Novel pyrrolopyrimidine derivatives

Abstract

The group of inventions relates to the field of the chemical-pharmaceutical industry, medicine and pharmacology, and concerns novel pyrrolopyrimidine derivatives, and also pharmaceutical compositions and medicaments containing said derivatives, which exhibit a high level of activity against autoimmune diseases and viral infections.

Description

[0001] NEW PYRROLOPYRIMIDINE DERIVATIVES

[0002] The invention relates to the field of chemical-pharmaceutical industry and medicine, and represents new derivatives of pyrrolopyrimidines.

[0003] LEVEL OF TECHNOLOGY

[0004] Autoimmune diseases affect 8-10% of the world's population, often young adults and children, who are susceptible to various immune system disorders. Autoimmune diseases are associated with dysfunction of the human immune system, which begins to perceive its own tissues as foreign and damage them. These disorders arise for various reasons, including, to a large extent, environmental factors and the aggressiveness of components in food, air, and water. Autoimmune diseases include rheumatoid arthritis, systemic lupus erythematosus, scleroderma, multiple sclerosis, atopic dermatitis, alopecia, and others.

[0005] Rheumatoid arthritis is a chronic inflammatory disease primarily associated with joint damage, leading to irreversible changes manifested in the degradation of cartilage and bone tissue and, subsequently, the weakening of muscles, ligaments, and tendons. The disease is caused by autoimmune inflammation, characterized by the immune system's attack on the body's own cells. In addition to joint damage, rheumatoid arthritis often affects internal organs such as blood vessels, the nervous system, kidneys, heart, and lungs. Timely diagnosis and treatment can help prevent irreversible complications.However, the treatment of rheumatoid arthritis requires a systematic approach based on a combination of supportive therapy (smoking cessation, balance of rest and exercise, therapeutic exercise, healthy sleep, diet, analgesics), drugs that slow the progression of the disease, and, if necessary, non-steroidal anti-inflammatory drugs.

[0006] The etiology of rheumatoid arthritis is complex due to its multifactorial nature [Skogoreva N.V., Makeeva A.V. Pathophysiological characteristics of rheumatoid arthritis: etiology, pathogenesis, and treatment principles. - 2015]. The disease can be caused by genetic predisposition, environmental factors, bad habits, infections, stress, and excessive physical activity. How infection leads to chronic joint inflammation is currently unknown. Rheumatoid arthritis may develop as a result of prolonged persistence of the pathogen in the joints or the accumulation of its waste products in the synovial membrane. It is possible that when joint tissue is damaged by infection, new antigens appear, triggering an immune response, thereby developing an autoimmune inflammation process.In addition, rheumatoid arthritis may be based on molecular mimicry (similarity between foreign and self-antigens), as a result of which, during the immune response to the pathogen's antigens, antibodies to the autoantigens of the joints are produced.

[0007] The treatment of rheumatoid arthritis is based on a combination of symptomatic and basic therapy. Basic therapy drugs have been used in rheumatology for over 30 years [Nasonov E.L. Use of tumor necrosis factor inhibitors in rheumatoid arthritis: the place of etanercept / / Scientific and practical rheumatology. - 2008. - No. 5. - Pp. 1-20]. Basic therapy includes antitumor and cytostatic drugs: Methotrexate, Leflunomide, Sulfasalazine, Chrysanol, Tauredon, Plaquenil. Modern methods of basic treatment also involve the use of biological drugs, such as Infliximab, Rituximab, Abatacept, Anakinra. Symptomatic drugs include glucocorticoids and non-steroidal anti-inflammatory drugs aimed at reducing pain and increasing joint mobility.Among the non-steroidal anti-inflammatory drugs are Celecoxib, Diclofenac, Lornoxicam, Movalis, Arcoxia, Nimesulide, Ibuprofen, and among the glucocorticoids are Dexamethasone, Triamcinolone, Prednisolone, Betamethasone.

[0008] By targeting the molecular mechanisms of autoimmune inflammation, we can more effectively combat the symptoms of rheumatoid arthritis and achieve sustained remission with timely therapy. An example of a modern approach to therapy is the use of Baricitinib, which acts by inhibiting cytokine signaling pathways through the reversible inhibition of enzymes known as Janus kinases (JAKs), specifically JAK1 and JAK2. JAK kinases are important growth factors and intercellular components of cytokine signaling pathways. JAK kinases phosphorylate and activate signal transducers and activators of transcription (STATs), which translocate to the nucleus and induce transcription of effector genes [Leonard WJ, O'Shea JJ Jaks and STATs: biological implications / / Annual review of immunology. - 1998. - V. 16. - P. 293; McInnes IB et al.Comparison of baricitinib, upadacitinib, and tofacitinib mediated regulation of cytokine signaling in human leukocyte subpopulations / / Arthritis Research & Therapy. - 2019. - Vol. 21. - No. 1. - Pp. 1-10]. The JAK family belongs to the non-receptor cytoplasmic protein tyrosine kinases (PTKs), including four types: JAK1, JAK2, JAK3, and TYK2 (tyrosine kinase 2) [McInnes I. B. et al. Comparison of baricitinib, upadacitinib, and tofacitinib mediated regulation of cytokine signaling in human leukocyte subpopulations / / Arthritis Research & Therapy. - 2019. - Vol. 21. - No. 1. - Pp. 1-10]. JAK1 has attracted considerable attention since being identified as a promising target for antirheumatoid arthritis drugs. Furthermore, other inflammatory conditions are closely linked to JAK / STAT signaling [Gao H. et al. Study on the binding mode of a pyrrolotriazine derivative with JAK2 by docking and MD simulation / / Molecular Simulation. - 2019. - Vol. 45. - No. 3. - Pp. 230-238].

[0009] Baricitinib's efficacy has been demonstrated in mouse models of colorectal rheumatoid arthritis and other autoimmune diseases such as atopic dermatitis and alopecia [Fridman JS et al. Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050 / / The Journal of Immunology. - 2010. - Vol. 184. - No. 9. - Pp. 5298-5307; Hoy SM Baricitinib: a review in moderate to severe atopic dermatitis / / American journal of clinical dermatology. - 2022. - Vol. 23. - No. 3. - Pp. 409-420; Kwon O. et al. Efficacy and safety of baricitinib in patients with severe alopecia areata over 52 weeks of continuous therapy in two phase III trials (BRAVE-AA1 and BRAVE-AA2) / / American Journal of Clinical Dermatology. - 2023. - T. 24. - No. 3. - pp. 443-451].

[0010] In addition to its use in the treatment of autoimmune diseases, baricitinib has other applications. Recently, baricitinib became the first immunomodulatory drug for the treatment of COVID-19 to receive approval from the Food and Drug Administration [Rubin R. Baricitinib is first approved COVID-19 immunomodulatory treatment / / JAMA. - 2022. - Vol. 327. - No. 23. - Pp. 2281-2281].

[0011] One of the main manifestations of a viral disease is a cytokine storm associated with an excessive inflammatory response. The inhibitory effect of Baricitinib on Janus kinases leads to a decrease in cytokine activity and, as a consequence, suppression of inflammatory processes [Roskoski Jr R. Janus kinase (JAK) inhibitors in the treatment of inflammatory and neoplastic diseases / / Pharmacological research. - 2016. - Vol. 111. - Pp. 784-803]. In addition, there is an assumption that Baricitinib can block the entry of the SARS-CoV-2 virus into cells by inhibiting the AP2-associated kinase pathway, which is necessary for the endocytosis of the virus into cells [Stebbing J. et al. The mechanism of baricitinib supports artificial intelligence-predicted testing in COVID-19 patients / / EMBO molecular medicine. - 2020. - Vol. 12. - No. 8. - C. el2697].Indeed, baricitinib has gained particular notoriety for its use in COVID-19 treatment, including approval for use in combination with other active agents, such as remdesivir. Numerous studies have shown that baricitinib can reduce mortality and improve clinical outcomes in patients with severe viral infections, particularly those caused by RNA viruses.

[0012] Along with high activity among the qualities of Baricitinib, negative manifestations are also noted in the form of side effects expressed in an increase in LDL (low density lipoprotein) (33.6%), upper respiratory tract infection (14.7%), nausea (2.8%), impaired fertility, manifestation of teratogenicity and embryolethality. Cases of anemia [Deprez V. et al. Therapeutic Maintenance of Baricitinib and Tofacitinib in Real Life / / Journal of Clinical Medicine. - 2020. - T. 9. - No. 10. - P. 3319], palmoplantar rash [Koumaki D. et al. Palmoplantar pustulosis-like eruption induced by baricitinib for the treatment of rheumatoid arthritis / / European Journal of Case Reports in Internal Medicine. - 2020], psoriasis [Di Domizio J. et al. Baricitinib-induced paradoxical psoriasis / / Journal of the European Academy of Dermatology and Venereology. - 2020. - T. 34. - No. 8. - pp. e391-e393].The prior art also reports a risk of thrombosis with the use of JAK inhibitors, in particular Baricitinib [Faquetti M. L. et al. Identification of novel off targets of baricitinib and tofacitinib by machine learning with a focus on thrombosis and viral infection / / Scientific reports. - 2022. - Vol. 12. - No. 1. - Pp. 1-11].

[0013] Also known in the prior art are attempts to create baricitinib analogues with similar activity and a number of favorable pharmaceutical properties. For example, such analogues are disclosed in patent RU2601410, the compound of which was selected by the authors as the closest analogue to the present invention.

[0014] It's important to note that even modern medications for autoimmune diseases do not increase life expectancy or prevent early disability. For example, despite treatment, only 10% of patients experience a benign course of rheumatoid arthritis with rare exacerbations. In 65-70%, the disease is characterized by slow but steady progression with frequent exacerbations and incomplete remissions. The remainder develop a "malignant" course with multiple joint lesions, resistance to drug therapy, and severe, potentially fatal organ dysfunction.

[0015] The development of modern, affordable approaches to treating autoimmune diseases, as well as new agents capable of slowing their progression, is currently a pressing issue of high social significance. However, delayed diagnosis and inappropriate treatment of autoimmune diseases have a devastating impact on the health, life expectancy, and quality of life of patients, leading to complete loss of ability to work and irreversible disability.

[0016] The development of new molecules active in the treatment of autoimmune diseases and viral infections opens up opportunities to improve the physicochemical, technological, and pharmacological characteristics of pharmaceutical products. This expands the range of active agents available to drug developers when developing a new drug with improved properties. Sustainable development of modern approaches to the synthesis of new active agents enables the implementation of environmentally friendly, resource-efficient, and atom-saving innovative technologies in production, which contribute to economic development and minimize environmental impact.

[0017] The discovery of the possibility of selective inhibition of cytokine signaling pathways using reversible inhibition of JAK enzymes has expanded the possibilities of therapy for autoimmune diseases and viral infections.

[0018] Thus, there is currently an urgent need to develop new active agents with improved profiles of physicochemical, technological and pharmacological properties for the treatment of autoimmune diseases and viral infections.

[0019] In connection with the Decree of the President of the Russian Federation of May 7, 2024 No. 309 "On the national development goals of the Russian Federation for the period up to 2030 and for the prospect of 2036" within the framework of the import substitution program "Pharma-2030", the authors of the present invention have made efforts aimed at strengthening technological sovereignty in the pharmaceutical industry, to create an innovative product based on new derivatives of pyrrolopyrimidines that exhibit high activity in the treatment of autoimmune diseases and viral infections.

[0020] According to Order No. 514n of the Russian Ministry of Health "On Approval of the Criteria for Classifying Goods, Works, and Services as Innovative and High-Tech Products for the Purposes of Forming a Procurement Plan for Such Products," the novel pyrrolopyrimidine derivatives of the present invention satisfy a set of criteria that classify the present inventions as innovative products. These compounds differ significantly from their closest analogues and possess improved properties. Furthermore, the method for producing these compounds utilizes new technologies, intermediates, and materials. Consequently, the compounds and methods for their preparation according to the present invention meet the criteria for scientific and technical novelty.

[0021] This group of inventions is also science-intensive, applied, and has practical applications. In the future, with the use of highly skilled intellectual labor and the results of intellectual activity, it will be actively implemented in the domestic chemical and pharmaceutical industries. Furthermore, the price of new medicinal products based on this invention, with improved efficacy, will be significantly lower than that of similar products currently available in the Russian Federation, thereby achieving a positive economic effect from product sales in the Russian Federation.

[0022] It should also be noted that, in accordance with the above-mentioned Order of the Ministry of Health of the Russian Federation No. 514n, the present group of inventions pertains to high-tech products, since it corresponds to the priority areas of development of science, technology and engineering in the Russian Federation, namely, biomedical and veterinary technologies (in accordance with the Decree of the President of the Russian Federation of July 7, 2011 No. 899 "On approval of priority areas of development of science, technology and engineering in the Russian Federation and the list of critical technologies of the Russian Federation"), is manufactured and carried out by enterprises of knowledge-intensive sectors of the economy, namely, pharmaceutical and chemical; is manufactured and carried out using the latest samples of technological equipment, technological processes and technologies with the participation of highly qualified, specially trained personnel.

[0023] DISCLOSURE OF THE ESSENCE OF THE INVENTION

[0024] The objective of the present invention was to create new pyrrolopyrimidine derivatives exhibiting high activity against autoimmune diseases and viral infections.

[0025] The inventors of the present invention have obtained and studied new pyrrolopyrimidine derivatives, in a particular embodiment of the invention, compounds of formulas (A - C, A" - C") and their pharmaceutically acceptable salts, which have improved activity and selectivity compared to analogs with respect to autoimmune diseases, in particular with respect to the inhibition of JAK enzymes, as well as viral infections, while the inventors have succeeded in achieving an improved safety profile, which is expressed, among other things, in a reduction in the undesirable effects from taking the new pyrrolopyrimidine derivatives of the present invention, such as, among other things, impaired fertility, teratogenicity and embryolethality. Studies of the properties of the new pyrrolopyrimidine derivatives within the framework of the present invention have made it possible to establish their improved physicochemical and technological properties.

[0026]

[0027] New derivatives of pyrrolopyrimidine.

[0028]

[0029] Particular cases of new pyrrolopyrimidine derivatives, namely 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile (A), 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile (B), 2-(3-(4-(7H-pyrrolo[2,3- ]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanoyl)azetide yn-3-yl)acetonitrile (C).

[0030] The compounds of the present invention, including their salts, can be prepared according to the general synthesis scheme described below: R,

[0031] I

[0032] la base;, base;

[0033] la palladium organo

[0034]

[0035] catalyst; organic solvent

[0036] solvent / water

[0037] R, R] - protective groups

[0038] 0 Y = C|-Sb-alkylene, Z = -O-(C|-Sb-alkyl) or -8-(C]-Sb-

[0039]

[0040] alkyl) Scheme of synthesis of pyrrolopyrimidine derivatives according to the present invention.

[0041] The compounds of the present invention, including their salts, can be prepared according to the general synthesis scheme described below:

[0042]

[0043] catalyst; organic solvent

[0044] solvent / water Xi - acid residue R, R] - protective groups

[0045]

[0046] Scheme of synthesis of pyrrolopyrimidine derivatives according to the present invention.

[0047] The compounds of the invention, including their salts, can be prepared according to the general synthesis scheme described below.

[0048] NM-'L, CN HX, VV- 7 N — N

[0049] organic,,

[0050] For' R

[0051]

[0052] catalyst; solvent; organic solvent

[0053] X] - acid residue solvent / water

[0054] R, R] - protective group

[0055] o 5a, B X = V C y y = -(CH2CH2)-, Z = -OCH3;

[0056] O

[0057]

[0058] 6th, С Х^ Y = -(CHjCH?)-, Z = -SCH3;

[0059] Scheme of synthesis of new derivatives of pyrrolopyrimidines A - C. In the first stage, 4-(1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidine (1a), protected at the amino group of the pyrrole ring, was obtained. For this purpose, the calculated amount of 4-chloro-7H-pyrrolo[2,3-d]pyrimidine (I) protected at the amino group of the pyrrole ring, 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole and a base (preferably alkali or alkaline earth metal carbonates or phosphates, tertiary amines, in particular aliphatic ones, more preferably sodium carbonate) were loaded into a mixture of a water-miscible organic solvent (more preferably dioxane, acetone, acetonitrile) and purified water in a weight ratio of 1:10 to 10:1. The reaction vessel was evacuated and filled with an inert gas. Then a palladium catalyst (more preferably Pd(PPh3)4) was added and the mixture was boiled for 8 to 48 h (more preferably 16 h).The reaction mixture was diluted with a water-immiscible solvent (more preferably ethyl acetate) and purified water. The organic layer was separated, dried over sodium sulfate and concentrated on a rotary evaporator. An organic solvent (more preferably methyl tert-butyl ether (MTBE), diisopropyl ether, diethyl ether, tetrahydrofuran (THF), methyltetrahydrofuran, heptane, hexane) was added to the residue and kept at 2-10 °C (more preferably at 4 °C) for 2-24 h (more preferably overnight). Formation of a precipitate was observed. The separated precipitate was filtered, washed with an organic solvent (more preferably MTBE, diisopropyl ether, diethyl ether, THF, methyltetrahydrofuran, heptane, hexane) and dried.

[0060] In the second stage, the synthesis of the amino-protected pyrrole and pyrazole ring 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-azetidineacetonitrile (2a) was carried out. For this purpose, an organic solvent (more preferably acetonitrile, acetone, methanol, dimethylformamide) and a catalyst, for example, an organic base (preferably alkyl substituted guanidine, quaternary ammonium base), were added to the calculated amount of the amino-protected pyrrole ring 4-(1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidine (1a) and the amino-protected pyrazole ring 2-(3-azetidinylidene)acetonitrile. The resulting mixture was stirred for 8-48 h (preferably 16 h) at 10-50 °C (preferably at room temperature). The reaction mixture was concentrated on a rotary evaporator. The residue was dissolved in a water-immiscible organic solvent (preferably ethyl acetate) and washed with purified water.The organic layer was separated, dried over sodium sulfate and concentrated on a rotary evaporator.

[0061] In the third step, the protective group of the pyrazole ring of the amino-protected pyrrole and pyrazole ring of 3-[4-(7H-pyrrolo[2,3-]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-azetidineacetonitrile (2a) was removed according to methods known from the prior art [Wuts P. G. M., Greene T. W. Greene's Protective Groups in Organic Synthesis. - John Wiley & Sons, 2006.] to obtain the amino-protected pyrrole ring of 3-[4-(7H-pyrrolo[2,3-]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-azetidineacetonitrile (3a).

[0062] At the fourth stage, the synthesis of products 4a was carried out ; 5a ;6a. For this purpose, a base (preferably a tertiary amine, pyridine or quinoline derivatives, more preferably triethylamine) and an oxycarboxylic acid derivative (more preferably 3-methoxypropionic acid, 2-(methylthio)acetic acid, 3-(methylthio)propionic acid) were added to a solution of the calculated amount of the amino-protected pyrrole ring of 3-[4-(7H-pyrrolo[2, 3-d]pyrimidine-4-yl)-1H-pyrazol-1-yl]-3-azetidineacetonitrile (3a) in an aprotic organic solvent (more preferably dichloromethane, tetrahydrofuran, acetone). The reaction mixture was stirred at 10-50 °C (more preferably at room temperature) for 8-48 h (more preferably 16 h). It was then diluted with purified water. The organic layer was separated, dried over sodium sulfate, and concentrated on a rotary evaporator. The product was isolated by silica gel column chromatography.

[0063] At the fifth stage, the synthesis of products A, B, C was carried out. For this, a reaction was carried out to remove the protective group of the pyrrole ring of compound 4a, 5a or 6a, in accordance with methods known from the prior art [Wuts P. G. M., Greene T. W. Greene's protective groups in organic synthesis. - John Wiley & Sons, 2006].

[0064] To obtain a salt of any of compounds A, B, or C, a calculated amount of acid in a protic organic solvent or water, or a mixture thereof, was added to a solution of the calculated amount of any of compounds A, B, or C in the calculated amount of a protic organic solvent or water, or a mixture thereof. The reaction mixture was stirred at 5-70 °C (more preferably at room temperature) for 1-24 h (more preferably for two hours). Upon completion of the reaction, the precipitate was filtered or the reaction mixture was evaporated, and the residue was dried under reduced pressure (0.1-0.8 atm) at a temperature of 5-70 °C (more preferably at room temperature).

[0065] and the compounds according to the invention, including their salts, can also be obtained according to the general synthesis scheme described below.

[0066] o 5, B X =, Y = -(CH2CH2)-, Z = -OSH,;

[0067] ABOUT

[0068]

[0069] 6, C X = V Cy, Y = -(СН2СН2)-, Z = -SCH3

[0070] Scheme of synthesis of new derivatives of pyrrolopyrimidines A - C.

[0071] In the first step, 4-(1H-pyrazol-4-yl)-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidine (1) was obtained. For this, the calculated amount of 4-chloro-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidine (I), 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole and a base (preferably alkali or alkaline earth metal carbonates or phosphates, tertiary amines, in particular aliphatic ones, more preferably sodium carbonate) were loaded into a mixture of a water-miscible organic solvent (more preferably dioxane, acetone, acetonitrile) and purified water in a weight ratio of 1:10 to 10:1. The reaction vessel was evacuated and filled with an inert gas. A palladium catalyst (preferably Pd(PPh3)4) was then added, and the mixture was refluxed for 8–48 h (preferably 16 h). The reaction mixture was diluted with a water-immiscible solvent (preferably ethyl acetate) and purified water.The organic layer was separated, dried over sodium sulfate and concentrated on a rotary evaporator. An organic solvent (more preferably methyl tert-butyl ether (MTBE), diisopropyl ether, diethyl ether, tetrahydrofuran (THF), methyltetrahydrofuran, heptane, hexane) was added to the residue and kept at 2-10 °C (more preferably at 4 °C) for 2-24 h (more preferably overnight). Formation of a precipitate was observed. The formed precipitate was filtered, washed with an organic solvent (more preferably MTBE, diisopropyl ether, diethyl ether, THF, methyltetrahydrofuran, heptane, hexane) and dried.

[0072] In the second stage, tert-butyl 3-(cyanomethyl)-3-(4-(7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)azetidine-1-carboxylate (2) was synthesized. For this purpose, a polar organic solvent (preferably acetonitrile, acetone, methanol, dimethylformamide) and a strong organic base (preferably alkyl substituted guanidine, quaternary ammonium base) were added to the calculated amount of 4-(1H-pyrazol-4-yl)-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidine (1) and tert-butyl 3-(cyanomethylene)azetidine-1-carboxylate. The resulting mixture was stirred for 8-48 h (preferably 16 h) at 10-50 °C (preferably at room temperature). The reaction mixture was concentrated on a rotary evaporator. The residue was dissolved in a water-immiscible organic solvent (preferably ethyl acetate) and washed with purified water.The organic layer was separated, dried over sodium sulfate and concentrated on a rotary evaporator.

[0073] At the third stage, the synthesis of 2-(3-(4-(7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)azetidin-3-yl)acetonitrile salt (3) was carried out. For this purpose, a solution of an acid with a concentration of 0.5 - 30 May was added to a solution of the calculated amount of tert-butyl 3 -(cyanomethyl)-3-(4-(7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)azetidine-1-carboxylate (2) in the calculated amount of an aprotic organic solvent (more preferably THF, ethyl acetate, acetonitrile). % (preferably hydrohalic acid, sulfuric acid derivatives, sulfuric acid, trifluoroacetic acid) in an aprotic organic solvent (more preferably dioxane, acetone, acetonitrile) in a molar ratio of compound 2 to acid of 1:1 - 1:100, and stirred for 8 - 48 (more preferably 16 h) at 10 - 50 °C (more preferably at room temperature). The reaction mixture was concentrated on a rotary evaporator.

[0074] At the fourth stage, the synthesis of products 4 5 6 was carried out. For this purpose, a base (preferably a tertiary amine, pyridine or quinoline derivatives, more preferably triethylamine) and a derivative of an oxycarboxylic acid (more preferably 3-methoxypropionic acid, 2-(methylthio)acetic acid, 3-(methylthio)propionic acid) were added to a solution of the calculated amount of 2-(3-(4-(7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2, 3 -d]pyrimidin-4-yl)-1H-pyrazol-1-yl)azetidin-3-yl)acetonitrile salt (3 ) in an aprotic organic solvent (more preferably dichloromethane, tetrahydrofuran, acetone). The reaction mixture was stirred at 10-50°C (preferably at room temperature) for 8-48 h (preferably 16 h). The mixture was then diluted with purified water. The organic layer was separated, dried over sodium sulfate, and concentrated on a rotary evaporator. The product was isolated by column chromatography on silica gel.

[0075] At the fifth stage, the synthesis of products A, B, C was carried out. For this, trifluoroacetic acid was added to a solution of the calculated amount of one of 4, 5, 6 in the calculated amount of an aprotic organic solvent (more preferably dichloromethane, tetrahydrofuran, acetonitrile). The reaction mass was stirred at 5-50 °C (more preferably at room temperature) for 0.5-5 h (more preferably 2 h), then concentrated on a rotary evaporator. The residue was dissolved in an aliphatic alcohol (more preferably methanol, ethanol, isopropanol, propanol). A solution of ammonia (3-25 wt.%) in purified water was added, and the mixture was stirred at 5-50 °C (more preferably at room temperature) for 8-48 h (more preferably 16 h). The resulting solution was concentrated on a rotary evaporator. The residue was diluted with purified water and acidified if necessary (preferably with potassium hydrogen sulfate (KHSO4)) to 4–6 (pH=4).Stirred at 5-50 °C (more preferably at room temperature) for 6-24 h (more preferably overnight). Formation of a precipitate was observed. The precipitate was filtered, concentrated if necessary and chromatographed on silica gel, washed with purified water and / or diethyl ether and dried. To obtain a salt of any of compounds A, B, C, to a solution of the calculated amount of any of compounds A, B, C in the calculated amount of a protic organic solvent or water was added the calculated amount of a solution of hydrochloric acid in a protic organic solvent or water. The reaction mass was stirred at 5-70 °C (more preferably at room temperature) for 1-24 h (more preferably for two hours). Upon completion of the reaction, the precipitate was filtered or the reaction mixture was evaporated, the residue was dried under reduced pressure (0.1-0.8 atm), at a temperature of 5-70 °C (more preferably at room temperature).

[0076] , Y" = -(CH2CH2)-, Z" = -OSH;;

[0077] ABOUT* В " X ” '< S y. Y" - -(СН2)-, Z"- -SCH3;

[0078] , Y" - -(СН2СН2)-, Z" - -SCH3;

[0079] and their pharmaceutically acceptable salts

[0080]

[0081] New derivatives of pyrrolopyrimidine.

[0082]

[0083] Particular cases of new derivatives of pyrrolopyrimidines, namely 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile (A' '), 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetide-3-yl)acetonitrile (B ”), 2-(3-(4-(7H-pyrrolo[2,3- ]pyrimidin-4-yl)-1H-pyrazol-1 -yl)- 1 -((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile (C”).

[0084] The compounds of the present invention, including their salts, can be prepared according to the general synthesis scheme described below:

[0085] catalyst; solvent

[0086]

[0087] organic solvent / water

[0088] R, R ] - protective groups

[0089]

[0090] where X" = -° Y" is C1-C6-alkylene, Z" is -O-(C1-C6-alkyl) or -8-(C]-C'6-alkyl)

[0091] Scheme of synthesis of pyrrolopyrimidine derivatives according to the present invention.

[0092] The compounds of the present invention, including their salts, can be prepared according to the general synthesis scheme described below: HN— N

[0093]

[0094] palladium organophosphate

[0095]

[0096] catalyst; solvent

[0097]

[0098] 2a solvent

[0099] organic

[0100] solvent / water X] - acid residue R, R | - protective groups

[0101] X- os acid residue where X" = Y" -• Ci-C6-alkylene, Z" = -O-(C]-C6-alkyl) or -8-(C]-C(,-alkyl)

[0102]

[0103] Scheme of synthesis of pyrrolopyrimidine derivatives according to the present invention.

[0104] The compounds of the present invention, including their salts, can be prepared according to the following synthesis scheme:

[0105]

[0106] base;

[0107] palladium

[0108]

[0109] catalyst; organic solvent

[0110] solvent / water

[0111] X| is the acid residue R, R] are the protective groups 4a", 5a", 6a" X2 is the acid residue

[0112] o...,0 4a", A" X" -, Y" = -(СН2СН2)-, Z" = -ОСН3;

[0113] O..,£> 5a", B" X” =, Y" = -(СН2)-, Z" = -SCH3;

[0114] Oh, Oh

[0115]

[0116] 6a", C" X" = % S y, Y "= -(СН2СН2)-, Z" = -SCH3Scheme of synthesis of new derivatives of pyrrolopyrimidines A” - C”.

[0117] In the first step, 4-(1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidine (1a) protected at the amino group of the pyrrole ring was obtained. For this, the calculated amount of 4-chloro-7H-pyrrolo[2,3-d]pyrimidine (I) protected at the amino group of the pyrrole ring, 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole and a base (preferably alkali or alkaline earth metal carbonates or phosphates, tertiary amines, in particular aliphatic ones, more preferably sodium carbonate) were loaded into a mixture of a water-miscible organic solvent (more preferably dioxane, acetone, acetonitrile) and purified water in a weight ratio of 1:10 to 10:1. The reaction vessel was evacuated and filled with an inert gas. A palladium catalyst (preferably Pd(PPh3)4) was then added, and the mixture was refluxed for 8–48 h (preferably 16 h). The reaction mixture was diluted with a water-immiscible solvent (preferably ethyl acetate) and purified water.The organic layer was separated, dried over sodium sulfate and concentrated on a rotary evaporator. An organic solvent (more preferably methyl tert-butyl ether (MTBE), diisopropyl ether, diethyl ether, tetrahydrofuran (THF), methyltetrahydrofuran, heptane, hexane) was added to the residue and kept at 2-10 °C (more preferably at 4 °C) for 2-24 h (more preferably overnight). Formation of a precipitate was observed. The formed precipitate was filtered, washed with an organic solvent (more preferably MTBE, diisopropyl ether, diethyl ether, THF, methyltetrahydrofuran, heptane, hexane) and dried.

[0118] In the second stage, the synthesis of the amino-protected pyrrole and pyrazole ring 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-azetidineacetonitrile (2a) was carried out. For this purpose, an organic solvent (more preferably acetonitrile, acetone, methanol, dimethylformamide) and a catalyst, for example, an organic base (preferably alkyl substituted guanidine, quaternary ammonium base), were added to the calculated amount of the amino-protected pyrrole ring 4-(1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidine (1a) and the amino-protected pyrazole ring 2-(3-azetidinylidene)acetonitrile. The resulting mixture was stirred for 8-48 h (preferably 16 h) at 10-50 °C (preferably at room temperature). The reaction mixture was concentrated on a rotary evaporator. The residue was dissolved in a water-immiscible organic solvent (preferably ethyl acetate) and washed with purified water.The organic layer was separated, dried over sodium sulfate and concentrated on a rotary evaporator.

[0119] In the third step, the protecting group of the pyrazole ring of the amino-protected pyrrole and pyrazole ring of 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-azetidineacetonitrile (2a) was removed according to methods known from the prior art [Wuts P. G. M., Greene T. W. Greene's Protective Groups in Organic Synthesis. - John Wiley & Sons, 2006.] to obtain the amino-protected pyrrole ring of 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-azetidineacetonitrile (3a).

[0120] At the fourth stage, the synthesis of products 4a” 5a” was carried out ;6a”. For this purpose, a base (preferably a tertiary amine, pyridine or quinoline derivatives, more preferably triethylamine) and a sulfonyl chloride derivative or an activated thiocarboxylic acid derivative (more preferably 2-methoxyethane-1-sulfonyl chloride, 2-(methylthio)ethane-1-sulfonyl chloride, (methylthio)methanesulfonyl chloride, benzenemethanesulfonyl chloride) were added to a solution of the calculated amount of the amino-protected pyrrole ring of 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-azetidineacetonitrile (3a) in an aprotic organic solvent (more preferably dichloromethane, tetrahydrofuran, acetone). The reaction mixture was stirred at 10-50 °C (more preferably at room temperature) 8–48 h (preferably 16 h). The mixture was then diluted with purified water. The organic layer was separated, dried over sodium sulfate, and concentrated on a rotary evaporator. The product was isolated by column chromatography on silica gel.

[0121] At the fifth stage, the synthesis of products A”, B”, C” was carried out. For this, a reaction of removing the protective group of the pyrrole ring of compound 4a”, 5a” or 6a” was carried out in accordance with methods known from the prior art [Wuts P. G. M., Greene T. W. Greene's protective groups in organic synthesis. - John Wiley & Sons, 2006].

[0122] To obtain a salt of any of the compounds A”, B”, C”, the calculated amount of acid in a protic organic solvent or water, or a mixture thereof, was added to a solution of the calculated amount of any of the compounds A”, B”, C” in the calculated amount of a protic organic solvent or water, or a mixture thereof. The reaction mixture was stirred at 5-70 °C (more preferably at room temperature) for 1-24 h (more preferably for two hours). Upon completion of the reaction, the precipitate was filtered or the reaction mixture was evaporated, the residue was dried under reduced pressure (0.1-0.8 atm), at a temperature of 5-70 °C (more preferably at room temperature).

[0123] The compounds of the invention, including their salts, can also be prepared according to the general synthesis scheme described below:

[0124]

[0125] X] is the acid residue X2 is the acid residue

[0126] o,. "O 4", A" X" =, Y" = -(СН2СН2)-, Z" = -ОСН3;

[0127] O.. "O 5", B" X" =, Y" = -(СН2)-, Z"= -SCH3;

[0128] Oh...Oh

[0129]

[0130] 6”, C" X" = ■x s y, Y" = -(СН2СН2)-, Z" = -SCH3.

[0131] Scheme of synthesis of new derivatives of pyrrolopyrimidines A” - C”.

[0132] In the first step, 4-(1H-pyrazol-4-yl)-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidine (1) was obtained. For this, the calculated amount of 4-chloro-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidine (I), 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole and a base (preferably alkali or alkaline earth metal carbonates or phosphates, tertiary amines, in particular aliphatic ones, more preferably sodium carbonate) were loaded into a mixture of a water-miscible organic solvent (more preferably dioxane, acetone, acetonitrile) and purified water in a weight ratio of 1:10 to 10:1. The reaction vessel was evacuated and filled with an inert gas. A palladium catalyst (preferably Pd(PPh3)4) was then added, and the mixture was refluxed for 8–48 h (preferably 16 h). The reaction mixture was diluted with a water-immiscible solvent (preferably ethyl acetate) and purified water.The organic layer was separated, dried over sodium sulfate and concentrated on a rotary evaporator. An organic solvent (more preferably methyl tert-butyl ether (MTBE), diisopropyl ether, diethyl ether, tetrahydrofuran (THF), methyltetrahydrofuran, heptane, hexane) was added to the residue and kept at 2-10 °C (more preferably at 4 °C) for 2-24 h (more preferably overnight). Formation of a precipitate was observed. The formed precipitate was filtered, washed with an organic solvent (more preferably MTBE, diisopropyl ether, diethyl ether, THF, methyltetrahydrofuran, heptane, hexane) and dried.

[0133] In the second stage, tert-butyl 3-(cyanomethyl)-3-(4-(7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)azetidine-1-carboxylate (2) was synthesized. For this purpose, a polar organic solvent (preferably acetonitrile, acetone, methanol, dimethylformamide) and a strong organic base (preferably alkyl substituted guanidine, quaternary ammonium base) were added to the calculated amount of 4-(1H-pyrazol-4-yl)-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidine (1) and tert-butyl 3-(cyanomethylene)azetidine-1-carboxylate. The resulting mixture was stirred for 8-48 h (preferably 16 h) at 10-50 °C (preferably at room temperature). The reaction mixture was concentrated on a rotary evaporator. The residue was dissolved in a water-immiscible organic solvent (preferably ethyl acetate) and washed with purified water.The organic layer was separated, dried over sodium sulfate and concentrated on a rotary evaporator.

[0134] At the third stage, the synthesis of 2-(3-(4-(7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)azetidin-3-yl)acetonitrile salt (3) was carried out. For this purpose, a solution of an acid with a concentration of 0.5 - 30 May was added to a solution of the calculated amount of tert-butyl 3 -(cyanomethyl)-3-(4-(7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)azetidine-1-carboxylate (2) in the calculated amount of an aprotic organic solvent (more preferably THF, ethyl acetate, acetonitrile). % (preferably hydrohalic acid, sulfuric acid derivatives, sulfuric acid, trifluoroacetic acid) in an aprotic organic solvent (more preferably dioxane, acetone, acetonitrile) in a molar ratio of compound 2 to acid of 1:1 - 1:100, and stirred for 8 - 48 (more preferably 16 h) at 10 - 50 °C (more preferably at room temperature). The reaction mixture was concentrated on a rotary evaporator.

[0135] At the fourth stage, the synthesis of products 4”, 5”, 6” was carried out. For this purpose, a base (preferably a tertiary amine, pyridine or quinoline derivatives, more preferably triethylamine) and a sulfochloride derivative or an activated thiocarboxylic acid derivative (more preferably 2-methoxyethane-1-sulfonyl chloride, 2-(methylthio)ethane-1-sulfonyl chloride, (methylthio)methanesulfonyl chloride, benzenesulfonyl chloride). The reaction mixture was stirred at 10-50 °C (more preferably at room temperature) for 8-48 h (more preferably 16 h). Then it was diluted with purified water. The organic layer was separated, dried over sodium sulfate, and concentrated on a rotary evaporator.The product was isolated by column chromatography on silica gel.

[0136] At the fifth stage, the synthesis of products A”, B”, C” was carried out. For this, trifluoroacetic acid was added to a solution of the calculated amount of one of 4”, 5”, 6” in the calculated amount of an aprotic organic solvent (more preferably dichloromethane, tetrahydrofuran, acetonitrile). The reaction mass was stirred at 5-50 °C (more preferably at room temperature) for 0.5-5 h (more preferably 2 h), then concentrated on a rotary evaporator. The residue was dissolved in an aliphatic alcohol (more preferably methanol, ethanol, isopropanol, propanol). A solution of ammonia (3-25 wt.%) in purified water was added, stirred at 5-50 °C (more preferably at room temperature) for 8-48 h (more preferably 16 h). The resulting solution was concentrated on a rotary evaporator. The residue was diluted with purified water and acidified if necessary (preferably with potassium hydrogen sulfate (KHSO4)) to 4–6 (pH=4).The mixture was stirred at 5–50°C (preferably at room temperature) for 6–24 h (preferably overnight). A precipitate was observed to form. The precipitate was filtered, concentrated if necessary, and chromatographed on silica gel, washed with purified water and / or diethyl ether, and dried.

[0137] To obtain a salt of any of the compounds A”, B”, C”, a calculated amount of an acid, including hydrochloric acid, in a protic organic solvent or water was added to a solution of a calculated amount of any of the compounds A”, B”, C” in a calculated amount of a protic organic solvent or water. The reaction mixture was stirred at 5-70 °C (more preferably at room temperature) for 1-24 hours (more preferably for two hours). Upon completion of the reaction, the precipitate was filtered or the reaction mixture was evaporated, the residue was dried under reduced pressure (0.1-0.8 atm), at a temperature of 5-70 °C (more preferably at room temperature). The terms used in the description of the present invention are given below. Unless otherwise specified, all technical and special terms used in the description have the meaning generally accepted in the art.

[0138] In the context of the present invention, the term “pharmaceutically acceptable excipient” characterizes substances of inorganic or organic origin used in the process of production and manufacture of medicinal products to impart the necessary physicochemical properties to them.

[0139] The term "pharmaceutical composition" in the context of the present invention means a substance that includes a therapeutically active agent and at least one of pharmaceutically acceptable and pharmacologically compatible excipients, such as, but not limited to, fillers, solubilizers, solvents, co-solvents, antioxidants, buffering agents, cryoprotectants, diluents, preservatives, stabilizers, humectants, emulsifiers, lubricants, lubricants, glidants, suspending agents, thickeners, binding agents, sweeteners, flavorings, effervescent agents, flavorings, antibacterial agents, fungicides, prolonged delivery regulators, isotonic agents, pH regulating agents, the choice and ratio of which depends on the nature, purpose and dosage of the therapeutically active agent.

[0140] Non-limiting examples of suspending agents include ethoxylated isostearyl alcohol, polyoxyethylene, sorbitol, and sorbitol ester, as well as mixtures of these substances. Stabilizers that can be used, but are not limited to, include mannitol, microcrystalline cellulose, sodium carboxymethylcellulose, polyvinylpyrrolidone, colloidal silicon dioxide, polysorbate 80, sodium croscarmellose, and sodium lauryl sulfate.

[0141] The following may be used as antioxidants in the pharmaceutical composition: mannitol, ascorbic acid, tocopherol, β-carotene, lycopene.

[0142] The following may be used as fillers in the pharmaceutical composition: starch, glucose, sucrose, lactose, magnesium oxide, sodium chloride, sodium bicarbonate, kaolin, cellulose derivatives, calcium carbonate, dextrin, sorbitol, sodium croscarmellose, hydroxypropyl methylcellulose, magnesium stearate.

[0143] Protection of a pharmaceutical composition from the action of microorganisms can be ensured by using a variety of antibacterial and antifungal agents, such as sorbic acid, parabens (methylparaben, propylparaben, ethylparaben, butylparaben, isobutylparaben, isopropylparaben, benzylparaben, heptylparaben and mixtures thereof), chlorobutanol and similar compounds.

[0144] The pharmaceutical composition may include, but is not limited to, sugars, sodium chloride, sodium bicarbonate, etc. as isotonic agents. The prolonged action of the pharmaceutical composition may be ensured, but is not limited to, by using agents that slow down the absorption of the active agent (for example, hydrophilic and hydrophobic polymeric release retardants).

[0145] Non-limiting (illustrative) examples of suitable fillers include lactose, various types of starch, mannitol, microcrystalline cellulose, calcium carbonate and phosphate, etc.

[0146] Solvents and diluents that can be used include, but are not limited to, water, organic esters suitable for parenteral forms, ethanol, polyalcohols, and mixtures thereof. Examples of lubricants include, but are not limited to, magnesium or calcium stearate, talc, sodium lauryl sulfate, and sodium stearyl fumarate. Lubricants that can include, but are not limited to, silicon dioxide, talc, kaolin, bentonites, and others. Various organic and inorganic acids or alkalis can be used to adjust pH, such as, but not limited to, hydrochloric acid, malic acid, ascorbic acid, citric acid, acetic acid, succinic acid, tartaric acid, fumaric acid, lactic acid, aspartic acid, glutaric acid, glutamic acid, sorbic acid, sodium hydroxide, and the like. Examples of dispersing agents and spreading agents are starch, alginic acid and its salts, silicates.

[0147] The pharmaceutical composition can be administered to animals and humans orally, parenterally (intradermally, subcutaneously, intramuscularly, intravenously, intraarterially, into cavities), sublingually, locally, including but not limited to ocular, nasal administration, etc., rectally in a standard form of administration, in the form of a mixture with traditional pharmaceutical carriers. Suitable standard forms of administration include (without limitation) oral forms: tablets, capsules, pellets, granules, powders, solutions, solutions for spraying in the mouth and nose, syrups, suspensions, etc., oral: solutions, suspensions, emulsions, concentrates for the preparation of injection and infusion dosage forms, aerosols and powders for inhalation administration, pulmonary powders (powders for spraying using an inhaler directly into the lungs), powders and lyophilisates for the preparation of injection and infusion dosage forms; rectal: suppositories, capsules, etc.; eye drops.The term "pharmaceutically acceptable" in the context of the present invention means that the substance or composition to which the term is applied must be chemically and / or toxicologically compatible with the other ingredients of the preparation and safe for the person being treated with the substance or composition.

[0148] "Pharmaceutically acceptable salt" in the context of the present invention means relatively safe and non-toxic organic and inorganic salts of the acids and bases claimed in the present invention.

[0149] The term "medicinal product" in the context of the present invention characterizes substances or combinations thereof that come into contact with the human or animal body, penetrate the organs and tissues of the human or animal body, and are used for the prevention or treatment of diseases. Medicinal products include drugs in the form of finished dosage forms intended for administration to the animal or human body by various routes, such as, but not limited to, orally, sublingually, topically, rectally, and parenterally.

[0150] The term "pharmaceutical substance" or "substance" in the context of the present invention means a product of synthesis, which is any substance or mixture of substances of synthetic or other (biological, biochemical, mineral, plant, animal, microbial, and other) origin, intended for the production of pharmaceutical compositions and medicinal products, which, during the production process of a medicinal product (preparation), becomes the active ingredient of this medicinal product and determines its effectiveness. Such substances are intended to exhibit pharmacological activity or another direct effect in the diagnosis, treatment, symptomatic relief, or prevention of disease and symptomatic relief, or to affect the structure or function of the body.

[0151] The term “comprising”, “comprises” in the context of the present invention means that the said pharmaceutical substances, pharmaceutical compositions and medicinal products include the listed components, but do not exclude the inclusion of other components.

[0152] The term "effective amount" in the context of the present invention means an amount of a substance (as well as a combination of substances) that, when administered to a subject for the treatment or prevention of a disease, or at least one of the clinical symptoms of a disease or disorder, is sufficient to achieve the effect of such treatment and / or prevention on the disease, disorder or symptom. An "effective amount" is determined depending on the disease, disorder and / or symptoms of the disease or disorder, the severity of the disease, disorder and / or symptoms of the disease or disorder, the clinical picture and general health of the patient, as well as the age and / or weight of the subject requiring such treatment (prevention).

[0153] The term "dosage" as used herein characterizes the content of one or more active agents in quantitative terms per unit dose, or unit volume, or unit mass in accordance with the medicinal product, or for some types of medicinal products, the amount of active agent released from the medicinal product per unit time.

[0154] The term "powder" used here means a state of matter in which the solid substance or substances that comprise it are in a free dispersed system without a dispersion medium with a dispersion phase in the form of solid particles of various shapes.

[0155] The terms “approximately” and “about” used in the text mean approximately plus or minus ten percent of the specified value.

[0156] The term "impurities" in the context of the present invention refers to any component of a pharmaceutical substance that is not an active agent. The quality indicator of a pharmaceutical substance characterizes the content of impurities in the pharmaceutical substance that were introduced during its synthesis, both production (process impurities) and related impurities, as well as those formed during degradation during storage, and is expressed as a percentage. Sources of impurities may include reagents used in the synthesis of starting materials, catalysts, process equipment, filter material residues, and insufficiently purified raw materials used in the synthesis of pharmaceutical substances.

[0157] The term “physicochemical properties of substances” in the context of the present invention characterizes the density, shape, size and nature of the surface of particles, the specific surface of particles, the forces of adhesion (sticking together on the surface) and cohesion (sticking together of particles inside the body), surface activity, melting point, solubility, hygroscopicity, stability, reactivity of substances, etc.

[0158] Solubility, in the context of the present invention, characterizes the ability of a substance to form homogeneous systems with other substances—solutions in which the substance exists as individual atoms, ions, molecules, or particles. Solubility is expressed as the concentration of the dissolved substance in its saturated solution, either as a percentage or in units of weight or volume, referred to g or cm 3 (ml) of solvent (e.g. g / 100 g, or cm 3 / 100 cm 3 , or g / ml).

[0159] The term "autoimmune diseases," as used herein, refers to a class of diseases in which the body's immune system mistakenly identifies its own cells, tissues, or organs as foreign and attacks them, resulting in damage and destruction of normal tissue and the development of autoimmune inflammation. Examples of autoimmune diseases include, but are not limited to, rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, type 1 diabetes mellitus, Guillain-Barré syndrome, chronic inflammatory demyelinating polyneuropathy, psoriasis, Graves' disease, Hashimoto's thyroiditis, myasthenia gravis, scleroderma, and vasculitis.

[0160] The term "immunomodulator," as used herein, describes a group of biologically active substances that influence the immune system or participate in its functioning. This class of immunomodulators includes immunosuppressants (substances that suppress the immune response) and immunostimulants (substances that enhance the immune response, activate immune cells, increase antibody production, and improve the body's ability to fight infections and diseases).

[0161] Stability is the ability of a medicinal product to maintain its properties and quality characteristics within specified limits over a specified shelf life and period of use, under established storage conditions. Medicinal product stability is essential for ensuring its therapeutic effect or the absence of new adverse reactions.

[0162] Depending on the preserved properties and quality characteristics, the following types of drug stability are distinguished:

[0163] - chemical stability, which maintains the chemical integrity and activity of the active substance within the limits specified in the specification;

[0164] - physical stability, which preserves the original physical properties of the drug, including appearance, taste, homogeneity, solubility, suspensibility, etc.;

[0165] - microbiological stability, which maintains the sterility or microbiological purity of the medicinal product in accordance with the specified requirements, or the effectiveness of the antimicrobial preservatives included in its composition within the specified limits; - toxicological stability, which does not significantly increase the toxicity of the medicinal product;

[0166] - therapeutic stability, in which the therapeutic effect of the drug remains unchanged.

[0167] The term “technological properties of substances” in the context of the present invention characterizes the bulk density, degree of compaction, flowability, moisture, fractional composition, dispersion, porosity, pressability of substances, etc.

[0168] For the preparation of the novel pyrrolopyrimidine derivatives of the present invention, the following solvents known in the art, their deuterated derivatives or mixtures thereof can be used: alcohols such as methanol, ethanol, n-propanol, isopropanol, n-butanol, 2-butanol, isobutanol, tert-butanol, amyl alcohol and its isomers, cyclohexanol, benzyl alcohol, ethylene glycol, 1,2-propanediol, 1,3-propanediol, ketones such as acetone, butanone, methyl isobutyl ketone, 2-hexanone, cyclopentanone, cyclohexonone, ethers such as ethyl formate, methyl acetate, ethyl acetate, n-propyl acetate, isopropyl acetate, n-butyl acetate, isobutyl acetate, ethylene glycol diacetate, propylene glycol diacetate, Glycerol triacetate, diethyl ether, diisopropyl ether, dibutyl ether, tetrahydrofuran, methyltetrahydrofuran, dioxane, anisole, methyl tert-butyl ether, ethyl tert-butyl ether, cyclopentyl methyl ether, dimethoxyethane, diethoxymethane, diglyme, lactones such as butyrolactone, valerolactone, hydrocarbons such as n-pentane,n-hexane, n-heptane, n-octane, cyclohexane, methylcyclohexane, benzene, toluene, xylenes, cumene, tetralin, limonene, turpentine, halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, 1,2-dichloroethane, 1, 1-dichloroethylene, cis-dichloroethylene, trans-dichloroethylene, 1,1,2-trichloroethylene, 1,1,1-trichloroethane, 1-chlorobutane, chlorobenzene, dichlorobenzene, aprotic polar solvents such as acetonitrile, propionitrile, dimethylformamide, dimethylacetamide, N-methylpyrrolidone, dimethylolethylene urea, dimethylolpropylene urea, dimethyl sulfoxide, sulfolane, nitromethane, bifunctional solvents such as methoxyethanol, ethoxyethanol, 1-methoxypropan-2-ol, furfuryl alcohol, tetrahydrofurfuryl alcohol, ethyl lactate, protic solvents such as water, acids such as formic acid, acetic acid, propionic acid, trifluoroacetic acid, methanesulfonic acid, trifluoromethanesulfonic acid, anhydrides such as acetic anhydride, ammonia, amines,such as pyridine, triethylamine, as well as supercritical fluids such as carbon dioxide, water, methane, ethane, propane, ethylene, propylene, methanol, ethanol, acetone, nitrogen oxides, sulfur oxide. The term "alkyl" in the context of the present invention refers to a saturated hydrocarbon group with a straight or branched chain. Examples of alkyl groups include methyl, ethyl, propyl (e.g., n-propyl and isopropyl), butyl (e.g., n-butyl, isobutyl, sec-butyl, tert-butyl), pentyl (e.g., n-pentyl, isopentyl, tert-pentyl, neopentyl), etc. An alkyl group may contain from 1 to about 20, from 2 to about 20, from 1 to about 10, from 1 to about 8, from 1 to about 6, from 1 to about 4, or from 1 to about 3 carbon atoms.

[0169] The term "alkylene" as used herein refers to divalent saturated aliphatic radicals (e.g., ethylene) wherein the free valences are located at different carbon atoms.

[0170] The term "aliphatic" in the context of the present invention refers to hydrocarbons that do not contain rings.

[0171] The term "compound" in the context of the present invention includes all stereoisomers, geometric isomers, tautomeric forms, salts, hydrates, solvates, clathrates, anhydrides, unsolvated forms, and isotopic forms. The compounds of the invention, including their salts, can be prepared using known methods of organic synthesis and by any of numerous possible synthetic routes.

[0172] The term "tautomeric forms" in the context of the present invention refers to compounds formed by the displacement of a double bond into the location of an adjacent single bond with the accompanying migration of a proton. Tautomeric forms include prototropic tautomers, which are isomeric protonation states that have the same empirical formula and overall charge.

[0173] The term "isotopic forms" in the context of the present invention refers to forms of compounds that include all possible isotopes of the atoms present in the compound or its precursor. Isotopes include atoms that have the same atomic number but different mass numbers.

[0174] The term "room temperature" in the context of the present invention means a temperature that approximately corresponds to the temperature in the room where the reaction or process is carried out, for example, a temperature of from about 20 to about 30°C.

[0175] The term "purified water," as used herein, refers to an excipient or component for preparing medicinal products for use, for use in synthesis as a reagent or solvent, or for cleaning containers, equipment, and primary packaging materials. Purified water is produced using methods such as ion exchange, reverse osmosis or two-stage reverse osmosis, ultrafiltration, and / or electrodeionization, as well as distillation from water that meets drinking water quality requirements. Drinking water quality requirements are established by the Sanitary Rules and Regulations (SanPiN) "Drinking Water. Hygienic Requirements for Water Quality in Centralized Drinking Water Systems. Quality Control."

[0176] The term "organic solvent" in the context of the present invention means a substance of organic origin that has the ability to dissolve various compounds.

[0177] The term "polar organic solvent" in the context of the present invention means a class of organic solvents that have the ability to dissolve polar compounds. Polar organic solvents include, but are not limited to, alcohols, in particular methanol, ethanol, propanol, isopropanol, butanol, ketones, in particular acetone, methyl ethyl ketone, acids, in particular formic acid, acetic acid, tetrahydrofuran, ethyl acetate, dimethylformamide, acetonitrile, dimethyl sulfoxide, nitromethane, acetonitrile, ethylene glycol, nitrobenzene, N-methylpyrrolidone.

[0178] The term "non-polar organic solvent" in the context of the present invention refers to a class of organic solvents capable of dissolving non-polar compounds. Non-polar organic solvents include, but are not limited to, hexane, benzene, toluene, chloroform, dichloromethane, diethyl ether, diisopropyl ether, dibutyl ether, and dioxane.

[0179] The term "protic organic solvent" in the context of the present invention means a class of organic solvents containing a hydrogen atom capable of dissociating as a proton. Protic organic solvents include, but are not limited to, alcohols, in particular methanol, ethanol, propanol, isopropanol, butanol, acids, in particular formic acid, acetic acid, The term "aprotic organic solvent" in the context of the present invention means a class of organic solvents that do not contain a hydrogen atom capable of dissociating as a proton. Aprotic organic solvents include, but are not limited to, hexane, benzene, toluene, dioxane, chloroform, diethyl ether, dichloromethane, tetrahydrofuran, ethyl acetate, acetone, dimethylformamide, acetonitrile, dimethyl sulfoxide.

[0180] The term "water-miscible solvent" in the context of the present invention refers to a class of solvents miscible with water. Water-miscible solvents include, but are not limited to, tetrahydrofuran, methanol, isopropanol, ethanol, dioxane, dimethyl sulfoxide, dimethylformamide, acetonitrile, and acetone.

[0181] The term "water-immiscible solvent" in the context of the present invention refers to a class of solvents that are immiscible with water. Water-miscible solvents include, but are not limited to, toluene, pentane, methyl ethyl ketone, methyl tert-butyl ether, isooctane, hexane, heptane, diethyl ether, ethyl acetate, dichloromethane, dichloroethane, cyclohexane, chloroform, carbon tetrachloride, butanol, and benzene.

[0182] The term "base" in the context of the present invention means organic or inorganic compounds capable of accepting a proton. Organic bases include, but are not limited to, pyridine and its derivatives, in particular collidine, 2,6-lutidine, ammonium derivatives, in particular tributylamine, triethylamine, imidazole and its derivatives, benzimidazole and its derivatives, histidine, guanidine, in particular 1,1,3,3-tetramethylguanidine (TMG), phosphazenes, 1,5,7-triazabicyclo(4.4.0)dec-5-ene (TBD), 7-methyl-1,5,7-triazabicyclo(4.4.0)dec-5-ene (MTBD), 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU), 1,5-diazabicyclo[4.3.0]non-5-ene (DBN), quinuclidine, 2,2,6,6-tetramethylpiperidine (TMP), pempidine, 1,4-diazabicyclo[2.2.2]octane. Inorganic bases include, but are not limited to, ammonia or its solutions in water, soluble and slightly water-soluble hydroxides of alkali and alkaline earth metals, amides, carbonates, and bicarbonates.Strong inorganic bases include water-soluble alkali and alkaline earth metal hydroxides and amides. Weak inorganic bases include ammonium hydroxide, sparingly soluble metal hydroxides, carbonates, and bicarbonates.

[0183] The term "palladium catalyst" in the context of the present invention means compounds with catalytic activity containing palladium, or palladium. Palladium catalysts include, but are not limited to, tetrakis(triphenylphosphine)palladium, bis[1,2-bis(diphenylphosphino)ethane]palladium, dichlorobis(methyldiphenylphosphine)palladium, palladium on carbon, and palladium(II) acetate (palladium acetate).

[0184] The term "hydrohalic acid" in the context of the present invention means an acid selected from hydrofluoric, hydrochloric, hydrobromic, hydroiodic.

[0185] BRIEF DESCRIPTION OF THE DRAWINGS The present invention is further illustrated by Fig. 1.1, Fig. 1.2, Fig. 2.1 and Fig. 2.2.

[0186] Fig. 1.1 and Fig. 1.2 show the average severity of symptoms of arthritis induced by collagen antibodies across experimental groups.

[0187] Fig. 2.1 and Fig. 2.2 show the average levels of cytokine activity in lung tissue and bronchoalveolar fluid across the experimental groups.

[0188] IMPLEMENTATION OF THE INVENTION

[0189] The stated problem is solved, and the claimed technical result is achieved due to a compound selected from a group including compounds characterized by formula (I):

[0190] (Ri)'

[0191]

[0192] or its pharmaceutically acceptable salt,

[0193] where (X)', (Y)' independently of each other represent -CH or N; a = 1, 2, 3, 4, 5;

[0194] b = 1, 2, 3, 4, 5;

[0195] (Ri)', R2, independently of each other, represent a group A or B, where A represents a branched or unbranched alkyl, cycloalkyl, alkenyl (an unsaturated hydrocarbon with a double bond), a branched or unbranched hydrocarbon chain, a branched or unbranched alkyloxy, a branched or unbranched alkylthio, a heterocycle or aryl;

[0196] B is hydroxy, mercapto, amino, halogen, azido, nitroso, nitro, nitrile, cyano, diazo, sulfo, COR3, SO3R3, C(NR6)NR4R5, OOR7, NR4R5, NHNHR3, NNR3, (NO)NR3, CH(NR3)R3, (SO)R3, SO2R3, SO(NR4)R3; R3 is any one of A, hydrogen, hydroxy, halogen, OM (where M = metal or ammonium cation), NR4R5;

[0197] R4, R5 independently of each other represent any of A;

[0198] Re represents any of A;

[0199] R7 represents any of A or hydrogen;

[0200] wherein A may be substituted by one or more substituents selected from A or B.

[0201] The stated problem is solved, and the claimed technical result is achieved due to a compound selected from a group including compounds characterized by formula (I):

[0202] (Ri)'

[0203]

[0204] or its pharmaceutically acceptable salt,

[0205] where (X)', (Y)' independently of each other represent -CH- or -N-;

[0206] a = 1, 2 or 3;

[0207] b = 1, 2 or 3;

[0208] (Ri)' is A, mercapto, -C(O)R3, -C(NR6)NR4R5, -NR4R5, -NHNHR3, -NNR3, -CH(NR3)R3, -SO2R3, or -SO3R3;

[0209] R3 is any of A, hydrogen, hydroxy, halogen, or NR4R5;

[0210] R4, R5 Re independently of each other represent any of A;

[0211] A is C3-C6-cycloalkyl, C4-C6-heterocycle, C4-C6-aryl, branched or unbranched C1-C6-alkyl, branched or unbranched C1-C6-alkyloxy (-O-C1-6-alkyl), branched or unbranched C1-C6-alkylthio (-S-C1-6-alkyl), or branched or unbranched C2-C6-alkenyl; R-2 is any of A, hydroxy, mercapto, amino, halogen, azido, nitroso, nitro, nitrile, cyano, diazo, sulfo, -C(O)R3, -C(NR6)NR4R5, -NR4R5, -NHNHR3, -NNR3, CH(NR3)R3, -SO2R3, or -SO3R3,

[0212] wherein A may be substituted by one or more substituents selected from A, hydroxy, mercapto, amino, halogen, azido, nitroso, nitro, nitrile, cyano, diazo, sulfo, -C(O)R3, -C(NR6)NR4R5, -NR4R5, -NHNHR3, -NNR3, CH(NR3)R3, -SO2R3, and -SO3R3.

[0213] The stated problem is solved and the claimed technical result is achieved by a compound selected from the group including compounds characterized by formula (I)', or its pharmaceutically acceptable salt,

[0214] where (X)', (Y)' independently of each other represent -CH- or -N-;

[0215] a = 1; b = 1;

[0216] (Ri)' is A, -C(O)R3, -SO2R3, or -SO3R3;

[0217] R3 represents any of A;

[0218] A is branched or unbranched Ci-C6-alkyl, branched or unbranched Ci-C6-alkyloxy (-O-Ci-6-alkyl), branched or unbranched Ci-C6-alkylthio (-S-Ci-6-alkyl), or branched or unbranched Cr-C6-alkenyl;

[0219] R2 is any one of A, hydroxy, mercapto, amino, halogen, azido, nitroso, nitro, nitrile, cyano, diazo, sulfo, -C(O)R3, -C(NR6)NR4R5, -NR4R5, -NHNHR3, -NNR3, CH(NR3)R3, -SO2R3, or -SO3R3,

[0220] wherein A may be substituted by one or more substituents selected from A, hydroxy, mercapto, amino, halogen, azido, nitroso, nitro, nitrile, cyano, diazo, sulfo, -C(O)R3, -C(NR6)NR4R5, -NR4R5, -NHNHR3, -NNR3, CH(NR3)R3, -SO2R3, and -SO3R3.

[0221] The stated problem is solved and the claimed technical result is achieved by a compound selected from the group including compounds characterized by formula (I)', or its pharmaceutically acceptable salt,

[0222] where (X)' represents -N-, (Y)' represents -CH-;

[0223] a = 1; b = 1;

[0224] (Ri)' is A, -C(O)R3, -SO2R3, or -SO3R3;

[0225] R3 represents any of A;

[0226] A is branched or unbranched C-C6-alkyl, branched or unbranched C-C6-alkyloxy (-O-Ci-6-alkyl), branched or unbranched C-C6-alkylthio (-S-Ci-6-alkyl), or branched or unbranched Cr-C6-alkenyl;

[0227] R2 represents any of A,

[0228] wherein A is substituted with one or more substituents selected from A, hydroxy, mercapto, amino, halogen, azido, nitroso, nitro, nitrile and cyano.

[0229] The stated problem is solved and the claimed technical result is achieved by a compound selected from the group including compounds characterized by formula (I)', or its pharmaceutically acceptable salt,

[0230] where (X)' represents -N-, (Y)' represents -CH-;

[0231] a = 1; b = 1;

[0232] (Ri)' represents -C(O)R3 or -SO2R3;

[0233] R3 represents any of A;

[0234] R2 represents any of A;

[0235] A is a branched or unbranched Ci-C6-alkyl, branched or unbranched Ci-C6-alkyloxy (-O-Ci-6-alkyl), or branched or unbranched Ci-C6-alkylthio (-S-Ci-6-alkyl);

[0236] wherein A is substituted by one or more substituents selected from A and cyano.

[0237] For the purposes of the present invention, "halogen" in compounds characterized by formula (I)' is a chlorine, fluorine, bromine, or iodine atom (-Cl, -F, -Br, or -I, respectively).

[0238] The stated problem is solved, and the claimed technical result is achieved due to a compound selected from a group including compounds characterized by formula (I)' (the structure and radicals are indicated above), with the exception of:

[0239] if R2 is methyl substituted with cyano, (X)' is a nitrogen atom, (Y)' is -CH-, a = 1, b = 1, then (R0' is not C6-alkyl, C3-cycloalkyl, phenyl, 5- or 6-membered heteroaryl, indolyl, -NQ2Q3 or -OQ4, wherein said C6-alkyl, C3-cycloalkyl, phenyl or 5- or 6-membered heteroaryl optionally contains 1, 2 or 3 substituents independently selected from -F, -CN and -C1-4-alkyl; Q2 and Q3 are independently selected from -H, C1-4-alkyl and phenyl and Q4 is C6-alkyl, phenyl or benzyl;

[0240] if R2 is methyl substituted by cyano, (X)' and (Y)' represent a nitrogen atom; or (X)' represents a nitrogen atom and (Y)' represents -CH-1; or (X)' represents -CH- and (Y)' represents a nitrogen atom (R0' does not represent -SO2(CH2) n CH2OH, -SO2(CH2) n CH2F, -SO2(CH2) n CHF2, -SO2(CH2) n CF3, -SO2(CH2) n CO2R la , -SO2(CH2) nCO2H, -CH2CH2SO2CH3, -CH2CH2SO3H, -CH2CH2SO2NH2; n=l or 2; R la is C6-alkyl or C3-cycloalkyl;

[0241] if R2 is methyl substituted by cyano, (X)' and (Y)' represent a nitrogen atom, or (X)' represents -CH- and (Y)' represents a nitrogen atom, (Ri)' does not represent -SO2CH2CH3,

[0242] if R2 is methyl substituted by cyano, (X)' is a nitrogen atom, (Y)' is -CH-, a = 1, b = 1, then (Ri)' does not represent a fragment of formula II:

[0243] N

[0244]

[0245] if R2 is methyl substituted by cyano, (X)' is a nitrogen atom, (Y)' is -CH-, a = 1, b = 1, then (Ri)' does not represent a fragment of formula III:

[0246]

[0247] Sh

[0248] 1) T = -H, L = -CH3, -CH2CH3, -Ph, -CH(CH3)2, -CF3, cyclopropyl;

[0249] 2) T = -CH3, L = -CH3, -CH2CH3, -CH2CH2F, cyclopropyl;

[0250] 3) T = -CH(CH3)Ph, L = -CH3;

[0251] 4) T = cyclopropyl, L = -CH3;

[0252] 5) T = -CH(CH3)2, L = -CH3;

[0253] 6) T = -CH2CH3, L = cyclopropyl;

[0254] 7) T = cyclopropyl, L = cyclopropyl, -CH2CH3;

[0255] 8) T = -CH2SR3, cyclopropyl.

[0256] The stated problem is solved, and the claimed technical result is achieved due to a compound selected from a group including compounds characterized by formula IV: X

[0257]

[0258] Formula IV

[0259] or a pharmaceutically acceptable salt thereof, wherein X is a carbonyl (-C(O)-) radical; Y is C6-alkylene; Z is C6-alkyloxy (-O-C6-alkyl) or C6-alkylthio (-S-C6-alkyl) radical.

[0260] One embodiment of the invention is the preparation of a compound characterized by formula IV, or a pharmaceutically acceptable salt thereof, where Y is C6-alkylene, Z is C6-alkyloxy, and X is carbonyl (-C(O)-).

[0261] One embodiment of the invention is to obtain a compound characterized by formula IV, or a pharmaceutically acceptable salt thereof, where Y is C6-alkylene, Z is C6-alkylthio, and X is a carbonyl (-C(O)-) radical.

[0262] One embodiment of the invention is to obtain a compound characterized by formula IV, or a pharmaceutically acceptable salt thereof, where Y is C6-alkylene, Z is C6-alkyloxy, and X is a carbonyl (-C(O)-) radical, or a pharmaceutically acceptable salt thereof.

[0263] One embodiment of the invention is to obtain a compound characterized by formula IV, or a pharmaceutically acceptable salt thereof, where Y is C6b-alkylene, Z is C6b-alkylthio, and X is a carbonyl (-C(O)-) radical, or a pharmaceutically acceptable salt thereof.

[0264] The stated problem is solved, and the stated technical result is achieved due to a compound selected from a group including compounds characterized by formula IV' ':

[0265]

[0266] Formula IV”

[0267] or a pharmaceutically acceptable salt thereof, where X" is a sulfonyl (-SO2-) radical; Y" is a C6-alkylene; Z" is a C6-alkyloxy (-O-C6-alkyl) or C6-alkylthio (-S-C6-alkyl) radical.

[0268] One embodiment of the invention is the preparation of a compound characterized by formula IV”, where Y” is C6b-alkylene, Z” is C6b-alkyloxy, and X” is a sulfonyl (-SO2-) radical or a pharmaceutically acceptable salt thereof.

[0269] One embodiment of the invention is to obtain a compound characterized by formula IV”, where Y” is C6b-alkylene, Z” is C6b-alkylthio, and X” is a sulfonyl (-SO2-) radical or a pharmaceutically acceptable salt thereof.

[0270] One embodiment of the invention is the preparation of a compound characterized by formula IV”, where Y” is C6b-alkylene, Z” is C6b-alkyloxy, and X” is a sulfonyl (-SO2-) radical or a pharmaceutically acceptable salt thereof.

[0271] One embodiment of the invention is to obtain a compound characterized by formula IV”, where Y” is C6b-alkylene, Z” is C6b-alkylthio, and X” is a sulfonyl (-SO2-) radical or a pharmaceutically acceptable salt thereof.

[0272] The stated problem is solved and the claimed technical result is achieved due to 2-(3 -(4-(7H-pyrrolo[2, 3 -d]pyrimidin-4-yl)-1 H-pyrazol-1 -yl)-1 -(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile, characterized by the formula A o

[0273]

[0274] or its pharmaceutically acceptable salt.

[0275] The stated problem is solved, and the claimed technical result is achieved due to the pharmaceutically acceptable salt of 2-(3-(4-(7H-pyrrolo[2,3-]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile, characterized by the formula Aa

[0276]

[0277] X2- acid

[0278] The stated problem is solved, and the claimed technical result is achieved due to 2-(3-(4-(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile, characterized by formula B

[0279]

[0280] or its pharmaceutically acceptable salt.

[0281] The stated problem is solved, and the claimed technical result is achieved due to the pharmaceutically acceptable salt of 2-(3-(4-(7H-pyrrolo[2,3-]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile, characterized by formula Bb

[0282]

[0283] HT is an acid.

[0284] The stated problem is solved, and the claimed technical result is achieved due to 2-(3 -(4-(7H-pyrrolo[2, 3 -d]pyrimidin-4-yl)-1 H-pyrazol-1-yl)-1 -(3 - (methylthio)propanoyl)azetidin-3-yl)acetonitrile, characterized by formula C

[0285]

[0286] or its pharmaceutically acceptable salt.

[0287] The stated problem is solved, and the claimed technical result is achieved due to the pharmaceutically acceptable salt of 2-(3-(4-(7H-pyrrolo[2,3-]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methyl thio) propanone l) az ethide in-3-yl)acetonitrile a, characterized by the formula Cc

[0288]

[0289] X2- acid

[0290] The stated problem is solved, and the claimed technical result is achieved due to 2-(3 -(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1 -((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula (A)”

[0291]

[0292] or its pharmaceutically acceptable salt.

[0293] The stated problem is solved, and the claimed technical result is achieved due to the pharmaceutically acceptable salt of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by the formula Aa”

[0294]

[0295] The stated problem is solved, and the claimed technical result is achieved due to 2-(3 -(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1 -(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula B”

[0296] f^" s

[0297] 0=3 — o

[0298]

[0299] or its pharmaceutically acceptable salt.

[0300] The stated problem is solved, and the claimed technical result is achieved due to the pharmaceutically acceptable salt of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by the formula Bb”

[0301]

[0302] Bb"

[0303] X2- acid

[0304] The stated problem is solved, and the claimed technical result is achieved due to 2-(3 -(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by the formula C”

[0305]

[0306] or its pharmaceutically acceptable salt.

[0307] The stated problem is solved, and the claimed technical result is achieved due to the pharmaceutically acceptable salt of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by the formula Cc' '

[0308]

[0309] X2- acid

[0310] In one embodiment of the present invention, X2 is an acid.

[0311] More preferably, the acid of the present invention is a monobasic, dibasic or tribasic acid.

[0312] More preferably, the acid of the present invention is a monobasic, dibasic or polybasic acid.

[0313] In one embodiment of the present invention, the pharmaceutically acceptable salt of compound Aa is a salt formed between compound A and an inorganic acid.

[0314] In one embodiment of the present invention, the pharmaceutically acceptable salt of compound Bb is a salt formed between compound B and an inorganic acid.

[0315] In one embodiment of the present invention, the pharmaceutically acceptable salt of compound Cc is a salt formed between compound C and an inorganic acid.

[0316] In one embodiment of the present invention, the pharmaceutically acceptable salt of compound Aa" is a salt formed between compound A" and an inorganic acid.

[0317] In one embodiment of the present invention, the pharmaceutically acceptable salt of compound Bb" is a salt formed between compound B" and an inorganic acid.

[0318] In one embodiment of the present invention, the pharmaceutically acceptable salt of compound Cc" is a salt formed by compound C" and an inorganic acid.

[0319] More preferably, X2 is an inorganic acid. More preferably, the inorganic acid of the present invention is a monobasic, dibasic, or tribasic acid.

[0320] If the inorganic acid is a monobasic acid, then the molar ratio of the salt-forming acid to compound A is 1:1, or if the inorganic acid is a monobasic acid, then z = 1.

[0321] If the inorganic acid is a monobasic acid, then the molar ratio of the salt-forming acid to compound B is 1:1, or if the inorganic acid is a monobasic acid, then z = 1.

[0322] If the inorganic acid is a monobasic acid, then the molar ratio of the salt-forming acid to the compound C is 1:1, or if the inorganic acid is a monobasic acid, then z = 1.

[0323] If the inorganic acid is a monobasic acid, then the molar ratio of the salt-forming acid to compound A” is 1:1, or if the inorganic acid is a monobasic acid, then z = 1.

[0324] If the inorganic acid is a monobasic acid, then the molar ratio of the salt-forming acid to compound B” is 1:1, or if the inorganic acid is a monobasic acid, then z = 1.

[0325] If the inorganic acid is a monobasic acid, then the molar ratio of the salt-forming acid to the compound C” is 1:1 or, if the inorganic acid is a monobasic acid, then z = 1.

[0326] More preferably, within the framework of the present invention, the monobasic inorganic acid is selected from the group including, but not limited to, hydrochloric, hydrofluoric, hydrobromic, hydroiodic, nitric and nitrous acids.

[0327] If the inorganic acid is a dibasic acid, then the molar ratio of the salt-forming acid to compound A is 1:1 or 1:2, or if the inorganic acid is a dibasic acid, then z = 1.2.

[0328] If the inorganic acid is a dibasic acid, then the molar ratio of the salt-forming acid to compound B is 1:1 or 1:2, or if the inorganic acid is a dibasic acid, then z = 1.2.

[0329] If the inorganic acid is a dibasic acid, then the molar ratio of the salt-forming acid to the compound C is 1:1 or 1:2, or if the inorganic acid is a dibasic acid, then z = 1.2.

[0330] If the inorganic acid is a dibasic acid, then the molar ratio of the salt-forming acid to compound A” is 1:1 or 1:2, or if the inorganic acid is a dibasic acid, then z = 1.2.

[0331] If the inorganic acid is a dibasic acid, then the molar ratio of the salt-forming acid to compound B” is 1:1 or 1:2, or if the inorganic acid is a dibasic acid, then z = 1.2.

[0332] If the inorganic acid is a dibasic acid, then the molar ratio of the salt-forming acid to the compound C” is 1:1 or 1:2, or if the inorganic acid is a dibasic acid, then z = 1.2.

[0333] More preferably, within the framework of the present invention, the dibasic inorganic acid is selected from the group including, but not limited to, hydrogen sulfide, sulfurous, sulfuric and carbonic acids.

[0334] If the inorganic acid is a tribasic acid, then the molar ratio of the salt-forming acid to compound A is 1:1, 1:2, or 1:3, or if the inorganic acid is a tribasic acid, then z = 1, 2, 3.

[0335] If the inorganic acid is a tribasic acid, then the molar ratio of the salt-forming acid to compound B is 1:1, 1:2, or 1:3, or if the inorganic acid is a tribasic acid, then z = 1, 2, 3.

[0336] If the inorganic acid is a tribasic acid, then the molar ratio of the salt-forming acid to compound C is 1:1, 1:2, or 1:3, or if the inorganic acid is a tribasic acid, then z = 1, 2, 3.

[0337] If the inorganic acid is a tribasic acid, then the molar ratio of the salt-forming acid to compound A” is 1:1, 1:2, or 1:3, or if the inorganic acid is a tribasic acid, then z = 1, 2, 3.

[0338] If the inorganic acid is a tribasic acid, then the molar ratio of the salt-forming acid to compound B” is 1:1, 1:2, or 1:3, or if the inorganic acid is a tribasic acid, then z = 1, 2, 3.

[0339] If the inorganic acid is a tribasic acid, then the molar ratio of the salt-forming acid to the compound C” is 1:1, 1:2, or 1:3, or if the inorganic acid is a tribasic acid, then z = 1, 2, 3.

[0340] More preferably, in the context of the present invention, the tribasic inorganic acid is, but is not limited to, phosphoric acid.

[0341] In one embodiment of the present invention, the pharmaceutically acceptable salt of compound A, B or C is a salt formed by compound A, B or C and an organic acid.

[0342] In one embodiment of the present invention, the pharmaceutically acceptable salt of compound A”, B” or C” is a salt formed by compound A”, B” or C” and an organic acid.

[0343] More preferably, X2 is an organic acid.

[0344] More preferably, the organic acid of the present invention is a monobasic, dibasic or polybasic acid.

[0345] If the organic acid is a monobasic acid, then the molar ratio of the salt-forming acid to compound A is 1:1, or if the organic acid is a monobasic acid, then z = 1.

[0346] If the organic acid is a monobasic acid, then the molar ratio of the salt-forming acid to compound B is 1:1, or if the organic acid is a monobasic acid, then z = 1.

[0347] If the organic acid is a monobasic acid, then the molar ratio of the salt-forming acid to the compound C is 1:1, or if the organic acid is a monobasic acid, then z = 1.

[0348] If the organic acid is a monobasic acid, then the molar ratio of the salt-forming acid to compound A” is 1:1, or if the organic acid is a monobasic acid, then z = 1.

[0349] If the organic acid is a monobasic acid, then the molar ratio of the salt-forming acid to compound B” is 1:1 or, if the organic acid is a monobasic acid, then z = 1. If the organic acid is a monobasic acid, then the molar ratio of the salt-forming acid to compound C” is 1:1 or, if the organic acid is a monobasic acid, then z = 1.

[0350] More preferably, within the framework of the present invention, the monobasic organic acid is selected from the group including, but not limited to, formic, acetic, monofluoroacetic, difluoroacetic, trifluoroacetic, propionic, butyric, isobutyric, valerianic, caproic, enanthoic, p-toluic, anisic and phenylacetic acid.

[0351] If the organic acid is a dibasic acid, then the molar ratio of the salt-forming acid to compound A is 1:1 or 1:2, or if the organic acid is a dibasic acid, then z = 1.2.

[0352] If the organic acid is a dibasic acid, then the molar ratio of the salt-forming acid to compound B is 1:1 or 1:2, or if the organic acid is a dibasic acid, then z = 1.2.

[0353] If the organic acid is a dibasic acid, then the molar ratio of the salt-forming acid to the compound C is 1:1 or 1:2, or if the organic acid is a dibasic acid, then z = 1.2.

[0354] If the organic acid is a dibasic acid, then the molar ratio of the salt-forming acid to compound A” is 1:1 or 1:2, or if the organic acid is a dibasic acid, then z = 1.2.

[0355] If the organic acid is a dibasic acid, then the molar ratio of the salt-forming acid to compound B” is 1:1 or 1:2, or if the organic acid is a dibasic acid, then z = 1.2.

[0356] If the organic acid is a dibasic acid, then the molar ratio of the salt-forming acid to the compound C” is 1:1 or 1:2, or if the organic acid is a dibasic acid, then z = 1.2.

[0357] More preferably, within the framework of the present invention, the dibasic organic acid is selected from the group including, but not limited to, oxalic, malonic, succinic, dioxosuccinic, glutaric, a-hydroxyglutaric, 2-oxoglutaric, 3-oxoglutaric, adipic, pimelic, diaminopimelic, phthalic, isophthalic, teryphthalic, malic, suberic, azelaic, maleic, fumaric, tartaric, aspartic, glutamic, arabic and D-glucaric acid.

[0358] If the organic acid is a tribasic acid, then the molar ratio of the salt-forming acid to compound A is 1:1, 1:2, or 1:3, or if the organic acid is a tribasic acid, then z = 1, 2, 3.

[0359] If the organic acid is a tribasic acid, then the molar ratio of the salt-forming acid to compound B is 1:1, 1:2, or 1:3, or if the organic acid is a tribasic acid, then z = 1, 2, 3.

[0360] If the organic acid is a tribasic acid, then the molar ratio of the salt-forming acid to compound C is 1:1, 1:2, or 1:3, or if the organic acid is a tribasic acid, then z = 1, 2, 3.

[0361] If the organic acid is a tribasic acid, then the molar ratio of the salt-forming acid to compound A” is 1:1, 1:2, or 1:3, or if the organic acid is a tribasic acid, then z = 1, 2, 3.

[0362] If the organic acid is a tribasic acid, then the molar ratio of the salt-forming acid to compound B” is 1:1, 1:2, or 1:3, or if the organic acid is a tribasic acid, then z = 1, 2, 3.

[0363] If the organic acid is a tribasic acid, then the molar ratio of the salt-forming acid to the compound C” is 1:1, 1:2, or 1:3, or if the organic acid is a tribasic acid, then z = 1, 2, 3.

[0364] More preferably, within the framework of the present invention, the tribasic organic acid is selected from the group including, but not limited to, citric, isocitric, aconitic, β-carboxyglutaric, 2-hydroxy-1,2,3-nonadecanetricarboxylic and benzene-1,3,5-tricarboxylic acid.

[0365] One embodiment of the present invention is 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile hydrochloride. One embodiment of the present invention is 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetide yn-3-yl)acetonitrile hydrochloride.

[0366] One embodiment of the present invention is 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanoyl)azetide yn-3-yl)acetonitrile hydrochloride.

[0367] One embodiment of the present invention is 2-(3-(4-(7H-pyrrolo[2,3-b]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile hydrochloride.

[0368] One embodiment of the present invention is 2-(3-(4-(7H-pyrrolo[2,3-b]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile hydrochloride.

[0369] One embodiment of the present invention is 2-(3-(4-(7H-pyrrolo[2,3-b]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile hydrochloride.

[0370] The compounds of formulas A, B, C, A”, B”, C”, or pharmaceutically acceptable salts thereof, of the present invention can be administered in the form of prodrugs. A prodrug can include a covalently linked carrier that releases the active parent drug upon administration to a mammalian subject. Prodrugs can be prepared by modifying functional groups present in the compounds such that the modifications cleave, either during routine manipulation or in vivo, to the parent compounds. Prodrugs include, for example, compounds in which a hydroxyl or amino group is linked to any group that, upon administration to a subject, cleaves to form a free hydroxyl or amino group. Examples of prodrugs include, but are not limited to, acetate, formate, and benzoate derivatives of alcohol functional groups in the compounds.

[0371] Typical prodrugs form the active metabolite by conversion of the prodrug by hydrolytic enzymes, hydrolysis of amides, lactams, peptides, carboxylic acid esters, epoxides, or cleavage of inorganic acid esters.

[0372] The stated problem is solved, and the claimed technical result is also achieved, by a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor, containing a compound characterized by formula (I), formula IV, or formula IV”, or a pharmaceutically acceptable salt thereof. The stated problem is solved, and the claimed technical result is also achieved, by a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor, for the treatment of autoimmune diseases, containing a compound, a compound characterized by formula (I), formula IV, or formula IV”, or a pharmaceutically acceptable salt thereof.

[0373] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

[0374] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing in a therapeutically effective amount a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof.

[0375] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing in a therapeutically effective amount a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

[0376] One embodiment of the present invention is also a pharmaceutical composition containing a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 100.00 wt. % of the weight of the pharmaceutical composition.

[0377] One embodiment of the present invention is also a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing a compound characterized by formula (I), formula IV, or formula IV”, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 99.99 wt.% by weight of the pharmaceutical composition.

[0378] More preferably, the content of the compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 0.01 to 85.00 May %, from 0.01 to 80.00 May %, from 0.01 to 75.00 May %, from 0.01 to 70.00 May %, from 0.01 to 65.00 May %, from 0.01 to 60.00 May %, from 0.01 to 55.00 May %, from 0.01 to 40.00 May %, from 0.01 to 35.00 May %, from 0.01 to 30.00 May %, from 0.01 to 25.00 May %, from 0.01 to 20.00 May. %, from 0.01 to 15.00 May %, from 0.01 to 10.00 May %, from 0.01 to 9.00 May %, from 0.01 to 8.00 May %, from 0.01 to 7.00 May %, from 0.01 to 6.00 May %, from 0.01 to 5.00 May %, from 0.01 to 4.00 May %, from 0.01 to 3.00 May %, from 0.01 to 2.00 May % or from 0.01 to 1.00 May % by weight of the pharmaceutical composition.

[0379] More preferably, the content of the compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 0.10 to 85.00 May %, from 0.10 to 80.00 May %, from 0.10 to 75.00 May %, from 0.10 to 70.00 May %, from 0.10 to 65.00 May %, from 0.10 to 60.00 May %, from 0.10 to 55.00 May %, from 0.10 to 40.00 May %, from 0.10 to 35.00 May %, from 0.10 to 30.00 May %, from 0.10 to 25.00 May %, from 0.10 to 20.00 May. %, from 0.10 to 15.00 May %, from 0.10 to 10.00 May %, from 0.10 to 9.00 May %, from 0.10 to 8.00 May %, from 0.10 to 7.00 May %, from 0.10 to 6.00 May %, from 0.10 to 5.00 May %, from 0.10 to 4.00 May %, from 0.10 to 3.00 May %, from 0.10 to 2.00 May % or from 0.10 to 1.00 May % by weight of the pharmaceutical composition.

[0380] More preferably, the content of the compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 1.00 to 85.00 May. %, from 1.00 to 80.00 May. %, from 1.00 to 75.00 May. %, from 1.00 to 70.00 May. %, from 1.00 to 65.00 May. %, from 1.00 to 60.00 May. %, from 1.00 to 55.00 May. %, from 1.00 to 40.00 May. %, from 1.00 to 35.00 May. %, from 1.00 to 30.00 May. %, from 1.00 to 25.00 May. %, from 1.00 to 20.00 May. %, from 1.00 to 15.00 May %, from 1.00 to 10.00 May %, from 1.00 to 9.00 May %, from 1.00 to 8.00 May %, from 1.00 to 7.00 May %, from 1.00 to 6.00 May %, from 1.00 to 5.00 May %, from 1.00 to 4.00 May %, from 1.00 to 3.00 May % or from 1.00 to 2.00 May % by weight of the pharmaceutical composition.

[0381] More preferably, the content of the compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 5.00 to 85.00 May %, from 5.00 to 80.00 May %, from 5.00 to 75.00 May %, from 5.00 to 70.00 May %, from 5.00 to 65.00 May %, from 5.00 to 60.00 May %, from 5.00 to 55.00 May %, from 5.00 to 40.00 May %, from 5.00 to 35.00 May %, from 5.00 to 30.00 May %, from 5.00 to 25.00 May %, from 5.00 to 20.00 May. %, from 5.00 to 15.00 May %, from 5.00 to 10.00 May %, from 5.00 to 9.00 May %, from 5.00 to 8.00 May %, from 5.00 to 7.00 May % or from 5.00 to 6.00 May % of the weight of the pharmaceutical composition.

[0382] More preferably, the content of the compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 10.00 to 85.00 May. %, from 10.00 to 80.00 May. %, from 10.00 to 75.00 May. %, from 10.00 to 70.00 May. %, from 10.00 to 65.00 May. %, from 10.00 to 60.00 May. %, from 10.00 to 55.00 May. %, from 10.00 to 40.00 May. %, from 10.00 to 35.00 May. %, from 10.00 to 30.00 May. %, from 10.00 to 25.00 May. %, from 10.00 to 20.00 May % or from 10.00 to 15.00 May % of the weight of the pharmaceutical composition.

[0383] More preferably, the content of the compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 15.00 to 85.00 May. %, from 15.00 to 80.00 May. %, from 15.00 to 75.00 May. %, from 15.00 to 70.00 May. %, from 15.00 to 65.00 May. %, from 15.00 to 60.00 May. %, from 15.00 to 55.00 May. %, from 15.00 to 40.00 May. %, from 15.00 to 35.00 May. %, from 15.00 to 30.00 May. %, from 15.00 to 25.00 May. % or from 15.00 to 20.00 May. % of the weight of the pharmaceutical composition.

[0384] More preferably, the content of the compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 0.50 to 5.00 wt. %, from 0.50 to 4.50 wt. %, from 0.50 to 4.00 wt. %, from 0.50 to 3.50 wt. %, from 0.50 to 3.00 wt. %, from 0.50 to 2.50 wt. %, from 0.50 to 2.00 wt. %, from 0.50 to 1.50 wt. % or from 0.50 to 1.00 wt. % of the weight of the pharmaceutical composition.

[0385] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile, characterized by formula A, or its pharmaceutically acceptable salt.

[0386] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile, characterized by formula A, or its pharmaceutically acceptable salt.

[0387] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile, characterized by formula A, or its pharmaceutically acceptable salt, and at least one pharmaceutically acceptable excipient. The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile, characterized by formula A, or a pharmaceutically acceptable salt thereof, in a therapeutically effective amount.

[0388] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing a therapeutically effective amount of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile, characterized by formula A, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

[0389] One embodiment of the present invention is also a pharmaceutical composition containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetide yn-3-yl)acetonitrile, characterized by formula A, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 100.00 wt. % of the weight of the pharmaceutical composition.

[0390] One embodiment of the present invention is also a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile, characterized by formula A, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 99.99 wt. % by weight of the pharmaceutical composition.

[0391] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile characterized by formula A or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 0.01 to 85.00 May %, from 0.01 to 80.00 May %, from 0.01 to 75.00 May %, from 0.01 to 70.00 May %, from 0.01 to 65.00 May %, from 0.01 to 60.00 May %, from 0.01 to 55.00 May %, from 0.01 to 40.00 May. %, from 0.01 to 35.00 May %, from 0.01 to 30.00 May %, from 0.01 to 25.00 May %, from 0.01 to 20.00 May %, from 0.01 to 15.00 May %, from 0.01 to 10.00 May %, from 0.01 to 9.00 May %, from 0.01 to 8.00 May %, from 0.01 to 7.00 May %, from 0.01 to 6.00 May %, from 0.01 to 5.00 May %, from 0.01 to 4.00 May %, from 0.01 to 3.00 May %, from 0.01 to 2.00 May % or from 0.01 to 1.00 May. % of the weight of the pharmaceutical composition.More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile characterized by formula A or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 0.10 to 85.00 wt. %, from 0.10 to 80.00 wt. %, from 0.10 to 75.00 wt. %, from 0.10 to 70.00 wt. %, from 0.10 to 65.00 wt. %, from 0.10 to 60.00 wt. %, from 0.10 to 55.00 wt. %, from 0.10 to 40.00 wt. %, from 0.10 to 35.00 May %, from 0.10 to 30.00 May %, from 0.10 to 25.00 May %, from 0.10 to 20.00 May %, from 0.10 to 15.00 May %, from 0.10 to 10.00 May %, from 0.10 to 9.00 May %, from 0.10 to 8.00 May %, from 0.10 to 7.00 May %, from 0.10 to 6.00 May %, from 0.10 to 5.00 May %, from 0.10 to 4.00 May %, from 0.10 to 3.00 May %, from 0.10 to 2.00 May % or from 0.10 to 1.00 May. % of the weight of the pharmaceutical composition.

[0392] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile characterized by formula A or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 1.00 to 85.00 May %, from 1.00 to 80.00 May %, from 1.00 to 75.00 May %, from 1.00 to 70.00 May %, from 1.00 to 65.00 May %, from 1.00 to 60.00 May %, from 1.00 to 55.00 May %, from 1.00 to 40.00 May. %, from 1.00 to 35.00 May %, from 1.00 to 30.00 May %, from 1.00 to 25.00 May %, from 1.00 to 20.00 May %, from 1.00 to 15.00 May %, from 1.00 to 10.00 May %, from 1.00 to 9.00 May %, from 1.00 to 8.00 May %, from 1.00 to 7.00 May %, from 1.00 to 6.00 May %, from 1.00 to 5.00 May %, from 1.00 to 4.00 May %, from 1.00 to 3.00 May % or from 1.00 to 2.00 May % by weight of the pharmaceutical composition.

[0393] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile characterized by formula A or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 5.00 to 85.00 May %, from 5.00 to 80.00 May %, from 5.00 to 75.00 May %, from 5.00 to 70.00 May %, from 5.00 to 65.00 May %, from 5.00 to 60.00 May %, from 5.00 to 55.00 May %, from 5.00 to 40.00 May. %, from 5.00 to 35.00 May %, from 5.00 to 30.00 May %, from 5.00 to 25.00 May %, from 5.00 to 20.00 May %, from 5.00 to 15.00 May %, from 5.00 to 10.00 May %, from 5.00 to 9.00 May %, from 5.00 to 8.00 May %, from 5.00 to 7.00 May % or from 5.00 to 6.00 May % by weight of the pharmaceutical composition.

[0394] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile characterized by formula A or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 10.00 to 85.00 May %, from 10.00 to 80.00 May %, from 10.00 to 75.00 May %, from 10.00 to 70.00 May %, from 10.00 to 65.00 May %, from 10.00 to 60.00 May %, from 10.00 to 55.00 May %, from 10.00 to 40.00 May. %, from 10.00 to 35.00 May. %, from 10.00 to 30.00 May. %, from 10.00 to 25.00 May. %, from 10.00 to 20.00 May. % or from 10.00 to 15.00 May. % of the weight of the pharmaceutical composition.

[0395] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile characterized by formula A or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 15.00 to 85.00 May %, from 15.00 to 80.00 May %, from 15.00 to 75.00 May %, from 15.00 to 70.00 May %, from 15.00 to 65.00 May %, from 15.00 to 60.00 May %, from 15.00 to 55.00 May %, from 15.00 to 40.00 May. %, from 15.00 to 35.00 May %, from 15.00 to 30.00 May %, from 15.00 to 25.00 May % or from 15.00 to 20.00 May % of the weight of the pharmaceutical composition.

[0396] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile characterized by formula A or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 0.50 to 5.00 wt. %, from 0.50 to 4.50 wt. %, from 0.50 to 4.00 wt. %, from 0.50 to 3.50 wt. %, from 0.50 to 3.00 wt. %, from 0.50 to 2.50 wt. %, from 0.50 to 2.00 wt. %, from 0.50 to 1.50 wt. % or from 0.50 to 1.00 wt. % of the weight of the pharmaceutical composition.

[0397] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxpropanoyl)azetidin-3-yl)acetonitrile, characterized by formula B, or its pharmaceutically acceptable salt.

[0398] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3 -d]pyrimidine yn-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetide yn-3-yl)acetonitrile, characterized by formula B, or a pharmaceutically acceptable salt thereof.

[0399] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3 -d]pyrimidine yn-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetide yn-3-yl)acetonitrile, characterized by formula B, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient. The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile, characterized by formula B, or a pharmaceutically acceptable salt thereof, in a therapeutically effective amount.

[0400] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing a therapeutically effective amount of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile, characterized by formula B, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

[0401] In some embodiments of the present invention, the pharmaceutical composition can be prepared using known, conventional methods in the pharmaceutical field.

[0402] One embodiment of the present invention is also a pharmaceutical composition containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile, characterized by formula B, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 100.00 wt. % of the weight of the pharmaceutical composition.

[0403] One embodiment of the present invention is also a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile, characterized by formula B, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 99.99 wt. % by weight of the pharmaceutical composition.

[0404] One embodiment of the present invention is a pharmaceutical composition comprising 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile, characterized by formula B, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 99.00 wt. % of the weight of the pharmaceutical composition.

[0405] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile characterized by formula B or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 0.01 to 95.00 wt. %, from 0.01 to 90.00 wt. %, from 0.01 to 85.00 wt. %, from 0.01 to 80.00 wt. %, from 0.01 to 75.00 wt. %, from 0.01 to 70.00 wt. %, from 0.01 to 65.00 wt. %, from 0.01 to 60.00 wt. %, from 0.01 to 55.00 wt. %, from 0.01 to 50.00 wt. % or from 0.01 to 40.00 wt. % of the weight of the pharmaceutical composition.

[0406] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile characterized by formula B or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 0.01 to 85.00 May %, from 0.01 to 80.00 May %, from 0.01 to 75.00 May %, from 0.01 to 70.00 May %, from 0.01 to 65.00 May %, from 0.01 to 60.00 May %, from 0.01 to 55.00 May %, from 0.01 to 40.00 May. %, from 0.01 to 35.00 May %, from 0.01 to 30.00 May %, from 0.01 to 25.00 May %, from 0.01 to 20.00 May %, from 0.01 to 15.00 May %, from 0.01 to 10.00 May %, from 0.01 to 9.00 May %, from 0.01 to 8.00 May %, from 0.01 to 7.00 May %, from 0.01 to 6.00 May %, from 0.01 to 5.00 May %, from 0.01 to 4.00 May %, from 0.01 to 3.00 May %, from 0.01 to 2.00 May % or from 0.01 to 1.00 May. % of the weight of the pharmaceutical composition.

[0407] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile characterized by formula B or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 0.10 to 99.00 wt. %, from 0.10 to 95.00 wt. %, from 0.10 to 90.00 wt. %, from 0.10 to 85.00 wt. %, from 0.10 to 80.00 wt. %, from 0.10 to 75.00 wt. %, from 0.10 to 70.00 wt. %, from 0.10 to 65.00 wt. %, from 0.10 to 60.00 May. %, from 0.10 to 55.00 May. %, from 0.10 to 40.00 May. %, from 0.10 to 35.00 May. %, from 0.10 to 30.00 May. %, from 0.10 to 25.00 May. %, from 0.10 to 20.00 May. %, from 0.10 to 15.00 May. %, from 0.10 to 10.00 May. %, from 0.10 to 9.00 May. %, from 0.10 to 8.00 May. %, from 0.10 to 7.00 May. %, from 0.10 to 6.00 May. %, from 0.10 to 5.00 May. %, from 0.10 to 4.00 May %, from 0.10 to 3.00 May %, from 0.10 to 2.00 May % or from 0.10 to 1.00 May % of the weight of the pharmaceutical composition.

[0408] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile characterized by formula B or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 0.50 to 99.00 wt. %, from 0.50 to 95.00 wt. %, from 0.50 to 90.00 wt. %, from 0.50 to 85.00 wt. %, from 0.50 to 80.00 wt. %, from 0.50 to 75.00 wt. %, from 0.50 to 70.00 wt. %, from 0.50 to 65.00 wt. %, from 0.50 to 60.00 wt. %, from 0.50 to 55.00 wt. %, from 0.50 to 50.00 wt. %, from 0.50 to 45.00 wt. % or from 0.50 to 40.00 wt. % of the weight of the pharmaceutical composition.

[0409] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile characterized by formula B or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 1.00 to 99.00 wt. %, from 1.00 to 95.00 wt. %, from 1.00 to 90.00 wt. %, from 1.00 to 85.00 wt. %, from 1.00 to 80.00 wt. %, from 1.00 to 75.00 wt. %, from 1.00 to 70.00 wt. %, from 1.00 to 65.00 wt. %, from 1.00 to 60.00 May. %, from 1.00 to 55.00 May. %, from 1.00 to 40.00 May. %, from 1.00 to 35.00 May. %, from 1.00 to 30.00 May. %, from 1.00 to 25.00 May. %, from 1.00 to 20.00 May. %, from 1.00 to 15.00 May. %, from 1.00 to 10.00 May. %, from 1.00 to 9.00 May. %, from 1.00 to 8.00 May. %, from 1.00 to 7.00 May. %, from 1.00 to 6.00 May. %, from 1.00 to 5.00 May. %, from 1.00 to 4.00 May %, from 1.00 to 3.00 May % or from 1.00 to 2.00 May % of the weight of the pharmaceutical composition.

[0410] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile characterized by formula B or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 5.00 to 85.00 May %, from 5.00 to 80.00 May %, from 5.00 to 75.00 May %, from 5.00 to 70.00 May %, from 5.00 to 65.00 May %, from 5.00 to 60.00 May %, from 5.00 to 55.00 May %, from 5.00 to 40.00 May. %, from 5.00 to 35.00 May %, from 5.00 to 30.00 May %, from 5.00 to 25.00 May %, from 5.00 to 20.00 May %, from 5.00 to 15.00 May %, from 5.00 to 10.00 May %, from 5.00 to 9.00 May %, from 5.00 to 8.00 May %, from 5.00 to 7.00 May % or from 5.00 to 6.00 May % by weight of the pharmaceutical composition.

[0411] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile characterized by formula B or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 10.00 to 85.00 May %, from 10.00 to 80.00 May %, from 10.00 to 75.00 May %, from 10.00 to 70.00 May %, from 10.00 to 65.00 May %, from 10.00 to 60.00 May %, from 10.00 to 55.00 May %, from 10.00 to 40.00 May. %, from 10.00 to 35.00 May. %, from 10.00 to 30.00 May. %, from 10.00 to 25.00 May. %, from 10.00 to 20.00 May. % or from 10.00 to 15.00 May. % of the weight of the pharmaceutical composition.

[0412] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile characterized by formula B or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 15.00 to 85.00 May %, from 15.00 to 80.00 May %, from 15.00 to 75.00 May %, from 15.00 to 70.00 May %, from 15.00 to 65.00 May %, from 15.00 to 60.00 May %, from 15.00 to 55.00 May %, from 15.00 to 40.00 May. %, from 15.00 to 35.00 May %, from 15.00 to 30.00 May %, from 15.00 to 25.00 May % or from 15.00 to 20.00 May % of the weight of the pharmaceutical composition.

[0413] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile characterized by formula B or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 0.50 to 5.00 wt. %, from 0.50 to 4.50 wt. %, from 0.50 to 4.00 wt. %, from 0.50 to 3.50 wt. %, from 0.50 to 3.00 wt. %, from 0.50 to 2.50 wt. %, from 0.50 to 2.00 wt. %, from 0.50 to 1.50 wt. % or from 0.50 to 1.00 wt. % of the weight of the pharmaceutical composition.

[0414] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanoyl)azetidin-3-yl)acetonitrile, characterized by formula C, or its pharmaceutically acceptable salt.

[0415] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo [2, 3 -d] pyrimidin-4-yl)-1 H-pyrazol-1-yl)-1-(3-(methylthio)propanoyl)azetide yn-3-yl)acetonitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof.

[0416] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo [2, 3 -d] pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanoyl)azetide yn-3-yl)acetonitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

[0417] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanoyl)azetidin-3-yl)acetonitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof, in a therapeutically effective amount.

[0418] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing a therapeutically effective amount of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanoyl)azetidin-3-yl)acetonitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

[0419] In some embodiments of the present invention, the pharmaceutical composition can be prepared using known, conventional methods in the pharmaceutical field.

[0420] One embodiment of the present invention is also a pharmaceutical composition containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanoyl)azetidin-3-yl)acetonitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 100.00 wt. % of the weight of the pharmaceutical composition.

[0421] One embodiment of the present invention is also a pharmaceutical composition exhibiting Janus kinase (JAK) inhibitor properties for the treatment of autoimmune diseases, comprising 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanoyl)azetidin-3-yl)acetonitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 99.99 wt. % by weight of the pharmaceutical composition.

[0422] One embodiment of the present invention is a pharmaceutical composition containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanoyl)azetidin-3-yl)acetonitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 99.00 wt. % of the weight of the pharmaceutical composition.

[0423] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanone l) azetide yn-3-yl)acetoneitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 0.01 to 95.00 wt. %, from 0.01 to 90.00 wt. %, from 0.01 to 85.00 wt. %, from 0.01 to 80.00 wt. %, from 0.01 to 75.00 wt. %, from 0.01 to 70.00 wt. %, from 0.01 to 65.00 wt. %, from 0.01 to 60.00 wt. %, from 0.01 to 55.00 wt. %, from 0.01 to 50.00 wt. % or from 0.01 to 40.00 wt. %, from 0.01 to 35.00 wt. %, from 0.01 to 30.00 wt. %, from 0.01 to 25.00 wt. %, from 0.01 to 20.00 wt. %, from 0.01 to 15.00 wt. %, from 0.01 to 10.00 wt. %, from 0.01 to 9.00 wt. %, from 0.01 to 8.00 wt. %, from 0.01 to 7.00 wt. %, from 0.01 to 6.00 wt. %, from 0.01 to 5.00 May %, from 0.01 to 4.00 May %, from 0.01 to 3.00 May %, from 0.01 to 2.00 May % or from 0.01 to 1.00 May % of the weight of the pharmaceutical composition.

[0424] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanone l) azetide yn-3-yl)acetoneitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 0.10 to 99.00 wt. %, from 0.10 to 95.00 wt. %, from 0.10 to 90.00 wt. %, from 0.10 to 85.00 wt. %, from 0.10 to 80.00 wt. %, from 0.10 to 75.00 wt. %, from 0.10 to 70.00 wt. %, from 0.10 to 65.00 wt. %, from 0.10 to 60.00 wt. %, from 0.10 to 55.00 wt. %, from 0.10 to 50.00 wt. %, from 0.10 to 45.00 wt. %, or from 0.10 to 40.00 wt. %, from 0.10 to 35.00 wt. %, from 0.10 to 30.00 wt. %, from 0.10 to 25.00 wt. %, from 0.10 to 20.00 wt. %, from 0.10 to 15.00 wt. %, from 0.10 to 10.00 wt. %, from 0.10 to 9.00 wt. %, from 0.10 to 8.00 wt. %, from 0.10 to 7.00 May. %, from 0.10 to 6.00 May. %, from 0.10 to 5.00 May. %, from 0.10 to 4.00 May. %, from 0.10 to 3.00 May. %, from 0.10 to 2.00 May. % or from 0.10 to 1.00 May. % of the weight of the pharmaceutical composition.

[0425] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanone l) azetide yn-3-yl)acetoneitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 0.50 to 99.00 wt. %, from 0.50 to 95.00 wt. %, from 0.50 to 90.00 wt. %, from 0.50 to 85.00 wt. %, from 0.50 to 80.00 wt. %, from 0.50 to 75.00 wt. %, from 0.50 to 70.00 wt. %, from 0.50 to 65.00 wt. %, from 0.50 to 60.00 wt. %, from 0.50 to 55.00 wt. %, from 0.50 to 50.00 wt. %, from 0.50 to 45.00 wt. % or from 0.50 to 40.00 wt. % of the weight of the pharmaceutical composition.

[0426] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanone l) azetide yn-3-yl)acetoneitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 1.00 to 99.00 wt. %, from 1.00 to 95.00 wt. %, from 1.00 to 90.00 wt. %, from 1.00 to 85.00 wt. %, from 1.00 to 80.00 wt. %, from 1.00 to 75.00 wt. %, from 1.00 to 70.00 wt. %, from 1.00 to 65.00 wt. %, from 1.00 to 60.00 wt. %, from 1.00 to 55.00 wt. %, from 1.00 to 50.00 wt. %, from 1.00 to 45.00 wt. % or from 1.00 to 40.00 wt. %, from 1.00 to 35.00 wt. %, from 1.00 to 30.00 wt. %, from 1.00 to 25.00 wt. %, from 1.00 to 20.00 wt. %, from 1.00 to 15.00 wt. %, from 1.00 to 10.00 wt. %, from 1.00 to 9.00 wt. %, from 1.00 to 8.00 wt. %, from 1.00 to 7.00 May. %, from 1.00 to 6.00 May. %, from 1.00 to 5.00 May. %, from 1.00 to 4.00 May. %, from 1.00 to 3.00 May. % or from 1.00 to 2.00 May.% by weight of the pharmaceutical composition. More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanone l) azetide yn-3-yl)acetoneitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 5.00 to 85.00 wt. %, from 5.00 to 80.00 wt. %, from 5.00 to 75.00 wt. %, from 5.00 to 70.00 wt. %, from 5.00 to 65.00 wt. %, from 5.00 to 60.00 wt. %, from 5.00 to 55.00 wt. %, from 5.00 to 40.00 May %, from 5.00 to 35.00 May %, from 5.00 to 30.00 May %, from 5.00 to 25.00 May %, from 5.00 to 20.00 May %, from 5.00 to 15.00 May %, from 5.00 to 10.00 May %, from 5.00 to 9.00 May %, from 5.00 to 8.00 May %, from 5.00 to 7.00 May % or from 5.00 to 6.00 May % by weight of the pharmaceutical composition.

[0427] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanone l) azetide yn-3-yl)acetoneitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 10.00 to 85.00 wt. %, from 10.00 to 80.00 wt. %, from 10.00 to 75.00 wt. %, from 10.00 to 70.00 wt. %, from 10.00 to 65.00 wt. %, from 10.00 to 60.00 wt. %, from 10.00 to 55.00 wt. %, from 10.00 to 40.00 May %, from 10.00 to 35.00 May %, from 10.00 to 30.00 May %, from 10.00 to 25.00 May %, from 10.00 to 20.00 May % or from 10.00 to 15.00 May % of the weight of the pharmaceutical composition.

[0428] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanone l) azetide yn-3-yl)acetoneitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 15.00 to 85.00 wt. %, from 15.00 to 80.00 wt. %, from 15.00 to 75.00 wt. %, from 15.00 to 70.00 wt. %, from 15.00 to 65.00 wt. %, from 15.00 to 60.00 wt. %, from 15.00 to 55.00 wt. %, from 15.00 to 40.00 May %, from 15.00 to 35.00 May %, from 15.00 to 30.00 May %, from 15.00 to 25.00 May % or from 15.00 to 20.00 May % of the weight of the pharmaceutical composition.

[0429] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanone l) azetide yn-3-yl)acetoneitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 0.50 to 5.00 wt. %, from 0.50 to 4.50 wt. %, from 0.50 to 4.00 wt. %, from 0.50 to 3.50 wt. %, from 0.50 to 3.00 wt. %, from 0.50 to 2.50 wt. %, from 0.50 to 2.00 wt. %, from 0.50 to 1.50 wt. % or from 0.50 to 1.00 mass % of the weight of the pharmaceutical composition.

[0430] The stated problem is solved and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2, 3-(1]pyrimidine-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula A”, or a pharmaceutically acceptable salt thereof.

[0431] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula A”, or its pharmaceutically acceptable salt.

[0432] The stated problem is solved and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-y]pyrimidine-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula A”, or its pharmaceutically acceptable salt and at least one pharmaceutically acceptable excipient.

[0433] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula A”, or a pharmaceutically acceptable salt thereof, in a therapeutically effective amount.

[0434] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing in a therapeutically effective amount 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula A”, or its pharmaceutically acceptable salt and at least one pharmaceutically acceptable excipient.

[0435] In some embodiments of the present invention, the pharmaceutical composition can be prepared using known, conventional methods in the pharmaceutical field.

[0436] One of the embodiments of the present invention is also a pharmaceutical composition containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula A”, or a pharmaceutically acceptable salt thereof in an amount of 0.01 to 100.00 wt. % of the weight of the pharmaceutical composition.

[0437] One embodiment of the present invention is also a pharmaceutical composition exhibiting Janus kinase (JAK) inhibitor properties for the treatment of autoimmune diseases, comprising 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula A”, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 99.99 wt. % by weight of the pharmaceutical composition.

[0438] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile represented by formula A" or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 0.01 to 85.00 May %, from 0.01 to 80.00 May %, from 0.01 to 75.00 May %, from 0.01 to 70.00 May %, from 0.01 to 65.00 May %, from 0.01 to 60.00 May %, from 0.01 to 55.00 May %, from 0.01 to 40.00 May %, from 0.01 to 35.00 May %, 0.01 to 30.00 May %, 0.01 to 25.00 May %, 0.01 to 20.00 May %, 0.01 to 15.00 May %, 0.01 to 10.00 May %, 0.01 to 9.00 May %, 0.01 to 8.00 May %, 0.01 to 7.00 May %, 0.01 to 6.00 May %, 0.01 to 5.00 May %, 0.01 to 4.00 May %, 0.01 to 3.00 May %, 0.01 to 2.00 May % or 0.01 to 1.00 May % by weight pharmaceutical composition.

[0439] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile represented by formula A" or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 0.10 to 85.00 wt. %, from 0.10 to 80.00 wt. %, from 0.10 to 75.00 wt. %, from 0.10 to 70.00 wt. %, from 0.10 to 65.00 wt. %, from 0.10 to 60.00 wt. %, from 0.10 to 55.00 wt. %, from 0.10 to 40.00 wt. %, from 0.10 to 35.00 May %, from 0.10 to 30.00 May %, from 0.10 to 25.00 May %, from 0.10 to 20.00 May %, from 0.10 to 15.00 May %, from 0.10 to 10.00 May %, from 0.10 to 9.00 May %, from 0.10 to 8.00 May %, from 0.10 to 7.00 May %, from 0.10 to 6.00 May %, from 0.10 to 5.00 May %, from 0.10 to 4.00 May %, from 0.10 to 3.00 May %, from 0.10 to 2.00 May % or from 0.10 to 1.00 May % by weight pharmaceutical composition.

[0440] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile represented by formula A" or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 1.00 to 85.00 wt. %, from 1.00 to 80.00 wt. %, from 1.00 to 75.00 wt. %, from 1.00 to 70.00 wt. %, from 1.00 to 65.00 wt. %, from 1.00 to 60.00 wt. %, from 1.00 to 55.00 wt. %, from 1.00 to 40.00 wt. %, from 1.00 to 35.00 May %, from 1.00 to 30.00 May %, from 1.00 to 25.00 May %, from 1.00 to 20.00 May %, from 1.00 to 15.00 May %, from 1.00 to 10.00 May %, from 1.00 to 9.00 May %, from 1.00 to 8.00 May %, from 1.00 to 7.00 May %, from 1.00 to 6.00 May %, from 1.00 to 5.00 May %, from 1.00 to 4.00 May %, from 1.00 to 3.00 May % or from 1.00 to 2.00 May % by weight of the pharmaceutical composition.

[0441] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile represented by formula A" or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 5.00 to 85.00 wt. %, from 5.00 to 80.00 wt. %, from 5.00 to 75.00 wt. %, from 5.00 to 70.00 wt. %, from 5.00 to 65.00 wt. %, from 5.00 to 60.00 wt. %, from 5.00 to 55.00 wt. %, from 5.00 to 40.00 wt. %, from 5.00 to 35.00 May %, from 5.00 to 30.00 May %, from 5.00 to 25.00 May %, from 5.00 to 20.00 May %, from 5.00 to 15.00 May %, from 5.00 to 10.00 May %, from 5.00 to 9.00 May %, from 5.00 to 8.00 May %, from 5.00 to 7.00 May % or from 5.00 to 6.00 May % of the weight of the pharmaceutical composition.

[0442] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile characterized by formula A" or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 10.00 to 85.00 wt. %, from 10.00 to 80.00 wt. %, from 10.00 to 75.00 wt. %, from 10.00 to 70.00 wt. %, from 10.00 to 65.00 wt. %, from 10.00 to 60.00 wt. %, from 10.00 to 55.00 wt. %, from 10.00 to 40.00 May. %, from 10.00 to 35.00 May. %, from 10.00 to 30.00 May. %, from 10.00 to 25.00 May. %, from 10.00 to 20.00 May. % or from 10.00 to 15.00 May. % of the weight of the pharmaceutical composition.

[0443] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile characterized by formula A" or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 15.00 to 85.00 wt. %, from 15.00 to 80.00 wt. %, from 15.00 to 75.00 wt. %, from 15.00 to 70.00 wt. %, from 15.00 to 65.00 wt. %, from 15.00 to 60.00 wt. %, from 15.00 to 55.00 wt. %, from 15.00 to 40.00 May. %, from 15.00 to 35.00 May. %, from 15.00 to 30.00 May. %, from 15.00 to 25.00 May. % or from 15.00 to 20.00 May. % of the weight of the pharmaceutical composition.

[0444] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile represented by formula A”, or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 0.50 to 5.00 wt. %, from 0.50 to 4.50 wt. %, from 0.50 to 4.00 wt. %, from 0.50 to 3.50 wt. %, from 0.50 to 3.00 wt. %, from 0.50 to 2.50 wt. %, from 0.50 to 2.00 wt. %, from 0.50 to 1.50 wt. % or from 0.50 to 1.00 mass % of the mass of the pharmaceutical composition.

[0445] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula B”, or its pharmaceutically acceptable salt.

[0446] The stated problem is solved and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-y]pyrimidine-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula B”, or a pharmaceutically acceptable salt thereof.

[0447] The stated problem is solved and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-y]pyrimidine-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula B”, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

[0448] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula B”, or a pharmaceutically acceptable salt thereof, in a therapeutically effective amount.

[0449] The stated problem is solved and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile characterized by formula B”, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient in a therapeutically effective amount. In some embodiments of the present invention, the pharmaceutical composition can be obtained using known generally accepted methods in the field of pharmaceuticals.

[0450] One of the embodiments of the present invention is also a pharmaceutical composition containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula B”, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 100.00 wt. % of the weight of the pharmaceutical composition.

[0451] One embodiment of the present invention is also a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula B”, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 99.99 wt. % by weight of the pharmaceutical composition.

[0452] One embodiment of the present invention is a pharmaceutical composition containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula B”, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 99.00 wt. % of the weight of the pharmaceutical composition.

[0453] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile characterized by formula B”, or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 0.01 to 95.00 wt. %, from 0.01 to 90.00 wt. %, from 0.01 to 85.00 wt. %, from 0.01 to 80.00 wt. %, from 0.01 to 75.00 wt. %, from 0.01 to 70.00 wt. %, from 0.01 to 65.00 wt. %, from 0.01 to 60.00 wt. %, from 0.01 to 55.00 wt.%, from 0.01 to 50.00 wt.% or from 0.01 to 40.00 wt.% of the weight of the pharmaceutical composition.

[0454] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile characterized by formula B”, or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 0.01 to 85.00 May. %, from 0.01 to 80.00 May. %, from 0.01 to 75.00 May. %, from 0.01 to 70.00 May. %, from 0.01 to 65.00 May. %, from 0.01 to 60.00 May. %, from 0.01 to 55.00 May. %, from 0.01 to 40.00 May. %, from 0.01 to 35.00 May %, from 0.01 to 30.00 May %, from 0.01 to 25.00 May %, from 0.01 to 20.00 May %, from 0.01 to 15.00 May %, from 0.01 to 10.00 May %, from 0.01 to 9.00 May %, from 0.01 to 8.00 May %, from 0.01 to 7.00 May %, from 0.01 to 6.00 May %, from 0.01 to 5.00 May %, from 0.01 to 4.00 May %, from 0.01 to 3.00 May %, from 0.01 to 2.00 May % or from 0.01 to 1.00 May % by weight of the pharmaceutical composition.

[0455] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile characterized by formula B”, or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 0.10 to 99.00 wt. %, from 0.10 to 95.00 wt. %, from 0.10 to 90.00 wt. %, from 0.10 to 85.00 wt. %, from 0.10 to 80.00 wt. %, from 0.10 to 75.00 wt. %, from 0.10 to 70.00 wt. %, from 0.10 to 65.00 wt. %, from 0.10 to 60.00 May %, from 0.10 to 55.00 May %, from 0.10 to 40.00 May %, from 0.10 to 35.00 May %, from 0.10 to 30.00 May %, from 0.10 to 25.00 May %, from 0.10 to 20.00 May %, from 0.10 to 15.00 May %, from 0.10 to 10.00 May %, from 0.10 to 9.00 May %, from 0.10 to 8.00 May %, from 0.10 to 7.00 May %, from 0.10 to 6.00 May %, from 0.10 to 5.00 May %, from 0.10 to 4.00 May %, from 0.10 to 3.00 May %, from 0.10 to 2.00 May % or from 0.10 to 1.00 May % of the weight of the pharmaceutical composition.

[0456] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile characterized by formula B”, or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 0.50 to 99.00 wt. %, from 0.50 to 95.00 wt. %, from 0.50 to 90.00 wt. %, from 0.50 to 85.00 wt. %, from 0.50 to 80.00 wt. %, from 0.50 to 75.00 wt. %, from 0.50 to 70.00 wt. %, from 0.50 to 65.00 wt. %, from 0.50 to 60.00 wt. %, from 0.50 to 55.00 wt. %, from 0.50 to 50.00 wt. %, from 0.50 to 45.00 wt. % or from 0.50 to 40.00 wt. % of the weight of the pharmaceutical composition.

[0457] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile characterized by formula B”, or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 1.00 to 99.00 wt. %, from 1.00 to 95.00 wt. %, from 1.00 to 90.00 wt. %, from 1.00 to 85.00 wt. %, from 1.00 to 80.00 wt. %, from 1.00 to 75.00 wt. %, from 1.00 to 70.00 wt. %, from 1.00 to 65.00 wt. %, from 1.00 to 60.00 May %, from 1.00 to 55.00 May %, from 1.00 to 40.00 May %, from 1.00 to 35.00 May %, from 1.00 to 30.00 May %, from 1.00 to 25.00 May %, from 1.00 to 20.00 May %, from 1.00 to 15.00 May %, from 1.00 to 10.00 May %, from 1.00 to 9.00 May %, from 1.00 to 8.00 May %, from 1.00 to 7.00 May %, from 1.00 to 6.00 May %, from 1.00 to 5.00 May %, from 1.00 to 4.00 May %, from 1.00 to 3.00 May % or from 1.00 to 2.00 May % of the weight of the pharmaceutical composition.More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile characterized by formula B”, or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 5.00 to 85.00 May. %, from 5.00 to 80.00 May. %, from 5.00 to 75.00 May. %, from 5.00 to 70.00 May. %, from 5.00 to 65.00 May. %, from 5.00 to 60.00 May. %, from 5.00 to 55.00 May. %, from 5.00 to 40.00 May. %, from 5.00 to 35.00 May %, from 5.00 to 30.00 May %, from 5.00 to 25.00 May %, from 5.00 to 20.00 May %, from 5.00 to 15.00 May %, from 5.00 to 10.00 May %, from 5.00 to 9.00 May %, from 5.00 to 8.00 May %, from 5.00 to 7.00 May % or from 5.00 to 6.00 May % of the weight of the pharmaceutical composition.

[0458] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile represented by formula B" or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 10.00 to 85.00 May %, from 10.00 to 80.00 May %, from 10.00 to 75.00 May %, from 10.00 to 70.00 May %, from 10.00 to 65.00 May %, from 10.00 to 60.00 May %, from 10.00 to 55.00 May %, from 10.00 to 40.00 May %, from 10.00 to 35.00 May %, from 10.00 to 30.00 May %, from 10.00 to 25.00 May %, from 10.00 to 20.00 May % or from 10.00 to 15.00 May % of the weight of the pharmaceutical composition.

[0459] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile characterized by formula B" or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 15.00 to 85.00 May %, from 15.00 to 80.00 May %, from 15.00 to 75.00 May %, from 15.00 to 70.00 May %, from 15.00 to 65.00 May %, from 15.00 to 60.00 May %, from 15.00 to 55.00 May %, from 15.00 to 40.00 May %, from 15.00 to 35.00 May %, from 15.00 to 30.00 May %, from 15.00 to 25.00 May % or from 15.00 to 20.00 May % of the weight of the pharmaceutical composition.

[0460] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile characterized by formula B”, or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 0.50 to 5.00 wt. %, from 0.50 to 4.50 wt. %, from 0.50 to 4.00 wt. %, from 0.50 to 3.50 wt. %, from 0.50 to 3.00 wt. %, from 0.50 to 2.50 wt. %, from 0.50 to 2.00 wt. %, from 0.50 to 1.50 wt. % or from 0.50 to 1.00 wt. % of mass of the pharmaceutical composition.

[0461] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula C”, or its pharmaceutically acceptable salt.

[0462] The stated problem is solved and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-c!]pyrimidine-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula C”, or a pharmaceutically acceptable salt thereof.

[0463] The stated problem is solved and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-c!]pyrimidine-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula C”, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

[0464] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula C”, or a pharmaceutically acceptable salt thereof, in a therapeutically effective amount.

[0465] The stated problem is solved, and the claimed technical result is also achieved due to a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula C”, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient in a therapeutically effective amount.

[0466] In some embodiments of the present invention, the pharmaceutical composition can be prepared using known, conventional methods in the pharmaceutical field.

[0467] One of the embodiments of the present invention is also a pharmaceutical composition containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula C”, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 100.00 wt. % of the weight of the pharmaceutical composition.

[0468] One embodiment of the present invention is also a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula C”, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 99.99 wt. % by weight of the pharmaceutical composition.

[0469] One embodiment of the present invention is a pharmaceutical composition containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula C”, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 99.00 wt. % of the weight of the pharmaceutical composition.

[0470] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile characterized by formula C”, or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 0.01 to 95.00 wt. %, from 0.01 to 90.00 wt. %, from 0.01 to 85.00 wt. %, from 0.01 to 80.00 wt. %, from 0.01 to 75.00 wt. %, from 0.01 to 70.00 wt. %, from 0.01 to 65.00 wt. %, from 0.01 to 60.00 wt. %, from 0.01 to 55.00 wt. %, from 0.01 to 50.00 wt. % or from 0.01 to 40.00 wt. %, from 0.01 to 35.00 wt. %, from 0.01 to 30.00 wt. %, from 0.01 to 25.00 wt. %, from 0.01 to 20.00 wt. %, from 0.01 to 15.00 wt. %, from 0.01 to 10.00 wt. %, from 0.01 to 9.00 wt. %, from 0.01 to 8.00 wt. %, from 0.01 to 7.00 wt. %, from 0.01 to 6.00 wt. %, from 0.01 to 5.00 wt. %, from 0.01 to 4.00 wt. %, from 0.01 to 3.00 May %, from 0.01 to 2.00 May % or from 0.01 to 1.00 May % of the weight of the pharmaceutical composition.

[0471] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile characterized by formula C”, or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 0.10 to 99.00 wt. %, from 0.10 to 95.00 wt. %, from 0.10 to 90.00 wt. %, from 0.10 to 85.00 wt. %, from 0.10 to 80.00 wt. %, from 0.10 to 75.00 wt. %, from 0.10 to 70.00 wt. %, from 0.10 to 65.00 wt. %, from 0.10 to 60.00 wt. %, from 0.10 to 55.00 wt. %, from 0.10 to 50.00 wt. %, from 0.10 to 45.00 wt. %, or from 0.10 to 40.00 wt. %, from 0.10 to 35.00 wt. %, from 0.10 to 30.00 wt. %, from 0.10 to 25.00 wt. %, from 0.10 to 20.00 wt. %, from 0.10 to 15.00 wt. %, from 0.10 to 10.00 wt. %, from 0.10 to 9.00 wt. %, from 0.10 to 8.00 wt. %, from 0.10 to 7.00 wt. %, from 0.10 to 6.00 May %, from 0.10 to 5.00 May %, from 0.10 to 4.00 May %, from 0.10 to 3.00 May %, from 0.10 to 2.00 May % or from 0.10 to 1.00 May. % of the weight of the pharmaceutical composition.

[0472] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile represented by formula C”, or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 0.50 to 99.00 wt. %, from 0.50 to 95.00 wt. %, from 0.50 to 90.00 wt. %, from 0.50 to 85.00 wt. %, from 0.50 to 80.00 wt. %, from 0.50 to 75.00 wt. %, from 0.50 to 70.00 wt. %, from 0.50 to 65.00 wt. %, from 0.50 to 60.00 wt. %, from 0.50 to 55.00 wt. %, from 0.50 to 50.00 wt. %, from 0.50 to 45.00 wt. % or from 0.50 to 40.00 wt. % of the weight of the pharmaceutical composition.

[0473] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile characterized by formula C”, or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 1.00 to 99.00 wt. %, from 1.00 to 95.00 wt. %, from 1.00 to 90.00 wt. %, from 1.00 to 85.00 wt. %, from 1.00 to 80.00 wt. %, from 1.00 to 75.00 wt. %, from 1.00 to 70.00 wt. %, from 1.00 to 65.00 wt. %, from 1.00 to 60.00 wt. %, from 1.00 to 55.00 wt. %, from 1.00 to 50.00 wt. %, from 1.00 to 45.00 wt. % or from 1.00 to 40.00 wt. %, from 1.00 to 35.00 wt. %, from 1.00 to 30.00 wt. %, from 1.00 to 25.00 wt. %, from 1.00 to 20.00 wt. %, from 1.00 to 15.00 wt. %, from 1.00 to 10.00 wt. %, from 1.00 to 9.00 wt. %, from 1.00 to 8.00 wt. %, from 1.00 to 7.00 wt. %, from 1.00 to 6.00 May. %, from 1.00 to 5.00 May. %, from 1.00 to 4.00 May. %, from 1.00 to 3.00 May. % or from 1.00 to 2.00 May.% of the weight of the pharmaceutical composition.

[0474] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile represented by formula C" or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 5.00 to 85.00 wt. %, from 5.00 to 80.00 wt. %, from 5.00 to 75.00 wt. %, from 5.00 to 70.00 wt. %, from 5.00 to 65.00 wt. %, from 5.00 to 60.00 wt. %, from 5.00 to 55.00 wt. %, from 5.00 to 40.00 wt. %, from 5.00 to 35.00 May %, from 5.00 to 30.00 May %, from 5.00 to 25.00 May %, from 5.00 to 20.00 May %, from 5.00 to 15.00 May %, from 5.00 to 10.00 May %, from 5.00 to 9.00 May %, from 5.00 to 8.00 May %, from 5.00 to 7.00 May % or from 5.00 to 6.00 May % of the weight of the pharmaceutical composition.

[0475] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile represented by formula C" or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 10.00 to 85.00 wt. %, from 10.00 to 80.00 wt. %, from 10.00 to 75.00 wt. %, from 10.00 to 70.00 wt. %, from 10.00 to 65.00 wt. %, from 10.00 to 60.00 wt. %, from 10.00 to 55.00 wt. %, from 10.00 to 40.00 May. %, from 10.00 to 35.00 May. %, from 10.00 to 30.00 May. %, from 10.00 to 25.00 May. %, from 10.00 to 20.00 May. % or from 10.00 to 15.00 May. % of the weight of the pharmaceutical composition.

[0476] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile characterized by formula C”, or a pharmaceutically acceptable salt thereof in the pharmaceutical composition of the present invention is from 15.00 to 85.00 wt. %, from 15.00 to 80.00 wt. %, from 15.00 to 75.00 wt. %, from 15.00 to 70.00 wt. %, from 15.00 to 65.00 wt. %, from 15.00 to 60.00 wt. %, from 15.00 to 55.00 wt. %, from 15.00 to 40.00 May. %, from 15.00 to 35.00 May. %, from 15.00 to 30.00 May. %, from 15.00 to 25.00 May. % or from 15.00 to 20.00 May. % of the weight of the pharmaceutical composition.

[0477] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile represented by formula C”, or a pharmaceutically acceptable salt thereof according to the present invention in the pharmaceutical composition is from 0.50 to 5.00 wt. %, from 0.50 to 4.50 wt. %, from 0.50 to 4.00 wt. %, from 0.50 to 3.50 wt. %, from 0.50 to 3.00 wt. %, from 0.50 to 2.50 wt. %, from 0.50 to 2.00 wt. %, from 0.50 to 1.50 wt. % or from 0.50 to 1.00 mass % of the mass of the pharmaceutical composition.

[0478] One embodiment of the present invention is any of the above-mentioned pharmaceutical compositions, wherein at least one pharmaceutically acceptable excipient is selected from the group consisting of excipients, stabilizers, solubilizers, solvents, humectants, lubricants, glidants, thickeners, sweeteners, flavorings, aromatizers, fungicides, prolonged delivery regulators, co-solvents, diluents, fillers, emulsifiers, preservatives, antioxidants, buffering agents, cryoprotectants, pH-regulating agents, substances for maintaining isotonicity or correcting substances.

[0479] One embodiment of the present invention is any of the above-mentioned pharmaceutical compositions, characterized in that it contains at least one pharmaceutically acceptable excipient in an amount of from 0.00 to 99.99% by weight of the pharmaceutical composition.

[0480] One embodiment of the present invention is a pharmaceutical composition characterized in that it contains at least one pharmaceutically acceptable excipient in an amount of from 0.01 to 99.99% by weight of the pharmaceutical composition.

[0481] More preferably, the content of at least one pharmaceutically acceptable excipient in the above-mentioned pharmaceutical composition of the present invention is from 0.01 to 95.00 wt. %, from 0.01 to 90.00 wt. %, from 0.01 to 85.00 wt. %, from 0.01 to 80.00 wt. %, from 0.01 to 75.00 wt. %, from 0.01 to 70.00 wt. %, from 0.01 to 65.00 wt. %, from 0.01 to 60.00 wt. %, from 0.01 to 55.00 wt. %, from 0.01 to 50.00 wt. % or from 0.01 to 40.00 wt. % of the weight of the pharmaceutical composition.

[0482] More preferably, the content of at least one pharmaceutically acceptable excipient in the above-mentioned pharmaceutical composition is from 0.10 to 99.99 wt. %, from 0.10 to 95.00 wt. %, from 0.10 to 90.00 wt. %, from 0.10 to 85.00 wt. %, from 0.10 to 80.00 wt. %, from 0.10 to 75.00 wt. %, from 0.10 to 70.00 wt. %, from 0.10 to 65.00 wt. %, from 0.10 to 60.00 wt. %, from 0.10 to 55.00 wt. %, from 0.10 to 50.00 wt. %, from 0.10 to 45.00 wt. %, or from 0.10 to 40.00 wt. % of the weight of the pharmaceutical composition.

[0483] More preferably, the content of at least one pharmaceutically acceptable excipient in the pharmaceutical composition of the present invention is from 1.00 to 95.00 wt. %, from 1.00 to 90.00 wt. %, from 1.00 to 85.00 wt. %, from 1.00 to 80.00 wt. %, from 1.00 to 75.00 wt. %, from 1.00 to 70.00 wt. %, from 1.00 to 65.00 wt. %, from 1.00 to 60.00 wt. %, from 1.00 to 55.00 wt. %, from 1.00 to 50.00 wt. %, from 1.00 to 45.00 wt. % or from 1.00 to 40.00 wt. % of the weight of the pharmaceutical composition.

[0484] More preferably, the content of at least one pharmaceutically acceptable excipient in the pharmaceutical composition of the present invention is from 1.00 to 99.90 wt. %, from 10.00 to 99.90 wt. %, from 20.00 to 99.90 wt. %, from 30.00 to 99.90 wt. %, from 40.00 to 99.90 wt. %, from 50.00 to 99.90 wt. %, from 60.00 to 99.90 wt. %, from 70.00 to 99.90 wt. %, from 80.00 to 99.90 wt. %, from 90.00 to 99.90 wt. %, from 95.00 to 99.90 wt. % or from 97.00 to 99.90 wt. % of the weight of the pharmaceutical composition.

[0485] More preferably, the content of at least one pharmaceutically acceptable excipient in the pharmaceutical composition of the present invention is from 10.00 to 99.50 wt. %, from 10.00 to 99.40 wt. %, from 10.00 to 99.30 wt. %, from 10.00 to 99.20 wt. %, from 10.00 to 99.10 wt. %, from 10.00 to 99.00 wt. %, from 10.00 to 98.90 wt. %, from 10.00 to 98.80 wt. %, from 10.00 to 98.70 wt. %, from 10.00 to 98.60 wt. %, from 10.00 to 98.50 wt. %, from 10.00 to 98.40 wt. %, from 10.00 to 98.30 wt. %, from 10.00 to 98.20 wt. %, from 10.00 to 98.10 wt. %, from 10.00 to 98.00 wt. % of the weight of the pharmaceutical composition.

[0486] More preferably, the content of at least one pharmaceutically acceptable excipient in the pharmaceutical composition of the present invention is from 90.00 to 99.90 wt. %, from 90.00 to 99.80 wt. %, from 90.00 to 99.70 wt. %, from 90.00 to 99.60 wt. %, from 90.00 to 99.50 wt. %, from 90.00 to 99.40 wt. %, from 90.00 to 99.30 wt. %, from 90.00 to 99.20 wt. %, from 90.00 to 99.10 wt. %, from 90.00 to 99.00 wt. %, from 90.00 to 98.90 wt. %, from 90.00 to 98.80 wt. %, from 90.00 to 98.70 wt. %, from 90.00 to 98.60 wt. %, from 90.00 to 98.50 wt. %, from 90.00 to 98.40 wt. %, from 90.00 to 98.30 wt. %, from 90.00 to 98.20 wt. %, from 90.00 to 98.10 wt. %, from 90.00 to 98.00 wt. %, from 95.00 to 99.90 wt. %, from 96.00 to 99.90 wt. %, from 97.00 to 99.90 wt. % or from 98.00 to 99.90 wt. % of the weight of the pharmaceutical composition.

[0487] One embodiment of the present invention is any of the above-mentioned pharmaceutical compositions comprising a compound of formula A or a pharmaceutically acceptable salt thereof, a compound of formula B or a pharmaceutically acceptable salt thereof, a compound of formula C or a pharmaceutically acceptable salt thereof, a compound of formula A' ' or a pharmaceutically acceptable salt thereof, a compound of formula B", or a pharmaceutically acceptable salt thereof, or a compound of formula C" or a pharmaceutically acceptable salt thereof, characterized in that it exhibits therapeutic activity against autoimmune diseases selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, juvenile arthritis, atopic dermatitis, lupus and alopecia.

[0488] More preferably, a pharmaceutical composition comprising a compound of formula A or a pharmaceutically acceptable salt thereof, a compound of formula B or a pharmaceutically acceptable salt thereof, a compound of formula C or a pharmaceutically acceptable salt thereof, a compound of formula A" or a pharmaceutically acceptable salt thereof, a compound of formula B" or a pharmaceutically acceptable salt thereof, or a compound of formula C" or a pharmaceutically acceptable salt thereof, is characterized in that it exhibits therapeutic activity against a disease according to the present invention selected from the group of JAK-mediated diseases or disorders.

[0489] More preferably, a pharmaceutical composition comprising a compound of formula A or a pharmaceutically acceptable salt thereof, a compound of formula B or a pharmaceutically acceptable salt thereof, a compound of formula C or a pharmaceutically acceptable salt thereof, a compound of formula A" or a pharmaceutically acceptable salt thereof, a compound of formula B" or a pharmaceutically acceptable salt thereof, or a compound of formula C" or a pharmaceutically acceptable salt thereof, is characterized in that it exhibits therapeutic activity against diseases selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, juvenile arthritis, chronic polyarthritis, atopic dermatitis, juvenile idiopathic arthritis, alopecia (focal alopecia, frontal fibrosing alopecia, alopecia areata, including in severe or very severe forms), multiple sclerosis, multiple sclerosis, amyotrophic lateral sclerosis, neurodegenerative Alzheimer's disease,

[0490] Type 1 diabetes, diabetic kidney disease, aggressive albuminuria reduction in biopsy-proven diabetic nephropathy, lupus, systemic lupus erythematosus, lupus nephritis, psoriasis,

[0491] inflammatory bowel disease, ulcerative colitis, Crohn's disease, severe pseudoparalytic myasthenia, immunoglobulin nephropathy, autoimmune thyroid disease, pemphigus vulgaris, bullous pemphigoid, allergic reactions such as asthma, food allergies, atopic dermatitis and rhinitis,

[0492] viral diseases such as Epstein-Barr virus, hepatitis B, hepatitis C, human immunodeficiency virus, varicella-zoster virus and human papillomavirus, coronavirus, COVID-19,

[0493] Skin rashes, skin irritations, skin sensitization (e.g. contact dermatitis or allergic contact dermatitis), cutaneous lichen planus, cancer, including cancer characterized by the formation of solid tumors (e.g. prostate cancer, kidney cancer, liver cancer, pancreatic cancer, stomach cancer, breast cancer, lung cancer, head and neck cancer, thyroid cancer, glioblastoma, Kaposi's sarcoma, Castleman's disease, melanoma, etc.), blood cancer (e.g., lymphoma, leukemia such as acute lymphoblastic leukemia, acute myelogenous leukemia (AML), or multiple myeloma) and skin cancer such as cutaneous T-cell lymphoma (CTCL) and cutaneous B-cell lymphoma, typical cutaneous T-cell lymphomas include Sézary syndrome and mycosis fungoides, myeloproliferative disorders (MPDs) such as polycythemia vera (PV), essential thrombocythemia (ET), myelofibrosis with myeloid metaplasia (MFM), chronic myeloid leukemia (CML), chronic myelomonocytic leukemia (CMML), hypereosinophilic syndrome (HES), systemic mastocytosis (SM) associated with colitis, colon cancer, colorectal cancer colon, gastric cancer, gastrointestinal carcinoid tumor, gastrointestinal stromal tumor (GIST), adenocarcinoma, small intestine cancer, rectal cancer, etc.

[0494] Inflammatory diseases include inflammatory diseases of the eye (e.g., iritis, uveitis, scleritis, conjunctivitis, or related diseases), refractory non-infectious non-anterior uveitis, inflammatory diseases of the airways (e.g., upper respiratory tract, including diseases of the nose and sinuses, such as rhinitis or sinusitis, lower respiratory tract, including bronchitis, chronic non-specific lung disease, etc.), inflammatory myopathy, such as myocarditis, and other inflammatory diseases, ischemia-reperfusion injury or diseases or conditions associated with an inflammatory ischemic event, such as stroke or cardiac arrest, systemic inflammatory response syndrome, septic shock, large inflammatory hepatocellular adenomas,

[0495] anorexia, cachexia, or fatigue caused by or associated with cancer,

[0496] pathological conditions associated with hypoxia or astrogliosis, such as diabetic retinopathy, cancer or neurodegeneration,

[0497] Gout, prostate enlargement, dry eye syndrome and related disorders, IgG4-related disorders, idiopathic granulomatous mastitis, pyoderma gangrenosum, cutaneous dermatomyositis, idiopathic inflammatory myositis, chronic atypical neutrophilic dermatosis with lipodystrophy and fever (Nakayo-Nishimura syndrome), interferon gene promoter-associated vasculopathy, Aicardi-Goutières syndrome, graft-versus-host disease, including after peripheral blood hematopoietic cell transplantation, neuromyelitis, immune thrombocytopenia, coronavirus pneumonia (COVID-19), symptoms associated with COVID-19 infection, hospital-acquired pneumonia in critically ill patients with a proinflammatory phenotype, lung injury after spontaneous subarachnoid hemorrhages, ocular mucosal pemphigoid, oral lichen planus, steroid-resistant / relapsing immune thrombocytopenia,Pulmonary injury after intracerebral hemorrhage, moderate to severe traumatic intracerebral hemorrhage / contusion, recurrent giant cell arteritis, systemic sclerosis, treatment of nonsegmental vitiligo, treatment of HIV symptoms, autoinflammatory syndrome, primary biliary cholangitis, recurrent or naive dermatomyositis, Sjogren's syndrome, inflammation and depression in people with HIV, APOL1-associated kidney disease, polymyalgia rheumatica, idiopathic inflammatory myopathy.

[0498] In some embodiments, one or more compounds of the present invention may be used in combination with other active agents.

[0499] The stated problem is solved, and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof.

[0500] The stated problem is solved, and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

[0501] The stated problem is solved, and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing in an effective amount a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

[0502] One embodiment of the present invention is a medicinal product containing a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof in an amount of from 0.50 to 100.00 mg.

[0503] One embodiment of the present invention is a medicinal product containing a therapeutically effective amount of a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof in an amount of from 0.50 to 100.00 mg.

[0504] More preferably, the content of the compound represented by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof according to the present invention in the medicament is from 0.50 to 95.00 mg, from 0.50 to 90.00 mg, from 0.50 to 85.00 mg, from 0.50 to 80.00 mg, from 0.50 to 75.00 mg, from 0.50 to 70.00 mg, from 0.50 to 65.00 mg, from 0.50 to 60.00 mg, from 0.50 to 55.00 mg, from 0.50 to 50.00 mg, from 0.50 to 45.00 mg, from 0.50 to 40.00 mg, from 0.50 to 35.00 mg, from 0.50 to 30.00 mg, 0.50 to 25.00 mg, 0.50 to 20.00 mg, 0.50 to 15.00 mg, 0.50 to 10.00 mg, 0.50 to 9.00 mg, 0.50 to 8.00 mg, 0.50 to 7.00 mg, 0.50 to 6.00 mg, 0.50 to 5.00 mg, 0.50 to 4.00 mg, 0.50 to 3.00 mg, 0.50 to 2.00 mg, or 0.50 to 1.00 mg.

[0505] One embodiment of the present invention is a medicinal product containing a therapeutically effective amount of a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof in an amount of from 0.50 to 10.00 mg.

[0506] More preferably, the content of the compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof according to the present invention in the medicament is from 0.50 to 9.50 mg, from 0.50 to 9.00 mg, from 0.50 to 8.50 mg, from 0.50 to 8.00 mg, from 0.50 to 7.50 mg, from 0.50 to 7.00 mg, from 0.50 to 6.50 mg, from 0.50 to 6.00 mg, from 0.50 to 5.50 mg, from 0.50 to 5.00 mg, from 0.50 to 4.50 mg, from 0.50 to 4.00 mg, from 0.50 to 3.50 mg, from 0.50 to 3.00 mg, from 0.50 up to 2.50 mg or from 0.50 to 2.00 mg.

[0507] One embodiment of the present invention is a medicinal product containing a therapeutically effective amount of a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof in an amount of from 1.00 to 5.00 mg or from 2.00 to 4.00 mg.

[0508] One embodiment of the present invention is a medicinal product containing a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 99.00 mass % of the mass of the medicinal product.

[0509] More preferably, the content of the compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof according to the present invention in the drug is from 0.01 to 95.00 wt. %, from 0.01 to 90.00 wt. %, from 0.01 to 85.00 wt. %, from 0.01 to 80.00 wt. %, from 0.01 to 75.00 wt. %, from 0.01 to 70.00 wt. %, from 0.01 to 65.00 wt. %, from 0.01 to 60.00 wt. %, from 0.01 to 55.00 wt. %, from 0.01 to 50.00 wt. %, from 0.01 to 40.00 wt. %,

[0510] from 0.10 to 99.00 wt. %, from 0.10 to 95.00 wt. %, from 0.10 to 90.00 wt. %, from 0.10 to 85.00 wt. %, from 0.10 to 80.00 wt. %, from 0.10 to 75.00 wt. %, from 0.10 to 70.00 wt. %, from 0.10 to 65.00 wt. %, from 0.10 to 60.00 wt. %, from 0.10 to 55.00 wt. %, from 0.10 to 50.00 wt. %, from 0.10 to 45.00 wt. %, from 0.10 to 40.00 wt. %,

[0511] from 0.50 to 99.00 wt. %, from 0.50 to 95.00 wt. %, from 0.50 to 90.00 wt. %, from 0.50 to 85.00 wt. %, from 0.50 to 80.00 wt. %, from 0.50 to 75.00 wt. %, from 0.50 to 70.00 wt. %, from 0.50 to 65.00 wt. %, from 0.50 to 60.00 wt. %, from 0.50 to 55.00 wt. %, from 0.50 to 50.00 wt. %, from 0.50 to 45.00 wt. %, from 0.50 to 40.00 wt. %, from 1.00 to 99.00 wt. %, from 1.00 to 95.00 wt. %, from 1.00 to 90.00 wt. %, from 1.00 to 85.00 wt. %, from 1.00 to 80.00 wt. %, from 1.00 to 75.00 wt. %, from 1.00 to 70.00 wt. %, from 1.00 to 65.00 wt. %, from 1.00 to 60.00 wt. %, from 1.00 to 55.00 wt. %, from 1.00 to 50.00 wt. %, from 1.00 to 45.00 wt. %, from 1.00 to 40.00 wt. %,

[0512] from 0.50 to 5.00 wt. %, from 0.50 to 4.50 wt. %, from 0.50 to 4.00 wt. %, from 0.50 to 3.50 wt. %, from 0.50 to 3.00 wt. %, from 0.50 to 2.50 wt. %, from 0.50 to 2.00 wt. %, from 0.50 to 1.50 wt. % or from 0.50 to 1.00 wt. % of the weight of the medicinal product.

[0513] In one embodiment of the present invention, the effective dosage of a compound characterized by formula (I)', formula IV, or formula IV", or a pharmaceutically acceptable salt thereof, is in the range of about 0.05 to 50.00 mg per day per patient in need of such treatment.

[0514] More preferably, the effective dosage of the compound of formula (I)', formula IV, or formula IV", or a pharmaceutically acceptable salt thereof, according to the present invention is from 0.05 to 10.00 mg, from 0.05 to 9.00 mg, from 0.05 to 8.00 mg, from 0.05 to 7.00 mg, from 0.05 to 6.00 mg, from 0.05 to 5.00 mg, from 0.05 to 4.00 mg, from 0.05 to 3.50 mg, from 0.05 to 3.00 mg, from 0.05 to 2.50 mg, from 0.05 to 2.00 mg, from 0.05 to 1.50 mg, from 0.05 to 1.00 mg, from 0.05 to 0.50 mg, or from 0.50 up to 5.00 mg, from 0.50 to 4.50 mg, from 0.50 to 4.00 mg, from 0.50 to 3.50 mg, from 0.50 to 3.00 mg, from 0.50 to 2.50 mg, from 0.50 to 2.00 mg or from 1.00 to 5.00 mg, from 1.00 to 4.50 mg, from 1.00 to 4.00 mg, from 1.00 to 3.50 mg, from 1.00 to 3.00 mg, from 1.00 to 2.50 mg, from 1.00 to 2.00 mg or from 2.00 to 5.00 mg or from 1.00 to 4.00 mg per day.

[0515] If necessary, doses are usually divided into several smaller doses to be administered throughout the day.

[0516] The stated problem is solved, and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile, characterized by formula A, or its pharmaceutically acceptable salt.

[0517] The stated problem is solved, and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor, for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile, characterized by formula A, or its pharmaceutically acceptable salt, and at least one pharmaceutically acceptable excipient. The stated problem is solved, and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing in an effective amount 2-(3-(4-(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile, characterized by formula A, or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient.

[0518] One embodiment of the present invention is a medicinal product containing 2-(3-(4-(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile, characterized by formula A, or a pharmaceutically acceptable salt thereof in an amount of 0.50 to 100.00 mg.

[0519] One embodiment of the present invention is a medicinal product containing a therapeutically effective amount of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile, characterized by formula A, or a pharmaceutically acceptable salt thereof in an amount of from 0.50 to 100.00 mg.

[0520] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile characterized by formula A or a pharmaceutically acceptable salt thereof according to the present invention in the drug is from 0.50 to 95.00 mg, from 0.50 to 90.00 mg, from 0.50 to 85.00 mg, from 0.50 to 80.00 mg, from 0.50 to 75.00 mg, from 0.50 to 70.00 mg, from 0.50 to 65.00 mg, from 0.50 to 60.00 mg, from 0.50 to 55.00 mg, from 0.50 to 50.00 mg, 0.50 to 45.00 mg, 0.50 to 40.00 mg, 0.50 to 35.00 mg, 0.50 to 30.00 mg, 0.50 to 25.00 mg, 0.50 to 20.00 mg, 0.50 to 15.00 mg, 0.50 to 10.00 mg, 0.50 to 9.00 mg, 0.50 to 8.00 mg, 0.50 to 7.00 mg, 0.50 to 6.00 mg, 0.50 to 5.00 mg, 0.50 to 4.00 mg, 0.50 to 3.00 mg, 0.50 to 2.00 mg or 0.50 up to 1.00 mg.

[0521] One embodiment of the present invention is a medicinal product containing a therapeutically effective amount of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile, characterized by formula A, or a pharmaceutically acceptable salt thereof in an amount of from 0.50 to 10.00 mg.

[0522] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile characterized by formula A or a pharmaceutically acceptable salt thereof according to the present invention in the medicinal product is from 0.50 to 9.50 mg, from 0.50 to 9.00 mg, from 0.50 to 8.50 mg, from 0.50 to 8.00 mg, from 0.50 to 7.50 mg, from 0.50 to 7.00 mg, from 0.50 to 6.50 mg, from 0.50 to 6.00 mg, from 0.50 to 5.50 mg, from 0.50 to 5.00 mg, from 0.50 to 4.50 mg, 0.50 to 4.00 mg, 0.50 to 3.50 mg, 0.50 to 3.00 mg, 0.50 to 2.50 mg, or 0.50 to 2.00 mg.

[0523] One embodiment of the present invention is a medicinal product containing a therapeutically effective amount of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile, characterized by formula A, or a pharmaceutically acceptable salt thereof in an amount of from 1.00 to 5.00 mg or from 2.00 to 4.00 mg.

[0524] One embodiment of the present invention is a medicinal product containing 2-(3-(4-(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile, characterized by formula A, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 99.00 wt. % of the mass of the medicinal product.

[0525] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile characterized by formula A or a pharmaceutically acceptable salt thereof according to the present invention in the drug is from 0.01 to 95.00 wt. %, from 0.01 to 90.00 wt. %, from 0.01 to 85.00 wt. %, from 0.01 to 80.00 wt. %, from 0.01 to 75.00 wt. %, from 0.01 to 70.00 wt. %, from 0.01 to 65.00 wt. %, from 0.01 to 60.00 wt. %, from 0.01 to 55.00 mass %, from 0.01 to 50.00 mass %, from 0.01 to 40.00 mass %,

[0526] from 0.10 to 99.00 wt. %, from 0.10 to 95.00 wt. %, from 0.10 to 90.00 wt. %, from 0.10 to 85.00 wt. %, from 0.10 to 80.00 wt. %, from 0.10 to 75.00 wt. %, from 0.10 to 70.00 wt. %, from 0.10 to 65.00 wt. %, from 0.10 to 60.00 wt. %, from 0.10 to 55.00 wt. %, from 0.10 to 50.00 wt. %, from 0.10 to 45.00 wt. %, from 0.10 to 40.00 wt. %,

[0527] from 0.50 to 99.00 wt. %, from 0.50 to 95.00 wt. %, from 0.50 to 90.00 wt. %, from 0.50 to 85.00 wt. %, from 0.50 to 80.00 wt. %, from 0.50 to 75.00 wt. %, from 0.50 to 70.00 wt. %, from 0.50 to 65.00 wt. %, from 0.50 to 60.00 wt. %, from 0.50 to 55.00 wt. %, from 0.50 to 50.00 wt. %, from 0.50 to 45.00 wt. %, from 0.50 to 40.00 wt. %,

[0528] from 1.00 to 99.00 wt. %, from 1.00 to 95.00 wt. %, from 1.00 to 90.00 wt. %, from 1.00 to 85.00 wt. %, from 1.00 to 80.00 wt. %, from 1.00 to 75.00 wt. %, from 1.00 to 70.00 wt. %, from 1.00 to 65.00 wt. %, from 1.00 to 60.00 wt. %, from 1.00 to 55.00 wt. %, from 1.00 to 50.00 wt. %, from 1.00 to 45.00 wt. %, from 1.00 to 40.00 wt. %,

[0529] from 0.50 to 5.00 wt. %, from 0.50 to 4.50 wt. %, from 0.50 to 4.00 wt. %, from 0.50 to 3.50 wt. %, from 0.50 to 3.00 wt. %, from 0.50 to 2.50 wt. %, from 0.50 to 2.00 wt. %, from 0.50 to 1.50 wt. % or from 0.50 to 1.00 wt. % of the weight of the medicinal product. In one embodiment of the present invention, the effective dosage of 2-(3-(4-(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile, characterized by formula A, or a pharmaceutically acceptable salt thereof, is in the range of about 0.05 to 50.00 mg per day per patient in need of such treatment.

[0530] More preferably, the effective dosage of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidine yn-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetide yn-3-yl)acetonitrile characterized by formula A, or a pharmaceutically acceptable salt thereof, according to the present invention is from 0.05 to 10.00 mg, from 0.05 to 9.00 mg, from 0.05 to 8.00 mg, from 0.05 to 7.00 mg, from 0.05 to 6.00 mg, from 0.05 to 5.00 mg, from 0.05 to 4.00 mg, from 0.05 to 3.50 mg, from 0.05 to 3.00 mg, from 0.05 to 2.50 mg, from 0.05 to 2.00 mg, 0.05 to 1.50 mg, 0.05 to 1.00 mg, 0.05 to 0.50 mg or 0.50 to 5.00 mg, 0.50 to 4.50 mg, 0.50 to 4.00 mg, 0.50 to 3.50 mg, 0.50 to 3.00 mg, 0.50 to 2.50 mg, 0.50 to 2.00 mg or 1.00 to 5.00 mg, 1.00 to 4.50 mg, 1.00 to 4.00 mg, 1.00 to 3.50 mg, 1.00 to 3.00 mg, 1.00 to 2.50 mg, 1.00 to 2.00 mg or 2.00 to 5.00 mg or 1.00 to 4.00 mg per day.

[0531] If necessary, doses are usually divided into several smaller doses to be administered throughout the day.

[0532] The stated problem is solved, and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3 -d]pyrimidine yn-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetide yn-3-yl)acetonitrile, characterized by formula B, or a pharmaceutically acceptable salt thereof.

[0533] The stated problem is solved, and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor, for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3 -d]pyrimidine yn-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetide yn-3-yl)acetonitrile, characterized by formula B, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

[0534] The stated problem is solved, and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing in an effective amount 2-(3-(4-(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile, characterized by formula B, or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient.

[0535] One embodiment of the present invention is a medicinal product containing 2-(3-(4-(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile, characterized by formula B, or a pharmaceutically acceptable salt thereof in an amount of 0.50 to 100.00 mg.

[0536] One embodiment of the present invention is a medicinal product containing a therapeutically effective amount of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile, characterized by formula B, or a pharmaceutically acceptable salt thereof in an amount of 0.50 to 100.00 mg.

[0537] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile characterized by formula B or a pharmaceutically acceptable salt thereof according to the present invention in the drug is from 0.50 to 95.00 mg, from 0.50 to 90.00 mg, from 0.50 to 85.00 mg, from 0.50 to 80.00 mg, from 0.50 to 75.00 mg, from 0.50 to 70.00 mg, from 0.50 to 65.00 mg, from 0.50 to 60.00 mg, from 0.50 to 55.00 mg, from 0.50 to 50.00 mg, 0.50 to 45.00 mg, 0.50 to 40.00 mg, 0.50 to 35.00 mg, 0.50 to 30.00 mg, 0.50 to 25.00 mg, 0.50 to 20.00 mg, 0.50 to 15.00 mg, 0.50 to 10.00 mg, 0.50 to 9.00 mg, 0.50 to 8.00 mg, 0.50 to 7.00 mg, 0.50 to 6.00 mg, 0.50 to 5.00 mg, 0.50 to 4.00 mg, 0.50 to 3.00 mg, 0.50 to 2.00 mg or 0.50 up to 1.00 mg.

[0538] One embodiment of the present invention is a medicinal product containing a therapeutically effective amount of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile, characterized by formula B, or a pharmaceutically acceptable salt thereof in an amount of 0.50 to 10.00 mg.

[0539] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile characterized by formula B or a pharmaceutically acceptable salt thereof according to the present invention in the drug is from 0.50 to 9.50 mg, from 0.50 to 9.00 mg, from 0.50 to 8.50 mg, from 0.50 to 8.00 mg, from 0.50 to 7.50 mg, from 0.50 to 7.00 mg, from 0.50 to 6.50 mg, from 0.50 to 6.00 mg, from 0.50 to 5.50 mg, from 0.50 to 5.00 mg, from 0.50 to 4.50 mg, from 0.50 to 4.00 mg, from 0.50 to 3.50 mg, from 0.50 to 3.00 mg, from 0.50 to 2.50 mg or from 0.50 to 2.00 mg. One embodiment of the present invention is a medicament containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidine-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile characterized by formula B, or a pharmaceutically acceptable salt thereof in an amount of from 1.00 to 5.00 mg, from 2.00 to 4.00 mg in a therapeutically effective amount.

[0540] One embodiment of the present invention is a medicinal product containing 2-(3-(4-(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile, characterized by formula B, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 99.00 wt. % of the mass of the medicinal product.

[0541] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetidin-3-yl)acetonitrile characterized by formula B or a pharmaceutically acceptable salt thereof according to the present invention in the drug is from 0.01 to 95.00 wt. %, from 0.01 to 90.00 wt. %, from 0.01 to 85.00 wt. %, from 0.01 to 80.00 wt. %, from 0.01 to 75.00 wt. %, from 0.01 to 70.00 wt. %, from 0.01 to 65.00 wt. %, from 0.01 to 60.00 wt. %, from 0.01 to 55.00 mass %, from 0.01 to 50.00 mass %, from 0.01 to 40.00 mass %,

[0542] from 0.10 to 99.00 wt. %, from 0.10 to 95.00 wt. %, from 0.10 to 90.00 wt. %, from 0.10 to 85.00 wt. %, from 0.10 to 80.00 wt. %, from 0.10 to 75.00 wt. %, from 0.10 to 70.00 wt. %, from 0.10 to 65.00 wt. %, from 0.10 to 60.00 wt. %, from 0.10 to 55.00 wt. %, from 0.10 to 50.00 wt. %, from 0.10 to 45.00 wt. %, from 0.10 to 40.00 wt. %,

[0543] from 0.50 to 99.00 wt. %, from 0.50 to 95.00 wt. %, from 0.50 to 90.00 wt. %, from 0.50 to 85.00 wt. %, from 0.50 to 80.00 wt. %, from 0.50 to 75.00 wt. %, from 0.50 to 70.00 wt. %, from 0.50 to 65.00 wt. %, from 0.50 to 60.00 wt. %, from 0.50 to 55.00 wt. %, from 0.50 to 50.00 wt. %, from 0.50 to 45.00 wt. %, from 0.50 to 40.00 wt. %,

[0544] from 1.00 to 99.00 wt. %, from 1.00 to 95.00 wt. %, from 1.00 to 90.00 wt. %, from 1.00 to 85.00 wt. %, from 1.00 to 80.00 wt. %, from 1.00 to 75.00 wt. %, from 1.00 to 70.00 wt. %, from 1.00 to 65.00 wt. %, from 1.00 to 60.00 wt. %, from 1.00 to 55.00 wt. %, from 1.00 to 50.00 wt. %, from 1.00 to 45.00 wt. %, from 1.00 to 40.00 wt. %,

[0545] from 0.50 to 5.00 wt. %, from 0.50 to 4.50 wt. %, from 0.50 to 4.00 wt. %, from 0.50 to 3.50 wt. %, from 0.50 to 3.00 wt. %, from 0.50 to 2.50 wt. %, from 0.50 to 2.00 wt. %, from 0.50 to 1.50 wt. %, from 0.50 to 1.00 wt. % of the weight of the medicinal product.

[0546] In one embodiment of the present invention, the effective dosage of 2-(3-(4-(7H-pyrrolo[2, 3-d]pyrimidine-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetide-3-yl)acetonitrile, characterized by formula B, or a pharmaceutically acceptable salt thereof, is in the range of about 0.05 to 50.00 mg per day per patient in need of such treatment.

[0547] More preferably, the effective dosage of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidine-4-yl)-1H-pyrazol-1-yl)-1-(3-methoxypropanoyl)azetide-3-yl)acetonitrile a, characterized by formula B, or a pharmaceutically acceptable salt thereof, according to the present invention is from 0.05 to 10.00 mg, from 0.05 to 9.00 mg, from 0.05 to 8.00 mg, from 0.05 to 7.00 mg, from 0.05 to 6.00 mg, from 0.05 to 5.00 mg, from 0.05 to 4.00 mg, from 0.05 to 3.50 mg, from 0.05 to 3.00 mg, from 0.05 to 2.50 mg, from 0.05 to 2.00 mg, 0.05 to 1.50 mg, 0.05 to 1.00 mg, 0.05 to 0.50 mg or 0.50 to 5.00 mg, 0.50 to 4.50 mg, 0.50 to 4.00 mg, 0.50 to 3.50 mg, 0.50 to 3.00 mg, 0.50 to 2.50 mg, 0.50 to 2.00 mg or 1.00 to 5.00 mg, 1.00 to 4.50 mg, 1.00 to 4.00 mg, 1.00 to 3.50 mg, 1.00 to 3.00 mg, 1.00 to 2.50 mg, 1.00 to 2.00 mg or 2.00 to 5.00 mg or 1.00 to 4.00 mg per day.

[0548] If necessary, doses are usually divided into several smaller doses to be administered throughout the day.

[0549] The stated problem is solved, and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanoyl)azetide yn-3-yl)acetonitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof.

[0550] The stated problem is solved and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanoyl)azetide yn-3-yl)acetonitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

[0551] The stated problem is solved, and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing in an effective amount 2-(3-(4-(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanoyl)azetidin-3-yl)acetonitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient. One embodiment of the present invention is a medicinal product containing 2-(3-(4-(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanoyl)azetidin-3-yl)acetonitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof in an amount of from 0.50 to 100.00 mg, from 0.50 to 100.00 mg.

[0552] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanone l) azetide yn-3-yl)acetoneitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof according to the present invention in the medicinal product is from 0.50 to 95.00 mg, from 0.50 to 90.00 mg, from 0.50 to 85.00 mg, from 0.50 to 80.00 mg, from 0.50 to 75.00 mg, from 0.50 to 70.00 mg, from 0.50 to 65.00 mg, from 0.50 to 60.00 mg, from 0.50 to 55.00 mg, 0.50 to 50.00 mg, 0.50 to 45.00 mg, 0.50 to 40.00 mg, 0.50 to 35.00 mg, 0.50 to 30.00 mg, 0.50 to 25.00 mg, 0.50 to 20.00 mg, 0.50 to 15.00 mg, 0.50 to 10.00 mg, 0.50 to 9.00 mg, 0.50 to 8.00 mg, 0.50 to 7.00 mg, 0.50 to 6.00 mg, 0.50 to 5.00 mg, 0.50 to 4.00 mg, 0.50 to 3.00 mg, 0.50 to 2.00 mg or from 0.50 to 1.00 mg.

[0553] One embodiment of the present invention is a medicinal product containing a therapeutically effective amount of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanoyl)azetidin-3-yl)acetonitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof in an amount of from 0.50 to 10.00 mg.

[0554] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanone l) azetide in-3-yl)acetoneitrile a, characterized by formula C, or its pharmaceutically acceptable salt according to the present invention in the drug is from 0.50 to 9.50 mg, from 0.50 to 9.00 mg, from 0.50 to 8.50 mg, from 0.50 to 8.00 mg, from 0.50 to 7.50 mg, from 0.50 to 7.00 mg, from 0.50 to 6.50 mg, from 0.50 to 6.00 mg, from 0.50 to 5.50 mg, from 0.50 up to 5.00 mg, from 0.50 to 4.50 mg, from 0.50 to 4.00 mg, from 0.50 to 3.50 mg, from 0.50 to 3.00 mg, from 0.50 to 2.50 mg or from 0.50 to 2.00 mg.

[0555] One embodiment of the present invention is a medicinal product containing a therapeutically effective amount of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanoyl)azetidin-3-yl)acetonitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof in an amount of from 1.00 to 5.00 mg, from 2.00 to 4.00 mg.

[0556] One embodiment of the present invention is a medicinal product containing 2-(3-(4-(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanoyl)azetidin-3-yl)acetonitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 99.00 wt. % of the mass of the medicinal product.

[0557] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanone l) azetide yn-3-yl)acetoneitrile, characterized by formula C, or its pharmaceutically acceptable salt according to the present invention in the drug is from 0.01 to 95.00 wt. %, from 0.01 to 90.00 wt. %, from 0.01 to 85.00 wt. %, from 0.01 to 80.00 wt. %, from 0.01 to 75.00 wt. %, from 0.01 to 70.00 wt. %, from 0.01 to 65.00 wt. %, from 0.01 to 60.00 wt. %, from 0.01 to 55.00 wt. %, from 0.01 to 50.00 wt. %, from 0.01 to 40.00 wt. %,

[0558] from 0.10 to 99.00 wt. %, from 0.10 to 95.00 wt. %, from 0.10 to 90.00 wt. %, from 0.10 to 85.00 wt. %, from 0.10 to 80.00 wt. %, from 0.10 to 75.00 wt. %, from 0.10 to 70.00 wt. %, from 0.10 to 65.00 wt. %, from 0.10 to 60.00 wt. %, from 0.10 to 55.00 wt. %, from 0.10 to 50.00 wt. %, from 0.10 to 45.00 wt. %, from 0.10 to 40.00 wt. %,

[0559] from 0.50 to 99.00 wt. %, from 0.50 to 95.00 wt. %, from 0.50 to 90.00 wt. %, from 0.50 to 85.00 wt. %, from 0.50 to 80.00 wt. %, from 0.50 to 75.00 wt. %, from 0.50 to 70.00 wt. %, from 0.50 to 65.00 wt. %, from 0.50 to 60.00 wt. %, from 0.50 to 55.00 wt. %, from 0.50 to 50.00 wt. %, from 0.50 to 45.00 wt. %, from 0.50 to 40.00 wt. %,

[0560] from 1.00 to 99.00 wt. %, from 1.00 to 95.00 wt. %, from 1.00 to 90.00 wt. %, from 1.00 to 85.00 wt. %, from 1.00 to 80.00 wt. %, from 1.00 to 75.00 wt. %, from 1.00 to 70.00 wt. %, from 1.00 to 65.00 wt. %, from 1.00 to 60.00 wt. %, from 1.00 to 55.00 wt. %, from 1.00 to 50.00 wt. %, from 1.00 to 45.00 wt. %, from 1.00 to 40.00 wt. %,

[0561] from 0.50 to 5.00 wt. %, from 0.50 to 4.50 wt. %, from 0.50 to 4.00 wt. %, from 0.50 to 3.50 wt. %, from 0.50 to 3.00 wt. %, from 0.50 to 2.50 wt. %, from 0.50 to 2.00 wt. %, from 0.50 to 1.50 wt. %, from 0.50 to 1.00 wt. % of the weight of the medicinal product.

[0562] In one embodiment of the present invention, the effective dosage of 2-(3-(4-(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanoyl)azetidin-3-yl)acetonitrile, characterized by formula C, or a pharmaceutically acceptable salt thereof, is in the range of about 0.05 to 50.00 mg per day per patient in need of such treatment.

[0563] More preferably, the effective dosage of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(3-(methylthio)propanoyl)azetidin-3-yl)acetonitrile represented by formula C or a pharmaceutically acceptable salt thereof according to the present invention is from 0.05 to 10.00 mg, from 0.05 to 9.00 mg, from 0.05 to 8.00 mg, from 0.05 to 7.00 mg, from 0.05 to 6.00 mg, from 0.05 to 5.00 mg, from 0.05 to 4.00 mg, from 0.05 to 3.50 mg, from 0.05 to 3.00 mg, from 0.05 to 2.50 mg, from 0.05 to 2.00 mg, 0.05 to 1.50 mg, 0.05 to 1.00 mg, 0.05 to 0.50 mg or 0.50 to 5.00 mg, 0.50 to 4.50 mg, 0.50 to 4.00 mg, 0.50 to 3.50 mg, 0.50 to 3.00 mg, 0.50 to 2.50 mg, 0.50 to 2.00 mg or 1.00 to 5.00 mg, 1.00 to 4.50 mg, 1.00 to 4.00 mg, 1.00 to 3.50 mg, 1.00 to 3.00 mg, 1.00 to 2.50 mg, 1.00 to 2.00 mg or 2.00 to 5.00 mg or 1.00 to 4.00 mg per day.

[0564] If necessary, doses are usually divided into several smaller doses to be administered throughout the day.

[0565] The stated problem is solved and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-y]pyrimidine-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula A”, or a pharmaceutically acceptable salt thereof.

[0566] The stated problem is solved and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-y]pyrimidine-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula A”, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

[0567] The stated problem is solved, and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing in an effective amount 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula A”, or its pharmaceutically acceptable salt and at least one pharmaceutically acceptable excipient.

[0568] One embodiment of the present invention is a medicinal product containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula A”, or a pharmaceutically acceptable salt thereof in an amount of 0.50 to 100.00 mg.

[0569] One embodiment of the present invention is a medicament comprising a therapeutically effective amount of 2-(3-(4-(7H-pyrrolo[2,3-<1]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile characterized by formula A", or a pharmaceutically acceptable salt thereof in an amount of from 0.50 to 100.00 mg. More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile characterized by formula A", or a pharmaceutically acceptable salt thereof according to the present invention in the medicament is from 0.50 to 95.00 mg, from 0.50 to 90.00 mg, from 0.50 to 85.00 mg, from 0.50 to 80.00 mg, from 0.50 to 75.00 mg, from 0.50 to 70.00 mg, from 0.50 to 65.00 mg, from 0.50 to 60.00 mg, from 0.50 to 55.00 mg, from 0.50 to 50.00 mg, from 0.50 to 45.00 mg, from 0.50 to 40.00 mg, from 0.50 to 35.00 mg, from 0.50 to 30.00 mg, from 0.50 to 25.00 mg, from 0.50 to 20.00 mg, from 0.50 to 15.00 mg, 0.50 to 10.00 mg, 0.50 to 9.00 mg, 0.50 to 8.00 mg, 0.50 to 7.00 mg, 0.50 to 6.00 mg, 0.50 to 5.00 mg, 0.50 to 4.00 mg, 0.50 to 3.00 mg, 0.50 to 2.00 mg, or 0.50 to 1.00 mg.

[0570] One embodiment of the present invention is a medicinal product containing a therapeutically effective amount of 2-(3-(4-(7H-pyrrolo[2,3-<1]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula A”, or a pharmaceutically acceptable salt thereof in an amount of 0.50 to 10.00 mg.

[0571] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile represented by formula A”, or a pharmaceutically acceptable salt thereof according to the present invention in the medicinal product is from 0.50 to 9.50 mg, from 0.50 to 9.00 mg, from 0.50 to 8.50 mg, from 0.50 to 8.00 mg, from 0.50 to 7.50 mg, from 0.50 to 7.00 mg, from 0.50 to 6.50 mg, from 0.50 to 6.00 mg, from 0.50 to 5.50 mg, from 0.50 to 5.00 mg, from 0.50 to 4.50 mg, from 0.50 to 4.00 mg, from 0.50 to 3.50 mg, from 0.50 to 3.00 mg, from 0.50 to 2.50 mg or from 0.50 to 2.00 mg.

[0572] One embodiment of the present invention is a medicinal product containing a therapeutically effective amount of 2-(3-(4-(7H-pyrrolo[2,3-<1]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula A”, or a pharmaceutically acceptable salt thereof in an amount of from 1.00 to 5.00 mg or from 2.00 to 4.00 mg.

[0573] One embodiment of the present invention is a medicinal product containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula A”, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 99.00 wt. % of the mass of the medicinal product.

[0574] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile characterized by formula A”, or a pharmaceutically acceptable salt thereof according to the present invention in the drug is from 0.01 to 95.00 wt. %, from 0.01 to 90.00 wt. %, from 0.01 to 85.00 wt. %, from 0.01 to 80.00 wt. %, from 0.01 to 75.00 wt. %, from 0.01 to 70.00 wt. %, from 0.01 to 65.00 wt. %, from 0.01 to 60.00 wt. %, from 0.01 to 55.00 wt. %, from 0.01 to 50.00 wt. %, from 0.01 to 40.00 wt. %,

[0575] from 0.10 to 99.00 wt. %, from 0.10 to 95.00 wt. %, from 0.10 to 90.00 wt. %, from 0.10 to 85.00 wt. %, from 0.10 to 80.00 wt. %, from 0.10 to 75.00 wt. %, from 0.10 to 70.00 wt. %, from 0.10 to 65.00 wt. %, from 0.10 to 60.00 wt. %, from 0.10 to 55.00 wt. %, from 0.10 to 50.00 wt. %, from 0.10 to 45.00 wt. %, from 0.10 to 40.00 wt. %,

[0576] from 0.50 to 99.00 wt. %, from 0.50 to 95.00 wt. %, from 0.50 to 90.00 wt. %, from 0.50 to 85.00 wt. %, from 0.50 to 80.00 wt. %, from 0.50 to 75.00 wt. %, from 0.50 to 70.00 wt. %, from 0.50 to 65.00 wt. %, from 0.50 to 60.00 wt. %, from 0.50 to 55.00 wt. %, from 0.50 to 50.00 wt. %, from 0.50 to 45.00 wt. %, from 0.50 to 40.00 wt. %,

[0577] from 1.00 to 99.00 wt. %, from 1.00 to 95.00 wt. %, from 1.00 to 90.00 wt. %, from 1.00 to 85.00 wt. %, from 1.00 to 80.00 wt. %, from 1.00 to 75.00 wt. %, from 1.00 to 70.00 wt. %, from 1.00 to 65.00 wt. %, from 1.00 to 60.00 wt. %, from 1.00 to 55.00 wt. %, from 1.00 to 50.00 wt. %, from 1.00 to 45.00 wt. %, from 1.00 to 40.00 wt. %,

[0578] from 0.50 to 5.00 wt. %, from 0.50 to 4.50 wt. %, from 0.50 to 4.00 wt. %, from 0.50 to 3.50 wt. %, from 0.50 to 3.00 wt. %, from 0.50 to 2.50 wt. %, from 0.50 to 2.00 wt. %, from 0.50 to 1.50 wt. % or from 0.50 to 1.00 wt. % of the weight of the medicinal product.

[0579] In one embodiment of the present invention, the effective dosage of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula A”, or a pharmaceutically acceptable salt thereof, is in the range of about 0.05 to 50.00 mg per day per patient in need of such treatment.

[0580] More preferably, the effective dosage of 2-(3-(4-(7H-pyrrolo[2,3-<1]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile represented by formula A”, or a pharmaceutically acceptable salt thereof, according to the present invention is from 0.05 to 10.00 mg, from 0.05 to 9.00 mg, from 0.05 to 8.00 mg, from 0.05 to 7.00 mg, from 0.05 to 6.00 mg, from 0.05 to 5.00 mg, from 0.05 to 4.00 mg, from 0.05 to 3.50 mg, from 0.05 to 3.00 mg, from 0.05 to 2.50 mg, from 0.05 to 2.00 mg, 0.05 to 1.50 mg, 0.05 to 1.00 mg, 0.05 to 0.50 mg or 0.50 to 5.00 mg, 0.50 to 4.50 mg, 0.50 to 4.00 mg, 0.50 to 3.50 mg, 0.50 to 3.00 mg, 0.50 to 2.50 mg, 0.50 to 2.00 mg or 1.00 to 5.00 mg, 1.00 to 4.50 mg, 1.00 to 4.00 mg, 1.00 to 3.50 mg, 1.00 to 3.00 mg, 1.00 to 2.50 mg, 1.00 to 2.00 mg or 2.00 to 5.00 mg or 1.00 to 4.00 mg per day. If necessary, doses are usually divided into several smaller doses for administration throughout the day.

[0581] The stated problem is solved and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-y]pyrimidine-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula B”, or a pharmaceutically acceptable salt thereof.

[0582] The stated problem is solved and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-y]pyrimidine-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula B”, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

[0583] The stated problem is solved, and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing in an effective amount 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula B”, or its pharmaceutically acceptable salt and at least one pharmaceutically acceptable excipient.

[0584] One embodiment of the present invention is a medicinal product containing 2-(3-(4-(7H-pyrrolo[2, 3-<1]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula B”, or a pharmaceutically acceptable salt thereof in an amount of 0.50 to 100.00 mg.

[0585] One embodiment of the present invention is a medicinal product containing a therapeutically effective amount of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetide yn-3-yl)acetonitrile, characterized by formula B”, or a pharmaceutically acceptable salt thereof in an amount of from 0.50 to 100.00 mg.

[0586] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3- ]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetide yn-3-yl)acetonitrile, characterized by formula B”, or a pharmaceutically acceptable salt thereof according to the present invention in the drug is from 0.50 to 95.00 mg, from 0.50 to 90.00 mg, from 0.50 to 85.00 mg, from 0.50 to 80.00 mg, from 0.50 to 75.00 mg, from 0.50 to 70.00 mg, from 0.50 to 65.00 mg, from 0.50 to 60.00 mg, from 0.50 to 55.00 mg, from 0.50 to 50.00 mg, 0.50 to 45.00 mg, 0.50 to 40.00 mg, 0.50 to 35.00 mg, 0.50 to 30.00 mg, 0.50 to 25.00 mg, 0.50 to 20.00 mg, 0.50 to 15.00 mg, 0.50 to 10.00 mg, 0.50 to 9.00 mg, 0.50 to 8.00 mg, 0.50 to 7.00 mg, 0.50 to 6.00 mg, 0.50 to 5.00 mg, 0.50 to 4.00 mg, 0.50 to 3.00 mg, 0.50 to 2.00 mg or from 0.50 to 1.00 mg.

[0587] One embodiment of the present invention is a medicinal product containing a therapeutically effective amount of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetide yn-3-yl)acetonitrile, characterized by formula B”, or a pharmaceutically acceptable salt thereof in an amount of 0.50 to 10.00 mg.

[0588] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile represented by formula B”, or a pharmaceutically acceptable salt thereof according to the present invention in the medicinal product is from 0.50 to 9.50 mg, from 0.50 to 9.00 mg, from 0.50 to 8.50 mg, from 0.50 to 8.00 mg, from 0.50 to 7.50 mg, from 0.50 to 7.00 mg, from 0.50 to 6.50 mg, from 0.50 to 6.00 mg, from 0.50 to 5.50 mg, from 0.50 to 5.00 mg, from 0.50 to 4.50 mg, 0.50 to 4.00 mg, 0.50 to 3.50 mg, 0.50 to 3.00 mg, 0.50 to 2.50 mg, or 0.50 to 2.00 mg.

[0589] One embodiment of the present invention is a medicinal product containing a therapeutically effective amount of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetide yn-3-yl)acetonitrile, characterized by formula B”, or a pharmaceutically acceptable salt thereof in an amount of from 1.00 to 5.00 mg or from 2.00 to 4.00 mg.

[0590] One embodiment of the present invention is a medicinal product containing 2-(3-(4-(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula B”, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 99.00 wt. % of the mass of the medicinal product.

[0591] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetide yn-3-yl)acetonitrile, characterized by formula B”, or a pharmaceutically acceptable salt thereof according to the present invention in the drug is from 0.01 to 95.00 wt. %, from 0.01 to 90.00 wt. %, from 0.01 to 85.00 wt. %, from 0.01 to 80.00 wt. %, from 0.01 to 75.00 wt. %, from 0.01 to 70.00 wt. %, from 0.01 to 65.00 wt. %, from 0.01 to 60.00 wt. %, from 0.01 to 55.00 wt. %, 0.01 to 50.00 wt. %, 0.01 to 40.00 wt. %, 0.10 to 99.00 wt. %, 0.10 to 95.00 wt. %, 0.10 to 90.00 wt. %, 0.10 to 85.00 wt. %, 0.10 to 80.00 wt. %, 0.10 to 75.00 wt. %, 0.10 to 70.00 wt. %, 0.10 to 65.00 wt. %, 0.10 to 60.00 wt. %, 0.10 to 55.00 wt. %, 0.10 to 50.00 wt. %, 0.10 to 45.00 wt. %, from 0.10 to 40.00 wt. %,

[0592] from 0.50 to 99.00 wt. %, from 0.50 to 95.00 wt. %, from 0.50 to 90.00 wt. %, from 0.50 to 85.00 wt. %, from 0.50 to 80.00 wt. %, from 0.50 to 75.00 wt. %, from 0.50 to 70.00 wt. %, from 0.50 to 65.00 wt. %, from 0.50 to 60.00 wt. %, from 0.50 to 55.00 wt. %, from 0.50 to 50.00 wt. %, from 0.50 to 45.00 wt. %, from 0.50 to 40.00 wt. %

[0593] from 1.00 to 99.00 wt. %, from 1.00 to 95.00 wt. %, from 1.00 to 90.00 wt. %, from 1.00 to 85.00 wt. %, from 1.00 to 80.00 wt. %, from 1.00 to 75.00 wt. %, from 1.00 to 70.00 wt. %, from 1.00 to 65.00 wt. %, from 1.00 to 60.00 wt. %, from 1.00 to 55.00 wt. %, from 1.00 to 50.00 wt. %, from 1.00 to 45.00 wt. %, from 1.00 to 40.00 wt. %,

[0594] from 0.50 to 5.00 wt. %, from 0.50 to 4.50 wt. %, from 0.50 to 4.00 wt. %, from 0.50 to 3.50 wt. %, from 0.50 to 3.00 wt. %, from 0.50 to 2.50 wt. %, from 0.50 to 2.00 wt. %, from 0.50 to 1.50 wt. % or from 0.50 to 1.00 wt. % of the weight of the medicinal product.

[0595] In one embodiment of the present invention, the effective dosage of 2-(3-(4-(7H-pyrrolo[2,3-<1]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula B", or a pharmaceutically acceptable salt thereof, is in the range of about 0.05 to 50.00 mg per day per patient in need of such treatment.

[0596] More preferably, the effective dosage of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetide yn-3-yl)acetonitrile characterized by formula B”, or a pharmaceutically acceptable salt thereof, according to the present invention is from 0.05 to 10.00 mg, from 0.05 to 9.00 mg, from 0.05 to 8.00 mg, from 0.05 to 7.00 mg, from 0.05 to 6.00 mg, from 0.05 to 5.00 mg, from 0.05 to 4.00 mg, from 0.05 to 3.50 mg, from 0.05 to 3.00 mg, from 0.05 to 2.50 mg, from 0.05 to 2.00 mg, 0.05 to 1.50 mg, 0.05 to 1.00 mg, 0.05 to 0.50 mg or 0.50 to 5.00 mg, 0.50 to 4.50 mg, 0.50 to 4.00 mg, 0.50 to 3.50 mg, 0.50 to 3.00 mg, 0.50 to 2.50 mg, 0.50 to 2.00 mg or 1.00 to 5.00 mg, 1.00 to 4.50 mg, 1.00 to 4.00 mg, 1.00 to 3.50 mg, 1.00 to 3.00 mg, 1.00 to 2.50 mg, 1.00 to 2.00 mg or 2.00 to 5.00 mg or 1.00 to 4.00 mg per day.

[0597] If necessary, doses are usually divided into several smaller doses to be administered throughout the day.

[0598] The stated problem is solved and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-c!]pyrimidine-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula C”, or a pharmaceutically acceptable salt thereof.

[0599] The stated problem is solved and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing 2-(3-(4-(7H-pyrrolo[2,3-y]pyrimidine-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula C”, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

[0600] The stated problem is solved, and the claimed technical result is also achieved by means of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases, containing in an effective amount 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula C”, or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient.

[0601] One embodiment of the present invention is a medicinal product containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula C”, or a pharmaceutically acceptable salt thereof in an amount of from 0.50 to 100.00 mg.

[0602] One embodiment of the present invention is a medicinal product containing a therapeutically effective amount of 2-(3-(4-(7H-pyrrolo[2,3-<1]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula C”, or a pharmaceutically acceptable salt thereof in an amount of from 0.50 to 100.00 mg.

[0603] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile represented by formula C”, or a pharmaceutically acceptable salt thereof according to the present invention in the drug is from 0.50 to 95.00 mg, from 0.50 to 90.00 mg, from 0.50 to 85.00 mg, from 0.50 to 80.00 mg, from 0.50 to 75.00 mg, from 0.50 to 70.00 mg, from 0.50 to 65.00 mg, from 0.50 to 60.00 mg, from 0.50 to 55.00 mg, from 0.50 to 50.00 mg, 0.50 to 45.00 mg, 0.50 to 40.00 mg, 0.50 to 35.00 mg, 0.50 to 30.00 mg, 0.50 to 25.00 mg, 0.50 to 20.00 mg, 0.50 to 15.00 mg, 0.50 to 10.00 mg, 0.50 to 9.00 mg, 0.50 to 8.00 mg, 0.50 to 7.00 mg, 0.50 to 6.00 mg, 0.50 to 5.00 mg, 0.50 to 4.00 mg, 0.50 to 3.00 mg, 0.50 to 2.00 mg or from 0.50 to 1.00 mg.

[0604] One embodiment of the present invention is a medicinal product containing a therapeutically effective amount of 2-(3-(4-(7H-pyrrolo[2,3-<1]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula C”, or a pharmaceutically acceptable salt thereof in an amount of from 0.50 to 10.00 mg.

[0605] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile represented by formula C”, or a pharmaceutically acceptable salt thereof according to the present invention in the drug is from 0.50 to 9.50 mg, from 0.50 to 9.00 mg, from 0.50 to 8.50 mg, from 0.50 to 8.00 mg, from 0.50 to 7.50 mg, from 0.50 to 7.00 mg, from 0.50 to 6.50 mg, from 0.50 to 6.00 mg, from 0.50 to 5.50 mg, from 0.50 to 5.00 mg, 0.50 to 4.50 mg, 0.50 to 4.00 mg, 0.50 to 3.50 mg, 0.50 to 3.00 mg, 0.50 to 2.50 mg, or 0.50 to 2.00 mg.

[0606] One embodiment of the present invention is a medicinal product containing a therapeutically effective amount of 2-(3-(4-(7H-pyrrolo[2,3-<1]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula C”, or a pharmaceutically acceptable salt thereof in an amount of from 1.00 to 5.00 mg or from 2.00 to 4.00 mg.

[0607] One embodiment of the present invention is a medicinal product containing 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula C”, or a pharmaceutically acceptable salt thereof in an amount of from 0.01 to 99.00 wt. % of the mass of the medicinal product.

[0608] More preferably, the content of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile represented by formula C”, or a pharmaceutically acceptable salt thereof according to the present invention in the drug is from 0.01 to 95.00 wt. %, from 0.01 to 90.00 wt. %, from 0.01 to 85.00 wt. %, from 0.01 to 80.00 wt. %, from 0.01 to 75.00 wt. %, from 0.01 to 70.00 wt. %, from 0.01 to 65.00 wt. %, from 0.01 to 60.00 wt. %, from 0.01 to 55.00 wt. %, from 0.01 to 50.00 wt. %, from 0.01 to 40.00 wt. %,

[0609] from 0.10 to 99.00 wt. %, from 0.10 to 95.00 wt. %, from 0.10 to 90.00 wt. %, from 0.10 to 85.00 wt. %, from 0.10 to 80.00 wt. %, from 0.10 to 75.00 wt. %, from 0.10 to 70.00 wt. %, from 0.10 to 65.00 wt. %, from 0.10 to 60.00 wt. %, from 0.10 to 55.00 wt. %, from 0.10 to 50.00 wt. %, from 0.10 to 45.00 wt. %, from 0.10 to 40.00 wt. %, from 0.50 to 99.00 wt. %, from 0.50 to 95.00 wt. %, from 0.50 to 90.00 wt. %, from 0.50 to 85.00 wt. %, from 0.50 to 80.00 wt. %, from 0.50 to 75.00 wt. %, from 0.50 to 70.00 wt. %, from 0.50 to 65.00 wt. %, from 0.50 to 60.00 wt. %, from 0.50 to 55.00 wt. %, from 0.50 to 50.00 wt. %, from 0.50 to 45.00 wt. %, from 0.50 to 40.00 wt. %,

[0610] from 1.00 to 99.00 wt. %, from 1.00 to 95.00 wt. %, from 1.00 to 90.00 wt. %, from 1.00 to 85.00 wt. %, from 1.00 to 80.00 wt. %, from 1.00 to 75.00 wt. %, from 1.00 to 70.00 wt. %, from 1.00 to 65.00 wt. %, from 1.00 to 60.00 wt. %, from 1.00 to 55.00 wt. %, from 1.00 to 50.00 wt. %, from 1.00 to 45.00 wt. %, from 1.00 to 40.00 wt. %,

[0611] from 0.50 to 5.00 wt. %, from 0.50 to 4.50 wt. %, from 0.50 to 4.00 wt. %, from 0.50 to 3.50 wt. %, from 0.50 to 3.00 wt. %, from 0.50 to 2.50 wt. %, from 0.50 to 2.00 wt. %, from 0.50 to 1.50 wt. % or from 0.50 to 1.00 wt. % of the weight of the medicinal product.

[0612] In one embodiment of the present invention, the effective dosage of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile, characterized by formula C", or a pharmaceutically acceptable salt thereof, is in the range of about 0.05 to 50.00 mg per day per patient in need of such treatment.

[0613] More preferably, the effective dosage of 2-(3-(4-(7H-pyrrolo[2,3-<1]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile represented by formula C”, or a pharmaceutically acceptable salt thereof, according to the present invention is from 0.05 to 10.00 mg, from 0.05 to 9.00 mg, from 0.05 to 8.00 mg, from 0.05 to 7.00 mg, from 0.05 to 6.00 mg, from 0.05 to 5.00 mg, from 0.05 to 4.00 mg, from 0.05 to 3.50 mg, from 0.05 to 3.00 mg, from 0.05 to 2.50 mg, 0.05 to 2.00 mg, 0.05 to 1.50 mg, 0.05 to 1.00 mg, 0.05 to 0.50 mg or 0.50 to 5.00 mg, 0.50 to 4.50 mg, 0.50 to 4.00 mg, 0.50 to 3.50 mg, 0.50 to 3.00 mg, 0.50 to 2.50 mg, 0.50 to 2.00 mg or 1.00 to 5.00 mg, 1.00 to 4.50 mg, 1.00 to 4.00 mg, 1.00 to 3.50 mg, 1.00 to 3.00 mg, 1.00 to 2.50 mg, 1.00 to 2.00 mg or 2.00 to 5.00 mg or 1.00 to 4.00 mg per day.

[0614] If necessary, doses are usually divided into several smaller doses to be administered throughout the day.

[0615] One embodiment of the present invention is a medicinal product characterized in that at least one pharmaceutically acceptable excipient is selected from the group consisting of excipients, stabilizers, solubilizers, solvents, humectants, lubricants, glidants, thickeners, sweeteners, flavorings, aromatizers, fungicides, prolonged delivery regulators, co-solvents, diluents, fillers, emulsifiers, preservatives, antioxidants, buffering agents, cryoprotectants, pH-regulating agents, substances for maintaining isotonicity or correcting substances.

[0616] One embodiment of the present invention is a medicinal product exhibiting Janus kinase (JAK) inhibitor properties for the treatment of autoimmune diseases, characterized in that the autoimmune disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, juvenile arthritis, atopic dermatitis, lupus and alopecia.

[0617] More preferably, the disease of the present invention is selected from the group of JAK-mediated diseases or disorders.

[0618] In some embodiments, one or more compounds of the present invention may be used in combination with other active agents.

[0619] One embodiment of the present invention is a medicinal product containing a compound characterized by formula (I)', formula IV, formula IV”, formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient in an amount of from 1.00 to 99.99 mass % of the mass of the medicinal product.

[0620] More preferably, the content of at least one pharmaceutically acceptable excipient in the drug of the present invention is from 1.00 to 95.00 wt. %, from 1.00 to 90.00 wt. %, from 1.00 to 85.00 wt. %, from 1.00 to 80.00 wt. %, from 1.00 to 75.00 wt. %, from 1.00 to 70.00 wt. %, from 1.00 to 65.00 wt. %, from 1.00 to 60.00 wt. %, from 1.00 to 55.00 wt. %, from 1.00 to 50.00 wt. %, from 1.00 to 45.00 wt. % or from 1.00 to 40.00 wt. % of the drug weight.

[0621] More preferably, the content of at least one pharmaceutically acceptable excipient in the medicament of the present invention is from 1.00 to 99.90 wt. %, from 10.00 to 99.90 wt. %, from 20.00 to 99.90 wt. %, from 30.00 to 99.90 wt. %, from 40.00 to 99.90 wt. %, from 50.00 to 99.90 wt. %, from 60.00 to 99.90 wt. %, from 70.00 to 99.90 wt. %, from 80.00 to 99.90 wt. %, from 90.00 to 99.90 wt. %, from 95.00 to 99.90 wt. % or from 97.00 to 99.90 wt. % of the mass of the drug.

[0622] More preferably, the content of at least one pharmaceutically acceptable excipient in the medicament of the present invention is from 10.00 to 99.50 wt. %, from 10.00 to 99.40 wt. %, from 10.00 to 99.30 wt. %, from 10.00 to 99.20 wt. %, from 10.00 to 99.10 wt. %, from 10.00 to 99.00 wt. %, from 10.00 to 98.90 wt. %, from 10.00 to 98.80 wt. %, from 10.00 to 98.70 wt. %, from 10.00 to 98.60 wt. %, from 10.00 to 98.50 wt. %, from 10.00 to 98.40 wt. %, from 10.00 to 98.30 mass. %, from 10.00 to 98.20 mass. %, from 10.00 to 98.10 mass. %, from 10.00 to 98.00 mass. % of the mass of the medicinal product.

[0623] More preferably, the content of at least one pharmaceutically acceptable excipient in the medicament of the present invention is from 90.00 to 99.90 wt. %, from 90.00 to 99.80 wt. %, from 90.00 to 99.70 wt. %, from 90.00 to 99.60 wt. %, from 90.00 to 99.50 wt. %, from 90.00 to 99.40 wt. %, from 90.00 to 99.30 wt. %, from 90.00 to 99.20 wt. %, from 90.00 to 99.10 wt. %, from 90.00 to 99.00 wt. %, from 90.00 to 98.90 wt. %, from 90.00 to 98.80 wt. %, from 90.00 to 98.70 wt. %, from 90.00 to 98.60 wt. %, from 90.00 to 98.50 wt. %, from 90.00 to 98.40 wt. %, from 90.00 to 98.30 wt. %, from 90.00 to 98.20 wt. %, from 90.00 to 98.10 wt. %, from 90.00 to 98.00 wt. %, from 95.00 to 99.90 wt. %, from 96.00 to 99.90 wt. %, from 97.00 to 99.90 wt. % or from 98.00 to 99.90 wt. % of the weight of the medicinal product.One embodiment of the present invention is a medicinal product containing a compound characterized by formula (I)', formula IV, formula IV”, compound A or compound B, or compound C, compound A” or compound B”, or compound C”, or a pharmaceutically acceptable salt thereof, which is a solid medicinal product.

[0624] More preferably, the solid dosage form of the present invention is, but is not limited to, a tablet, capsule, pellet, dragee, granule, sachet, powder, lyophilisate.

[0625] More preferably, the solid preparation of the present invention is, but is not limited to, a dispersible tablet including an orodispersible tablet, a lyophilized tablet, a film-coated tablet, a buccal tablet, an effervescent tablet, a delayed / extended / modified release tablet.

[0626] One embodiment of the invention is a medicinal product that is a liquid medicinal product.

[0627] More preferably, the liquid medicinal product of the present invention is, but is not limited to, a solution, a concentrate for the preparation of a solution, a syrup, or a suspension. One embodiment of the invention is a medicinal product that is a parenteral medicinal product.

[0628] Parenteral administration of drugs refers to routes of administration that bypass the gastrointestinal tract, as opposed to oral administration. Parenteral drugs are sterile preparations intended for administration by injection, infusion, inhalation, or implantation into the human or animal body. These include solutions, emulsions, suspensions, aerosols, powders, and tablets for solution and implantation, powders for inhalation, and lyophilized preparations for parenteral dosage forms (subcutaneously, intramuscularly, intravenously, intraarterially, or into various cavities).

[0629] Parenteral routes of administration include administration into tissues (intradermally, subcutaneously, intramuscularly, intraosseously), into vessels (intravenously, intraarterially, into lymphatic vessels), into cavities (into the pleural, abdominal, cardiac and joint cavities), into the subarachnoid space, as well as inhalation, intranasal and subconjunctival administration.

[0630] More preferably, the parenteral drug of the present invention is an infusion solution.

[0631] More preferably, the parenteral drug of the present invention is an injection solution.

[0632] The stated problem is solved and the claimed technical result is achieved by using a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the production of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases.

[0633] The stated task is solved and the stated technical result is achieved in

[0634] by using a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the preparation of a medicament for the treatment of autoimmune diseases by inhibiting Janus kinase.

[0635] The stated task is solved and the stated technical result is achieved in

[0636] by using a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the preparation of a medicament for the treatment of diseases by inhibiting Janus kinase.

[0637] The stated task is solved and the stated technical result is achieved in

[0638] by using a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the production of a medicament for the treatment of diseases.

[0639] The stated task is solved and the stated technical result is achieved in

[0640] by using a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the production of a medicament for the treatment of autoimmune diseases.

[0641] The stated task is solved and the stated technical result is achieved in

[0642] by using a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the preparation of a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases.

[0643] The stated task is solved and the stated technical result is achieved in

[0644] by using a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the preparation of a pharmaceutical composition for the treatment of autoimmune diseases by inhibiting Janus kinase.

[0645] The stated task is solved and the stated technical result is achieved in

[0646] by using a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the preparation of a pharmaceutical composition for the treatment of diseases by inhibiting Janus kinase.

[0647] The stated task is solved and the stated technical result is achieved in

[0648] by using a compound characterized by formula (I), formula IV, or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the production of a pharmaceutical composition for the treatment of diseases. The stated problem is solved, and the claimed technical result is achieved

[0649] by using a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the preparation of a pharmaceutical composition for the treatment of autoimmune diseases.

[0650] The stated task is solved and the stated technical result is achieved in

[0651] by using a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the treatment of autoimmune diseases by inhibiting Janus kinase.

[0652] The stated task is solved and the stated technical result is achieved in

[0653] by using a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the treatment of diseases by inhibiting Janus kinase.

[0654] The stated task is solved and the stated technical result is achieved in

[0655] by using a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the treatment of diseases.

[0656] The stated task is solved and the stated technical result is achieved in

[0657] by using a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the treatment of autoimmune diseases.

[0658] The stated task is solved and the stated technical result is achieved in

[0659] by using a pharmaceutical composition containing a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, exhibiting properties of a Janus kinase (JAK) inhibitor, for the treatment of autoimmune diseases.

[0660] The stated task is solved and the stated technical result is achieved in

[0661] by using a pharmaceutical composition containing a compound characterized by formula (I), formula IV, or formula IV”, or a pharmaceutically acceptable salt thereof, for the treatment of autoimmune diseases by inhibiting Janus kinase.

[0662] The stated task is solved and the stated technical result is achieved in

[0663] by using a pharmaceutical composition containing a compound characterized by formula (I), formula IV, or formula IV”, or a pharmaceutically acceptable salt thereof, for the treatment of diseases by inhibiting Janus kinase.

[0664] The stated task is solved and the stated technical result is achieved in

[0665] by using a pharmaceutical composition containing a compound characterized by formula (I), formula IV, or formula IV”, or a pharmaceutically acceptable salt thereof, for the treatment of diseases.

[0666] The stated task is solved and the stated technical result is achieved in

[0667] by using a pharmaceutical composition containing a compound characterized by formula (I), formula IV, or formula IV”, or a pharmaceutically acceptable salt thereof, for the treatment of autoimmune diseases.

[0668] The stated task is solved and the stated technical result is achieved in

[0669] by using a medicinal product containing a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, exhibiting properties of a Janus kinase (JAK) inhibitor, for the treatment of autoimmune diseases.

[0670] The stated task is solved and the stated technical result is achieved in

[0671] by using a medicinal product containing a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, for the treatment of autoimmune diseases by inhibiting Janus kinase.

[0672] The stated task is solved and the stated technical result is achieved in

[0673] by using a medicinal product containing a compound characterized by formula (I), formula IV, or formula IV”, or a pharmaceutically acceptable salt thereof, for the treatment of diseases by inhibiting Janus kinase. The stated problem is solved, and the claimed technical result is achieved

[0674] by using a medicinal product containing a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, for the treatment of diseases.

[0675] The stated task is solved and the stated technical result is achieved in

[0676] by using a medicinal product containing a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, for the treatment of autoimmune diseases.

[0677] The stated task is solved and the stated technical result is achieved in

[0678] by using a pharmaceutical composition containing a compound characterized by formula (I), formula IV, or formula IV”, or a pharmaceutically acceptable salt thereof, to obtain a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases.

[0679] The stated task is solved and the stated technical result is achieved in

[0680] by using a pharmaceutical composition containing a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment of autoimmune diseases by inhibiting Janus kinase.

[0681] The stated task is solved and the stated technical result is achieved in

[0682] by using a pharmaceutical composition containing a compound characterized by formula (I), formula IV, or formula IV”, or a pharmaceutically acceptable salt thereof, to obtain a medicament for the treatment of diseases by inhibiting Janus kinase.

[0683] The stated task is solved and the stated technical result is achieved in

[0684] by using a pharmaceutical composition containing a compound characterized by formula (I), formula IV, or formula IV”, or a pharmaceutically acceptable salt thereof, to obtain a medicinal product for the treatment of diseases. The stated problem is solved, and the claimed technical result is achieved

[0685] by using a pharmaceutical composition containing a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, for the production of a medicinal product for the treatment of autoimmune diseases.

[0686] The stated problem is solved and the claimed technical result is achieved by using a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the production of a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of viral diseases.

[0687] The stated task is solved and the stated technical result is achieved in

[0688] by using a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the production of a medicament for the treatment of viral diseases.

[0689] The stated task is solved and the stated technical result is achieved in

[0690] by using a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the production of a medicament for the treatment of viral diseases by inhibiting Janus kinase.

[0691] The stated task is solved and the stated technical result is achieved in

[0692] by using a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the preparation of a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of viral diseases.

[0693] The stated task is solved and the stated technical result is achieved in

[0694] by using a compound characterized by formula (I), formula IV, or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the preparation of a pharmaceutical composition for the treatment of viral diseases by inhibiting Janus kinase. The stated problem is solved, and the claimed technical result is achieved

[0695] by using a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the preparation of a pharmaceutical composition for the treatment of viral diseases.

[0696] The stated task is solved and the stated technical result is achieved in

[0697] by using a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the treatment of viral diseases by inhibiting Janus kinase.

[0698] The stated task is solved and the stated technical result is achieved in

[0699] by using a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the treatment of viral diseases by inhibiting Janus kinase.

[0700] The stated task is solved and the stated technical result is achieved in

[0701] by using a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof according to the present invention for the treatment of viral diseases.

[0702] The stated task is solved and the stated technical result is achieved in

[0703] by using a pharmaceutical composition containing a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, exhibiting properties of a Janus kinase (JAK) inhibitor, for the treatment of viral diseases.

[0704] The stated task is solved and the stated technical result is achieved in

[0705] by using a pharmaceutical composition containing a compound characterized by formula (I), formula IV, or formula IV”, or a pharmaceutically acceptable salt thereof, for the treatment of viral diseases by inhibiting Janus kinase.

[0706] The stated problem is solved and the claimed technical result is achieved through the use of a pharmaceutical composition containing a compound characterized by formula (I), formula IV or formula IV”, or its pharmaceutically acceptable salt, for the treatment of viral diseases by inhibiting Janus kinase.

[0707] The stated task is solved and the stated technical result is achieved in

[0708] by using a pharmaceutical composition containing a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, for the treatment of viral diseases.

[0709] The stated task is solved and the stated technical result is achieved in

[0710] by using a medicinal product containing a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, exhibiting the properties of a Janus kinase (JAK) inhibitor, for the treatment of viral diseases.

[0711] The stated task is solved and the stated technical result is achieved in

[0712] by using a medicinal product containing a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, for the treatment of viral diseases by inhibiting Janus kinase.

[0713] The stated task is solved and the stated technical result is achieved in

[0714] by using a medicinal product containing a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, for the treatment of viral infections by inhibiting Janus kinase.

[0715] The stated task is solved and the stated technical result is achieved in

[0716] by using a medicinal product containing a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, for the treatment of viral diseases.

[0717] The stated task is solved and the stated technical result is achieved in

[0718] by using a pharmaceutical composition containing a compound characterized by formula (I), formula IV, or formula IV”, or a pharmaceutically acceptable salt thereof, to obtain a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of viral diseases.

[0719] The stated task is solved and the stated technical result is achieved in

[0720] by using a pharmaceutical composition containing a compound characterized by formula (I), formula IV, or formula IV”, or a pharmaceutically acceptable salt thereof, to obtain a medicament for the treatment of viral diseases by inhibiting Janus kinase.

[0721] The stated task is solved and the stated technical result is achieved in

[0722] by using a pharmaceutical composition containing a compound characterized by formula (I), formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, to obtain a medicinal product for the treatment of viral diseases.

[0723] The stated task is solved and the stated technical result is achieved in

[0724] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the production of a medicament exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases.

[0725] The stated task is solved and the stated technical result is achieved in

[0726] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the production of a medicament for the treatment of autoimmune diseases by inhibiting Janus kinase.

[0727] The stated task is solved and the stated technical result is achieved in

[0728] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the production of a medicament for the treatment of diseases by inhibiting Janus kinase.

[0729] The stated problem is solved and the claimed technical result is achieved through the use of a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or its pharmaceutically acceptable salt according to the present invention for the production of a medicinal product for the treatment of diseases.

[0730] The stated task is solved and the stated technical result is achieved in

[0731] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the production of a medicament for the treatment of autoimmune diseases.

[0732] The stated task is solved and the stated technical result is achieved in

[0733] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the preparation of a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases.

[0734] The stated task is solved and the stated technical result is achieved in

[0735] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the preparation of a pharmaceutical composition for the treatment of autoimmune diseases by inhibiting Janus kinase.

[0736] The stated task is solved and the stated technical result is achieved in

[0737] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the preparation of a pharmaceutical composition for the treatment of diseases by inhibiting Janus kinase.

[0738] The stated task is solved and the stated technical result is achieved in

[0739] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the preparation of a pharmaceutical composition for the treatment of diseases.

[0740] 111 The stated problem is solved, and the stated technical result is achieved in

[0741] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the preparation of a pharmaceutical composition for the treatment of autoimmune diseases.

[0742] The stated task is solved and the stated technical result is achieved in

[0743] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the treatment of autoimmune diseases by inhibiting Janus kinase.

[0744] The stated task is solved and the stated technical result is achieved in

[0745] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the treatment of diseases by inhibiting Janus kinase.

[0746] The stated task is solved and the stated technical result is achieved in

[0747] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the treatment of diseases.

[0748] The stated task is solved and the stated technical result is achieved in

[0749] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the treatment of autoimmune diseases.

[0750] The stated task is solved and the stated technical result is achieved in

[0751] by using a pharmaceutical composition containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, exhibiting the properties of a Janus kinase (JAK) inhibitor, for the treatment of autoimmune diseases. The stated problem is solved, and the claimed technical result is achieved

[0752] by using a pharmaceutical composition containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, for the treatment of autoimmune diseases by inhibiting Janus kinase.

[0753] The stated task is solved and the stated technical result is achieved in

[0754] by using a pharmaceutical composition containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, for the treatment of diseases by inhibiting Janus kinase.

[0755] The stated task is solved and the stated technical result is achieved in

[0756] by using a pharmaceutical composition containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, for the treatment of diseases.

[0757] The stated task is solved and the stated technical result is achieved in

[0758] by using a pharmaceutical composition containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, for the treatment of autoimmune diseases.

[0759] The stated task is solved and the stated technical result is achieved in

[0760] by using a medicinal product containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, exhibiting properties of a Janus kinase (JAK) inhibitor, for the treatment of autoimmune diseases.

[0761] The stated task is solved and the stated technical result is achieved in

[0762] by using a medicinal product containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, for the treatment of autoimmune diseases by inhibiting Janus kinase.

[0763] 113 The stated problem is solved, and the stated technical result is achieved in

[0764] by using a medicinal product containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, for the treatment of diseases by inhibiting Janus kinase.

[0765] The stated task is solved and the stated technical result is achieved in

[0766] by using a medicinal product containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, for the treatment of diseases.

[0767] The stated task is solved and the stated technical result is achieved in

[0768] by using a medicinal product containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, for the treatment of autoimmune diseases.

[0769] The stated task is solved and the stated technical result is achieved in

[0770] by using a pharmaceutical composition containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, to obtain a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases.

[0771] The stated task is solved and the stated technical result is achieved in

[0772] by using a pharmaceutical composition containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, to obtain a medicament for the treatment of autoimmune diseases by inhibiting Janus kinase.

[0773] The stated task is solved and the stated technical result is achieved in

[0774] by using a pharmaceutical composition containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, to obtain a medicament for the treatment of diseases by inhibiting Janus kinase.

[0775] The stated task is solved and the stated technical result is achieved in

[0776] by using a pharmaceutical composition containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, to obtain a medicinal product for the treatment of diseases.

[0777] The stated task is solved and the stated technical result is achieved in

[0778] by using a pharmaceutical composition containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, for the production of a medicinal product for the treatment of autoimmune diseases.

[0779] The stated task is solved and the stated technical result is achieved in

[0780] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the production of a medicament exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of viral diseases.

[0781] The stated task is solved and the stated technical result is achieved in

[0782] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the production of a medicament for the treatment of viral diseases by inhibiting Janus kinase.

[0783] The stated task is solved and the stated technical result is achieved in

[0784] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the production of a medicament for the treatment of viral diseases by inhibiting Janus kinase.

[0785] The stated problem is solved and the claimed technical result is achieved through the use of a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or its pharmaceutically acceptable salt according to the present invention for the production of a medicinal product for the treatment of viral diseases.

[0786] The stated task is solved and the stated technical result is achieved in

[0787] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the preparation of a pharmaceutical composition exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of viral diseases.

[0788] The stated task is solved and the stated technical result is achieved in

[0789] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the preparation of a pharmaceutical composition for the treatment of viral diseases by inhibiting Janus kinase.

[0790] The stated task is solved and the stated technical result is achieved in

[0791] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the preparation of a pharmaceutical composition for the treatment of viral diseases by inhibiting Janus kinase.

[0792] The stated task is solved and the stated technical result is achieved in

[0793] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the preparation of a pharmaceutical composition for the treatment of viral diseases.

[0794] The stated task is solved and the stated technical result is achieved in

[0795] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the treatment of viral diseases by inhibiting Janus kinase. The stated problem is solved, and the claimed technical result is achieved

[0796] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the treatment of viral diseases by inhibiting Janus kinase.

[0797] The stated task is solved and the stated technical result is achieved in

[0798] by using a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof according to the present invention for the treatment of viral diseases.

[0799] The stated task is solved and the stated technical result is achieved in

[0800] by using a pharmaceutical composition containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, exhibiting properties of a Janus kinase (JAK) inhibitor, for the treatment of viral diseases.

[0801] The stated task is solved and the stated technical result is achieved in

[0802] by using a pharmaceutical composition containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, for the treatment of viral diseases by inhibiting Janus kinase.

[0803] The stated task is solved and the stated technical result is achieved in

[0804] by using a pharmaceutical composition containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, for the treatment of viral diseases by inhibiting Janus kinase.

[0805] The stated task is solved and the stated technical result is achieved in

[0806] by using a pharmaceutical composition containing a compound characterized by formula A, formula B, formula C, formula A, formula B, or formula C, or a pharmaceutically acceptable salt thereof, for the treatment of viral diseases. The stated problem is solved, and the claimed technical result is achieved

[0807] by using a medicinal product containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, exhibiting the properties of a Janus kinase (JAK) inhibitor, for the treatment of viral diseases.

[0808] The stated task is solved and the stated technical result is achieved in

[0809] by using a medicinal product containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, for the treatment of viral diseases by inhibiting Janus kinase.

[0810] The stated task is solved and the stated technical result is achieved in

[0811] by using a medicinal product containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, for the treatment of viral diseases by inhibiting Janus kinase.

[0812] The stated task is solved and the stated technical result is achieved in

[0813] due to the use of a medicinal product containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, for the treatment of viral diseases.

[0814] The stated task is solved and the stated technical result is achieved in

[0815] by using a pharmaceutical composition containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, to obtain a medicinal product exhibiting the properties of a Janus kinase (JAK) inhibitor for the treatment of viral diseases.

[0816] The stated task is solved and the stated technical result is achieved in

[0817] by using a pharmaceutical composition containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, to obtain a medicinal product for the treatment of viral diseases by inhibiting Janus kinase.

[0818] The stated task is solved and the stated technical result is achieved in

[0819] by using a pharmaceutical composition containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, to obtain a medicinal product for the treatment of viral diseases by inhibiting Janus kinase.

[0820] The stated task is solved and the stated technical result is achieved in

[0821] by using a pharmaceutical composition containing a compound characterized by formula A, formula B, formula C, formula A”, formula B” or formula C”, or a pharmaceutically acceptable salt thereof, to obtain a medicinal product for the treatment of viral diseases.

[0822] More preferably, the autoimmune disease of the present invention is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, juvenile arthritis, atopic dermatitis, lupus and alopecia.

[0823] More preferably, the disease of the present invention is selected from the group of JAK-mediated diseases or disorders.

[0824] More preferably, the disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, juvenile arthritis, chronic polyarthritis, atopic dermatitis, juvenile idiopathic arthritis,

[0825] alopecia (focal alopecia, frontal fibrosing alopecia, alopecia areata, including severe or very severe forms), multiple sclerosis, multiple sclerosis, amyotrophic lateral sclerosis, neurodegenerative Alzheimer's disease,

[0826] Type 1 diabetes, diabetic kidney disease, aggressive albuminuria reduction in biopsy-proven diabetic nephropathy, lupus, systemic lupus erythematosus, lupus nephritis, psoriasis,

[0827] Inflammatory bowel disease, ulcerative colitis, Crohn's disease, severe pseudoparalytic myasthenia, immunoglobulin nephropathy, autoimmune thyroid disease, pemphigus vulgaris, bullous pemphigoid, allergic reactions such as asthma, food allergies, atopic dermatitis and rhinitis, viral diseases such as Epstein-Barr virus, hepatitis B, hepatitis C, human immunodeficiency virus, varicella-zoster virus and human papillomavirus, coronavirus, COVID-19,

[0828] Skin rashes, skin irritations, skin sensitization (e.g. contact dermatitis or allergic contact dermatitis), cutaneous lichen planus, cancer, including cancer characterized by the formation of solid tumors (e.g. prostate cancer, kidney cancer, liver cancer, pancreatic cancer, stomach cancer, breast cancer, lung cancer, head and neck cancer, thyroid cancer, glioblastoma, Kaposi's sarcoma, Castleman's disease, melanoma, etc.), blood cancer (e.g., lymphoma, leukemia such as acute lymphoblastic leukemia, acute myelogenous leukemia (AML), or multiple myeloma) and skin cancer such as cutaneous T-cell lymphoma (CTCL) and cutaneous B-cell lymphoma, typical cutaneous T-cell lymphomas include Sézary syndrome and mycosis fungoides, myeloproliferative disorders (MPDs) such as polycythemia vera (PV), essential thrombocythemia (ET), myelofibrosis with myeloid metaplasia (MFM), chronic myeloid leukemia (CML), chronic myelomonocytic leukemia (CMML), hypereosinophilic syndrome (HES), systemic mastocytosis (SM) associated with colitis, colon cancer, colorectal cancer colon, gastric cancer, gastrointestinal carcinoid tumor, gastrointestinal stromal tumor (GIST), adenocarcinoma, small intestine cancer, rectal cancer, etc.

[0829] Inflammatory diseases include inflammatory diseases of the eye (e.g., iritis, uveitis, scleritis, conjunctivitis, or related diseases), refractory non-infectious non-anterior uveitis, inflammatory diseases of the airways (e.g., upper respiratory tract, including diseases of the nose and sinuses, such as rhinitis or sinusitis, lower respiratory tract, including bronchitis, chronic non-specific lung disease, etc.), inflammatory myopathy, such as myocarditis, and other inflammatory diseases, ischemia-reperfusion injury or diseases or conditions associated with an inflammatory ischemic event, such as stroke or cardiac arrest, systemic inflammatory response syndrome, septic shock, large inflammatory hepatocellular adenomas,

[0830] anorexia, cachexia or fatigue caused by or associated with cancer, pathological conditions associated with hypoxia or astrogliosis, such as diabetic retinopathy, cancer or neurodegeneration,

[0831] Gout, prostate enlargement, dry eye syndrome and related disorders, IgG4-related disorders, idiopathic granulomatous mastitis, pyoderma gangrenosum, cutaneous dermatomyositis, idiopathic inflammatory myositis, chronic atypical neutrophilic dermatosis with lipodystrophy and fever (Nakayo-Nishimura syndrome), interferon gene promoter-associated vasculopathy, Aicardi-Goutières syndrome, graft-versus-host disease, including after peripheral blood hematopoietic cell transplantation, neuromyelitis, immune thrombocytopenia, coronavirus pneumonia (COVID-19), symptoms associated with COVID-19 infection, hospital-acquired pneumonia in critically ill patients with a proinflammatory phenotype, lung injury after spontaneous subarachnoid hemorrhages, ocular mucosal pemphigoid, oral lichen planus, steroid-resistant / relapsing immune thrombocytopenia,Pulmonary injury after intracerebral hemorrhage, moderate to severe traumatic intracerebral hemorrhage / contusion, recurrent giant cell arteritis, systemic sclerosis, treatment of nonsegmental vitiligo, treatment of HIV symptoms, autoinflammatory syndrome, primary biliary cholangitis, recurrent or naive dermatomyositis, Sjogren's syndrome, inflammation and depression in people with HIV, APOL1-associated kidney disease, polymyalgia rheumatica, idiopathic inflammatory myopathy.

[0832] The stated problem is solved and the claimed technical result is achieved by using a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, or a compound of formula A or a pharmaceutically acceptable salt thereof, or a compound of formula B or a pharmaceutically acceptable salt thereof, or a compound of formula C or a pharmaceutically acceptable salt thereof, or a compound of formula A” or a pharmaceutically acceptable salt thereof, or a compound of formula B”, or a pharmaceutically acceptable salt thereof, or a compound of formula C” or a pharmaceutically acceptable salt thereof, for the treatment of diseases in humans and animals.

[0833] The stated problem is solved and the claimed technical result is achieved by using a compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof, or a compound of formula A or a pharmaceutically acceptable salt thereof, or a compound of formula B or a pharmaceutically acceptable salt thereof, a compound of formula C or a pharmaceutically acceptable salt thereof, or a compound of formula A" or a pharmaceutically acceptable salt thereof, or a compound of formula B", or a pharmaceutically acceptable salt thereof, or a compound of formula C" or a pharmaceutically acceptable salt thereof, for the production of a pharmaceutical composition or a medicinal product for the treatment of diseases in humans and animals.

[0834] The stated problem is solved and the claimed technical result is achieved through the use of a pharmaceutical composition containing a compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof, or a compound of formula A or a pharmaceutically acceptable salt thereof, or a compound of formula B, or a pharmaceutically acceptable salt thereof, or a compound of formula C or a pharmaceutically acceptable salt thereof, or a compound of formula A" or a pharmaceutically acceptable salt thereof, or a compound of formula B", or a pharmaceutically acceptable salt thereof, or a compound of formula C", or a pharmaceutically acceptable salt thereof, for the treatment of diseases in humans and animals.

[0835] The stated problem is solved and the claimed technical result is achieved through the use of a medicinal product containing a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, or a compound of formula A or a pharmaceutically acceptable salt thereof, or a compound of formula B or a pharmaceutically acceptable salt thereof, or a compound of formula C or a pharmaceutically acceptable salt thereof, or a compound of formula A” or a pharmaceutically acceptable salt thereof, or a compound of formula B”, or a pharmaceutically acceptable salt thereof, or a compound of formula C”, or a pharmaceutically acceptable salt thereof, for the treatment of diseases in humans and animals.

[0836] The stated problem is solved and the claimed technical result is achieved by using a pharmaceutical composition containing a compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof, or a compound of formula A or a pharmaceutically acceptable salt thereof, or a compound of formula B, or a pharmaceutically acceptable salt thereof, or a compound of formula C or a pharmaceutically acceptable salt thereof, or a compound of formula A" or a pharmaceutically acceptable salt thereof, or a compound of formula B", or a pharmaceutically acceptable salt thereof, or a compound of formula C", or a pharmaceutically acceptable salt thereof, for the production of a medicinal product for the treatment of diseases in humans and animals.

[0837] The stated problem is solved and the claimed technical result is achieved by using a compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof, or a compound of formula A or a pharmaceutically acceptable salt thereof, or a compound of formula B or a pharmaceutically acceptable salt thereof, or a compound of formula C or a pharmaceutically acceptable salt thereof, or a compound of formula A" or a pharmaceutically acceptable salt thereof, or a compound of formula B", or a pharmaceutically acceptable salt thereof, or a compound of formula C", or a pharmaceutically acceptable salt thereof, for the production of a pharmaceutical composition or a medicinal product for the treatment of autoimmune diseases by inhibiting Janus kinase in humans and animals.

[0838] The stated problem is solved and the claimed technical result is achieved by using a pharmaceutical composition containing a compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof, or a compound of formula A or a pharmaceutically acceptable salt thereof, or a compound of formula B, or a pharmaceutically acceptable salt thereof, or a compound of formula C or a pharmaceutically acceptable salt thereof, or a compound of formula A" or a pharmaceutically acceptable salt thereof, or a compound of formula B", or a pharmaceutically acceptable salt thereof, or a compound of formula C", or a pharmaceutically acceptable salt thereof, for the treatment of autoimmune diseases by inhibiting Janus kinase in humans and animals.

[0839] The stated problem is solved and the claimed technical result is achieved by using a medicinal product containing a compound characterized by formula (I)', formula IV or formula IV”, or a pharmaceutically acceptable salt thereof, or a compound of formula A or a pharmaceutically acceptable salt thereof, or a compound of formula B or a pharmaceutically acceptable salt thereof, or a compound of formula C or a pharmaceutically acceptable salt thereof, or a compound of formula A” or a pharmaceutically acceptable salt thereof, or a compound of formula B”, or a pharmaceutically acceptable salt thereof, or a compound of formula C”, or a pharmaceutically acceptable salt thereof, for the treatment of autoimmune diseases by inhibiting Janus kinase in humans and animals.

[0840] The stated problem is solved and the claimed technical result is achieved by using a pharmaceutical composition containing a compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof, or a compound of formula A or a pharmaceutically acceptable salt thereof, or a compound of formula B, or a pharmaceutically acceptable salt thereof, or a compound of formula C or a pharmaceutically acceptable salt thereof, or a compound of formula A" or a pharmaceutically acceptable salt thereof, or a compound of formula B", or a pharmaceutically acceptable salt thereof, or a compound of formula C", or a pharmaceutically acceptable salt thereof, for the production of a medicinal product for the treatment of autoimmune diseases by inhibiting Janus kinase in humans and animals.

[0841] The stated problem is solved and the claimed technical result is achieved by using a compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof, or a compound of formula A or a pharmaceutically acceptable salt thereof, or a compound of formula B, or a pharmaceutically acceptable salt thereof, or a compound of formula C or a pharmaceutically acceptable salt thereof, or a compound of formula A" or a pharmaceutically acceptable salt thereof, or a compound of formula B", or a pharmaceutically acceptable salt thereof, or a compound of formula C", or a pharmaceutically acceptable salt thereof, for the production of a pharmaceutical composition or a medicinal product for the treatment of autoimmune diseases by inhibiting Janus kinase in mammals, including humans and animals.

[0842] The stated problem is solved and the claimed technical result is achieved by using a pharmaceutical composition containing a compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof, or a compound of formula A or a pharmaceutically acceptable salt thereof, or a compound of formula B, or a pharmaceutically acceptable salt thereof, or a compound of formula C or a pharmaceutically acceptable salt thereof, or a compound of formula A" or a pharmaceutically acceptable salt thereof, or a compound of formula B", or a pharmaceutically acceptable salt thereof, or a compound of formula C", or a pharmaceutically acceptable salt thereof, for the treatment of autoimmune diseases by inhibiting Janus kinase in mammals, including humans and animals.

[0843] The stated problem is solved and the claimed technical result is achieved by using a medicinal product containing a compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof, a compound of formula A or a pharmaceutically acceptable salt thereof, or a compound of formula B, or a pharmaceutically acceptable salt thereof, or a compound of formula C or a pharmaceutically acceptable salt thereof, or a compound of formula A" or a pharmaceutically acceptable salt thereof, or a compound of formula B", or a pharmaceutically acceptable salt thereof, or a compound of formula C", or a pharmaceutically acceptable salt thereof, for the treatment of autoimmune diseases by inhibiting Janus kinase in mammals, including humans and animals.

[0844] The stated problem is solved and the claimed technical result is achieved by using a pharmaceutical composition containing a compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof, or a compound of formula A or a pharmaceutically acceptable salt thereof, or a compound of formula B, or a pharmaceutically acceptable salt thereof, or a compound of formula C or a pharmaceutically acceptable salt thereof, or a compound of formula A" or a pharmaceutically acceptable salt thereof, or a compound of formula B", or a pharmaceutically acceptable salt thereof, or a compound of formula C", or a pharmaceutically acceptable salt thereof, for the production of a medicinal product for the treatment of autoimmune diseases by inhibiting Janus kinase in mammals, including humans and animals.

[0845] The stated problem is solved and the claimed technical result is achieved by using a compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof, or a compound of formula A or a pharmaceutically acceptable salt thereof, or a compound of formula B, or a pharmaceutically acceptable salt thereof, or a compound of formula C or a pharmaceutically acceptable salt thereof, or a compound of formula A" or a pharmaceutically acceptable salt thereof, or a compound of formula B", or a pharmaceutically acceptable salt thereof, or a compound of formula C", or a pharmaceutically acceptable salt thereof, for the production of a pharmaceutical composition or a medicinal product for the treatment of diseases by inhibiting Janus kinase in mammals, including humans and animals.

[0846] The stated problem is solved and the claimed technical result is achieved by using a pharmaceutical composition containing a compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof, or a compound of formula A or a pharmaceutically acceptable salt thereof, or a compound of formula B, or a pharmaceutically acceptable salt thereof, or a compound of formula C or a pharmaceutically acceptable salt thereof, or a compound of formula A" or a pharmaceutically acceptable salt thereof, or a compound of formula B", or a pharmaceutically acceptable salt thereof, or a compound of formula C", or a pharmaceutically acceptable salt thereof, for the treatment of diseases by inhibiting Janus kinase in mammals, including humans and animals.The stated problem is solved and the claimed technical result is achieved through the use of a medicinal product containing a compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof, or a compound of formula A or a pharmaceutically acceptable salt thereof, or a compound of formula B, or a pharmaceutically acceptable salt thereof, or a compound of formula C or a pharmaceutically acceptable salt thereof, or a compound of formula A" or a pharmaceutically acceptable salt thereof, or a compound of formula B", or a pharmaceutically acceptable salt thereof, or a compound of formula C", or a pharmaceutically acceptable salt thereof, for the treatment of diseases by inhibiting Janus kinase in mammals, including humans and animals.

[0847] The stated problem is solved and the claimed technical result is achieved by using a pharmaceutical composition containing a compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof, or a compound of formula A or a pharmaceutically acceptable salt thereof, or a compound of formula B, or a pharmaceutically acceptable salt thereof, or a compound of formula C or a pharmaceutically acceptable salt thereof, or a compound of formula A" or a pharmaceutically acceptable salt thereof, or a compound of formula B", or a pharmaceutically acceptable salt thereof, or a compound of formula C", or a pharmaceutically acceptable salt thereof, for the production of a medicinal product for the treatment of diseases by inhibiting Janus kinase in mammals, including humans and animals.

[0848] The stated problem is solved and the claimed technical result is achieved by using a compound characterized by formula (I)', formula IV or formula IV", or a pharmaceutically acceptable salt thereof, or a compound of formula A or a pharmaceutically acceptable salt thereof, or a compound of formula B, or a pharmaceutically acceptable salt thereof, or a compound of formula C or a pharmaceutically acceptable salt thereof, or a compound of formula A" or a pharmaceutically acceptable salt thereof, or a compound of formula B", or a pharmaceutically acceptable salt thereof, or a compound of formula C", or a pharmaceutically acceptable salt thereof for the treatment of diseases by inhibiting Janus kinase in mammals, including humans and animals.

[0849] More preferably, within the framework of the present invention, mammals include domestic animals. More preferably, within the framework of the present invention, domestic animals include, for example, but not limited to, sheep, goats, pigs, horses, camels, deer, rabbits, cats, and dogs.

[0850] More preferably, the animal disease of the present invention is selected from the group consisting of rheumatoid arthritis, atopic dermatitis, focal alopecia, coronavirus infection, including covid-19, various types of cancer, asthma, itching, including that associated with allergic dermatitis, allergies, chronic respiratory diseases and other diseases in which immunosuppression and / or immunomodulation is desirable.

[0851] Within the framework of the present invention, the stated problem is solved, and the claimed technical result is achieved by means of a method for obtaining a new compound characterized by formula (I)', which includes removing the protective group R of the compound of formula aaa:

[0852]

[0853] Within the framework of the present invention, the stated problem is solved, and the claimed technical result is achieved by means of a method for obtaining a new compound characterized by formula (I)', or a pharmaceutically acceptable salt thereof, which includes removing the protective group R of the compound of formula aaa or its salt:

[0854]

[0855] Within the framework of the present invention, the stated problem is solved, and the claimed technical result is achieved by means of a method for obtaining a new compound characterized by formula (I)', or a pharmaceutically acceptable salt thereof, which includes removing the protective group R of the compound of formula aaa:

[0856]

[0857] Within the framework of the present invention, the stated problem is solved, and the claimed technical result is achieved by means of a method for obtaining a new compound characterized by formula (I)', or its salt, which includes removing the protective group R of the compound of formula aaa or its salt: (Ri)'

[0858] N

[0859] b

[0860]

[0861] In one embodiment of the present invention, a salt, including a pharmaceutically acceptable salt, of a compound characterized by formula (I)' is a salt formed by a compound characterized by formula (I)' and an acid.

[0862] More preferably, the acid of the present invention is a monobasic, dibasic or tribasic acid.

[0863] More preferably, the acid of the present invention is a monobasic, dibasic or polybasic acid.

[0864] In one embodiment of the present invention, the salt of the compound characterized by formula (I)' is a salt formed between the compound characterized by formula (I)' and an inorganic acid.

[0865] More preferably, the inorganic acid of the present invention is a monobasic, dibasic or tribasic acid.

[0866] If the inorganic acid is a monobasic acid, the molar ratio of the salt-forming acid to the compound characterized by formula (I)' is 1:1.

[0867] More preferably, within the framework of the present invention, the monobasic inorganic acid is selected from the group including, but not limited to, hydrochloric, hydrofluoric, hydrobromic, hydroiodic, nitric and nitrous acids.

[0868] If the inorganic acid is a dibasic acid, the molar ratio of the salt-forming acid to the compound characterized by formula (I)' is 1:1 or 1:2.

[0869] More preferably, within the framework of the present invention, the dibasic inorganic acid is selected from the group including, but not limited to, hydrosulfuric, sulfurous, sulfuric, and carbonic acids. If the inorganic acid is a tribasic acid, the molar ratio of the salt-forming acid to the compound characterized by formula (I)' is 1:1, 1:2, or 1:3.

[0870] More preferably, in the context of the present invention, the tribasic inorganic acid is, but is not limited to, phosphoric acid.

[0871] In one embodiment of the present invention, the salt of the compound characterized by formula (I)' is a salt formed between the compound characterized by formula (I)' and an organic acid.

[0872] More preferably, the organic acid of the present invention is a monobasic, dibasic or polybasic acid.

[0873] If the organic acid is a monobasic acid, the molar ratio of the salt-forming acid to the compound characterized by formula (I)' is 1:1.

[0874] More preferably, within the framework of the present invention, the monobasic organic acid is selected from the group including, but not limited to, formic, acetic, monofluoroacetic, difluoroacetic, trifluoroacetic, propionic, butyric, isobutyric, valerianic, caproic, enanthoic, p-toluic, anisic and phenylacetic acid.

[0875] If the organic acid is a dibasic acid, the molar ratio of the salt-forming acid to the compound characterized by formula (I)' is 1:1 or 1:2.

[0876] More preferably, within the framework of the present invention, the dibasic organic acid is selected from the group including, but not limited to, oxalic, malonic, succinic, dioxosuccinic, glutaric, α-hydroxyglutaric, 2-oxoglutaric, 3-oxoglutaric, adipic, pimelic, diaminopimelic, phthalic, isophthalic, teryphthalic, malic, suberic, azelaic, maleic, fumaric, tartaric, aspartic, glutamic, arabic and D-glucaric acid.

[0877] If the organic acid is a tribasic acid, the molar ratio of the salt-forming acid to the compound characterized by formula (I)' is 1:1, 1:2, or 1:3.

[0878] More preferably, within the framework of the present invention, the tribasic organic acid is selected from the group including, but not limited to, citric, isocitric, aconitic, β-carboxyglutaric, 2-hydroxy-1,2,3-nonadecanetricarboxylic and benzene-1,3,5-tricarboxylic acid.

[0879] In one embodiment of the present invention, the salt of compound aa is a salt formed between compound aaa and an acid.

[0880] More preferably, the acid of the present invention is a monobasic, dibasic or tribasic acid.

[0881] More preferably, the acid of the present invention is a monobasic, dibasic or polybasic acid.

[0882] In one embodiment of the present invention, the salt of compound aaa is a salt formed between compound aaa and an inorganic acid.

[0883] More preferably, the inorganic acid of the present invention is a monobasic, dibasic or tribasic acid.

[0884] If the inorganic acid is a monobasic acid, then the molar ratio of the salt-forming acid to the compound aaa is 1:1.

[0885] More preferably, within the framework of the present invention, the monobasic inorganic acid is selected from the group including, but not limited to, hydrochloric, hydrofluoric, hydrobromic, hydroiodic, nitric and nitrous acids.

[0886] If the inorganic acid is a dibasic acid, then the molar ratio of the salt-forming acid to the compound aaa is 1:1 or 1:2.

[0887] More preferably, within the framework of the present invention, the dibasic inorganic acid is selected from the group including, but not limited to, hydrogen sulfide, sulfurous, sulfuric and carbonic acids.

[0888] If the inorganic acid is a tribasic acid, the molar ratio of the salt-forming acid to the compound aaa is 1:1, 1:2, or 1:3.

[0889] More preferably, in the context of the present invention, the tribasic inorganic acid is, but is not limited to, phosphoric acid.

[0890] In one embodiment of the present invention, the salt of compound aaa is a salt formed between compound aaa and an organic acid.

[0891] More preferably, the organic acid of the present invention is a monobasic, dibasic, or polybasic acid. If the organic acid is a monobasic acid, the molar ratio of the salt-forming acid to the compound aaa is 1:1.

[0892] More preferably, within the framework of the present invention, the monobasic organic acid is selected from the group including, but not limited to, formic, acetic, monofluoroacetic, difluoroacetic, trifluoroacetic, propionic, butyric, isobutyric, valerianic, caproic, enanthoic, p-toluic, anisic and phenylacetic acid.

[0893] If the organic acid is a dibasic acid, then the molar ratio of the salt-forming acid to the compound aaa is 1:1 or 1:2.

[0894] More preferably, within the framework of the present invention, the dibasic organic acid is selected from the group including, but not limited to, oxalic, malonic, succinic, dioxosuccinic, glutaric, α-hydroxyglutaric, 2-oxoglutaric, 3-oxoglutaric, adipic, pimelic, diaminopimelic, phthalic, isophthalic, teryphthalic, malic, suberic, azelaic, maleic, fumaric, tartaric, aspartic, glutamic, arabic and D-glucaric acid.

[0895] If the organic acid is a tribasic acid, the molar ratio of the salt-forming acid to the compound aaa is 1:1, 1:2, or 1:3.

[0896] More preferably, within the framework of the present invention, the tribasic organic acid is selected from the group including, but not limited to, citric, isocitric, aconitic, β-carboxyglutaric, 2-hydroxy-1,2,3-nonadecanetricarboxylic and benzene-1,3,5-tricarboxylic acid.

[0897] In one embodiment of the present invention, the protecting group R is benzyloxycarbonyl, 2,2,2-trichloroethoxycarbonyl, 2-(trimethylsilyl)ethoxycarbonyl, 2-(4-trifluoromethylphenylsulfonyl)ethoxycarbonyl, tert-butoxycarbonyl, 1-adamantyloxycarbonyl, 2-adamantylcarbonyl, 2,4-dimethylpent-3-yloxycarbonyl, cyclohexyloxycarbonyl, 1,1-dimethyl-2,2,2-trichloroethoxycarbonyl, vinyl, 2-chloroethyl, 2-phenylsulfonylethyl, allyl, benzyl, 2-nitrobenzyl, 4-nitrobenzyl, diphenyl-4-pyridylmethyl, N',N'-dimethylhydrazinyl, methoxymethyl, tert-butoxymethyl, benzyloxymethyl, 2-tetrahydropyranyl, N-pivaloyloxymethyl or 2-(trimethylsilyl)ethoxymethyl.

[0898] More preferably, the protecting group R is 2-(trimethylsilyl)ethoxycarbonyl. One embodiment of the present invention is a method for preparing a compound characterized by formula (I)' or a salt thereof, characterized in that the removal of the protecting group R of the compound of formula aaa or its salt occurs in an organic solvent.

[0899] One embodiment of the present invention is a method for producing a compound characterized by formula (I)' or a salt thereof, characterized in that the removal of the protective group R of the compound of formula aaa or its salt occurs in water or an ammonia solution.

[0900] One embodiment of the present invention is a method for producing a compound characterized by formula (I)' or a salt thereof, characterized in that the removal of the protective group R of the compound of formula aaa or its salt occurs in a mixture of an organic solvent and water or in a mixture of an organic solvent and an ammonia solution.

[0901] One embodiment of the present invention is a method for producing a compound characterized by formula (I)' or a salt thereof, characterized in that the removal of the protective group R of the compound of formula aaa or its salt occurs in an aprotic organic solvent or a mixture thereof with water or an ammonia solution.

[0902] One embodiment of the present invention is a method for producing a compound characterized by formula (I)' or a salt thereof, characterized in that the removal of the protective group R of the compound of formula aaa or its salt occurs in a protic organic solvent or a mixture thereof with water or an ammonia solution.

[0903] One embodiment of the present invention is a method for producing a compound characterized by formula (I)' or a salt thereof, characterized in that the removal of the protective group R of the compound of formula aaa or its salt is carried out by reacting the compound of formula aaa or its salt with a fluorine-containing compound.

[0904] One embodiment of the present invention is a method for producing a compound characterized by formula (I)' or a salt thereof, characterized in that the removal of the protective group R of the compound of formula aaa or its salt is carried out by reacting the compound of formula aaa or its salt with a fluorine-containing compound, followed by treatment with a base.

[0905] One embodiment of the present invention is a method for producing a compound characterized by formula (I)' or a salt thereof, characterized in that the removal of the protective group R of the compound of formula aaa or its salt is carried out by reacting the compound of formula aaa or its salt with a fluorine-containing acid, followed by treatment with a base.

[0906] One embodiment of the present invention is a method for producing a compound characterized by formula (I)' or a salt thereof, characterized in that the removal of the protective group R of the compound of formula aaa or its salt is carried out by reacting the compound of formula aaa or its salt with an organic fluorine-containing acid, followed by treatment with a base.

[0907] One embodiment of the present invention is a method for producing a compound characterized by formula (I)' or a salt thereof, characterized in that the removal of the protective group R of the compound of formula aaa or its salt is carried out by reacting the compound of formula aaa or its salt with an organic fluorine-containing acid, followed by treatment with an organic base.

[0908] More preferably, when removing the protective group R, the subsequent treatment is carried out with a base according to the present invention, which is an aqueous ammonia solution.

[0909] More preferably, when removing the protective group R, the subsequent treatment is carried out with a base according to the present invention, which is a solution of ammonia in alcohol.

[0910] More preferably, when removing the protecting group R, the subsequent treatment is carried out with a base according to the present invention, which is a hydroxides or halides of quaternary ammonium cations.

[0911] More preferably, the hydroxide or halide of quaternary ammonium cations, without limitation, is selected from tetramethylammonium hydroxide, tetraethylammonium bromide, tetrapropylammonium chloride, tetrabutylammonium fluoride or benzalkonium chloride.

[0912] More preferably, when removing the protective group R, the subsequent treatment is carried out with an organic base according to the present invention, which is an amine, including a primary amine.

[0913] The stated problem is solved, and the stated technical result is achieved by combining the formula aaa: (Ri)'

[0914] N

[0915] b

[0916]

[0917] where R is a protecting group.

[0918] The stated problem is solved and the stated technical result is achieved by combining the formula aaa:

[0919] (Ri)'

[0920] N

[0921] ь

[0922]

[0923] or its salts, where R is a protecting group.

[0924] Within the framework of the present invention, the stated problem is solved, and the claimed technical result is achieved by means of a method for obtaining a new compound characterized by formula IV, which includes removing the protective group R of the compound of formula aa:

[0925]

[0926] Within the framework of the present invention, the stated problem is solved, and the claimed technical result is achieved by means of a method for obtaining a new compound characterized by formula IV, or a pharmaceutically acceptable salt thereof, which includes removing the protective group R of the compound of formula aa or its salt:

[0927]

[0928] Within the framework of the present invention, the stated problem is solved, and the claimed techn...

Claims

Invention formula 1. A compound characterized by formula (I): (R0' or its pharmaceutically acceptable salts, where (X)', (Y)' independently of each other represent -CH- or -N-; a = 1, 2 or 3; b = 1, 2 or 3; (Ri)' is A, mercapto, -C(O)R3, -C(NR )NR.4R5, -NR4R5, -NHNHR3, -NNR3, -CH(NR3)R3, -SO2R3, or -SO3R3; R3 is any of A, hydrogen, hydroxy, halogen, or NR4R5; R4, R5 Re independently of each other represent any of A; A is C3-C6-cycloalkyl, C4-C6-heterocycle, C4-C6-aryl, branched or unbranched C1-C6-alkyl, branched or unbranched C1-C6-alkyloxy (-O-Ci-e-alkyl), branched or unbranched C1-C6-alkylthio (-S-C1-6-alkyl), or branched or unbranched C2-C6-alkenyl; R2 is any one of A, hydroxy, mercapto, amino, halogen, azido, nitroso, nitro, nitrile, cyano, diazo, sulfo, -C(O)R3, -C(NR6)NR4R5, -NR4R5, -NHNHR3, -NNR3, CH(NR3)R3, -SO2R3, or -SO3R3, wherein A may be substituted by one or more substituents selected from A, hydroxy, mercapto, amino, halogen, azido, nitroso, nitro, nitrile, cyano, diazo, sulfo, -C(O)R3, -C(NR6)NR4R5, -NR4R5, -NHNHR3, -NNR3, CH(NR3)R3, -SO2R3, and -SO3R3.

2. A compound according to claim 1, characterized in that (X)' is -N-, (Y)' is -CH-; a = 1; b = 1; (Ri)' is A, -C(O)R3, -SO2R3, or -SO3R3; R3 represents any of A; A is branched or unbranched C-C6-alkyl, branched or unbranched C-C6-alkyloxy (-O-Ci-e-alkyl), branched or unbranched C-C6-alkylthio (-S-Ci-b-alkyl), or branched or unbranched Cr-C6-alkenyl; R2 represents any of A, wherein A is substituted with one or more substituents selected from A, hydroxy, mercapto, amino, halogen, azido, nitroso, nitro, nitrile and cyano.

3. The compound according to item 1, characterized in that (X)' is -N-, (Y)' is -CH-; a = 1; b = 1; (Ri)' represents -C(O)R3 or -SO2R3; R3 represents any of A; R2 represents any of A; A is a branched or unbranched C-C6-alkyl, a branched or unbranched Ci-C6-alkyloxy (-O-Ci-6-alkyl), or a branched or unbranched Ci-C6-alkylthio (-S-Ci-6-alkyl); wherein A is substituted by one or more substituents selected from A and cyano.

4. Pi connection. 1-3 selected from the group consisting of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(2-(methylthio)acetyl)azetidin-3-yl)acetonitrile, 2-(3 -(4-(7H-pyrrolo[2, 3 -d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1 -(3 -methoxypropanoyl)azetide yn-3 -yl)acetonitrile, 2-(3 -(4-(7H-pyrrolo[2, 3 -d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1 -(3 -(methylthio)propanoyl)azetidin-3 -yl)acetonitrile, 2-(3 -(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-((2-methoxyethyl)sulfonyl)azetidin-3-yl)acetonitrile, 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(((methylthio)methyl)sulfonyl)azetide-3-yl)acetonitrile and 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1 -((2-(methylthio)ethyl)sulfonyl)azetidin-3-yl)acetonitrile.

5. A pharmaceutical composition exhibiting Janus kinase (JAK) inhibitor properties for the treatment of autoimmune diseases, comprising a therapeutically effective amount of a compound according to any one of paragraphs 1-4 and at least one pharmaceutically acceptable excipient.

6. The pharmaceutical composition according to claim 5, characterized in that the autoimmune disease is selected from the group including rheumatoid arthritis, psoriatic arthritis, juvenile arthritis, atopic dermatitis, lupus and alopecia.

7. The pharmaceutical composition according to claim 5, characterized in that at least one pharmaceutically acceptable excipient is selected from the group consisting of excipients, stabilizers, solubilizers, humectants, lubricants, glidants, thickeners, sweeteners, flavorings, aromatizers, prolonged delivery regulators, diluents, fillers, emulsifiers, preservatives, antioxidants, buffering agents, cryoprotectants, pH-regulating agents, substances for maintaining isotonicity, and correcting substances.

8. A medicinal product exhibiting Janus kinase (JAK) inhibitor properties for the treatment of autoimmune diseases, comprising an effective amount of a compound according to any one of paragraphs 1-4 and at least one pharmaceutically acceptable excipient.

9. The medicinal product according to claim 8, characterized in that at least one pharmaceutically acceptable excipient is selected from the group consisting of excipients, stabilizers, solubilizers, humectants, lubricants, glidants, thickeners, sweeteners, flavorings, aromatizers, prolonged delivery regulators, diluents, fillers, emulsifiers, preservatives, antioxidants, buffering agents, cryoprotectants, pH-regulating agents, substances for maintaining isotonicity, and correcting substances.

10. The medicinal product according to claim 8, characterized in that the autoimmune disease is selected from the group including rheumatoid arthritis, psoriatic arthritis, juvenile arthritis, atopic dermatitis, lupus and alopecia.

11. A medicinal product according to clause 8, characterized in that it is a solid medicinal product.

12. A medicinal product according to item 11, characterized in that it is a tablet or capsule.

13. Use of a compound according to any one of paragraphs 1-4 for the preparation of a medicament for the treatment of autoimmune diseases by inhibiting Janus kinase.

14. The use according to claim 13, characterized in that the autoimmune disease is selected from the group including rheumatoid arthritis, psoriatic arthritis, juvenile arthritis, atopic dermatitis, lupus and alopecia.

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