried preparation is 0.01-99%. The freeze-dried preparation is prepared by freeze-drying a pre-blended solution containing the triterpenoid saponin and the binder. When the mass percentage of the triterpenoid saponin in the pre-blended solution is 0.001-50% and the mass percentage of the binder in the pre-blended solution is 0.01-50%, and the mass of the triterpenoid saponin increases along with the increase of the mass of the binder; and when the mass percentage of the triterpenoid saponin in the pre-blended solution is 50-95% and the mass percentageof the binder in the pre-blended solution is 0.01-20%, the mass of the triterpenoid saponin decreases with the increase of the mass of the binder. When used as an oral preparation, a solid beverage ora non-washing skin care product, the freeze-dried preparation has the advantage of quick disintegration.

It is an object of the present invention to provide improved pharmacological properties to molecules which bind to a target with low affinity (hereinafter referred to as a “ligand moiety”) through linkage of such molecules to a metal binding moiety, thereby generating a combination molecule commonly referred to as a “metallodrug” or “metallotherapeutic.” The metal binding domain of metallodrugs typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, resulting in modification of proteins and nucleic acids that are in close proximity due to binding of the ligand moiety to its target.

The present invention relates to bradykinin receptor modulators and pharmaceutical compositions thereof for use as a medicament for modulating collateral blood vessel growth of collateral arteries and / or other blood vessels of pre-existing arterial networks. The bradykinin receptor modulators of arteriogenesis are applicable in the treatment and / or prevention of disorders associated with defective blood flow or blood vessel malformation. A preferred aspect of the invention relates to bradykinin receptor agonists for use as a medicament for the prevention of cardiovascular ischemic disease in a patient at risk thereof. Further, the invention relates to a bradykinin receptor agonist for use in a method for treating a cardiovascular ischemic disease in a patient in need thereof, wherein said cardiovascular ischemic disease is a peripheral limb disease.

It is an object of the present invention to provide improved pharmacological properties to molecules which bind to a target with low affinity (hereinafter referred to as a “ligand moiety”) through linkage of such molecules to a metal binding moiety, thereby generating a combination molecule commonly referred to as a “metallodrug” or “metallotherapeutic.” The metal binding domain of metallodrugs typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, resulting in modification of proteins and nucleic acids that are in close proximity due to binding of the ligand moiety to its target.

The invention discloses a nano-gold miR-885-5p conjugate as well as a preparation method and an application thereof. The conjugate comprises nano-gold particles and double-stranded nucleotide, wherein the double-stranded nucleotide is double-stranded miR-885-5p of which the double strands both have 28 bases, or is double-stranded nucleotide which has a sequence homology of 95%-100% with the double-stranded miR-885-5p and has the same coding function as the double-stranded miR-885-5p, wherein the double-stranded nucleotide comprises two stem-loop structures, and a 5'-terminal of each antisense strand contains hexacarbon alkyl mercaptan and is coupled with the nano-gold particles. The nano-gold miR-885-5p conjugate has a remarkable growth inhibition effect on both liver cancer cells in vitro and liver cancer nude mouse transplanted tumors in vivo, and has a beneficial effect in the application for treating the liver cancer.

The invention discloses a nano-gold miR-375 conjugate, and a preparation method and application thereof. The conjugate comprises nano-gold particles and double-strand nucleotide, wherein two strands of the double-strand nucleotide are double-strand miR-375 with 28 basic groups, or double-strand nucleotide with homology of 95-100 percent and same coding function of the double-strand miR-375 sequence; the double-strand oligonucleotide has two stem-loop structures, and the 5' terminal of an antisense strand has C6 alkyl mercaptan, and is coupled with the nano-gold particles. The nano-gold miR-375 conjugate has a remarkably growth inhibiting effect on in-vitro liver cancer cells and in-vivo transplantation tumor in nude mice with liver cancer, has beneficial effects in liver cancer treatment and application, and can be potentially applied to treatment of tumors of other digestive systems.

A cationic liposome is proportionally prepared from DOPE, DOTMA and cholesterol and can be used to encapsulate the object (adenovirus carrier) to obtain a recombinant human endostatin adenovirus-cationic liposome composition carrying the active antineoplastic genes for suppressing the growth of tumor. Its preparing process is also disclosed.

The invention belongs to the technical field of medicinal chemistry, in particular to N-(3,5-dimethyladamantane-1-yl)-N'-substituted phenylurea compounds as well as preparation methods and application thereof. The compounds have the structure shown in the formula I. The compounds are proved that the compounds can improve the image recognition memory, the working and learning memory, the spatial learning and memory ability of model rats and has good anti-alzheimer effects by the new object discrimination experiments, Y-maze experiments, positioning navigation and space exploration experiments in mats. The formula I is shown in the description.