Combination treatment of cancer

FIELD: pharmacology.

SUBSTANCE: proposed: a combination for application as a drug for cancer treatment, containing: (S)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363) or a salt thereof with an androgen receptor signal modulator selected from 4-{3-[4-cyano-3-(trifluoromethyl)-phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl}-2-fluoro-N-methylbenzamide (MDV-3100) and N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)-sulfonyl]-2-hydroxy-2-methylpropanamide (bicalutamide) or a salt thereof, a set of these components for application in cancer treatment (versions).

EFFECT: greater inhibition of tumour growth by combining the said compound against monotherapy of castration-resistant prostate cancer, the combination showed good tolerability.

9 cl, 3 dwg, 1 tbl

 



 

Same patents:

FIELD: chemistry.

SUBSTANCE: present invention relates to biotechnology and provides a α1,6-glucan-containing compound of Helicobacter pylori. The present invention also discloses a conjugate for inducing immune response against H.pylori, which contains said compound conjugated with a carrier protein. The present invention also discloses an immunogenic composition, use of said composition and a method of inducing immune response against H.pylori using said composition. The present invention also discloses immune serum for neutralising H.pylori in mammals, which is obtained by immunising said mammal with an immunogenic composition containing said immunogenic composition. The present invention discloses an antibody which recognises said α1,6-glucan-containing compound of H.pylori, use of said antibody and a method of inducing complement-mediated bacteriolysis of H.pylori strains which express α1,6-glucan using said antibody.

EFFECT: invention improves the effectiveness of immunogenic compositions against Hpylori.

27 cl, 8 dwg, 21 tbl, 11 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to 2-(3-amino-1-(2,4-difluorophenyl)-1H-1,2,4-triazol-5-yl)-N-methyl-4,5-dihydrobenzo[b]thieno[2,3-d]oxepin-8-carboxamide. As well as to a pharmaceutical composition containing the above compound, to the use thereof and a set for treating.

EFFECT: 2-(3-amino-1-(2,4-difluorophenyl)-1H-1,2,4-triazol-5-yl)-N-methyl-4,5-dihydrobenzo[b]thieno[2,3-d]oxepin-8-carboxamide inhibiting PI3 kinase (PI3K).

6 cl, 15 dwg, 1 tbl, 610 ex

FIELD: medicine.

SUBSTANCE: claimed invention relates to the field of biotechnology. Claimed are versions of a humanised anti-CD79b antibody, each of which is characterised by the presence of a light and heavy chain and a set of 6 CDR with a determined amino acid sequence. An epitope of the antibody from 11 amino acids is determined by the Biacore method. Disclosed are: an immunoconjugate of the antibody with a medication or means for inhibiting cell growth, where the antibody is bound with means covalently, and versions of the composition, based on an effective quantity of the immunoconjugate or the antibody, used for inhibiting B-cell proliferation; as well as a method of determining CD79b in a sample with the application of the antibody. Described are: an antibody-coding polynucleotide, as well as an expression vector and an isolated cell, containing the vector for obtaining the antibody. Disclosed are versions of applying the antibody or immunoconjugate for obtaining the medication for inhibiting the growth of CD79b-expressing cells for the treatment of an individual, affected with cancer, for the treatment of proliferative disease or for inhibiting B-cell proliferation.

EFFECT: invention provides novel antibodies, which can find further application in the therapy of proliferative CD79b-associated diseases.

91 cl, 8 tbl, 9 ex, 20 dwg

FIELD: medicine.

SUBSTANCE: invention refers to biotechnology, virology and medicine. The method provides administering a pox virus containing the defect F2L gene into a host body or a cell. What is also described is using this pox virus for producing a drug preparation for treating proliferative diseases or diseases accompanied by osteoclast hyperactivity. The invention can be used in medicine.

EFFECT: what is presented is the method of treating proliferative diseases or diseases accompanied by osteoclast hyperactivity.

28 cl, 10 dwg, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to methods of obtaining heteroaryl compounds, represented by structural formulae (I) or (II): where R1-R4 have values, given in subcl. 1,14 of the formula.

EFFECT: compounds can be used for treatment or prevention of cancer, inflammatory states, immunological states, etc.

29 cl, 20 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel choline salt of 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid, corresponding to formula and to its crystalline form. Crystalline form of salt (A) has characteristic peaks at diffraction angles (2θ(E)) 7.1, 11.5, 19.4, 20.3, 21.5, 22.0, 22.6, 23.5 and 26.2 in diagram of powder diffraction of X-rays, characteristic peaks of values of chemical shifts (δ(ppm)) 155.8, 149.8, 145.3, 118.0, 113.7, 111.6, 110.3, 98.1, 69.8, 58.7, 57.1 and 55.5 in solid-state 13C NMR spectrum and characteristic peaks of values of chemical shifts (δ(ppm)) -131.6, -145, and -151.8 in solid-state 19F NMR spectrum, as well as endothermic peak about 213°C in diagram of differential-thermal analysis.

EFFECT: compound has excellent solubility and stability in storage.

5 cl, 5 dwg, 3 tbl, 8 ex

FIELD: chemistry.

SUBSTANCE: invention relates to biotechnology, specifically to novel hetero-multimeric proteins obtained from modified ubiquitin, and can be used in medicine to treat or diagnose diseases associated with hyperprodution of the extradomain B of fibronectin (ED-B). The protein includes two monomeric ubiquitin links which are differently modified through substitutions of at least 6 amino acids in positions 4, 6, 8, 62, 63, 64, 65 and 66 of SEQ ID NO: 1. In the first monomer link the substitutions include: F4W, K6(H, W or F), Q62N, E64(K, R or H), S65(L, F or W), T66(S or P), and in the second monomer link: K6(T, N, S or Q), L8(Q, T, N or S), Q62(W or F), K63(S, T, N or Q), E64(N, S, T or Q), S65(F or W), T66(E or D).

EFFECT: invention enables to obtain a modified heterodimeric ubiquitin protein, capable of binding with ED-B with high affinity.

28 cl, 18 dwg, 3 tbl, 7 ex

FIELD: chemistry.

SUBSTANCE: invention relates to field of biotechnology, namely to internalisation of therapeutic molecules into cell, and can be applied in medicine. Obtained is composition for delivering molecules of nucleic acids into cells, containing at least one peptide with at least 92% identity to GAAEAAARVYDLGLRRLRQRRRLRRERVRA (SEQ ID NO: 2); IREIMEKFGKQPVSLPARRLKLRGRKRRQR (SEQ ID NO: 3); or YLKVVRKHHRVIAGQFFGHHHTDSFRMLYD (SEQ ID NO: 4), bound to one or several molecules of nucleic acids.

EFFECT: invention makes it possible to increase efficiency of delivery of molecules of nucleic acids into mammalian cell due to peptide, capable of internalisation into mammalian cell with efficiency, constituting at least 200% of efficiency of internalisation of peptide TAT, which has amino acid sequence GRKKRRQRRRPPQ (SEQ ID NO: 1).

8 cl, 16 dwg, 1 tbl, 8 ex

FIELD: chemistry.

SUBSTANCE: invention relates to field of organic chemistry, namely to polymorphs of form 1 and form 2 of (-)trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolon-I-yl)-4-(1H-indol-3-yl)pyrrolidin-2,5-dione. Invention also relates to methods of obtaining said polymorphs and pharmaceutical composition on their basis.

EFFECT: novel polymorphs of (-)trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolon-I-yl)-4-(1H-indol-3-yl)pyrrolidin-2,5-dione are obtained, useful in cancer treatment.

23 cl, 26 dwg, 2 tbl, 27 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to biotechnology and represents an immunogenic composition for preventing and treating cancer diseases, which contains the non-functional BORIS protein, a sequence of which is free from the zinc finger protein. The present invention also discloses an immunotherapeutic cancer composition containing the above non-functional BORIS protein or a bacterial, mammalian or yeast cell, or a viral particle able to express the above non-functional BORIS protein. The present invention also discloses a method for immunising a patient by administering an effective amount of the above immunotherapeutic composition, as well as using the above immunotherapeutic composition for preparing the cancer vaccine.

EFFECT: invention enables increasing the efficacy of the immunoprophylactic and therapeutic cancer vaccine.

22 cl, 7 dwg, 2 tbl, 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel compounds of formula I, possessing ability of binding with delta-opioid receptors. In formula R1 is selected from the group, consisting of i) phenyl, optionally substituted with one-two substituents, independently selected from the group, consisting of C1-4alkyl, C1-4alcoxy, C1-4alkylthio, hydroxyl, di(C1-4alkyl), aminocarbonyl, chlorine and fluorine, in such a way that only one di(C1-4alkyl)aminocarbonyl is present; ii) naphthyl; iii) pyridinyl, optionally substituted with one substituent, selected from the group, consisting of C1-4alkyl, C1-4alcoxy, C1-4alkylthio, hydroxy, fluorine, chlorine and cyano; iv) pyrimidin-5-yl; v) furanyl; vi) thienyl; vii) 5-oxo-4,5-dihydro-[1,2,4]oxodiazol-3-yl; and viii) di(C1-2alkyl)aminocarbonyl; Y represents ethyl, vinyl or bond; or Y represents O, when R1 represents optionally substituted phenyl, where substituent represents C1-4alcoxy; R2 represents phenyl, optionally substituted with one-two substituents, independently selected from the group, consisting of C1-4alkyl, C1-4alcoxy, fluorine, chlorine and cyano, trifluoromethoxy and hydroxy; or R2 represents phenyl, substituted with one aminocarbonyl, di(C1-4alkyl)aminocarbonyl, C1-4alcoxycarbonyl or carboxysubstituent; R3 is selected from the group, consisting of i) 3-aminocyclohexyl; ii) 4-aminocyclohexyl; iii) piperidin-3-yl; iv) piperidin-4-yl; v) pyrrolodin-2-yl-methyl, in which pyrrolodin-2-yl is optionally substituted by 3-rd or 4-th position with one or two fluorine-substituents; vi) azetidin-3-yl; vii) 2-(N-methylamino)ethyl; viii) 3-hydroxy-2-aminopropyl; ix) piperidin-3-yl-methyl; x) 1-azabicyclo[2.2.2]octan-3-yl; and xi) 8-azabicyclo[3.2.1]octan-3-yl; or R3 together with Ra and nitrogen atom, which they both are bound to, form piperazinyl, optionally substituted with 4-C1-4alkyl; Ra represents hydrogen, 2-(N-methylamino)ethyl or C1-2alkyl, optionally substituted with azetidin-3-yl.

EFFECT: compounds can be used in treatment of pain in the range from medium to strong, caused by diseases or conditions, such as osteoarthritis, migraine, burn, fibromyalgia, cystitis, rhenite, neuropathic pain, idiopathic neuralgia, toothache, etc.

21 cl, 4 tbl, 26 ex

FIELD: medicine.

SUBSTANCE: invention represents an agent for preventing and treating prostatitis and prostate adenoma in the form of a capsule, which contains doxazosin, diisopropylammonium dichroloacetate, afobazol, copper glycinate, vitamin E (d-alpha tocopherol acetate), zinc glycinate; L-Glutamine; L-Alanine; L-Arginine and excipients: corn starch and talc.

EFFECT: extended range of products for treating and preventing prostatitis and prostate adenoma.

4 ex, 3 tbl

FIELD: medicine.

SUBSTANCE: method involves a course of 5-7 pulse ultrasonic procedures having an intensity of 0.2-0.4 W/cm2 of 5-7 minutes daily. That is combined with enzyme therapy with Longidaza 3,000 units 2 times a week for 1 month. Besides, Trilon B rectal suppositories 1,000 mg and Dimexidum 200 mg are administered daily for the night for 3 months. The bacteria are detected by a microscopic and microbiologic examination of ejaculate that is followed by a 4-6-week antibacterial therapy by administering an antibacterial preparation taking into account the microflora sensitivity.

EFFECT: such implementation of the method provides removing the prostate stones or decreasing the number thereof, reducing a probability of the inflammatory process in the prostate, ensuring a differentiated therapeutic approach by detecting the group of patients whom the antibacterial therapy is indicated to.

3 cl, 3 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to urology and balneotherapy, and can be used for treating patients with benign prostatic hyperplasia complicated by chronic prostatitis with a dominant symptom of nocturia. That is ensured by performing EHF therapy. The above is combined with an integrated resort treatment: oral administration of carbonate-hydrocarbonate-sulphate sodium-calcium low-mineralised (3.6-3.7 g/l) water in an amount of 280-300 ml three times a day 40-45 minutes before meals. The balneological treatment is prescribed: taking baths with similar mineral water at a temperature of 36-37°C with the exposure of each procedure 15 minutes in the number of 8 procedures every second day. Phytomicroenemas are prescribed in the number of 8 procedures every second day. That is combined with drug therapy with artesine 2 mg/day for 10 days.

EFFECT: method enables the rehabilitation treatment which provides higher adaptation capabilities of the body, reducing the symptoms of the lower urinary tract with the dominant symptom of nocturia from 4-5 to 1-2 urinations a night and improving the quality of life in the patients undergoing the resort therapy It is manifested by the positive improvement of the patients' status as shown by the clinical examination, as well as by IPSS, Q max values.

3 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: present group of inventions refers to medicine, namely to urology, and concerns treating prostatic diseases. That is ensured by administering a therapeutic agent containing an activated-potentiated form of prostate-specific antigen antibody and using the activated-potentiated form of endothelial NO-synthase antibodies as an additional exalting agent.

EFFECT: administering this combined therapeutic agent provides the effective treatment of the prostatic diseases by the synergetic effect of the ingredients consisting in intensifying the antiproliferative, anti-inflammatory effects and improving the functional state of the prostate.

10 cl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, namely to an agent for treating benign prostatic hyperplasia. The antiproliferative agent for treating benign prostatic hyperplasia which contains red deer's antler lipids prepared by extraction of the red deer's antlers in a mixture of the solvents ethanol: ethyl acetate: water in the specific environment.

EFFECT: agent is effective for treating benign prostatic hyperplasia.

2 tbl

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to methods of treating diseases of various aetiologies and injuries of various visceras. Electropunctural pre-examination aims at determining the patient's overall potential and the potential in a point on the body surface at a minimal distance from the viscera to be treated, or in its immediate projection tender zones. A stem cell growth area is stimulated by placing a bee within the sternum. Then, an irritation centre is created using vacuum- or hirudotherapy in a point on the body surface at a minimal distance from the above viscera or in its immediate projection tender zones. The irritation centre is created to be intensive and short-term at the level of the potential in the point below the overall potential, or to be weak and long-term at the level of the potential in a point above the overall potential.

EFFECT: method provides the effective local therapeutic effect on the involved visceral tissues ensured by a combination of the used components of the effect.

2 cl, 3 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to urology, and can be used for treatment of benign hyperplasia of prostate gland. For this purpose dynamic examination of prostate gland is carried out before drug therapy and 3, 6 and 9 months after that. Dynamic examination includes transrectal ultrasound examination (TRUSE) with Dopplerography and sonoelastography (SEG) of prostate gland. Comparison of prostate size values, hyperplasia size, blood flow in capsular and parauretral arteries, blood flow in adenomatous nodes and density of transitory zones of prostate is carried out in SEG. If values of examined parameters by TRUSE data decrease by 15% and more, each parameter is given 1 point. If density of transitory zones of prostate in sonoelastography is higher than 35 KPa, 1 point is given too. As a result if the sum is not less than 4 points, conservative therapy is stopped. If the sum of points is less than 4 points, therapy is continued. Examination is repeated after next 3 months.

EFFECT: method ensures reduction of terms of drug treatment and increase of treatment quality due to possibility of determining indications for complete or partial cancellation of drug treatment within 3-6 months.

1 tbl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: what is presented is using at least one protease for producing a drug preparation for treating and/or preventing benign prostatic hypertrophy/hyperplasia wherein the drug preparation is acceptable for the oral administration with at least one protease being specified in a group consisting of plant and microorganism proteases, and with at least one protease being administered in the amount of 1 to 100 mg/kg of body weight, and a respective pharmaceutical preparation.

EFFECT: what is shown is reducing high vascular endothelial growth factor in patient's blood under the action of a mixture of enzymes that makes it possible to inhibit angiogenic growth factors (VEGF), thereby leading to lower vascularisation, and reducing benign prostatic hypertrophy/hyperplasia, with the enzymatic therapy under the present invention having no effect on the normal VEGF level.

13 cl, 7 dwg

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely urology, and may be used for treating suppurative septic complications of prostate adenoma. For this purpose, with underlying administering antibiotics, ozonised saline solution in the concentration of 3 to 6 mg/l in the amount of 200 to 400 ml is additionally intravenously administered; the therapeutic course is 3-5 injections depending on the patient's state. Besides, ozonised saline solution in the concentration of 5 to 8 mg/l is injected into the bladder in the preoperative preparation period, and from the second postoperative day, saline solution is introduced drop-by-drop in the amount of 400.0 ml daily five times with a two-way flushing system.

EFFECT: method enables reducing the risk of urosepsis, eliminating intoxication and accelerating postoperative wound healing of a BPH bed by anti-inflammatory, detoxification, analgesic action, improved blood rheology and microcirculation, increased local immunity with activated regenerative and reparative processes.

2 tbl, 1 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel choline salt of 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid, corresponding to formula and to its crystalline form. Crystalline form of salt (A) has characteristic peaks at diffraction angles (2θ(E)) 7.1, 11.5, 19.4, 20.3, 21.5, 22.0, 22.6, 23.5 and 26.2 in diagram of powder diffraction of X-rays, characteristic peaks of values of chemical shifts (δ(ppm)) 155.8, 149.8, 145.3, 118.0, 113.7, 111.6, 110.3, 98.1, 69.8, 58.7, 57.1 and 55.5 in solid-state 13C NMR spectrum and characteristic peaks of values of chemical shifts (δ(ppm)) -131.6, -145, and -151.8 in solid-state 19F NMR spectrum, as well as endothermic peak about 213°C in diagram of differential-thermal analysis.

EFFECT: compound has excellent solubility and stability in storage.

5 cl, 5 dwg, 3 tbl, 8 ex

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