59 results about "Uterine leiomyoma" patented technology

The present invention relates, inter alia, to compounds having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —NC4H8, —NC5H10, —NC4H8O, —CHO, —CH(OH)CH3, —C(O)CH3, —O(CH2)2N(CH3)2, and —O(CH2)2NC5H10; R2 is a member selected from the group consisting of hydrogen, halogen, alkyl, acyl, hydroxy, alkoxy (e.g., methoxy, ethoxy, vinyloxy, ethynyloxy, cyclopropyloxy, etc.), acyloxy (e.g., acetoxy, glycinate, etc.), alkylcarbonate, cypionyloxy, S-alkyl, —SCN, S-acyl and —OC(O)R6, wherein R6 is a functional group including, but not limited to, alkyl (e.g., methyl, ethyl, etc.), alkoxy ester (e.g., —CH2OCH3) and alkoxy (—OCH3); R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of ═O and ═N—OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl.In addition to providing the compounds of Formula I, the present invention provides methods wherein the compounds of Formula I are advantageously used, inter alia, to antagonize endogenous progesterone; to induce menses; to treat endometriosis; to treat dysmenorrhea; to treat endocrine hormone-dependent tumors; to treat meningiomas; to treat uterine leiomyomas; to treat uterine fibroids; to inhibit uterine endometrial proliferation; to induce cervical ripening; to induce labor; and for contraception.

Provided are novel methods and compositions for the diagnosis, prognosis and treatment of leiomyomas, in particular uterine leiomyoma (UL). In addition, methods of identifying anti-tumor agents are described. Furthermore, novel methods and compositions are provided for the treatment of diseases characterized by an aberrant growth of mesenchymal stem cells and their descendants and for the treatment of obesity are disclosed.

A medicament for the preventive and / or therapeutic treatment of allergic diseases and / or endometriosis and / or hysteromyoma which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring Z represents an arene which may have one or more substitutents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above, or a heteroarene which may have one or more substitutents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above.

Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents H, C1-6-alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R2 represents H, C1-6alkyl (optionally substituted by R3), phenyl (optionally substituted by CN), or Het; R3 represents OH, CN, Het, —R4—C1-6alkyl, or CONR5R6; R4 represents —CO2—, or —O—; R5 and R6 independently represent H, C1-6alkyl (optionally substituted by OR7) or C3-8cycloalkyl; R7 represents H or C1-6alkyl; Het represents a five or six membered aromatic heterocyclic group containing (i) from one to four nitrogen heteroatom(s) or (ii) one or two nitrogen heteroatom(s) and one oxygen or one sulphur heteroatom or (iii) one or two oxygen or sulphur heteroatom(s), said heterocyclic group being optionally substituted by one or more groups selected from CN and C1-6 alkyl; R8 represents C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R9 and R10 independently represent H, C1-6alkyl, C1-6alkyloxy, CN, CF3 or halo; may be useful for treating endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.

A method for treating uterine leiomyomas, which includes vaginally accessing the cardinal ligament surrounding at least one uterine artery, and occluding the flow of blood through the least one uterine artery. The blood can be occluded by compression. The artery can be compressed by ligating the cardinal ligament. In addition, at least one uterosacral ligament can be ligated. In addition, the artery can be compressed by, clipping, stapling or clamping the cardinal ligament. The blood can also be occluded by coagulating the at least one artery. Coagulation can be done with a laser or a cauterizing device. A system for treating uterine leiomyomas, which includes vaginally accessing the cardinal ligament surrounding at least one uterine artery using a surgical suture passing device to extend a ligature around the ligament, and affixing a ligature around the cardinal ligament to occlude the flow of blood through at least one uterine artery. Also, a system for treating uterine leiomyomas, which includes vaginally accessing the cardinal ligament surrounding at least one uterine artery, providing an absorbable clip and / or staple, and affixing the clip and / or staple around the ligament to occlude the flow of blood through the at least one uterine artery.

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 provides a medicine for treating tumor and its preparation process, wherein the medicine is prepared from Baoniangsong, cyperus tuber, Chinese dates and fresh ginger through watering and boiling, merging the two filtrates, concentrating, alcohol deposition, cooling down to normal temperature, and seasoning the plaster form article. The medicine can be prepared into electuary, tablet or capsule.

The present invention relates, inter alia, to compounds having the general formula:in which R1, R2, R3, R4 and X are as defined by the present specification. In addition to providing the compounds of Formula I, the present invention provides methods wherein the compounds of Formula I are advantageously used, inter alia, to antagonize endogenous progesterone; to induce menses; to treat endometriosis; to treat dysmenorrhea; to treat endocrine hormone-dependent tumors; to treat meningiomas; to treat uterine leiomyomas; to treat uterine fibroids; to inhibit uterine endometrial proliferation; to induce cervical ripening; to induce labor; and for contraception.

Disclosed is a proprietary Chinese traditional medicine for treating hysteromyoma, process for preparation and quality controlling method, which is prepared from root of red rooted saliva, notoginseng, burred tuber, zedoary, peach kernels, Chinese angelica root, turtle shell, seaweed, eucommia bark, white atractylodes rhizome, barbat skullcap and cassia twig.

The invention belongs to the field of traditional Chinese medicines and discloses a traditional Chinese medicinal composition for treating uterine leiomyoma. The traditional Chinese medicinal composition mainly comprises the following traditional Chinese medicinal components in parts by weight: 10g of rhizoma sparganii, 10g of curcuma zedoary, 10g of root-bark of tree peony, 10g of cassia twig, 10g of peach kernel, 10g of safflower, 15g of rhizoma atractylodis, 15g of nutgrass galingale rhizome, 15g of prepared rhizome of rehmannia, 10-12g of fructus aurantii, 10-12g of red paeony root, 10-12g of eucommia bark and 10-12g of himalayan teasel root. The traditional Chinese medicinal composition has the functions of smoothening qi and activating blood and removing blood stasis and dispersing phlegm, is used for treating uterine fibroid and is low in toxic or side effect and definite in curative effect.

Compounds useful as GnRH receptor antagonists are provided. The present inventors have further examined propane-1,3-dione derivatives and confirmed as a result that a propane-1,3-dione having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene), or a compound which has benzene or thiophene ring substituted with a group derived from 1-hydroxymethyl, shows excellent availability, in addition to its excellent GnRH receptor antagonism, thereby accomplishing the invention. Since the compound of the invention shows excellent availability, in addition to its strong GnRH receptor antagonism, it can be expected that it exerts superior drug effect in the living body, and it is useful for the treatment of sex hormone dependent diseases such as prostate cancer, breast cancer, endometriosis, uterine leiomyoma, benign prostatic hypertrophy and the like. In addition, since the compound of the invention is excellent in metabolic stability in human and also is less in drug interaction, it has more desirable properties as a medicament to be used for the aforementioned diseases.

Compounds useful as GnRH receptor antagonists are provided. The present inventors have further examined propane-1,3-dione derivatives and confirmed as a result that a propane-1,3-dione having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene), or a compound which has benzene or thiophene ring substituted with a group derived from 1-hydroxymethyl, shows excellent availability, in addition to its excellent GnRH receptor antagonism, thereby accomplishing the invention. Since the compound of the invention shows excellent availability, in addition to its strong GnRH receptor antagonism, it can be expected that it exerts superior drug effect in the living body, and it is useful for the treatment of sex hormone dependent diseases such as prostate cancer, breast cancer, endometriosis, uterine leiomyoma, benign prostatic hypertrophy and the like. In addition, since the compound of the invention is excellent in metabolic stability in human and also is less in drug interaction, it has more desirable properties as a medicament to be used for the aforementioned diseases.

The invention discloses a pharmaceutical composition for treating leiomyoma of uterus and an application thereof and relates to the technical field of traditional Chinese medicines. The pharmaceutical composition comprises the following traditional Chinese medicinal materials in parts by weight: 35-42 parts of curcuma zedoary, 20-26 parts of leonurus, 18-25 parts of rhizoma sparganii, 18-25 parts of largehead atractylodes rhizome, 16-20 parts of Chinese angelica, 16-20 parts of root of bidentate achyranthes, 7-10 parts of liquorice and 5-8 parts of peach seed. The pharmaceutical composition disclosed by the invention can obviously improve symptom of myoma of uterus and inhibit growth of the myoma or eliminate the myoma, and can show the superiority of non-surgical treatment.

The present invention relates to a selective estrogen receptor modulator selected from the group consisting of: (I) or a pharmaceutical salt thereof; useful, e.g., for treating endometriosis and uterine leiomyoma.

The invention relates to a gynaecological Chinese medicine with health care effects of invigorating blood circulation, eliminating stasis, relieving pain, and the like, and a preparation method thereof. At present, gynecological diseases are the commonly seen and frequently encountered diseases of women, especially the diseases which are considered native bothers of mass women, such as uncomfortable symptoms of hysteromyoma, oophoritic cyst, and the like, and refractory profuse leucorrhea, abdominal masses, thamuria, astriction, lower abdominal pain, menostaxis, cunt irregular bleeding, lumbago, hypodynamia and the like. With the deterioration of diseases, specific patients are led to irregular bleeding and profuse menstruation resulting in anaemia and even infertility. The gynaecological Chinese medicine is prepared by adopting dozens of Chinese medicines, such as walnut meat, radices paeoniae rubra, fructus forsythia, honeysuckle, curcuma, rhizoma sparganii, saponaria vaccaria, radices curcumae zedoariae, frankincense, myrrh, borneol, and the like, through scientific and reasonable extraction and refining active ingredients in the medicines and utilizing percutaneous absorption technology of the modern medicine according to the method of 'internal diseases treated by external therapy' of the traditional medicine, has the effects of promoting blood circulation to remove meridian obstruction, eliminating stasis, relieving pain, being anti-inflammatory and analgetic, eliminating pathogenic heat from the blood, inducing resuscitation, refreshing clearing away heat to and alleviating pain. The detection of clinical experiments proves that the gynaecological Chinese medicine is easy to consolidate and safe to use, has short treatment period, operate fast, no toxicity or side effects, with simple, convenient and practical technique and remarkable curative effects.

The present invention relates to a selective estrogen receptor modulator of formula I: I; or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and uterine leiomyoma.

A compound of formula (I) wherein one of X and Y is silicon, and the other is carbon or silicon; Z is oxygen, sulphur or —N(R)—, wherein R is hydrogen or alkyl; R1 is hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy or cycloalkyl; and R2 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, -alkyl-cycloalkyl, -alkyl-heterocycloalkyl, -alkyl-aryl or -alkyl-heteroaryl; or a pharmaceutically acceptable salt thereof. The compounds are used in the manufacture of a medicament for the treatment or prevention of a disease or condition associated with GnRH (gonadotropin-releasing hormone), e.g. for the treatment or prevention of progression of cancer (e.g. leukaemia therapy), of a fertility disorder, of HIV infection or AIDS, of Alzheimer's disease of fibrosis, of endometriosis, of uterine fibroids or of uterine leiomyoma.

The invention refers to the use of androgen receptor antagonists for the treatment and / or prevention of fibroids, also known as uterine leiomyoma, leiomyomata. Particularly, the invention refers to the use of an androgen receptor antagonist being any one of the compounds according to the following list: cyproterone acetate, oxendolone, chlormadinone acetate, spironolactone, osaterone acetate, dienogest, flutamide, hydroxyflutamide, nilutamide, bicalutamide, RU 58841, LGD-2226, MDV3100, BMS-641988, BMS-779333, or 4-(3-{[6-(2-hydroxy-2-methylpropoxy)pyridin-3-yl]methyl}-4,4-dimethyl-5-oxo-2-thioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile (thioxoimidazolidine derivative) for the treatment of fibroids.

The invention discloses a medicine for curing hysteromyoma. It uses alga, burred tuber, duchesnea, Chinese sage, liquorice, barbat skullcap, bistort, co donopsis pilosula root as materials. Through extraction, condensing, drying and crash the materials can be produced into extractive powder, then adds in accessories and produces the capsule. The medicine in the invention has functions of pathogen dispersing, stimulating circulation to end stasis, supporting the healthy energy. It can be applied to hysteromyoma, the symptom is the menstrual period is prolongs, and the quantity is overmuch, and so on. The medicine has an excellent effect and it has no toxin and side effects.

A uterine leiomyoma cutting device comprises a plastic bag and a cutting knife, wherein that plastic bag is use for placing uterine leiomyoma therein, and the cutting knife is used for cutting uterineleiomyoma in the plastic bag. Four broaching ropes are arranged around the plastic bag, and a broaching ring is arranged at the end of the broaching rope. The cutting tool comprises a semicircular handle connected with a semicircular groove at one end of the semicircular handle, and a cutting tool is arranged on the semicircular groove. The invention provides a uterine myoma cutting device, whichavoids the use of a uterine myoma electric rotary cutter from the source, avoids the malignant component splashing into the pelvis and abdominal cavity when the uterine myoma sarcoma changes, and improves the safety of the laparoscopic uterine myoma operation.

The present invention relates to a selective estrogen receptor modulator of formula I or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and / or uterine leiomyoma / leiomyomata.

Spiroindoline derivatives, processes for their preparation and pharmaceutical compositions thereof, their use for the treatment of diseases, and their use for the manufacture of medicaments for the treatment of diseases, especially sex-hormone-related diseases in both men and women, in particularly those selected from the group of endometriosis, uterine leiomyoma (fibroids), polycystic ovarian disease, menorrhagia, dysmenorrhea, 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, infertility and 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 present invention provides a composition for external application treatment of hysteromyoma and ovarian cysts, and a preparation method thereof, wherein the composition is mainly prepared from the following raw materials: radix ginseng rubra, large root panax notoginseng, fritillaria cirrhosa, leech, ground beetle, complete centipede, cassiatwig, tuckahoe, tree peony bark, semen persicae, amber, faeces trogopterori, prunella vulgaris, drifting seaweed, licorice root, prepared rheum palmatum, eupolyphaga, gadfly, grub, toxicodendron vernicifluum, semen armeniacae amarum, cynanchum otophyllum, cortex moutan, white gourd seed, and mirabilite. According to the present invention, the traditional Chinese medicine preparations with main effects of blood circulation activating and qi promoting are used to prepare the hysteromyoma, and after the medication, the patient hysteromyoma can be controlled to varying degrees, the hysteromyoma size is reduced, and Menoxenia, waist and abdomen pain, and other symptoms are significantly improved. In addition, the pharmaceutical composition of the present invention provides significant treatment effects on ovarian cysts, and has characteristics of low side effect and low treatment cost.

The present invention discloses a kind of hysteromyoma treating suppository and its preparation process. The hysteromyoma treating suppository is prepared with danozol 10-20 wt%, stearic acid 10-20 wt% and semi-synthetic fatty acid ester 60-80 wt%. The preparation process includes the following steps: heating stearic acid and semi-synthetic fatty acid ester in water bath at 60-90 deg.c; adding danozol after cooling to 40-50 deg.c; preparing in hot smelting process and sealing and packing. The present invention has the beneficial effects of: raised curative effect, reduced toxic side effect on liver of the medicine, less stimulation on stomach, etc.

The present invention relates to a selective estrogen receptor modulators of formula I (I); or a pharmaceutical acid addition salt thereof; and of formula II (II); or a pharmaceutical salt thereof; useful, e.g., for treating endometriosis and / or uterine leiomyoma / leiomyomata.