摘要:
Certain novel compounds having the structural formula where R₂, R₃ and R₄ are each selected from the group consisting of H and OA; A is H or is selected from the group consisting of hydrocarbyl radicals, e.g. lower alkyl radicals, i.e. methyl, ethyl, propyl, etc., or wherein R₅ is selected from the group consisting of hydrocarbyl radicals, e.g. alkyl and aromatic residues; n is 2 or 3; and R₁ is selected from the group consisting of organic radicals having fused aromatic rings, that is, radicals comprising at least two rings that share a pair of carbon atoms or share a carbon and nitrogen atom are useful for inducing a dopaminergic response and reducing the intraocular pressure in a mammal.
摘要:
The present invention relates to compounds which are allenyl amines, more specifically, β-ethenylidene-(substituted)ethanamines, possessing antihypertensive activity. They are prepared by a novel reaction of a protected N,N-bis-(trimethylsilyl)-4-methoxy-2-butynylamine compound with a metallo-organic compound, with subsequent removal of the silyl protecting groups to provide the desired compound.
摘要:
The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.
摘要:
This invention relates to novel compounds with skin lightening properties based on an aromatic hydrazine carboxyimidoamide structure, topical skin lightening compositions comprising the same and a method of skin lightening using the said compositions. In particular, the skin lightening benefit is selected from any one of the group consisting of treating melasma, treating post-inflammatory hyperpigmentation, treating age spots, treating dark spots and treating uneven skin tone. Desired skin colour is a major unmet consumer need around the world and especially in Asia. Consumers particularly desire even skin colour, absence of age spots (solar lentigines), absence of hyperpigmentation and lighter overall skin tone. One solution is to use biological actives that reduce the activity of melanocyte cells in skin. These cells, present in the basal layer of the epidermis, make the dark coloured pigment melanin and export it, in small export vesicles called melanosomes, to the neighbouring keratinocytes. It is well described in the literature that compounds which reduce melanin synthesis when topically applied to the skin will reduce skin darkness over time and can generate a more even skin tone. Tyrosinase is a very popular target for the regulation of melanocyte pigment production. However effective inhibitors of tyrosinase are bedevilled by safety issues causing, for example, melanocyte cell death, permanent depigmentation, irritation and allergic reactions. Often effective inhibitors kill melanocytes (for example hydroquinone) or cause sensitisation reactions. There is therefore a great need for safe and effective inhibitors of skin pigment production that work through an alternative safe mechanism. The inventors have observed that selected compounds of the same generic structure inhibit the production of soluble melanin by B16 mouse melanoma cells without cell toxicity.
摘要:
The invention provides a polymerizable compound represented by formula (I), a polymerizable composition, and a polymer that have a practical low melting point, can be produced at low cost, and can produce an optical film that achieves uniform conversion of polarized light over a wide wavelength band, and an optically anisotropic article. In the formula: Y 1 -Y 6 represent a single bond, -O-, -O-C(=O)-, -C(=O)-O-, or the like; G 1 and G 2 represent a bivalent aliphatic group, or the like, of C1-20; Z 1 and Z 2 represent a C2-10 alkenyl group or the like; A x represents a C2-30 organic group, or the like, having at least one aromatic ring selected from an aromatic hydrocarbon ring and a hetero-aromatic ring; A y represents a hydrogen atom, a C1-6 alkyl group, or a C2-30 organic group, or the like, having at least one aromatic ring selected from an aromatic hydrocarbon ring and a hetero-aromatic ring; A 1 represents a trivalent aromatic group or the like; A 2 and A 3 represent a bivalent aromatic group or the like; Q 1 represents a hydrogen atom, a C1-6 alkyl group, or the like. A x and A y may form a ring together.
摘要:
The present invention relates to compounds of formula I or II, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
摘要:
The present invention provides compounds and compositions that can modulate formation of Toll-like receptor 3 (TLR3) and double-stranded RNA (dsRNA) complex, and methods for using the same. In particular, some aspects of the invention provide compounds of the formula: compositions comprising and methods for using the same, where n, Ar1, Ar2, X1, X2, X3, Z1, and Z2 are those defined herein.