42 results about "Lhrh antagonist" patented technology

In this invention, a release-delaying system is to be developed for LHRH antagonists, in particular for cetrorelix, which allows the active compound to be released in a controlled manner over several weeks by complexation with suitable biophilic carriers. The acidic polyamino acids polyglutamic acid and polyaspartic acid were selected for complexation with cetrorelix. The cetrorelix polyamino acid complexes are prepared from aqueous solutions by combination of the solutions and precipitation of the complexes, which are subsequently centrifuged off and dried over P2O5 in vacuo. If complexes having a defined composition are to be obtained, lyophilization proves to be a suitable method. The cetrorelix-carboxylic acid complexes were also prepared from the aqueous solutions. In the random liberation system, the acidic polyamino acids poly-Glu and poly-Asp showed good release-delaying properties as a function of the hydrophobicity and the molecular mass of the polyamino acid. In animal experiments, it was possible to confirm the activity of the cetrorelix-polyamino acid complexes as a depot system in principle. It is thus possible by complexation of cetrorelix with polyamino acids to achieve testosterone suppression in male rats over 600 hours. The release of active compound here can be controlled by the nature and the molecular mass of the polymers.

LHRH analogues and LHRH antagonists for use in the treatment or prophylaxis of hormone-dependent cancers, in particular prostate cancer, prostate carcinoma and / or advanced prostate carcinoma, by administering an initial dose of an LHRH analogue over a first period sufficient to effect hormonal castration, then administering a maintenance dose of an LHRH antagonist over a second period, the dose being insufficient to achieve and / or maintain hormonal castration.

The present disclosure provides methods for gene therapy utilizing hematopoietic stem cells, lymphoid progenitor cells, and / or myeloid progenitor cells. The cells are genetically modified to provide a gene that is expressed in these cells and their progeny after differentiation. In one embodiment the cells contain a gene or gene fragment that confers to the cells resistance to HIV infection and / or replication. The cells are administered to a patient in conjunction with treatment to reactivate the patient's thymus. The cells may be autologous, syngeneic, allogeneic or xenogeneic, as tolerance to foreign cells is created in the patient during reactivation of the thymus. In one embodiment the hematopoietic stem cells are CD34+. The patient's thymus is reactivated by disruption of sex steroid mediated signaling to the thymus. In another embodiment, this disruption is created by administration of LHRH agonists, LHRH antagonists, anti-LHRH receptor antibodies, anti-LHRH vaccines or combinations thereof.

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

In this invention, a release-delaying system is to be developed for LHRH antagonists, in particular for cetrorelix, which allows the active compound to be released in a controlled manner over several weeks by complexation with suitable biophilic carriers. The acidic polyamino acids polyglutamic acid and polyaspartic acid were selected for complexation with cetrorelix. The cetrorelix polyamino acid complexes are prepared from aqueous solutions by combination of the solutions and precipitation of the complexes, which are subsequently centrifuged off and dried over P2O5 in vacuo. If complexes having a defined composition are to be obtained, lyophilization proves to be a suitable method. The cetrorelix-carboxylic acid complexes were also prepared from the aqueous solutions. In the random liberation system, the acidic polyamino acids poly-Glu and poly-Asp showed good release-delaying properties as a function of the hydrophobicity and the molecular mass of the polyamino acid. In animal experiments, it was possible to confirm the activity of the cetrorelix-polyamino acid complexes as a depot system in principle. It is thus possible by complexation of cetrorelix with polyamino acids to achieve testosterone suppression in male rats over 600 hours. The release of active compound here can be controlled by the nature and the molecular mass of the polymers.

The present disclosure provides methods for enhancing the response of a patient's immune system to vaccination. This is accomplished by reactivating the thymus. Optionally, hematopoietic stem cells, autologous, syngeneic, allogeneic or xenogeneic, are delivered to increase the speed of regeneration of the patient's immune system. In one embodiment the hematopoietic stem cells are CD34+. The patient's thymus is reactivated by disruption of sex steroid mediated signaling to the thymus. In one embodiment, this disruption is created by administration of LHRH agonists, LHRH antagonists, anti-LHRH receptor antibodies, anti-LHRH vaccines or combinations thereof.

The invention relates to a controlled-release implanting preparation used for injecting an LHRH (luteinizing hormone releasing hormone) antagonist. The invention is characterized in that the LHRH antagonist, namely cetrorelix acetate is loaded into a high polymer material carrier in a certain proportion, and then compressed into an implanting preparation of a certain shape so as to be used for implanting injection, thereby achieving the effect of long-acting controlled release. The controlled-release implanting preparation consists of the cetrorelix acetate with the effective dose for cancer resisting and controlled-release auxiliary materials, and the controlled-release auxiliary materials mainly comprise a biodegradable and biocompatible macromolecule copolymer; and the controlled-release implanting preparation is injected into tumors or around tumors, thereby being favorable for the effective diffusion of the medicament in the solid tumors, selectively improving the local medicament concentration of the tumors, reducing the injection times and the medicament tolerance, enhancing the compliance of patients and facilitating the clinical use and the medication for the patients.

Methods for treating hormone associated conditions, such as endometriosis, uterine leiomata, ovarian cancer, breast cancer, or vaginal bleeding, using LHRH antagonists and selective estrogen receptor modulators are disclosed. The methods include administering to a subject a combination of an LHRH antagonist and a selective estrogen receptor modulator. Pharmaceutical compositions and kits for use in the methods of the invention are also provided.

The invention relates to an injection slow-release micro ball of LHRH antagonist material, wherein its average diameter is 0.5-100 mum, with high package ratio. And it comprises LHRH antagonist material, degradable macromolecule findings, and other acceptable findings. The invention uses emulsion-liquid drying method, single-emulsion-liquid drying method, S / O / O method, atomization drying method, etc. Said micro ball can prolong drug function time, improve utilization of LHRH antagonist material, and reduce side effect.

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.

The invention relates to decapeptide derivative which has LHRH receptor antagonism activity, an effect of inhibiting pituitary to excrete gonadotrophic hormone, an effect of inhibiting the gonad to excrete steroid hormone and has a lower histamine releasing effect, its producing method, the drug combination and its drug applications for treating the sex hormone correlated disease such as prostatecancer and the disease correlated to the anti-histamine or reducing histamine release.

The present invention provides at least one LHRH antagonist for the treatment or prophylaxis of at least one lower urinary tract symptom in mammals which is to be administered in an intermediate dose, which does not cause chemical (hormonal) castration.

The invention belongs to the field of medicine and chemistry and particularly relates to a luteinizing hormone-releasing hormone (LHRH) antagonist derivative which is represented as formula (I), a preparation method of the LHRH antagonist derivative and application for preparation of drugs curing related sex hormone diseases or contraceptives. The invention also relates to a stereoisomeride of the LHRH antagonist derivative which is represented as the formula (I), a solvate of the LHRH antagonist derivative which is represented as the formula (I), or physio-toxicity-free salt of the LHRH antagonist derivative which is represented as the formula (I) and a pharmaceutical composition which contains compounds such as the LHRH antagonist derivative, the stereoisomeride, the solvate or the salt. An LHRH antagonist is modified with a water soluble group and a water soluble vitamin structure, the obtained LHRH antagonist derivative can maintain the activity of original antagonists, has low histamine-releasing activity and is beneficial to the clinic application and the water solubility is increased. The formula (I) is R-D-NAI-D-Cpa-D-Aaa3-Ser-Aaa5-Aaa6-Leu-Aaa8-Pro-D-Ala-B.

The invention relates to a sustained release preparation for injection of LHRH antagonist substances and a preparation method thereof. The sustained release preparation comprises a therapeutic effective dose of an active component in a structure of a formula (I) or pharmaceutically acceptable salts or prodrugs thereof, and oily solvent.

The invention relates to a decapeptide derivative with LHRH receptor antagonism activity and actions of restricting a pituitarium to secrete gonadotrophins and restricting a gonad to secrete steroid hormones, a preparation method thereof, a medicine composition containing the decapeptide derivative and the application of the medicine composition on treating prostatic cancer, endometrial cancer, interrelated sex hormone dependence diseases relative to reproduction, contraception, and the like.

The present disclosure provides methods for inducing tolerance in a recipient to a mismatched graft of an organ, tissue, and / or cells, by disrupting sex steroid signaling in the patient, wherein the bone marrow and other immune cell functionality is improved without, prior to, or concurrently with, thymic regeneration. In some embodiments, sex steroid signaling in the patient, is interrupted or ablated by the administration of LHRH agonists, LHRH antagonists, anti-LHRH receptor antibodies, anti-LHRH vaccines, anti-androgens, anti-estrogens, selective estrogen receptor modulators (SERMs), selective androgen receptor modulators (SARMs), selective progesterone response modulators (SPRMs), ERDs, aromatase inhibitors, or various combinations thereof.

The invention relates to methods of treatment or prophylaxis of physiological and / or pathological conditions with at least one LHRH antagonist, in particular at least one peptidomimetic LHRH antagonistsuch that the at least one LHRH antagonist is administered in a dose, which does not cause chemical (hormonal) castration.

The novel tripeptides Ac-D-2Nal-D-4ClPhe-D-3Pal-OH and Boc-D-2Nal-D-4ClPhe-D-3Pal-OH are intermediates useful in the synthesis of LHRH analogs by coupling with suitable heptapeptides, in particular with the heptapeptides P1-Ser(P2)-NMeTyr(P3)-D-Lys(Nic)-Leu-Lys(iPr, P4)-Pro-D-AlaNH2 and P1-Ser(P2)-NMeTyr(P3)-D-Asn-Leu-Lys(iPr, P4)-Pro-D-AlaNH2.

The present disclosure provides methods for gene therapy utilizing hematopoictic stem cells, lymphoid progenitor cells, and / or myeloid progenitor cells. The cells are genetically modified to provide a gene that is expressed in these cells and their progeny after differentiation. In one embodiment the cells contain a gene or gene fragment that confers to the cells resistance to HIV infection and / or replication. The cells are administered to a patient in conjunction with treatment to reactivate the patient's thymus. The cells may be autologous, syngeneic, allogeneic or xenogeneic, as tolerance to foreign cells is created in the patient during reactivation of the thymus. In one embodiment the hematopoietic stem cells are CD34+. The patient's thymus is reactivated by disruption of sex steroid mediated signaling to the thymus. In another embodiment, this disruption is created by administration of LHRH agonists, LHRH antagonists, anti-LHRH receptor antibodies, anti-LHRH vaccines or combinations thereof.

A method of treating infertility disorders by 1) administering an LH-RH antagonist, preferably Cetrorelix, in amounts to selectively suppress endogenous LH but not FSH secretion and 2) inducing follicle growth by administration of exogenous gonadotropin. The selective suppression OF LH allows FSH secretion to be at natural levelS thereby not affecting individual estrogen development. The LH-RH antagonist can be given as a single or dual subcutaneous dose in the range of 1 mg to 10 mg, preferably 2 mg-6 mg. In multiple dosing-posology, LH-RH antagonist can be administered subcutaneously in an amount in the range of 0.1 to 0.5 mg of LH-RH antagonist / day. LH-RH antagonist is applied starting cycle day 1 to 10, preferably on day 4 to 8, and ovulation can be induced between day 9 and 20 of the menstruation cycle by administering rec. LH, native LH-RH, LH-RH agonist or by HCG. In addition rec. LH, native LH-RH or LH-RH agonist can be given to avoid hyperstimulation syndrome and native LH-RH or a LH-RH agonist can be administered to avoid luteal phase stimulation by neutralizing the negative effects of HCG.

LHRH analogs and LHRH antagonists for use in the treatment or prophylaxis of hormone-dependent cancers, in particular prostate cancer, prostate carcinoma and / or advanced prostate carcinoma, by administering an initial dose of an LHRH analog over a first period sufficient to effect hormonal castration, then administering a maintenance dose of an LHRH antagonist over a second period, the dose being insufficient to achieve and / or maintain hormonal castration.

The present invention relates to decapeptide derivatives with LHRH receptor antagonistic activity, the function of inhibiting pituitary gland secretion of gonadotropin and gonadal secretion of steroid hormones, their preparation method, their pharmaceutical composition and their role in the treatment of prostate cancer and Use for sex hormone dependence-related diseases related to reproduction.

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.

The invention relates to methods of treatment or prophylaxis of physiological and / or pathological conditions with at least one LHRH antagonist, in particular at least one peptidomimetic LHRH antagonist such that the at least one LHRH antagonist is administered in a dose, which does not cause chemical (hormonal) castration.

The invention provides an injection sustained-release preparation containing an LHRH (luteinizing hormone releasing hormone) antagonist substance or a pharmaceutically acceptable salt thereof and a preparation method thereof.

The present invention is directed to a method for essentially complete oxidation of a concentrated liquor containing oxidizable organic matter. Each step of the method is performed under substantially superatmospheric pressure. Initially, the liquor is preheated to a temperature higher than about 10° C. below the boiling point of water at the substantially superatmospheric pressure. A feed formed of the concentrated liquor is then essentially completely oxidized at a temperature of at least 800° C. in the presence of a gas comprising at least sixty percent by volume of oxygen to form a suspension of a hot gas and a molten slag. The molten slag is separated from the hot gas before the slag is dissolved in water to form a brine. The separated hot gas is then cooled to a temperature below 250° C. by quenching with an aqueous liquid. Finally, the aqueous liquid is separated from the hot gas.

Disclosed are 3',3'-N-bisdesmethyl-3',3'-N-bis-substituted-6-O-methyl-11-deoxy-11,12 -cyclic carbamate erythromycin A derivatives of formula (I) which are antagonists of lutenizing hormone-releasing hormone (LHRH). Also disclosed are pharmaceutical compositions comprising the compounds, methods of using the compounds and the process of making the same.