32 results about "Hormone Receptor Antagonists" patented technology

There are provided a fused pyrimidine compound having antagonistic activity against luteinizing hormone releasing hormone, and a medicine containing the compound. A luteinizing hormone releasing hormone antagonist containing a compound represented by the formula:

wherein R^1a is a hydrocarbon group which may be substituted or a hydrogen atom,

• • ring A^a is a 6-membered aromatic ring which may be further substituted,
  • ring B^a is a homocyclic or heterocyclic ring which may be further substituted,
  • W^a is an oxygen atom or a sulfur atom,
  • X^a1 and X^a2, which may be identical or different, are each a hydrogen atom, a hydrocarbon group which may be substituted, or a heterocyclic group which may be substituted, or X^a1 and X^a2 together may form an oxygen atom, a sulfur atom or NR^3a (wherein R^3a is a hydrocarbon group which may be substituted or a hydrogen atom), and
  • Y^a is C_1-6 alkylene which may be substituted or a bond, or a salt or prodrug thereof.

An improvement to the method of intrauterine insemination by the administration of luteinizing hormone-releasing hormone antagonists (LHRH antagonists).

One aspect of the present invention is concerned with a method of controlled ovarian hyperstimulation in a mammalian female, said method comprising the co-administration to said female of a substance having follicle stimulating hormone activity (FSH substance) in an amount effective to stimulate multiple follicular development;—gonadotropin releasing hormone (GnRH) antagonist in an amount equivalent to a daily subcutaneous dose of at least 0.5 mg ganirelix to prevent a premature LH-surge; and—a LH substance in an amount effective to prevent or suppress symptoms of luteinising hormone (LH) deficiency resulting from the administration of the GnRH antagonist; followed by administering a meiosis and luteinisation inducing substance (ML substance) in an amount effective to stimulate resumption of meiosis and luteinisation, and wherein the LH substance is not obtained from the urine of human females. Another aspect of the to invention relates to a pharmaceutical kit for use in a method of controlled hyperstimulation, which kit comprises:—at least one parenteral or oral dosage unit containing one or more FSH substances in an amount equivalent to a subcutaneous dose of 50-1500 I.U. FSH;—at least one parenteral dosage unit containing one or more GnRH antagonists in an amount equivalent to a subcutaneous dose of 0.5-25 mg ganirelix;—at least one parenteral dosage unit containing one or more LH substances in an amount equivalent to a subcutaneous dose of 50-3000 I.U. recombinant LH; wherein the LH substance is not obtained from the urine of human females.

This disclosure provides compounds and methods of using those compounds to treat metabolic disorders and hyperproliferative disorders, including administration of the compounds in conjunction with hormone receptor antagonists.

The invention discloses a manufacture method for ultrathin size cocoon filaments, which comprises the steps of: breeding a trimolter variety which can be stably genetic to a newly molted second larva or a newly molted third larva stage according to a normal breeding method; using an antijuvenile hormone antagonist to induce the trimolter variety in the newly molted second larva or newly molted third larva stage into a dimolter; and then carrying out normal mulberry leaf feeding, frame mounting, cocoon drying, cocoon cooking and silk reeling in turn. The manufacture method can obtain the top-grade ultra-thin size cocoon filaments with average size of 0.7 to 0.9 dtex; the thinnest can achieve 0.4dtex. The manufactured cocoon filaments have the advantages of excellent solving, thin size, small size error, good purity, high mightiness, good cohesive force, and the like. Simultaneously the method can effectively shorten the sericiculture period, which has extremely large promoting effects on adjusting the labors and improving the production efficiency of the sericiculture; besides, the method can reduce the disease rate of silkworms, reduce the harm to the production of the silkworms in summer and autumn and is beneficial to improving the safety.

The invention provides methods of treating endometriosis in a patient by administration of a gonadotropin-releasing hormone (GnRH) antagonist, for instance, according to dosing regimens predicated on the patient's level of anti-Müllerian hormone (AMH) or β17-estradiol (E2).

The invention relates to a hormone releasing hormone receptor antagonists and uses thereof. The invention relates to the field of organic chemistry, in particular to a compound or pharmaceutically acceptable salt, isomer, prodrug, polymorphic substance or solvate thereof as well as a preparation method and application of same. The invention provides a compound or a pharmaceutically acceptable salt, an isomer, a prodrug, a polymorphic substance or a solvate thereof. The chemical structural formula of the compound is as shown in formula I in the specification. The compound provided by the invention is used as a GnRHR antagonist in a calcium flow detection experiment, the activity of the compound is equivalent to or better than that of Elagolix, and the compound has better pharmacokinetic characteristics.

This invention relates generally to N-benzylamino cyclic thioureas, pharmaceutical compositions containing them, and their use as antagonists of melanin-concentrating hormone receptor (MCH receptor).