39 results about "GnRH Antagonist" patented technology

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.

This invention relates to combination therapies for the treatment of breast cancer comprising administering to a subject in need thereof a compound of Formula I or a pharmaceutically acceptable salt thereof and an anti-estrogenic agent (e.g., an aromatase inhibitor, a SERM that is not the SERM of Formula I, a GNRH agonist, a GNRH antagonist, or an estrogen receptor downregulator) and to compositions (e.g., pharmaceutical compositions) comprising a compound of Formula I or a pharmaceutically acceptable salt thereof and an anti-estrogenic agent. This invention also relates to a method of treating the side effects (e.g., vasomotor disturbances, osteoporosis and musculoskeletal complaints) associated with anti-estrogen therapy in a subject treated with one or more anti-estrogenic agents (e.g., an aromatase inhibitor, a SERM that is not the SERM of Formula I, a GNRH agonist, a GNRH antagonist or an estrogen receptor downregulator). The method comprises administering to the subject an effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof.

The invention provides methods and dosing regimens for safely and effectively treating androgen-dependent prostate cancer with a gonadotrophin releasing hormone (GnRH) antagonist without causing a testosterone spike and / or other side effect of GnRH agonist therapy such as a urinary tract infection, or an arthralgia-related or cardiovascular side effect. The present disclosure also provides for methods for treating prostate cancer in a patient with a history of at least one cardiovascular event, wherein administration of degarelix to the subject decreases the likelihood of developing or experiencing an additional cardiovascular event compared to treatment with a gonadotrophin releasing hormone (GnRH) agonist.

The invention relates to methods for treating prostate cancer comprising administration of an anti-CTLA4 antibody, or an antigen-binding portion thereof, particularly a human antibody to human CTLA4, e.g., antibody 3.1.1, 4.1.1, 4.8.1, 4.10.2, 4.13.1, 4.14.3, 6.1.1, ticilimumab (also known as 11.2.1), 11.6.1, 11.7.1, 12.3.1.1, 12.9.1.1, and ipilimumab (also known as MDX-010 and 10D1), in combination with hormonal therapy. Hormonal therapy agents include, inter alia, an anti-androgen (e.g., megestrol, cyproterone, flutamide, nilutamide, and bicalutamide), a GnRH antagonist (e.g., abarelix and histrelin), and a LH-RH agonist (e.g., leuprolide, goserelin, and buserelin). The invention relates to neoadjuvant therapy, adjuvant therapy, therapy for rising PSA, first-line therapy, second-line therapy, and third-line therapy of prostate cancer, whether localized or metastasized.

The invention relates to a system for predicting the number of oocytes obtained during ovarian stimulation of an object receiving a standard GnRH antagonist solution for ovulation induction. The system comprises a data acquisition module used for obtaining data of the anti-mullerian hormone (AMH) level, basal follicle stimulating hormone (FSH) level and antrum follicle count (AFC) of the object and a module used for predicting the number of the oocytes obtained during the ovarian stimulation and calculating the information obtained in the data acquisition module to calculate the number of theoocytes (NROs) obtained by the object.

The present invention relates to compositions comprising a selective androgen receptor modulators (SARM) and a gonadotropin releasing hormone (GnRH) agonist or a GnRH antagonist, and their use, inter-alia for treating hormone-associated conditions in males and females, which arise as a result of androgen decline, suppression or abrogation, or in treating, suppressing, inhibiting or preventing prostate cancer.

The present disclosure relates to pharmaceutical compositions comprising a gonadotropin-releasing hormone (GnRH) antagonist and methods of preparing and using such compositions. The disclosure also relates to methods of facilitating release of a GnRH antagonist from a pharmaceutical composition.

The present invention provides cancer treatment preparations of excellent targetability. The sugar chain-modified liposomes of the present invention, which contain an aromatase inhibitor, anti-androgenic agent, lyase inhibitor, GnRH agonist, GnRH antagonist, anti-angiogenic agent, tyrosine kinase inhibitor, serine-threonine kinase inhibitor, antibody having an anticancer activity, ansamitocin, capecitabine, celmoleukin, docetaxel hydrate, gemcitabine hydrochloride, oxaliplatin, prednisolone, tegafur-uracil mixtures, zinostatin stimalamer or arsenic trioxide may be used as cancer treatment preparations having an excellent targetability.

The present disclosure relates to pharmaceutical compositions comprising a gonadotropin-releasing hormone (GnRH) antagonist and methods of preparing and using such compositions. The disclosure also relates to methods of facilitating release of a GnRH antagonist from a pharmaceutical composition.

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 present invention relates to a method for treating prostate cancer, which comprises administering an anti-CTLA4 antibody, or an antigen-binding portion thereof, especially a human antibody against human CTLA4, such as antibodies 3.1.1, 4.1.1, 4.8.1, 4.10.2 , 4.13.1, 4.14.3, 6.1.1, ticilimumab (also known as 11.2.1), 11.6.1, 11.7.1, 12.3.1.1, 12.9.1.1, and ipilimumab (also known as MDX-101 and 10D1) , in combination with hormone therapy. Hormone therapy agents include, inter alia, antiandrogens (e.g., megestrol, cyproterone, flutamide, nilutamide, and bicalutamide), GnRH antagonists (e.g., ababa Rick and histrelin), and LH-RH agonists (eg, leuprolide, goserelin, and buserelin). The present invention relates to neoadjuvant therapy, adjuvant therapy, treatment of elevated PSA, first-line treatment, second-line treatment and third-line treatment of localized or metastatic prostate cancer.

A method for recognizing and evaluating the presence and function of GnRH receptors on tumor cells originating in the brain and / or nervous system and / or the meninges and / or reactive neuroglia cells and / or primitive neuroectodermal tumor cells and / or on Kaposi sarcoma is provided. Furthermore a method for reducing degenerate GnRH-positive tumor cells and / or for decreasing cellular replication of the above GnRH-positive tumor cells comprising administering to a cell or to a subject a replication decreasing amount of a GnRH agonist and / or GnRH antagonist and / or an erythropoietin agonist, and / or a thrombopoietin agonist, and / or a endothelin antagonist and / or a gonadotropin inhibiting hormone agonist is also provided. Furthermore, a diagnostic kit for detecting GnRH receptors on tumor cells according to the present methods is disclosed.

The invention provides compositions and methods for long term release of Gonadotropin-releasing hormone (GnRH) antagonists, and uses thereof. Specifically, the invention provides polymer compositions and methods for controlled release of GnRH antagonists.

The present disclosure relates to pharmaceutical compositions comprising a gonadotropin-releasing hormone (GnRH) antagonist and methods of preparing and using such compositions. The disclosure also relates to methods of facilitating release of a GnRH antagonist from a pharmaceutical composition.

The present invention relates to the screening, diagnosis, prognostic evaluation, and treatment or prevention of age associated inflammation, chronic inflammation, and inflammatory diseases. In particular, the present invention relates to treating or preventing inflammatory diseases (e.g. rheumatoid arthritis or spondyloarthritis) or patients with inflammatory peripheral GnRH with GnRH antagonists or drugs that lower the effects of GnRH.

A method for recognizing and evaluating the presence and function of GnRH receptors on tumor cells including those originating in the brain and / or nervous system and / or the meninges and / or reactive neuroglia cells and / or primitive neuroectodermal tumor cells and / or on Kaposi sarcoma is provided. Furthermore, a method for reducing degenerate GnRH-positive tumor cells and / or for decreasing cellular replication of the above GnRH-positive tumor cells comprising administering to a cell or to a subject a replication decreasing amount of a GnRH agonist and / or GnRH antagonist and / or an erythropoietin agonist, and / or a thrombopoietin agonist, and / or a endothelin antagonist and / or a gonadotropin inhibiting hormone agonist is also provided. Furthermore, a diagnostic kit for detecting GnRH receptors on tumor cells according to the present methods is disclosed.

A method for reducing the incidence or delaying the onset of diabetes in diabetes-susceptible mammals (e.g., mice, rats, humans) is provided wherein the mammals are treated with a gonadotropin-releasing hormone (GnRH) antagonist. Preferably, the antagonist is administered repeatedly over time by subcutaneous injection. A useful antagonist is Acetyl-beta-[2-Naphthyl]-D-Ala-D-p-Chloro-Phe-beta-[3-Pyridyl]-D-Ala-Ser-Nepsi-[Nicotinoyl]-Lys-Nepsi-[Nicotinoyl]-D-Lys-Leu-Nepsi-[Isopropyl]-Lys-Pro-D-Ala-NH2. Other useful antagonists are Nal-Glu, PPI-149 and acryline.

The invention provides methods and dosing regimens for safely and effectively treating androgen-dependent prostate cancer with a gonadotrophin releasing hormone (GnRH) antagonist without causing a testosterone spike and / or other side effect of GnRH agonist therapy such as a urinary tract infection, or an arthralgia-related or cardiovascular side effect.

A compound of formula (I): wherein either B is absent and A and Z are the same or different and are each hydrogen, halogen, alkyl, hydroxy, alkoxy, —CN, —C(Rc)2OH, —N(Rd)C(═X)Rc, —C(═X)N(Rc)(Rd), —S(O)m—Rc, —N(Rc)(Rd)S(O)2, —S(O)2N(Rc)(Rd), —N(Rc)2, aryl optionally substituted with Ra or —O-aryl optionally substituted with Ra; or B is present and is —(CH2)n—, —C(Rb)2— or —O—, or B taken together with A or Z can be —C═C(Rb)—, —C(Rb)═C—, —CH2—CH(Rb)— or —CH(Rb)—CH2—; D is —O— or —S(O)m′—; E is a bond or is —(CH2)n—, —N(Rd)—, —(CH2)nN(Rd)— or —N(Rd)(CH2)n—; F is —C(═X)—; G is —(CH2)n—, —N(Rd)—, —(CH2)nN(Rd)— or —N(Rd)(CH2)n; J is a bond, —O—, —N(RC)C(═X)—, —C(═X)N(Rc)—, —S(O)m′—, —N(Rc)S(O)m—, —S(O)nN(Rc)—, —N(Rc)— or —N(Rg)(Rh); K is a bond, alkylene, cycloalkylene, cycloalkenylene, arylene, heterocycloalkylene, heterocycloalkylene or heteroarylene; and L is hydrogen or a terminal group; has therapeutic utility.

Methods for treating uterine fibroids, endometriosis, adenomyosis, or heavy menstrual bleeding in a subject, which include administering to the subject from 10 mg to 60 mg per day of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N'-methoxyurea, and from 0.01 mg to 5 mg per day of a hormone replacement medicament. The present disclosure has methods for reducing menstrual bleeding in a subject, reducing bone mineral density loss in a subject caused by administering a GnRH antagonist to the subject, suppressing sex hormones in a subject, reducing vasomotor symptoms or hot flashes in a subject, and reducing symptoms of decreased libido in a subject having uterine fibroids, endometriosis, or adenomyosis. Further provided are methods of maintaining blood glucose profile, maintaining lipid profile, and / or maintaining bone mineral density in a pre-menopausal woman being treated for one or moreconditions or symptoms of endometriosis, adenomyosis, uterine fibroids, or heavy menstrual bleeding; and methods of contraception and treating infertility.

The invention discloses a post-treatment method of a GnRH antagonist. The GnRH antagonist is subjected to concentration treatment by combining a nanofiltration process with a subsequent freeze-dryingprocess. The method can improve the purity and yield of the product, simplify the steps, reduce the cost, obtain a stable product with controllable moisture, acetic acid and optical density, and is more suitable for large-scale industrial production.

The invention relates to 7-methoxy-1H-indole compounds, a preparation method, a pharmaceutical composition and application, and belongs to the technical field of chemical medicine. The 7-methoxyl-1H-indole compound has a structure as shown in formula I: wherein, R 1 Represents a substituted or unsubstituted phenyl or aromatic heterocyclic group, R 2 Represents a substituted or unsubstituted phenyl or aromatic heterocyclic group, R 1 and R 2 Can be the same or different. The 7-methoxyl-1H-indole compounds, pharmaceutically acceptable salts, and pharmaceutical compositions containing these compounds as active ingredients are used as GnRH antagonists for the treatment of sex hormone-related diseases, with less side effects; Patients in need of such treatment or prevention are given therapeutically effective doses of one or more 7-methoxy-1H-indole compounds described in the present invention to achieve the purpose of treatment. The synthesis method of the 7-methoxyl-1H-indole compound has few by-products and high yield.