33 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 R1a is a hydrocarbon group which may be substituted or a hydrogen atom, ring Aa is a 6-membered aromatic ring which may be further substituted, ring Ba is a homocyclic or heterocyclic ring which may be further substituted, Wa is an oxygen atom or a sulfur atom, Xa1 and Xa2, 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 Xa1 and Xa2 together may form an oxygen atom, a sulfur atom or NR3a (wherein R3a is a hydrocarbon group which may be substituted or a hydrogen atom), and Ya is C1-6 alkylene which may be substituted or a bond, or a salt or prodrug thereof.

Pharmaceutical compositions are provided for the treatment of steroid-dependent and other diseases. The compositions are solutions for subcutaneous or intramuscular injection, and the active agent is a GnRH antagonist peptide according to general formula (1): Ac-DNal-DCpa-DPal-Ser-Aph(X1)-DAph(X2)-Leu-Lys(iPr)-Pro-DAla-NH2 present at a concentration sufficient to from a gel following administration.

A patch for topical application of an anti-acne formulation has in various embodiments a backing film, a release layer and at least one adhesive polymeric matrix layer located between the backing film and the release layer. The anti-acne formulation is uniformly distributed throughout one or more polymeric matrix layers and has an anti-acne effective amount of at least two agents selected from the group consisting of an anti-microbial, an antiseptic, an anti-irritant, a keratolytic agent, a hormone, a hormone agonist and a hormone antagonist.

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

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

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 provides melanin-concentrating hormone receptor antagonists containing as the active ingredient piperidine derivatives represented by the general formula [I]: [wherein R1 is hydrogen, hydroxyl, lower alkyl, or the like; R2, R3a, R3b, R4a, R4b, R5a, R5b and R6 each stands for hydrogen, halogen, or the like; W1 and W2 each independently stands for —O—, —CH2—, or the like; Y1, Y2, Y3 and Y4 stand for —CH—, —CF—, —N—, or the like; Z stands for lower alkyl, an aliphatic heterocyclic group, or the like; Ar is a mono- or bi-cyclic aliphatic heterocycle or an aromatic heterocycle; and n is an integer of 1 to 8]. The compounds act as antagonist against melanin-concentrating hormone receptor and are useful as drugs for central diseases, circulatory diseases, or metabolic diseases.

Peptides are provided which have improved duration of GnRH antagonistic properties. These antagonists may be used to regulate fertility and to treat steroid-dependent tumors and for other short-term and long-term treatment indications. These antagonists have a derivative of aminoPhe or its equivalent in the 5- or the 5- and 6-positions. This derivative is modified so as to contain a carbamoyl group or heterocycle, including a urea moiety, in its side chain. Decapeptides having the formula:wherein Q2 is Cbm or MeCbm and Xaa10 is D-Ala-ol or Ala-ol are particularly effective and continue to exhibit very substantial suppression of LH secretion at 96 hours following injection.

The invention relates to an LHRH (luteinizing hormone-releasing hormone antagonist) lyophilized powder injection with improved stability. The preparation mainly comprises cetrorelix as an active ingredient, an excipient, a pH regulator, an antioxidant and a local analgesic agent, wherein the addition of the antioxidant can improve the stability of the preparation, and the addition of the local analgesic agent can relieve the pains of patients while having no impact on the active ingredient. The preparation process of the preparation mainly comprises weighing, dissolving, adsorbing pyrogen with activated carbon, filtering, final filtering, subpackaging, vacuum drying, plugging, and covering. The LHRH lyophilized powder injection provided by the invention can control the stimulatory function of an ovary, prevent early release of immature ovarian follicles, and help become pregnant. The LHRH lyophilized powder injection has the advantages of stable quality, definite therapeutic effect, and good patient compliance.

Spiroindoline derivatives, process for their preparation and pharmaceutical compositions thereof, their use for the treatment and / or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and / or prophylaxis of diseases, especially sex-hormone-related diseases in both men and women, in particularly those selected from the group of endometriosis, uterine fibroids, polycystic ovarian disease, hirsutism, precocious puberty, gonadal steroid-dependent neoplasia such as cancers of the prostate, breast and ovary, gonadotrope pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hypertrophy, contraception and infertility (e.g., assisted reproductive therapy such as in vitro fertilization). The present application relates in particular to spiroindoline derivatives as gonadotropin-releasing hormone (GnRH) 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.

GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure:wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, R7 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

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).

The invention relates to an amorphous solid dispersion comprising elagolix sodium and at least one silicon-based inorganic compound and to a process for preparing the same. Furthermore, it relates to a pharmaceutical composition comprising said solid dispersion and one or more additional pharmaceutical acceptable excipient(s), wherein the pharmaceutical composition can be used as a medicament, in particular for the treatment of endometriosis and uterine fibroids.

The invention provides compositions and methods for reducing the volume of menstrual blood loss in a patient, such as a human patient, for instance, that has uterine fibroids, by administration of a gonadotropin-releasing hormone (GnRH) antagonist. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxypheny I]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof.

The present invention is directed to novel 7-heterocyclyl quinoline and thieno[2,3-b]pyridine derivatives of the general formula (I) or (II), wherein all variables are as herein defined, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions associated with gonadotropin releasing hormone (GnRH). The compounds of the invention are antagonists of GnRH, useful in the treatment of the infertility, prostate cancer, benign prostate hyperplasia (BPH) and as contraceptives.