7 results about "Hormone analog" patented technology

The present invention provides an application of thyroid hormones and its analogues in preparation of drugs for treating alpha-thalassemia, especially in preparation of drugs for regulating expression of zeta-globin gene. During differentiation of K562 cells, thyroid hormone analogue (Triac) can significantly up-regulate the expression of zeta-globin gene (HBZ) by 50 folds or above. The expression of zeta-globin gene (hbae5) can also be up-regulated by 30-70 folds in zebrafish treated with thyroid hormones and thyroid hormones analogues. Therefore, according to the present invention, the expression of zeta-globin gene can be significantly activated by thyroid hormones and its analogues, which may develop new potential therapies for patients with alpha-thalassemia. It provides an economical, safe and effective method for treating alpha-thalassemia and can be widely used.

The present invention provides a preparation method for Resmetirom and an intermediate I thereof. In the method, by means of a continuous process, there is no need to separate the intermediate and perform post-reaction work-up, thereby saving a plurality of procedures and operation time; and the work-up is simple and efficient, and the use of a highly polluting reagent pyridine is avoided. Moreover, by adjusting a material feeding order, the reaction can be promoted and the color of a product can be effectively improved. The entire process is simple to operate and cost-effective, uses a green and environmentally friendly reagent, and is suitable for large-scale industrial production.

Described are lipidated GnRH analogues, wherein the GnRH analogues are lipidated at one or more of amino acid positions, such as amino acid position 1, 5, 6 and / or 8 of a GnRH analogue peptide backbone. Also described are methods of making the lipidated compounds, pharmaceutical compositions comprising the lipidated compounds, and their use in methods of treatment.

The present invention relates to alpha-melanocyte stimulating hormone analogs targeting the melanocortin-1 receptor.

To provide methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs.SOLUTION: A synthesis method comprises (a) contacting R1MgX or R1 Li with a compound of Formula (I) to form a compound of Formula (II), and then converting it to a compound of Formula (III). In the formulas, R1 is isopropyl or isopropenyl, X is halo, and R2 is H or an amine protecting group.SELECTED DRAWING: Figure 1

The conjugation of luteinizing hormone-releasing hormone analogs (LHRHa) to highly potent payloads via spacers (linear or branched) and cleavable peptidic linkers generate peptide drug conjugates (PDCs) with stable triazole, thioether, oxime or amide bonds. The PDCs target tumor cells that express LHRH receptor (LHRH-R) and release their payloads inside the lysosomes. The PDCs may be used in a method for killing or inhibiting the growth of a tumor cell, especially in late state, highly invasive and aggressive stage IV tumors and in reoccurring tumors.

The present technology comprises methods of treating, preventing, reducing, or otherwise ameliorating one or more symptoms or conditions that may benefit from weight gain or a reduction in weight loss. The methods comprise administering a non-naturally occurring melanocortin analog of the present technology to a subject in need thereof. The methods may promote fat gain (e.g., epididymal fat or perirenal fat), increase muscle mass, increase body weight, accelerate weight gain, increase fat mass to lean mass ratio, improve body composition and / or BMI (e.g., for underweight conditions), increase waist circumference, increase cardiac mass, increase brain mass, or any combination thereof, relative to a control.