WO2021028005A1 - A medicament comprising anabasine for treatment of asthma, chest allergy and atopic dermatits - Google Patents
A medicament comprising anabasine for treatment of asthma, chest allergy and atopic dermatits Download PDFInfo
- Publication number
- WO2021028005A1 WO2021028005A1 PCT/EG2019/000032 EG2019000032W WO2021028005A1 WO 2021028005 A1 WO2021028005 A1 WO 2021028005A1 EG 2019000032 W EG2019000032 W EG 2019000032W WO 2021028005 A1 WO2021028005 A1 WO 2021028005A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- medicament
- anabasine
- chest
- allergy
- patients
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Ceased
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
Definitions
- 2- current medicament comprises of (L)(-)Anabasine as an active ingredient at 0.1 : 0.15 mg/kg of body weight and a pharmacologically acceptable excipient , diluent or carrier .
- 3- Medicament at mentioned doses is described to be administered by oral route twice per day for a period from 30 : 40 days for asthmatics and patients of chest allergy according to severity and condition development and from 21 : 40 days for patients of atopic dermatitis according to severity and condition development .
- medication is one course only .
- Receptors function modulation also may last longly after removal of (L) anabasine due to the permanent loss of functional channels within prolonged desensitizationfSimasko et al.,1986;Boyd,1987; Lukas, 1991; Buisson and Bertrand, 2002 ).
- This administering also negatively adapts signaling pathways .
- ALL these mutations may lead to a specific cholinergic modulation of allergic effector cells.
- this desensitization also shapes cholinergic signaling which regulates and drives skeletal muscles contraction including airways smooth muscle, which plays an integral part in the pathophysiology of asthma.
- nicotinic acetylcholine receptors in the peripheral nervous system transmit outgoing signals from the presynaptic to the postsynaptic cells within the sympathetic and parasympathetic nervous system , Heterologous desensitization also may thereafter leads these receptors to internalization .
- Role of receptor-mediated endocytosis is will recognized up take downregulation of transmembrane signal transduction but can also promote sustained signal transduction . It is actively implicated in transducing signals from the cell periphery to the nucleus .
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pulmonology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
The current invention relates to a novel oral medicament comprising (L)(-)Anabasine as an active ingredient at a dose concentration of about 0.1:0.15 mg/kg of body weight and a pharmacologically acceptable excipient, diluent or carrier. The medicament normalizes and treats asthma, chest allergies and atopic dermatitis, due to full agonistic action of Anabasine on al nicotinic acetylcholine receptors.
Description
Title Of The Invention
A MEDICAMENT COMPRISING ANABASINE FOR TREATMENT OF ASTHMA, CHEST ALLERGY AND ATOPIC DERMATITS
Technical Field
Therapeutic drugs discovery .
Background Art
All approved drugs which medicate all asthmatics types or patients of chest allergy and atopic dermatitis are symptomatic types , non therapeutic .
Disclosure Of Invention
1- The innovative element in current medicament that, in contrast of related approved types, that it normalizes and treats all asthmatics types and patients of chest allergy and atopic dermatitis permanently and releases them from their chronic pathological phenomenons .
2- current medicament comprises of (L)(-)Anabasine as an active ingredient at 0.1 : 0.15 mg/kg of body weight and a pharmacologically acceptable excipient , diluent or carrier .
3- Medicament at mentioned doses is described to be administered by oral route twice per day for a period from 30 : 40 days for asthmatics and patients of chest allergy according to severity and condition development and from 21 : 40 days for patients of atopic dermatitis according to severity and condition development . Herein medication is one course only .
4 - As fundamental causes of asthma types , chest allergy and atopic dermatitis are not completely understood to date , administering current medicament as described terminates them permanently . In light of publications which are free from binding between anabasine and asthma or allergic diseases and also free from detecting efforts to develop anabasine as a human drug or trials to generate a hope for that , mentioned unique effect is probably elucidated as anabasine has a full agonist action
on a7 nicotinic acetylcholine receptors which found in the central and peripheral nervous system, muscle, and many other tissues of human body. At the neuromuscular junction . So repeated ( L ) anabasine administering as described above to patients of same conditions at this minor concentration, for one course , so far from reported toxic dose and also teratogenic dose which was reported at 2.6 mg/kg animals body weight , this administering causes nicotinic acetylcholine receptors heterologous desensitization which may has the pivotal role in normalizing and treating them permanently via the mechanism of nicotinic acetylcholine receptors function modulation by phosphorylation beside the induced conformational changing in them particularly in alpha7 ligand binding domain . Receptors function modulation also may last longly after removal of (L) anabasine due to the permanent loss of functional channels within prolonged desensitizationfSimasko et al.,1986;Boyd,1987; Lukas, 1991; Buisson and Bertrand, 2002 ). This administering also negatively adapts signaling pathways . ALL these mutations may lead to a specific cholinergic modulation of allergic effector cells. mast cells, basophils, and eosinophils. Furthermore this desensitization also shapes cholinergic signaling which regulates and drives skeletal muscles contraction including airways smooth muscle, which plays an integral part in the pathophysiology of asthma. It is responsible for acute bronchoconstriction, which is potentiated by constrictor hyper responsiveness, impaired relaxation and length adaptation .Thus this shaping may modulate or normalize its contractile properties . On the other hand , nicotinic acetylcholine receptors in the peripheral nervous system transmit outgoing signals from the presynaptic to the postsynaptic cells within the sympathetic and parasympathetic nervous system , Heterologous desensitization also may thereafter leads these receptors to internalization . Role of receptor-mediated endocytosis is will recognized up take downregulation of transmembrane signal transduction but can also promote sustained signal transduction . It is actively implicated in transducing signals from the cell periphery to the nucleus . Herein noteworthy point , After receptors-mediated endocytosis process resulting it has been proposed that there are mechanismsrtpermanentlyf) downregulating incoming all antecedent signals are strong enough to shut down signaling completely without additional signal- transducing mechanisms .Considering that nAChRs are expressed in many regions of central and peripheral nervous system and a7nAChR is present in various non neuronal tissues as lung cells , epithelial cells , fibroblasts , endothelial cells , blood cells , gila and all types of immune cells , antecedent mechanisms which downregulate incoming signals permanently likely have an integral key role in terminating asthma types , chest allergy and atopic dermatitis permanently . These mechanisms sequently are attributed to nAChRs internalization induced by heterologous desensitization resulted in prolonged nAChRs exposure to low concentration of a 7nAChR agonist (L) anabsine .
Chemical Structure DepictionAnabasine
Claims
Claims
1) Current medicament normalizes and treats all asthmatics types , patients of chest allergy and patients of atopic dermatitis to have a permanent cure after one medication course .
2) Current medicament is comprising of (L)(-) Anabasine or its salt as an active ingredient and a pharmacologically acceptable excipient , diluent or carrier .
3) Medicament is formulated for administering (L)(-) Anabasine by oral route at about 0.03 mg /kg to 2 mg / kg of body weight
4) Medicament at mentioned doses is described to be administered by oral route twice per day for a period from 30 : 40 days for asthmatics and patients of chest allergy according to severity and condition development and from 21: 40 days for patients of atopic dermatitis according to severity and condition development . Herein medication is one course only .
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EG2019081276 | 2019-08-15 | ||
| EG2019081276 | 2019-08-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2021028005A1 true WO2021028005A1 (en) | 2021-02-18 |
Family
ID=74571262
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/EG2019/000032 Ceased WO2021028005A1 (en) | 2019-08-15 | 2019-12-30 | A medicament comprising anabasine for treatment of asthma, chest allergy and atopic dermatits |
Country Status (1)
| Country | Link |
|---|---|
| WO (1) | WO2021028005A1 (en) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1992015306A1 (en) * | 1991-03-01 | 1992-09-17 | University Of Florida | Use of nicotinic analogs for treatment of degenerative diseases of the nervous system |
| GB2381750A (en) * | 2001-10-10 | 2003-05-14 | Inspire Pharmaceuticals Inc | Treatment for enhancing joint lubrication |
-
2019
- 2019-12-30 WO PCT/EG2019/000032 patent/WO2021028005A1/en not_active Ceased
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1992015306A1 (en) * | 1991-03-01 | 1992-09-17 | University Of Florida | Use of nicotinic analogs for treatment of degenerative diseases of the nervous system |
| GB2381750A (en) * | 2001-10-10 | 2003-05-14 | Inspire Pharmaceuticals Inc | Treatment for enhancing joint lubrication |
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