CN107744520A - Pyrimidines are preparing the application in promoting small bowel peristalsis medicine - Google Patents
Pyrimidines are preparing the application in promoting small bowel peristalsis medicine Download PDFInfo
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- CN107744520A CN107744520A CN201711016503.8A CN201711016503A CN107744520A CN 107744520 A CN107744520 A CN 107744520A CN 201711016503 A CN201711016503 A CN 201711016503A CN 107744520 A CN107744520 A CN 107744520A
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- Prior art keywords
- aminopyridine
- piperazinyl
- phenylamino
- small bowel
- pyridine radicals
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention relates to 2 phenylamino 4 pyrrolidinyl 6 (5 (piperazinyl of 4 methyl 1) 2 pyridine radicals) aminopyridine, simultaneously [3,4 d] pyrimidine is preparing the application in promoting small bowel peristalsis medicine.Find out from pharmacological evaluation, 2 phenylamino 4 pyrrolidinyl 6 (5 (piperazinyl of 4 methyl 1) 2 pyridine radicals) aminopyridine simultaneously [3,4 d] pyrimidine plays the role of preferably to promote small bowel peristalsis, possess prominent substantive distinguishing features, while promote small bowel peristalsis medicine obviously with significant progressive for preparing.
Description
Technical field
The invention belongs to field of medicaments, and in particular to a kind of new pharmaceutical use of pyrimidines, more particularly to 2- benzene
Simultaneously [3,4-d] pyrimidine is preparing rush to amino -4- pyrrolidinyls -6- (5- (4- methyl isophthalic acids-piperazinyl) -2- pyridine radicals) aminopyridine
The application entered in small bowel peristalsis medicine.
Background technology
Enterocinesia, refer to the vermicular motion of wriggling class, espespecially the wavy contraction of intestines, it is coarse that fibre-bearing is more but nutrition is low
Food, it can stimulate enterocinesia.Thick, the indigestible plant that fiber food one kind is mainly made up of polysaccharide (such as cellulose)
Material, the wriggling of intestines can be stimulated after wedging.If wriggling can slowly cause constipation.
Pyrimidines 2- phenylaminos -4- pyrrolidinyls -6- (5- (4- methyl isophthalic acids-piperazinyl) -2- of the present invention
Pyridine radicals) simultaneously [3,4-d] pyrimidine, CN107245075A disclose 2- phenylamino -4- pyrrolidinyls -6- (5- (4- first to aminopyridine
Base -1- piperazinyls) -2- pyridine radicals) aminopyridine simultaneously [3,4-d] pyrimidine preparation method, there is presently no 2- phenylamino -4- pyrroles
Cough up alkyl -6- (5- (4- methyl isophthalic acids-piperazinyl) -2- pyridine radicals) aminopyridine simultaneously [3,4-d] pyrimidine promote small bowel peristalsis phase
Close report.
The content of the invention
Object of the present invention is to provide 2- phenylamino -4- pyrrolidinyls -6- (5- (4- methyl isophthalic acids-piperazinyl) -2- pyrroles
Piperidinyl) simultaneously [3,4-d] pyrimidine is preparing the application in promoting small bowel peristalsis medicine to aminopyridine.
Another object of the present invention is to provide 2- phenylamino -4- pyrrolidinyls -6- (5- (4- methyl isophthalic acids-piperazinyl) -
2- pyridine radicals) simultaneously [3,4-d] pyrimidine prepares the method for promoting small bowel peristalsis pharmaceutical preparation to aminopyridine.
The present inventor be surprised to find that in test 2- phenylamino -4- pyrrolidinyls -6- (5- (4- methyl isophthalic acids-piperazinyl) -
2- pyridine radicals) simultaneously [3,4-d] pyrimidine is preparing the application in promoting small bowel peristalsis medicine, 2- phenylamino -4- pyrroles to aminopyridine
Simultaneously [3,4-d] pyrimidine has preferably promotion small intestine compacted to alkyl -6- (5- (4- methyl isophthalic acids-piperazinyl) -2- pyridine radicals) aminopyridine
Dynamic effect.
Compound 2- phenylaminos -4- pyrrolidinyls -6- (5- (4- methyl isophthalic acids-piperazinyl) -2- pyridine radicals) the amino pyrrole
Pyridine is simultaneously shown in [3,4-d] pyrimidine structure such as formula (I)：
Aminopyridine is simultaneously [3,4-d] by 2- phenylamino -4- pyrrolidinyls -6- (5- (4- methyl isophthalic acids-piperazinyl) -2- pyridine radicals)
Pyrimidine is preparing the application in promoting small bowel peristalsis medicine.
Prepared by one kind promotes small bowel peristalsis pharmaceutical preparation, and the active component in the pharmaceutical preparation stated includes 2- phenylaminos -4-
Pyrrolidinyl -6- (5- (4- methyl isophthalic acids-piperazinyl) -2- pyridine radicals) aminopyridine simultaneously [3,4-d] pyrimidine.
Described prepare promotes small bowel peristalsis pharmaceutical preparation, and preparation method comprises the following steps：Take 2- phenylamino -4- pyrrolidines
Base -6- (5- (4- methyl isophthalic acids-piperazinyl) -2- pyridine radicals) aminopyridine simultaneously [3,4-d] pyrimidine, add auxiliary material, prepare piece agent,
One kind in the oral formulations such as capsule, granule, oral liquid, dripping pill.
The treatment and prevention kidney fibrosis pharmaceutical preparation, in preparation method auxiliary material be lactose, starch, microcrystalline cellulose,
Mannitol, dextrin, pregelatinized starch, PVPP, sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose, cross-linked carboxymethyl
One or more in sodium cellulosate, magnesium stearate, talcum powder, silica.
Pharmacology contrast test discovery of the invention by mouse, 2- phenylamino -4- pyrrolidinyls -6- (5- (4- methyl -
1- piperazinyls) -2- pyridine radicals) aminopyridine simultaneously [3,4-d] pyrimidine low dose group mouse small intestine push wriggle compared with blank group
It increased, difference has significant (P<0.01)；2- phenylamino -4- pyrrolidinyls -6- (5- (4- methyl isophthalic acids-piperazinyl) -
2- pyridine radicals) simultaneously [3,4-d] pyrimidine high dose group has significant to aminopyridine compared with blank group, difference.Therefore,
Aspeverin is used for the medicine for preparing the bad disease of a variety of small bowel peristalsises, has good development prospect.
Embodiment
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by specific reality
Any restrictions of example are applied, but are defined in the claims.
Embodiment 1：Compound 2- phenylaminos -4- pyrrolidinyls -6- involved in the present invention (5- (4- methyl isophthalic acids-piperazinyl) -
2- pyridine radicals) aminopyridine simultaneously [3,4-d] pyrimidine tablet preparation：
By the method for CN107245075A disclosed embodiments 1 prepare 2- phenylamino -4- pyrrolidinyls -6- (5- (4- methyl -
1- piperazinyls) -2- pyridine radicals) aminopyridine simultaneously [3,4-d] pyrimidine, take 20 g of compound 2- phenylamino -4- pyrrolidinyls -6-
(5- (4- methyl isophthalic acids-piperazinyl) -2- pyridine radicals) simultaneously [3,4-d] pyrimidine, addition prepare the customary adjuvant 180 of tablet to aminopyridine
Gram, mix, conventional tablet presses are made 1000.
Embodiment 2：Compound 2- phenylaminos -4- pyrrolidinyls -6- involved in the present invention (5- (4- methyl isophthalic acids-piperazinyl) -
2- pyridine radicals) aminopyridine simultaneously [3,4-d] pyrimidine capsule preparation：
By the method for CN107245075A disclosed embodiments 1 prepare 2- phenylamino -4- pyrrolidinyls -6- (5- (4- methyl -
1- piperazinyls) -2- pyridine radicals) aminopyridine simultaneously [3,4-d] pyrimidine, take 20 g of compound 2- phenylamino -4- pyrrolidinyls -6-
(5- (4- methyl isophthalic acids-piperazinyl) -2- pyridine radicals) simultaneously [3,4-d] pyrimidine, addition prepare the customary adjuvant of capsule to aminopyridine
Such as 180 grams of starch, mix, it is encapsulated to be made 1000.
Its pharmaceutical activity is further illustrated below by pharmacodynamic experiment.
Experimental example：Compound 2- phenylamino -4- pyrrolidinyls -6- (5- (4- methyl isophthalic acids-piperazine are evaluated using pharmacological evaluation method
Piperazine base) -2- pyridine radicals) the aminopyridine influence that simultaneously [3,4-d] pyrimidine is wriggled to small intestine promotion
1st, method：Kunming mice 30,20 ± 5g is taken, male and female half and half, by sex, body weight is randomly divided into 3 groups, i.e. blank
Group, 2- phenylamino -4- pyrrolidinyls -6- (5- (4- methyl isophthalic acids-piperazinyl) -2- pyridine radicals) aminopyridine simultaneously [3,4-d] pyrimidine
(0.06mg/10g, 0.24mg/10g) two dosage groups.Every group 10,2- phenylamino -4- pyrrolidinyls -6- (5- (4- methyl -
1- piperazinyls) -2- pyridine radicals) simultaneously suspension, blank is made in [3,4-d] pyrimidine and 5% charcoal end, 10% Arabic gum to aminopyridine
Group is not added with medicine and is suspended directly to charcoal end, Arabic gum, uses normal saline.Mouse fasting 24 hours before experiment.Mouse
Gastric infusion 0.2ml/10g, 30min is put to death after administration.Pylorus is taken to ileocecus digest tube, without traction tiling and thin plate
On, total length and pylorus are surveyed to the distance in charcoal end forward position, thus extrapolate ink propulsive rate.
2. result：Statistical result shows 2- phenylamino -4- pyrrolidinyls -6- (5- (4- methyl isophthalic acids-piperazinyl) -2- pyridines
Base) aminopyridine simultaneously [3,4-d] pyrimidine low dose group mouse small intestine push wriggle increased compared with blank group, difference has aobvious
Work property meaning (P<0.01)；2- phenylamino -4- pyrrolidinyls -6- (5- (4- methyl isophthalic acids-piperazinyl) -2- pyridine radicals) aminopyridine
And [3,4-d] pyrimidine high dose group, compared with blank group, difference has significant (P<0.001) result such as table 1.
The influence (x+s) that the Aspeverin of table 1 is wriggled to mouse small intestine pushability
Compared with blank group, * * P<0.001*P<0.01
Shown by above-mentioned experimental example, 2- phenylamino -4- pyrrolidinyls -6- of the invention (5- (4- methyl isophthalic acids-piperazinyl) -
2- pyridine radicals) aminopyridine simultaneously [3,4-d] pyrimidine low dose group mouse small intestine push wriggle increased compared with blank group, it is poor
It is different to have significant (P<0.01)；2- phenylamino -4- pyrrolidinyls -6- (5- (4- methyl isophthalic acids-piperazinyl) -2- pyridine radicals) ammonia
Simultaneously [3,4-d] pyrimidine high dose group has significant to yl pyridines compared with blank group, difference.Thus prove, 2- phenylaminos of the invention
Simultaneously [3,4-d] pyrimidine has preferable rush to aminopyridine to base -4- pyrrolidinyls -6- (5- (4- methyl isophthalic acids-piperazinyl) -2- pyridine radicals)
Enter the effect of small bowel peristalsis.It can be used for the treatment of the bad disease of a variety of small bowel peristalsises.
Claims (4)
- Simultaneously [3,4-d] is phonetic for aminopyridine by 1.2- phenylamino -4- pyrrolidinyls -6- (5- (4- methyl isophthalic acids-piperazinyl) -2- pyridine radicals) Pyridine is preparing the application in promoting small bowel peristalsis medicine.
- 2. prepared by one kind promote small bowel peristalsis pharmaceutical preparation, it is characterised in that the active component in described pharmaceutical preparation includes 2- phenylamino -4- pyrrolidinyls -6- (5- (4- methyl isophthalic acids-piperazinyl) -2- pyridine radicals) aminopyridine simultaneously [3,4-d] pyrimidine.
- Promote small bowel peristalsis pharmaceutical preparation 3. preparing according to claim 2, it is characterised in that preparation method includes following step Suddenly：Taking 2- phenylamino -4- pyrrolidinyls -6- (5- (4- methyl isophthalic acids-piperazinyl) -2- pyridine radicals), simultaneously [3,4-d] is phonetic for aminopyridine Pyridine, auxiliary material is added, prepare one kind in the oral formulations such as piece agent, capsule, granule, oral liquid, dripping pill.
- 4. kidney fibrosis pharmaceutical preparation is treated and prevented according to claim 3, it is characterised in that auxiliary material is in preparation method Lactose, starch, microcrystalline cellulose, mannitol, dextrin, pregelatinized starch, PVPP, sodium carboxymethyl starch, low substitution hydroxyl One or more in propyl cellulose, Ac-Di-Sol, magnesium stearate, talcum powder, silica.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711016503.8A CN107744520A (en) | 2017-10-25 | 2017-10-25 | Pyrimidines are preparing the application in promoting small bowel peristalsis medicine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711016503.8A CN107744520A (en) | 2017-10-25 | 2017-10-25 | Pyrimidines are preparing the application in promoting small bowel peristalsis medicine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107744520A true CN107744520A (en) | 2018-03-02 |
Family
ID=61254102
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201711016503.8A Withdrawn CN107744520A (en) | 2017-10-25 | 2017-10-25 | Pyrimidines are preparing the application in promoting small bowel peristalsis medicine |
Country Status (1)
| Country | Link |
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| CN (1) | CN107744520A (en) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1252069A (en) * | 1997-04-16 | 2000-05-03 | 艾博特公司 | 5,6,7-trisubstituted-4-aminopyrido [2,3-d] pyrimidine compounds |
| CN107245075A (en) * | 2017-08-04 | 2017-10-13 | 西安交通大学 | Simultaneously [3,4 d] pyrimidines and its salt and the application of 2,4,6 3 substituted pyridines |
-
2017
- 2017-10-25 CN CN201711016503.8A patent/CN107744520A/en not_active Withdrawn
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1252069A (en) * | 1997-04-16 | 2000-05-03 | 艾博特公司 | 5,6,7-trisubstituted-4-aminopyrido [2,3-d] pyrimidine compounds |
| CN107245075A (en) * | 2017-08-04 | 2017-10-13 | 西安交通大学 | Simultaneously [3,4 d] pyrimidines and its salt and the application of 2,4,6 3 substituted pyridines |
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| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
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| WW01 | Invention patent application withdrawn after publication |
Application publication date: 20180302 |
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| WW01 | Invention patent application withdrawn after publication |