CN106619625B - A kind of medicine for treating atrophic gastritis and its purposes in the medicine for preparing treatment atrophic gastritis - Google Patents
A kind of medicine for treating atrophic gastritis and its purposes in the medicine for preparing treatment atrophic gastritis Download PDFInfo
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- CN106619625B CN106619625B CN201611019488.8A CN201611019488A CN106619625B CN 106619625 B CN106619625 B CN 106619625B CN 201611019488 A CN201611019488 A CN 201611019488A CN 106619625 B CN106619625 B CN 106619625B
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- atrophic gastritis
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- gastric mucosa
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
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- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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Abstract
The present invention relates to a kind of medicine for treating atrophic gastritis, the medicine includes the compound or its stereoisomer, geometric isomer, dynamic isomer, pharmaceutically acceptable salt shown in following formula, and pharmaceutically acceptable carrier, excipient, diluent, assistant agent, medium or its combination：Wherein R1 is H, CH3, F, Cl or Br.Medicine of the present invention can significantly reduce MDA contents in gastric mucosa, improve SOD, GSH Px vigor, so as to weaken lipid peroxidation, play a part of protecting gastric mucosa and repair damage gastric mucosa.
Description
Technical field
The present invention relates to field of medicaments, specifically, the present invention relates to a kind of medicine for treating atrophic gastritis and
Its purposes in the medicine for preparing treatment atrophic gastritis.
Background technology
Atrophic gastritis is also referred to as atrophic gastritis, and with gastric epithelial and body of gland atrophy, number is reduced, and gastric mucosa becomes
Thin, mucous membrane basic unit thickens, or with gland metaplasia and intestinal gland metaplasia, or the chronic digestible system disease for thering is atypical hyperplasia to be characterized
Disease.Upper abdomen secret anguish, turgor, belch often are shown as, is lost the appetite, or is become thin, anaemia etc., no specificity.It is a kind of more pathogenic
Factor disease and precancerous lesion, the symptom of atrophic gastritis, sign are without specificity, it is impossible to as the foundation of diagnosis, make a definite diagnosis master
Lean on gastroscope and gastric mucosa living tissue pathologic finding.Visible 1. gastric mucosa color is thin out under gastroscope；2. submucosal blood vessel is seen through；③
Mucosal fold is tiny or even disappears；4. atrophic gastritis is with body of gland neck hyperplasia or intestinal metaplasia, mucomembranous surface
It is rough, it is in granular form or nodositas, it is seen that pseudopolyp is formed；5. atrophy mucosal friability increases, easy bleeding, and can have erosion
Stove；6. atrophic gastritis can be simultaneously with the performance of chronic superficial gastritis, such as congested erythema, attachment mucus, and reflective increasing
It is strong etc..
The content of the invention
It is an object of the invention to provide a kind of medicine for treating atrophic gastritis.
In order to realize the purpose of the present invention, the present invention provides a kind of medicine for treating atrophic gastritis, the medicine
Comprising the compound shown in following formula or its stereoisomer, geometric isomer, dynamic isomer, pharmaceutically acceptable salt, with
And pharmaceutically acceptable carrier, excipient, diluent, assistant agent, medium or its combination：
Wherein R1 is H, CH3, F, Cl or Br.
Preferably, R1 F.
Preferably, R1 CH3。
It is highly preferred that tablet, capsule, suppository or injection can be made in the medicine.
The present invention also provides purposes of the compound in the medicine for preparing treatment atrophic gastritis,
Wherein R1 is H, CH3, F, Cl or Br.
Preferably, R1 F.
Preferably, R1 CH3。
It is highly preferred that the medicine can be the stereoisomer of the compound, geometric isomer, dynamic isomer,
Pharmaceutically acceptable salt, and pharmaceutically acceptable carrier, excipient, diluent, assistant agent, medium or its combination.
It is highly preferred that tablet, capsule, suppository or injection can be made in the medicine.
Unless otherwise indicated, all scientific and technical terminologies used in the present invention have with those skilled in the art of the invention's
It is generally understood that identical implication.All patents of the present invention and public publication are integrally incorporated this hair by reference
It is bright.
Any disease of term " treatment " or illness as used in the present invention, refer to improvement disease in some of these embodiments
Disease or illness (slow down or prevent mitigate disease or the development of its at least one clinical symptoms).In other embodiments
In, " treatment " refers to mitigation or improves at least one body parameter, including the body parameter that may not be discovered by patient.Another
In a little embodiments, " treatment " refers to from body (such as stablizing perceptible symptom) or physiologically (such as stablizes body
Parameter) or above-mentioned two aspects regulation disease or illness.In other embodiments, " treatment " refers to prevention or delay disease or disease
Breaking-out, generation or the deterioration of disease.
As described herein, term " pharmaceutically acceptable carrier " includes any solvent, decentralized medium, coating agents,
Surfactant, antioxidant, preservative (such as antibacterial agent, antifungal agent), isotonic agent, salt, drug stabilizing agent, bonding
Agent, excipient, dispersant, lubricant, sweetener, flavor enhancement, colouring agent, or its composition, these carriers are all affiliated technologies
Known (such as Remington's Pharmaceutical Sciences, 18thEd.Mack of art personnel
Printing Company, described in 1990, p1289-1329).Except any conventional carrier situation incompatible with active component
Outside, its purposes in treatment or pharmaceutical composition is covered.
Term " study subject " used in the present invention refers to animal.Typically described animal is mammal.It is tested right
As, such as also refer to primate (such as mankind, sex), ox, sheep, goat, horse, dog, cat, rabbit, rat, small
Mouse, fish, bird etc..In certain embodiments, the study subject is primate.In other embodiments, it is described by
It is people to try object.
Term " patient " used in the present invention refers to people (including adult and children) or other animals.In some implementations
In scheme, " patient " refers to people.
Term "comprising" is open language, that is, includes the content specified by the present invention, but be not precluded from otherwise
Content.
" stereoisomer " refers to there is identical chemical constitution, but the spatially different change of arrangement mode of atom or group
Compound.Stereoisomer includes enantiomter, diastereoisomer, rotamer (rotational isomer), geometric isomer
(cis/trans) isomers, atropisomer, etc..
" enantiomter " refers to that two of a compound can not isomers that is overlapping but being mutually mirror.
" diastereoisomer " refers to have two or more chiral centres and its molecule not alloisomerism of mirror image each other
Body.Diastereoisomer has different physical properties, such as fusing point, boiling point, spectral quality and reactivity.Diastereoisomer mixes
Compound can be operated such as electrophoresis and chromatogram, such as HPLC by high resolution analysis to separate.
Term " dynamic isomer " or " tautomeric form " refer to there is being built by low energy for different-energy
(lowenergybarrier) constitutional isomer of mutual inversion of phases., can be with if tautomerism is possible (as in the solution)
Reach the chemical balance of dynamic isomer.For example, (also referred to as proton translocation is mutual for proton tautomer (protontautomer)
Tautomeric (prototropictautomer)) include by proton migration the mutual inversion of phases that carries out, such as keto-enol isomery
Change and imine-enamine isomerizations.Valence tautomerism body (valencetautomer) includes the restructuring by some bonding electrons
Come the mutual inversion of phases carried out.The instantiation of ketoenol tautomerization is pentane -2,4- diketone and the amyl- 3- alkene -2- ketone of 4- hydroxyls
The change of dynamic isomer.Another tautomeric example is phenol-keto tautomerism.One of phenol-keto tautomerism is specific
Example is the change of pyridine -4- alcohol and pyridine -4 (1H) -one dynamic isomer.Unless otherwise noted, the institute of the compounds of this invention
There are tautomeric forms to be within the scope of the present invention.
" pharmaceutically acceptable salt " used in the present invention refers to the organic salt and inorganic salts of the compound of the present invention.Medicine
Acceptable salt is known to us in art on, such as document：S.M.Bergeetal.,describe
pharmaceutically acceptable salts in detail in J.Pharmaceutical Sciences,
1977,66:It is 1-19. described.The salt that pharmaceutically acceptable nontoxic acid is formed includes, but is not limited to, with amino base
The inorganic acid salt that group's reaction is formed has hydrochloride, hydrobromate, phosphate, sulfate, perchlorate, and acylate, such as second
Hydrochlorate, oxalates, maleate, tartrate, citrate, succinate, malonate, or by being remembered on books document
The other method of load such as ion-exchange obtains these salt.Other pharmaceutically acceptable salts, including adipate, alginic acid
Salt, ascorbate, aspartate, benzene sulfonate, benzoate, bisulphate, borate, butyrate, camphor hydrochlorate, camphor tree
Brain sulfonate, cyclopentyl propionate, digluconate, lauryl sulfate, esilate, formates, fumaric acid
Salt, gluceptate, glycerophosphate, gluconate, Hemisulphate, enanthate, caproate, hydriodate, 2- hydroxyls-second
Sulfonate, lactobionate, lactate, laruate, lauryl sulfate, malate, malonate, mesylate, 2-
Naphthalene sulfonate, nicotinate, nitrate, oleate, palmitate, pectate, persulfate, 3- phenylpropionic acid salt, picric acid
Salt, pivalate, propionate, stearate, rhodanate, tosilate, undecylate, valerate, etc..By suitable
When the obtained salt of alkali include：Alkali metal, the salt of alkaline-earth metal.The present invention is also intended to contemplate the change of any included N group
The quaternary ammonium salt that compound is formed.Water-soluble or oil-soluble or dispersion product can be obtained by quaternization.Alkali metal or alkali
Earth metal salt includes sodium, lithium, potassium, calcium, magnesium, etc..Pharmaceutically acceptable salt further comprises appropriate, nontoxic ammonium, season
The amine cation that ammonium salt and gegenions are formed, such as halide, hydroxide, carboxylate, hydrosulphate, phosphoric acid compound, nitre
Acidulants, C1-8Azochlorosulfonate acid compound and aromatic sulphonic acid compound.
Medicine of the present invention can significantly reduce MDA contents in gastric mucosa, SOD, GSH-Px vigor be improved, so as to subtract
Weak lipid peroxidation, play a part of protecting gastric mucosa and repair damage gastric mucosa.
Embodiment
Below by way of the description of embodiment, the invention will be further described, but this is not the limit to the present invention
System, those skilled in the art according to the present invention basic thought, various modifications may be made or improve, but without departing from this
The basic thought of invention, within the scope of the present invention.
Therapeutic effect of the experimental example medicine of the present invention for atrophic gastritis
Medicine of the present invention：
Take 60 healthy cleaning grade SD rats, 180~200g of weight, male and female dual-purpose.Concentration is 180mgL-1's
N- methyl-N '-nitro-N nitrosoguanidine (MNNG) aqueous solution replace drinking water feeding modeling rat, totally 8 weeks.It is all common to raise
Material raising.
Rat is randomly divided into 6 groups, every group 10, be respectively Normal group, model group, Omeprazole positive drug group,
Medicine high dose group of the present invention, middle dose group, low dose group.In modeling the 9th week, MNNG solution was drunk in stopping, and each group is big
Mouse starts gastric infusion, one time a day, each 10mLkg-1Weight.Medicine of the present invention gives high dose group 10.98gkg-1Body
Quality, middle dose group 5.49gkg-1Weight, low dose group 2.745gkg-1Administration, Omeprazole positive drug is by daily
1.6g·kg-1Weight is administered, and Normal group and model group rats gavage physiological saline, one time a day, each 10mL
kg-1Weight, continuous 90d.
Gastric mucosa SOD, GSH-Px and MDA measure
After 90d is administered, Rat Fast 16h, urethane anesthesia is conventional to dissect mouse stomach, cleans gastric content, distilled water flushing
2 times, filter paper suck dry moisture.1/3 full gastric mucosa of careful scraping, weighs, and adds appropriate distilled water homogenate, gastric mucosa homogenate is made.
GSH-Px, SOD and MDA measure are by superoxide dismutase (SOD), glutathione (GSH-Px), MDA (MDA) kit
(build up Bioengineering Research Institute purchased from Nanjing) is carried out.As a result see the table below.
Statistical method
Test data analysis is carried out using SPSS17.0 statistical softwares.It is mainly measurement data to observe data, with
Represent, pass through test of normality.Multigroup is compared using one-way analysis of variance, is more then examined two-by-two for HSD-q.Examine
Level α=0.05.
Each group gastric mucosa of rat tissue GSH-Px, SOD, MDA content (N=10)
Note:Compared with Normal group△P<0.05,△△P<0.01；Compared with model is according to group▲P<0.05,▲▲P<0.01；With
Positive drug group compares﹟P<0.05。
Compared with Normal group, model group rats mucosa tissue SOD, GSH-Px activity reduces, MDA contents level liters
Height, difference have conspicuousness (P<0.05,P<0.01).Compared with model control group, the basic, normal, high dosage group rat of medicine of the present invention
SOD, GSH-Px activity significantly rise (P in gastric mucosa<0.05,P<0.01), MDA contents significantly reduce (P<0.05,P<0.01).
Compared with positive drug group, SOD, GSH-Px activity significantly rise (P in the middle and high dosage group rat ulcer tissue of medicine of the present invention<
0.05), MDA contents significantly reduce (P<0.05).
Claims (4)
1. purposes of the compound in the medicine for preparing treatment atrophic gastritis, it is characterised in that
, wherein R1 is H, CH3, F, Cl or Br.
2. purposes according to claim 1, it is characterised in that R1 F.
3. purposes according to claim 1, it is characterised in that R1 CH3。
4. the purposes according to Claims 2 or 3, it is characterised in that tablet, capsule, suppository or note is made in the medicine
Penetrate agent.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611019488.8A CN106619625B (en) | 2016-11-17 | 2016-11-17 | A kind of medicine for treating atrophic gastritis and its purposes in the medicine for preparing treatment atrophic gastritis |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611019488.8A CN106619625B (en) | 2016-11-17 | 2016-11-17 | A kind of medicine for treating atrophic gastritis and its purposes in the medicine for preparing treatment atrophic gastritis |
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| Publication Number | Publication Date |
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| CN106619625A CN106619625A (en) | 2017-05-10 |
| CN106619625B true CN106619625B (en) | 2018-02-02 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111297872A (en) * | 2020-03-02 | 2020-06-19 | 牡丹江医学院 | Medicine for treating chronic atrophic gastritis and preparation method thereof |
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- 2016-11-17 CN CN201611019488.8A patent/CN106619625B/en not_active Expired - Fee Related
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111297872A (en) * | 2020-03-02 | 2020-06-19 | 牡丹江医学院 | Medicine for treating chronic atrophic gastritis and preparation method thereof |
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| CN106619625A (en) | 2017-05-10 |
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| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| CB03 | Change of inventor or designer information | ||
| CB03 | Change of inventor or designer information |
Inventor after: Jiang Lu Inventor after: Ding Jian Inventor after: Zhang Yanyan Inventor before: Song Jian |
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| TA01 | Transfer of patent application right | ||
| TA01 | Transfer of patent application right |
Effective date of registration: 20180108 Address after: No. 42, culture West Road, Ji'nan, Shandong Province, Shandong Applicant after: Jiang Lu Address before: 050035 Tianshan Street, Shijiazhuang high tech Development Zone, Shijiazhuang, Hebei Province Applicant before: Song Jian |
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| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20180202 Termination date: 20181117 |