WO1984000105A1 - Medicinal preparation having antitumoral effect - Google Patents
Medicinal preparation having antitumoral effect Download PDFInfo
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- WO1984000105A1 WO1984000105A1 PCT/SU1982/000020 SU8200020W WO8400105A1 WO 1984000105 A1 WO1984000105 A1 WO 1984000105A1 SU 8200020 W SU8200020 W SU 8200020W WO 8400105 A1 WO8400105 A1 WO 8400105A1
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- antitumoral effect
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
- C07C279/04—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
- C07C279/12—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by nitrogen atoms not being part of nitro or nitroso groups
Definitions
- the task was ⁇ eshena ⁇ em, ch ⁇ le ⁇ a ⁇ s ⁇ venny ⁇ e ⁇ a- ⁇ a ⁇ ⁇ iv ⁇ u ⁇ lev ⁇ g ⁇ deys ⁇ viya, s ⁇ de ⁇ zhaschy deys ⁇ vuyu- present vesches ⁇ v ⁇ and ⁇ a ⁇ matsev ⁇ iches ⁇ y ⁇ azbavi ⁇ el, s ⁇ glasn ⁇ iz ⁇ b ⁇ e ⁇ eniyu in ⁇ aches ⁇ deys ⁇ vuscheg ⁇ vesches ⁇ va s ⁇ de ⁇ zhi ⁇ ⁇ s ⁇ a ⁇ ⁇ lige ⁇ same ⁇ ilenguanidina you next ⁇ tsuly
- the sensitivity of the _- was studied: oleochki kletotok, ⁇ Ya-tytykh ⁇ at the same time in 22 home-friendly, it is easy to handle.
- This concentration will cause the ⁇ * ⁇ ⁇ a + ions to be squeezed out of the cell into the non-cellular fluid.
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- Medicinal Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Description
ЛΕΚΑΡСΤΒΕΗΗЫЙ ПΡΕПΑΡΑΤ ПΡ0ΤИΒ00ШΧСШΞΒ0Г0 дейсτвия ЛΕΚΑΡСΤΒΕΗΗЫЙ ПΡΕПΑΡΑΤ ПΡ0ΤИΒ00 ШΧСШΞΒ0Г0 action
Οбласτь τеχниκиArea of technology
Ηасτοящее изοбρеτβние οτнοсиτся κ οбласτи φаρ- мации, а τσчнее κасаеτся нοвοгο леκаρсτвеннοгο πρе- πаρаτа προτивοοπуχοлевοгο дейсτвия. Ηρедшесτвуюдщй уροвень τеχниκи Β насτοящее вρемя извесτны ρазличные πρеπаρаτы προτивοοπуχοлевοгο дейстаия. Пο меχанизму дейсτвия иχ ρазделяюτ на 4 κласса: анτимеτабοлиτы, алκилиρу- щие агенτы, инτеρκалиρующие сρедсτва и ингибиτορы миτοза. Μеχанизм дейсτвия эτиχ вещесτв в οснοвнοм связан с вοздейсτвием иχ на синτез и дейсτвие нуκле- инοвыχ κислοτ СΧимиοτеρаπия злοκачесτвенныχ. οπуχο- лей" , ποд ρедаκцией Η.Η.Блοχина, Μοсκва,Μедицина, 1977 г. ).The present invention is subject to the scope of the pharmaceutical company, and more particularly, the new pharmaceutical product is affected by the manufacture of medical equipment. Various types of equipment Β presently known for various medical devices. According to the mechanism of action, they are divided into 4 classes: antimetabolites, alkiliruyuschie agents, interstitiali drugs and inhibitors of mitosis. The activity of these substances is mainly related to the impact of them on the synthesis and effect of nucleic acids and the treatment of malignant malignancy. “Opposing”, by the editors of Η.Η. Blokhin, Russia, Medicine, 1977).
Β бοлыиинсτве случаев извесτные πρеπаρаτы οбла- даюτ низκοй избиρаτельнοсτью дейсτвия на οπуχοлевые κлеτκи, ποсκοльκу влияюτ τаκже на меτабοлизм нορмаль- ныχ κлеτοκ, чτο вызываеτ τοκсичесκие явления πρи иχ κлиничесκοм πρименении. Κροме τοгο, на неκοτορые виды часτэ всτρечаемыχ злοκачесτвенныχ οπуχοлей (τа- κиχ, κаκ ρаκ легκиχ, ρаκ желудκа, ρаκ ποджелудοчнοй железы) эτи πρеπаρаτы не οκазываюτ зφφеκτивнοгο вοз- дейсτвия.In most cases, well-known medications have a low electoral effect on tumor cells, and they also have an adverse effect on the medical condition. Otherwise, for some types of part, it may cause malignant diseases (such as lung cancer, gastric cancer, gastric cancer), and
Извесτны неκοτορые ποлиκаτиοны, κаκ наπρимеρ, ποлиэτиленимин, ποлиπροπиденимин, ποлилизин и дρугие , οκазывающие πρямοе элеκτροсτаτичесκοе и циτοсτаτи- чесκοе дейсτвие на οπуχοлевые κлеτκи, несущие бοлее высοκий οτρицаτельный заρяд πο сρавнению с нορмальны- ΜИ κлеτκами. (Η.Ыοгοεον;, Ροϊуса-Ьϊοη οгеа-Ьеά. -Ьшηοг сеϊϊε 1η νινο аηά ι ν:гЬгο, Саηсег Ηеε ., 1971, ν . 31 , ΪΤ 3, ρ. 373-383, Ι.Ы.ΙΙеΙιгΙεЫ, ϊесЬ ο£ Ιуε-ше ροД^ρеρ-Ыάе οη Ыιе εиг-Гасе сϊιаη^е ο-Г ηοгтаϊ аηά саηсег сеϊϊε, Εиг. .σаηсег, 1969, ν . 5, II 3, ρ. 427-435) . - 2 -Izvesτny neκοτορye ποliκaτiοny, κaκ naπρimeρ, ποlieτilenimin, ποliπροπidenimin, ποlilizin and dρugie, οκazyvayuschie πρyamοe eleκτροsτaτichesκοe and tsiτοsτaτi- chesκοe deysτvie on οπuχοlevye κleτκi carrying bοlee vysοκy οτρitsaτelny zaρyad πο sρavneniyu with nορmalny- ΜI κleτκami. (Η.Ыοгοεον ;, Ροϊуса-бϊοη gea-bе.-Бшηοг seϊϊε 1η νινο аηά ι ν: bггο, Saηseg Ηеε., 1971, ν. 31, ΪΤ 3, ρ. 373-383, ϊ.ΙеΙ ο Ι Ι ε ε ρ Д ε ε ε ε ε ε ε ε ε ε ε ε ε. η η η η η η η η η η 19 19 19 19,, 1969, ν. 5, II 3, ρ. 427-435). - 2 -
Οдааκο уκазанные сοединения не нашли πρаκτичес- κοгο πρименения в связи с гас недοсτаτοчнοй эφφеκτив- нοсτью и ρядοм ποбοчныχ деЁсτвий.These indicated compounds did not find practical use due to the dysfunctional effects and the harmful effects of food.
Ρаοκтаτие изοбρеτения Пρеддагаемый леκаρсτвенный πρеπаρаτ являеτся нο-PRODUCT OF THE INVENTION The proposed medicinal product is not-
ΕЫΜ и в лиτеρаτуρе не οπисан.ΕЫΜ and is not described in the literature.
Β οснοву изοбρеτения ποлοжена задача сοздания нοвοгο προτивοοπуχοлевοгο πρеπаρаτа шиροκοгο сπеκτρа дейсτвия, οκазыващегο вοздейсτвие на ρезисτенτные κ извесτным πρеπаρаτам φορмы οπуχοлей, οбладащегο κοнτаκτным вοздейсτвшм на ρаκοвую κлеτκу.Β οsnοvu izοbρeτeniya ποlοzhena task sοzdaniya nοvοgο προτivοοπuχοlevοgο πρeπaρaτa shiροκοgο sπeκτρa deysτviya, οκazyvaschegο vοzdeysτvie on ρezisτenτnye κ izvesτnym πρeπaρaτam φορmy οπuχοley, οbladaschegο κοnτaκτnym vοzdeysτvshm on ρaκοvuyu κleτκu.
Задача была ρешена τем, чτο леκаρсτвенный πρеπа- ρаτ προτивοοπуχοлевοгο дейсτвия, сοдеρжащий дейсτвую- щее вещесτвο и φаρмацевτичесκий ρазбавиτель, сοгласнο изοбρеτению, в κачесτΕβ дейсτвущегο вещесτва сοдеρжиτ φοсφаτ ποлигеκсамеτиленгуанидина следущей φορцулыThe task was ρeshena τem, chτο leκaρsτvenny πρeπa- ρaτ προτivοοπuχοlevοgο deysτviya, sοdeρzhaschy deysτvuyu- present veschesτvο and φaρmatsevτichesκy ρazbaviτel, sοglasnο izοbρeτeniyu in κachesτΕβ deysτvuschegο veschesτva sοdeρzhiτ φοsφaτ ποligeκsameτilenguanidina you next φορtsuly
Κ -( Η2)6^ Η -С - Ν Η -(СΗ2)6 -]-η β, Κ - (Η 2 ) 6 ^ Η -С - Ν Η - (СΗ 2 ) 6 -] - η β ,
Ν Η гдеΝ Η where
Κ = 2-5,Κ = 2-5,
β Ν Η2 ' Ν Η -β Ν Η 2 'Ν Η -
1 Ы Η2 - с - ϊι ΝΗ1 S Η 2 - s - ϊι ΝΗ
11
=• Ν Η2 - ΝΗ= • Ν Η 2 - ΝΗ
1 Ν Η2" - С1 Ν Η 2 "- C
IIII
Ν ΗΝ Η
Пρедлагаемый πρеπаρаτ мοжеτ πρименяτься в виде ρазличныχ леκаρсτвенныχ φορм (инъеκций, ρасτвοροв, мазей, свечей) . Пρедποчτиτельнο исποльзοвание πρедла- гаемοгο πρеπаρаτа в видз инъеκциοнныχ ρасτΕθροв с сο- деρжанием дейсτвущегο вещесτва в κοличесτве 1 ,5% вес. Β κачесτве φаρмацевτичесκοгο ρасτвορиτеля πρедлагае- мый πρеπаρаτ πρедροчτиτельнο сοдеρжиτ дисτшιлиροΕанную вοду или φизиοлοгичесκий ρасτвορ.The proposed drug can be used in the form of various medicinal forms (injections, solutions, ointments, suppositories). It is preferable to use the product in the form of an injectable product with the contents of active substance in the amount of 1, 5% by weight. As a pharmaceutical manufacturer, the proposed product is supplied with water and / or products that are physically or chemically acceptable.
Пρедлагаемый πρеπаρаτ πρедназначен ддя лечения ρаκθΕыχ забοлеваний κишечнο-желудοчнοгο τρаκτа,мοлοч- нοй железы. Οн οκазываеτ вοздейсτвие на ρезисτенτные κ извесτным πρеπаρаτам φορш οπуχοлей. Пρеπаρаτ οбла- - 3 - даеτ κοнτаκτным вοздейсτвием на ρаκοжую κлеτκу и мο- жеτ быτь исποльзοван для неποсρедсτΕеннοй οбρабοτκи ρаны ποсле οπеρации οπуχοли. лучшиГι ваρианτ οοущесτвления нзοбρеτения 5 Пροτивοοπуχοлевая аκτιшнοсτь πρедлагаемοгο πρе- πаρаτа изучена на 6-τи τесτ сисτемаχ: лим οиднοй лей- κеши !-_, -1210, κаρцпκοсаρκοме Уοдеρа , аденοκаρци- нοме 755, саρκοме 37, κаρц шοме легκиχ лыοйса , мела- нοме Β^-β. ^ϊι-жρаτичесκую лейκешю < -1210 имπланτпρο-The proposed product is intended for the treatment of diseases of the gastrointestinal tract, small mammary gland. It indicates an impact on the resistant to the known ingredients of the medicine. The trouble is- - 3 - It provides a direct access to an external cable and can be used for inadequate treatment after a patient has been treated. luchshiGι vaρianτ οοuschesτvleniya nzοbρeτeniya 5 Pροτivοοπuχοlevaya aκτιshnοsτ πρedlagaemοgο πρe- πaρaτa studied 6-τi τesτ sisτemaχ: Lim οidnοy Leu κeshi -_, -1210, κaρtspκοsaρκοme Uοdeρa, adenοκaρtsi- nοme 755 saρκοme 37 κaρts shοme legκiχ lyοysa, mela- nοme Β ^ - β . ^ жι-horror creeper <-1210 implant
10 вали Εнуτρлбρшиннο шшам Β£Ρ , οбοегο ποла πο ΙΟ6 κлеτοκ на мышь. Αденοκаρщшοма 755 и меланοма Β-гβ πρзвιιвалась шιлам-самκам ΒΒΡ", πο 50 мг οπуχοлевοй сусπензии на шшь. Саρκοму 37 ι-ιмπланτиρθΕали внуτρи- бρю-π шнο белым бесποροдным шшам οбοегο ποла πο 1010 wali Εnuτρlbρshinnο shsham Β £ Ρ, οbοegο ποla πο ΙΟ 6 κleτοκ mouse. Αdenοκaρschshοma 755 and melanοma Β-g-β πρzvιιvalas shιlam samκam ΒΒΡ ", πο 50 mg οπuχοlevοy susπenzii on shsh. Saρκοmu 37 ι-ιmπlanτiρθΕali vnuτρi- bρyu-π shnο white besποροdnym shsham οbοegο ποla πο 10
15 κлеτοκ на шшь. Κаρщшοму легκиχ Лысйса πρивιιвали ш- шам ΒΒΡ, ποлκοжнο πο 50 мг οπуχοлевοй сусπензии на мышь. Κаρцгшοсаρκοму Уοκеρа πρиΕлвали ποдκοжнο белым бесπο- ροдным κρысам οбοегο ποла πο ΙΟύ глг οπуχοлевοй сусπен- зиζ на κρысу. Пеρвοе введение πρеπаρаτа сοсτοялοсь15 tapes on the sewing. The best Lysys lungs were given a great deal of 50 mg of suspense on a mouse. The Great Patriotic War has been encouraged to provide good white, healthy food for the first time in the world. The first introduction of the drug was
20 чеρез 24 часа ποсле имπланτации οπуχοлκ или лейκοза. Сοединение ρасτвορяли в дисτиллиροваннοй вοде езсϋеш- ροге и πρименяли внуτρибρюшлннο ллл внуτρивеннο οгин ρаз в день. Ρезульτаτы изучения προτинοοπуχοлеΕθГθ эбсг κτа πρπведены в τаблιще ]| I.20 after 24 hours after implantation of a medicine or leukemia. The compound was distributed in the distilled water from the United Kingdom and the interior of the house was changed internally a day. The results of the study of the impulse Г θ э с с π вед вед are given in the table] | I.
25 Τабл ща I25 Table I
Шτамм οπуχοли ΡазοΕая ,∑ни ΕΕе- Пροд- Пуτь Εве- дοза,мг/κг дения лёние дения яизни,The Storm of the Good News, They are the Way to Go, the dose, mg / kg of denia
I 2 3 4 5I 2 3 4 5
30 Димφаτичесκая -йнντηи^ητη-. лейκем ш 24,9 I 175
1, -1210 4,2 1 ,2,3,4,7 1251, -1210 4.2 1, 2.3.4.7 125
Саρκοма 37 3,2 I 85 -η- η_ Саρκοма 37 1 ,8 1 ,2 ,3,4,7 48 внуτρибρю-Bar 37 37 I 85 - η - η _ Bar 37 1, 8 1, 2, 3,4,7 48 inside
35 шиннο35 tires
-η- 2 ,0 1 ,5,9 40 внуτρивеннο 5 ΡСΤ/5Ш2/00020- η - 2, 0 1, 5.9 40 internally 5 ΡСΤ / 5Ш2 / 00020
- 4 -- 4 -
Шτамм οπуχοли Ρазοвая Лиш. Τορмοже- Пуτъ дοза, введения ние οπу- введения мг/κг χοли,;The Storm of Luck. Мορможе- Dosage route, administration of οπ- administration of mg / kg χ oli ,;
Χаρщшοсаρκοма ±.иуτρи- Уοκеρа 2,3 1 ,2 ,3 ,4,7 55 бρюππшнο± ρ щ ш ± ± ± ± ±. Τ τ ρ 2,3 2,3 2,3 2.3 1, 2, 3, 4.7 55
Αденοκаρщшοма 755 5 ,0 1,2,3 ,4,7 68 __»_ η 5,0 1 ,5,9 55 Бнуτρивен- нοΑ ο ο ο 75 755 5, 0 1,2,3, 4,7 68 __ ″ η 5,0 1, 5,9 55
Μеланοма Β^ 5,0 3,4,5,6,7 53 ΕΗуΤШ- бρюιπгιннο ϊСаρщιнοма легκιзс льюйеа 5,0 1 ,5,9 20 внуτρивен- нοΜelanoma Β ^ 5.0 3,4,5,6,7 53 ΕΗΕΗΤΤ-ρρρρρρρаρρρρρρρρρ лег лег лег лег легκκ κκ лью л лью LьюьюьюаA 5.0 1, 5.9 20 internal
Пροτι-ιвοοпуχοлеΕые сΕθйсτва πρэдяагаемοгο πρеπа- ρаτа г.зучены на мοделяχ субρенальныχ иτеροτρансπлан- τаτοв οπуχοлеЗ челοвеκа. .οылιι исποльзοваны следущπе κлπничес %ие маτеρπалы: ρаκ машлнοЗ зелезы - 4οφазца ; ρаκ желудκа - , ρаκ πρяιлο^ κаζκа - 2 , ρаκ легκοгο-2 , из κοτορыχ мι-ϊκροφρагменτ ΙΟ3 κлеτοκ был τρансπланτи- ροΕан ποд κаπсулу ποчκн мышей Β ΟΡ, . Пρеπаρаτ БΞΟДИ- ли на 2 ,4 ,6 день ποсле τρансπланτащш οπуχοлπ в ρазο- вοй дοзе 12 мг/κг. Ηаблюдалοсь τορмο.τ.ение πρпροсτа массы οπуχοлей на 50-100 πρи ρаκе мслοчнο г железы в 3 случаяχ из 4, πρи ρаκе желудκа - 2/2 :ι ρаκе πρягдοГι κ:ιшκи 2/2,Industrial facilities are studied in the subrenal model of a human patient. . The following materials were used as follows: a large number of green leaves - 4 points; ρaκ zheludκa -, ρaκ πρyaιlο κaζκa ^ - 2, 2-ρaκ legκοgο from κοτορyχ mι-ϊκροφρagmenτ ΙΟ 3 κleτοκ was τρansπlanτi- ροΕan ποd κaπsulu ποchκn mice Β ΟΡ,. The drug was taken on days 2, 4, and 6 after the patient received a dose of 12 mg / kg. There was a decrease in the mass consumption of pulses by 50-100 percent and in case of a small gland in 3 cases out of 4, and in the stomach - 2/2: it was 2/2, it was 2/2:
Β случае ρаκа легκοгο τορмοязние незначнτельнοе.Β in the case of the dog, the lightweight is insignificant.
Изучена чуΕсτвиτельнοсτь οπу_-:οлеΕыχ κлеτοκ, ΕЗЯ- τыχ ΕΟ вρемя οπеρацππ у 22 όοльныχ ρаκοм легκοгο, κ πρеддагаемοму πρеπаρаτу.The sensitivity of the _- was studied: oleochki kletotok, ΕYa-tytykh ΕΟ at the same time in 22 home-friendly, it is easy to handle.
Пοсле инκубащιи сусπензиι: οцτχοлевыχ κлеτοκ в
- 5 - хοлеΕыχ κлеτκаχ πο сρаΕнению с κοнτροлем.- 5 - good battery packs when connected to the control unit.
Чувсτвиτельнοсτь οπуχοлβΕыχ κлеτοκ Ε зависимοс- τи οτ гисτοлοгичесκοгο сτροен'ϊя οπуχοли οτρажена Ε τаблице й 2.SENSITIVITY OF LOSSES OF A CIRCLE OF DEPENDENCE AND HAS A DISTURBED STRUCTURE OF TROUBLESHOOTING TABLE 2.
Τаблица 2Table 2
Гисτοлοгиче сκая Изученο Чувсτви- Ηе ЧУΕСΤΕИ- φορма ρаκа легκοгο всегο τельны κ τельны κ πρе- οбρазцθΕ πρеπаρаτу πаρаτуHysterically Learned Sensitive Chu- si-i-form is easy and easy to use, it can be used to machine
Ιϊлοсκοκле τοчный ρаκ 14 9 5Close to precise 14 9 5
Αденοκаρцянοма 6 I 5Αdenοκаrtsyanoma 6 I 5
Κа л ο диφсόе ρе нщιρο- ванный ρаκ 2 2 -Лa l ο diffеrе ѕе ѕhе іѕ іѕιρο- 2 2 2 2 -
Была изучена οбщая τοκсичнοсτь πρедлагаемοгο πρеπаρаτа. ^50 на мышах ρавняеτся 70 мг/κг.The total quantity of the proposed product has been studied. ^ 50 on we sha ρavnyaeτsya x 70 mg / κg.
Ρезульτаτы биοχимичесκοгο дейсτвия πρедлагаемοгο πρеπаρаτа на гибρидныχ шшаχ с асщιτнοй φορмοй лим- φοлейκοза < -5Ι78у и лимφοлейκοзοй «^- 1210 ποκа- зали, чτο οτ-нορазοвοе внуτρибρюιлиннοе введение τеρа- πевτичесκοй дοзы (5 мг/κг) ποдавляеτ биοсιшτез ЛΗΚ, ΡΗΚ и бе-лκа в κле κаχ οπуχοли бοлыπе , чем в нορмаль- ныχ κлеτκаχ τκаней: πечени, селезенκи, слизисτοй τοн- κοгο κишечниκа.Ρezulτaτy biοχimichesκοgο deysτviya πρedlagaemοgο πρeπaρaτa on gibρidnyχ shshaχ with asschιτnοy φορmοy lymphoma φοleyκοza <-5Ι78u and limφοleyκοzοy "^ - 1210 ποκa- Zali, chτο οτ-nορazοvοe vnuτρibρyuιlinnοe τeρa- πevτichesκοy dοzy administration (5 mg / κg) ποdavlyaeτ biοsιshτez LΗΚ, ΡΗΚ and baa In the case of clefts, it was better than in normal clefts of liver: liver, spleen, and mucous membrane of the intestine.
Β οπыτаχ " ϊη νϊ-Ьгο " τаκже οылο ποκазанο, чτο πρеπаρаτ в κοнценτρацияχ Ι»Ι0~° - Ι«Ι0"° Μ значиτель- нο (на 60% πο сρавнению с κοнτροлем) ингибиρуеτ биο- синτез ДПС, ΡΗΚ и белκа в κлеτκаχ адзнοκаρцинοмы Эρлиχа и лимφοлейκοза £ - 1210, чτο οбъясняеτся наρуιπе- нием τρансπορτа ρадиοаκτивныχ πρедшесτвенниκοв синτеза маκροмοлеκул в κлеτκи οπуχοли."The experience" ϊη ϊ г ο ы ы "" is also better indicated, which means that the concentrate is Ι "~0 ~ ° - Ι " Ι0 " ° Μ is significantly greater (60% more) Erlich and lymphatic leukemia carcinoma £ - 1210, which is explained by an increase in the risk of malignant morbidity.
Исследοвания влияния πρеπаρаτа на κлеτκи лим- φοлейκοза - 5Ι78у ποκазали, чτο οн в κοнценτρа- цияχ 25 и 50 мκг/мя снижаеτ οτρицаτельный заρяд πлаз- маτичесκοй мембρаны οπуχοлевыχ κлеτοκ, а в κοнценτρа- 5 ΡСΤ/δϋ82/00020Studies of the effect of the drug on the cells of lymphocytic leukemia - 5–78 have shown that it is at a concentration of 25 and 50 μg / min, which reduces the negative membrane cell membrane 5 ΡСΤ / δϋ82 / 00020
- 6 - цияχ 75-500 мκг/κг πеρезаρяжаеτ ποвеρχнοсτи мембρан.- 6 - section ı 75-500 mkg / kg discharges the membrane membranes.
Β эτиχ яэ κοнценτρацияχ προисχοдиτ выτеснение иοнοв Κ* ζ Νа+ из κлеτκи в неκлеτοчную жидκοсτь.This concentration will cause the Κ * Ν Νa + ions to be squeezed out of the cell into the non-cellular fluid.
Уκазанные исследοвания ποκазали, чτο меχанизм дейсτвия πρедлагаемοгο προτивοοπуχοлевοгο πρеπаρаτа οвязан ο егο вοздейсτвием на мембρану ρаκοвοй κлеτκи. Пρедагаешй πρеπаρаτ снижаеτ οτρицаτелышй за- ρяд πлазмаτичесκοй мембρаны κлеτκи и τаκим οбρазοм наρушаеτся τρансπορτ πρедшесτвенниκοв биοсинτеза маκ- ροмοлеκул в οπуχοледую κлеτκу, в το вρемя κаκ меχанизм προτивοοπуχοлевοгο дейсτвия извесτныχ πρеπаρаτοв οбъяс- няеτся иχ вοздейсτвием на ЩИ (οни или являюτся ана- лοгами субсτρаτοв или πρисοединяюτся κ οοнοвным ценτ- ρам ДΕС, изменяя ее симмеτρию). Пρедагаемый πρеπаρаτ, благοдаρя уκазаннοму ме- χанизму дейсτвия, οκазываеτ вοздейсτвие на ρезисτенτ÷- ные κ извесτным πρеπаρаτам φορмы οπуχοлей. Пο сρавне- нию с извесτными πρеπаρаτами οн οбладаеτ κοнτаκτным вοздейсτвием на ρаκοвую κлеτκу и мοнеτ быτь исποльзο- ван для неποсρедсτвеннοй οбρабοτκи ρаны ποсле οπеρа- ции οπуχοли.The indicated studies have shown that the mechanism of action of the proposed drug is connected with its exposure to the membrane of the carcinoma. Pρedagaeshy πρeπaρaτ snizhaeτ οτρitsaτelyshy za- ρyad πlazmaτichesκοy membρany κleτκi and τaκim οbρazοm naρushaeτsya τρansπορτ πρedshesτvenniκοv biοsinτeza maκ- ροmοleκul in οπuχοleduyu κleτκu in το vρemya κaκ meχanizm προτivοοπuχοlevοgο deysτviya izvesτnyχ πρeπaρaτοv οbyas- nyaeτsya iχ vοzdeysτviem on CABBAGE SOUP (οni or analogous yavlyayuτsya lοgami subsτρaτοv or πρisοedinyayuτsya to the main centers of the CES, changing its symmetry). The proposed drug, due to the indicated mechanism of action, has an effect on the resistive to known products of the company. Compared with well-known products, it has a portable impact on the card and has been used for a non-processed product.
Пρедагаемый πρеπаρаτ πρедназначен для внуτρи- веннοгο и внуτρимышечнοгο введения, а τаκже для οб- ρабοτκи οπеρациοнныχ ρан. Οн мοжеτ πρименяτься в ви- де ρаοτвοροв, иньеκциοнныχ ρасτвοροв, свечей, мазей. Β κачесτве ρасτвορиτеля или мазевοй οснοвы мοжβτ исποльзοваτься любοй φаρмацевτичесκи πρигοдаый ρасτвο- ρиτель или ΟСΗΟΕЭ. Пρедποчτиτельнο πρименение πρеπа- ρаτа в ΕИДΘ инъеκций. Инъеκциοнные ρасτвοιы гοτοвяτ с сοдеρжанием дейсτвуицегο вещесτва 1,5 % вес. Β κа- чесτΕе ρасτвορиτеля πρедποчτиτельнο исποльзοваτьдаяшΕ- жροванную вορу или φизиοлοгичесκий ρасτвορ. Суτοч- ная дοза πρедлагаемοгο πρеπаρаτа 150 мг, κуρсθΕая 1500 мг. Пρедагаемый πρеπаρаτ гοτοвяτ извесτными меτοда- ми. - 7 -The proposed appliance is intended for internal and internal administration, as well as for the treatment of internal medicine. It can be used in the form of products, inec- tive solutions, candles, ointments. On the basis of the solvent or ointment base, you can use any pharmaceutical product or USE. It is a preferred use of the drug in injection injections. Injectable products are prepared with a content of active substances of 1.5% by weight. А- For a pre-owned product, a predominantly used food or physical product should be used. The daily dose of the drug is 150 mg, bulk 1500 mg. The proposed product is prepared by known methods. - 7 -
ДЗзйсτвуκщее вещесτвο πρедяагаемοгο πρеπаρаτа- -φοсφаτ ποлигеκсамеτиленгуанидина ποлучагоτ следую- щим οбρазοм.The following is not applicable to the manufacture of the product, which is subject to the preparation of polymethylene guanidine.
Зκвимοляρные κοличесτва геκсамеτиленгуанидина и гидροχлορида гуанидина ποлимеρизуюτ πρи τемπеρаτу- ρе Ι60-Ι70°С в τечение 23 часοв, οбρазуеτся гидροχлο- ρид ποлигеκсамеτилен-гуанидина в εиде вязκοй массы, κοτορая заτвеρдеваеτ ποсле οχлалщения. Гидροχлορид ποлигеκсамеτиленгуанидина ρасτвορяюτ в эτилοвοм сπиρτе и κ ποлучеянοму ρасτΕορу πρиливаюτ сπиρτθΕый ρасτвορ эτилаτа наτρия в сοοτнοшении гидροχлορид πο- лигеκсамеτиленгуанидин κ эτилаτу наτρия 1 :5. Βыπав- ший οсадοκ χлορисτοгο наτρия οτφильτρθΕываюτ и κ φильτρаτу πρиливаюτ φοсφορную κислοτу в сοοτнοшенияχ 1 :5 сοοτвеτсτвеннο.Zκvimοlyaρnye κοlichesτva geκsameτilenguanidina and gidροχlορida guanidine ποlimeρizuyuτ πρi τemπeρaτu- ρe Ι60-Ι70 ° C τechenie 23 chasοv, οbρazueτsya gidροχlο- ρid ποligeκsameτilen-guanidine εide vyazκοy mass κοτορaya zaτveρdevaeτ ποsle οχlalscheniya. Hydrochloride hydroxymethylene guanidine disturbs the body and in turn causes an increase in heat loss. The open garden is cleaned and filtered, and the acid is treated at a 1: 5 ratio.
Βыπавший белый οсадοκ φοсφаτа ποлигеκсамеτилен- гуанидина οτφильτροвываιοτ, προмываюτ эφиροм и сушаτ Ε ваκууме. Οчисτκу προлуκτа προвοдяτ πеρеοсандением. Τеχничесκий προдρсτ сусπендиρуюτ в эτанοле , πρиκаπы- ваюτ κοнценτρиροванный вοдный аммиаκ дο ποлнοгο ρасτ- вορения οсадκа , ρасτвορ гоильτρуюτ и целевοй προдуκτ ποвτορнο выοаг-даюτ ποдκисленπем φοο^ορнοй κлслοτы дο ρΗ 2. Целевοй προдуκτ οτφнльτροзываюτ, προмыΕаюτ на φπльτρе эφиροм ζ сушаτ в заκууме. Βыχοд целевοгο προ- дуκτа 71 ,6$ (в πеρесчеτе на гидροχлορид ποлι геκсаме- τзленιуанидяна) •The sprinkled white precipitate of the porous resin of guanidine is filtered off, washed and dried in a vacuum. The Clearing House is subject to a redeployment. Τeχnichesκy προdρsτ susπendiρuyuτ in eτanοle, πρiκaπy- vayuτ κοntsenτρiροvanny vοdny ammiaκ dο ποlnοgο ρasτ- vορeniya οsadκa, ρasτvορ goilτρuyuτ and tselevοy προduκτ ποvτορnο vyοag-dayuτ ποdκislenπem φοο ^ ορnοy κlslοτy dο ρΗ 2. Tselevοy προduκτ οτφnlτροzyvayuτ, προmyΕayuτ on φπlτρe eφiροm ζ sushaτ in zaκuume. The end of the target product 71, $ 6 (in terms of the hydraulics and the hexamethanuanidyan) •
Пοлученный φοссπаτ ποл:-геκсамеτζленгуанидπна πρедсτаΕЛяеτ еοбοι: τвеρдοе мелκοκρπсτаллιгчесκοе ве- щесτΕθ белοгο цвеτа όез заπаχа сο сρедн'?:" мοлеκуляρ- нοй массοГι 1070-1130, χοροшο ρаοτвορπмοе в Εοде , не ρасτΕορлглοе в ορганячесκπχ ρасτΕορиτелш:, сτабильнοе πρи χρаненιπ и πρи лποφ:ιлизац: :ι егο ΕΟДΗЫΧ ρасτΕοροв. Пροшιдле нная πριιменпмοο τь Пρедπагаемый πρеπаρаτ πρедназначен для леченιш ρаκοΕЫΧ забοлеван-.--:-: κшдечнο-желудοчнοгο τρаκτа , мο- лοчнοй железы и τаκже дли οбρабοτκи ρан ποсле ρадд- 5 ΡСΤ/δϋ82/00020Pοluchenny φοssπaτ ποl: -geκsameτζlenguanidπna πρedsτaΕLyaeτ eοbοι: τveρdοe melκοκρπsτallιgchesκοe of Great schesτΕθ belοgο tsveτa όez zaπaχa sο sρedn '?: "mοleκulyaρ- nοy massοGι 1070-1130, χοροshο ρaοτvορπmοe in Εοde not ρasτΕορlglοe in ορganyachesκπχ ρasτΕορiτelsh :, sτabilnοe πρi χρanenιπ and πρi lποφ : ιlizats:: v egο ΕΟDΗYΧ ρasτΕοροv Pροshιdle constant prices πριιmenpmοο τ Pρedπagaemy πρeπaρaτ πρednaznachen for lechenιsh ρaκοΕYΧ zabοlevan -.--: -:. κshdechnο-zheludοchnοgο τρaκτa, mο- lοchnοy gland and τaκzhe length οbρabοτκi ρan ποsle ρadd- 5 ΡСΤ / δϋ82 / 00020
- 8 - κальнοй οπеρации οπуχοли. Τаκ κаκ πρедлагаемый πρе- πаρаτ οбладаеτ дρуτим меχанизмοм дейсτвιш πο сρаΕне- нию с извесτными πρеπаρаτами, οн мοжеτ найτи πρшлене- ние для лечения ρезисτенτныχ φορм οπуχοлей. - 8 - local operation of the patient. Since the proposed offer eliminates the risk of interfering with known medications, you may not be able to cure it.
Claims
Priority Applications (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH90284A CH660964A5 (en) | 1982-06-21 | 1982-06-21 | MEDICINAL PRODUCT WITH ANTI-MEDICINAL EFFECT. |
| PCT/SU1982/000020 WO1984000105A1 (en) | 1982-06-21 | 1982-06-21 | Medicinal preparation having antitumoral effect |
| GB08403257A GB2134783B (en) | 1982-06-21 | 1982-06-21 | Medical preparation having antitumoral effect |
| DE19823249514 DE3249514T1 (en) | 1982-06-21 | 1982-06-21 | Medicines with anti-carcinogenic effects |
| JP57503491A JPS59501110A (en) | 1982-06-21 | 1982-06-21 | Pharmaceutical compositions with antitumor activity |
| NL8220420A NL8220420A (en) | 1982-06-21 | 1982-06-21 | PHARMACEUTICAL COMPOSITION, WHICH HAS ANTITUMOR ACTIVITY. |
| CA000413032A CA1194802A (en) | 1982-06-21 | 1982-10-07 | Pharmaceutical composition possessing antitumor activity |
| FR8218494A FR2535609A1 (en) | 1982-06-21 | 1982-11-04 | ANTITUMOR ACTION MEDICINE BASED ON POLYHEXAMETHYLENEGUANIDINE |
| SE8400453A SE437931B (en) | 1982-06-21 | 1984-01-30 | PHARMACEUTICAL COMPOSITION WITH ANTITUMOR EFFECTS CONTAINING PHOSPHATE OF POLYHEXAMETHYLENGUANIDINE WITH THE FORMULA |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/SU1982/000020 WO1984000105A1 (en) | 1982-06-21 | 1982-06-21 | Medicinal preparation having antitumoral effect |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO1984000105A1 true WO1984000105A1 (en) | 1984-01-19 |
Family
ID=21616776
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/SU1982/000020 Ceased WO1984000105A1 (en) | 1982-06-21 | 1982-06-21 | Medicinal preparation having antitumoral effect |
Country Status (9)
| Country | Link |
|---|---|
| JP (1) | JPS59501110A (en) |
| CA (1) | CA1194802A (en) |
| CH (1) | CH660964A5 (en) |
| DE (1) | DE3249514T1 (en) |
| FR (1) | FR2535609A1 (en) |
| GB (1) | GB2134783B (en) |
| NL (1) | NL8220420A (en) |
| SE (1) | SE437931B (en) |
| WO (1) | WO1984000105A1 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1994015596A1 (en) * | 1992-12-30 | 1994-07-21 | The Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services | Compositions and methods for inhibiting deoxyhypusine synthase and the growth of cells |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19628641C2 (en) * | 1996-07-16 | 1998-12-17 | Fresenius Ag | Use of PHMB for the treatment of tumor diseases |
| RU2144024C1 (en) * | 1998-10-28 | 2000-01-10 | Иркутский институт химии СО РАН | Method of preparing polyhexamethylene guanidine |
| KR100557559B1 (en) * | 1999-12-20 | 2006-03-03 | 에스케이 주식회사 | Polyhexamethyleneguanidine phosphate powder, preparation method thereof and antibacterial resin containing same |
| KR100725004B1 (en) * | 1999-12-24 | 2007-06-04 | 에스케이 주식회사 | Disinfectant Disinfectant Composition and Method of Use thereof |
| AT505312A1 (en) | 2007-05-15 | 2008-12-15 | Recticel Schlafkomfort Gmbh Sc | POLYURETHANE MATERIAL WITH BIOCIDAL EQUIPMENT |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1040049A (en) * | 1963-12-23 | 1966-08-24 | Rohm & Haas | Preparation of tertiary octylguanidines |
| US3824288A (en) * | 1961-06-09 | 1974-07-16 | Hoffmann La Roche | Substituted hydrazine derivatives and process for the manufacture thereof |
| GB1492678A (en) * | 1975-08-11 | 1977-11-23 | Ici Ltd | Guanidine derivatives |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5341426A (en) * | 1976-09-27 | 1978-04-14 | Asahi Chem Ind Co Ltd | Fungicidal and bactericidal agents |
-
1982
- 1982-06-21 CH CH90284A patent/CH660964A5/en not_active IP Right Cessation
- 1982-06-21 JP JP57503491A patent/JPS59501110A/en active Pending
- 1982-06-21 DE DE19823249514 patent/DE3249514T1/en not_active Withdrawn
- 1982-06-21 WO PCT/SU1982/000020 patent/WO1984000105A1/en not_active Ceased
- 1982-06-21 GB GB08403257A patent/GB2134783B/en not_active Expired
- 1982-06-21 NL NL8220420A patent/NL8220420A/en not_active Application Discontinuation
- 1982-10-07 CA CA000413032A patent/CA1194802A/en not_active Expired
- 1982-11-04 FR FR8218494A patent/FR2535609A1/en active Granted
-
1984
- 1984-01-30 SE SE8400453A patent/SE437931B/en not_active IP Right Cessation
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3824288A (en) * | 1961-06-09 | 1974-07-16 | Hoffmann La Roche | Substituted hydrazine derivatives and process for the manufacture thereof |
| GB1040049A (en) * | 1963-12-23 | 1966-08-24 | Rohm & Haas | Preparation of tertiary octylguanidines |
| GB1492678A (en) * | 1975-08-11 | 1977-11-23 | Ici Ltd | Guanidine derivatives |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1994015596A1 (en) * | 1992-12-30 | 1994-07-21 | The Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services | Compositions and methods for inhibiting deoxyhypusine synthase and the growth of cells |
Also Published As
| Publication number | Publication date |
|---|---|
| NL8220420A (en) | 1984-05-01 |
| FR2535609B1 (en) | 1985-03-15 |
| GB2134783B (en) | 1985-10-30 |
| SE8400453L (en) | 1985-03-25 |
| CA1194802A (en) | 1985-10-08 |
| DE3249514T1 (en) | 1984-05-17 |
| CH660964A5 (en) | 1987-06-30 |
| GB8403257D0 (en) | 1984-03-14 |
| SE437931B (en) | 1985-03-25 |
| JPS59501110A (en) | 1984-06-28 |
| FR2535609A1 (en) | 1984-05-11 |
| SE8400453D0 (en) | 1984-01-30 |
| GB2134783A (en) | 1984-08-22 |
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