Sodium salt of 9-hydroxy-19,20-norprostanic acid possessing hypolipemic and antiulcer activity

专利摘要:
The invention relates to 19,20-bis-nor-prostanoic acids, and their functional derivatives, endowed with hypolipemic, and antiulcerous properties.
公开号:SU794003A1
申请号:SU752163119
申请日:1975-08-07
公开日:1981-01-07
发明作者:Валкави Умберто
申请人:Иституто Биокимико Итальяноди Лоредана Лоренцини (Фирма)；Др. Мадаус Энд Компани (Фирма)；
IPC主号:

专利说明:

(54) SODIUM SALT 9-OXY-19,20-BISNORPROSTANIC ACID, MANIFESTING
HYPOLIPEMIC AND CONTRACTIVE
ACTIVITY 3 weight 320; IR bands at 3400, 3300, 1565, 1460, 1390. The novel salt of formula (1) exhibits hypolipemic and anti-ulcer activity. Below are the biological is-5 attempts at new salt (1).
Control Salt ()
glycemia test (repetition), mg / 100 ml of blood + ES:
Control Salts (I) Treatment is administered at doses of 200 mg / kg endoperitoneally 2 hours before the test. Rats Motility Time 25.3 ± 0.2 29.0 ± 0.4, 001
Repeat coagulation test, 0.1 min + ES:
Mobility Time Clotting Time
Control 25.8 ± 0.495.0 ± 1.5
Salt (I) 29.3 ± 0.3, 00111.8 ± 1.4, 001
Treatment lead doses of 200 mg / kg endo-d) Platelet adhesion caused
peritoneally 2 hours before the test. Rat-ADR. The test results are given
males Spreg-Dauley 150 g each, groups of 6c table. one.
animals.15
63.8 ± 4.1
, 001 99.3 ± 2.7
81.1 ± 3.5
}, 0 121.4 ± 9.8
Clotting time 84.5 ± 1.6 98.8 ± 0.9, 001
Table 1 4 Pharmacological action. a) LDso is orally administered to mice at about 3000 mg / kg; c) speed test for glycemia, mg / 100 MJJ bloodI + ES: Sprag-Dowley males, 150 g each, groups of 6 animals. c) Coagulation test, min / 10 ± E5:
 Treatment is carried out with doses of 200 ml / kg endoperitoneally 1 or 2 hours before opening. The males of the Spreg Dawley rats, average weight 150 g.
Alcohol sample: triglyceridemi and cholesterol, mg / 100 ml + ES. The test results are shown in Table. 2
Treatment is carried out for 1 week. CP1B-BBA 200 mg / kg is endoperitoneally. Salt (1) 50 kg / kg endoperitoialio, 1 time per day. Test rats male SpregDouly 150 g, groups of 6 rats. CP1B -
Checklists
Salt (I) endoperitonal
Salt (I) orally
Treatment for 3 days with an endoperitonal or oral dose of 50 mg / kg. Male Spreg Dawley rats weighing 150 g each, groups of 6 rats.
Control Diet Nata
Diet Nata + Salt (I) (endoperitoneally)
Diet Nat salt (I) (orally) 1) Compared with the control, 02. 2) Compared to the Nat diet, 05. Treatment 25 mg / kg daily for 1 noncontrolled
Diet Nata + salt (I)
Diet Nata + salt (I)
1) Compared with the controls, 001) Compared with the Nat diet, 01 3) Compared with the Nat diet, 001.
Treatment with 25 and 50 mg / kg per day endope-Compound (1) was tested pharmacologically for 1 week for male rats. 15 for the purpose of showing a possible prostate Spreg-Dawley weighing 15 g each, of a group of polandin-like activity. Compound
12 animals. (1) studied by the above parameters.
General pharmacologists. On the trachea of the guinea pig, the stripes of the bottom table 2
clofibrate; BBA - p-benzalmasl acid on 1B1; TE - triglyceridemi; CHOL - cholesterol.
Fast glycemia test, mg / 100 ml blood-f-ES:
, 02, 01
Hyperlipid diet according to Nath: triglyperides or cholesterol, mg / 100 ml of blood + EZ:
riglycerides
Cholesterol 96.9 ± 9.4
72.6 ± 4.31 134.9 ± 9.41
333.3 ± 29.91
169.3 ± 26.8 91.9 ± 16.3
109.4 ± 6.92
380.2 ± 77.8a
Cholesterol
riglycerides 91.1 + 13.5 64.4 ± 2, .81
25 mg
81.5 ± 13.3
108.3 ± 13.92
50 mg 101.8 ± 4.48 43.1 ± 6.1 Delhi male Spreg-Dawley rats weighing up to 150 g; groups of 12 animals. Hyperlipid diet according to Nath; trigig.rides and cholesterol, mg / 100 ml of blood + E3.

权利要求:
Claims (1)
[1]
Claim
In both doses, the substance noticeably suppresses the ulcer-forming effect of aspirin.
Phenylbutazone ulcer.
Experimental female animals of Wister rats weighing 170 + 18 g. Animals were kept under constant environment for at least 2 weeks before the start of the experiment. 24 hours before the start of the experiment, the animals were not given food, but water was given as needed.
Each experimental group consisted of 10 animals. The substance in question was first administered 15 minutes before the administration of phenylbutazone (200 mg / kgX 1 ml) in a 0.5% aqueous solution of tragacanth resin, orally, then 2.5 hours after administration
40 Sodium salt of 9-hydroxy-19,20-bis-polproflural acid of the formula (1)
45 y — SOOID
It exhibits hypolipemic and antiulcer activity.

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引用文献:

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CA1027118A|1972-04-03|1978-02-28|Martin J. Weiss|3-alkyl-2- cyclopentanones and esters and salts thereof|US4239778A|1978-09-12|1980-12-16|The University Of Illinois Foundation|Azaprostanoic acid analogs and their use as inhibitors of platelet aggregation|

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US4374856A|1980-09-10|1983-02-22|The Upjohn Company|Liver cytoprotection using PGE's|

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IT1190400B|1985-10-04|1988-02-16|Istituto Biochimico Italiano|19,20-BIS ACID DERIVATIVES, NOR-PROSTANOIC WITH ANTI-ULTER AND ANOREXIVE ACTIVITY, PROCEDURE FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS|

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IT1205183B|1987-06-25|1989-03-15|Istituto Biochimico Italiano|PROSTAGLANDIN DERIVATIVES, PROCEDURES TO PREPARE THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM|

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EP2404890B1|2003-01-23|2017-07-26|Esperion Therapeutics Inc.|Hydroxyl compounds and compositions for cholesterol management and related uses|

法律状态:

优先权:

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申请号 | 申请日 | 专利标题

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IT26111/74A|IT1060366B|1974-08-07|1974-08-07|ACIDS 19.20 BIS NOR PROSTANOIC AS HYPOLYPEMIC COMPOUNDS|

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