4'-SENESIOILOXYOSTOL COMPOUND FOR USE AS AN ANTI-INFLAMMATORY AGENT

Abstract

The present invention relates to the use of the active substance 4'-senesioiloxyostol, obtained from natural sources, as an anti-inflammatory agent and to pharmaceutical formulations containing this agent.

Description

4'-SENESIOILOXYOSTOL FOR USE AS AN ANTI-INFLAMMATORY AGENT. COMPOUND Technical Area The present invention involves the production of the active substance 4'-senesioiloxyostol from natural sources. This relates to its use as an anti-inflammatory agent and to pharmaceutical formulations containing this agent. State of the Art Inflammatory diseases are a common medical problem, affecting various parts of the body. It can affect these areas. Currently, traditional chemical anti-inflammatory agents are widely used. It is used to treat diseases caused by inflammation. However, although Although currently considered the best option, these chemical agents have an effect on the body. It can have negative side effects. As an alternative to chemical agents, natural products derived from plants and plants Anti-inflammatory agents can be used to treat these conditions, but without the negative side effects. It has the potential to be highly effective. Examples of natural anti-inflammatory agents include: It contains omega-3 fatty acids, which are found in ginger, turmeric, and fish oil. Despite the availability of various anti-inflammatory agents, diseases associated with inflammation still persist. New agents that can effectively treat this are needed. This is because a single agent cannot achieve this. It is not effective for all such situations and some people have reactions to certain agents. It is possible to demonstrate this. In addition, research into the mechanisms related to these diseases continues. As we do this, we target specific pathways related to inflammation, including LOX enzyme inhibition, or The need for new agents to target these mechanisms is inevitable. One of the mechanisms of action of anti-inflammatory agents is the LOX (lipoxygenase) enzyme. It is the inhibition of LOX. LOX plays a role in the production of inflammatory mediators, and inhibiting this enzyme... It can reduce inflammation in the body. Therefore, LOX enzyme inhibition activity is new. This is an important consideration when developing anti-inflammatory agents. 2 Taking into account their known technical knowledge and the needs mentioned above, inventors, a naturally derived anti-inflammatory agent for the treatment of inflammation-related diseases They have developed an anti-inflammatory agent suitable for the invention, obtained from plants or plant sources. It is produced and has the potential to be as effective as chemical agents, but has known negative side effects. They have no side effects or have less toxicity and / or side effects compared to their chemical counterparts. The invention also provides an alternative for individuals who may have reactions or sensitivities to certain substances. by providing an option and causing inflammation, including LOX enzyme inhibition. Targeting specific pathways or mechanisms leads to a surge in interest in new anti-inflammatory agents. It meets the need. Brief Description of the Invention Taking into account the known problems in the technique described above, the inventors have developed a system to reduce inflammation. 4'- for use as an anti-inflammatory agent in the treatment of diseases caused by senesioiloxyostol as the active ingredient and, optionally, at least one pharmaceutical ingredient. They have developed pharmaceutical compounds containing usable excipients. Detailed Description of the Invention The present invention provides an active substance for use as a drug in the treatment of inflammatory diseases. as 4'-senesioiloxyostol (Formula I) and optionally accepted as at least one pharmaceutical. This relates to pharmaceutical compositions containing excipients. Formula I 3 The inventors created the enzyme using 4'-senesioiloxyostol at a concentration of 20 µg / ml. In inhibition studies, the active ingredient 4'-senesioiloxyostol, consistent with the invention, inhibited the LOX enzyme. They found that it inhibited it by 40%. Even among known chemically derived anti-inflammatory agents, there are those that can inhibit the LOX enzyme. Due to the limited number of agents available, compounds containing 4'-senesioiloxyostol are considered an anti-inflammatory agent. This makes the technical benefit obtained by using it even more valuable. The inflammatory diseases mentioned within the scope of this invention are inflammatory diseases of the nervous system. diseases, inflammatory diseases of the cardiovascular system, respiratory system inflammatory diseases, inflammatory diseases of the digestive system, inflammatory diseases of the skin systems inflammatory diseases, inflammatory diseases of the musculoskeletal system, urinary system inflammatory diseases, inflammatory diseases of the reproductive system, endocrine system These could be inflammatory diseases or inflammatory diseases of the lymphatic system. Here, we discuss inflammatory diseases of the nervous system such as encephalitis, myelitis, meningitis, and neuritis. Dacryoadenitis, scleritis, episcleritis, keratitis, retinitis, chorioretinitis, blepharitis, conjunctivitis, uveitis, external Examples include ear infection, middle ear infection, labyrinthitis, and mastoiditis. Here, we will discuss inflammatory diseases of the cardiovascular system such as carditis and myocarditis. Examples include endocarditis, pericarditis, vasculitis, arteritis, phlebitis, and capillaritis. Here, we discuss inflammatory diseases of the respiratory system such as sinusitis, rhinitis, pharyngitis, and laryngitis. Examples include bronchitis, bronchiolitis, pneumonia, pleuritis, tracheitis, and mediastinitis. Here, we discuss inflammatory diseases of the digestive system such as stomatitis, gingivitis, and gingivostomatitis. tonsillitis, glossitis, sialadenitis, parotitis, cheilitis, pulpitis, gnathitis, esophagitis, gastritis, gastroenteritis, enteritis, colitis, enterocolitis, duodenitis, ileitis, typhitis, appendicitis, proctitis, hepatitis, pancreatitis, cholecystitis, cholangitis, Peritonitis can be included. Here, we discuss inflammatory diseases of the skin system such as dermatitis, folliculitis, cellulitis, and hidradenitis. countable. Here, we will discuss inflammatory diseases of the musculoskeletal system such as arthritis, dermatomyositis, and myositis. synovitis, tenosynovitis, bursitis, enthesitis, fasciitis, capsulitis, epicondylitis, tendinitis, panniculitis, Examples include osteochondritis, osteitis, osteomyelitis, spondylitis, periostitis, and chondritis. 4 Here, we discuss inflammatory diseases of the urinary system such as nephritis, glomerular nephritis, and pyelonephritis. Examples include ureteritis, cystitis, and urethritis. Here, we discuss inflammatory diseases of the reproductive system such as oophoritis, salpingitis, and endometritis. parametritis, cervicitis, vaginitis, vulvitis, mastitis, orchitis, epididymitis, prostatitis, seminal vesiculitis, balanitis, Examples include posthitis, balanoposthitis, chorioamnionitis, funisitis, and omphalitis. Here, we discuss inflammatory diseases of the endocrine system such as insulinitis, pituitaryitis, and thyroiditis. Examples include parathyroiditis and adrenalitis. Here, lymphangitis and lymphadenitis can be mentioned as inflammatory diseases of the lymphatic system. The subject of this invention is pharmaceutical compositions containing the active ingredient 4'-senesioiloxyostol. in the treatment of at least one, some, or all of the previous inflammatory diseases For use only. A preferred application of the invention is 4'-senesioiloxyostol as the active ingredient and optionally... a pharmaceutical containing at least one excipient that can be considered a pharmaceutical compounds LOX, COX-1, COX-2, NO, PGE2 in the treatment of inflammatory diseases This relates to the use of inhibitor agents, especially preferably LOX inhibitor agents. The invention also relates to pharmaceutical compounds containing 4'-senesioiloxyostol as the active ingredient. It is my relationship. The compounds subject to the invention, in addition to 4'-senesioiloxyostole, are considered pharmaceutically. It may contain at least one excipient. This excipient is pharmaceutical. well-known in technology, in the preparation of the formulation, its bioavailability and / or lacking any therapeutic activity that would be beneficial in regulating its release It can be selected from among the items. Pharmaceutical compositions suitable for the invention may be chosen taking into account the patient's physical condition, the type of disease, or related factors. It can be prepared in different pharmaceutical forms, taking similar conditions into consideration. The terms "treatment" or "therapeutic activity" mentioned within the scope of the invention refer to the duration of treatment. shortening of the duration of recovery, acceleration of healing, disappearance of at least one symptom of the illness, a reduction in at least one symptom of the condition, a decrease in inflammation, inflammation disappearance, decrease in the level of the relevant inflammation marker, or the inflammation marker itself. disappearance or inflammation markers within the limits normally accepted It means returning to a level where it will remain within. 5 In the context of the invention, the word "containing" is also used in the sense of "encompassing". Where technically feasible, applications of the invention may be combined. EXAMPLES 1 Sample 1: X-NMR analysis bulks of 4'-senesioyloxyostol ethanol Formula I 1 H NMR (400 MHz, CDCl δ ppm: 7.61 (1H, d, J = 9.5 Hz, H-4); 7.30 (1H, d, J = 3 8.7 Hz, H-5); 6.82 (1H, d, J = 8.7 Hz, H-6); 6.23 (1H, d, J = 9.5 Hz, H-3); 5.72 (2H, q, J = 1.0 Hz, H 2”); 5.51 (1H, br t, J = 7.7 Hz, H-2'); 4.87 (2H, s, H-4'); 3.90 (3H, s, OMe); 3.62 (2H, d, J = 7.7 Hz, H-1'); 2.19 (3H, d, J = 1.0 Hz, H-4”); 1.89 (3H, d, J =1.0 Hz, H-5”); 1.72 (3H, s, H- 5').

Claims

1. 4'- as an active ingredient for use as a drug in the treatment of inflammatory diseases. The compound senesioyloxyostol (formula I). Formula I 2. The inflammatory diseases mentioned are inflammatory diseases of the nervous system, Inflammatory diseases of the cardiovascular system, inflammatory diseases of the respiratory system diseases, inflammatory diseases of the digestive system, inflammatory diseases of the skin systems diseases, inflammatory diseases of the musculoskeletal system, inflammatory diseases of the urinary system diseases, inflammatory diseases of the reproductive system, inflammatory diseases of the endocrine system Use according to Claim 1, which includes diseases or inflammatory diseases of the lymphatic system. for the compound 4'-senesioiloxyostol (formula I).

3. The aforementioned inflammatory diseases of the nervous system include encephalitis, myelitis, meningitis, neuritis, Dacryoadenitis, scleritis, episcleritis, keratitis, retinitis, chorioretinitis, blepharitis, conjunctivitis, uveitis, Use according to Claim 2 for conditions such as external ear infection, middle ear infection, labyrinthitis, and mastoiditis. for the compound 4'-senesioiloxyostol (formula I).

4. The aforementioned inflammatory diseases of the cardiovascular system include carditis and myocarditis. For use according to Claim 2, which includes endocarditis, pericarditis, vasculitis, arteritis, phlebitis, and capillaryitis. 4'-senesioiloxyostol (formula I) compound.

5. The aforementioned inflammatory diseases of the respiratory system include sinusitis, rhinitis, pharyngitis, laryngitis, Use according to Request 2 for bronchitis, bronchiolitis, pneumonia, pleuritis, tracheitis, and mediastinitis. 4'-senesioiloxyostol (formula I) compound. 7 6. The aforementioned inflammatory diseases of the digestive system include stomatitis and gingivitis. gingivostomatitis, tonsillitis, glossitis, sialadenitis, parotitis, cheilitis, pulpitis, gnathitis, esophagitis, gastritis, gastroenteritis, enteritis, colitis, enterocolitis, duodenitis, ileitis, typhitis, appendicitis, proctitis, hepatitis, According to Request 2, for use in cases of pancreatitis, cholecystitis, cholangitis, and peritonitis, 4'- The compound senesioyloxyostol (formula I).

7. Inflammatory diseases of the aforementioned skin systems include dermatitis, folliculitis, and cellulitis. The compound 4'-senesioiloxyostol (formula I) is intended for use as hidradenite according to Claim 2.

8. The aforementioned inflammatory diseases of the musculoskeletal system include arthritis and dermatomyositis, myositis, synovitis, tenosynovitis, bursitis, enthesitis, fasciitis, capsulitis, epicondylitis, tendinitis, panniculitis, According to Claim 2, osteochondritis, osteitis, osteomyelitis, spondylitis, periostitis, chondritis are present. 4'-senesioiloxyostol (formula I) compound for use.

9. The aforementioned inflammatory diseases of the urinary system include nephritis, glomerular nephritis, pyelonephritis, For use in cases of ureteritis, cystitis, or urethritis according to Claim 2, 4'-senesioiloxyostol (formula I) compound.

10. The aforementioned inflammatory diseases of the reproductive system include oophoritis, salpingitis, and endometritis, parametritis, cervicitis, vaginitis, vulvitis, mastitis, orchitis, epididymitis, prostatitis, seminal vesiculitis, According to Claim 2, the condition is balanitis, posthitis, balanoposthitis, chorioamnionitis, funiitis, and omphalitis. 4'-senesioiloxyostol (formula I) compound for use.

11. The aforementioned inflammatory diseases of the endocrine system include insulinitis, pituitaryitis, thyroiditis, 4'-senesioiloxyostol (formula I) for use according to Claim 2 for parathyroiditis and adrenalitis. compound.

12. The inflammatory diseases of the lymphatic system mentioned are lymphangitis and lymphadenitis. 4'-senesioiloxyostol (formula I) compound for use according to claim 2.