UA71952C2 - Urea aromatic derivatives as antiinflammatory agents - Google Patents

Abstract

Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.

Description

Description of the invention

The present invention relates to new compounds that inhibit the production of cytokines involved in inflammatory 2 processes, and therefore can be used for the treatment of diseases and pathological conditions accompanied by inflammation, such as chronic inflammatory diseases. The present invention also relates to methods of obtaining such compounds and pharmaceutical compositions containing these compounds.

Tumor necrosis factor (TNF) and interleukin-1 (1/-1) are important biological factors collectively known as anti-inflammatory cytokines. Together with some other related molecules, they mediate the inflammatory response associated with the immunological recognition of infectious agents. The general response plays an important role in limiting the development of pathogenic infections and fighting them.

Elevated levels of anti-inflammatory cytokines are also associated with numerous autoimmune diseases, such as toxic shock syndrome, rheumatoid arthritis, osteoarthritis, diabetes, and inflammatory bowel disease (S.A.

Oipageio et al., Chem. Ipiesi Oisease 6: 51, 1984). In such diseases, chronic amplification of the reaction exacerbates 72 or causes many of the observed chronic manifestations. So, for example, with rheumatism, inflammatory cells penetrate into the synovial tissue, which lead to the destruction of cartilage and bone (A.E. Kosi et al., in). Ipmevi Honey. 43: 28-38, 1995). In such diseases, an important and recognized therapeutic approach, based on the possible use of drugs, is to reduce the levels of pro-inflammatory cytokines, such as TME (in the form isolated from cells, also called TMRa) and I/-10. A large number of therapeutic agents for the treatment of cytokine-mediated diseases are currently undergoing clinical trials. For numerous autoimmune diseases, the effectiveness of the use of a monoclonal antibody against TMR was confirmed (R. Neaii, "SORB57U1: Ap Epdipeegeai Nytap Id4 Apii- TMERa Apiiirodu", materials of the IVS Meeipd op SufiukKipe conference

Apiadopiwiz, Philadelphia, st. Pennsylvania, April 24-25, 1997). Such fields of application include the treatment of rheumatoid arthritis, Crohn's disease and ulcerative colitis (E.S.S. KapkKip et al., Vgyizy 9. KPetst. 35: 334-342, p. 29 1997; MU.A. Egask et al., I Apseii 349: 521-524, 1997). It is assumed that the monoclonal antibody performs its Ge) function by binding both soluble TMRa and membrane-bound TME.

A soluble TMEa receptor interacting with TMRa was constructed. This approach is similar to the approach described above for monoclonal antibodies to TMRa, thereby reducing its concentration. For one of the variants of this design, called Epbgei! (Ittipeh, Seattle, WA) recently demonstrated efficacy in treating arthritis in phase I clinical trials (Whomeg et al., Mayte yu

Phytobiology 15: 1240, 1997). For another version of the TMERa receptor, Ko 45-2081 (Noitanp-I aKkosne Ips.,

Nutli, pc. New Jersey), the effectiveness of its use was demonstrated in various animal models of allergic inflammation, mild and acute lung injury. Ko 45-2081 is a "-- recombinant chimeric molecule, constructed by fusing the soluble human TME receptor, which has a molecular weight of 55 kDa, with the gene of the hinge region of the heavy chain of Id1, which is expressed in eukaryotic cells (Kepgeyi et al., Ipiatt . Kez. 46: p. 143, 1997).

I--1 as an immunological effector molecule is involved in the development of numerous diseases. Receptor antagonist

I--1 (1--1ha) was studied in clinical trials on humans. It has been shown to be effective in the treatment of rheumatoid arthritis (Anthril, Amgen). In a phase I human clinical trial, ІІ/-Igta resulted in a І decrease in mortality in patients suffering from septic shock syndrome (Oipageyo, Miigshiop 11, 492, p 1995). Osteoarthritis is a slowly progressive disease characterized by the destruction of cartilage

From" the joint. II/-1 was detected in synovial fluid and in the cartilage matrix of joints affected by osteoarthritis. On various experimental models of arthritis, it was established that I/-1 antagonists allow to reduce the decomposition of cartilage matrix components (Spemaiieg. Vioted RNpaptasoiNeg., 51, 58, 1997). Recently, it has been established that nitric oxide, which is a mediator of cardiovascular homeostasis, nerve and impulse transmission, and immune function, plays an important role in modulating bone regeneration. Cytokines, such as I/-1 and TME, are strong stimulators of MO production. MO is a molecule with an important regulatory function in bone, affecting cells lining the osteoblast and osteoclast (Emapz et al., U, Vope Mipeg Kez. 11, 380, o 1996). Increased destruction of beta cells, which leads to the development of insulin-dependent diabetes mellitus, sl 20 depends on 11-1. Some of these injuries may be mediated by other effectors, such as prostaglandins and thromboxanes. I/-1 can affect this process by controlling the level of expression of both cyclooxygenase II and inducible nitric oxide synthetase (Meyupiel et al., Rgos. Bos. Ehr. Viol. Mead., 211, 24, 1996).

It is assumed that inhibitors of cytokine production block the expression of inducible cyclooxygenase 29 (COX-2). It was established that the expression of COX-2 increases under the influence of cytokines and it is assumed that it represents

GF) is an isoform of cyclooxygenase, which causes inflammation (M.K. O'Vapiop et al., Rgos. May. Asad. Zsi. O.5.A. 89, 4888, 1992). Therefore, it should be expected that inhibitors of cytokines such as II-1 should be effective against disorders currently treated with COX inhibitors such as conventional non-steroidal anti-inflammatory drugs (NSAIDs). Such disorders include acute and chronic pain, as well as inflammatory 60 symptoms and cardiovascular diseases.

It was established that the level of certain cytokines increases in inflammatory bowel disease (C3C3K). In patients suffering from CKD, there is an imbalance of II-1 and II-1ha in the intestinal mucosa. Inadequate production of endogenous IL-IgT can influence the pathogenesis of CKD (Sotipeiyi et al., AItepi. Rpagtasoi. Teg. 10, 49, 1996). Alzheimer's disease is characterized by the presence of beta-amyloid protein deposits, the presence of neurofibrillary tangles and cholinergic dysfunction in the hippocampus. Structural and metabolic disorder,

which appears in Alzheimer's disease is probably caused by a constant elevated level of II -1 (Noidep et al.,

Honey. Nuroipezez, 45, 559, 1995). It has been established that 1-1 plays a role in the pathogenesis caused by the human immunodeficiency virus (HIV). A clear connection of II-yiga with acute inflammations, as well as with various stages of the disease in the pathophysiology of HIV infection was established (Kgepygeg et al., Sip. Ehr. Ittipoi., 109, 54, 1997). 1-1 and

TMEs are involved in periodontal disease. The process of destruction associated with periodontal disease can be caused by a violation of the regulation of both II -1 and TME (Noucheiyiv, Ogai Oiv. 1, 266, 1995).

Proinflammatory cytokines, such as TMRa apa 11-IU, are also important mediators of septic shock and associated cardiopulmonary dysfunction, adult acute respiratory distress syndrome (ARDS), and multiple organ failure. TMRa is also involved in cachexia and degradation of muscle tissue associated with

HIV infection (I apaimega, etc., Ateg. ). Mei., 85, 289, 1988). Obesity is accompanied by an increased likelihood of infection, diabetes and cardiovascular diseases. It was established that for each of the above conditions there are abnormalities in the expression level of TMER (Goyteda et al. EBABEV 3). 12, 57, 1998).

It is assumed that elevated levels of TMRa are also present in other eating disorders, such as /5 Anorexia nervosa and bulimia nervosa. Pathophysiological parallels between anorexia nervosa and cancer cachexia have been revealed (Noidep et al., Med. NuroiNpezez 47, 423, 1996). Using an experimental model, it was established that the inhibitor of TMER production NOI-211 improves rehabilitation after a closed brain injury (Zpopati et al., U. Meyigoittipoi. 72, 169, 1997). It is known that there is an inflammatory component in the development of atherosclerosis, and it is assumed that such cytokines as II-1 and TME stimulate the development of the disease. In an animal model, it was established that an antagonist of the 1-1 receptor inhibits the formation of a fatty layer (Einade et al.,

Sigstiayop, 97, 242, 1998).

Abnormal expression of inducible nitric oxide synthetase (IMO5) was accompanied by the development of hypertension in rats with spontaneous hypertension (Spoi et al., Nuregiepviop, 31, 643, 1998). II-1 affects the expression of IMO and therefore can also participate in the pathogenesis of hypertension (Zipdy et al., Ateg. U. Nuregiepziop, 9, 867, 1996). high school

It was established that 1/-1 induces the development of uveitis in rats, which can be inhibited with the help of I/-1 blockers (Htsap et al., ! Oscshiag Rpaptasoi, apa TNeg., 14, 31, 1998). It has been demonstrated that cytokines, (8) including 1-1, TME and zM-C5E, stimulate the proliferation of blasts of acute myelogenous leukemia (Vgyzegid,

And eiKetia Kev. 20, 65, 1996). It was established that II/-1 is important for the development of both inflammatory and allergic contact dermatitis. Sensitization of the surface of the skin can be prevented by injecting a monoclonal antibody to II-1 before applying the allergen to the skin (Miieg et al. At. /. Sopiasi. Oegtai. 7, 177, 1996).

The results obtained in experiments on mice that did not have 1I-1 indicate that this cytokine is of crucial importance in the development of the placenta (Kipdeg et al., Siip. Ehr. RIaptasoi. RpPusio., 25, 141, 1998 ). Different Ge! cytokines, including TME, 1-1, 1/-6, and 1/-8, initiate the acute phase response, which is usually characteristic of the sarcoid, with malaise, myalgia, headaches, cellular hypermetabolism, and numerous endocrine and -- enzymatic responses (Weizei , At. ). Siip. Myig. 62, 813, 1995). After injury or infection with pathogenic organisms, the production of these inflammatory cytokines quickly begins.

Other proinflammatory cytokines are associated with various disease states. The level of II/-8 correlates with the influx of neutrophils to sites of inflammation or damage. Using blocking antibodies to II-8, it was established that 1-8 plays a role in neutrophil-mediated tissue damage during acute inflammation (Nagada et al., MoiIescshiag Meaisipe Todau 2, 482, 1996). Thus, an inhibitor of 1I/-8 production can be used to treat diseases that are mainly mediated by neutrophils, such as stroke and myocardial infarction, resulting from or independent of thrombolytic therapy, heat injury, ;" adult respiratory distress syndrome (RDSD), or chronic organ damage as a result of trauma, acute glomerulonephritis, dermatoses that include components of acute inflammation, acute purulent meningitis or other disorders of the central nervous system, hemodialysis, leukopheresis, transfusion-related syndromes - And granulocytes, and necrotic enterocolitis.

Rhinovirus initiates the production of various pro-inflammatory cytokines, optimally 1-8, which causes symptomatic diseases, such as acute rhinitis (U/ipiNeg, etc., At. .). Laugh! 12, 17, 1998).

Ge) Other diseases, in the development of which II-8 participates, include myocardial ischemia and reperfusion, inflammatory bowel diseases and many other diseases. o Proinflammatory cytokine 1-6 participates in the acute phase of the reaction. And -6 is a growth factor for many

Ge oncological diseases, including multiple myeloma and related dyscrasias of plasma cells (Tgeop et al., Sitepi

Oriope ip NetaiioiIodu 5: 42, 1998). It has been established that it is an important mediator of inflammation in the central nervous system. Increased levels of I/-b have been found in some neurological disorders, including AIDS-related dementia complex, Alzheimer's disease, multiple sclerosis, systemic lupus erythematosus, trauma

Central nervous system and viral and bacterial meningitis (see et al., MoIesshag Meygobioyudu 15: 307, 1997). 1-6 also (F, plays an important role in osteoporosis. In mouse modeling, it was found that it mediates bone resorption and induces osteoclast activity (EgePieg et al., Oemeyurtepi apa Sotragaiime Ittipoi. 21: 487, 1997). Marked discrepancies levels of cytokines, such as levels of II/-b, have been found to differ between osteoclasts in healthy bone and bone from patients with Paget's disease (Miiiz et al., Saisii Tivvce Ipi. 61, 16, 1997). It has been established that many cytokines are involved in the development of cancer cachexia. The severity of the main symptoms of cachexia can be reduced by treatment with antibodies to 1-6 or antagonists of the I/-6 receptor (Zigazztapp et al., Suiyukipz Moi. Teg. 1, 107, 1995). In some infectious diseases, such like flu, II -6 and

IEMa are the main factors both for the formation of symptoms and for the protection of the host (Naudep et al., 9. Siip. 65 Ipmevi. 101, 643, 1998). Overexpression of I-b6 mediates the pathology of many diseases, including multiple myeloma, rheumatoid arthritis, Castleman's disease, psoriasis, and postmenopausal osteoporosis (Zitrzop et al.,

Rhoivip Zsi. 6, 929, 1997). Compounds affecting the production of cytokines, including II-6 and TME, have been shown to be effective in blocking passive cutaneous anaphylaxis in mice (Zspoi2 et al., U. Med. Spet., 41, 1050,

O-M-C5E is another pro-inflammatory cytokine associated with numerous therapeutic diseases. It affects not only the proliferation and differentiation of stem cells, but also regulates some other cells involved in acute and chronic inflammation. Attempts have been made to treat many painful conditions with ZM-SZE, including burn wound healing, skin graft resorption, and mucositis induced by cytostatic agents and radiotherapy (Magzissi, Medisa! Opsoiodu 13: 149, 7/0 1996). ZM-SZBE is also believed to play a role in the replication of the human immunodeficiency virus (HIV) in the cells lining the macrophages in the treatment of AIDS (Stgomje et al., doigpa!oi IeiKosuie Vioidou 62, 41, 1997). Bronchial asthma is characterized by the presence of an inflammatory process in the lungs. Cytokines involved in this include, among others, OM-S5BE (I ee, y). K. SoiI. Rpuzisiapv I op., 32, 56, 1998).

It has been established that interferon 49 (IEM-9) is involved in the development of many diseases. It is associated with increased collagen deposition, which is the main histopathological feature of the disease "graft against the host" (Ragktap, Sit. Orip. Netaiy!., 5, 22, 1998). One of the patients was diagnosed with acute myelogenous leukemia after kidney transplantation. Retrospective analysis of peripheral blood cytokines revealed elevated levels (ZM-C5E and IRM-9. These elevated levels correlate with an increase in the number of leukocytes in peripheral blood (Vygke et al., Geschk. I utrpota. 19, 173, 1995). Development of insulin-dependent diabetes ( type 1) can be correlated with the accumulation in the cells of the pancreatic islet of T-cells that produce IEM-9 (Arishptipiiev et al., 9U. Atsioittip., 11, 73, 1998). IBM-d along with TME, 1-2 and 1/-6 causes the activation of most peripheral T cells before the development of lesions in the central nervous system in diseases such as multiple sclerosis (MS) and the dementia complex associated with AIDS (Mapipo ei ai!., 1998, App

Mesgoi 43, 340). Atherosclerotic lesions cause arterial disease, which can lead to heart and brain infarction. In the areas of such injuries, there are numerous activated immune cells, mainly

T-cells and macrophages. These cells produce large amounts of pro-inflammatory cytokines, such as TME, and)

I--1 st TEM-d. It is assumed that these cytokines are involved in stimulating apoptosis (i.e., programmed cell death) of surrounding vascular smooth muscle cells, which leads to atherosclerotic lesions (Sepd, Neag Mezzeiv Zirri, 12, 76, 1997). In the body of people suffering from allergies, after infection with wasp venom (Mezrsha river), mRNA specific for IRM-9 is produced (Vopau et al., Sip. Ehr. Ittipoi., 109, 342, 1997). It was established that after a delayed-type hypersensitivity reaction, the expression of many cytokines increases, including IPM-d, which indicates the role of IEM-ud in the development of atopic dermatitis (ZgerieimuvKi et al.

Hg. 9U. OegtaiyoI. 137, 195, 1997). For cases of fatal cerebral palsy, histopathological and immunohistopathological studies were conducted. An increased level of IEM-d was found in comparison with other cytokines, which indicates its role in the development of this disease (Odotvzaporeiysy et al., At. i-

U. Ttor. Honey. Boredom. 57, 501, 1997). It has been established that various free radicals are involved in the pathogenesis of various infectious diseases. As a response to infection with certain viruses, the nitric oxide synthesis pathway is activated as a result of the induction of pro-inflammatory cytokines, such as IEM-d (AKaiKe et al., Rgos. os. Ehr. Vioi. Med. 217, 64, 1998). Patients who are chronic carriers of the hepatitis B virus (HBV) may develop cirrhosis and hepatocellular carcinoma. The expression of the viral gene and its replication in transgenic mice infected with HBV can be pla)s suppressed with the help of a post-transcriptional mechanism mediated by IEM-9, TME and 1-2 (Spizaghi et al.,

Zrgipdeg Zetip. Ittiporaiyoi. 17, 261, 1995). IRM-d can selectively inhibit cytokine-induced resorption;" bones This process occurs, presumably, with the participation of nitric oxide (NO), which is an important regulatory agent that affects the recovery of the cyst. MO may participate as a mediator of bone disease for such diseases as

AS rheumatoid arthritis, osteolysis-related tumor and postmenopausal osteoporosis (Emapz et al., U. Vope -I Mipeg Kez. 11, 300, 1996). Studies conducted in mice deficient in the gene demonstrated that I/-12-dependent production of IEM plays a critical role in controlling parasite growth at the initial stage. Although this process does not depend on nitric oxide, the effectiveness of combating chronic infection obviously depends on

Ge) MO (AIehapdeg et al., Ryyov. Tgapv. K. ZBos. opa. V. VioYi. Zsi. 352, 1355, 1997). MO is an important vasodilator, and there is evidence that it plays a role in the development of cardiovascular shock (Kirotsygp et al., Oiv. Mop. 43, 277, 1997). IEM-d is involved in the development of chronic

Intestinal inflammation in diseases such as Crohn's disease and inflammatory bowel disease (IBD) is optimally due to the presence of CO4 lymphocytes, which are thought to belong to the TN1 phenotype (Zapog, AIytepi

Ripagtasoi. Tag. 10, supplement 2, 43, 1996). Elevated levels of serum Id are associated with various atonic diseases, such as bronchial asthma and atopic dermatitis. The level of IEM-ud negatively correlates with the level of Id in the serum, which indicates the role of IEM-d in the development of atopic diseases in patients (Tegatoyo et al., Siip. Ehr.

F) Aiegou 28, 74, 1998). Compounds having the ability to modulate one or more of the above-mentioned inflammatory cytokines can be used to treat diseases mediated by the release of these cytokines. So, for example, UMO bo 98/52558 describes heteroarylurea derivatives that can be used for the treatment of cytokine-mediated diseases. Another class of urea derivatives useful as anti-inflammatory agents is described in MO 99/23091.

Patent 5,162,360 describes (M-substituted aryl)-M'-heterocyclyl-substituted urea derivatives that can be used to treat hypercholesterolemia and atherosclerosis.

The publications cited above suggest that inhibition of cytokine production may have important 65 Value in various disease states. Some protein-based therapeutics are under development or approved for use in certain cases. Protein-based therapeutics are expensive and have certain problems related to bioavailability and stability. Therefore, there is a need to develop novel small molecular weight cytokine inhibitors that have optimal efficacy, pharmacokinetics, and safety profiles.

In light of the above publications, there is a need in the art for compounds that inhibit cytokine production for the treatment of various disease states.

Thus, the present invention was based on the task of obtaining new compounds that inhibit the release of inflammatory cytokines, such as interleukin 1 and tumor necrosis factor.

Another task of the invention is to develop a method of treating inflammatory diseases and pathological conditions, such as chronic inflammatory diseases, using new compounds according to the invention.

Also, the task of the invention is to develop a method of obtaining the above-mentioned new compounds.

According to the first object, the invention offers compounds of formula (1):

M peik Mr. N

IC B) in which

Ag is selected from the group consisting of pyrrole, pyrrolidine, pyrazole, imidazole, oxazole, thiazole, furan and thiophene, while Ag. and can be replaced by one or more groups K., K» or Kz,

Ago means phenyl, naphthyl, quinoline, isoquinoline, tetrahydronaphthyl, tetrahydroquinoline, tetrahydroisoquinoline, benzimidazole, benzofuran, indanyl, indenyl or indole, each of which is optionally substituted with 0-3 groups K", X means a) C5-Cvcycloalkyl or cycloalkenyl, optionally substituted with 0-2 oxo groups or 0-3 branched or unbranched C.-C.alkyl, C.4-C. , pyridine, pyrimidine, pyridinone, dihydropyridinone, maleimide, dihydromaleimide, piperidine, piperazine or pyrazine, each of which is independently optionally substituted with 0-3 substituents selected from the group consisting of branched or unbranched C .-sualalkyl,

C.-C.alkyl group, hydroxy group, nitrile, mono- or di(C.i.C.alkyl)amino group, C.-C.alkyl-C(O)t or C.M. halogen,

U means a bond or a saturated or unsaturated branched or unbranched S.-C. carbon chain, which is not necessarily partially or fully halogenated, while one or more methylene groups are not necessarily He) replaced by O, МН, 5( 0), 5(0)2 or 5, and U is not necessarily independently substituted by 0-2 oxo groups and one or several branched or unbranched C.-C; alkyl groups that can be substituted by one or several halogen atoms, - 2 means a) phenyl, pyridine, pyrimidine, pyridazine, imidazole, furan, thiophene, pyran, which are optionally substituted with 1-3 substituents selected from the group consisting of halogen, C.i-Salkyl, C-Salkyl, hydroxy group, mono - or "di(C.4-Salkyl)amino group, C-Salkyl-Z(O)"t group, COOH group and phenylamino group, while the phenyl ring is optionally substituted with 1-2 substituents selected from halogen, C-Salkyl and C--Svaloxy groups, - c b) tetrahydropyran, tetrahydrofuran, 1,3-dioxolanone, 1,3-dioxanone, 1,4-dioxane, morpholine, thiomorpholine, and thiomorpholine sulfoxide, piperidine, piperidinone, piperazine, tetrahydropyrimidone, cyclohexanone, cyclohexanol, "» pentamethylene sulfide, pentamethylene sulfoxide, pentamethylene sulfone, tetramethylene sulfide, tetramethylene sulfoxide or tetramethylene sulfone, optionally substituted with 1-3 substituents selected from nitrile, S.--Svalkilu, S.i -Salkoxy groups, hydroxy groups, mono- or di(C.--Salkyl)amino-C.4-Salkyl, -and phenylamino-C.4-Salkyl and C4-Salkoxy-C.4-Salkyl, or - c) Si- C-alkyl, secondary or tertiary amine, where the amine nitrogen is covalently bonded to groups selected from the group consisting of C 1-C alkyl, C 1-C alkyl, pyridinyl-C 1-C alkyl, (Ce) imidazolyl-C 4-C alkyl , tetrahydrofuranyl-C-Salkyl, a phenylamino group, where the optional phenyl ring is substituted by 1-2 halogen atoms, C-Salkyloxy groups, hydroxy groups or mono- or di(C1-Salkyl)amino groups, group C-Salkyl-Z (O) t and the phenyl-5(O) t group, in which the phenyl ring is optional (which) is replaced by 1-2 halogen atoms, S.-Svalkoksig groups, hydroxy groups or mono- or di(C.4-Salkyl)amino groups,

K. means a) branched or unbranched C3-Sialkyl, which is optionally partially or completely bicyclo 1-3 phenyl, naphthyl or heterocyclic groups selected from the series to which pyridinyl belongs,

IF) pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, imidazolyl, pyrazolyl, thienyl, furyl, isoxazolyl. (name) isothiazolyl, wherein each such phenyl, naphthyl or heterocycle selected from the series described above in this paragraph is substituted with 0-5 substituents selected from the group consisting of halogen, branched or unbranched or C.i. necessarily partially or fully halogenated, C 3 z -Saccycloalkyl, C 1 -C 2 cycloalkenyl, hydroxy group, nitrile, C 1 -C alkyloxy group, which is optionally partially or fully halogenated, group

MNHC(O) and di(C1-C3)alkylaminocarbonyl, b) C3-Ccycloalkyl selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, bicyclopentanyl, bicyclohexanyl and bicycloheptanyl, each of which is optionally partially or b5 is completely bicyclo with 1-3 C-C alkyl groups, or an analogue of such a cycloalkyl group in which 1-3 ring methylene groups are replaced by groups, independently of each other, selected from the series to which 0, 5 belong,

СНОН, 2-0, 2О5 and МН, c) branched C3-Siralkenyl, which is optionally partially or fully halogenated and optionally substituted with 1-3 substituents selected from branched or unbranched C-Svalkyl, phenyl, naphthyl or heterocyclic groups, wherein each such heterocyclic group is independently selected from the group consisting of pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, imidazolyl, pyrazolyl, thienyl, furyl, isoxazolyl, and isothiazolyl, and each of said phenyl, naphthyl, or heterocyclic groups is substituted with 0 - 5 substituents selected from the group consisting of halogen, branched or unbranched C .-alkyl, which is optionally partially or fully halogenated, cyclopropyl, cyclobutyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, 70 bicyclopentanyl, bicyclohexanyl, bicycloheptanyl, hydroxy group, nitrile, C1-C3-alkyloxy group, which is optionally partially or fully halogenated, the group МНХС(О) and mono- or di(C1-C3)alkylaminocarbonyl, d) C1-C3cycloalkenyl selected from the group, which includes cyclopentenyl, cyclohexenyl, cyclohexadienyl, cycloheptenyl, cycloheptadienyl, bicyclohexenyl and bicycloheptenyl, while each such cycloalkenyl group is optionally substituted with 1-3 C-Salkyl groups, e) or nitrile e) branched or unbranched C.--Sulfoxycarbonyl, branched or unbranched

S.-Salkylaminocarbonyl, branched or unbranched S.-Salkylcarbonylamino-C 1-Salkyl,

Co means a branched or unbranched C-Salkyl, which is optionally partially or fully halogenated, acetyl, aroyl, a branched or unbranched C--C.AlkoxyC.Alkoxy group, which is optionally partially or fully halogenated, halogen, methoxycarbonyl or phenylsulfonyl,

Ez means a) phenyl, naphthyl or heterocyclic group selected from the group consisting of pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, imidazolyl, pyrazolyl, thienyl, furyl, tetrahydrofuryl, isoxazolyl, isothiazolyl, quinolinyl, isoquinolinyl, indolyl, benzimidazolyl, benzofuranyl, benzoxazolyl, benzisoxazolyl, ch benzpyrazolyl, benzothiofuranyl, cinolinyl, pterindinyl, phthalazinyl, naphthylpyridinyl, quinoxalinyl, quinozolinyl, purinyl and indazolyl, while such a phenyl, naphthyl or heterocyclic group is optional and) substituted with 1-5 substituents selected from the group , which include phenyl, naphthyl, heterocycle selected from the series described above in this paragraph, branched or unbranched C 4-Salkyl, which is optionally partially or fully halogenated, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, bicyclopentyl, suso bicyclohexyl , bicycloheptyl, phenyl-C.i-Svalkyl, naphthyl-C--Svalkyl, halogen, hydroxy group, nitrile,

C.i-C alkyloxy group, which can optionally be partially or completely halogenated, phenyloxy group, o naphthyloxy group, heteroaryloxy group, where the heterocyclic fragment is selected from the above described in this paragraph (du row, nitro group, amino group, mono- or di(C 4-C3 )alkylamino group, phenylamino group, naphthylamino group, heterocyclylamino group, where the heterocyclyl fragment is selected from the series described above in this paragraph, group (7 zv МН»С(О), mono- or di(C.i-C3)alkylaminocarbonyl, C.4-Svalkyl -С(О0)-Си-С; alkyl, amino-С--Salkyl, mono- or di(С4-С3)alkylamino-С--Salkyl, group amino-5(О0)", group di(С4и -C3)alkylamino-5(O0)2, /K/-C.4-Svalkyl,

K5-C4-Salkyloxy group, Ka-FK(0)-C.4-Salkyl, group K/-C-Salkyl(Kα)M, carboxy-mono- or di-C-Salkylamino group, b) condensed aryl, selected from the group consisting of benzocyclobutanyl, indanyl, indenyl, dihydronaphthyl, tetrahydronaphthyl, benzocycloheptanyl, and benzocycloheptenyl, or a fused heterocyclyl selected from the group consisting of cyclopentenopyridine, cyclohexanopyridine, cyclopentanopyrimidine, cyclohexanopyrimidine, cyclopentanopyrazine, cyclohexanopyridine, cyclopentanopyridine, , з циклопентанохінолін, циклогексанохінолін, циклопентаноізохінолін, циклогексаноізохінолін, циклопентаноіндол, циклогексаноіндол, циклопентанобензімідазол, циклогексанобензімідазол, циклопентанобензоксазол, циклогексанобензоксазол, циклопентаноїімідазол, циклогексаноїмідазол, циклопентанотіофен і -І циклогексанотіофен, при цьому зазначені конденсоване арильне чи конденсоване гетероциклільне кільце заміщено 0-3 замісниками, вибраними з групи , which includes phenyl, naphthyl and heterocyclyl selected from the group consisting of pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, imidazolyl, pyrazolyl, thienyl, furyl,

He) isoxazolyl and isothiazolyl, branched or unbranched C.-Salkyl, which is not necessarily partially or fully halogenated, halogen, nitrile, C.--Salkoxy group, which is not necessarily partially or completely halogenated, o phenyloxy group, naphthyloxy group, heterocyclyloxy group, in which the heterocyclyl fragment is selected from the described

He is above in this paragraph a group, a nitro group, an amino group, a mono- or di(C.-C3) alkylamino group, a phenylamino group, a naphthylamino group, a heterocyclylamino group in which the heterocyclyl moiety is selected from the group described above in this paragraph, a MNHS(O) group, a mono- or di(C.-C.sub.3)alkylaminocarbonyl, group Ci-C;alkyl-OC(O), branched or unbranched C.i-Salkyl-C(O)-Ci-Slalkyl, amino-Ci-Salkyl, mono- or di(C.--C3)alkylamino-C-alkyl,

K.-C4-Salkyl, Kio-C4-Salkyloxy group, K44-C(0)-C.-Salkyl and group K.42-C4-Salkyl(K 415) M, (F, c) cycloalkyl selected from the group, which include cyclopentyl, cyclohexyl, cycloheptyl, bicyclopentyl, ka bicyclohexyl and bicycloheptyl, while such cycloalkyl is optionally partially or fully halogenated and optionally substituted with 1-3 C-C alkyl groups, in d) C-C7 cycloalkenyl selected from the group , which include cyclopentenyl, cyclohexenyl, cyclohexadienyl, cycloheptenyl, cycloheptadienyl, bicyclohexenyl and bicycloheptenyl, while such a cycloalkenyl group is optionally substituted with 1-3 C-C alkyl groups, e) acetyl, aroyl, alkoxycarbonylalkyl or phenylsulfonyl or e) branched or unbranched C .-Svalkyl, which is optionally partially or fully halogenated, or 65 Ku and K» together may optionally form a condensed phenolic or pyridinyl ring,

Ca ii Keys are each independently selected from the group consisting of hydrogen and a branched or unbranched S. alkyl, which is optionally partially or fully halogenated,

Ku, K5, Kv, K7, Ko, Ko, K44 and Ki" are each independently selected from the group consisting of morpholine, piperidine, piperazine, imidazole and tetrazole, where t is 0, 1 or 2,

MU stands for O or 5 and their pharmaceutically acceptable derivatives.

According to one of the variants of implementation of the invention, compounds of the formula (I) are preferred, in which Ag» means naphthyl, tetrahydronaphthyl, indanyl or indenyl, and MU means 0.

In another embodiment of the invention, among those directly indicated above, those compounds of formula (I) in which

Ag is selected from thiophene and pyrazole,

X means C5-C, cycloalkyl or Ce-C, cycloalkenyl, optionally substituted by 0-2 oxo groups or 0-3 branched or unbranched C.-C. alkyl groups, C.-C. alkoxy groups or

C.i.-C.alkylamino groups, or X represents phenyl, pyridine, tetrahydropyridine, pyrimidine, furan or thiophene, each of which /5 independently of each other is optionally substituted with 0-3 substituents selected from the group consisting of branched or unbranched C.i-Slalkyl, C.i-C,alkoxy group, hydroxy group, nitrile, mono- or di(C.4-Salkyl)amino group, C.-Svalkyl-Z(O) group and halogen,

Ki means branched or unbranched C.-C., alkyl, cyclopropyl or cyclohexyl, optionally partially or fully halogenated and optionally substituted with 1-3 C. and C. alkyl groups,

Kz means branched or unbranched C1-C6 alkyl, phenyl, pyrimidinyl, pyrazolyl or pyridinyl, each of which is optionally substituted as specified in the description of the first object of the invention, alkoxycarbonylalkyl or cyclopropyl or cyclopentyl, each of which is optionally necessarily partially or fully halogenated and optionally substituted, as indicated in the description of the first object of the invention.

According to another embodiment of the invention, among the directly mentioned above, those compounds of the formula (I) are preferred, in which

Ag means pyrazole and i)

X means cyclopentenyl, cyclohexenyl or cycloheptenyl, optionally substituted with an oxo group or 0-3 substituents selected from the group consisting of branched or unbranched C 1 -C 6 alkyl, C 1 -C 6 -alkyl and C 4 -C 6 -alkylamino, or X means phenyl, pyridine, furan, or thiophene, each of which is independently substituted with 0-3 substituents selected from the group consisting of branched or unbranched

C-Alkyl, C--C-Alkoxy group, hydroxy group, nitrile, mono- or di(C-4-C-Alkyl)amino group, group o

C.4-Svalkyl-Z(O) t and halogen. Gee!

According to the following embodiment of the invention, among those directly mentioned above, those compounds of formula (I) are preferred in which --

U means -СНо-, -СНХСН»-, -СНОМН-, -СНОСНоМН- or a bond and 7 means phenyl, imidazole, furan, piperazine, y-tetrahydropyran, morpholine, thiomorpholine, thiomorpholine sulfoxide, piperidine, pyridine, secondary or a tertiary amine, wherein the amine nitrogen is covalently bonded to groups selected from the group consisting of C 4 -C alkyl and

C.S-Calkoxyalkyl, or further means a phenylamino group in which the phenyl ring is optionally substituted with 1-2 substituents selected from halogen, C.I-Salkoxy groups, hydroxy groups and mono- or di(C.S-Calkyl)amino groups, "

TrUPU Ci-Salkyl-(O) t and the phenyl-5(O) t group, in which the phenyl ring is optionally substituted with 1-2 substituents, with c selected from halogen, Ci-Salkyloxy group, hydroxy group and mono- or di(C .4-Szalkyl)amino groups.

According to another variant of the implementation of the invention, among those directly mentioned above, those are the best;" compounds of formula (I), in which

Agi means 5-tert-butylpyrazol-3-yl, where the pyrazole ring can be replaced by a Kz group, while

Ez means -I branched or unbranched C1-C6 alkyl, phenyl, pyrimidinyl, pyrazolyl or pyridinyl, each of which is optionally substituted as indicated in the description of the first object of the invention, alkoxycarbonylalkyl or - cyclopropyl or cyclopentyl, each of which which are optionally substituted, as indicated in the description of the first object according to the invention.

In another embodiment of the invention, among those directly indicated above, those compounds of formula (I) in which X stands for pyridinyl are preferred.

According to the following embodiment of the invention, among the directly mentioned above, those compounds of formula (I) in which pyridinyl is attached to Ag are preferred. in the 3rd position of pyridinyl.

As examples of compounds of formula (I) according to the invention, the following can be mentioned. 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-(4-(4-(morpholin-4-yl)phenyl)naphthalen-1-yl) Urea, 1 -(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-(4-(4--(morpholin-4-ylmethyl)phenyl)naphthalen-1-yl)urea,

F) 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(4-(-2-(morpholin-4-yl)ethyl)phenyl)naphthalene -1-yl|Urea, ka 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4--4-dimethylaminophenyl)naphthalen-1-yl)urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylI|-3-I(4-(3-(morpholin-4-yl)phenyl)naphthalen-1-yl|Urea, in 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylI|-3-I(4-(3-(morpholin-4-ylmethyl)phenyl)naphthalen-1-yl)urea , 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea) , 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(5-morpholin-4-ylmethylpyridin-2-yl)naphthalen-1-yl|urea) , 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(5-morpholin-4-ylmethylfur-2-yl)naphthalen-1-yl|urea) , 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(6b-morpholin-4-ylmethylpyridin-3-yl)naphthalene-1 65-yl|Urea, 1-(b-tert-butyl-2-methyl-2H-pyrazol-3-yl|-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl |)urea,

1-(b-tert-butyl-2-phenyl-2H-pyrazol-3-ylI-3-I4-(4-piperidin-1-ylmethylphenyl)naphthalen-1-yl|Urea, 1-(b-tert-butyl -2-phenyl-2H-pyrazol-3-ylI-3-(4-(4--4-methylpiperazin-1-yl)umethylphenyl)naphthalen-1-yl)urea, 1-(b-tert-butyl-2 -p-tolyl-2H-pyrazol-3-yl|-3-I(4-(3,4-di(morpholin-4-ylmethyl)phenyl)naphthalen-1-yl|Urea, 1-(b-tert- butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(b-pyridin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1-( b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I(4-(6-(1-oxothiomorpholin-4-ylmethyl)pyridin-3-yl) naphthalene-1-yl|urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(6-(1-oxothiomorpholin-4-ylmethyl)pyridine -3-yl)naphthalen-1-yl 7/o /Urea, 1-Ib-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I(4- (b-tetrahydropyran-4-ylmethylpyridin-3-yl)unaphthalin-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-yl) -3-I(4-(6-(1-oxotetrahydrothiophen-3-ylmethyl)pyridin-3-yl)unaphtalin-1-yl|Urea, 1-(b-tert-butyl-2-(b-methylpyridin-3 -il) -2H-pyrazol-3-ylI-3-I(4-(6-(imidazol-1-ylmethyl)pyridin-3-yl)naphthalene -1-yl)urea, 1--2--3-dimethylaminomethylphenyl)- 5-(1-methylcyclohexyl)-2H-pyrazol-3-yl|-3-I4-(b-morpholin-4-ylmethylpyridin -3-yl)unaphthalin-1-yl|Urea, 1-(2-(5- (1-methylcyclohexyl)-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-yl|-3-I4-(b6-morpholin-4-ylmethylpyridin-3-2oip)naphthalen-1-yl |urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4--2-morpholin-4-ylmethylpyrimidin-5-yl)naphthalen-1-yl |Urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI|-3-I4-(3-methoxy-5-(2-morpholine-4 -ylethoxy)phenyl)na phthalin-1-yl|Urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI|-3-I4-(3 -(2-morpholin-4-ylethoxy)phenyl)naphthalene-1-st lysine, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-yl| -3-(4-3--(dimethylamino)phenyl)naphthalen-1-yl|urea, and) 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3 -yl|-3-(4-3-"methylsulfonyl)phenyl)naphthalen-1-yl)urea

NU, methyl ether c zo B-tert-butyl-3-13-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-ylIureido)thiophene-2-carboxylic acid, methylamide 5B-tert-butyl- 3-13-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)ureido)thiophene-2-carboxylic acid, b methyl ether

B-tert-butyl-|-methyl-3-(3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl/ureido)-1H-pyrrole-2-carboxylic acid --

With ACIDS, cha methylamide

B-tert-butyl-1-methyl-3-(3-14--'b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)/ureido)-1H-pyrrole-2-carboxylic acid, 2-acetylamino-N-(5-tert-butyl-3-13-14-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)ureido)hyophen-2-ylmethyl)acetamide, with c 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-(4-(3-morpholin-4-ylcyclohex-1-enyl)naphthalen-1-yl) Isechevin, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylI|-3-I(4-(3-morpholin-4-ylcyclohept-1-enyl)naphthalene-1- 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylI|-3-I(4-(3-(2-morpholin-4-ylethylamino)cyclohex -1-enyl)naphthalene-1-lysine, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylI|-3-I(4-(3-morpholin-4-ylcyclohept -1-enyl)naphthalen-1-yl)urea, -I 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI|-3-I4-( 3-(pyridin-4-ylmethylamino)cyclohex-1-enyl)naphthalen-1-yl|urea, - 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3 -ylI-3-I4-(3--dimethylaminoethylamino)cyclohex-1-enyl)n

Ge) aphthalin-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI|-3-I4-(3-(pyridin- 3-ylmethylamino)cyclohex-1-enyl) o naphthalene-1-yl|urea,

Ge 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(3-"-phenylmethylamino)cyclohex-1-enyl)naphthalene n- 1-yl|Urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(3--2-phenylethylamino)cyclohex-1 -enyl)naphthal di H-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(3-" furan-2-ylmethylamino)cyclohex-1-enyl)na

F) Phthalin-1-yl|urea, ka 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(3-(2- pyridin-2-ylethylamino)cyclohex-1-enyl)naphthalen-1-yl|urea, in 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI- 3-I4-(3-(2-piperidin-1-ylethylamino)cyclohex-1-enyl)unaphtalin-1-yl|Urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl) )-2H-pyrazol-3-ylI-3-I4-(3-(2-imidazol-4-ylethylamino)cyclohex-1-ene l)naphthalen-1-yl|urea, 1-(b-tert-butyl- 2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI|-3-I4-(3-(pyridin-2-ylmethylamino)cyclohex-1-enyl) 65 naphthalene-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI|-3-I4-(3-(2-(4-methoxyphenyl)ethylamino)cyclohex-1 -

enyl)naphthalen-1-yl|Urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylI|-3-(4--4-morpholin-4-ylmethyl-3- oxocyclohex-1-enyl)naphthalen-1-yl urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(4-(1-oxotetrahydrothiophene- 3-ylmethyl)-3-oxocyclohex-1-en yl)unanaphthalen-1-yl|Urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4 -(4-(1-oxothiomorpholin-4-ylmethyl)-3-oxocyclohex-1-enyl)na phthalin-1-yl|Urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol- 3-yl|-3-(4-(4-methylpiperazin-1-ylmethyl)-3-oxocyclohex-1-enyl)naphthal 70. In-1-yl|urea, 1-(b-tert-butyl-2- (b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I(4-6-oxo-1-(tetrahydropyran-4-ylmethyl)-1,2,3, b-tetrahydropyridin-4- Ilinanaphthalen-1-yl|Urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI|-3-I4-(2-oxo-1-pyridine -4-ylmethylpiperidin-4-yl)na phthalin-1-yl|Urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylI|-3-(4-(6- oxo-1-pyridin-4-yl-1,2,3,6-tetrahydropyridin-4-yl)unaphtalin-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3 -il)- 2H-pyrazol-3-ylI|-3-I(4-(b-oxo-1-pyridin-4-yl-1,2,3,6-tetrahydropyridin-4-yl)naphthalen-1-yl|urea , methyl ether

B-tert-butyl-3-13-I4-(6-oxo-1-pyridin-4-yl-1,2,3,6-tetrahydropyridin-4-yl)naphthalen-1-ylureido)thiophene-2-carbo new acid, methyl ether

B-tert-butyl-1-methyl-3-(3-I4-(b-oxo-1-pyridin-4-yl-1,2,3,6-tetrahydropyridin-4-yl)naphthalen-1-yl) ureido)pyrrole-2-carboxylic acid, methyl amide

B-tert-butyl-1-methyl-3-(3-I4-(b-oxo-1-pyridin-4-yl-1,2,3,6-tetrahydropyridin-4-yl)naphthalen-1-yl) ureido) pyrrole- and) 2-carboxylic acid, methyl ether

B-tert-butyl-3-13-14-(3-morpholin-4-ylcyclohex-1-enyl)naphthalene-1-ylureido)thiophene-2-carboxylic acid, c zo methyl ether

B-tert-butyl-1-methyl-3-13-14--"3-morpholin-4-ylcyclohex-1-enyl)naphthalene-1-yl)ureido)pyrrole-2-carboxylic acid and o methylamide Ge!

B-tert-butyl-1-methyl-3-13-I4-(3-morpholin-4-ylcyclohex-1-enyl)naphthalene-1-ylureido)pyrrole-2-carboxylic acid, as well as their pharmaceutically acceptable derivatives. --

According to another embodiment of the invention, it also offers the following compounds of formula (1): 4-(morpholin-4-ylmethyl)phenyl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-( 4-(2-(morpholin-4-yl)ethyl)phenyl)naphthalen-1-yl|Urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3- I(4-(3-(morpholin-4-ylmethyl)phenyl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylI|-3- (4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, « 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3 -(4--5-morpholin-4-ylmethylpyridin-2-yl)naphthalen-1-yl|urea, with c 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl| -3-(4--5-morpholin-4-ylmethylfur-2-yl)naphthalen-1-yl|)urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)- 2H-pyrazol-3-ylI-3-I4-(6b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1?-yl|urea, 1-(b-tert-butyl-2-methyl-2H- pyrazol-3-yl|-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, as well as their pharmaceutical morning derivatives. -I The second object of the invention is compounds of the formula (Ia): shk UM with water cyc ho with 70 Pa)

Co) in which

Ag. means pyrrole, pyrrolidine, pyrazole, imidazole, oxazole, thiazole, furan and thiophene, while Ag. optionally substituted by one or more groups K., K» or Kz,

Ago means phenyl, naphthyl, quinoline, isoquinoline, tetrahydronaphthyl, tetrahydroquinoline, o tetrahydroisoquinoline, benzimidazole, benzofuran, indanyl, indenyl and indole, each of which is optionally substituted with 0-3 Co groups, ime) X means - C5-Cvcycloalkyl or cycloalkenyl , optionally substituted by 1-2 oxo groups or 1-3 C --C alkyl, because C-C-Alkoxy- or C-C-Alkylamino chains, each of which is branched or unbranched, - phenyl, furanyl, thienyl , pyrrolyl, pyrazolyl, imidazolyl, pyridinyl, tetrahydropyridinyl, pyrimidinyl, pyridinonyl, dihydropyridinonyl, maleimidyl, dihydromaleimidyl, piperidinyl, benzimidazole,

ZH-imidazo|4,5-bpyridine, piperazinyl, pyridazinyl or pyrazinyl, each of which is independently optionally substituted with 1-3 substituents selected from the group consisting of C 4-Slalkyl, C 1-C 6 , hydroxy, hydroxy, 65 nitrile, amino group, mono- or di(C.4-Salkyl)amino group, mono- or di(C.4-Salkylamino)carbonyl, group MNHS(O), group C.i-Salkyl-Z(O) dt and halogen,

M means a bond or a saturated or unsaturated, branched or unbranched C 4-C,-carbon chain, optionally partially or fully halogenated, with one or more C atoms optionally replaced by O, M or 5(O )»t, and M in each case is independently optionally substituted by 1-2 oxo groups, nitrile, phenyl, hydroxy group or one or more C.-C., alkyl groups, optionally substituted by one or more halogen atoms, 2 means aryl , indanyl, heteroaryl selected from benzimidazolyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, furanyl, thienyl and pyranyl, heterocycle, 70 selected from piperazinyl, tetrahydropyrimidonyl, cyclohexanonyl, cyclohexanolyl, 2-oxa- or 2 -thia-5-azabicyclo|2.2.1|heptanyl, pentamethylenesulfidyl, pentamethylenesulfoxidyl, pentamethylenesulfonyl, tetramethylenesulfidyl, tetramethylenesulfoxidyl or tetramethylenesulfonyl, tetrahydropyranyl, tetrahydrofuranyl, 1,3Z-dioxole nonyl, 1,3-dioxanonyl, 1,4-dioxanyl, morpholino, thiomorpholino, thiomorpholinosulfoxidyl, thiomorpholinosulfonyl, piperidinyl, piperidinonyl, pyrrolidinyl, and dioxolanyl, while each of the above 72 groups is optionally substituted with 1-3 substituents selected from groups that include halogen, C 4-Salkyl, C-Salkyl, C.i4-Salkoxy-C.i-Salkyl, C.i-Salkoxycarbonyl, aroyl, heteroaroyl, heterocycleCi-Szacyl, where heteroaryl and heterocycle have the above in this paragraph meaning, (F 1-Szacyl, oxo group, hydroxy group, pyridinyl-C. the ring is optionally substituted with 1-2 substituents selected from the group consisting of a halogen, a C/S-alkyloxy group, a hydroxy group and a mono- or di(C.i-Salkyl)uamino group, an amino-B(O)»l group, a C group .-Svalkyl-B(O)»t and the group phenyl-B(O),t, where the phenyl ring is optionally replaced by 1-2 halogen atoms, C 4-C alkyl, hydroxy, or mono- or di(C 1 -C 1 alkyl)amino groups, C or 7 is optionally substituted with 1-3 substituents selected from the group consisting of an amino group, an aminocarbonyl, and an amino-C 4 -C 1 alkyl, where the M atom independently optionally mono- or disubstituted amino with 4-Salkyl, C4-Salkyl, i) aryl-Salkyl, C-Salkyl, C-Salkyl, C-Salkyl, aroyl, C-Salkyl, group

C.-Salkyl-B(O)»t- or the group aryl-Salkyl-(O)»1-, while each of the above alkyls and aryls attached to the amino group is optionally substituted with 1-2 substituents selected from the group , which include halogen, c zo C1-Salkyl, C1-Salkyl, a hydroxy group and a mono- or di(C1-Salkyl)amino group, or 7 is optionally substituted with 1-3 substituents selected from the group consisting of aryl , heterocycle or heteroaryl, as defined above in this paragraph, while each of the given substituents in turn is optionally substituted by halogen, (33

C.-Salkyl or C.-Salkyl, or 7 means a hydroxy group, hydroxyCi-Salkyl, halogen, nitrile, amino group, where the M atom is independently (87 optionally mMono- or disubstituted by Cbo4-Salkyl, amino/--Salkyl, arylCo -Szalkilom, eat-

C4-SalkoxyC.i-Salkyl, C.i-Salkoxy group, aroyl, C--Szacyl, group C.-Salkyl-3(O)"-, group arylCo-Salkyl-3(O) t-, nitrileC-C; alkyl or C.i-SzalkoxyS.-Szalkyl, while each of the above alkyls and aryls attached to the amino group is optionally substituted by 1-2 substituents selected from the group, which includes halogen, C 4-Swalkyl, C.-- C1-C1-C3-C3 alkyl) amino group, C1-C1-C3-C3 alkyl, C1-C1-C3-C3 alkyl heteroaryl, C1-C3-C3 alkyl heteroaryl, C3-C3 alkyl heteroaryl or C3-C3 alkyl heterocycle, where heteroaryl and /7-C3 heterocycle have the meanings given above in this paragraph , . or 7 means a branched or unbranched S.-Svalkyl, S.--Svaloxy group, S.--Szacylamino group, and? nitrileC.-C.alkyl, C4i-Salkyl-Z(O)»t and phenyl-(O)»4, where the phenyl ring is optionally substituted by 1-2 halogen atoms, C-Salkyloxy groups, hydroxy groups or mono- or di( C4-Salkyl) amino groups,

K. means -And a) branched or unbranched C.-Siralalkyl, which is optionally partially or fully halogenated and optionally substituted by 1-3 substituents selected from the group, which includes phenyl, naphthyl and heterocyclic groups, - selected from the series , which includes pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, imidazolyl,

Ge) pyrazolyl, thienyl, furyl, isoxazolyl and isothiazolyl, while each of the indicated phenyl, naphthyl or heterocyclic groups selected from the above series is substituted with 0-5 substituents selected from the group where o includes halogen, branched or unbranched C 1 -Svalkil, which is optional in part or in full

He is halogenated, C3-Cacycloalkyl, C5-Cacycloalkenyl, hydroxy group, nitrile, C--C6alkyloxy group, optionally partially or fully halogenated, MNHC(O) group and di(C..3)alkylaminocarbonyl, b) C3-Ccycloalkyl, selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl,

B cyclohexyl, bicyclopentyl, bicyclohexyl and bicycloheptyl, each of which is optionally partially or fully halogenated and optionally substituted with 1-3 C.i.sub.6 alkyl groups, or an analogue of a similar cycloalkyl group,

Ф) in which 1-3 ring methylene groups are replaced by groups, independently of each other, selected from the series to which 0, 5, СНОН, 2-0, 20-51 МН belong, c) branched C3-C-ralkenyl, which is optionally partially or fully halogenated and optionally substituted with 1-3 substituents selected from the group consisting of branched or unbranched C 1 -alkyl, phenyl, naphthyl and heterocyclic groups, wherein each such heterocyclic group is independently selected from the group consisting of which includes pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, imidazolyl, pyrazolyl, thienyl, furyl, isoxazolyl, and isothiazolyl, and each such phenyl, naphthyl, or heterocyclic group is substituted with 0-5 substituents selected from the group consisting of halogen, branched or unbranched C /-C alkyl, which is optionally partially or fully halogenated, cyclopropyl, cyclobutyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, bicyclopentanyl, bicyclohexanyl, bicycloheptanyl, hydroxy group, nitrile, C.-S-alkyloxy group,

optionally partially or fully halogenated, MNHS(O) group and mono- or di(C.-C.sub.3)alkylaminocarbonyl, d) C.sub.7-C.cycloalkenyl selected from the group consisting of cyclopentenyl, cyclohexenyl, cyclohexadienyl, cycloheptenyl, cycloheptadienyl, bicyclohexenyl and bicycloheptenyl, while each such cycloalkenyl group is optionally substituted by 1-3 C. and C. alkyl groups, e) nitrile or e) branched or unbranched C.--Salkoxycarbonyl, branched or unbranched

S.-Salkylaminocarbonyl, branched or unbranched S.-Salkylcarbonylamino-C 1-Salkyl,

Co means a branched or unbranched S.-Svalkyl, which is optionally partially or fully halogenated and optionally substituted with a nitrile, or K" means acetyl, aroyl, branched or unbranched

C.-C.AlkoxyAlkoxy group, which is not necessarily partially or fully halogenated, halogen, methoxycarbonyl or phenylsulfonyl,

Ez means a) phenyl, naphthyl or heterocyclic group selected from the group consisting of pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, imidazolyl, pyrazolyl, thienyl, furyl, tetrahydrofuryl, isoxazolyl, isothiazolyl, quinolinyl, isoquinolinyl, indolyl, benzimidazolyl, benzofuranyl, benzoxazolyl, benzisoxazolyl, benzpyrazolyl, benzothiofuranyl, cinnolinyl, pterindinyl, phthalazinyl, naphthylpyridinyl, quinoxalinyl, quinazolinyl, purinyl and indazolyl, wherein such phenyl, naphthyl or heterocyclic group is optionally substituted with 1-5 substituents selected from the group consisting of phenyl, naphthyl, heterocycle selected from the series described above in this paragraph, branched or unbranched C /-C alkyl, which is optionally partially or fully halogenated, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, bicyclopentyl, bicyclohexyl, bicycloheptyl, phenyl -S.--Svalkyl, naphthyl-S.i-Sralkyl, halogen, hydroxy group, oxo group, nitrile,

C.-SalkoxyC.alkoxy group, which is not necessarily partially or fully halogenated, C 4-SalkoxyC.-Svalkyl,

C.-Czthioalkyl, C.i-CzthioalkylC--Salkyl, phenyloxy group, naphthyloxy group, heteroaryloxy group, in which the heterocyclic fragment is selected from the series described above in this paragraph, nitro group, amino group, mono- or di(C1-C3)alkylamino group, phenylamino group, naphthylamino group, heterocyclylamino group, in which the heterocyclyl i) fragment is selected from the series described above in this paragraph, the group МН 25С(О), mono- or di(С41-С3) alkylaminocarbonyl, S.-Svalkyl-С(О0)-С .-Sualkyl, amino-C.--Sualkyl, mMono- or di(C4-C3)alkylamino-C -Sualkyl, group amino-5(O)", group di(Ci-C3)alkylamino-z(O)2 , K/-Si-Svalkil, su

RB-Ci1-Svaloxy group, Ke-FK(0)-C.4-Svalkyl, group K,-C.4-Svalkyl(Ka)M and carboxy-mono- or di(C.4-C3)alkylamino group, o b ) fused oaryl selected from the group consisting of benzocyclobutanyl, indanyl, |indenyl, and dihydronaphthyl. tetrahydronaphthyl, benzocycloheptanyl and benzocycloheptenyl, or fused heterocyclyl selected from the group consisting of cyclopentenopyridine, cyclohexanopyridine, cyclopentanopyrimidine, --

Зз5 циклогексанопіримідин, циклопентанопіразин, циклогексанопіразин, циклопентанопіридазин, р циклогексанопіридазин, циклопентанохінолін, циклогексанохінолін, циклопентаноізохінолін, циклогексаноізохінолін, циклопентаноіндол, циклогексаноіндол, циклопентанобензімідазол, циклогексанобензімідазол, циклопентанобензоксазол, циклогексанобензоксазол, циклопентаноімідазол, циклогексаноїмідазол, циклопентанотіофен і циклогексанотіофен, при цьому зазначені конденсоване арильне чи «

The fused heterocyclyl ring is substituted with 0-3 substituents independently selected from the group consisting of phenyl, naphthyl and heterocyclyl selected from the group consisting of pyridinyl, pyrimidinyl, pyrazinyl, . pyridazinyl, pyrrolyl, imidazolyl, pyrazolyl, thienyl, furyl, isoxazolyl and isothiazolyl, branched or unbranched S.--Svalkyl, which is not necessarily partially or fully halogenated, halogen, nitrile,

Ci-SalkoxySlalkoxy group, which is optionally partially or fully halogenated, phenyloxy group, naphthyloxy group, heterocyclyloxy group, in which the heterocyclyl fragment is selected from the series described above, -I nitro group, amino group, mono- or di(C.1-C3)alkylamino group, phenylamino group, naphthylamino group, heterocyclylamino group, in which the heterocyclyl fragment is selected from the series described above, group MH 5C(O), - mono- or di(C.4-C3)alkylaminocarbonyl, group C.-C;, alkyl- 0OC(O), branched or unbranched

Ge) C.-Salkyl-C(0)-C.-C,alkyl, amino-Ci-Salkyl, mono- or di(Ci-C3)alkylamino-C.i-Salkyl, Ke-C4-Salkyl, 0 Clo -Ci1-Svalkoxy group, K441-C(0)-C4-Svalkyl and the group K42-C4-Svalkyl(K c) M, o c) cycloalkyl selected from the group which includes cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl,

From cycloheptyl, bicyclopentyl, bicyclohexyl and bicycloheptyl, while such cycloalkyl is optionally partially or fully halogenated and optionally substituted with 1-3 C.i.sub.6 alkyl groups, d) C.sub.7-cycloalkenyl selected from the group consisting of cyclopentenyl, cyclohexenyl , cyclohexadienyl, dv Cycloheptenyl, cycloheptadienyl, bicyclohexenyl and bicycloheptenyl, while such a cycloalkenyl group is optionally substituted with 1-3 C-C alkyl groups,

f) e) acetyl, aroyl, C--Svaloxycarbonyl 4-Svalky or phenylsulfonyl or ka f) branched or unbranched C.-Svalky, which is optionally partially or fully halogenated, or

Ku and Ke" together optionally form a fused phenyl or pyridinyl ring, 60 Ka and Kis are each independently selected from the group consisting of hydrogen and branched or unbranched S.-Sualalkyl, which is optionally partially or fully halogenated,

Ku, K5, Kv, K7, Ka, Ko, Ku4 and Ki" each independently selected from the group consisting of morpholine, piperidine, piperazine, imidazole and tetrazole, t means 0, 1 or 2, 65 M means O or 5, while X is directly attached to one or two groups -Y-7,

and their pharmaceutically acceptable derivatives.

According to one of the variants of implementation of the invention, compounds of the formula (Ia), in which Ago means naphthyl, tetrahydronaphthyl, indanyl or indenyl, and MU means O

In another embodiment of the invention, the compounds of formula (Ia) in which

Ag means thiophene or pyrazole, each of which is independently substituted by 1-3 groups K., K» or Kz,

X means - C5B-Sucycloalkyl or cycloalkenyl, optionally substituted by 1-2 oxo groups or 1-3 C 4-C;.alkyl, 70. C41-Slalkoxy- or C-C.alkylamino chains, each of which is branched or unbranched, - phenyl, indanyl, furanyl, thienyl, imidazolyl, pyridinyl, pyrazinyl, tetrahydropyridinyl, pyrimidinyl, pyridinonyl, piperidinyl, benzimidazole, or piperazinyl, each of which is independently optionally substituted with 1-3 substituents selected from the group consisting of C 4 -Alkyl, C.-C.;. . . . . . . . . . . . . . . . . . . . . . /5 Group Si-Svalkyl-5(O) t and halogen,

M means a bond or saturated or unsaturated, branched or unbranched C 4-C; carbon chain, which is optionally partially or fully halogenated, with one or more C atoms optionally replaced by O or M, and M in each case independently optionally substituted by 1-2 oxo groups, nitrile, phenyl, hydroxy or by one or more C.-C., alkyl groups optionally substituted by one or more halogen atoms, 2 means - phenyl, heteroaryl selected from pyridinyl, imidazolyl, furanyl and thienyl, heterocycle selected from piperazinyl, /2-oxa- 5-azabicyclo|2.2.1)heptanyl, pentamethylene sulfidyl, pentamethylene sulfoxidyl, pentamethylene sulfonyl, tetrahydrofuranyl, morpholino group, thiomorpholino group, and piperidinyl, while each of the above 72 groups is optionally substituted with 1-3 substituents selected from the group that includes halogen , C 4-Swalkyl, C--Swalkoxy group, C.i4-Szalkoxy-S.i-Szalkyl, S.i-Swalkoxycarbonyl, i) aroyl, morpholinocarbonyl, S.--Szatyl, oxo group, hydroxy group, pyridinyl-C-- Szalkyl, imidazolyl-S.--Szalkyl, tet rahydrofuranil-C.-Salkyl, nitrile-C.-Salkyl, nitrile, carboxy group, phenyl, where the phenyl ring is optionally substituted with 1-2 halogen atoms, C-Salkyloxy groups, hydroxy groups or mono- or ) amino groups, group amino-(O) t; the C.i-Svalkyl-5(O)n group and the phenyl-B(O)u group, where the phenyl ring is optionally substituted with 1-2 halogen atoms, C 4-Svaloxy groups, hydroxy groups or mono- or di(C. 4-Szalkyl)amino groups, Ge! or 7 is optionally substituted with 1-3 substituents selected from the group consisting of an amino group, an aminocarbonyl group, and an amino-C.--C-alkyl, where the M-atom in each case is independently optionally mono- or disubstituted -- with amino/- -Svalkilom, S.-Szalkilom, aryl-Szalkilom, S.-Svalkoxy--Szalkilom, S.i-Svalkoxy group, aroyl, Kk.

C.i-Zacyl, C.-Salkyl-Z(O)2t- group or arylCo-Szalkyl-Z(O)»n- group, while each of the indicated alkyls and aryls attached to the amino group is optionally substituted by 1 -2 substituents selected from the group consisting of halogen, C4-Salkyl, and C-Salkyloxy, or 7 optionally substituted with 1-3 aryl, heterocyclic, or heteroaryl groups as defined above in this paragraph, each of which in turn, optionally substituted with a halogen, Si-Svalkyl or 7) with a Si-Svalkoxy group, . or 7 means a hydroxy group, hydroxyC-C alkyl, halogen, nitrile, amino group, where the M atom in each case and is independently optionally mono- or disubstituted by aroyl. (Fi. 14-Szatsilom, S.-Svalkilom,

C-SalkoxyC.1-Salkyl, pyridinylC--Salkyl, tetrahydrofuranyl.--Salkyl, nitrileC.--Slalkyl or phenyl, while the phenyl ring is optionally substituted with 1-2 substituents selected from the group, which include -I halogen, C.-Salkyloxy group, hydroxy group and mono- or di(C.-Salkyl)amino group, or 7 means branched or unbranched C.-Salkyl, C.4i--Salkyloxy group or nitrileC.-C.sub.alkyl, - K. means co - branched or unbranched, optionally partially or fully halogenated C.-Alalkyl, - cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, which are optionally partially or completely halogenated and optionally substituted with 1-3 C and -Alalkyl groups, or an analogue of such cycloalkyl group, u

In which 1-3 ring methylene groups are replaced by groups independently selected from О, 5 and МН, - branched C3-C.oalkenyl, which is optionally partially or fully halogenated and optionally substituted by 1-3 branched or unbranched C.-Alalkyl groups, - cyclopentenyl and cyclohexenyl, optionally substituted with 1-3 C.-Alalkyl groups,

Ko means branched or unbranched S.-Svalkil, which is not necessarily partially or completely

Ф) halogenated and optionally substituted by a nitrile, and Kz means - a phenyl or heterocyclic group selected from the series that includes pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl and pyrazolyl, while such a phenyl or heterocyclic group is optionally substituted by 1- 5 substituents selected from the group consisting of phenyl, heterocycle selected from the series described above in this paragraph, branched or unbranched C . . Svalkil, S.-Szthioalkil,

C-C3thioalkylC-C3alkyl, phenyloxy group, naphthyloxy group, heteroaryloxy group in which the heterocyclic fragment is selected from the series described above in this paragraph, nitro group, amino group, mono- or di(C1-C3)alkylamino group, phenylamino group, naphthylamino group, heterocyclylamino group in which heterocyclyl the fragment is selected from the series described above in this paragraph, group MH 2C(O0), mono- or di(C41-C3)alkylaminocarbonyl, C.-Salkyl-C(O0)-C.-Salkyl, amino-C.4-Salkyl , mMono- or di(C4-C3)alkylamino-C -Svalkyl, amino-5(O) group", di(C.--C3)alkylamino-5(O)" group, C.-C.4-Svalkyl ,

K5-C4-Svalkoxy group, Ke-FK(0)-C.4-Svalkyl, group K,-C.4-Svalkyl(Ka)M and carboxy-mono- or di(C4-Cv)-alkylamino group, - condensed aryl , selected from the group consisting of benzocyclobutanyl, indanyl, indenyl, wherein such 7/0 Condensed aryl is substituted with 0-3 substituents independently selected from the group consisting of phenyl, naphthyl and heterocyclyl, selected from pyridinyl, pyrimidinyl, pyrazinyl . , phenyloxy group, naphthyloxy group, heterocyclyloxy group, in which the heterocyclyl fragment is selected from the group described above in this paragraph, nitro group, amino group, mono- or di(C.1-C3)alkylamino group, phenylamino group, naphthylamino group, heterocyclylamino group, in which the heterocyclyl fragment is selected from the described groups above in this paragraph, the MNHS(O) group, and mono- or di(C41-C3)alkylaminocarbonyl, the C1-C13alkyl-OC(O) group, branched or unbranched

C.-Salkyl-C(0)-C.-C,alkyl, amino-C-Salkyl, mono- or di(Ci-C3)alkylamino-C.i-Salkyl, Coe-C4-Salkyl, 20. Rlo- C1-Salkyloxy group, K414-C(0)-C-Salkyl and group K/2-C4-Salkyl(K 3) M, - cycloalkyl selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, while such cycloalkyl is not necessarily partially or fully halogenated and optionally substituted with 1-3 C.-Salkyl groups, - C-Salkyloxycarbonyl 1-Salkyl, or c

Ku and KE" together optionally form a condensed phenyl or pyridinyl ring,

Ka ii Kiz are each independently selected from the group consisting of hydrogen and branched or i) unbranched S.-Slalkyl, which is optionally partially or fully halogenated, and

Ku, K5, Kv, K7, Ka, Ko, Ku4, and Ki" are each independently selected from the group consisting of morpholine, piperidine, piperazine, imidazole, and tetrazole, wherein X is directly attached to one -Y-7 group. с зо In the next embodiment of the invention, the compounds of the formula (Ia) in which o

Agi means pyrazole, Ge!

X means - cyclopentenyl, cyclohexenyl, cycloheptenyl, optionally substituted by an oxo group or (1-3 -- with C1-Slalkyl, C-Slalkoxy- or C.-Slalkylamino chains, each of which is branched or unbranched, and - phenyl, furanyl . heteroaryl selected from pyridinyl, imidazolyl and furanyl, heterocycle selected from 3 ptsh) with 2-oxa-5-azabicyclo|2.2.1)heptanyl, pentamethylene sulfidyl, pentamethylene sulfoxidyl, . pentamethylenesulfonyl, tetrahydrofuranyl, tetrahydropyranyl, piperazinyl, morpholino group, and? thiomorpholino group, thiomorpholinosulfoxide and piperidinyl, while each of the above 72 groups is optionally substituted with 1-3 substituents selected from the group consisting of halogen, C 1-Salkyl, C-Salkyl, C4-Salkoxy-C-Salkyl, C .i-Svaloxycarbonyl, -I aroyl, morpholinocarbonyl, C.--Szacyl, oxo group, hydroxy group, pyridinyl-C. nitrile, carboxy group, phenyl, where the phenyl ring is optionally substituted with 1-2 halogen atoms, C --Sulfoxy groups, hydroxy groups or mono- or

Ge) di(C.4-Salkyl)amino groups, the amino-5(O) group, the C--Salkyl-Z(O) group and the phenyl-Z(O)» group, where the phenyl ring is optionally substituted 1-2 halogen atoms, C-C-alkyloxy groups, hydroxy groups or mono- or di(C.4-Salkyl)amino groups,

He or 7 is optionally substituted by 1-3 amino groups, aminocarbonyl groups or amino-C/-Salkyl groups, where the M atom is optionally mono- or disubstituted by amino 4-Salkyl in each case,

C-C alkyl, aryl-C alkyl, C-C alkyl, C alkyl, C alkyl, aroyl, C alkyl, two C alkyl groups, pyridinyl C alkyl, tetrahydrofuranylCo-C alkyl or the group arylCo-Szalkyl-Z(O)1-, while each of the above alkyls and aryls attached to the amino group,

Ф) optionally substituted by 1-2 halogen atoms, C-Salkyl groups or C-Salkyloxy groups, ka or 7 means a hydroxy group, hydroxyC.-Szalkyl, halogen, nitrile, amino group, where the M atom is optional in each case independently Mmono- or disubstituted by S.-Svalky, pyridinyl-Szalky, because tetrahydrofuranyl-C zalky, S.i-Svalkoxy4-Szalky, S.-Szacyl, nitriles--S. alkyl or phenyl, while the phenyl ring is optionally substituted by 1-2 halogen atoms, C -Salkyloxy groups, hydroxy groups or mono- or di(C.Salkyl)amino groups, or 7 means branched or unbranched C.Salkyl, C4i-- Svaloxy group or nitrile C.-C.sub.6 alkyl,

K. means 65 - branched or unbranched C-alkyl, which is optionally partially or fully halogenated, - cyclopropyl, cyclobutyl, cyclopentanyl, cyclohexanyl and cycloheptanyl, optionally partially or fully halogenated and optionally substituted by 1-3 C. - By alkyl groups, or an analogue of such a cycloalkyl group, in which 1-3 ring methylene groups are replaced by groups independently selected from О, 5 and МН, - branched C5-Sioralkenyl, which is optionally partially or fully halogenated and optionally substituted 1-3 branched or unbranched C.--C alkyl groups, - cyclopentenyl and cyclohexenyl, optionally substituted with 1-3 C.-C alkyl groups,

Co means a branched or unbranched S.-Svalkyl, which is optionally partially or fully halogenated and optionally substituted with a nitrile,

Ez means 70 - phenyl or heterocyclic group selected from the group consisting of pyridinyl, pyrimidinyl, pyridazinyl and pyrazolyl, while such phenyl or heterocyclic group is optionally substituted with 1-5 substituents selected from the group consisting of phenyl, heterocyclic , selected from the group described above in this paragraph, branched or unbranched C.-Salkyl, which is optionally partially or fully halogenated, phenyl-C.-Salkyl, halogen, hydroxy group, oxo group, nitrile, C.i.S.-SalkoxySlalkoxy group, optionally /5 partially or fully halogenated, C.-C3-thioalkyl, C.4-C3-thioalkylCi-Salkyl, amino group, mono- or di(C41-C3)alkylamino group, MNHS(O) group or mono- or di(C.- C3)alkylaminocarbonyl, - C1-Salkyloxycarbonyl 1-Salkyl, or Kz means cyclopropyl or cyclopentyl, each of which is optionally partially or fully halogenated and optionally substituted with 1-3 C1-Salkyl groups, or

Ku and Ke" together optionally form a condensed phenyl or pyridinyl ring.

According to the next embodiment of the invention, the compounds of formula (Ia) in which

M stands for -СНо-, -ОО-(СНо)оз-, -СНоСН»о-, -СНОМН-, -СНо.СнНо-МН-, МН-СНСН»-, -СН.-МН-СНо-, -- МН-, -МН-С(О0)-, -С(0)-, -СН(ОН)-, -СН(СНоСН»)- or bond, with

X means - cyclohexenyl, optionally substituted by an oxo group or 1-3 C -C/lalkyl, C.-C, alkoxy- or i)

C.-C. alkylamino chains, each of which is branched or unbranched, - phenyl, pyridinyl, pyrazinyl, piperidinyl or pyrimidinyl, each of which is optionally independently substituted with 1-3 substituents selected from the group which includes C.4-Soalkyl, Ci-So-Alkoxy group, hydroxy group and halogen, c zo 2 means - phenyl, heteroaryl selected from pyridinyl, imidazolyl and furanyl, heterocycle selected from o 2-oxa-5-azabicyclo|2.2.1)heptanyl, pentamethylenesulfidyl, pentamethylenesulfoxidyl, (33 pentamethylenesulfonyl, tetrahydrofuranyl, tetrahydropyranyl, piperazinyl, morpholino group, thiomorpholino group, thiomorpholinosulfoxide and piperidinyl, -- while each of the above 7 groups is optionally substituted with 1-3 substituents, selected (p groups, which include halogen, C 4-Svalkyl, C--Swalkoxy group, C.i4-Szalkoxy-S.i-Szalkyl, S.i-Swalkoxycarbonyl, aroyl, morpholinocarbonyl, S.--Szatyl, oxo group, hydroxy group, pyridinyl-S.--Szalkyl, imidazolyl-S.i -Szalkyl, tetrahydrofuranil-S.-Szalkyl, nit ryl-C.-Salkyl, nitrile, carboxy group, phenyl, where the phenyl ring is optionally substituted with 1-2 halogen atoms, C --Salkyloxy groups, hydroxy groups or mono- or "

BY(C1-Szalkyl)amino groups, the group amino-z(O) t"; the group C.i-Svalkyl-5(O) t and the group phenyl-B(O) y, where the phenyl ring Che) c is optionally substituted with 1-2 halogen atoms, C --Svalkoxy groups, hydroxy groups or mono- or di( C.4-Szalkyl)amino groups, ;" or 7 is optionally substituted by 1-3 amino groups or aminocarbonyl groups, where the M-atom is optionally in each case independently mono- or disubstituted by amino--Salkyl, C.i-Salkyl, aryl-Salkyl, 45. C1-Szalkoxy- -S-alkyl, C-S-alkyloxy group, aroyl, C--Szacyl, group C-S-alkyl-Z(O)t- or group -I aryl-S-alkyl-Z(O)»y1-, while each of the above alkyls and aryls , attached to an amino group, optionally substituted by 1-2 halogen atoms, C-Salkyl groups or C-Salkyloxy groups, - or 7 means a hydroxy group, hydroxyC.-Salkyl, halogen, nitrile, amino group, where the M atom is optionally in

Ge) in each case independently mono- or disubstituted by C.-Salalkyl, pyridinyl--Salkyl, 5-tetrahydrofuranyl by 1-Salkyl, S.-Salkoxy--Salkyl, C-Szacyl, nitrile/-Salylalkyl, phenyl, while the phenyl ring is not is substituted by 1-2 halogen atoms, C-sulfoxy groups, hydroxy groups or mono-

He or di(Ci-Salkyl)amino groups, or 7 means a branched or unbranched C-Salkyl, C4i--Salkyloxy group or nitrileC-Su,alkyl,

Ki means branched or unbranched C,-C, alkyl, which is not necessarily partially or fully 5 Hhalogenated,

Ko means branched or unbranched S.-Szalkil, which is not necessarily partially or completely

Ф) halogenated and optionally substituted by a nitrile, where Kz means - a phenyl or heterocyclic group selected from the group consisting of pyridinyl, pyrimidinyl and pyrazolyl, while such a phenyl or heterocyclic group is optionally substituted with 1-5 substituents selected from the group consisting of branched or unbranched C 4-C 4-C alkyl, which is optionally partially or fully halogenated, C 1-C 4-C , alkyloxy, which is optionally partially or fully halogenated,

C.-Czthioalkyl, C4-CzthioalkylC /-Czalkyl, an amino group or a MNHS(O) group, - C-Czalkoxycarbonyl, 65 or Kz means cyclopropyl or cyclopentyl, each of which is optionally partially or fully halogenated and optionally substituted with 1- 3 by C-Szalkyl groups.

According to another embodiment of the invention, the compounds of formula (Ia) in which

Agi means 5-tert-butylpyrazol-3-yl, where the pyrazole ring in each case is independently substituted by 1-2 K» or Kz groups,

X means - cyclohexenyl, - phenyl, pyridinyl, pyrazinyl, piperidinyl or pyrimidinyl, each of which is optionally independently substituted

C.1-Soalkyl or hydroxy, 70 2 means phenyl, heteroaryl selected from pyridinyl and furanyl, heterocycle selected from 2-oxa-5-azabicyclo|2.2.1)heptanyl, pentamethylene sulfidyl, pentamethylene sulfoxidyl, tetrahydrofuranyl, piperazinyl, morpholino group, thiomorpholino group and piperidinyl, while each of the above 72 groups is optionally substituted with 1-3 substituents selected from 7/5 "Groups, which include S.-Szalkyl, C.-Szalkoxy group, oxo group, hydroxy group and MNHS(O)- group . C-C alkyl, or 7 means nitrile and alkyl,

Ez means a phenyl or heterocyclic group selected from the group consisting of pyridinyl, pyrimidinyl, and pyrazolyl, and such a phenyl or heterocyclic group is optionally substituted by 1-2 substituents selected from the group consisting of C 1-6 alkyl, which is necessarily partially or fully halogenated, C 4-SoalkoxySalkoxy group, which is not necessarily partially or fully halogenated, C 4-Sothioalkyl, C.4-Sothioalkyl-Ci-Salkyl, an amino group and a group MNHS(O), - C-Salkoxycarbonyl , i) whether Kz means cyclopropyl or cyclopentyl, each of which is optionally partially or fully halogenated and optionally substituted with 1-3 C-C alkyl groups.

In another embodiment of the invention, the compounds of formula (Ia) in which X stands for pyridinyl are preferred among those directly indicated above.

According to the next embodiment of the invention, among those directly mentioned above, the compounds of formula (Ia) in which pyridinyl is attached to Ag are preferred. in the 3rd position of pyridinyl. Gee!

As examples of compounds of formula (Ia) according to the invention, the following can be named: 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl) )naphthalen-1-yl|Urea, -- 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(3--4-morpholin-4-ylmethylphenyl)naphthalene -1-yl|Urea, i- 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4--(5-morpholin-4-ylmethylfuran-2- yl)naphthalen-1-yl)urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-I(4-(3-(morpholin-4-ylmethyl) cyclohexenyl)naphthalen-1-yl|Urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylI|-3-I(4-(2-(4-morpholine-4- yl)ethylphenyl)naphthalene-1-yl|Urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4--4-dimethylaminomethylphenyl)naphthalene-1- yl|Urea, « 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylI|-3-I(4-(5-(morpholin-4-ylmethyl)pyridin-2-yl )naphthalen-1-yl)urea, with 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylI|-3-I(4-(6--"morpholine-4- ylmethyl)pyridin-3-yl)naphthalen-1-yl)urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4- (6-(morpholin-4-yl methyl)pyridin-3-yl)naphthalene and"-1-yl|urea, 1-(b-tert-butyl-2-methyl-2H-pyrazol-3-ylI-3-I4-(6-"(morpholine -4-ylmethyl)pyridin-3-yl)naphthalen-1-yl|Urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI|-3 -I4-(3-(2-(morpholin-4-yl)ethylamino)cyclohexenyl -I)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazole-3 -yl|-3-(4-(3,4-(morpholin-4-ylmethyl)phenyl)naphthalen-1-yl|urea, - 1-(b-tert-butyl-2-p-tolyl-2H-pyrazole -3-yl|-3-(4--4-methylpiperazin-1-ylmethyl)phenyl)naphthalen-1-yl|Urea,

Ge) 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(piperidin-1-ylmethyl)phenyl)naphthalen-1-yl|Urea, 1- (b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI|-3-I4-(3-(2-(pyridin-2-yl)ethylamino)cyclohexenyl) o naphthalene-1-yl|urea,

He 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(4-(2-(pyridin-4-yl)ethylaminomethyl)phenyl)naphthalene-1 -yl|urine, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-I(4-(4-(pyridin-3-ylmethylaminomethyl)phenyl)naphthalene- 1-il|urea

NU, 59 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(4-(3,4-dimethoxyphenylmethyl)-3-hydroxyphenyl

F) )naphthalen-1-yl|urea, ka 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(6-oxo-1,6- dihydropyridin-3-yl)naphthalen-1-yl|Urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(4- -(morpholin-4-ylmethyl)phenyl)naphthalen-1-yl|c urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI- 3-I4-(4-"morpholin-4-ylmethyl)imidazol-1-yl)naphthali n-1-yl|Urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3- ilI|-3-I(4-(4-(morpholin-4-ylmethyl)imidazol-1-yl)naphthalen-1-yl|Urea, 1-(b-tert-butyl-2-(b-methylpyridin-3 -yl)-2H-pyrazol-3-ylI-3-I4-(4-«(furan-3-ylmethyl)-3-hydroxyphenyl)naphthalene 65 n-1-yl|Urea, 1-Ib-tert-butyl- 2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I(4-(6-(4-hydroxybutylamino)pyridin-3-yl)naphthalin-1-yl|urea, 1 -(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(4-(pyridin-3-ylmethyl)-3-hydroxyphenyl)naphtha lin- 1-yl)urea, 1-(b-tert-butyl-2-(4-methyl-3-carbamylphenyl)-2H-pyrazol-3-ylI-3-I4-(6-"morpholin-4-ylmethyl)pyridine -3-yl)unapht alin-1-yl|urea y, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I(4-(4-(imidazol-2-ylmethyl)-3- hydroxyphenyl)naphthalin-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I(4-(4-( 3-hydroxymorpholin-4-ylmethyl)phenyl)naphtha 70. Llin-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI- 3-I4-(4-(("M-2-methoxyethyl-M-methylaminomethyl)phenyl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)- 2H-pyrazol-3-ylI-3-I(4-(4-(4-hydroxymorpholin-4-ylmethyl)phenyl)naphthalin-1-yl)urea, 1-(b-tert-butyl-2-(b -methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(3-"morpholin-4-ylmethyl)cyclohexenyl)naphthali n-1-yl|Urea, 1-(b-tert-butyl- 2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(4-(tetrahydrofuran-3-ylmethyl)-3-hydroxyphen yl)unanaphthalen-1-yl|Urea, 1- (b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I(4-(4-(M,Mm-ai-(2-methoxyethyl)aminomethyl) phenyl)n 2o aphthalin-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(6-(3 -cyanopropoxy) pyridin-3-yl)naphthalen-1-yl|Urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(4- morpholin-4-ylmethylpiperidinut)naphthalen-1-yl|Urea, sc 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I(4- (4-(M,M-di(2-cyanoethyl)aminomethyl)phenyl)naphthalin-1-yl|urea, and) 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3- yl|-3-I(4-(1-morpholin-4-ylindan-5-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl) -2H-pyrazol-3-ylI-3-I4-(4-(furan-2-ylmethyl)-3-hydroxyphenyl)naphthalene-1-yl|Urea, c zo 1-(b-tert-butyl-2- (b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(4-(thiomorpholin-4-ylmethyl)phenyl)naphthalene-1-lysine, about 1-(b-tert-butyl -2-(b-methylpyridin-3-yl)-2H-pyrazol-3-yl-3-(4-(4--3-carboxamidomorpholin-4-ylmethyl)phenyl)n Ge! aphthalin-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(4--2-methyl-3 -oxopiperazin-1-ylmethyl)phenyl) -- naphthalene-1-yl|urea, i- 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)-2H-pyrazol-3-yl| -3-(4-(6--«morpholin-4-ylmethyl)pyridin-3-yl)unaphthalin-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3- yl)-2H-pyrazol-3-ylI-3-I(4-(6-(4-hydroxybutyloxy)pyridin-3-yl)naphthalene n-1-yl|Urea, « 1-(3-tert-butyl- 1 H-/1,4bipyrazol-5-ylI|-3-I4-(6-(morpholin-4-ylmethyl)pyridin-3-yl)naphthalen-1-yl|Urea, with c 1-(b-tert- butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(4-(furan-2-ylmethyl)-3-methoxyphenyl)naphthalene-1-yl)urea, ; » 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(5-(morpholine-4-carbonyl)pyrazin-2-yl) naphthalene n-1-yl|Urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI|-3-I4-(b-(tetrahydrothiopyran-4 -ylamino)pyridin-3-I l)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(2-cyanoethyl)-2H-pyrazol-3-ylI|-3-I( 4-(6--"morpholin-4-ylmethyl)pyr dyn-3-yl)naphthalen-1-yl)se - potash,

Ge) 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(6-(-2,6-dimethylmorpholin-4-ylmethyl) pyridin-3-boron l)naphthalen-1-yl|urea, o 1-(b-tert-butyl-2-(2-methoxypyridin-5-yl)-2H-pyrazol-3-yl|-3-(4 -(6--"morpholin-4-ylmethyl)pyridin-3-yl)unaphthal

He in-1-yl|urea, 1-(b-tert-butyl-2-(2-aminopyridin-5-yl)-2H-pyrazol-3-ylI|-3-I4-(6-(morpholine-4 -ylmethyl)pyridin-3-yl)naphthalene-1-yl)urea, 1-(b-tert-butyl-2-(6-oxo-1,6-dihydropyridin-3-yl)-2H-pyrazol-3- ylI-3-I4-(6-(morpholin-4-ylmethyl)pyridin-3-yl)unaphtalin-1-yl|Urea,

F) 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(6-(morpholin-4-yl-4-carbonyl)pyridine -3-yl)na kaphthalin-1-yl|Urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(6 -(2-oxa-5-azabicyclo|2.2.1)hept-5-ylmethyl bo)pyridin-3-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-p-tolyl- 2H-pyrazol-3-yl|-3-(4-(4-(3-carbamylphenyl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl) -2H-pyrazol-3-ylI-3-I(4-(4-(M-(2-cyanoethyl)-M-(pyridin-3-ylmethyl)aminomethyl)phenyl)naphthalen-1-ylurea, 1 -(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I(4-(4-(M-(2-cyanoethyl)-M-(pyridine -2-ylmethyl)aminomethyl)phenyl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3- (4-(4-(M-(2-cyanoethyl)-M-(tetrahydrofuran-2-ylmethyl)aminomethyl)phenyl)naphthalen-1-yl|Urea, 1-(b-tert-butyl-2-(b -methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(6-(morpholin-4-ylmethyl)-4-methoxypyridin-3-yl)naphthalen-1-yl|urea, 1- (b-tert-butyl-2-(b-methylpyridin-3-yl)) -2H-pyrazol-3-ylI-3-I4-(6-(1-morpholin-4-ylpropyl)pyridin-3-yl)unaphthallin-1-yl)urea, 1-(b-tert-butyl-2 -(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(6-(M-(3-methoxypropyl)amino)pyridin-3-yl)una phthalin-1-yl|Urea , 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(6-(M-(3-methoxypropyl)-M-methylamino) pyridine 70. 73-yl)naphthalen-1-yl)urea, 1-(3-tert-butyl-1"-methyl-1H-(1,4bipyrazol-5-ylI|-3-I4-(6-" "morpholin-4-ylmethyl)pyridin-3-yl)naphthalen-1-yl urea, 1-(b-tert-butyl-2-benzyl-2H-pyrazol-3-ylI-3-(4-(6-( Morpholin-4-ylmethyl)pyridin-3-yl)naphthalen-1-yl|Urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3 -I4-(4-(M-M-di(2-cyanoethyl)aminomethyl)phenyl)naphth 7/5 alin-1-yl)urea, 1-(b-tert-butyl-2-p-tolyl-2H- pyrazol-3-yl|-3-(4-(4-(4-carbamylphenyl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(b-methyltridin-3-yl)-2H -pyrazol-3-ylI|-3-I(4-(6-(1-oxo-tetrahydrothiopyran-4-ylamino)pyridin-3-yl)naphthalen-1-yl|urea, 1-(b-tert- butyl-2-(b-methylpyridin-3-yl)-2H-pyrazole -3-ylI-3-I4-(6-(tetrahydropyran-4-ylamino)pyridin-3-yl)n 2o aphthalin-1-yl|urea, 1-III-tert-butyl-1'-(3-cyanopropyl )-1'H-/1,4bipyrazol-5-ylI-3-I4-(6-(morpholin-4-ylmethyl)pyridin-3-yl)unaphtalin-1-yl|urea, 1-(b- tert-butyl-2-p-tolyl-2H-pyrazol-3-ylI|-3-(4--(3-methanesulfinylphenyl)naphthalen-1-yl|Urea, 1-(b-tert-butyl-2-p -tolyl-2H-pyrazol-3-yl|-3-(4--(3-methanesulfonylphenyl)naphthalen-1-yl|Urea, sc 1-(b-tert-butyl-2-p-tolyl-2H-pyrazole) -3-yl|-3-(4--3-sulfonamidophenyl)naphthalen-1-yl|Urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylI|-3- I(4-(3-(morpholin-4-yl)ucarbonylphenyl)naphthalen-1-yl)urea, and) 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazole -3-ylI-3-I(4-(5-(tetrahydrothiopyran-4-ylamino)pyrazine-2-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(b- methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(6-(methylcarbonylamino)pyridin-3-yl)naphthalene c

Zo 7 1-yl|urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylI|-3-I(4-(6--("morpholin-4-yl- 4-carbonyl)phenyl)naphthalen-1-yl|Urea, about 1-(3-tert-butyl-1'-(3-methylsulfanylpropyl)-1'H-/1,4bipyrazol-5-ylI|-3-I4 -(6-(morpholin-4-ylmethyl)pyridin- Ge!

Z-yl)unaphtalin-1-yl|Urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-I(4-(5-«(morpholine-4 -yl-carbonyl)pyridin-3-yl)naphthalen-1-yl|urea, -- 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI- 3-I4-(5-(morpholin-4-ylmethyl)pyrazin-2-yl)naphthalene-1-yl)urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl) -2H-pyrazol-3-ylI-3-I(4-(b-aminopyridin-3-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3- yl)-2H-pyrazol-3-ylI-3-I(4-(6-(1-methylpiperidin-4-ylamino)pyridin-3-yl)naphthalen-1-yl|urea, « 1-(b-tert -butyl-2-(2-methylpyrimidin-5-yl)-2H-pyrazol-3-yl|-3-(4-(6-(2-methyl-3-oxopiperazin-1-ylmethyl)pyri with c din- 3-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)-2H-pyrazol-3-yl|-3-(4-(6 -(morpholin-4-yl-carbonyl)pyridin-3-yl)na and»phthalin-1-yl|Urea, 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)-2H -pyrazol-3-yl|-3-(4-(6-(M,M-di(2-methoxyethyl)aminomethyl)pyrides

H-Z-yl)naphthalen-1-yl|urea, -I 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)-2H-pyrazol-3-yl1|-3-(4 -(6-(1-oxothiomorpholin-4-ylmethyl)pyridin-3-yl)unaphtalin-1-yl|Urea, - 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)-2H -pyrazol-3-yl|-3-(4-(6-(tetrahydropyran-4-ylamino)pyridin-3-yl)

Ge))naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)-2H-pyrazol-3-yl|-3-I4-(5-«( morpholin-4-ylmethyl)pyrazin-2-yl)unaphthal o yn-1-yl|urea,

Ge 1-(b-tert-butyl-2-(2-methylthiopyrimidin-5-yl)-2H-pyrazol-3-yl|-3-I(4-(6--"morpholin-4-ylmethyl)pyridin- 3-yl)naphthalin-1-yl|urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(6-(2-methyl- 3-oxopiperazin-1-ylmethyl)pyridin-3-yl)naphthalene di H-1-yl|urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylI|-3- (4-(6-(pyridin-3-yloxy)pyridin-3-yl)naphthalen-1-yl|Urea,

F) 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(6-(pyridin-3-ylamino)pyridin-3-yl)naphthalene-1 -yl)urea, ka 1-(b-tert-butyl-2-(2-methoxypyrimidin-5-yl)-2H-pyrazol-3-ylI-3-I4-(6-"morpholin-4-ylmethyl)pyridine -3-yl)unaphtal alin-1-yl|urea, in 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-I(4-(5-carbamylpyridine- 3-yl)naphthalen-1-yl|Urea, 1-(b-tert-butyl-2-(2-aminopyrimidin-5-yl)-2H-pyrazol-3-ylI-3-I4-(6-"morpholine -4-ylmethyl)pyridin-3-yl)naphthalin-1-yl|urea, 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)-2H-pyrazol-3-yl|- 3-I4-(4-(morpholin-4-ylmethyl)phenyl)naphthalen-1-yl urea, 65 1-III-tert-butyl-1"-methyl-1H-/1,4bipyrazol-5-ylI-3 -I4-(6-(morpholin-4-ylmethyl)phenyl)naphthalen-1-yl|Urea, 1-(b-tert-butyl-2-(2-cyclopropylpyrimidin-5-yl)-2H-pyrazol-3- ylI-3-I4-(6-"morpholin-4-ylmethyl)pyridin-3-yl)

naphthalene-1-yl|urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(2-(pyridin-3-ylamino)pyrimidine-5 -yl)naphthalen-1-yl|Urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylI-3-(4-(6-(1-oxotetrahydrothiopyran-4-ylamino) )pyridin-3-yl)naphthalin-1-yl|urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(6-(thiomorpholine) -4-ylmethyl)pyridin-3-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(3 -benzyl-ZN-imidazo|4,5-BIpyridin-b-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol- 3-ylI|-3-I4-(6-(pyridin-3-ylmethyl)pyridin-3-yl)naphthalen-1-yl|Urea, 70 1-(b-tert-butyl-2-p-tolyl-2H -pyrazol-3-yl|-3-I(4-(2-(morpholin-4-ylcarbonyl)pyrimidin-5-yl)naphthalen-1-yl|urine, 1-(b-tert-butyl-2- p-tolyl-2H-pyrazol-3-yl|-3-I(4-(2-(morpholin-4-ylmethyl)pyrimidin-5-yl)naphthalen-1-yl|Urea, 1-(b-tert- butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(3-amino-4-carbamylphenyl)naphthalen-|-yl|urea, 1-(b-tert-butyl-2- p-tolyl-2H-pyrazol-3-yl|-3-(4-(6-(1-oxothiomorph lin-4-ylmethyl)pyridin-3-yl)naphthalen-1-yl 7/5 Urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylI|-3-(4 -(6-(pyridin-3-ylmethyl)pyridin-3-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3 -(4-(6-(hydroxypyridin-3Z-ylmethyl)pyridin-3-yl)naphthalen-1-yl urea, 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)- 2H-pyrazol-3-yl|-3-I(4-(2-(morpholin-4-ylmethyl)pyrimidin-5-yl)naphth 2o alin-1-yl|urea, as well as their pharmaceutically acceptable derivatives.

According to another embodiment of the invention, it also offers the following compounds of formula (Ia): 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-I(4-(5 -(morpholin-4-ylmethyl)pyridin-2-yl)naphthalen-1-yl)urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylI|-3-I (4-(6--"morpholin-4-ylmethyl)pyridin-3-yl)naphthalen-1-yl)urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H -pyrazol-3-ylI|-3-I4-(3-(2-(pyridin-2-yl)ethylamino)cyclohexenyl) naphthalene-1-yl)urea, 1-(b-tert-butyl-2- p-tolyl-2H-pyrazol-3-yl|-3-I(4-(4-(pyridin-3-ylmethylaminomethyl)phenyl)naphthalen-1-yl|urea and) on, 1-(b-tert-butyl -2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(4--(morpholin-4-ylmethyl)phenyl)naphthalen-1-yl|se urea, c zo 1-Ib-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I(4-(6-(4-hydroxybutylamino)pyridin-3-yl)naphthal and -1-yl|Iurea that) 1-(b-tert-butyl-2-(4-methyl-3-carbamylphenyl)-2H-pyrazol-3-ylI-3-I4-(6-"morpholine-4- ylmethyl)pyridin-3-yl)unapht Gelalin-1-yl)urea, 1-(b-tert-butyl-2-(b-methylpyridin-3- yl)-2H-pyrazol-3-ylI-3-I(4-(4-(3-hydroxypiperidin-1-ylmethyl)phenyl)naphth -- alin-1-yl)urea, i- 1-(b-tert -butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I(4-(4-(4-hydroxymorpholin-4-ylmethyl)phenyl)naphtha lin-1-yl) isurea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(3-"morpholin-4-ylmethyl)cyclohexenyl)naphthalene n- 1-yl|Urea, « 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(4-(tetrahydrofuran-3-ylmethyl) -3-hydroxyphen with c yl)unanaphthalen-1-yl|urea, . 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(4-(M,M-di(2-methoxyethyl)aminomethyl)phenyl) Phthalin-1-yl urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(6-( 3-cyanopropoxy)pyridin-3-yl)naphthalen-1-yl|urea, -I 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3 -I4-(4-morpholin-4-ylmethylpiperidinut)naphthalen-1-yl|urea, - 1-(b-tert-butyl-2-(b-methyltridin-3-yl)-2H-pyrazol-3-ylI| -3-I(4-(4-(M,M-di(2-cyanoethyl)aminomethyl)phenyl)naphtha

He)lin-1-yl)urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(4-(furan-2 -ylmethyl)-3-hydroxyphenyl)naphthalene 1 n-1-yl|Urea,

Ge 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(4-(thiomorpholin-4-ylmethyl)phenyl)naphthalene-1- and lysine, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(4-(3-carboxamidopiperidin-1-ylmethyl)phenyl) dv naphthalene-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(4--2-methyl- 3-oxopiperazin-1-ylmethyl)phenyl)

F) naphthalene-1-yl|urea, ka 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)-2H-pyrazol-3-yl|-3-(4-(6-- "morpholin-4-ylmethyl)pyridin-3-yl)unaphthalin-1-yl|Urea, in 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3- ylI-3-I(4-(6-(4-hydroxybutyloxy)pyridin-3-yl)naphthali n-1-yl|Urea, 1-(3-tert-butyl-1H-/1,4bipyrazol-5- ylI-3-I4-(6-(morpholin-4-ylmethyl)pyridin-3-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl) -2H-pyrazol-3-ylI|-3-I4-(b-(tetrahydrothiopyran-4-ylamino)pyridin-3-yl)naphthalen-1-yl|urea, 65 1-(b-tert-butyl-2 -(2-cyanoethyl)-2H-pyrazol-3-ylI|-3-I(4-(6--«morpholin-4-ylmethyl)pyridin-3-yl)naphthalen-1-yl)acetamine,

1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(6-(-2,6-dimethylmorpholin-4-ylmethyl)pyridin- 3-yl)unaphtalin-1-yl|urea, 1-(b-tert-butyl-2-(2-methoxypyridin-5-yl)-2H-pyrazol-3-yl|-3-(4-(6- -"morpholin-4-ylmethyl)pyridin-3-yl)unaphthalin-1-yl|urea, 1-(b-tert-butyl-2-(2-aminopyridin-5-yl)-2H-pyrazol-3- ilI|-3-I4-(6-(morpholin-4-ylmethyl)pyridin-3-yl)naphthalene-1-yl)urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl) )-2H-pyrazol-3-ylI-3-I4-(6-(morpholin-4-yl-4-carbonyl)pyridin-3-yl)na phthalin-1-yl|Urea, 70 1-(b-tert -butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(6-(2-oxa-5-azabicyclo|2.2.1)hept-5-ylmethyl)pyridine -3-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I(4-(4 -(M-(2-cyanoethyl)-M-(pyridin-3-ylmethyl)aminomethyl)phenyl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3- yl)-2H-pyrazol-3-ylI-3-(4-(4-(M-(2-cyanoethyl)-M-(tetrahydrofuran-2-yl 7/5 ethyl)aminomethyl)phenyl)naphthalen-1-yl |urea, 1-(b-tert-butyl-2-(b-methylpyride). in-3-yl)-2H-pyrazol-3-ylI-3-I4-(6-(morpholin-4-ylmethyl)-4-methoxypyridin-3-yl)naphthalen-1-yl|urea, 1-( b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(6-(1-morpholin-4-ylpropyl)pyridin-3-yl)unaphthalene -1-yl)urea, 1-(3-tert-butyl-1"-methyl-1H-/1,4bipyrazol-5-ylI|-3-I4-(6-(morpholin-4-ylmethyl)pyridin- 3-yl)naphthalen-1-yl urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I(4-(6-( 1-oxo-tetrahydrothiopyran-4-ylamino)pyridin-3-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol- 3-ylI-3-I4-(6-(tetrahydropyran-4-ylamino)pyridin-3-yl)n sch ov aphthalin-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridine) -3-yl)-2H-pyrazol-3-ylI-3-I(4-(5-(tetrahydrothiopyran-4-ylamino)pyrazin-2-y) l)naphthalen-1-yl|urea, 1-( b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(6-(methylcarbonylamino)pyridin-3-yl)naphthalene-1-yl)urea, c zo 1-(3-tert-butyl-1-(3-methylsulfanylpropyl)-1'H-(1,4Dbipyrazol-5-yl|-3-I4-(6-(morpholin-4-ylmethyl)pyridin-

C-yl)unaphtalin-1-yl|urea, o 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)-2H-pyrazol-3-yl1|-3-(4-(6 -(1-Oxothiomorpholin-4-ylmethyl)pyridin-3-Heyl)unnaphthalen-1-yl|urea, 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)-2H-pyrazole -3-yl|-3-(4-(6-(tetrahydropyran-4-ylamino)pyridin-3-yl -- )naphthalen-1-yl|urea, i- 1-(b-tert-butyl-2- (2-Methylthiopyrimidin-5-yl)-2H-pyrazol-3-yl|-3-I(4-(6--«morpholin-4-ylmethyl)pyridin-3-yl)naphthalen-1-yl|urea , 1-(b-tert-butyl-2-(2-aminopyrimidin-5-yl)-2H-pyrazol-3-ylI-3-I4-(6-"morpholin-4-ylmethyl)pyridin-3-yl) naphthalene-1-yl|Iurea, "1-3-tert-butyl-1"-methyl-1H-(1,4bipyrazol-5-ylI|-3-I4-(6--"morpholin-4-ylmethyl )phenyl)naphthalen-1-yl|urea, with c 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(6-(1-oxo- Tetrahydrothiopyran-4-ylamino)pyridin-3-yl)naphthalene-1-yl)urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-( 4-(6-«(thiomorpholin-4-ylmethyl)pyridin-3-yl)naphthalen-1-yl)urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl| -3-I(4-(2-(morpholin-4-yl-carbons). l)pyrimidin-5-yl)naphthalen-1-yl)se

CHOOVVINA, -I 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylI|-3-I(4-(-2-(morpholin-4-ylmethyl)pyrimidin-5-yl )naphthalen-1-yl|Urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(6-(1-oxothiomorpholin-4-ylmethyl) pyridin-3-yl)naphthalen-1-yl - Urea,

Ge) 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)-2H-pyrazol-3-yl|-3-I(4-(2-(morpholin-4-ylmethyl)pyrimidin- 5-yl)naphthoalin-1-yl|urea and their pharmaceutically acceptable derivatives. According to the third object of the invention, it further offers compounds of formula (II):

WITH

Ko) , lead x-x- by

In which o o means name) - aromatic C3-C:iocarbocycle or saturated or unsaturated unsaturated C3-C:iocarbocycle, - 6-10-membered heteroaryl containing one or more heteroatoms selected from O, Mi 5, 60 - B - 8--lene monocyclic heterocycle containing one or more heteroatoms selected from 0, M and 5, or - 8-11--lene bicyclic heterocycle containing one or more heteroatoms selected from O, Mi 5, while C substituted with one or more Cu, Co or Kz groups, Ag is phenyl, naphthyl, quinolinyl, isoquinolinyl, tetrahydronaphthyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, benzimidazolyl, benzofuranyl, dihydrobenzofuranyl, indolinyl, benzothienyl, dihydrobenzothienyl, indanyl, indenyl or indolyl, each of which is optionally substituted by one or more K or Kv groups,

X means

- C5-Ce cycloalkyl or cycloalkenyl, optionally substituted with 1-2 oxo groups or 1-3 C --C, alkyl,

C.4-Salkoxy- or C.-C, alkylamino chains, - phenyl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, pyridinyl, pyrimidinyl, pyridinonyl, dihydropyridinonyl, maleimidyl, dihydromaleimidyl, piperidinyl, benzimidazole, ЗН-imidazo|4,5 -p|Ipyridine, piperazinyl, pyridazinyl or pyrazinyl,

M means a bond or saturated or unsaturated branched or unbranched C 4-C; carbon chain, optionally partially or fully halogenated, with one or more methylene groups optionally replaced by O, M or 5(O)»t, and M optionally independently substituted by 1-2 oxo groups, phenyl or one or 70 by several C.4-C; alkyl groups, optionally substituted by one or more halogen atoms, 2 means - phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, furanyl, thienyl, pyranyl, each of which are optionally substituted by 1-3 substituents selected from the group consisting of halogen, Cb o4-Salkyl, C.i-Salkyloxy group, hydroxy group, amino group, MOono- or 7/5 VI(C4-Salkyl)amino group, group Si- Svalkyl-5(O) t, SM group, SOMN group, COOH group and phenylamino group, where the phenyl ring is optionally substituted with 1-2 halogen atoms, C -Svalkyl groups or

C.i-Svaloxy groups, - tetrahydropyranyl, tetrahydrofuranyl, 1,3-dioxolanonyl, 1,3-dioxanonyl, 1,4-dioxanyl, morpholinyl, thiomorpholinyl, thiomorpholinosulfoxidyl, thiomorpholinosulfonyl, piperidinyl, piperidinonyl, piperazinyl, tetrahydropyrimidonyl, cyclohexanonyl, pentamethylenesulfonyl, cyclohexanoyl , pentamethylenesulfoxidyl, pentamethylenesulfonyl, tetramethylene sulfide, tetramethylenesulfoxidyl or tetramethylenesulfonyl, each of which is optionally substituted with 1-3 substituents selected from the group consisting of nitrile, SI /4-Svalkyl,

C.-C-Alkoxy group, hydroxy group, amino group, mono- or di(C.--C.Alkyl)amino-C.-C.-Alkyl, group SOMN", phenylamino-C-C.Alkyl and C4--C.Alkoxy-C.-C.-Alkyl, sc - halogen, C.-C.alkyl, nitrile, amino group, hydroxy group, C.sub.-C.sub.alkyloxy group, MNHS(O) group, mono- or di(C.sub.1-C.alkyl)aminocarbonyl, mono- or di(C.-C.sub.alkyl)amino group, secondary or a tertiary amine, while i) the amine nitrogen is covalently linked to C 4-C 3 alkyl or C 4-C 3 alkyl, pyridinyl-C 4-C alkyl, imidazolyl-C 4-C alkyl, tetrahydrofuranyl-C 4 alkyl, nitrile -C--Salkyl, carboxamide-C--Salkyl, phenyl, where the phenyl ring is optionally substituted by 1-2 halogen atoms, C-Salkyloxy groups, hydroxy groups or mono-iso or di(C1-Salkyl)amino groups, group C- Svalkyl-5(O) t or a phenyl-(O)t group, where the phenyl ring is optionally substituted with 1-2 halogen atoms, Si-Svalkoxy groups, hydroxy groups or MOono- or di(C.4-Salkyl)amino groups, Ge! - Si-Svalkyl-B(O)»t and phenyl-5(O)2, where the phenyl ring is optionally replaced by 1-2 halogen atoms,

C.-Salkyloxy groups, hydroxy groups or mono- or di(C.-Salkyl)amino groups, --

Ki in each case independently means C.sub.-Suralalkyl, which is optionally partially or fully halogenated and optionally substituted with 1-3 substituents selected from the group consisting of C.sub.3-C.isocycloalkanyl, hydroxy group, phenyl, naphthyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, imidazolyl, pyrazolyl, thienyl, furyl, isoxazolyl. ( isothiazolyl, while each of the above substituents is optionally substituted with 1-5 substituents selected from "70 3 halogen, C.-Cylalkyl, which is not necessarily partially or fully halogenated, C 2 -C 2 cycloalkanyl, s C 5 -C 2 cycloalkenyl, hydroxy groups , a nitrile, a C-Salkyloxy group, which is optionally partially or fully halogenated, a MHC(O) group, a mono- or di(C-Salkyl)amino group and a mono- or di(C-Salkyl)aminocarbonyl, and a cyclopropyloxy group , a cyclobutyloxy group, a cyclopentyloxy group, a cyclohexyloxy group or a cycloheptyloxy group, each of which is optionally partially or fully halogenated and optionally substituted with 1-3 substituents selected from the group consisting of C 4-Salkyl, which is optionally partially or fully -I halogenated , the CM group, hydroxyC--Salkyl and aryl, or an analogue of such a cycloalkyl group, in which 1-3 ring methylene groups are independently replaced by O, З(О)7y, CHOH, »С-0, 2-5 or МН, - - a phenyloxy group or a benzyloxy group, each of which is optional partially or fully not halogenated and

Ge) is optionally substituted by 1-3 substituents selected from the group, which includes C 4-Salkyl, which is optionally partially or fully halogenated, the CM group, hydroxyC-Salkyl, and aryl, or an analogue of such a cycloaryl o group, in which 1-2 ring methylene groups are independently replaced by M,

He is cyclopropanyl, cyclobutanyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, bicyclopentanyl, bicyclohexanyl, or bicycloheptanyl, each of which is optionally partially or fully halogenated and optionally substituted with 1-3 substituents selected from the group consisting of C 4-C alkyl, which optionally 2 partially or fully halogenated, a CM group, hydroxyC.--Salkyl and aryl, or an analogue of such a cycloalkyl group, in which 1-3 ring methylene groups are independently replaced by 0, З(О)7у, СНОН, »С- 0, 20-55 or MH, (F, - branched or unbranched C3-Sioalkenyl, which in each case is optionally partially or completely halogenated and optionally substituted with 1-3 substituents selected from the group, which include branched or o unbranched S.--Sralkyl, phenyl, naphthyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, bo imidazolyl, pyrazolyl, thienyl, furyl, isoxazolyl and isothiazolyl, while each of the specified substituents is substituted with 1-5 substituents selected from the group, which includes ha logene, C.i-Salkyl, which is optionally partially or fully halogenated, cyclopropanyl, cyclobutanyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, bicyclopentanyl, bicyclohexanyl and bicycloheptanyl, s-hydroxy, nitrile, C.-Salkyloxy, which is optionally partially or fully halogenated , the MNoC(O) group and mono- or di(C..alkylsaminocarbonyl), while such branched or unbranched C3-C-iralkenyl is optionally interrupted by one or more heteroatoms selected from 0, M and (Ot,

- cyclopentenyl, cyclohexenyl, cyclohexadienyl, cycloheptenyl, cycloheptadienyl, bicyclohexenyl or bicycloheptenyl, while such a cycloalkenyl group is optionally substituted with 1-3 C.i.S.alkyl groups, - nitrile, halogen, - methoxycarbonyl, ethoxycarbonyl and propoxycarbonyl, - silyl, which contains three C-C alkyl groups, which are optionally partially or fully halogenated, - C3-Alkynyl branched or unbranched carbon chain, optionally partially or fully halogenated, while one or more methylene groups are optionally replaced by OO, MH or 5(O)m, and the indicated alkynyl group is optionally independently substituted by 1-2 oxo groups, pyrrolidinyl, pyrrolyl, one ur) or several C.4-C.alkyl groups, optionally substituted by one or several halogen atoms, nitrile, morpholino group, piperidinyl, piperazinyl, imidazolyl, phenyl, pyridinyl, tetrazolyl, or mono- or di(C.S-alkyl)amino group, optionally substituted by one or more atoms halogen,

EC", RK. and K5 each means - a branched or unbranched C.i.sub.6 alkyl, which is optionally partially or fully halogenated, /5 acetyl, aroyl, a branched or unbranched C.i.sub.1-Slalkoxy group, which in each case is optionally partially or fully halogenated, halogen, methoxycarbonyl, C-Salkyl-Z(O)»t group, which is not necessarily partially or fully halogenated, or phenylsulfonyl, - C-Salkyloxy group, hydroxy group, amino group, mono- or di(C,C,alkyl)amino group , or nitrile halogen, - group OK", - nitro group or - group mono- or di(C.i-C.alkyl)amino-5(O0)", which is not necessarily partially or fully halogenated, or group NaM5O",

Ez in each case independently means - phenyl, naphthyl, morpholinyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, pyrrolidinyl, sc imidazolyl, pyrazolyl, thiazolyl, oxazolyl, triazolyl, tetrazolyl, thienyl, furyl, tetrahydrofuryl, isoxazolyl, isothiazolyl, quinolinyl, isoquinolinyl, indolyl, benzimidazolyl, benzofuranyl, benzoxazolyl, (8) benzisoxazolyl, benzpyrazolyl, benzothiofuranyl, cinnolinyl, pterindinyl, phthalazinyl, naphthylpyridinyl, quinoxalinyl, quinazolinyl, purinyl or indazolyl, while each of the above radicals is optionally substituted with 1-3 substituents, selected from the group consisting of phenyl, naphthyl, heterocycle or heteroaryl described above in this paragraph, branched or unbranched C1-Salkyl, which is optionally partially or fully halogenated, cyclopropanyl, cyclobutanyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, bicyclopentanil, o bicyclohexanil, bicycloheptanil, phenyl-Si-Svalkyl, naphthyl-C.--Svalkyl, halogen, hydroxy group, oxo group, Ge! nitrile, C1-C6alkyloxyC.alkyloxy group, which is not necessarily partially or fully halogenated, phenyloxy group, naphthyloxy group, heteroaryloxy group and heterocyclooxy group, where heterocyclic or heteroaryl (the 7th fragment is described above in this paragraph, nitro group, amino group, mono- or di(C.4 -Salkyl)amino group, i-phenylamino group, naphthylamino group, heteroarylamino group or heterocyclamino group, where the heteroaryl or heterocyclic fragment is described above in this paragraph, the group МНЬС(О), mono- or di(C1-Salkyl)aminocarbonyl, C.-Salkyl-C( O0)-C.-Salkyl, amino-C.-Salkyl, mMono- or di(C.4-Salkyl)amino-C-Salkyl, amino-5(0)»2 group, di(C-Salkyl )amino-5(O)5, /K,-S.i-Svalkil, "

Kv-C1-Salkyloxy group, Kea-C(0)-C.4-Salkyl, Kio-C4-Salkyl(K44)M group and carboxy-mono- or Cs di(C.-Salkyl)amino group, Y . - кКонденсований арил, вибраний з бензоциклобутанілу, інданілу, інденілу, дигідронафтилу, а тетрагідронафтилу, бензоциклогептанілу і бензоциклогептенілу, або конденсований гетероарил, вибраний з циклопентенопіридинілу, циклогексанопіридинілу, циклопентанопіримідинілу, циклогексанопіримідинілу, Циклопентанопіразинілу, циклогексанопіразинілу, циклопентанопіридазинілу, циклогексанопіридазинілу, -І циклопентанохінолінілу, циклогексанохінолінілу, циклопентаноізохінолінілу , циклогексаноізохінолінілу, циклопентаноіндолілу, циклогексаноіндолілу, циклопентанобензімідазолілу, циклогексанобензімідазолілу, - циклопентанобензоксазолілу, циклогексанобензоксазолілу, циклопентаноімідазолілу, циклогексаноімідазолілу, со циклопентанотієнілу і циклогексанотієнілу, при цьому конденсоване арильне чи конденсоване гетероарильне 5р Кільце незалежне заміщено 0-3 замісниками, вибраними з групи, куди входять феніл, нафтил , pyridinyl, 1 pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, imidazolyl, pyrazolyl, thienyl, furyl, isoxazolyl, isothiazolyl,

He Si-Svalkyl, which is optionally partially or fully halogenated, halogen, nitrile,

C-C alkyloxy, optionally partially or fully halogenated, phenyloxy, naphthyloxy, heteroaryloxy or heterocyclooxy, wherein the heteroaryl or heterocyclic fragment is described above in this paragraph, a nitro group, an amino group, a mono- or di(C-C alkyl) amino group, phenylamino group, naphthylamino group, heteroarylamino group or heterocyclamino group, where heteroaryl or

Ф) heterocyclic fragment is described above in this paragraph, group МНЬС(О), mono- or ka di(C1-C alkyl)aminocarbonyl, group C4-C; alkyl-OC(O), C-C alkyl-C(O)- C.4-C,.alkyl, amino-Ci-Salkyl, mono- or di(C.4-C3)alkylamino-C--Salkyl, C.i2-Ci-Salkyl, C.i3-C4--Salkyloxy group, C.-C(0)-C.-Svalkyl and group 60 Ki5-C4-Svalkylk 6) M, - cyclopropanyl, cyclobutanyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, bicyclopentanyl, bicyclohexanyl or bicycloheptanyl, each of which is optional partially or completely halogenated and optionally substituted with 1-3 C and -C alkyl groups, or an analogue of such a cycloalkyl group, in which 1-3 ring methylene groups are independently replaced by O, 5, CHOH, 2C-0, 2-5 or MH, 65 - cyclopentenyl, cyclohexenyl, cyclohexadienyl, cycloheptenyl, cycloheptadienyl, bicyclohexenyl, or bicycloheptenyl, each of which is optionally substituted with 1-3 C.-C alkyl groups,

- C4-Alkylphenyl-C(O0)-C4-C; alkyl-, C.-C; alkyl-C(O0)- 4-Salkyl- or Ci-C; alkylphenyl-Z(O)t-C.4- Sulalkyl-, - Si-Svalkyl group or branched or unbranched C.i-Svalkoxy group, each of which is optionally partially or fully halogenated or optionally substituted by group K.7, - OKuv or Si-Svalkyl, optionally substituted by a group OK in, - an amino group or a mono- or di(C.-Svalkyl) amino group, optionally substituted by a group Ko, - Egos(O)(K 21)-, Kg20-, KozKodMS(O)-, Kov(СНо )p(OM(К21)- or KoС(ОХОН о) (К21)-, - C2-Svalkenyl, substituted by the group KozKo4МС(О)-, - C2-Svalkenyl branched or unbranched carbon chain, optionally partially or fully 70 halogenated , while one or more methylene groups are optionally replaced by 0, МН, 5(О) t, and the indicated alkynyl group is optionally independently substituted by 1-2 oxo groups, pyrrolidinyl, pyrrolyl, morpholinyl, piperidinyl, piperazinyl, imidazolyl, phenyl , pyridinyl, tetrazolyl, one or more

C.-C.alkyl groups, optionally substituted by one or more halogen atoms, nitrile, morpholino group, piperidinyl, piperazinyl, imidazolyl, phenyl, pyridinyl, tetrazolyl or mono- or 7/5 VI(C.-C.alkyl)amino group , which can be replaced by one or more halogen atoms, or - aroyl,

Ke means C-C alkyl, which is optionally partially or fully halogenated and optionally substituted by the Kev group,

EK, Ka, Ka, Kcho, Ki", Kis, Kia, Kv, K4i7, Kv, Kov and Kov each independently represent nitrile, phenyl, 2o morpholino group, piperidinyl, piperazinyl, imidazolyl, pyridinyl, tetrazolyl, amino group or mono - or di(C4-C.alkyl)aminoC zalkoxy group, which is not necessarily partially or fully halogenated,

Ku44 Her Kv each independently means hydrogen or C,-C, alkyl, which is not necessarily partially or fully halogenated,

Kv in each case independently means hydrogen or C1-C4 alkyl, which is not necessarily independently substituted by an oxo group or a Kov group,

Coo in each case independently means C-Cyralalkyl, which is not necessarily partially or fully i) halogenated, phenyl or pyridinyl,

Ko2i in each case independently means hydrogen or S-Svalkyl, which is not necessarily partially or fully halogenated, c zo Ko", Koz and Cod each independently of each other means hydrogen, C--Svalkyl, which is not necessarily partially or fully halogenated halogenated, and the indicated C.i-Svalkyl is not necessarily interrupted by one or more atoms of

O, M or 5, as well as independently optionally substituted mono- or di(C 41-Salkyl)aminocarbonyl, phenyl, Ge! pyridinyl, an amino group or a mono- or di(C1-C6 alkyl)amino group, while each of the specified substituents is optionally partially or completely halogenated and optionally substituted with a mono- or -- di(C1-C6 alkyl)amino group, or uh-

Koz and Cod together optionally form a heterocyclic or heteroaryl ring, t means 0, 1 or 2 and

M stands for O or 5, and pharmaceutically acceptable derivatives thereof. "

According to one of the variants of the implementation of the invention, among those directly indicated above, those compounds from c formula (II) in which o means;" - phenyl, naphthyl, benzocyclobutanyl, dihydronaphthyl, tetrahydronaphthyl, benzocycloheptanyl, benzocycloheptenyl, indanyl, indenyl, - pyridinyl, pyridonyl, quinolinyl, dihydroquinolinyl, tetrahydroquinoyl, isoquinolinyl, tetrahydroisoquinoyl, -And pyridazinyl, pyrimidinyl, pyrazinyl, benzimidazolyl, benzoylfuranyl, benzothiazolin benzothiophenyl, benzpyrazolyl, dihydrobenzofuranyl, dihydrobenzothiophenyl, benzooxazolonyl, - benzo|1,Zoxazin-3-onyl, benzodioxolyl, benzo|1,3|dioxol-2-onyl, benzofuran-Z-onyl,

Ge) tetrahydrobenzopyranyl, indolyl, indolinyl, indolonyl, indolinonyl, phthalimidyl, chromoyl, - oxetanyl, pyrrolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, piperidinyl, piperazinyl, morpholinyl, 1 tetrahydropyranyl, dioxanyl, tetramethylenesulfonyl, tetramethylenesulfoxidyl, oxazolinyl, thiazolinyl,

He imidazolinyl, tetrahydropyridinyl, homopiperidinyl, pyrrolinyl, tetrahydropyrimidinyl, decahydroquinolinyl, decahydroisoquinolinyl, thiomorpholinyl, thiazolidinyl, dihydrooxazinyl, dihydropyranyl, oxocanyl, heptacanyl, thioxanyl or dithianyl, while OS is substituted by one or more groups K., K» or Kz.

In another embodiment of the invention, the compounds of the formula (I), (F), in which ka b means phenyl, pyridinyl, pyridonyl, naphthyl, quinolinyl, isoquinolinyl, pyrazinyl, benzimidazolyl, benzoxazolyl, benzofuranyl, benzothiophenyl, benzpyrazolyl, dihydrobenzofuranyl , dihydrobenzothiophenyl, indanyl, indenyl, indolyl, indolinyl, indolonyl or indolinonyl, while C is substituted by one or more groups Ku, K» or Kz,

Ag means naphthyl, quinolinyl, isoquinolinyl, tetrahydronaphthyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, indanyl, indenyl or indolyl, each of which is optionally substituted with one or more groups K or K5, 65 X means phenyl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl , pyridinyl, pyrimidinyl, pyridinonyl, dihydropyridinonyl, maleimidyl, dihydromaleimidyl, piperidinyl, piperazinyl, pyridazinyl or pyrazinyl,

U means a connection, either saturated or unsaturated S.-S.; carbon chain, while one of the carbon atoms is optionally replaced by O, M or 5(O), and M is optionally independently substituted by 1-2 oxo groups, or phenyl by one or more C.i.-C.alkyl groups, optionally substituted by one or more halogen atoms, 2 means - phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, imidazolyl, furanyl, thienyl, dihydrothiazolyl, dihydrothiazolyl sulfoxidyl, pyranyl, pyrrolidinyl, which are optionally substituted by 1-3 substituents selected from the group , which contains a nitrile, C.4-Salkyl, C.sub.6-Salkoxy group, amino group, mono- or di(C.S.-Salkyl)amino group, group 7/0. SOMN; and the OH group, - tetrahydropyranyl, tetrahydrofuranyl, 1,3-dioxolanonyl, 1,3-dioxanonyl, 1,4-dioxanyl, morpholinyl, thiomorpholinyl, thiomorpholinosulfoxidyl, piperidinyl, piperidinonyl, piperazinyl, tetrahydropyrimidonyl, pentamethylene sulfidyl, pentamethylene sulfoxidyl, pentamethylene sulfonyl, tetramethylene sulfidyl, tetramethylene sulfoxide, or tetramethylenesulfonyl, optionally substituted with 1-3 substituents selected from /5 "Groups containing nitrile, C1-C6alkyl, C1-C6alkyl, amino group, mono- or di(C1-C6alkyl)amino group,

СОМН»» and the OH group, - nitrile, C.--Salkyl-B(O)t, halogen, hydroxy group, C.i.-C.alkoxy group, amino group, mono- or di(C1-Salkyl)amino group, mono- or di(S.-Szalkyl)aminocarbonyl or MNHS(O) group,

Ki in each case independently means - C3-Salkyl, which is optionally partially or fully halogenated and optionally substituted with 1-3 substituents selected from the group consisting of C3-Seccycloalkyl, phenyl, thienyl, furyl, isoxazolyl and isothiazolyl, where each of the specified substituents is optionally substituted with 1-3 substituents selected from halogen,

C-Salkyl, which is optionally partially or fully halogenated, hydroxy, nitrile and C-Salkoxy, which is optionally partially or fully halogenated, c - cyclopropyl, cyclobutyl, cyclopentanyl, cyclohexanyl, bicyclopentanyl or bicyclohexanyl, each of which is optional necessarily partially or fully halogenated and optionally substituted with 1-3 substituents selected from the group i) which contains C 4-Salkyl, optionally partially or fully halogenated, group CM, hydroxyC-Salkyl. and phenyl, or an analogue of such a cycloalkyl group, in which 1-3 ring methylene groups are independently replaced by 0, 5, CHOH, »С-0, 2-5 or МН, or с зо - silyl containing three С-С; alkyl groups, optionally partially or fully halogenated,

Co in each case independently means a halogen, a C.i-Szalkoxy group, a C.--Szalkyl-Z(O)t group, which is not necessarily partially or fully halogenated, phenylsulfonyl or nitrile, Ge!

Ez in each case independently means - phenyl, morpholino group, pyridinyl, pyrimidinyl, pyrazinyl, pyrrolyl, pyrrolidinyl, imidazolyl, pyrazolyl, --

Each of which is optionally substituted with 1-3 substituents selected from the group consisting of phenyl, naphthyl, n-heterocycle or heteroaryl described above in this paragraph, C-alkyl, which is optionally partially or fully halogenated, cyclopropanyl, cyclobutanyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, bicyclopentanyl, bicyclohexanyl, bicycloheptanyl, phenyl-Ci-Salkyl, naphthyl-C.--Salkyl, halogen, oxo group, hydroxy group, nitrile, C-Ci-SalkyloxyC.alkyl, which is optionally partially or fully halogenated , a phenyloxy group, a naphthyloxy group, a heteroaryloxy group or a heterocyclooxy group, where the heteroaryl or heterocyclic 7-3)c fragment is described above in this paragraph, a nitro group, an amino group, a mono- or di(C.4-Salkyl)amino group, . phenylamino group, naphthylamino group, heteroarylamino group or heterocyclamino group, where heteroaryl or the heterocyclic fragment is described above in this paragraph, the group MNHC(O), mono- or di(C4-Calkyl) aminocarbonyl, C.4-Salkyl-C(O0)-C.-C;alkyl, mono- or di(C. 4-Szalkyl) amino group, mono- or

ВІ(C1-C3)alkylamino-C 1-Svalkyl, group mMono- or di(C4-Salkyl)amino-Z(O) 2, K,-C.-Svalkyl, -I Ka-C--Svalkoxy group, Kea- C(0)-C.4-Salkyl, the Kio-C4-Salkyl(C44)M group and the carboxy-mono- or di(C4-C5)-alkyl-amino group, - - C-Salkyl or C.-C group; .alkoxy group, each of which is optionally partially or fully halogenated

Ge) or optionally substituted by the K.7 group, - OKuv or C.-Svalkyl, optionally substituted by the OK.v group, o - amino group or mono- or di(C.-Svalkyl)amino group, optionally substituted by the group Co,

Kz - Egos(O)(K 21)-, Kg20-, KozKodMS(O)-, KovSNo COM 21)- or KovS(O)SNo MK 21)-, - C--C.alkenyl, substituted by the group Kozko4MS(O )-, or - Co-C.alkynyl branched or unbranched carbon chain, which is optionally partially or completely halogenated and optionally independently substituted with 1-2 oxo groups, pyrrolidinyl, pyrrolyl, morpholinyl, piperidinyl, piperazinyl, imidazolyl, phenyl, pyridinyl, tetrazolyl or one chi

F) by several C4-C alkyl groups, optionally substituted by one or more halogen atoms, and Ka Koz and Kod together optionally form an imidazolyl, piperidinyl, morpholinyl, piperazinyl or pyridinyl ring. According to another embodiment of the invention, the compounds of formula (III) mentioned above are preferred, in which b means phenyl, pyridinyl, pyridonyl, naphthyl, quinolinyl, isoquinolinyl, pyrazinyl, benzothiophenyl, dihydrobenzofuranyl, dihydrobenzothiophenyl, indanyl, indolyl, indolinyl, indolonyl or indolinonyl, while o is substituted by one or more groups K., K» or Kz, 65 Ago means naphthyl,

X represents phenyl, imidazolyl, pyridinyl, pyrimidinyl, piperidinyl, piperazinyl, pyridazinyl or pyrazinyl,

each of which is optionally independently substituted with 1-3 substituents selected from the group consisting of C --C 1 alkyl,

C.-C.alkyl group, hydroxy group, nitrile, amino group, mono- or di(C.--Salkyl) amino group, mono- or di(C.sub.1-C alkylamino)carbonyl, MNHC(O) group, C--Salkyl-B group (O) n and halogen,

U means a bond or a saturated C.-Su/ carbon chain, while one of the carbon atoms is optionally replaced by 0, M or 5, and U is optionally independently substituted by an oxo group, 2 means - phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, imidazolyl, dihydrothiazolyl, dihydrothiazolyl sulfoxide, pyranyl or pyrrolidinyl, which are optionally substituted with 1-2 C 1-Soalkyl groups or 70. C1-C 6-Alkoxy groups, - tetrahydropyranyl, morpholinyl, thiomorpholinyl, thiomorpholinosulfoxidyl, piperidinyl, piperidinonyl, pyropyrazinyl or tetrahydropyranyl , which are optionally substituted by 1-2 C.--Soalkyl groups or

C.-Soalkoxy groups, or - C-Salkoxy group,

Ki in each case independently means - C3-Salkyl, which is optionally partially or fully halogenated and optionally substituted with phenyl substituted with 0-3 substituents selected from the group containing halogen, C-Salkyl, which is optionally partially or fully halogenated, a hydroxy group, nitrile and a C-C 6 -C 6 -C 6 -C 6 - alkoxy group, optionally partially or fully halogenated, - cyclopropyl, cyclobutyl, cyclopentanyl, cyclohexanyl, bicyclopentanyl or bicyclohexanyl, each of which is optionally partially or fully halogenated and optionally substituted by 1-3 substituents selected from the group consisting of C -Salkyl, optionally partially or fully halogenated, group CM, hydroxyC and -Salkyl. and phenyl, or an analog of cyclopropyl, cyclobutyl, cyclopentanyl, cyclohexanyl, bicyclopentanyl, or bicyclohexanyl, where one ring methylene group is replaced by 0, or s -silyl, which independently contains three C.4-C 6 -alkyl groups, which are optionally partially or fully halogenated ,

E" in each case independently means bromine, chlorine, fluorine, methoxy group, methylsulfonyl or nitrile, and)

Ez in each case independently means - phenyl, morpholino group, pyridinyl, pyrimidinyl, pyrrolidinyl, 2,5-pyrrolidinedionyl, imidazolyl, pyrazolyl, while each of the specified radicals is optionally substituted with 1-3 substituents selected from the group containing C-Salkyl, optionally partially or fully halogenated, halogen, oxo group, hydroxy group, nitrile and C--SalkyloxySalkoxy group, which is optionally partially or fully halogenated, o - C-Salkyl group or C-SalkoxySalkoxy group, which is optional Necessarily partially or fully halogenated He! or optionally substituted by the K.7 group, - OKuv or C.i-Czalkyl group, optionally substituted by the OK.c group, -- - amino group or mono- or di(C.--Czalkyl)amino group, optionally substituted by the group Ko, i- - Egos(O)(K 21)-, Kg20-, KozKodMS(O)-, KovSNo COM 21)- or KovS(O)SNo MK 21)-, - C--C.alkenyl, substituted by the group Kozko4MS(O)-, or - C.-C.alkynyl, substituted by pyrrolidinyl or pyrrolyl, and

Koz and Code together do not necessarily form a morpholino group. "

According to the following version of the invention, among those directly mentioned above, those of the compounds of formula (II), in ЯКкЙХ are the best. b means phenyl, pyridinyl, pyridonyl, naphthyl, quinolinyl, isoquinolinyl, dihydrobenzofuranyl, indanyl, and? indolinyl, indolonyl or indolinonyl, while C is substituted by one or more Ku, K» or BEZ groups,

Ag means 1-naphthyl,

X means phenyl, imidazolyl, pyridinyl, pyrimidinyl, piperidinyl, piperazinyl, pyridazinyl or pyrazinyl, -And Y means a bond or -CH»o-, -CHnoCH»-, -C(0)-, -O-, -5 -, -МН-СНоСНХСН»-, -МЩ(СНе)- or -MH-

Ki in each case independently means - - C3-Salkyl, which is optionally partially or fully halogenated and optionally substituted with phenyl,

Ge) - cyclopropyl, cyclopentanyl, cyclohexanyl or bicyclopentanyl, optionally substituted by 1-3 substituents, selected from the group containing methyl, which is optionally partially or fully halogenated, the CM group, hydroxymethyl and phenyl, or 2-tetrahydrofuranyl, substituted with methyl, or

He is trimethylsilyl,

Ez in each case independently means - phenyl, morpholinyl, pyridinyl, pyrimidinyl, pyrrolidinyl, 2,5-pyrrolidinedionyl, imidazolyl or pyrazolyl, while each of the indicated radicals is optionally substituted by C-C alkyl, optionally partially or fully halogenated ,

Ф) - C.-Szalkyl group or C--Szalkoxy group, each of which is optionally partially or completely halogenated or optionally substituted by a diethylamino group, - OKuv or C.i-Szalkyl, optionally substituted by a group OK in, in - an amino group or a mono- or di(C.--Salkyl) amino group, optionally substituted by a Co group, - СНЗС(О)МН-, К220-, КозКоМС(О)-, КовСНоС(О)М(К24)- or KovС(О)СНо MK) -, - C--C.alkenyl, substituted by the Kozko4MS(O)- group, or - C.-C.alkynyl, substituted by pyrrolidinyl or pyrrolyl,

Koz and Kod mean H or Koz and K24 together optionally form a morpholino group and 65 Eov means a morpholino group.

In another embodiment of the invention, the compounds of formula (I) are preferred among those directly indicated above,

in which b means phenyl, pyridinyl or naphthyl, while C is replaced by one or more groups K., K» or Kz,

X stands for imidazolyl or pyridinyl,

U means -СНо-, -МН-СНоОСНСН»- or -МН-, 27 means a morpholino group,

Ku in each case independently means tert-butyl, sec-butyl, tert-amyl or phenyl,

"ER" means chlorine and

Kz in each case independently means methyl, methoxy, methoxymethyl, hydroxypropyl, acetamide, 7/0 morpholino, or morpholinocarbonyl.

In the next embodiment of the invention, the compounds of formula (III) in which X stands for pyridinyl are preferred among those directly mentioned above.

According to another embodiment of the invention, the compounds of formula (III) in which pyridinyl is attached to Ag in the 3rd position of pyridinyl are preferred among those directly mentioned above.

As examples of compounds of formula (II) according to the invention, the following can be named: 1-(3-cyanophenyl)-3-I(4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1- (3-fluorophenyl)-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1--4-chloro-2-trifluoromethylphenyl)-3-I4-( b6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(2-chloro-5-trifluoromethylphenyl)-3-I4-(b6-morpholin-4-ylmethylpyridin-3-yl)naphthalene -1-yl|Urea, 1-(3,4-dimethylphenyl)-3-I(4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(3-iodophenyl )-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalene-1 -yl|-3-M-tolylurea, 1--4-methylsulfanylphenyl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(3-chloro -4-methylphenyl)-3-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, sc 1-(4-chloro-3-nitrophenyl)-3-I4-( b6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1--2,5-dichlorophenyl)-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalene -1-il| urea, and) 1-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|-3-naphthalen-2-ylurea, 1-(4-(b-morpholin-4-ylmethylpyridine) -3-yl)naphthalen-1-yl|-3-phenylurea, 1-(3-chlorophenyl)-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea . 4-ylmethylpyridin-3-yl)naphthalen-1-yl|-3-(2,4,6-trichlorophenyl)urea, o 1--2-methyl-3-nitrophenyl)-3-(4-(6-morpholine) -4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, Ge! 1-(4-methyl-2-nitrophenyl)-3-I(4-(6-morpholin-4-ylmethylgaridin-3-yl)naphthalen-1-yl|urea, 1--2,3-dichlorophenyl)-3 -I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, -- 1--2-methoxy-5-methylphenyl)-3-I4-(b6-morpholin-4 -ylmethylpyridin-3-yl)unaphthalin-1-yl|Urea, i- 1-(-2-chloro-6-methylphenyl)-3-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalene- 1-yl|urea, 1--2,4-dichlorophenyl)-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(4-methyl- C-nitrophenyl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1--2,4-dimethylphenyl)-3-I(4-(b6- morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, "1--2,3-dimethylphenyl)-3-I(4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalene- 1-yl|urea, with c 1-(4-cyanophenyl)-3-I(4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, . 1-(4-( b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|-3-(3,4,5-trimethoxyphenyl)urea, i?» 1-biphenyl-4-yl-3-I4-(6- Morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1--2,5-difluorophenyl)-3-I(4-(b6-morph Folin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1-(3-chloro-2-methoxyphenyl)-3-I(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalene -1-yl|urea, -I 1-(-2-fluoro-3-trifluoromethylphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1-- 4-benzyloxyphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-ylurea, - 1--2-methylsulfanylphenyl)-3-(4-(6-morpholin-4 -ylmethylpyridin-3-yl)naphthalen-1-yl|urea,

He) 1-(2-fluoro-6--rifluoromethylphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1--4-fluoro-3-trifluoromethylphenyl )-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, o 1-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1- yl|-3-(2,4,5-trimethylphenyl)urea,

Ge 1-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|-3-(4--rifluoromethylphenyl)urea, 1--3-methylsulfanylphenyl)-3-(4-( 6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1--2-methoxyphenyl)-3-I(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalene-1 -yl|urea, 1-(2-fluoro-5-trifluoromethylphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(4-methoxy-2 -methylphenyl)-3-I4-(β6-morpholin-4-ylmethylpyridin-3-yl)unaphthalin-1-yl|Urea,

F) 1-(2-fluoro-5-nitrophenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, ka 1-(4-ethoxyphenyl)-3- I(4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1--2,5-dimethoxyphenyl)-3-(4-(β-morpholin-4-ylmethylpyridin-3 -yl)naphthalen-1-yl|urea, in 1--4,5-dimethyl-2-nitrophenyl)-3-(4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl| Urea, 1-(5-chloro-2-methylphenyl)-3-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(2-isopropyl-bE-methylphenyl) )-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1--2-difluoromethoxyphenyl)-3-(4-(6-morpholin-4-ylmethylpyridin- 3-yl)naphthalen-1-yl|urea, 1-(4-isopropylphenyl)-3-(4-(b6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 65 1-- 4-methoxyphenyl)-3-I(4-(b-morpholin-4-ylmethyllyridin-3-yl)naphthalen-1-yl|urea, 1-(3-ethylphenyl)-3-I(4-(6-morpholine -4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea,

1-(2-ethoxyphenyl)-3-I(4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-"-4-butoxyphenyl)-3-I(4- (b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, ethyl ether 4-13-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl| -ureido)benzoic acid, 1--4-butyl-2-methylphenyl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1--2,6 -dibromo-4-isopropylphenyl)-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(3-methoxyphenyl)-3-I(4-( b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|-3--4- -rifluoromethylsulfanylphenyl)urea, 5-(3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl/ureido)isophthalic acid dimethyl ether, 70 1--3-cdcyclopentyloxy-4-methoxyphenyl) -3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, ethyl ether 3-(3-I4-(b-morpholin-4-ylmethylpyridin-3-yl) naphthalene-1-yl"ureido)benzoic acid, 1-(5-tert-butyl-2-hydroxyphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3 -yl)naphthalen-1-yl)urea, 1-(2-hydroxymethyl-4-phenylcyclohexyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1- -2-methylsulfanyl-5-trifluoromethylphenyl)-3-(4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1-(4-(β6-morpholin-4-ylmethylpyridin- 3-yl)naphthalen-1-yl|-3--4-pentyloxybiphenyl-3-yl)urea, methyl ether 4-methoxy-3-(3-I4-(b-morpholin-4-ylmethylpyridin-3-yl) naphthalene-1-yl"ureido)benzoic acid, 1--2,5-diethoxyphenyl)-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalene-1-yl|urea, 1- benzothiazol-b-yl-3-I4-(b6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea,

IM-(2,5-diethoxy-4-13-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-ylIureido)phenyl)benzamide, 1-(4-(b-morpholin-4- ylmethylpyridin-3-yl)naphthalen-1-yl|-3-(3-phenoxyphenyl)urea, 1-(5-ethanesulfonyl-2-methoxyphenyl)-3-I(4-(6-morpholin-4-ylmethylpyridin-Z -yl)naphthalen-1-yl|urea, 4-methoxy-3-(3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)ureido)-M-phenylbenzamide, 1- (-2-methyl-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl)-3-14-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl| with urea, with 1--2,3-dimethyl-1H-indol-5-yl)-3-14-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea,

M-butyl-4-methoxy-3-(3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)/ureido)benzenesulfonamide, and) 1-IZ3-(2-methyl- (/1,3|dioxolan-2-yl)phenyl|-3-I(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 1-(3-methoxy-5-trifluoromethylphenyl )-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1--2,4-dimethoxyphenyl)-3-(4-(b-morpholin-4- ylmethylpyridin-3-yl)naphthalene-1-ylurea, 1-(-2-methyl-4-nitrophenyl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalene-1 -yl|urea, 1-(2-methoxy-4-nitrophenyl)-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, about 1-(4- chloro-2-nitrophenyl)-3-I4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, He! 1-(5-chloro-2-methoxyphenyl)-3-I( 4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(3,5-dimethoxyphenyl)-3-(4-(b-morpholin-4-ylmethylpyridin-3-yl) )naphthalen-1-yl|urea, -- 1-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|-3--4-trifluoromethoxyphenyl)urea, and- 1-( 4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalene-1-i l|-3--3-Trifluoromethylsulfanylphenyl)urea, 1-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|-3-(2-phenoxy-phenyl)urea, 1- (2-Methoxy-5-nitrophenyl)-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(5-chloro-2,4-dimethoxyphenyl) -3-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(3,5-bitrifluoromethylphenyl)-3-14-(b-morpholin-4-ylmethylpyridine) -3-yl)naphthalen-1-yl)urea, with 1-(2-tert-butyl-5-methylpyridin-4-yl)-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl) naphthalene-1-yl|urea, . 1-(3-methylnaphthalen-2-yl)-3-14-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, y? 1-(3-tert-butylphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 1-(4-methylbiphenyl-3-yl)-3-I4 -(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1-(4-tert-butylbiphenyl-2-yl)-3-I4--b-morpholin-4-ylmethylpyridin-3 -yl)naphthalen-1-yl)urea, -I 1-(5-chloro-2,4-dimethoxyphenyl)-3-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl |urea, 1-(5-isopropyl-2-methylphenyl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, - 1-(5-tert-butyl -2-methoxyphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea,

Ge) 1-(5-tert-butyl-2-methoxy-3-propylphenyl)-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1-(5- tert-butyl-2-methoxymethylphenyl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, o 1-(5-tert-butyl-2-methoxyphenyl)- 3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea,

Ge 1-(5-tert-butyl-2-methylphenyl)-3-(4-16-((3-methoxy-propyl)methylamino|pyridin-3-ylnaphthalen-1-yl)urea, 1-(5-tert -butyl-2-methylphenyl)-3-I4-(4-morpholin-4-ylmethylimidazol-1-yl)naphthalen-1-yl)urea, 1-(5-tert-butyl-2-methylphenyl)-3-I4 -(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1-(5-tert-butyl-2-methylphenyl)-3-14-I6-(-3-methoxypropylamino)pyridine- 3-ylNaphthalin-1-yl)uretate, 1-(5-tert-butyl-2-methylpyridin-3-yl)-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl |Esechovin,

F) 1-(5-tert-butyl-2-morpholin-4-ylphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|)urea, ka 1-( b-tert-butyl-2-chloro-33-methylpyridin-4-yl)-3-I4-(b6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1-(4-( b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|-3-(3--fluoromethylphenyl)urea, in 1-(4-(b6-morpholin-4-ylmethylpyridin-3-yl)unaphtalsh- 1-yl|-3-"4-trifluoromethoxyphenyl)urea, 1-(5-(1,1-dimethylpropyl)-2-methoxyphenyl|-3-14-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalene -1-yl|Urea, 1-(b-tert-butyl-2-(1H-pyrazol-4-yl)phenyl)|-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalene -1-yl|Urea, 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)phenyl/1-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalene- 1-yl|urea, 65 1-Ib-tert-butyl-2-(3-hydroxypropyl)phenyl1|-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Iurea . and lysine, 1-(B-tert-butyl-2-(morpholine-4-carbonyl)phenyl/ |-3-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea y,

M-(5-tert-butyl-2-methoxy-3-13-14-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)ureido)phenyl)acetamide and their pharmaceutically acceptable derivatives.

In addition to the compounds given above as examples, the following possible compounds of formula (11) can also be obtained by the general synthesis methods described below: 1-I4-(6-Ibis(2-cyanoethyl)amino|methyl)pyridin-3-yl)naphthalen-1-yl |-3-(5-tert-butyl-2-methoxyphenyl)urea, 70 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(4-(-2-methyl-3-oxopiperazine-1) -ylmethyl)phenyl|naphthalen-1-yl)urea, 1-I4-(6-Tbis-(2-methoxyethyl)amino|methyl)pyridin-3-yl)naphthalen-1-yl|-3-(5-tert -butyl-2-methoxyphenyl)urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(6-(2-methyl-3-oxopiperazin-1-ylmethyl)pyridin-3-yl| naphthalene-1-yl)isoquinone, 1-(5-tert-butyl-2-methoxyphenyl)-3-74-(6-(1-oxo-114-thiomorpholin-4-ylmethyl)pyridin-3-yl|Inaphthalene -1-yl)urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-14-(b-thiomorpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-( 5-tert-butyl-2-methylphenyl)-3-14-I6-(1-oxo-I14-thiomorpholin-4-ylmethyl)pyridin-3-ylInaphthalen-1-ylurea, 1-(5-tert-butyl-2 -methylphenyl)-3-14-16-(2-methyl-3-oxopiperazin-1-ylmethyl)pyridin-3-yl|Inaphthalen-1-yl)use chows on, 7 1-(5-tert-butyl-2-methoxyphenyl)-3-74-(4-(1-oxo-11-thiomorpholin-4-ylmethyl)phenylInaphthalene-1-ylurea, 1-14-(4 -Tbis(2-cyanoethyl)amino|methyl)phenyl)naphthalen-1-ylI|-3-(5-tert-butyl-2-methoxyphenyl)urea, 1--2-methoxy-5-pentafluoroethylphenyl)-3-I4 -(4-morpholin-4-ylmethylpiperidin-1-yl)naphthalen-1-yl|Urea, 1--2-methoxy-5-trifluoromethylpyridin-3-yl)-3-14-(2-(4-oxopiperidin- 1-ylmethyl)pyrimidin-5-yl|Inaphthalen-1-yl)s s ov urea, 1--2-methoxy-5-trimethylsilanylphenyl)-3-14-I4-(tetrahydropyran-4-ylamino)phenyl|naphthalene- 1-yl)urea, and) 1-(3-methoxynaphthalen-2-yl)-3-(4-(4-morpholin-4-ylmethylpiperidin-1-yl)naphthalen-1-yl|urea, 1-(3 -methylnaphthalen-2-yl)-3-I(4-(4-morpholin-4-ylmethylphenyl)naphthalen-1-yl|urea, 1-(3-tert-butyl-5-methanesulfinylphenyl)-3-14-I6 -(1-methylpiperidin-4-ylmethyl)pyridin-3-yl|Inaphthalen-1-yl)urea, 1-(3-tert-butylphenyl)-3-I4-(3-pyridin-33-ylpropoxy) Naphthalin-1-yl|Urea, o 1-(3-tert-butylphenyl)-3-14-(4-morpholin-4-ylmethylphenyl)naphthalin-1-yl)urea, Ge! 1-(4-methoxybiphenyl-3-yl)-3-4-(4-(tetrahydropyran-4-ylmethyl)imidazol-1-yl|naphthalen-1-yl)urea, 1-(4-methylbiphenyl-3-yl) )-3-14-I4-(2-pyridin-4-ylethyl)piperazin-1-yl|Inaphthalen-1-yl)ridine, -- 1-(4-tert-butylbiphenyl-2-yl)-3-I4 -(pyridin-4-ylmethoxy)naphthalene-|-yl|urea, y- 1-(4-tert-butylbiphenyl-2-yl)-3-14-(2-(1-oxo-4-thiomorpholin-4- ylmethyl)-ZN-imidazol-4-yl|Inaphthalen-1-yl)retene, 1-(5-tert-butyl-2-hydroxyphenyl)-3-I4-(5-morpholin-(4-ylmethylpyrazin-2-yl) )naphthalen-1-yl|urea, 1-(5-tert-butyl-2-methoxy-3-propylphenyl)-3-(4-I(4-(pyrrolidin-1-carbonyl)phenyl)|naphthalen-1-yl )urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-I(4-(2-morpholin-4-ylmethylpyrimidin-5-yl)naphthalen-1-yl|Urea, « 1-(5- tert-butyl-2-methoxyphenyl)-3-I(4-(4-thiomorpholin-4-ylmethylphenyl)naphthalen-1-yl|urea, with c 1-(5-tert-butyl-2-methoxyphenyl)-3- 14-(b-morpholin-4-ylmethylphenyl)naphthalen-1-yl)urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-14-(4-(tetrahydropyran-4-ylamino)phenyl) 1-(5-tert-butyl-2-meth) oxyphenyl)-3-4-(6-(4-methylpiperazin-1-ylmethyl)pyridin-3-yl|Inaphthalen-|-yl) truncated, 1-(5-tert-butyl-2-methoxypyridin-3-yl) -3-4-(6-(4-oxopiperidin-1-ylmethyl)pyridin-3-ylInaphthalin-1-yl)usechov

МНВ, -І 1-(5-tert-butyl-2-methylbenzoxazol-7-yl)-3-І4-(6-pyridin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 1-( 5-tert-butyl-2-methylphenyl)-3-I4-(4-morpholin-4-ylmethylphenyl)naphthalen-1-yl|Urea, - 1-(5-tert-butyl-2-phenoxyphenyl)-3-4 -(b-(tetrahydropyran-4-yloxy)-pyridin-3-yl|Inaphthalen-1-yl) truncated,

Ge) 1-(5-tert-butyl-2-pyrrolidin-1-ylphenyl)-3-(4-(4-methoxy-6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|)urea

Wines, o 1-(5-tert-butyl-2-pyrrolidin-1-ylphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea,

Ge 1-(5-tert-butyl-3-cyano-2-methoxyphenyl)-3-14-(2-(2,6-dimethylmorpholin-4-ylmethyl)pyrimidin-5-yl)|naphthalene-1-yl )urea, 1-(5-tert-butyl-4"-dimethylaminobiphenyl-3-yl)-3-I4-(2-morpholin-4-ylmethylpyrimidin-5-yl)naphthalen-1-yl)urea na, 59 1 -(6-methoxy-3,3-dimethylindan-5-yl)-3-14-I(4-(morpholine-4-carbonyl)phenyl|naphthalen-1-yl) truncated,

F) 1-(b-tert-butyl-2-chloro-3-methylpyridin-4-yl)-3-I4-(b-thiomorpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea , 1-(b-tert-butylbenzo!|1,3|dioxo!-4-yl)-3-4-(b-"morpholin-4-ylamino)pyridin-3-ylInaphthalin-1-yl urea, in (7-methoxy-1,4,4-trimethyl-1,2,3,4-tetrahydroquinolin-b-yl)-3-14-Ib-(tetrahydropyran-4-yloxy)pyridin-3-yl naphthalene-1- yl)urea, 1-(7-tert-butyl-2,4-dimethyl-benzoxazol-5-yl)-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Iurea a, 1-(2-methoxy-5-(1-methyl-1-phenylethyl)phenyl/|-3-(4-16-(2-pyridin-4-ylethyl)pyridazin-3-yl|naphthalene-1- yl)urea, 65 1-(2-methoxy-5-(1-methylcyclohexyl)phenyl|-3-14-(4-(1-methylpiperidin-4-ylsulfanyl)phenyl|naphthalen-1-yl)urea wine,

1-(2-methoxy-5-(1-methylcyclopropyl)phenyl|-3-(4--2-morpholin-4-ylmethylpyrimidin-5-yl)naphthalen-1-yl|urea. 1-(2-methoxy- 5-(2-methyl-tetrahydrofuran-2-yl)phenyl|-3-I(4-(5-morpholin-4-ylmethylpyridin-2-yl)naphthalen-1-yl)urea, 1-(2-methoxy -5-(3-trifluoromethylbicyclo!|1.1.1|pent-1-iluphenyl)-3-(4-(4-morpholin-4-ylmethylphenyl)naphthalen-1-yl

Urea, 1-(3-tert-butyl-5-(1-methyl-1H-imidazol-4-yl)phenyl/|-3-14-(5-morpholin-4-ylmethylpyridin-2-yl)naphthalene-1 -yl|se urea, 1-13-tert-butyl-5-(2-pyrrolidin-1-ylethyl)phenyl1|-3-4-(6-(1-methylpiperidin-4-yloxy)pyridin-3-yl| Naphthalene-1-70yl)urea, 1-3-tert-butyl-5-(3-pyrrolidin-1-ylprop-1-ynyl)uphenyl|-3-14-(b-morpholin-4-ylmethylpyridin-3- yl)naphthalene-1-yl

Urea, 1-(4-(6-imidazol-1-ylmethylpyridin-3-yl)naphthalen-1-yl|-3-(2-methoxy-5-(1-phenylcyclopropyl)phenyl)|urea, 1-(5- (1,1-dimethylpropyl)-2-methoxyphenyl/|-3-I(4-(4-thiomorpholin-4-ylmethylphenyl)naphthalen-1-yl|urea, 1-(5-(1-cyanocyclopropyl)-2- methoxyphenyl|-3-(4-(2-morpholin-4-ylmethylpyrimidin-5-yl)naphthalen-1-yl|urea, 1-I5-(1-hydroxymethylcyclopropyl)-2-methoxyphenyl/|-3-I4-( 4-morpholin-4-ylmethylphenyl)naphthalen-1-yl|urea, 1-(b-tert-butyl-1-(2-diethylaminoethyl)-2-oxo-1,2-dihydropyridin-3-yl|-3- 14-I6-(1-Methylpiperidin-4-yloxy)pyridin-3-yl|Inaphthalin-1-yl)retinate, 1-(b-tert-butyl-2-(1H-pyrazol-4-yl)phenyl/ )|-3-(4-(2-morpholin-4-ylethoxy)naphthalen-1-yl)urea, 1-(b-tert-butyl-2-(1H-pyrazol-4-yl)phenyl)-3- 14-I4-(4-methylpiperazine-1-carbonyl)phenylInaphthalene-1-ylurea, 1-(b-tert-butyl-2-(2,5-dioxopyrrolidin-1-yl)uphenyl)-3-14-I6 -(1H-imidazol-2-ylmethyl)pyridin-3-ylInaphthalin-1-yl)urea, 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)phenyl/1-3-I4- (5-pyridin-4-ylmethylpyridin-2-yl)naphthalene- 1-yl)urea, 1-(b-tert-butyl-2-(2-morpholin-4-yl-2-oxoethoxy)phenyl/|-3-14-16-(2-pyridin-4-ylethyl)pyridazine -3-yl|Inaphthalene sc -1-yl)urea, 1-(b-tert-butyl-2-(2-morpholin-4-yl-2-oxoethylamino)phenyl/|-3-14-I(4- -1-methylpiperidin-4-ylamino)piperidin-1- i)yl|Inaphthalin-1-yl)urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)phenyl|-3- 4-(5-(2-pyrrolidin-1-ylethyl)pyridin-2-yl|Inaphthalen-1-yl)urea, c zo 1-(b-tert-butyl-2-methoxy-3-(3-morpholine) -4-yl-3-oxopropenyl)phenyl)-3-(4-(6-pyrrolidin-1-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, o 1-(b-tert-butyl-3 -(2-diethylaminoethoxy)-2-methoxyphenyl/|-3-14-14-(tetrahydropyran-4-yloxy)phenyl|naphthalene-1 Ge! -yl) truncated, 1-(b-tert-butyl-3-(2-pyrrolidin-1-ylethyl)benzofuran-7-yl|-3-(4--4-morpholin-4-ylmethylphenyl)naphthalene-1- Il|Sec --

Зз5 OvIyNa, cha 1-(b-tert-butyl-4-(2-dimethylaminoethyl)-3-oxo-3,4-dihydro-2H-benzo|1,oxazin-8-yl|-3-14-Ib- (thiomorpholin-4-ylamino)pyridin-3-yl|Inaphthalin-1-yl)urea, 1--5-tert-butyl-2-methoxy-3-(2-(1-methylpiperidin-4-yloxy)ethyl| phenyl)-3-(4-(4-morpholin-4-ylmethylphenyl)naphthalin-1-yl)urea, " 2-(4-tert-butyl-2-13-14-(5-pyrrolidin-1-ylmethylpyridine) -2-yl)naphthalen-1-yl)/ureido)phenoxy)-M-methylacetamide, with 2-ID-tert-butyl-2-(3-4-(6-(2,6-dimethylmorpholine-4- ylmethyl)-pyridin-3-yl|Inaphthalene-1-ylureido)phenoxy|aceta

MED, ; » 3-(5-tert-butyl-2-methoxy-3-(3-I4-(b-pyrrolidin-1-ylmethylpyridin-3-yl)naphthalen-1-yl/"ureido)phenyl)acrylamide, 3-IZ -tert-butyl-5-|3-(4-(4-(2-(1-oxo-114-thiazolidin-33-yl)ethyl|phenyl]inanaphthalen-1-yl)ureido|phenyl)-M,M-dimeth ylpropionamide, -I 3-14-I3-(5-tert-butyl-2-methoxyphenyl)ureido|naphthalen-1-yl)benzamide, 4-tert-butyl-2-13-I4-(-2-chloro-4 -morpholin-4-ylmethylphenyl)naphthalene-1-ylureido)benzamide, - M-(4-tert-butyl-2-13-(4-(6-oxo-1,6-dihydropyridin-3-yl)naphthalene-1 -ylureido)phenyl)-2-morpholine-4-ylacetamide,

Ge) IM-13-tert-butyl-5-(3-14-15-(tetrahydropyran-4-ylamino)pyridin-2-yl|naphthalen-1-yl)ureido)phenyl|-2-morpholine-4-ylacetamide .

He and their pharmaceutically acceptable derivatives.

According to another embodiment of the invention, it also offers the following compounds of formula (11): 1-(2-tert-butyl-5-methylpyridin-4-yl)-3-I4-(6-morpholin-4-ylmethylpyridin-3 -yl)naphthalen-1-yl|Iurea, 1-(3-methylnaphthalen-2-yl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1- (3-tert-butylphenyl)-3-I4-(4-morpholin-4-ylmethylphenyl)naphthalen-1-yl)urea,

F) 1-(3-tert-butylphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, ka 1--4-methylbiphenyl-3-yl)- 3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1-(4-tert-butylbiphenyl-2-yl)-3-(4--b-morpholin-4 -ylmethylpyridin-3-yl)naphthalen-1-yl)urea, in 1-(5-chloro-2,4-dimethoxyphenyl)-3-(4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalene- 1-yl)urea, 1-(5-isopropyl-2-methylphenyl)-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(5- t-butyl-2-methoxyphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(5-tert-butyl-2-methoxy-3-propylphenyl )-3-I4-(6b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(5-tert-butyl-2-methoxymethylphenyl)-3-(4-(6-morpholine -4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 65 1-(5-tert-butyl-2-methoxyphenyl)-3-I(4-(2-morpholin-4-ylmethylpyrimidin-5-yl )naphthalen-1-yl|urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-I(4-(4-thiomorpholin-4-ylmethylphenyl)naphthalen-1-yl|urea,

1-(5-tert-butyl-2-methoxyphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 1-(5-tert-butyl-2- methoxyphenyl)-3-I4-(b-morpholin-4-ylmethylphenyl)naphthalen-1-yl)urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-14-(4-(tetrahydropyran-4- ylamino)phenyl|naphthalen-1-yl)trunate, 1-(5-tert-butyl-2-methoxyphenyl)-3-74-(6-(4-methylpiperazin-1-ylmethyl)pyridin-3-yl|naphthalene- 1-yl)urea, 1-(5-tert-butyl-2-methylphenyl)-3-(4-16-((3-methoxypropyl)methylamino|pyridin-3-yl-naphthalen-1-yl)urea, 1 -(5-tert-butyl-2-methylphenyl)-3-I4-(4-morpholin-4-ylmethylimidazol-1-yl)naphthalen-1-yl)urea, 1-(5-tert-butyl-2-methylphenyl) )-3-I4-(4-morpholin-4-ylmethylphenyl)naphthalen-1-yl|Urea, 1-(5-tert-butyl-2-methylphenyl)-3-I4-(6-morpholin-4-ylmethylpyridin- 3-yl)naphthalen-1-yl|urea, 70 1-(5-tert-butyl-2-methylphenyl)-3-14-I6-(-3-methoxypropylamino)pyridin-3-yl|Inaphthalen-1-yl )urea, 1-(5-tert-butyl-2-methylpyridin-3-yl)-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Iurea, 1-(5 -tert-butyl-2-morpholine-4-i lphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-chloro-3-methylpyridin-4-yl)- 3-I4-(b6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-chloro-3-methylpyridin-4-yl)-3-I4 -(b-thiomorpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea na, 9 1-(2-methoxy-5-(1-methylcyclopropyl)phenyl|-3-(4--2-morpholine) -4-ylmethylpyrimidin-5-yl)naphthalen-1-yl|urea, 1-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|-3-(3-trifluoromethylphenyl) )urea, 1-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|-3-(4--riftomethoxyphenyl)urea, 1-(5-(1,1-dimethylpropyl) -2-methoxyphenyl/|-3-I(4-(4-thiomorpholin-4-ylmethylphenyl)naphthalen-1-yl|urea, 1-(5-(1,1-dimethylpropyl)-2-methoxyphenyl/|-3 -I4-(b6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Iurea, 1-(5-(1-cyanocyclopropyl)-2-methoxyphenyl|-3-(4-(2-morpholin- 4-ylmethylpyrimidin-5-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(1H-pyrazol-4-yl)phenyl/)|-3-(4-(6-morpholine) -4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)phenyl/1-3-I4-(5-pyridin-4-ylmethylpyridin-2-yl)naphthalen-1-yl)urea, 1 -(b-tert-butyl-2-(2-methylpyrimidin-5-yl)phenyl)1-3-14-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, that 1-(b-tert-butyl-2-(3-hydroxypropyl)phenyl/|-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-|-yl|Urea, and) 1- (b-tert-butyl-2-(3-morpholin-4-yl-3-oxopropyl)phenyl1-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl

Urea, 1-(b-tert-butyl-2-(morpholin-4-carbonyl)phenyl1|-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea c a, that 2-ID-tert-butyl-2-(3-4-(6-(2,6-dimethylmorpholin-4-ylmethyl)pyridin-3-ylnaphthalen-1-yl)ureido)phenoxy|acetamide, Ge» ) 3-14-I3-(5-tert-butyl-2-methoxyphenyl)ureido|naphthalen-1-yl)benzamide, d-tert-butyl-2-(3-I4-(2-chloro-4-morpholine- 4-ylmethylphenyl)naphthalene-1-yl)ureido)benzamide and their pharmaceutically acceptable derivatives.

In another embodiment of the invention, it further proposes the following compounds of formula (II): 1-(2-tert-butyl-5-methylpyridin-4-yl)-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl) )naphthalen-1-yl|Iurea, 1-(3-tert-butylphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 1--4-methylbiphenyl -3-yl)-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Iurea, « 1-(4-tert-butylbiphenyl-2-yl)-3-(4 --b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, with c 1-(5-isopropyl-2-methylphenyl)-3-I(4-(6-morpholin-4-ylmethylpyridine -3-yl)naphthalen-1-yl|urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-14-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl 1-(5-tert-butyl-2-methoxymethylphenyl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 1-(5 -tert-butyl-2-methoxyphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 1-(5-tert-butyl-2-methylphenyl)-3 -(4-6-((3-methoxypropyl)methylamino|pyridin-3-ylnaphthalen-1-yl)urea, -I 1-(5-tert-butyl-2-methylphenyl)-3-I4-(6-mor folin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(5-tert-butyl-2-methylpyridin-3-yl)-3-I4-(6-morpholin-4-ylmethylpyridin-3 -yl)naphthalen-1-yl|Iurea, - 1-(5-(1,1-dimethylpropyl)-2-methoxyphenyl/|-3-I4-(b6-morpholin-4-ylmethylpyridin-3-yl)naphthalene- 1-il|Urea,

Ge) 1-(b-tert-butyl-2-(1H-pyrazol-4-yl)phenyl)|-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl |urea, sl 50 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)phenyl/1-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalene-1- Il|Sechov ina,

Ge 1-(b-tert-butyl-2-(3-hydroxypropyl)phenyl1|-3-I4-(6b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(b- tert-butyl-2-(morpholin-4-carbonyl)phenyl1|-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea a,

M-(5-tert-butyl-2-methoxy-3-(3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)/ureido)phenyl)acetamide and their pharmaceutical acceptable derivatives. (Ф, The fourth object of the invention is compounds of formula (ІІІ):

E means carbon or a heteroatom-containing group selected from -O-, -MH- and -5-, o means 65 - aromatic Ce-Siocarbocycle or saturated or unsaturated unsaturated C5-Socarbocycle,

- 6-14-ene monocyclic, bicyclic or tricyclic heteroaryl, containing one or more heteroatoms selected from O, M and 5, - 6-in-ene monocyclic heterocycle, containing one or more heteroatoms selected from 0, M and 5, or - an 8-11-ene bicyclic heterocycle containing one or more heteroatoms selected from O, Mi 5, while OS is optionally substituted by one or more K., K» or Kz groups,

Ag is phenyl, naphthyl, quinolinyl, isoquinolinyl, tetrahydronaphthyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, benzimidazolyl, benzofuranyl, dihydrobenzofuranyl, indolinyl, benzothienyl, dihydrobenzothienyl, indanyl, indenyl or indolyl, each optionally substituted with one or more 7/0 K groups, or Kb,

X means - СвБ-Свcycloalkyl or cycloalkenyl, optionally substituted by 1-2 oxo groups or 1-3 С 4-С;.alkyl,

C.-C.Alkoxy- or C.-C.Alkylamino chains, each of which is branched or unbranched, - aryl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, pyridinyl, pyrimidinyl, pyridinonyl, dihydropyridinonyl, maleimidyl, dihydromaleimidyl, piperidinyl, benzimidazole , ЗН-imidazo|4,5-р|Ipyridine, piperazinyl, pyridazinyl or pyrazinyl, each of which is optionally independently substituted with 1-3 substituents selected from the group containing C -C alkyl, C 1 -C alkyl, hydroxy group, nitrile, amino group, mono- or di(C1-C6alkyl)amino group, mono- or di(C1-C6alkylamino)carbonyl, MNHC(O) group, C1-C6alkyl-3(O)t group halogen,

M means a bond or saturated or unsaturated, branched or unbranched C 4-C; a carbon chain, optionally partially or fully halogenated, while one or more C atoms are optionally replaced by O, M, or 5(O)uu, and X is optionally independently substituted with 1-2 oxo groups, nitrile, or phenyl by one or more C.i.-C.alkyl groups, optionally substituted by one or more halogen atoms, c 2 means aryl, heteroaryl selected from pyridinyl, piperazinyl, piperimidinyl, pyridazinyl, pyrazinyl, i) imidazolyl, pyrazolyl, triazolyl, tetrazolyl , furanyl, thienyl and pyranyl, a heterocycle selected from tetrahydropyrimidonyl, cyclohexanonyl, cyclohexanolyl, 2-oxa- or /2-thia-5-azabicyclo|2.2.1)heptanyl, pentamethylenesulfidyl, pentamethylenesulfoxidyl, pentamethylenesulfonyl, tetramethylenesulfidyl, tetramethylenesulfoxidyl or tetramethylenesulfonyl ) piperidinyl, piperidinonyl, pyrrolidinyl, and dioxolanyl, with each of the above 72 groups being optionally substituted with 1-3 substituents selected from the group consisting of halogen, C 4-Salkyl, C-Salkyl, C-4-Salkyl -C41-Salkyl, C-Salkyloxycarbonyl, (7-aroyl, C-Salkyl, oxo group, hydroxy group, pyridinyl-C-Salkyl, imidazolyl-C-Salkyl, tetrahydrofuranyl-C-Salkyl, nitrile-C-Salkyl , nitrile, carboxy group, phenyl, where the phenyl ring is optionally replaced by 1-2 halogen atoms, C-Salkyl-Z(O) 1 and the phenyl-5(O).2 group, where the phenyl ring is optionally substituted with 1-2 halogen atoms, C.-Salkoxy groups, hydroxy groups or MOono- or "

BY(C-Salkyl) amino groups, with C or 7 optionally substituted by 1-3 amino groups or amino-C/-Salkyl groups, while the M-atom is optionally independently mono- or disubstituted by amino 4-Salkyl, C.- -Szalkilom, arilo-Szalkilom, ;" C.i-Salkoxyi-Salkyl, C.--Salkoxy group, aroyl, C.--Szacyl, C.-alkyl-C3(O)»p-group or aryl-Salkyl-B(O)»t-, at each of the mentioned alkyls and aryls attached to the amino group is optionally substituted by 1-2 halogen atoms, C41-Salkyl groups or C.-Salkyloxy groups, -I or 7 is optionally substituted by 1-3 aryl groups, heterocyclic or heteroaryl groups , described above in this paragraph, while each of the specified groups in turn is optionally substituted - by a halogen, Si-Svalkyl or C.-Svalkoxy group,

Ge) or 7 means a hydroxy group, a halogen, a nitrile, an amino group, where the M-atom is not necessarily independently mono- or disubstituted by C.i-Szacyl, C.--Salkyl or C.-Szalkoxy-Szalky, branched or unbranched about Si- Svalkyl, C.--Svalkoxy group, S.i-Szacylamino group, nitrileO.-Slalkyl, C.--Svalkyl-Z(O) group". group or

He phenyl-B(O),t, where the phenyl ring is optionally substituted with 1-2 halogen atoms, C 4-Salkyloxy groups, hydroxy groups or mono- or di(C.--Salkyl)amino groups,

Ki in each case independently means 5B branched or unbranched C-C alkyl, which is optionally partially or fully halogenated, with one or more C atoms optionally independently replaced by O, M or 5(O) t, and S. Siralkil is indicated

F) optionally substituted with 1-3 substituents selected from the group containing C 3 -C 3 -cycloalkyl, hydroxy group, ka oxo group, phenyl, naphthyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, pyrrolidinyl, imidazolyl, pyrazolyl, thienyl , furyl, dioxolanyl, isoxazolyl, and isothiazolyl, and each of the specified substituents is optionally substituted with 1-5 substituents selected from halogen, C.-alkyl, which is optionally partially or fully halogenated, C3-sacycloalkanyl, C5-sacycloalkenyl, a hydroxy group, a nitrile, a C.--C-alkyloxy group, which is optionally partially or fully halogenated, a MH 25C(0O) group, a mono- or di(C.--C-alkyl)amino group and a mono- or di(C.-C-alkyl)aminocarbonyl . not necessarily in part or by fully halogenated,

nitrile, hydroxyC.--Alkyl and aryl, or an analogue of such a cycloalkyl group, in which 1-3 ring methylene groups are independently replaced by O, (0), CHOH, »C-0, 2-5 or MH, - a phenyloxy group or a benzyloxy group , each of which is optionally partially or fully halogenated and optionally substituted with 1-3 substituents selected from the group consisting of C 4-S alkyl, which is optionally partially or fully halogenated, nitrile, hydroxyC 4-S alkyl, and aryl, or an analogue of such a cycloaryl group in which 1-2 ring methylene groups are independently replaced by M, - cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, bicyclopentanyl, bicyclohexanyl or bicycloheptanyl, each of which is optionally partially or fully halogenated and optionally substituted with 1-3 70 substituents selected from the group consisting of C--C alkyl, which is optionally partially or fully halogenated, nitrile, hydroxyC--C alkyl, and aryl, or an analog of such a cycloalkyl group in which 1-3 ring methylene groups are independently replaced by О, З(О)у, СНОН, »С-0, 2-5 or МН, - branched or unbranched C3-Siralkenyl, which in each case is optionally partially or fully halogenated and optionally substituted with 1-3 substituents, selected from the group consisting of branched and unbranched C.i-Svalkyl, phenyl, naphthyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, imidazolyl, pyrazolyl, thienyl, furyl, isoxazolyl and isothiazolyl, while each of the specified substituents is substituted with 1- 5 substituents selected from the group containing halogen, C4i-Salkyl, which is optionally partially or fully halogenated, cyclopropanyl, cyclobutanyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, bicyclopentanyl, bicyclohexanyl or bicycloheptanyl, hydroxy, nitrile, C1-Salkyloxy, neoob' necessarily partially or fully halogenated, the MH»C(O) group and mono- or di(C.4-Salkyl)aminocarbonyl, while the specified branched or unbranched C3-Siralkenyl is optionally interrupted by one or more heteroatoms selected with 0, M and (Ot, - cyclopentenyl, cyclohexenyl, cyclohexadienyl, cycloheptenyl, cycloheptadienyl, bicyclohexenyl or bicycloheptenyl, while this cycloalkenyl group is optionally substituted by 1-3 C.i.C. alkyl groups, ch - an oxo group, nitrile, halogen, - silyl, containing three C.-C; alkyl groups, optionally partially or fully halogenated, or i) - C3-Alkynyl branched or unbranched carbon chain, optionally partially or fully halogenated, with one or more methylene groups are optionally replaced by OO, MH or 5(O)m, and the specified alkynyl group is optionally independently substituted by 1-2 oxo groups, a hydroxy group, pyrrolidinyl, c

With pyrrolyl, tetrahydropyranyl, one or more C.-C.alkyl groups, optionally substituted by several halogen atoms, nitrile, morpholino group, piperidinyl, piperazinyl, imidazolyl, phenyl, pyridinyl, tetrazolyl or mono- or di(C .i-Szalkyl)amino group, not necessarily Ge! substituted by one or more halogen atoms,

РЕ», B, and B5 each means -- - branched or unbranched Si-Svalkyl, which is not necessarily partially or fully halogenated, cha

C.Svacyl, aroyl, branched or unbranched C4-C.Alkoxy group, in each case optionally partially or fully halogenated, halogen, methoxycarbonyl, C-Salkyl-B(O)t group, which is optionally partially or fully halogenated , or a phenyl-Z(O)t group, - Oho, a C-Sulfoxy group, a hydroxy group, a nitrile, a nitro group, or a halogen " - an amino-5(O),1- group, where the M-atom is not necessarily independently mono- or disubstituted by C-Salkyl or pt) with aryl-Salkyl, or an amino group, where the M-atom is not necessarily independently mono- or disubstituted by C.-Salkyl, . by aryl-Szalkyl, C--Svacyl, by the group S.i-Svalkyl-Z(O) by an n-group or by aryl-Szalkyl-Z(O)t-, while each of y? alkyls and aryls specified in this paragraph are optionally partially or fully halogenated and optionally substituted with 1-2 C-Salkyl groups or C-Salkyloxy groups,

Ez in each case independently means -I - phenyl, naphthyl, morpholino group, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, pyrrolidinyl, imidazolyl, pyrazolyl, thiazolyl, oxazolyl, (1,3,oxadiazole, triazolyl, tetrazolyl, thienyl, furyl, - tetrahydrofuryl, isoxazolyl, isothiazolyl, quinolinyl, isoquinolinyl, indolyl, benzimidazolyl, benzofuranyl,

He) benzoxazolyl, benzisoxazolyl, benzpyrazolyl, benzothiofuranyl, cinolinyl, pterindinyl, phthalazinyl, 5-or naphthylpyridinyl, quinoxalinyl, quinazolinyl, purinyl or indazolyl, while each of the above radicals is optionally substituted with 1-3 substituents selected from the group containing phenyl , naphthyl, heterocycle or

Heteroaryl described in this paragraph, branched or unbranched C-Swalalkyl, which is optionally partially or fully halogenated, cyclopropanyl, cyclobutanyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, bicyclopentanyl, bicyclohexanyl, bicycloheptanyl, phenyl-S-Swalalkyl, naphthyl -C.-Salkyl, halogen, or phydroxy group, oxo group, nitrile, C.-C.AlkoxyC.alkyloxy group, which is optionally partially or fully halogenated, phenyloxy group, naphthyloxy group, heteroaryloxy group or heterocyclooxy group, where (F, heterocyclic or heteroaryl fragment is described above in in this paragraph, a nitro group, an amino group, a mono- or cad(C1-C alkyl)amino group, a phenylamino group, a naphthylamino group, a heteroarylamino group, or a heterocyclamino group, where the heterocyclic or heteroaryl moiety is described above in this paragraph, a MNHS(O) group, a mono- or bo di( C1-Salkyl) aminocarbonyl, C.-Salkyl-C(O0)-C.-Salkyl, amino-C.--Salkyl, mMono- or di(Ci-Salkyl) amino group, mono- or di(C.i-Salkyl )amino-S.--Szalkyl, ami group no- 5(0)", di(C.4-Salkyl)amino-5(O)2 group, KU-C4-Salkyl, Ka-C--Salkyloxy group, Ka-C(0)-C4-Salkyl, group K/o-C4-Salkyl(K 44)M and carboxy-mono- or di(C.--Salkyl)amino group, - kCondensed aryl selected from benzocyclobutanyl, indanyl, indenyl, dihydronaphthyl, 65 Tetrahydronaphthyl, benzocycloheptanyl and benzocycloheptenyl, or fused heteroaryl selected from cyclopentenopyridinyl, cyclohexanopyridinyl, cyclopentanopyrimidinyl, cyclohexanopyrimidinyl,

циклопентанопіразинілу, циклогексанопіразинілу, циклопентанопіридазинілу, циклогексанопіридазинілу, циклопентанохінолінілу, циклогексанохінолінілу, циклопентаноізохінолінілу, циклогексаноізохінолінілу, циклопентаноіндолілу, циклогексаноіндолілу, циклопентанобензімідазолілу, циклогексанобензімідазолілу, циклопентанобензоксазолілу, циклогексанобензоксазолілу, циклопентаноімідазолілу, циклогексаноімідазолілу, циклопентанотієнілу і циклогексанотієнілу, при цьому зазначене конденсоване арильне чи конденсоване гетероарильне кільце незалежно заміщено 0-3 substituents selected from the group consisting of phenyl, naphthyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, imidazolyl, pyrazolyl, thienyl, furyl, isoxazolyl, isothiazolyl, C.i.sylalkyl, which is optionally partially or fully halogenated, halogen , nitrile, 7/0. C41-C6alkyloxyC zalkoxy group, optionally partially or fully halogenated, phenyloxy group, naphthyloxy group, heteroaryloxy group or heterocyclooxy group, where the heteroaryl or heterocyclic moiety is described above in this paragraph, a nitro group, an amino group, a mono- or di(C.--C6alkyl)amino group, a phenylamino group , a naphthylamino group, a heteroarylamino group or a heterocyclamino group, where the heteroaryl or heterocyclic fragment is described above in this paragraph, the group МНХЬС(О), mono- or 75. DY(C.-Salkyl)aminocarbonyl, the group C-Slalkyl-OC(O), C- Svalkyl-C(O)-C4-C.alkyl, amino-Ci-Svalkyl, mono- or di(C4-C3)alkylamino-Si-Svalkyl, K./2-Si-Svalkyl, C.i3-Si-- Svalkoxy group, K.A-C(0)-S.-Svalkil and group

Ки5-С4-SvalkylkK 46) M - cyclopropanyl, cyclobutanyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, bicyclopentanyl, bicyclohexanyl or bicycloheptanyl, each of which is optionally partially or fully halogenated and optionally substituted with 1-3 C and -C alkyl groups, or an analogue of such a cycloalkyl group, in which 1-3 ring methylene groups are independently replaced by O, 5, CHOH, 2С-0, 2-5 or МН, is cyclopentenyl, cyclohexenyl, cyclohexadienyl, cycloheptenyl, cycloheptadienyl, bicyclohexenyl or bicycloheptenyl, each of which optionally substituted by 1-3 C.-C alkyl groups, - C4-Alkylphenyl-C(0)-C4-C; alkyl-, C4-C; alkyl-C(O)-C4-C; alkyl- or C- C;alkylphenyl-Z(O)t-C4-C;alkyl-, ch - a C-Salkyl group or a branched or unbranched C.i-Salkyloxy group, each of which is optionally partially or fully halogenated or optionally substituted by a K group .»7, i) - OKuv or C-Svalkyl, optionally substituted by the group OK in, - amino group or mono- or di(C.-Svalkyl)amino group, optionally substituted by the group Ko, - 0 Koob(О0М(Кой)-, о Ko20-, Koza MO(0)-, Koz(СНо)m(О)М(К 21)-, KozК24МО(0)-Si-Szalkoxygroup or suzo VoS (ОХСН (Во), - Со-Свалкеныл, substituted by the group KozКо4МС(О)-, о - С2-Свалкыныл branched or unbranched carbon chain, optionally partially or completely (33 halogenated, while one or more methylene groups are optional replaced by 0, МН, 5(О) t, and the specified alkynyl group is optionally independently substituted by 1-2 oxo groups, pyrrolidinyl, pyrrolyl, -- morpholino group, piperidinyl, piperazinyl, imidazolyl, phenyl, pyridinyl, tetrazolyl, one or more by several C.-C.alkyl groups optionally substituted by one or more halogen atoms, nitrile, morpholino group, piperidinyl, piperazinyl, imidazolyl, phenyl, pyridinyl, tetrazolyl or mono- or di(C.-C.alkyl)amino group, optionally substituted by one or more halogen atoms, - Si-Svacyl or aroyl, "

Ke means C.-C. alkyl, which is optionally partially or fully halogenated and optionally substituted with the Kev group. EK, Ka, Ka, Kcho, Ki", Kis, Kia, Kv, K4i7, Kv, Kov and Kov each independently of each other means nitrile, phenyl, and?" a morpholino group, piperidinyl, piperazinyl, imidazolyl, pyridinyl, tetrazolyl, an amino group, or a mono- or di(C4-Slalkyl)aminoC zalkoxy group, optionally partially or fully halogenated,

Ku44 Her Kv each, independently of each other, means hydrogen or C.-C., alkyl, which is not necessarily partially or -I fully halogenated,

Kv in each case independently means hydrogen or C-C alkyl, which is not necessarily independently substituted - by an oxo group or a Kov group,

Ge) Coo in each case independently means C-Cyralalkyl, which is not necessarily partially or fully halogenated, phenyl or pyridinyl, and Co2i in each case independently means hydrogen or C-Cyralalkyl, which is optionally partially or completely

With halogenated,

Ko", Koz and Kod each independently of each other means hydrogen, C--Svalkyl, which is not necessarily partially or fully halogenated, while said C.-Svalkyl is optionally interrupted by one or more O, M or 5 atoms, and also independently optionally substituted by mono- or di(C 41-C alkyl)aminocarbonyl, phenyl, pyridinyl, amino group or mono- or di(C 1-C alkyl)amino group, and each of the specified (F, radicals) optionally partially or fully halogenated and optionally substituted with a mono- or di(C1-C6alkyl)amino group, or

Coz and Cod together optionally form a heterocyclic or heteroaryl ring, where t means 0, 1 or 2 and

M stands for O or 5, and pharmaceutically acceptable derivatives thereof.

In another embodiment of the invention, the compounds of formula (III) in which

E means -CH»-, -MH- or -O-, 65 M means O and o means

- phenyl, naphthyl, benzocyclobutanyl, dihydronaphthyl, tetrahydronaphthyl, benzocycloheptanyl, benzocycloheptenyl, indanyl, indenyl, - pyridinyl, pyridonyl, quinolinyl, dihydroquinolinyl, tetrahydroquinoyl, isoquinolinyl, tetrahydroisoquinoyl, pyridazinyl, pyrimidinyl, pyrazinyl, benzoimidazolyl, benzofuranazolyl, benzothiazolyl, benzothiazolyl benzpyrazolyl, dihydrobenzofuranyl, dibenzofuranyl, dihydrobenzothiophenyl, benzooxazolonyl, benzo|1,Zoxazin-3-onyl, benzodioxolyl, benzo|1,3|dioxol-2-onyl, benzofuran-Z-onyl, tetrahydrobenzopyranyl, indolyl, 2,3-dihydro- 1H-indolyl, indolinyl, indolonyl, indolinonyl, phthalimidyl, - oxetanyl, pyrrolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, piperidinyl, piperazinyl, morpholino, 7/o tetrahydropyranyl, dioxanil, tetramethylenesulfonyl, tetramethylenesulfoxidyl, oxazolinyl, 3,4-dihydro-2H-benzo| 1, oxazinyl, thiazolinyl, imidazolinyl, tetrahydropyridinyl, homopiperidinyl, pyrrolinyl, tetrahydropyrimidinyl, decahydroquinolinyl, decahydroisoquinolinyl, a thiomorpholino group, thiazolidinyl, dihydrooxazinyl, dihydropyranyl, oxocanyl, heptacanyl, thioxanyl or dithianyl, while C is optionally substituted by one or more Ku, K» or Kz groups.

According to another embodiment of the invention, the compounds of formula (II) in which

E means -MH-, b means phenyl, pyridinyl, pyridonyl, naphthyl, quinolinyl, isoquinolinyl, pyrazinyl, benzimidazolyl, benzooxazolyl, benzooxazolonyl, benzofuranyl, benzothiophenyl, benzopyrazolyl, dihydrobenzofuranyl, dihydrobenzothiophenyl, 3,4-dihydro-2H-benzo|1, Stoxazinyl, indanyl, indenyl, indolyl, indolinyl, indolonyl, 2,3-dihydro-1H-indolyl or indolinonyl, while C is optionally substituted by one or more groups K., Ko» or Kz,

Ag means naphthyl, quinolinyl, isoquinolinyl, tetrahydronaphthyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, indanyl, indenyl or indolyl, each of which is optionally substituted by one or more groups K, or K5,

X represents phenyl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, pyridinyl, pyrimidinyl, pyridinonyl, (8) dihydropyridinonyl, maleimidyl, dihydromaleimidyl, piperidinyl, piperazinyl, pyridazinyl or pyrazinyl, each of which is optionally independently substituted with 1-3 substituents, selected from the group containing C1-C1-alkyl,

C.-C.alkyl group, hydroxy group, nitrile, amino group, mono- or di(C.-C alkyl)amino group, mono- or c.iso(C.1-C alkylamino)carbonyl, MNHC(O) group, C-C alkyl group -B(O) n and halogen,

U means a bond or a saturated or unsaturated C 4-C 4 carbon chain, where one or more C atoms o are optionally replaced by 0, M or З(О)t, and X is optionally independently substituted by 1-2 oxo groups , nitrile, or Ge! phenyl with one or more C1-C6 alkyl groups optionally substituted with one or more halogen atoms, -- 2 means phenyl, heteroaryl selected from pyridinyl, piperazinyl, pyrimidinyl, pyridazinyl, pyrazinyl, imidazolyl, furanyl, thienyl and pyranyl, a heterocycle selected from 2-oxa-5-azabicyclo|2.2.1|Iheptanyl, tetrahydropyrimidonyl, pentamethylenesulfidyl, pentamethylenesulfoxidyl, pentamethylenesulfonyl, tetramethylenesulfidyl, tetramethylenesulfoxidyl, tetramethylenesulfonyl, tetrahydropyranyl, tetrahydrofuranyl, 1,3-dioxolanonyl, 1,3- dioxanonyl, 1,4-dioxanyl, morpholino group, thiomorpholino group, Che) with thiomorpholino sulfoxidyl, piperidinyl, piperidinonyl, dihydrothiazolyl, dihydrothiazolyl sulfoxidyl, . pyrrolidinyl and dioxolanyl, each of which is optionally substituted with 1-3 substituents selected from the group where includes nitrile, C1-C6alkyl, C1-C6alkyl, amino group, mono- or di(C1-C6alkyl)amino group, COMH group and OH group, or 7 is optionally substituted with phenyl, heterocycle or heteroaryl as defined above in this -I paragraph, each of which in turn is optionally substituted by a halogen, C.4-Salkyl or C.-Salkyloxy group, or 7 means nitrile, nitrileC.--Salkyl, group C.--Salkyl-Z(O )»t, halogen, hydroxy group, C.-C alkyl, - C.-C zacylamino group, C.-C. alkoxy group, amino group, mono- or di(C.-C alkyl aminocarbonyl or amino group,

Ge) mono- or disubstituted aminoC.--Salkyl or C.-S-alkoxyC-S-alkyl,

Ki in each case independently means o - branched or unbranched S.-Svalkil, which is not necessarily partially or fully halogenated, when

Here, one or more C atoms are optionally independently replaced by O, M, or 5(0O) pt, and the specified C.Swalkyl is optionally substituted by 1-3 substituents selected from the group containing C.sub.-Swicycloalkyl, an oxo group, phenyl, dioxolanyl, pyrrolidinyl, furyl, isoxazolyl or isothiazolyl, each of which is optionally substituted with 1-3 substituents selected from the group consisting of halogen, C /-Salkyl, optionally partially or fully halogenated, hydroxy, nitrile and C.--CsalkoxyC;alkoxy group, optionally partially or fully (F, halogenated, ka - cyclopropyl, cyclobutyl, cyclopentanyl, cyclohexanyl, bicyclopentanyl or bicyclohexanyl, each of which is optionally partially or fully halogenated and optionally substituted 1 -3 C /-C alkyl groups, which are optionally partially or fully halogenated, nitrile, hydroxyC 1-C alkyl or phenyl, or an analogue of such a cycloalkyl group, in which 1-3 ring methylene groups are independently replaced by O, 5, CHOH, »C-0, 2-5 or

МН, - an oxo group, - C3-Alkynyl branched or unbranched carbon chain, optionally partially or fully 65 halogenated, while one or more methylene groups are optionally replaced by ОО, МН or 5(О)m, and the specified alkynyl group optionally independently substituted by 1-2 oxo groups, hydroxy group, pyrrolidinyl,

pyrrolyl, tetrahydropyranyl, C4-C; alkyl, optionally substituted by one or more halogen atoms, nitrile, morpholino group, piperidinyl, piperazinyl, imidazolyl, phenyl, pyridinyl, tetrazolyl, or mono- or di(C-C-C alkyl)amino group, necessarily substituted by one or more halogen atoms, or - silyl containing three C-C alkyl groups, optionally partially or fully halogenated,

E" in each case independently means - a branched or unbranched C.i.S.alkyl, which is not necessarily partially or fully halogenated, acetyl, aroyl, a branched or unbranched C.I.-C.Alkoxy group, in each case not necessarily partially or fully halogenated, halogen, methoxycarbonyl, a C.i.sub.6 alkyl-(O) group, which is not necessarily partially or fully halogenated, or a phenyl-Z(O)t group, - C.sub.6-alkyloxy group, a hydroxy group, a nitrile, a nitro group , halogen or - an amino-5(O)»- group, where the M-atom is optionally independently mono- or di-substituted with C--Salkyl or aryl-Salkyl, or an amino group where the M-atom is optionally independently mono- or disubstituted C .-Salkyl, aryl-Salkyl, C--Szacyl, group C.--Slalkyl-(O)-group or aryl-Salkyl-Z(O)t-, while each of the /5 alkyls specified in this paragraph and aryls are optionally partially or fully halogenated and optionally substituted with 1-2 C.i.sub.C alkyl groups or C.-C.sub.alkoxy groups,

Ez in each case independently means - phenyl, morpholino group, pyridinyl, pyrimidinyl, pyrazinyl, pyrrolyl, pyrrolidinyl, imidazolyl,

1,3,Shoxadiazole, pyrazolyl, each of which is optionally substituted with 1-3 substituents selected from the group consisting of phenyl, naphthyl, heterocycle or heteroaryl as described above in this paragraph, C /-Cylalkyl, which is optionally necessarily partially or fully halogenated, cyclopropanyl, cyclobutanyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, bicyclopentanyl, bicyclohexanyl, bicycloheptanyl, phenyl-C-C-alkyl, naphthyl-C-alkyl, halogen, oxo group, hydroxy group, nitrile, C-C-C alkyloxy , optionally partially or fully halogenated, phenyloxy group, naphthyloxy group, heteroaryloxy group or heterocyclooxy group, where the heteroaryl or heterocyclic moiety is described above in this paragraph, nitro group, amino group, mono- or di(C.4-Salkyl)amino group, phenylamino group, naphthylamino group , a heteroarylamino group or a heterocyclamino group, and) where the heteroaryl or heterocyclic fragment is described above in this paragraph, the group МНБС(О), mono- or di(C1-Calkyl)aminocarbonyl, C.-Salkyl-C(О0)-Ci-C ;,alkyl, mono- or di(C.sub.-C alkyl)uamino group, mono- or di(C.sub.4-C.sub.3)alkylamino-C.sub.alkyl, mMono- or di(C.sub.4-C.sub.alkyl)amino-Z(O) 2 group, K;-Si-Svalkil, su

Kv-C1-Salkyloxy group, Kea-C(0)-C.4-Salkyl, Kio-C4-Salkyl(K44)M group and carboxy-mono- or di(C4-C)-alkylamino group, o - C.-Salkyl group or C-C-Alkoxy group, each of which is optionally partially or fully halogenated Ge! or optionally replaced by a group

КИ17, - - ОКув or С.-Салкіл, optionally substituted by the group ОК в, і- - amino group or mono- or di(С.--Салкіл) amino group, optionally substituted by the group Ко, - КоосС(ОМ( Koa4)-, Kogo-, KozkoAMS(O)-, KozSNoSO)M(Koya4)-, Koza MC(O0)-C1-Sialkoxy group or

КовС(О)СНоМ(К21)-, « - С.-С.alkenyl, substituted by the group KozКо4МС(О)-, - С»-С»alkynyl branched or unbranched carbon chain, optionally partially or fully halogenated, at the same time, one of the methylene groups is optionally replaced by 0, and optionally independently substituted by 1-2 oxo groups, pyrrolidinyl, pyrrolyl, morpholino group, piperidinyl, piperazinyl, etc. imidazolyl, phenyl, pyridinyl, tetrazolyl or one or more C.-C.alkyl groups, optionally substituted by one or more halogen atoms, or - C.-Szatyl and

Koz and Cod together optionally form an imidazolyl, piperidinyl, morpholine, piperazinyl or -I pyridinyl ring.

According to the next embodiment of the invention, among the directly mentioned above, the compounds of the formula (PI) in which (Ce) means phenyl, pyridinyl, pyridonyl, naphthyl, quinolinyl, isoquinolinyl, pyrazinyl,

C,4-dihydro-2H-benzo|1,4oxazinyl, benzothiophenyl, dihydrobenzofuranyl, dihydrobenzothiophenyl, benzoxazolyl, i.e. indanyl, indolyl, indolinyl, indolonyl or indolinonyl, while C is optionally substituted by one or

With several groups K., K» or Kz,

Ag means naphthyl,

X represents phenyl, imidazolyl, pyridinyl, pyrimidinyl, piperidinyl, piperazinyl, pyridazinyl or pyrazinyl,

Each of which is optionally independently substituted with 1-3 substituents selected from the group consisting of C --C; alkyl,

C.-C. alkoxy group, hydroxy group, nitrile, amino group, mono- or di(C.-C. alkyl) amino group, mono- or

F, di(C1-Salkylamino)carbonyl, MNHS(O) group, C.-Sbalkyl-Z(O)n group and halogen, where M means a bond or a saturated C 41-C4 carbon chain, where one or more C -atoms are optionally substituted by 0, M or 5, and Y is optionally independently substituted by a nitrile or an oxo group, in 27 means phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, imidazolyl, dihydrothiazolyl, dihydrothiazolyl sulfoxide, pyranyl, pyrrolidinyl, phenylpiperazinyl, tetrahydropyranyl .

C.-Soalkyl groups or C.-Soalkyl groups, or 65 2 means a hydroxy group, C.--C.alkyl, C.-C.alkyloxy group, C.--C.acylamino group, C.--C.alkylsulfonyl, nitrile-C4-C.alkyl or amino group, mono- or disubstituted C4i-SzalkoxyS-Szalkyl,

Ki in each case independently means - branched or unbranched S.-Svalkyl, which is not necessarily partially or completely halogenated, while one or more C atoms are not necessarily independently replaced by O, M or 5(0O) n, and the indicated C-Salkyl is optionally substituted with oxo, dioxolanyl, pyrrolidinyl, furyl or phenyl, each of which is optionally substituted with 1-3 substituents selected from the group consisting of halogen, C 1-Salkyl, optionally partially or fully halogenated , a hydroxy group, a nitrile and a C.-C.-C.-C.-C.-C.-Alkoxy group, optionally partially or fully halogenated, - cyclopropyl, cyclobutyl, cyclopentanyl, cyclohexanyl, bicyclopentanyl or bicyclohexanyl, each of which 70 is optionally partially or fully halogenated and optionally substituted by 1 -3 C --C alkyl groups, optionally partially or fully halogenated, nitrile, hydroxyC i-C alkyl or phenyl, or an analog of cyclopropyl, cyclobutyl, cyclopentanyl, cyclohexanyl, bicyclopentanyl or bicyclohex sanyl, in which one ring methylene group is replaced by 0, - an oxo group, - C.-C.alkynyl, optionally partially or completely halogenated, while one or more methylene groups are optionally replaced by O, and optionally independently substituted by 1-2 oxo groups, hydroxy group, pyrrolidinyl, pyrrolyl, tetrahydropyranyl, C--C;, alkyl, optionally substituted by one or more halogen atoms, nitrile, morpholino group, piperidinyl, piperazinyl, imidazolyl, phenyl, pyridinyl, tetrazolyl or mono- or a di(C.sub.1-C alkyl)uamino group, optionally substituted by one or 2 by several halogen atoms, or - a silyl containing three C.sub.6 alkyl groups, optionally partially or fully halogenated,

Co in each case independently means C1-C6 alkyl, which is optionally partially or fully halogenated, C1-C6-alkyl, optionally partially or fully halogenated, bromine, chlorine, fluorine, methoxycarbonyl , a methyl-5(O)t group or an ethyl-3(O)t group, each of which is optionally partially or fully halogenated, or a phenyl-3(O)t group, or Ko means mono- or diC.i - Szacylamino group, amino-(O)t or group

З(О)t-amino group, where the M-atom is mono- or disubstituted by C.4-C alkyl or phenyl, nitrile, nitro group or amino group, and)

Ez in each case independently means - phenyl, morpholino group, pyridinyl, pyrimidinyl, pyrrolidinyl, 2,5-pyrrolidinedionyl, imidazolyl,

1,3,ShCoxadiazole, pyrazolyl, each of which is optionally substituted with 1-3 substituents selected from the group consisting of C.-Salkyl, optionally partially or fully halogenated, halogen, oxo, hydroxy, nitrile and C --SzalkoxySalkoxygroup, optionally partially or fully halogenated, o - C.-Szalkyl group or C.-SzalkoxySalkoxygroup, which is not necessarily partially or fully halogenated He! or optionally substituted by the group K.7, - OKuv or C.i-Szalkyl, optionally substituted by the group OK in, -- - amino group or mono- or di(C.--Szalkyl)amino group, optionally substituted by the group Co, i- - Egos(O)(K 21)-, Kg20-, KozKodMS(O)-, KovbSNoS(O)M(K21)-, MNoS(O)methoxy group or KovS(O)SNoM(K24)-, - C.-C.alkenyl, substituted by the group KozKo4MS(O)-, - C.-C.alkynyl, substituted by pyrrolidinyl or pyrrolyl, or - C-Szatyl and "

Koz and Code together do not necessarily form a morpholino group. with c According to another version of the invention, among those directly mentioned above, those are the best. compounds of the formula (PI), in which b means phenyl, pyridinyl, pyridonyl, 2-naphthyl, quinolinyl, isoquinolinyl, dihydrobenzofuranyl, indanyl, 5B-indolyl, 3Z-oxo-3,4-dihydro-2H-benzo|1,Coxazin-8-yl, benzooxalolyl, 2, 3-dihydrobenzoxazol-7-yl, 2-oxo-2,3-dihydro-1H-indol-b-yl, indolinyl, indolonyl or indolinonyl, while C is optionally substituted by -I with one or more groups Ku, K» or Kz,

Ag means 1-naphthyl, - X means phenyl, imidazolyl, pyridinyl, pyrimidinyl, piperidinyl, piperazinyl, pyridazinyl or pyrazinyl,

Ge) M means a bond or -СН 5-, -СНСН»-, -С(0)-, -О-, -5-, -МН-СНСНоСН»-, -Щ(СНУ»)-, СН (СМ)СНо-МН-СНо or 5о МН. o 7 means a morpholino group, dioxolanyl, tetrahydrofuranyl, pyridinyl, 2-oxa-5-azabicyclo|2.2.1)heptanyl,

Ge S.i-Szalkoxyphenylpiperazinyl, hydroxy group, S.-Szalkyl, M,M-di--Szalkoxy-C.4-Salkylamino group,

C.i-Szacylamino group, C--Szalkylsulfonyl or nitrile-Szalkyl,

Ki in each case independently means - C-Svalkyl, which is optionally partially or fully halogenated, while one or more C-atoms are optionally independently replaced by O or M, and the specified C.-Svalkyl is optionally substituted by an oxo group,

F) dioxolanil, pyrrolidinyl, furyl or phenyl, optionally substituted by a C.4-Salkoxy group, such as cyclopropyl, cyclopentanyl, cyclohexanyl and bicyclopentanyl, optionally substituted by 1-3 methyl groups, optionally partially or fully halogenated, nitrile, hydroxymethyl or phenyl, or 2g-tetrahydrofuranyl, substituted by methyl, - trimethylsilyl or - propynyl, substituted by a hydroxy group or a tetrahydropyran-2-yloxy group,

EK" means a mono- or diC-Szacylamino group, an amino-B(O)t or (OO)-amino group, where the M-atom is mono- or disubstituted by C-Szalkyl or phenyl, bromine, chlorine, fluorine, nitrile, nitro group, amino group, methylsulfonyl, 65 optionally partially or fully halogenated, or phenylsulfonyl,

Ez in each case independently means

- phenyl, morpholino group, pyridinyl, pyrimidinyl, pyrrolidinyl, 2,5-pyrrolidinyldionyl, imidazolyl, (1,3,Shoxadiazole or pyrazolyl, each of which is optionally substituted by C /-Soalkyl, optionally partially or fully halogenated, - Si -Szalkyl group or C.--Szalkoxy group, each of which is optionally partially or fully halogenated or optionally substituted by a diethylamino group, - OKuv or C.i-Szalkyl, optionally substituted by a group OK in, - amino group or mono- or di(C.--Szalkyl) amino group, optionally substituted by a Co group, - snNUFfomMnH-, Eogo-, KozKoMO(O)-, RovSNoS(OMKa34)-, MNHS(O)methoxy group or KoCS(O)СНоM(Ko) -, 70 - C.-C.alkenyl, substituted by the group KozKo4MS(O)-, - C.-C.alkynyl, substituted by pyrrolidinyl or pyrrolyl, or - C--Soacyl and

Koz and Kod mean H or Koz and K24 together optionally form a morpholino group and

Kov means a morpholino group.

According to another embodiment of the invention, among those directly indicated above, those compounds of the formula (PI) in which b means phenyl, pyridinyl, 5-indolyl, 3-oxo-3,4-dihydro-2H-benzo|1,Zoxazin-8 -yl, benzooxalolyl, 2,3-dihydrobenzoxazol-7-yl, 2-oxo-2,3-dihydro-1H-indol-b-yl or 2-naphthyl, while C is optionally substituted by one or more K groups. , K» or Kz,

X represents imidazolyl, pyridinyl, pyrimidinyl or pyrazinyl,

U means bond, СНСМ)СНо-МН-СН», -СНо-, -МН-СНоОСНОСН»- or -МН-, 2 means morpholin-4-yl, dioxolan-2-yl, tetrahydrofuranyl, pyridinyl, 2 -oxa-5-azabicyclo|2 2Ahept-5-yl, methoxyphenylpiperazinyl, hydroxy group, methyl, M,M-dimethoxyethylamino group, acetylamino group, methylsulfonyl or cyanoethyl, sc

K in each case independently means tert-butyl, sec-butyl, tert-amyl, phenyl, tetrahydropyran-2-yloxypropynyl, hydroxypropynyl, trihalomethyl, 2,2-diethylpropionyl or cyclohexanyl, and)

Co represents chlorine, nitro, amino, nitrile, methylsulfonylamino, diacetylamino, phenylsulfonylamino, M,M-di(methylsulfonyl)amino, methylsulfonyl or trihalomethylsulfonyl,

Kz in each case independently means methyl, C-C 6 hydroxy, methoxymethyl, hydroxypropyl, suso dimethylamino, C 1 -C 1 alkylamino, MNoC(O)methoxy, acetyl, pyrrolidinyl, imidazolyl, pyrazolyl, morpholino, or morpholinocarbonyl. at

In another embodiment of the invention, the compounds of formula (I), He! in which X is pyridinyl.

According to the following version of the invention, among those directly mentioned above, the best ones --

From compounds of formula (III), in which pyridinyl is attached to Ag in the 3rd position of pyridinyl. uh-

Examples of compounds of the formula (II) according to the invention include the following: 1-(4-tert-butylphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 1- (5-tert-butyl-2-methylphenyl)-3-I4-(4-morpholin-4-ylmethylpiperidin-1-yl)naphthalen-1-yl|urea, 1-(6-chloro-4-trifluoromethylpyridin-2- yl)-3-I4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, « 1--4-difluoromethoxyphenyl)-3-(4-(6-morpholin-4-ylmethylpyridine) -3-yl)naphthalen-1-yl|urea, with c 1-(3-methylnaphthalen-2-yl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl| Urea. ?» 3-(5-14-I3-(5-tert-butyl-2-methylphenyl)ureido|naphthalen-1-yl)pyridin-2-ylamino)propyl ether (5-tert-butyl-2-methylphenyl)carbamino acid, 1-(b-tert-butylbenzoic|1,3|dioxol-5-yl)-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, -I M -(5-tert-butyl-2-methoxy-3-13-14-(6-morpholin-4-ylmethylpyridin-3-yl)unaphthalin-1-yl)ureido)phenyl)acetami d, 1,3-bis4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, - 1-(b-tert-butyl-3-(2,2-dimethyl-|1 ,3|dioxolan-4-ylmethyl)-2-hydroxyphenyl/)-3-(4-(6-morpholin-4-ylmethylpyrides)

He) n-3-yl) unnaphthalen-1-yl| Urea, sl 50 1-(b-tert-butyl-2-(2-pyrrolidin-1-ylethoxy)phenyl)|-3-(4-(6- morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|wine urine,

Ge 1-(b-tert-butyl-3-(2,3-dihydroxypropyl)-2-hydroxyphenyl|-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl) Urea, 1--2,3-dimethyl-1H-indol-5-yl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(4- (b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|-3-(2-p-tolyloxy-5-trifluoromethylphenyl)urea, 1-(2--2-methoxyphenoxy)-5-trifluoromethylphenyl| -3-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea

The formation of 1-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|-3-naphthalen-1-ylurea, 1-x5-tert-butyl-2-methyl-3- 13-(tetrahydropyran-2-yloxy)prop-1-ynyl|phenyl)-3-I(4-(b-morpholin-4-ylmethylpyridine bo n-3-yl)naphthalen-1-yl|urea, 1-х5 -tert-butyl-2-(3-(tetrahydropyran-2-yloxy)prop-1-ynyl|phenyl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)n aphthalin-1-yl |urea, 1-(5-hydroxymethyl-2-methylphenyl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1--2-methoxydibenzofuran-3- yl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 65 1-22,5-di-tert-butylphenyl)-3-I4-(b- morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-I3-(4-bromo-1-methyl-1H-pyrazol-3-yl)phenyl|-3-(4-(6- Morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea,

1-(3-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-3-I(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 1 -"1-acetyl-2,3-dihydro-1H-indol-5-yl)-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(4 -(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|-3-(3-oxazol-5-ylphenyl)urea, 1-(4-(b6-morpholin-4-ylmethylpyridin-3- yl)naphthalen-1-yl|-3-(3-1,3,Zoxadiazol-2-ylphenyl)urea, 1--2-methoxy-5-trifluoromethylphenyl)-3-(4-(6-morpholine-4- ylmethylpyridin-3-yl)naphthalen-1-yl|urea, (4-tert-butyl-2-(3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl"ureido)phenyl )iamidfuran-2-carboxylic acid, 1-(-2-methoxy-4-phenylaminophenyl)-3-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 70 1- (5-methoxy-2-methylphenyl)-3-I4-(β6-morpholin-4-ylmethylpyridin-3-yl)unaphtalin-1-yl|Urea, 1-(3-hydroxynaphthalen-2-yl)-3-I4 -(b6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea,

M,M-diethyl-4-methoxy-3-13-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)/ureido)dbenzenesulfonamide, 1--2,2-difluorobenzo|1 ,3|dioxo1-5-yl)-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(5-(1,1-dimethylpropyl)-2- phenoxyphenyl|-3-I4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1-(5--2,2-dimethylpropionyl)-2-methylphenyl/|-3-I4 -(b6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, isopropyl ether 2-chloro-5-(3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalene- 1-yl"ureido)benzoic acid, 1-(4-amino-3,5-dibromophenyl)-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1- (b-tert-butyl-3-(3-hydroxyprop-i-ynyl)-2-methylphenyl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea , 1-(b-tert-butyl-2-(3-hydroxyprop-1-ynyl)uphenyl|-3-I(4-(b6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea inu, 1-(B-tert-butyl-3-(2,2-dimethyl-|1,3|dioxolan-4-ylmethyl)-2-methoxyphenyl/|-3-(4-(b-morpholin-4- ylmethylpyridin-3-yl)unnaphthalen-1-yl|urea, 1-( 5-tert-butyl-3-(2,3-dihydroxypropyl)-2-methoxyphenyl)-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalene-1 sc dv Silica, 1-( 5-tert-butoxy-2-methoxyphenyl)-3-I(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, and) 1-(5-"1-cyanocyclopropyl) -2-methoxyphenyl|-3-(4--b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(B-tert-butyl-3-(2-diethylamino-ethyl) -2-methoxyphenyl/|-3-I(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalene-1-lysine, c zo 1-(5-tert-butyl-2-methoxyphenyl)-3 -(4-(6-(/1,3|dioxolan-2-ylpyridin-3-yl)naphthalen-1-yl|urea, 1-(5-tert-butyl-2-pyrrolidin-1-ylphenyl)-3 -I(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(5-tert-butyl-2-dimethylaminophenyl)-3-(4-(b-morpholine) -4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, Ge! 1-(5-tert-butyl-2-propoxyphenyl)-3-I4-(6b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1-(5-tert-butyl-2- methoxyphenyl)-3-(4-(6b-hydroxymethylpyridin-3-yl)naphthalen-1-yl|urea, -- 1-(5-tert-butyl-2-methoxyphenyl)-3-14-(6--2 ,6-dimethylmorpholin-4-ylmethyl)pyridin-3-yl-naphthalen-1-yl)urea y- 2-(5-tert-butyl-2-methoxyphenyl)-M-I4-(b-morpholin-4-ylmethylpyridin-3 -yl)naphthalene-1-ilyacetamide, 1--2-methoxy-5-phenoxyphenyl)-3-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalene-1-yl|urea, 1-- 3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-7-yl)-3-(4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urine "

VINU, shsh c 1-(5-tert-butyl-2-cyclopentyloxyphenyl)-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, . 1-(5-tert-butyl-2-methoxyphenyl)-3-74-(6-(3-pyridin-3-ylpyrrolidin-1-ylmethyl)pyridin-3-ylnaphthalen-1-yl) wine, 1-(5-cyclohexyl-2-methoxyphenyl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1--2,4-dimethoxy-5 -trifluoromethylphenyl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, -I 1-(b-tert-butyl-3-oxo-3,4-dihydro -2H-benzo|1,oxazin-7-yl)-3-I(4--6-morpholin-4-ylmethylpyridin-3-yl)naphtha lin-1-yl)urea, - 1-(5-tert- butyl-2-methoxy-33-nitrophenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea,

Ge) 1-(3-amino-5-tert-butyl-2-methoxyphenyl)-3-I(4-(b-methylpyridin-3-yl)naphthalen-1-yl)urea,

M-acetyl-M-(5-tert-butyl-2-methoxy-3-13-14-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)/ureido)phenyl)ac 1 ethamide ,

Ge 1-(b-tert-butyl-4-methyl-3-oxo-3,4-dihydro-2H-benzo|1,Zoxazin-8-yl)-3-I4-(b-morpholin-4-ylmethylpyridin- 3-yl)unaphtalin-1-yl|Urea, 1-(b-tert-butyl-4-(2-morpholin-4-ylethyl)-3-oxo-3,4-dihydro-2H-benzo|1,Doxazin -8-ylI|-3-I(4-(6-morpholin-4-yl)methylpyridin-3-yl)naphthalen-1-yl|urea, 1-(5-tert-butyl-2-ethoxyphenyl)-3 -I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea,

F) 1-(5-tert-butyl-2-isopropoxyphenyl)-3-I(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, ka 1-(5-tert -butyl-2-imidazol-1-ylphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea,

M-(5-tert-butyl-2-methoxy-4-13-I4-(6-morpholin-4-ylmethylpyridin-3-yl)unaphthalin-1-yl)ureido)phenyl)methanesulfonamide, 1-(5 -tert-butyl-3-ethylamino-2-methoxyphenyl)-3-14-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea,

M-(5-tert-butyl-2-methoxy-3-13-14-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-ylureido)phenyl)bis(methanesulfon)amide, 1-( b-tert-butyl-2-(1-methyl-1H-pyrazol-4-yl)phenyl1-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea 65 ovInu, 1--2-methanesulfinyl-5-trifluoromethylphenyl)-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea,

1--2-ethanesulfonyl-5-trifluoromethylphenyl)-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-I4-(6-Ibis(2- methoxyethyl)amino|methyl)pyridin-3-yl)naphthalen-1-ylI|-3-(5-tert-butyl-2-methoxyphenyl)urea, 1-(5-tert-butyl-2-methoxyphenyl)-3- 4-(6-(3-Dimethylaminopyrrolidin-1-ylmethyl)pyridin-3-yl|Inaphthalin-1-yl)urea

BLAME

IM-(11-(5-4-(3-(5-tert-butyl-2-methoxyphenyl)ureido|naphthalen-1-yl)pyridin-2-ylmethyl)-pyrrolidin-3-yl|Iacetamide, 1-- 1-acetyl-3,3-dimethyl-2,3-dihydro-1H-indol-5-yl)-3-I(4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl| )se chovino,

M-(5-tert-butyl-2-methoxy-3-13-14-(6-morpholin-4-ylmethyltridin-3-yl)naphthalen-1-ylureido)phenyl)propionamide, 70 1-(5-tert- butyl-2-methylbenzoxazol-7-yl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(4-(b-morpholin-4-ylmethylpyridine) -3-yl)naphthalen-1-yl|-3--Trifluoromethanesulfonylphenyl)urea,

M-(5-tert-butyl-2-methoxy-3-13-I4-(6-morpholin-4-ylmethylpyridin-3-yl)unaphthalin-1-yl)ureido)phenyl)isobutyramid, 2-(4- tert-butyl-2-13-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)ureido)phenoxy)acetamide, 1-(5-tert-butyl-2-oxo-2, 3-dihydrobenzoxazol-7-yl)-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl urea, 1-(b-tert-butyl-3-cyano-2- methoxymethoxypyridin-4-yl)-3-I4-'b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl urea, 1-(b-tert-butyl-3-cyano-2-hydroxypyridin-4 -yl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea

MNU, 1-(5-tert-butyl-3-cyano-2-methoxyphenyl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(4 -(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|-3-(1,3,3-trimethyl-2,3-dihydro-1H-indol-5-yl)urea, 1- (5-tert-butylbenzoxazol-7-yl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea,

M-(5-tert-butyl-2-methoxy-3-13-I4-(6-morpholin-4-ylmethylpyridin-3-yl)unaphthalin-1-yl)ureido)phenyl)benzenesulch fonamide, (5-tert -butyl-2-methoxy-3-(3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)ureido)phenyl)amide and) ethanesulfonic acid, 1-(5-tert- butyl-2-methoxyphenyl)-3-I(4-(4-morpholin-4-ylmethylpiperidin-1-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(1-methyl- 1H-pyrazol-4-yl)phenyl|-3-I4-(4-morpholin-4-ylmethylpiperidin-1-yl)naphthalen-1-yl|s with urea, 1-(5-tert-butyl-2- methoxyphenyl)-3-I(4-(2-morpholin-4-ylmethylpyrimidin-5-yl)naphthalen-1-yl|urea, o 1-(5-tert-butyl-2-methylsulfanylphenyl)-3-I(4 -(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, He! 1-(5-tert-butyl-2-methoxypyridin-3-yl)-3-14-(b-morpholine -4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, (5-tert-butyl-2-methoxy-3-(3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalene- 1-yl/ureido)phenyl)amide 2,2,2-tri-fluoroethanesulfonic acid,

M-(5-4-(3-(5-tert-butyl-2-methylphenyl)ureido|naphthalen-1-yl/pyrazin-2-yl)umethanesulfonamide, 1-I4-(6-Tibis(2-cyanoethyl) amino|methyl)pyridin-3-yl)naphthalen-1-ylI|-3-(5-tert-butyl-2-methoxyphenyl)urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-4- (6-(4-methylpiperazin-1-ylmethyl)pyridin-3-yl|naphthalen-1-yl)uretate, 1-(5-tert-butyl-2-methoxyphenyl)-3-I4-(b-thiomorpholine-4 -ylmethylpyridin-3-yl)naphthalen-1-yl)urea, " 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(6-(2,6-dimethylpiperidin-1-ylmethyl)-pyridine -3-yl|Inaphthalin-1-yl) usecovy z

NU, - 1-(5-tert-butyl-2-methoxyphenyl)-3-74-(6-(1-oxotetrahydrothiopyran-4-ylamino)pyridin-3-yl|Inaphthalin-1-yl)urea Ovine, 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(b-(tetrahydropyran-4-ylamino)pyridin-3-yl|Inaphthalin-1-yl)uretate, 1-(5-tert -butyl-2-methoxyphenyl)-3-14-(6-4(2-cyanoethyl)-(tetrahydrofuran-2-ylmethyl)amino)methyl)pyridin-3-yl)naphthalen-1-ylurea, and 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(6-(2-methoxymethylmorpholin-4-ylmethyl)pyridin-3-ylInaphthalin-1-yl) truncated,

Ge) 1-(5-tert-butyl-2-methoxyphenyl)-3-(4-16-((2-morpholin-4-ylethylamino)methyl|pyridin-3-ylenenaphthalen-1-yl)urea

NU, o 20 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(6-(2-methyl-3-oxopiperazin-1-ylmethyl)pyridin-3-yl|naphthalen-1-yl) all the way

From wine, 1-(5-4-13-(5-tert-butyl-2-methoxyphenyl)ureido|naphthalen-1-yl)pyridin-2-ylmethyl)piperidine-3-carboxylic acid amide, 1-(5 -4-I(3-(5-tert-butyl-2-methoxyphenyl)ureido|naphthalene-1-ylpyridin-2-ylmethyl)piperidine-4-carboxylic acid,

F) 1-(5-tert-butyl-2-methoxyphenyl)-3-74-(6-(1-oxo-114-thiomorpholin-4-ylmethyl)pyridin-3-yl|naphthalen-1-yl)urea ) inuU, 1-(3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalene -1-yl|) urine bo VINU, 1-(5-tert-butyl-2-methoxyphenyl)-3-74-(6-(3-oxopiperazin-1-ylmethyl)pyridin-3-yl|Inaphthalene-1- yl)urea, 1-4-(6-(4-acetylpiperazin-1-ylmethyl)-pyridin-3-yl|Inaphthalen-1-yl-3-(5-tert-butyl-2-methoxyphenyl)urea, ethyl ether 4-(5-4-I(3-(5-tert-butyl-2-methoxyphenyl)ureido|naphthalen-1-yl)upyridin-2-ylmethyl)piperazine-1-carboxylic acid, 65 1-(5-tert -butyl-2-methoxyphenyl)-3-(4-16-((2-pyridin-3-ylethylamino)methyl|pyridin-3-ylnaphthalen-1-yl)urea, 1-(5-tert-butyl-2- methoxyphenyl)-3-(4-16-((tetrahydrofuran-33-ylamino)methyl-pyridin-3-ylenenaphthalen-1-yl)acetaminophen, 1-(5-tert-butyl-2-methoxyphenyl)-3-I4-( 6-4(2-cyanoethyl)pyridin-3-ylmethylamino|methyl)pyridin-3-yl)naphthalen-1-yl|urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-(4-16 -((2-methylsulfanylethylamino)meth yl|pyridin-3-ylnaphthalen-1-yl)urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-74-(6-(2-oxa-5-azabicyclo|2.2.1)hept -5-ylmethyl)pyridin-3-ylnaphthalen-1-yl)urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(6-(-2,6-dimethylmorphol-4-ylmethyl) pyridin-3-yl|naphthalen-1-yl)/urea t 1-(5-tert-butyl-2-methoxyphenyl)-3-(4-16-((2-piperazin-1-ylethylamino)methyl|pyridin- 3-ylnaphthalen-1-yl)urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(6-(4-pyrimidin-2-ylpiperazin-1-ylmethyl)pyridin-3-yl |Inaphthalin-1-shusech ovine, 1-(5-tert-butyl-2-methoxyphenyl)-3-74-(6-(4-pyridin-2-ylpiperazin-1-ylmethyl)pyridin-3-yl|Inaphthalin- 1-yl) alcohol, 1-(5-tert-butyl-2-methoxyphenyl)-3-(4-16-14-(3-methoxyphenyl)-piperazin-1-ylmethyl|pyridin-3-ylnaphthalene-1- yl)urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(b-(morpholine-4-carbonyl)pyridin-3-yl|Inaphthalen-1-yl)urea, 1-(5 -tert-butyl-2-methoxyphenyl)-3-74-(6-(2-thia-5-azabicyclo|2.2.1)hept-5-ylmethyl)pyridin-3-ylInaphthalin-1-lysine, 1-( 5-tert-butyl-2-methoxyphenyl)-3-I4--5-morpholine-4- ylmethylpyrazin-2-yl)naphthalen-1-yl)urea, 1-(b-tert-butyl-3-oxo-3,4-dihydro-2H-benzo|1,oxazin-8-yl)-3-(4 --6-morpholin-4-ylmethylpyridin-3-yl)naphthalene-1-yl)urea, sc 1-(3-amino-5-tert-butyl-2-methoxyphenyl)-3-I4-(b-morpholine -4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea,

M-(5-4-(3-(5-tert-butyl-2-methoxyphenyl)ureido|naphthalen-1-yl)pyridin-2-yl)acetamide, and)

M-(5-tert-butyl-2-methoxy-3-13-14-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-ylureido)phenyl)-M-methylacetamide,

M-(5-tert-butyl-2-methoxy-3-13-14-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)ureido)phenyl)-2,2,2-triph c zo toroacetamide, 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(6b-(pyridin-3-yloxy)pyridin-3-yl|Inaphthalin-1-yl)urea, o 1-( 5-tert-butyl-2-methoxyphenyl)-3-4-(6b-(pyridin-3-ylamino)pyridin-3-yl|Inaphtalin-1-yl)erucine, Ge!

C-tert-butylphenyl ester of I(4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)carbamic acid,

M-(5-tert-butyl-2-methoxy-3-13-I4-(6-morpholin-4-ylmethylpyridin-3-yl)unaphthalin-1-yl)ureido)phenyl)methanesulfonamide and their pharmaceutically acceptable derivatives uh-

According to another embodiment of the invention, it also offers the following compounds of formula (II): 1--3-methylnaphthalen-2-yl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalene-1 -il|Urea,

M-(5-tert-butyl-2-methoxy-3-13-I4-(6-morpholin-4-ylmethylpyridin-3-yl)unaphthalin-1-yl)ureido)phenyl)acetamide, 1-(b-tert -butyl-3-(2,3-dihydroxypropyl)-2-hydroxyphenyl|-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalene-« 1-yl|Urea, with c 1- -2,3-dimethyl-1H-indol-5-yl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1-x5-tert-butyl- 2-Methyl-3-3-(tetrahydropyran-2-yloxy)prop-1-ynyl|phenyl)-3-I(4-(b-morpholin-4-ylmethylpyridine and»n-3-yl)unanaphthalene-1 -yl|urea, 1--2-methoxy-5-trifluoromethylphenyl)-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(5-- 2,2-dimethylpropionyl)-2-methylphenyl/|-3-I4-(b6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, -I 1-(b-tert-butyl-3 -(3-hydroxyprop-1-ynyl)-2-methylphenyl|-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, - 1-(b-tert-butyl -2-(3-hydroxyprop-1-ynyl)uphenyl|-3-I(4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 1-(β-tert -butyl-3-(2,2-dimethyl-|1,3|dioxolan-4-ylmethyl)-2-methoxyphenyl/| -3-(4-(6-morpholin-4-ylmethylpyridin o -3-yl)unaphtalin-1-yl|urea,

Ge 1-(b-tert-butyl-3-(2,3-dihydroxypropyl)-2-methoxyphenyl)-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl |urea, 1-(5-tert-butoxy-2-methoxyphenyl)-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1-(5-(1- cyanocycloprogal)-2-methoxyphenyl|-3-(4-(6b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-3-(2-diethylaminoethyl) -2-methoxyphenyl|-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl (F) |Urea, ka 1-(5-tert-butyl-2-methoxyphenyl)-3 -I4-(6-(1,3|dioxolan-2-ylpyridin-3-yl)naphthalen-1-yl)urea, 1-(5-tert-butyl-2-pyrrolidin-1-ylphenyl)-3-I4 -(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, in 1-(5-tert-butyl-2-dimethylaminophenyl)-3-I(4-(b-morpholin-4- ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(5-tert-butyl-2-propoxyphenyl)-3-I(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalene-1 -yl)urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-I4-(b-hydroxymethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(5-tert-butyl-2 -methoxyphenyl)-3-4-(6-(2,6-dimethyl morpholin-4-ylmethyl)pyridin-3-ylNaphthalin-1-yl)retinate 65 1-(5-cyclohexyl-2-methoxyphenyl)-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalene -1-yl|urea, 1--2,4-dimethoxy-5-trifluoromethylphenyl)-3-I4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Iurea,

1-(5-tert-butyl-2-methoxy-3-nitrophenyl)-3-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(3-amino -5-tert-butyl-2-methoxyphenyl)-3-I(4-(b-methylpyridin-3-yl)naphthalen-1-yl|urea,

M-acetyl-M-(5-tert-butyl-2-methoxy-3-13-14-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)/ureido)phenyl)acetamide, 1-(b-tert-butyl-4-methyl-3-oxo-3,4-dihydro-2H-benzo|1,Zoxazin-8-yl)-3-I4-(b-morpholin-4-ylmethylpyridin-3 - yl)unaphthalin-1-yl|urea, 1-(5-tert-butyl-2-ethoxyphenyl)-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalin-1-yl|Iurea, 1-(5-tert-butyl-2-isopropoxyphenyl)-3-I(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 70 1-(5-tert-butyl -2-imidazol-1-ylphenyl)-3-I4--b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 1-(5-tert-butyl-3-ethylamino-2- methoxyphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea,

M-(5-tert-butyl-2-methoxy-3-13-14-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)ureido)phenyl)bis(methanesulfon)amide, 1 -(b-tert-butyl-2-(1-methyl-1H-pyrazol-4-yl)phenyl1-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea / 5 wine, 1--2-methanesulfinyl-5-trifluoromethylphenyl)-3-I(4-(6b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-I4-(6-Tbis -(2-methoxyethyl)amino|methyl)pyridin-3-yl)naphthalen-1-yl|-3-(5-tert-butyl-2-methoxyphenyl)urea,

IM-(11-(5-4-(3-(5-tert-butyl-2-methoxyphenyl)ureido|naphthalen-1-yl)upyridin-2-ylmethyl)pyrrolidin-3-ilyacetamide, 1--1-acetyl -3,3-dimethyl-2,3-dihydro-1H-indol-5-yl)-3-I(4-(β-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl) ,

M-(5-tert-butyl-2-methoxy-3-13-14-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-ylureido)phenyl)propionamide, 1-(5-tert-butyl -2-methylbenzoxazol-7-yl)-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Iurea, 1-(4-(b-morpholin-4-ylmethylpyridin-3 -yl)naphthalen-1-yl|-3--Trifluoromethanesulfonylphenyl)urea,

M-(5-tert-butyl-2-methoxy-3-13-14-(6-morpholin-4-ylmethylpyridin-3-yl)unaphthalin-1-yl)ureido)phenyl)isobutyrami o d, 2-(4 -tert-butyl-2-13-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)ureido)phenoxy)acetamide, 1-(5-tert-butyl-2-oxo-2 ,3-dihydrobenzoxazol-7-yl)-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, c zo 1-(5-tert-butyl-3-cyano -2-methoxyphenyl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(5-tert-butylbenzoxazol-7-yl)-3-I4- (b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, o

M-(5-tert-butyl-2-methoxy-3-13-I4-(6-morpholin-4-ylmethylpyridin-3-yl)unaphtalin-1-yl)ureido)phenyl)benzenesul Ge! fonamide, (5-tert-butyl-2-methoxy-3-(3-14-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)ureido)phenyl)amide -- ethanesulfonic acid, - 1-(5-tert-butyl-2-methoxyphenyl)-3-I(4-(2-morpholin-4-ylmethylpyrimidin-5-yl)naphthalen-1-yl|Urea, 1-(5-tert-butyl -2-methylsulfanylphenyl)-3-I(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(5-tert-butyl-2-methoxypyridin-3-yl) -3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, (5-tert-butyl-2-methoxy-3-(3-I4-(b-morpholin-4 -ylmethylpyridin-3-yl)naphthalen-1-yl)ureido)phenyl)amide of 2,2,2-trifluoroethanesulfonic acid, with M-(5-4-(3-(5-tert-butyl-2-methylphenyl)ureido |naphthalen-1-yl/pyrazin-2-yl)umethanesulfonamide, 1-I4-(6-Ibis(2-cyanoethyl)amino|methyl)pyridin-3-yl)naphthalen-1-yl|-3-(5 -tert-butyl-2-methoxyphenyl)urea, and? 1-(5-tert-butyl-2-methoxyphenyl)-3-74-(6-(4-methylpiperazin-1-ylmethyl)pyridin-3-yl|naphthalen-1-yl)urea, 1-(5-tert -butyl-2-methoxyphenyl)-3-I4-(b-thiomorpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-4 -(6-(2,6-Dimethylpiperidin-1-ylmethyl)pyridin-3-ylInaphthalin-1-yl)erucine a, t 1-(5-tert-butyl-2-methoxyphenyl)-3-74-(6- (1-oxotetrahydrothiopyran-4-ylamino)pyridin-3-yl|Inaphthalin-1-yl)urea,

Ge) 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(6-(tetrahydropyran-4-ylamino)pyridin-3-yl|Inaphthalin-1-yl) erucate, 1-(5-tert -butyl-2-methoxyphenyl)-3-I4-(6-1(2-cyanoethyl)-(tetrahydrofuran-2-ylmethyl)amino|methyl)pyridin-3-o yl)unaphtalin-1-yl|urea,

He 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(6-(2-methoxymethylmorpholin-4-ylmethyl)pyridin-3-ylInaphthalin-1-yl) truncated, 1-(5-tert -butyl-2-methoxyphenyl)-3-4-(6-(2-methyl-3-oxopiperazin-1-ylmethyl)pyridin-3-yl|naphthalen-1-yl)

WINE, amide

F) 1-(5-4-I3-(5-tert-butyl-2-methoxyphenyl)ureido|naphthalen-1-yl)pyridin-2-ylmethyl)piperidine-3-carboxylic acid, ka 1-(5-tert -butyl-2-methoxyphenyl)-3-74-(6-(1-oxo-114-thiomorpholin-4-ylmethyl)pyridin-3-yl|naphthalen-1-yl)urea, in 1-(3,3 -dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-74-(6-(3-oxopiperazin-1-ylmethyl)pyridin-3-ylInaphthalen-1-ylurea, 1-(5-tert-butyl-2 -methoxyphenyl)-3-(4-16-K(tetrahydrofuran-3-ylamino)methyl|pyridin-3-ylnaphthalen-1-yl)urea wine, 65 1-(5-tert-butyl-2-methoxyphenyl)-3 -I4-(6-S(2-cyanoethyl)-pyridin-3-ylmethylamino|methyl)pyridin-3-yl)naphthali n-1-yl|Urea,

1-(5-tert-butyl-2-methoxyphenyl)-3-74-(6-(2-oxa-5-azabicyclo|2.2.1)hept-5-ylmethyl)pyridin-3-ylInaphthalin-1-yl) urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(6-(2,6-dimethylmorpholin-4-ylmethyl)pyridin-3-ylInaphthalen-1-yl)urea and 1-(5 -tert-butyl-2-methoxyphenyl)-3-(4-16-14-(3-methoxyphenyl)piperazin-1-ylmethyl|pyridin-3-yl-naphthalen-1-yl)urea, 1-(5-tert -butyl-2-methoxyphenyl)-3-4-(b-(morpholine-4-carbonyl)pyridin-3-ylInaphthalen-1-ylurea, 1-(5-tert-butyl-2-methoxyphenyl)-3-I4- (5-morpholin-4-ylmethylpyrazin-2-yl)naphthalen-1-yl|urea, 70 1-(b-tert-butyl-3-oxo-3,4-dihydro-2H-benzo|1,oxazin-8 -yl)-3-(4--6-morpholin-4-ylmethylpyridin-3-yl)naphthalin-1-yl)urea, 1-(3-amino-5-tert-butyl-2-methoxyphenyl)-3 -I(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea,

M-(5-4-(3-(5-tert-butyl-2-methoxyphenyl)ureido|naphthalen-1-yl)pyridin-2-yl)acetamide,

M-(5-tert-butyl-2-methoxy-3-13-14-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-ylureido)phenyl)-M-methylacetamide,

M-(5-tert-butyl-2-methoxy-3-13-14-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)ureido)phenyl)-2,2,2-triph toracetamide, 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(6b-(pyridin-3-yloxy)pyridin-3-yl|Inaphthalen-1-yl)urea,

C-tert-butylphenyl ester of I(4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)carbamic acid,

M-(5-tert-buThyl-2-methoxy-3-13-I4-(6-morpholin-4-ylmethyltridin-3-yl)inanaphthalen-1-yl)ureido)phenyl)methanesulfonamide and their pharmaceutically acceptable derivatives .

In addition to the compounds given above as examples, the following possible compounds of formula (II) can also be obtained by the general methods of synthesis described below: 1-(5-tert-butyl-2-methylsulfanylpyridin-3-yl)-3-I4-(b-morpholin-4 -ylmethylpyridin-3-yl)naphthalen-1-yl)urea ch 8. 1-(5-tert-butyl-2-chloropyridin-3-yl)-3-(4--b-morpholin-4-ylmethylpyridin-3 -yl)naphthalen-1-yl)urea, and) 1-(5-tert-butyl-2-methylaminopyridin-3-yl)-3-(4--b6-morpholin-4-ylmethylpyridin-3-yl)naphthalene -1-yl)urea,

M-(5-tert-butyl-3-13-14-(6-morpholin-4-ylmethylpyridin-3-yl)unaphthalin-1-yl|ureido)-2-oxo-2H-pyridin-1-yl)meth ansulfonamide, benzoamide B5-tert-butyl-7-13-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl/ureido)benzoxazole-2-carboxylic acid, 2- (5-tert-butyl-7-13-(4-(6-morpholin-4-ylmethylpyridin-3-yl)/naphthalene-1-ylureido)benzoxazol-2-yl)acetamide, Ge!

B-tert-butyl-2-methoxy-3-13-14-(6-morpholin-4-ylmethylpyridin-3-yl)unaphthalin-1-yl/ureido)benzamide and their pharmaceutically acceptable derivatives. --

Any compounds according to the invention containing one or more asymmetric carbon atoms can exist in the form of racemates and racemic mixtures, individual enantiomers, diastereomeric mixtures and individual diastereomers. All such isomeric forms of these compounds are included within the scope of this invention. Each stereogenic carbon atom can be in the K- or 5-configuration or in a combination of such configurations.

Some of the compounds of formulas (I), (Ia), (I) and (PP) can exist in more than one tautomeric form. All such tautomers are included within the scope of this invention. в с All terms used in this description have, unless otherwise indicated, generally accepted meanings in the field. So, for example, "C -C.alukoxy group" is C 4-C,alkyl with a terminal oxygen atom, ;» in particular methoxy-, ethoxy-, propoxy-, pentoxy- and hexoxy group. All alkyl, alkenyl and alkynyl groups can be branched or unbranched, if this is possible from the point of view of their structure and if not

Other specified. Other specific terms used in this specification are defined below. -I The term "aroyl" in the context of this description means "benzoyl" or "naphthoyl".

The term "carbocycle" means an aliphatic hydrocarbon radical containing from three to twelve carbon atoms. Carbocycles include hydrocarbon rings containing three to ten carbon atoms. Such

Ge) carbocycles can be either aromatic or non-aromatic ring systems. Non-aromatic ring systems can be mono- or polyunsaturated. Examples of preferred carbocycles include (but are not limited to) cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl,

He cycloheptanyl, cycloheptenyl, phenyl, indanyl, indenyl, benzocyclobutanyl, dihydronaphthyl, tetrahydronaphthyl, naphthyl, decahydronaphthyl, benzocycloheptanyl and benzocycloheptenyl. Certain terms relating to cycloalkyl, such as cyclobutanyl and cyclobutyl, may be used interchangeably.

The term "heterocycle" refers to a stable non-aromatic 4-8-membered (but preferably 5- or b-membered) monocyclic or non-aromatic 8-11 membered bicyclic heterocyclic radical, which may be (F, saturated or unsaturated. Each heterocycle consists of carbon atoms and one or more, optimally 1-4, heteroatoms selected from nitrogen, oxygen, and sulfur. The heterocycle may attach through any ring atom resulting in a stable structure. Unless otherwise noted, examples of heterocycles may be ( але не обмежуючи тільки ними) оксетаніл, піролідиніл, тетрагідрофураніл, тетрагідротіофеніл, піперидиніл, піперазиніл, морфолініл, тетрагідропіраніл, діоксаніл, тетраметиленсульфоніл, тетраметиленсульфоксидил, оксазолініл, тіазолініл, імідазолініл, тетрагідропіридиніл, гомопіперидиніл, піролініл, тетрагідропіримідиніл, декагідрохінолініл, декагідроізохінолініл, тіазолідиніл, дигідрооксазиніл, dihydropyranil, oxocanil, heptacanil, thioxanil, dithianil or 2-oxa- or 2-thia-5-azabicyclo|2.2.1)heptanyl. 65 The term "heteroaryl" refers to an aromatic 5-8-membered monocyclic or 8-11-membered bicyclic ring containing 1-4 heteroatoms such as M, O, and 5. Unless otherwise specified, such heteroaryls include pyridinyl, pyridonyl, quinolinyl, dihydroquinolinyl, tetrahydroquinoyl, isoquinolinyl, tetrahydroisoquinoyl, pyridazinyl, pyrimidinyl, pyrazinyl, benzimidazolyl, benzthiazolyl, benzoxazolyl, benzofuranyl, benzothiophenyl, benzpyrazoles, dihydrobenzofuranyl, dihydrobenzothiophenyl, benzooxazazolonyl, benzo-3,benzoxol, 1,3|dioxol-2-onyl, tetrahydrobenzopyranyl, indolyl, indolinyl, indolonyl, indolinonyl, phthalimidyl.

The term "heteroatom" as used herein refers to atoms other than a carbon atom, such as o,

M, Bi R.

The term "aryl" as used herein means an aromatic carbocycle or heteroaryl as defined above. 70 Terms analogous to the above cyclic residues, such as aryloxy or heteroarylamine, mean aryl, heteroaryl, heterocycle as defined above attached to their respective group.

In the context of this description, the terms "nitrogen" and "sulfur" include any oxidized form of nitrogen and sulfur and the quaternized form of any nitrogenous base.

The term "halogen" as used herein means bromine, chlorine, fluorine or iodine.

The compounds of the invention include only those compounds that are considered to be "chemically stable" as understood in the art. So, for example, a compound with a "mobile valency" ("Zapoiipou maiepsu") or a "carbanion" do not fall under the compounds of the invention.

The scope of the invention also includes pharmaceutically acceptable derivatives of compounds of formulas (I), (Ia), (I) and (PO.

The term "pharmaceutically acceptable derivative" refers to any pharmaceutically acceptable salt or pharmaceutically acceptable ester of a compound of the invention or any other compound which, when administered to a patient, is capable of being converted (directly or indirectly) into a compound of the invention, its pharmacologically active metabolite, or its pharmacologically active balance. "Pharmacologically active metabolite" here means any compound of the invention capable of enzymatic or chemical metabolism. Examples of such compounds are hydroxylated or oxidized derivatives of compounds of formulas (I), (Ia), (II) or (11). high school

Pharmaceutically acceptable salts of the compounds of the invention include salts obtained from pharmaceutically acceptable inorganic and organic acids and bases. Examples of suitable acids include hydrochloric, i) hydrogen bromide, sulfuric, nitric, perchloric, fumaric, maleic, phosphoric, glycolic, lactic, salicylic, succinic, toluene-p-sulphuric, tartaric, acetic, citric, methanesulfonic, formic, benzoic, malonic, naphthalene-2-sulphuric and benzenesulfonic acids. In addition, other acids can be used, such as oxalic acid, which, although not pharmaceutically acceptable in themselves, can nevertheless be used to obtain salts suitable for use as intermediates in the process of obtaining the compounds according to the invention and their pharmaceutically acceptable acceptable acid additive salts. Salts obtained from the corresponding bases include salts of alkali metals (for example, sodium), salts of alkaline earth metals (for example, magnesium), ammonium salts, and M-(C.-C;alkyl)4 salts. t

In addition, compounds according to the invention include prodrugs of compounds of formulas (I), (Ia), (I) and (PI). Prodrugs are in are such compounds that, as a result of a simple chemical transformation, turn into compounds according to the invention.

Such simple chemical transformations are hydrolysis, oxidation and reduction. So, in particular, when prodrugs according to the invention are administered to a patient, such prodrugs can be transformed into a compound according to the invention, thus exhibiting the targeted pharmacological effect.

Methods of application ts In the invention, methods of application of compounds of formulas (I), (Ia), (II) and (1) are proposed. The compounds of the invention effectively block the production of inflammatory cytokines by cells. Inhibition of cytokine production is a promising method of prevention and treatment of various diseases associated with excessive production of cytokines, such as diseases and pathological conditions associated with inflammation. Thus, the compounds of the invention can be used to treat such conditions. These conditions include chronic inflammatory diseases, including but not limited to osteoarthritis, multiple sclerosis, Guillain-Barré syndrome, Crohn's disease, ulcerative colitis, psoriasis, graft-versus-host disease, systemic lupus erythematosus, and insulin-dependent diabetes mellitus. diabetes. The compounds of the invention can also be used for the treatment of other disorders associated with the activity of pro-inflammatory cytokines present in elevated concentrations, such as responses to various infectious agents and numerous autoimmune diseases, such as rheumatoid arthritis, toxic shock syndrome, diabetes and inflammatory bowel disease, which do not belong to the diseases listed above, and which o) is described in the section "Prerequisites for the creation of the invention".

In addition, since the compounds of the invention are inhibitors of cytokine production, it should be expected that they should block the expression of inducible cyclooxygenase (COX-2). It was established that the expression of COX-2 is enhanced under the influence of cytokines, and it is assumed that this cyclooxygenase is an isoform

GF! cyclooxygenase, responsible for inflammation (M.K., O'vapiop, etc., Rhos. Maiyi). Asad All together. O.5.A., 89, 4888, 1992). Therefore, it should be expected that the new compounds of the invention should be effective against those diseases that are currently amenable to treatment with COX inhibitors, such as conventional non-steroidal anti-inflammatory drugs (NSAIDs). Such disorders include acute and chronic pain, as well as inflammatory symptoms and 60 cardiovascular diseases.

As mentioned in the section "Prerequisites of the invention", II-8 affects the influx of neutrophils to the sites of inflammation or damage. Thus, according to another object of the invention, the compounds of the invention can be used to treat diseases that are primarily mediated by neutrophils, such as stroke and myocardial infarction, resulting from or independent of thrombolytic therapy, heat injury, because respiratory distress -adult syndrome (ADDS), multiple organ damage as a result of trauma, acute glomerulonephritis, dermatoses that include components of acute inflammation, acute purulent meningitis or other disorders of the central nervous system, hemodialysis, leukopheresis, syndromes associated with granulocyte transfusion, and necrotic enterocolitis

For therapeutic purposes, the compounds of the invention may be administered in any suitable dosage form by any conventional route. Such methods of administration include (but are not limited to) intravenous, intramuscular, subcutaneous, intrasynovial, infusion, sublingual, transdermal, oral, or inhalation. Oral and intravenous methods of administration are best.

The compounds of the invention can be administered individually or in combination with adjuvants that increase the stability of inhibitors, facilitate the administration of pharmaceutical compositions of certain types that contain them, 70 provide higher solubility or dispersibility, increase inhibitory activity, provide the possibility of adjuvant therapy, etc. ., as well as with other active substances. In such combined therapies, lower doses of conventional therapeutic agents are optimally used, which allows to avoid possible toxic and harmful side effects that occur when such agents are used for monotherapy. The compounds of the invention can be physically combined with conventional therapeutic agents or other adjuvants in one pharmaceutical composition. Optimally, the compounds should be administered together as one standard dosage form. In specific embodiments, pharmaceutical compositions comprising such combinations of compounds contain at least about 595, more optimally at least about 20,905 (w/w), compounds of formula (I), (Ia), (I) or (IP) or combinations of these compounds. The optimal percentage content (95% by weight) of the compound according to the invention may vary and should be determined by specialists in this field. Alternatively, the compounds can be administered separately (serially or in parallel). Threaded injection allows for a more flexible dosing regimen.

As noted above, the dosage forms of the compounds of the present invention include pharmaceutically acceptable carriers and adjuvants known to those skilled in the art. Such carriers and adjuvants include, for example, ion exchange resins, aluminum oxide, aluminum stearate, lecithin, whey proteins, buffering agents, water, sodium salts or electrolytes, and cellulose-based compounds. The best dosage forms include tablets, capsules, caplets, liquids, solutions, suspensions, emulsions, lozenges, syrups, renewable powders, granules, suppositories, and transdermal patches. Methods of preparation of such dosage forms are known (see, for example, N.S. Apvei and M.O.

Roromizi, Riagtaseciisai Juozade Rogts apa Ogid Oeiimegu Zuvietv, 5th ed., ed-vo I ea apa Rebideg (1990)).

Dose levels and requirements are well known in the art and can be selected for a particular patient based on available methods and tools. In certain embodiments, dose levels are approximately 1-100 Ωg/dose for a patient weighing 7Okg. Although one dose per day may be sufficient, up to 5 doses per day are acceptable. When administered orally, a dose of up to 200 Ωg/day may be required. Gee!

A person skilled in the art can independently determine which - lower or higher - doses may be needed depending on specific factors. So, for example, specific doses and modes of administration may depend on such factors as the general state of health of the patient, the severity and progression of the disease in the patient or his predisposition to it, and they should be prescribed by the decision of the supervising physician.

Below, the invention is illustrated by examples. These examples illustrate preferred embodiments of the present invention and should not be construed as limiting its scope in any way.

Since, as stated above, the following examples are illustrative, it is obvious to those skilled in the art that, if necessary, specific reagents or reaction conditions for individual compounds can be changed accordingly. The starting products used in the reactions described below are either commercially available or readily obtainable by those skilled in the art from commercially available products. with General methods of synthesis

The compounds of the invention can be prepared by method A, B or C, as illustrated in scheme I, optimally

Method B. Additionally, such methods are described, for example, in PCT/O599/29165 and US patent applications -I 60/124148 and 60/165867. Each of these applications is incorporated herein by reference in its entirety. scheme! - Method A s r-nso o v. m o. AK sl 70 Mn, sidltl t y z iz m p

Method B 59 I. fosten 9) (F) scha ory with 2.0-M. nn dk Ia, 1st, or

M M SHE - MK) 60

Method B r-pl. Ge; in. SisOoRA in Kot m o.

MN, --- eh! !

N nn 65 IM Mi Ga, NP or

In the above scheme, Ю corresponds to the radical Ag-i (for compounds of formulas I and Ia) or b (for compounds of formulas I or II), БО' represents the group Ag 2-X-Ж-2 (or its predecessor) for compounds of formulas I and Ia or group

Ag-X-U-2 (or its predecessor) for a compound of the formula IYI or PP.

According to method A, a mixture of an amine of formula IM and an isocyanate of formula M is dissolved in an aprotic anhydrous solvent such as THF, ether, toluene, dioxane, or ethyl acetate. The best solvent is

THF. The mixture is stirred at a temperature from 0 to 45"C, optimally at 25"C, for 2-24 hours and volatile components are removed. Purification of the residue by recrystallization from a solvent suitable for this purpose, such as ethyl acetate/hexane, ethyl acetate/methanol, THF/petroleum ether, ethanol/water, or by chromatography on silica gel using, for example, hexane and ethyl acetate as eluents, gives the product of formula I , Ia, HER 7/0. or 1 (E means MH).

According to method B, the amine of formula IM is dissolved in a halogenated solvent such as methylene chloride or chloroform dichloroethane. The best solvent is methylene chloride. The mixture is diluted with aqueous alkali such as sodium bicarbonate or potassium carbonate, cooled in an ice bath and phosgene is added. The mixture is intensively stirred for 5-300 minutes, optimally for 10 minutes. The organic layer is dried with the help of such an agent as MaSO y or Ma»zO.), and the volatile components are removed to obtain the corresponding isocyanate 0О-М-С-ОО. This isocyanate and the amine of formula MI are then mixed in an aprotic anhydrous solvent such as

THF, ether, toluene, dioxane, methylene chloride or ethyl acetate. The best solvent is THF. The mixture is stirred at a temperature from 0 to 457"C, optimally at 25"C, for 2-24 hours and volatile components are removed. As a result of purification of the residue or recrystallization by chromatography on silica gel, as mentioned above, a product of formula I, Ia, Ii or PI is obtained (E means MH).

The required isocyanate can also be obtained from the carboxylic acid O-CO2H by reaction with a chloroformate, such as ethyl chloroformate, in the presence of an acceptable base, such as triethylamine, in a suitable solvent, such as THF, at a temperature of about 0°C. The resulting mixed anhydride is treated with aq. by a solution of sodium azide. When a solution of the obtained acyl azide is heated in a solvent suitable for this purpose, such as toluene, at approximately the distillation temperature, rearrangement occurs according to the Curtius reaction, which leads to the formation of the isocyanate O-M-C-O. i)

According to method B, the amine of formula IM is dissolved in an acceptable solvent, such as a halogenated solvent such as methylene chloride or chloroform dichloroethane. The best solvent is methylene chloride. At the same time, an acceptable base such as triethylamine can be added, followed by phenylchloroformate. The mixture is stirred with water at a temperature from 0 to 857C, optimally at the temperature of distillation, for 2-24 hours, and volatile components are removed to obtain the carbamate of formula II. This carbamate and amine of formula MI are mixed in an aprotic or anhydrous solvent such as THF, ether, toluene, dioxane, methylene chloride, or ethyl acetate. Best Ge! the solvent is THF. The mixture is stirred at a temperature from 0 to 1107"C, optimally at the distillation temperature, for 2-24 hours and the volatile components are removed. After purification of the residue, as described above, the product of the formula I, Ia, IYI or Z is obtained (E means MH). This method can also be carried out in the reverse sequence, i.e. first you can obtain a carbamate from C'MH»o and subject this carbamate to the reaction with an amine O-MH". Example 37 describes the process of synthesis of a compound of formula I, in which E means -O-, and in example 38, the synthesis of the compound of formula ІІ, in which E means -СН»о-, is considered.

The method used to prepare amines of formula IM depends on the nature of the target group 0. In Chilom, intermediates of formula IM can be prepared by methods known in the art. Some of these common methods are illustrated in the diagrams below. Compounds 0-МСО or 0-МНё on the scheme | is . commercially available compounds and can be obtained by methods known in the art If C is y? precursor of the Ago-X-Zh-2 or Ag-X-Zh-7 group, then the target end product of the formula !, Ia, I or I can be obtained by methods known in the field. Illustrative examples of such methods are given below

Below is the "Synthesis Examples" section. -I Aminopyrazoles of formula ХУ, necessary for obtaining compounds of formula I or Ia, can be obtained according to scheme II. Hydrazine of the formula X, bearing the Kz substituent, can be obtained by method G or D. According to the method - G, the aryl bromide of the formula MII is dissolved in an aprotic inert solvent, such as THF, 1,4-dioxane or

Ge) diethyl ether, and cooled to a low temperature in an inert atmosphere. At the same time, the best temperature for the solution is -777C. After that, a strong base dissolved in a non-protic inert solvent such as hexane, THF, or ether is added dropwise, maintaining the reaction temperature below RT.

He is optimally lower than -60"С. The best bases are alkyllithium reagents, the most optimal is t-butyllithium.

After adding the base, the reaction mixture is stirred for 30-9 minutes until the original aryl bromide is consumed. Next, an excess of dialkyl azodicarboxylate is added, maintaining the reaction temperature lower than bv OS, optimally lower than -60"C. It is optimal to use di-tert-butyl azodicarboxylate as a dialkyl azodicarboxylate. The reaction mixture is stirred at a reduced temperature and after completion

F) 0.5-2 hours are heated to room temperature. The reaction is stopped by adding water and the product is extracted with an aprotic solvent such as ethyl acetate, diethyl ether or chloroform. The organic layers are dried with agents such as Mo5O4 or Ma»5O), and volatile components are removed. The residue is dissolved in a protic solvent such as methanol or isopropanol, cooled, optimally to 0-57C, and treated with acid. At the same time, it is desirable to use hydrochloric, hydrobromic, sulfuric and trifluoroacetic acids.

Hydrochloric acid is best in gaseous form. After adding an excess of acid, the mixture is kept at the temperature of the distillation of the solvent until all the starting material is consumed. After cooling, the obtained arylhydrazine salt of formula X is filtered and dried. b5

HER scheme

Method D 1. the basis of Vg 2. 1-vpO, CM MSO-Vy

M. Shi

Method D, ku mim, sht x k.-MN, 1. mother;

THEM

2. restoration

Method B I. basis 9 SsnISM 2. KSO Me

Shi SHO Fr

Method Zh AK cm 1 -- hm

But see

Bush

XII Khni p

K, about

Method Z id

Metoya Y M z i

According to method D, an arylamine bearing a Kz substituent (formula IX) is dissolved in a concentrated aqueous cm ' C ' 30 acid, such as hydrochloric, hydrobromic, or sulfuric acid, and cooled to the temperature of an ice bath. At the same time, the best hydrochloric acid with a concentration of Zn . up to 8n., more optimally bn. Then a nitrosating agent is added dropwise in water, maintaining a reduced temperature. The best temperature is 0-57C. The best F reagent is sodium nitrite. The reaction mixture is stirred for 10-9 Ohv and then a reducing agent is added, while maintaining a reduced temperature. The best temperature is 0-57C. Zinc, iron, samarium iodide and stannous chloride can be used as a reducing agent. The best reducing agent is stannous chloride dissolved in aqueous hydrochloric acid with a concentration of Zn. up to 8n., more optimally bn. The reaction mixture is stirred for 0.5 hours and then the reaction is stopped by adding alkali to bring the p value to 12-14. At the same time, you can use such alkaline reagents as sodium hydroxide, potassium hydroxide, lithium hydroxide and calcium hydroxide. The best alkaline reagent is potassium hydroxide. The aqueous solution is extracted with an aprotic organic solvent such as diethyl ether, chloroform, ethyl acetate, and methylene chloride. The organic layers are dried with the help of such agents as MaOSO y and Ma»3O,, and volatile components are removed to obtain arylhydrazine :z» (formula X), which can be used in the next reaction without additional purification. p-Ketonitrile bearing the Ki substituent. (KHIM formula), can be obtained according to method E or Z.

According to method E, a metal hydride, such as sodium hydride, potassium hydride, or lithium hydride, is suspended in - 15 an anhydrous inert aprotic solvent, such as diethyl ether, THF, and dioxane, at a temperature ranging from 35 to 857°C. The best metal hydride is sodium hydride, and the best solvent is THF at a temperature of 757 C. Then, in an anhydrous inert aprotic solvent, such as diethyl ether, THF, or sodium dioxane, an alkyl ether, optimally methyl ether (formula XI), is dissolved, and acetonitrile and the resulting solution are added dropwise to the above metal hydride suspension. The best solvent is THF. The mixture is kept at elevated temperature for 3-24 hours, cooled to room temperature and diluted with aprotic "with solvent and aqueous acid. Then the organic layer is washed with water and brine, dried with the help of such agents as MazO; and Ma»zO), and volatile components are removed to obtain p-ketonitrile (formula KHM), which can be used further without additional purification.

In another embodiment, according to method G, a solution of a strong base, such as an alkyllithium and a metal amide, such as n-butyllithium, sec-butyllithium, methyllithium, and lithium diisopropylamide, in an anhydrous inert

HF) to an aprotic solvent, such as diethyl ether, THF, and dioxane, is cooled to a temperature below 07C. 7 The best base is n-butyllithium, the best solvent is THF, and the best temperature is -7776.

Next, a solution of cyanoacetic acid (formula XI) in an anhydrous inert aprotic solvent, such as diethyl ether, THF and dioxane, preferably THF, is added dropwise, maintaining the reaction temperature 60 below 0"C, optimally at -77"C. The reaction mixture is stirred for 10-45 minutes, heating it to 07C.

The cyanoacetic acid dianion solution is cooled to a temperature lower than -257"C, optimally to -77"7C. Then, alkyl acid chloride (formula XIII) dissolved in an anhydrous inert aprotic solvent such as diethyl ether, THF and dioxane, preferably THF, is added. The reaction mixture is heated for 10-3 hours to 0"7C and the reaction is stopped by adding aqueous acid. The product is extracted with an organic solvent, such as chloroform, ethyl acetate, simple ether, and methylene chloride. The combined organic extracts are dried using agents such as MozO and Ma»zO,), and volatile components are removed to obtain bb-ketonitrile (formula KHM), which can be used further without additional purification.

The target aminopyrazole (formula XM) can then be obtained according to method C or I. According to method C, arylhydrazine of formula X and p-ketonitrile of formula XIM are mixed in an organic solvent such as toluene, ethanol, isopropanol, or tert-butanol. The best solvent is ethanol. An acid such as hydrochloric acid, p-toluenesulfonic acid or sulfuric acid is then added. The best acid is concentrated hydrochloric acid. Next, the mixture is heated for 10-24 hours at a temperature of 50-1007C, optimally at 80"C, and then cooled to room temperature. The mixture is diluted with an aprotic organic solvent, such as ethyl acetate, simple ether, chloroform or methylene chloride, and washed with aqueous alkali, such as sodium bicarbonate and potassium carbonate. The organic layer is dried with agents such as MazoO y; eluents.Further, fractions with a high product content are collected and volatile components are removed to obtain the target aminopyrazole (formula XM).

In another variant, according to method I, arylhydrazine of formula X and p-ketonitrile of formula XIM are mixed in an organic solvent such as toluene, ethanol, isopropanol or tert-butanol. The best solvent is toluene.

The mixture is kept at the distillation temperature for 3-24 hours with azeotropic extraction of water, and after the processing described above, aminopyrazole of the formula ХУ is obtained.

Other necessary aminoheterocycles that can be used in the synthesis of compounds of formula I! or Ia, 2o can be obtained by methods known in the field and described in the literature. The examples shown in the following P-XM schemes are illustrative and, as is obvious to those skilled in the art, specific reagents and reaction conditions may vary depending on individual compounds. The intermediates used in the reactions in the schemes below are either commercially available or can be easily prepared by those skilled in the art from commercially available materials. high school

Scheme II, method K, illustrates the general process of synthesis of target aminothiophenes.

Scheme of HER Ge)

Metva K o resent K,

Lakoesona s vyt tn t siu ih 1 s y Ku km HM o

In, (22)

I. nitrate di - ---- 5 - 2. reduction of two

KhPI

A mixture of 1-aryl-5-alkylbutane-1,4-dione (HMI) and a sulfating agent such as Lavesson's reagent (Iaulgezzop) or phosphorus sulfide (M), optimally Lavesson's reagent, is dissolved in an aprotic anhydrous solvent such as toluene, THF or dioxane. The best solvent is toluene. The mixture is kept with heating at an elevated temperature, optimally at the solvent distillation temperature, for 1-1 hours. After C c extraction of volatile components, the residue is purified by chromatography on silica gel using hexanes and ethyl acetate as an eluent. Fractions with a high product content are collected and volatile components are extracted to obtain a substituted thiophene of the formula CHMI.

This substituted thiophene of the formula CHMII is dissolved in a solvent such as acetic anhydride or acetic acid. The best solvent is acetic anhydride. The mixture is cooled to 0-30"C, optimally to -102C. Next, a solution of concentrated nitric acid in a solvent such as acetic anhydride or acetic acid, optimally acetic anhydride, is added, cooling the mixture to 0-307C, optimally to -10"C . Then the mixture is stirred for 10-120 minutes, poured onto ice and extracted with an aprotic solvent such as diethyl ether, chloroform, ethyl acetate or methylene chloride. Organic extracts are washed with aqueous alkali, dried with 20 using such agents as MoZO 5 and Ma»5O), and volatile components are removed. The residue is purified by chromatography on silica gel using hexanes and ethyl acetate as eluents. Fractions with a high g" content of the product are collected and volatile components are removed to obtain 2-aryl-5-alkyl-3-nitrothiophene. This 2-aryl-5-alkyl-3-nitrothiophene is reduced with a metal such as iron, tin or zinc or by catalytic hydrogenation. It is optimal to use iron in acetic acid for reduction and carry out such reduction at a temperature in the range from 50 to 110, more optimally at 1002С, for 5-3ZOhv. After

HF) cooling to room temperature, the reaction mixture is diluted with water, neutralized with an alkali such as sodium hydroxide, potassium hydroxide, potassium carbonate or sodium bicarbonate, and extracted with an aprotic solvent such as diethyl ether, ethyl acetate or methylene chloride. The organic extracts are dried with agents such as Ma5O and Ma»z O, and the volatile components are removed to obtain the target aminothiophene of the formula 60 XM.

The IM scheme illustrates the general method of obtaining the required aminofurans, as described in Ziemepzop et al. (U. At. Spet. boss, 1937, 59, 2525). In this case, ethylaroyl acetate (formula XIX) is dissolved in an aprotic solvent, such as ether or THF, and treated with a strong base, such as sodium, sodium ethoxide, or sodium hydride, and the resulting anion is reacted with bromomethylalkylketone (formula XX) at a reduced temperature, for example at 02С. After stirring the reaction mixture until all the starting material is consumed, it is poured into cold water and extracted in an aprotic solvent. The combined extracts are then dried using such agents as Mo95O5 or Ma»ZO,. The resulting diketoether (formula XXI) can be used further without further purification or purified by distillation or chromatography on silica gel.

Next, the diketoether in a protic solvent, such as ethanol, is heated in the presence of a mineral acid, such as sulfuric or hydrochloric acid, for 5-10 hours and extracted with an aprotic solvent. The combined extracts are then dried with agents such as (Ma 5 O) or Ma 3 2 O). The obtained furan ether (formula XXIII) can be used further without additional purification or purified by distillation or chromatography on silica gel. Next, this furan ether in a protic solvent such as ethanol is treated with hydrazine hydrate and the 7/0 boom is kept with heating for 2-5 days. After that, hydrazine is isolated according to the method described above and treated with hot formic acid, after which the obtained furanamine (formula XXIII) is purified by distillation or chromatography on silica gel.

Scheme IX o o o o base 19 you ov i was ---- What ) Kk, хих хх хх B y hydrazine-v, acid o ke hydrate o re

Pt - -0th heating of acid in MH,

Kk in,

XXI XXI

Substituted 4-aminooxazoles can be synthesized similarly to the method described in I akpap et al. (9). Nei Spet., "M 1988, 25, 1413) and illustrated in scheme M. At the same time, a mixture of aroyl cyanide (formula XXIM), aldehyde o (formula XXU) and anhydrous ammonium acetate in acetic acid is kept with heating at 100-1107С for

By the way, cool to room temperature and then stop the reaction by adding water. After extraction with an aprotic solvent, a product of the formula XXMI is obtained, which can be used further without additional purification or purified by recrystallization or chromatography on silica gel. Ge

Scheme in

Khri MNuOAs eh yu vuktom KO yan nos uv, Me. you -

XXI xx xx

Substituted 3-aminopyrroles (formula XXX) can be synthesized analogously to the method described in Aieyo et al., 9. i-

Spent Zos. Regkeepz Tgapv. I, 1981, 1. This method is illustrated on the MI scheme. In this case, the mixture of aryldioxoalkane (formula XXMII) and amine (formula XXMII) in acetic acid is kept with heating at 100-110" for 3 hours and then processed in the usual way. After that, the product obtained (formula XXIX) in acetic acid is treated with a nitrating agent , such as nitric acid or potassium nitrate in concentrated sulfuric acid. The mixture is further poured into cold water and extracted with an aprotic solvent. The combined extracts from C are then dried with agents such as Mo5O; and Ma»5O). Obtained after removal of volatiles components "» nitropyrrole can be used further without further purification or purified by recrystallization or " chromatography on silica gel. This nitropyrrole is reduced to the amine with the help of iron in acetic acid or by catalytic hydrogenation using palladium on activated carbon. The resulting aminopyrrole (formula XXX) can be used further without additional purification or purify by recrystallization or chromatography on silica gels - Scheme MI o ik vt i k--MN, Ya, 5003 heating o o what) XX XXI

Kk, Kk, "7 in-M our in-

GF) and their 2. restoration and in 2 to t, R.

ХХХ ххх 6о Similarly, a mixture of amine of formula XXXI and 3-aryl-2,5-dioxoalkane (formula XXXI) in acetic acid is kept with heating at 80-1107C for 2-24 hours. Then the reaction mixture is diluted with water and extracted with an organic solvent. After that, the combined extracts are dried using agents such as MoZO/; or

Mao), and then the volatile components are removed. The resulting pyrrole is treated with a nitrating agent, and then reduced to the compound of formula XXXI according to the method described above. The obtained product can be used further without additional purification or purified by recrystallization or chromatography on silica gel. This process is illustrated in the MY diagram.

Scheme of MP their 9 1 НОдс у - НОо-ШН в ! many; M not 2. heating a

In about 3. restoration yet

xxxi xxxi xxxi! 70 Substituted 5-aminothiazoles (formula XXXMII) can be obtained analogously to the method described in Segmaia et al.,

U. Rhakb Spet. 1973, 315, 539. As shown in Scheme IIi, a base such as triethylamine is added dropwise to a mixture of an aminocyanide of formula XXXIM, an aldehyde of formula XXXU, and sulfur in an anhydrous solvent such as ethanol or methanol. The mixture is kept with heating at 507"C for 1 hour. After that, the mixture is cooled and the excess sulfur is removed. Next, acetic acid is added to the mixture to neutralize it and a solid 7/5 substance is collected. The obtained imine of the formula XXXMI is treated with an acid such as hydrochloric or toluenesulfonic acid, in water and an organic solvent After the starting material has been consumed, the reaction mixture is processed to give the product of formula XXXMII, which can be used further without further purification or purified by recrystallization or chromatography on silica gel.

MI scheme

V, sm o u-8 4 Z Y yo pic l Mrya Gchyy 1 in MN. in n

With 2 1 base and sch

XXX XXX XXXMI Fr

K. acid in water in, c in, t)

XXIII Ge"!

Substituted 2-aminothiophenes (formula XXXIX) can be synthesized analogously to the method described in Semaia et al. (U. Rgaki Spet., 1973, 315, 539) and illustrated in the scheme of THEM. At the same time, a mixture of disubstituted thiophene-Z-carboxylic acid (formula XXXMIII) in a protic solvent, such as acetic acid, is treated at a temperature of 0-50"C with a nitrating agent, such as nitric acid or potassium nitrate in concentrated sulfuric acid. After spending the original material, the reaction mixture is poured onto ice, and the product is extracted with an aprotic solvent. The combined extracts are dried with agents such as Mo 5 O y and "

Ma»zoO,, and volatile components are removed. The resulting nitrothiophene is reduced to the amine using iron in acetic acid or catalytic hydrogenation using palladium on activated carbon. The obtained aminothiophene can be used further without additional purification or purified by recrystallization or chromatography on silica gel. "» Their scheme

Kk, dream 1. acid K, - Kk; 5 2. recovery in; 5 MN, ise) XXXHM! XXXIX 1 20 i i inopi i i i I 1,5-disubstituted 3-aminopyrazoles (formula XIII) can be obtained according to scheme X, analogous to the method,

Ge described in Ede et al. (9. Nei. Spet., 1982, 19, 1267). At the same time, potassium is added to anhydrous tert-butanol and the mixture is cooled to 5"C. After that, hydrazine of the formula Xi is added, and then cyanodibromalkane of the formula XH.

Next, the mixture is heated under reflux for 3-10 hours at the distillation temperature. After that, the mixture is cooled to room temperature and poured onto a mixture of water and ice. The obtained product is extracted with an organic solvent. The combined extracts are dried with agents such as Mo5O, or (F, Ma»3O), and the volatile components are removed. The resulting product of formula XIII can be used further without additional purification or purified by recrystallization or chromatography on silica gel.

Schemes 60 Ve tert-butoxide Kk, vA-MAMN., Zh B, potassium -p7- cMo-H- SHYN M

М, иВвчОоН m Я хи хи ХЙЙ in 2-amino-3,5-disubstituted thiophenes can be synthesized according to scheme Хи, similar to the method described in

Come on! et al., U. Rgaki Spet., 1985, 327, 463. At the same time, a mixture of substituted M-(3-aminothisacryloyl)rorhamidine -B50-

(formula CP) and substituted bromide (formula CHM) in a protic solvent, such as methanol or ethanol, is heated, optimally kept at the distillation temperature for 5-3 minutes and then cooled to a temperature lower than room temperature. The obtained thiophenimine is filtered and dried. Further, thiophenimine of the formula CHM is converted into thiophenamine (formula Kh. MI) by treatment with aqueous acid.

The scheme of the ХІ вн heating of the windings І and кня ВО ВІТВО00--- 70 Р,

Hmm hmm

Kk, V, / 5 vodnya Y Z

ZM 7-60

OM acid and MH,

In in,

CHEM CHEM

1,4-disubstituted 2-aminopyrroles (formula I) can be synthesized similarly to the method described in VgoaigiskK et al. (U. Spet. Zos. RegKip Tgapv. I, 1975, 1910) and illustrated on the scheme of KhIi. At the same time, the potassium salt of formylnitrile of the formula CHEMISTRY! in water is treated with an amine of the CHEMISTRY formula and with acetic acid and the mixture is kept with heating at 50-907C for 5-30 minutes. After cooling, the resulting aminonitrile of the formula XII is collected by filtration and then stirred at room temperature in the presence of a base, such as ethanolic potassium ethoxide, for 2-5 hours and the volatile components are removed. The residue is diluted with water and extracted with an organic solvent. The combined extracts are dried with agents such as MaoSO; and Ma»zO,, and remove volatile i) components. The resulting product (formula D) can be used further without further purification or purified by recrystallization or chromatography on silica gel.

Scheme of the 12th school

B, Io) in the acid SM bultem I VAM, set same | b" heating of MN sno I

HOM HOM K, -- hih cha

IN,

KO! ud "

EUN mot;

Kk, - with and . ,» 1,2-disubstituted 4-aminoimidazoles (formula GII) can be obtained by reduction of the corresponding nitro compound (formula II), for example, with the help of iron in acetic acid or catalytic hydrogenation, by the method described in AI-Zpaag et al. (9. Spet. Zos. Regkip Tgapz. I, 1992, 2779) and illustrated on the HIPI diagram. - and Scheme of the HYIA

In | in -th M restoration of M x

X Fri

F vychynu, cue, p. 50

ISH IP g» 2,4-disubstituted 5-aminooxazoles (formula HMII) can be obtained similarly to the method described in Roiraeg et al. (Zupipeziv, 1972, 622) and illustrated on the KHIM scheme. In this case, acid chloride of the formula IP is added to a cooled mixture of 2-aminonitrile of the formula GIM and a base such as triethylamine in an aprotic solvent such as THF, benzene, toluene, or ether. The best temperature is 02C. Mixture

HF) are stirred for 12-24 hours and washed with water. After extracting the volatile components, the obtained product of formula IM is treated with ethyl mercaptan and dry hydrogen chloride in dry methylene chloride for 5-3 hours. where The solid hydrochloride of 5-imino-1,3-oxazole (IMI formula) is collected by filtration, dissolved in dry pyridine and the solution is saturated with hydrosulfide for 4 h at 0"C. The mixture is diluted with an organic solvent, 60 is washed with water and dried. After extraction of volatile components obtain 5-amino-1,3-oxazole (formula

YIMII), which can be used further without additional purification or purified by chromatography on silica gel. b5

The scheme of chemical engineering and metallurgy, the basis of G ik:

And I ra -08-- you A vus tem y, 9 WE What they in. Kk,

EN uro pyridine ze -- - M MN ----- M Mn, not in. She

IM LEE

1,4-disubstituted 2-aminopyrazoles can be synthesized according to the XM scheme by the method described in I Apsip et al., U. Nei. Spet., 1966, 3, 152. At the same time, aqueous sodium hydroxide is added to the mixture of substituted amino ketone (IMI formula) and cyanamide in 75% water and acetic acid until the p value reaches 4.5. After that, the mixture is kept with heating at 50-907C for 1-5 hours, cooled and alkalized with ammonium hydroxide.

The resulting product of formula IH is collected by filtration and dried.

Scheme of ХУ

In water and food, pH 45, weighing, to nM-SM ---- «kv, ' heating |І

Kk

SM them

Arylamine and heteroarylamine intermediates of the formula IM (5-MH") for the synthesis of compounds of the formulas I! and I are either commercially available products or can be readily obtained by methods known in the art. Thus, (8) for example, the required arylamines and heteroarylamines can be obtained by nitration and reduction of a substituted aryl or heteroaryl ring, as illustrated for the synthesis of some 5-membered heterocyclic amines (Ag/-MNo) in the above schemes. In another variant, a substituted aryl ether can be converted from zo to an arylamine, as illustrated for the substituted furan in the above scheme M and described below in example 17. In the section "Examples of synthesis" the processes for the preparation of other compounds З-МН» and Agi- MN". at

Methods that allow obtaining intermediate products of the formulas M and Mi (scheme I, ОЯ' means the group Ag-X-U-727 or Ge!

Ago-X-U-7), described below.

Scheme ХУ1 че

Method /L - (c) РО(РАЗ)»ІІ; 9) dFFp c nya pot -

Nama We Mu omanso; but p" dMF Ag p « their IHI then their p 1-4

Ag-Agabo Ag, Method B or B | shi s (o) and phosgene He) and » ss, Method A

IH --- --- -zh LYA Y. water. MANSO» OosM r y Ag v

Os TA d -I SH ihM -

Method M se) ! 1. EV ikh sia 70 Veh-o teya- o VvyHO0-t 0 NAlaEHO

In 2. Vshbpsi their RO(RRPU); SUMI r» O0-U-2 or Ag Agabo Ag, predecessor

According to Method L (scheme XMI), a bromoarylamine of the formula XI, which may either be a commercially available product or readily available to one skilled in the art, is reacted with a cycloalkenone of the formula XI in the presence of a transition metal catalyst, such as a catalyst based on ) palladium(I), such as bis(triphenylphosphine)palladium(I) chloride, and in the presence of a bis(triphenylphosphine) chelating agent such as 1,2-bis(idiphenylphosphino)ethane (DFFE), 1,1'-bis( idiphenylphosphino)ferrocene 60 (DFFF) or 1,3-bisidiphenylphosphino)propane (DFFP), optimally DFFF, and a base, optimally sodium bicarbonate, in an acceptable solvent, optimally DMF, at a temperature of about 1507C to give a compound of formula I XII. This compound of formula IXIII can then be used (as a compound of formula MI) in method B (Scheme I) or converted to an isocyanate of formula IXII by reaction with phosgene or a phosgene equivalent in the presence of a base such as sodium bicarbonate in a suitable solvent such as dichloromethane , at a temperature of about 0"C and used (as a compound of formula M) in method A. The resulting product of formula I can be further modified by methods known to those skilled in the art to provide the target compounds of formula and as described below examples of synthesis.

According to method M, a bromide of formula XM is reacted in the presence of a strong base such as tert-butyllithium in an acceptable solvent such as THF with tributyltin chloride at a temperature in the range of about -50 to -100°C, optimally at about -78°C , with the preparation of the compound of formula I HMI.

This compound of formula I HMI is further reacted with a compound of formula I X in an acceptable solvent such as

THF o or 14-dioxane, in the presence of a catalyst based on a transition metal, optimally tetrakis(triphenylphosphine)palladium(0), at a temperature from about 50 to 1507C, optimally at about 1007C, in a hermetically sealed tube to obtain a compound of formula I KhMII. This compound of formula I CHMII 7/0 can then be used (as a compound of formula MI) in method B or B (Scheme I) or converted to the corresponding isocyanate as described for method L and used (as a compound of formula M) in method A.

The CHMI scheme illustrates the methods that allow the attachment of Y and 27 to X. According to method H, if necessary, a product can be obtained in which XU includes an amine nitrogen attached to X, the group X containing a ketone can be reacted with the group M-7, containing a terminal primary or secondary amine, under the conditions of 7/5 Podroamination. For example, a ketone of the formula CHM is combined with a primary or secondary amine in an acceptable solvent such as THF. Next, an acid such as acetic acid is added, followed by an acceptable reducing agent, optimally sodium cyanoborohydride or sodium (triacetoxy)borohydride, to give the target product of formula I CHEMISTRY.

Using the example of the OO method, the process of obtaining a methylene group for M and a primary or secondary amine for 7 is illustrated. At the same time, the X group, which carries an aldehyde and a halogen, optimally bromine (formula I XIX), can be subjected to interaction with a primary or secondary amine under the conditions of hydroamination , as described for method H, to obtain a compound of formula I XX. This intermediate can then be used similarly to method M.

Scheme of HM

Method H mV s 25 o o ! MNE nn 7 OA Zh, A r Shy Ag iv hydproami- o Viy ch y

iv) the encouragement of Fr

ХМ ХМ s 30 pe 1-4 -M(VUV t «7-7 yu

Ag Agabo Ag, pa b

Method 0 h- 35 MNE: h vVeZhSNO 0---- 0 VEH-SNAMSCHEA hydproami-

As in the cases discussed above, additional intermediates corresponding to the formulas M, MI, and MI can be synthesized by methods similar to those described in the literature or known to specialists in the field. Several examples of such synthesis are given below in the section "Examples of synthesis". :z» Examples of synthesis

Example 1 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(2-cyclohexenon-3-yl)naphthalen-1-yl|Urea-I 19 ) - Ve NI RI(RRNU'SI;

Nn leey. manso, (Se) zh a i o " no Ya

N ho lm, 1509 M s 50 n

XXI XX

Ko) sisosiI about | s piaslyudyka SO, her so

And I In the village

Ayu

M n (F; "m A F

She M o F pF, Kg 60 1 XXI

According to the method L described above, 4-bromo-1-naphthylamine (IXHI) (1.97g, 8.Omoles, Eq.), 2-cyclohexenone (1.65g, 17 .2 mmol, in 1.0 equiv.), powdered sodium bicarbonate (2.17 g, 25.8 mmol, 2.9 equiv.), 1,3-bis(diphenylphosphino)propane (177 mg, 0.4 mmol, 0.05 equiv.), bis(triphenylphosphine)palladium(i) chloride (302 mg, O0.4 mmol, O, Obeq.) and DMF (degassed,

100 ml). The mixture is kept with heating at 15073 for 8 hours. After cooling again to ambient temperature, the mixture is diluted with 100 ml of ES and filtered through diatomaceous earth. Next, this solution is transferred to a separatory funnel and washed with water (100 ml) and saturated brine (100 ml). After drying over Mo5oO, volatile

The components are removed under vacuum. The product is then purified by column chromatography using EtOAc (from 10 to 5095) in hexanes as an eluent to obtain 1.3 g of material, which is recrystallized from a hot mixture

EtOAc/hexane to obtain 800 mg of the compound of formula I XXI! (3.4 mmol, yield 3895) as a dark brown solid.

The compound of the formula I XXIII (10 Ω, 0.42 mmol, Teq.) is dissolved in methylene chloride (20 ml) and a saturated 70% aqueous solution of sodium bicarbonate (20 ml) is added. The mixture is intensively stirred at 0"C for 15 min. Then the stirring is interrupted and phosgene (approximately 2.0 molar solution in toluene, 0.b3ml, 1.2 bmmol, 3.Eq.) is added to the organic layer in one portion using a syringe. Directly. after that, stirring is resumed and continued at 0"C for 20 minutes. Then the layers are separated, after which the aqueous phase is extracted with methylene chloride (1x25 ml). The combined organic phases are dried (Ma»5O)), filtered and 7/5 of the solvent is removed under vacuum. Immediately after this, this solution of the isocyanate of the formula IXXIII is diluted with anhydrous THF (8 ml) and treated with the compound of the formula IXXIM at room temperature (method A). The mixture was then allowed to stir overnight under a nitrogen atmosphere, after which MeOH (2 mL) was added and the volatiles were removed in vacuo. In this way, the title compound 1 is obtained as a yellow-brown/red foamy substance (200 mg, 0.4 mmol, 7495). This product was recrystallized twice overnight from EtOAc to give 49 mg of yellow crystals (dL 168-170°C).

Example 2 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-14-3-(morpholin-4-yl)cyclohexen-1-yl|Inaphthalen-1-yl ) section of (9) 25 Y | 0, to her s by ba so o shk shk 2 snnn-- that "AH SHCHI a non shh mavgolsn | | Phew theo. AsON nn n o, h 30

According to method H described above, the product from example (1) (9Uzmg, 0.19mmol, eq.) and morpholine (30mcl, about 0O, Za4mmol, 1, eq.) are dissolved in 1.0ml of anhydrous THF and treated with acetic acid (1bmcl . The reaction mixture is stirred at room temperature for 2 days, and then a 595% aqueous Mahon solution (3ml) is added, and after that the reaction (735ml) is extracted with EtOAc (3x3ml). The combined organic phases are washed once with water and then with brine, - dried (Ma»3O, filtered and the solvents are removed in a vacuum. After column chromatography using

EOAc/hexanes as an eluent yield 4 mg of a yellowish-brown foamy substance (0.11 mmol, 6090). This product was re-chromatographed using 59o MeonH in methylene chloride to give the title compound 2 as a pale purple foam (50mgHg). " 40 Example C z c 115-tert-butyl'2-p-tolyl-2H-pyrazol-3-yl 3-C-15(morpholin-1-ylmethyl)fur-2-yl-naphthalen-1-yl)urea and shchi o x 1revsh z ved shiy MO 7) Vokhvpsi son, Ma(Nv(OAsi)zY ikhhu v (khm - NA С B; M -y Dt IXHI SHCHI a p a FU (se) TRYA(RRNU)»)

ХХМИ ХУ с 50 а фак ше ий буре др в во о (FI иххМ 3 7 According to the above-described method O to a mixture of 5-bromo-2-furaldehyde (I ХХМ) (1.76 g) and morpholine (1.0 Oml) in Acetic acid (0.6Oml) is added to 40ml of anhydrous THF at room temperature, followed by sodium triacetoxyborohydride (3.28g). The mixture is stirred at room temperature for 1h and then poured into saturated sodium bicarbonate solution (10Oml). After intensive stirring for 5min The layers were separated and the aqueous layer was extracted with EtOAc.The combined organic layers were washed with brine, dried (M2SO4), filtered and evaporated to dryness. After purification of the residue by express chromatography, 2.09 g (8.49 mmol, yield 8495) of compound I XXMI is obtained.

According to method M described above, compound I XXMI (0.678g, 2.7bmmol) is dissolved in 10ml of anhydrous THF in an inert gas atmosphere and the solution is cooled to -78°C. Then tert-butyllithium (4.00ml) is added dropwise

of a 1.7-molar solution in pentane) and the solution is stirred at -787"C for 30 minutes. After that, tributyltin chloride (0.bOml, 0.72 g, 2.2 mmol) is added and the solution is stirred for 30 minutes at -787C. Then add buffer with pH 7 (sat. MagRO,/Ma»HRO),) (1 Oml) and the mixture is heated to room temperature. The layers are separated and the aqueous layer is extracted with E(SO4). The combined organic layers are washed with brine, dried (Ma»5O) ), filtered and dried.

This compound I XXMII (0.399g, 0.874mmol) and compound I XXI (0.200g, O0.901mmol) according to the method M described above are dissolved in 1Oml of anhydrous 1,4-dioxane in a hermetically sealed tube in an atmosphere of inert /o gas. The solution is degassed and purged with nitrogen (twice). Next, tetrakis(triphenylphosphine)palladium(O0) (0.057g, 0.049mmol) is added, after which the solution is degassed and again purged with nitrogen (twice). The tube is hermetically sealed and heated to 1007C for 24 hours. After cooling to room temperature, the mixture is diluted with E(SO4), a saturated aqueous solution of potassium carbonate (1 Oml) is added, and the mixture is stirred for an hour at room temperature. Then the mixture is filtered through diatomaceous earth and the layers are separated. The aqueous layer extract E(Ac.

The combined organic layers are washed with brine, dried (Ma»5O)), filtered and evaporated to dryness. After purification of the residue by express chromatography, 0.314 g of yellow oil is obtained, which contains compound I XXMII along with tributyltin bromide. This mixture is used at the next stage without additional purification.

Compound GXXMII (0.283g, 0.917mmol) is reacted with phenylcarbamate IXXIM (0.395g, 1.13mmol) according to method B. The resulting product is purified by express chromatography to obtain the compound C specified in Title 2 in the form of a yellow solid (0.338g, 0.60O0mmol, yield 6595), which is further purified by recrystallization to obtain 0.131g of the title compound C (ecl 144-1467C).

Example 4 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-14-I(b--("morpholin-4-ylmethyl)pyridin-3-yl|Inaphthalene) -1-il)isecuvina o o re S RIDFFFI,SII se LIBAG g s viya SoMeONIVVM vry oy viy Ge)

ХХХХХХХХХХХХХ

ASONLVINV(OASY Ve | and 0 I you | "y Sya p

V I XXXHI XXX IS o) 4-4

ХХХ (C -- - --yaiya nm

IRF(RRN.) FI ikhkhm - s i S zh td o S "DY (in) " bit ze A s ------ n spav - 7 9 :z" shi 4

Similar to the method described in K.). Spatrbegz and A. Mapai (Zupipeis Sottipisayopv, 1997, 27, 515), a mixture of 2,5-dibromopyridine (XXIX) (9.90g, 41.78mmol), RY(DFFF)SI 5 (1.51g, 1.85mmol) , anhydrous MeOH (40 ml), -I anhydrous DMF (40 ml) and anhydrous triethylamine (12 ml) are blown in a Parr apparatus with a stream of carbon monoxide for 1 hour and then stirred at a carbon monoxide pressure of 8 Olbs/sq.in. at 507C for 4 hours. - The mixture is diluted with E(UAs (b00ml), washed with water (2x100ml) and brine (1x1000ml), dried (sodium sulfate),

He) is filtered and evaporated to dryness. The residue is purified by flash chromatography on silica gel (40956th EtOAc in 5% Hexanes) to obtain compound I XXX in the form of a light yellow-hot solid (33.733g, 17.28mmol, 4190). o To a solution of compound I XXX (165.9 mg, 0.7679 mmol) in anhydrous THF (1 Oml) at -78"C, add dropwise

He diisobutylaluminum hydride (1.0 molar solution in THF) (2.00 mL, 2.0 mmol). The mixture is stirred at -787C for 2 hours, after which a saturated solution of potassium carbonate (0.bml) is added, the mixture is heated to room temperature and stirred for another 30 minutes. Next, sodium sulfate is added and the mixture is stirred for 10 minutes. The solid is removed by filtration and the filtrate is evaporated to dryness. The residue is purified by express chromatography on silica gel (2096th E (OAc in hexanes)) to obtain aldehyde I XXXI in the form of a white (F) solid substance (8Omg, O0.4Zmmol, 56905). ka To a solution of compound I XXXI (367.7 mg . sodium triacetoxyborohydride (625 mg, 2.95 mmol). The mixture is stirred at room temperature for 30 minutes. Next, a saturated solution of sodium bicarbonate (1 Oml) is added and the mixture is intensively stirred for another 30 minutes. The layers are separated and the aqueous layer is extracted with E(OAc (3x20 Oml). the combined organic layers are washed with brine, dried (sodium sulfate), filtered and evaporated to dryness. After flash chromatography (196th triethylamine in EtOAc) of the residue, compound I XXXIII is obtained as a light yellow oil (460.8 mg, 1.79 mmol, 9190). 65 To a solution of tert-butyllithium (1.42-molar solution in pentane) (2.8O0ml, 3.98mmol) in anhydrous THF (20ml) at -7 A solution of compound IXXXII (460.8 mg, 1.792 mmol) in anhydrous THF (1 Oml) was added dropwise at 8 °C and the mixture was stirred at -78 °C for 10 min. Next, tributyltin chloride (0.49 ml, 0.59 g, 1.8 mmol) is added and the mixture is stirred at -78"C for another 15 minutes. After that, a buffer with pH 7 is added (sat. Ma"HPO,/Ma"PO,) ( 1Oml) and the mixture is warmed to room temperature.The layers are separated and the aqueous layer is extracted with EAs (3x2Oml).

The combined organic layers are washed with brine, dried (sodium sulfate), filtered and evaporated to dryness. After express chromatography (E(OAc)) of the residue, compound I XXIII was obtained as a colorless oil (548.8 mg, 1.17 mmol, 6596).

A degassed solution of compound I XXXI (302 mg, 0.64 mmol), compound I XXI (177 mg, 0.797 mmol) and RY(PPRI z)4 (55 mg, 0.48 mmol) in anhydrous 1,4-dioxane (LOml) is heated to 1007 in hermetically sealed tube 7/0 within 16 hours. The black precipitate is removed by filtration and the tube is washed with EAs. The combined filtrates are mixed with a solution of potassium fluoride (40956) (1 Oml) for 30 minutes. Next, water and brine are added, the layers are separated and the aqueous layer is extracted with E(OAc (4x5Oml). The combined organic layers are washed with brine, dried (sodium sulfate), filtered and evaporated to dryness. After express chromatography (596 Meon and 195 and triethylamine in EUAs) of the residue, compound I XXIII is obtained as a light brown solid (157 mg,

Oh, 49 mmol, 7690).

Compound YXXXIM and phenylcarbamate IIHIM are reacted according to method B. After purification by express chromatography using 595th Meon and 196th triethylamine in EtOAc as an eluent, followed by recrystallization from E(Ac/hexanes), the title compound 4 is obtained as a white of solid matter (Il 169-170").

Example 5 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-14-3-(morpholin-4-yl)phenyl-naphthalen-1-yl) truncated g nish

AH shi Vi M 2) Vyzbysi s y " she I XXXHI what

The same "Ve o

AND

- F i Zh M shi t, u nd (A sh p

Sov IRR"). ! fi u

HM IHHHHMY

(22) a and is M - zv v uvyv V oche F shcha sia, y ish f

From "Method b) o (XM of them 70 Z-bromoaniline (Z,Oml 4.7g, 28mmol), 2-bromomethyl ether (4.2ml, 7.7g, 3Zmmol) and isopropylethylamine c (15ml, 11g, vbmmol) are dissolved in anhydrous DMF (20 ml) in an inert gas atmosphere and heated to 1007 °C for two hours. After cooling to room temperature, the mixture was poured into water (ZOO ml) and extracted with E(Ac.

The combined organic layers are washed with brine, dried (Ma»5O)), filtered and evaporated to dryness. After purification of the residue by express chromatography, 2.9 g (12 mmol, yield 4395) of compound I XXXMI is obtained. - 15 Compound GXXXHMI (1.73g, 7.1Zmmol) is dissolved in anhydrous THF (ZOml) and cooled to -787C. Next, tert-butyllithium (10.0 ml of a 1.7-molar solution in pentane) is added dropwise and the solution is stirred at -787C for 30 minutes. After that, tributyltin chloride (1.9 Oml, 2.28 g, 7.00 mmol) is added and the solution is stirred again for 45 min at -78"C. Then a buffer with pH 7 is added (sat. (1 Oml) and the mixture was warmed to room temperature. The layers were separated and the aqueous layer was extracted with EtOAc. The combined organic layers were washed with 1 20 brine, dried (MgSO), filtered and evaporated to dryness. After purification of the residue by flash chromatography

2.28 g (5.3 mmol, yield 7790) of compound I XXXMII are obtained.

The compound GXXXHMI (1.49g, C3.51mmol) and the compound XXI (0.69g, C3.11mmol) are dissolved in 20ml of anhydrous 1,4-dioxane in a hermetically sealed tube under an inert gas atmosphere. Next, the solution is degassed and purged with nitrogen (twice). After that, tetrakis(triphenylphosphine)palladium(0) (0.21 g, 0.18 mmol) is added and the solution is again degassed and purged with nitrogen (twice). The tube is hermetically sealed and kept with heating at 1007C

GF) within 17 hours. After cooling to room temperature, the mixture is diluted with EtOAc, a saturated 7 aqueous solution of potassium carbonate (1 Oml) is added, and the mixture is stirred for 1 hour at room temperature. After that, the mixture is filtered through diatomaceous earth and the layers are separated. The aqueous layer is extracted with EtOAc. The combined organic layers washed with brine, dried (Ma»5O)), filtered and evaporated to dryness. After purification of residue 60 by express chromatography, 0.363 g (1.19 mmol, 3895) of compound I XXXMIII is obtained.

Compound and XXXMII! (0.360g, 1.18mmol) according to method B is subjected to interaction with phenylcarbamate and CHM (0.69g, 1.97mmol). The obtained product was purified by flash chromatography to give a colorless solid (0.433 g, 0.77 mmol, yield 6690), which was further purified by recrystallization from EtOAc/hexanes to give 0.344 g of the title compound 5 (Ch 188-190"). Table 1 shows other compounds according to the invention obtained by methods similar to those described above.

Table I about angle and i

Gee! n in, approx

Ah p. yoh ZK from u r. v,

Prikl V x na y ish S m is fesvoameyu Fe 000 lo Cheyuorrlnya net 5 Gvevtsymet fen 00 nuye | azurfolnii 5 pevo|emon Fey 0 15S emoriolnya PE) 20. about zealous for feeverdmez Zolivnyan ON, norrolnya rn from asoriolnia)

IR. tre-Vy |6-Me-3- |Z-pyridyl |e-(CH2) 4-morpholinyl 162-165 pyridyl pa rveveme stayu TEN) amovfonnya vn sch 15 tre-Vy |b-Me-3- | I-cyclohexenyl |z-(CHN-4-morpholinyl He) pyridyl (CH)

Note: "the number refers to the position of X attached to the naphthalene ring (Ag), p - 166-

IF) bdigit refers to the position of X attached to Y, o "digit refers to the position of 7 attached to Y (or X, if Y denotes a bond), or "digit refers to the position of X attached to 7. and -

Example 16 1-I4-(6-Bis-(2-cyanoethyl)amino|methyl)pyridin-3-yl)naphthalen-1-yl|-3-(5-tert-butyl-2-methylphenyl)urea

Mo, vE, ! hu n, ras and y: 1 with sleep bottom di-tret butyl that shsh 4 ncarbona! c and c). хз» A r хх хи У

A She and |c) we B: ko and 2 | XXIX | ho M -I t - o he her Tue SI - - SUN, MEb ZI i i)

Method V Y dn (se) ho 1 o s

I Zin u M s o p» gy M no

To. still ma M cheh en 1 |) HER ma(dso)VN 59 non rya sISNSNSY «v - 2 M yuyu u ah y z o Z M

Height cm 60, height 16

Tetrafluoroborate in nitrile ion (40.5 mmol) is added to a solution of 4-tert-butyltoluene (33.7 mmol) in acetonitrile (1500 ml) at 0"C. After standing for 30 minutes at room temperature, the reaction mixture is diluted with water (50 ml) and extracted with EAs ( The combined organic extracts were washed with brine and dried

(Mo950,) The residue obtained after extraction of volatile components in a vacuum is purified by express chromatography using 10956 methylene chloride/petroleum ether as an eluent to obtain 4-ter-buty-2-nitrotoluene. 4-tert-butyl-2-nitrotoluene (1.1 mmol) was dissolved in DMF (1 mL). Next, a catalyst (1096 Pa/s, 5 mgH) is added, and then di-tert-butyl dicarbonate (1.4 mmol) is added. This mixture is blown with argon, and then kept in a NO (Tatm) atmosphere for 12 hours. The mixture is filtered through a pad of diatomaceous earth, the filtrate is diluted with water and extracted with E(Ac (3x10ml). The combined organic extracts are washed with brine and dried (MazO)).

After evaporation of the volatile components, 26b5mg of M-Boc-5-tert-butyl-2-methylaniline are obtained in the form of a 7/0 crystalline solid.

Boron trichloride (0.4 mmol) is added to a mixture of M-Boc-5-tert-butyl-2-methylaniline (0.0 mmol) and triethylamine (0.22 mol) in benzene (1 0 ml) at room temperature using a syringe. The resulting inhomogeneous mixture is stirred at 807C for 30 minutes. After that, remove the heat source and add aminonaphthalene And! XXXIX (O.7 mmol). The reaction mixture was stirred at room temperature for 1 hour. Then the reaction mixture /5 is diluted with water (10 ml) and extracted with EtOAc (3x10 ml). The combined organic extracts are washed with brine and dried (Mo5O);) The residue obtained after the extraction of volatile components in a vacuum is purified by express chromatography using 1095-th MeonH/EUdAs as an eluent to obtain ZOOmg of the target urea XO.

This urea is placed under acidic conditions to extract the acetal, which reveals the presence of the aldehyde function. To this aldehyde in 1,2-dichloroethane is added 1.25 equivalents of bis(2-cyanoethyl)amine, followed by addition of sodium triacetoxyborohydride (1.5 equivalents). After column chromatography (596th Meon/EuAc), the title compound 16 is obtained.

Example 17 1-(b-tert-butyl-2-chloro-3-methylpyridin-4-yl)-3-I4-(b6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea 7 g 206.0 0 o so nn o

Z 595 НС со І я туту зу» шу с о 5 Ра(РРА);

Xo 2 M mass. DME IS (22) o o sh S - m He ch rche do -

Nei, dioxane maon y so 4 el A du y y N non -o s hsy Hei "" To a stirred solution of M-Vos-1-amino-4-bromonaphthalene (15.5 mmol) in anhydrous THF (40 ml) at -787C " -Vigy (47 mmol) is added. The resulting yellow-green solution was stirred at -78"C for 2 hours, and then transferred to a solution of trimethylborate (5.64g, 54.2mmol) in anhydrous THF (25ml) at -42"C. The reaction mixture is allowed to warm to room temperature overnight as the bath is heated. After stirring for 16 hours, add 595th aqueous NOSI (25 ml) and stir the mixture for 15 minutes. The water layer is saturated with Masi and the layers are separated. The aqueous phase is extracted with diethyl ether (30 ml) and then the combined organic phases are extracted with a 0.5-molar Mahon solution (30 ml). The combined alkaline extracts are acidified with 3M HCl (about 10 ml) to about p 2 and the suspension is extracted with diethyl ether (3x10 ml). The combined ether extracts with 20 are dried (Mo5O)), filtered and the solvent is removed to obtain boronic acid XCI in the form of a beige solid (2.3 g), which is used further without additional purification. g» of 5-bromo-2-(morpholin-4-ylmethyl)pyridine (0.7 mmol) and compound XCI (0.70 mmol) are dissolved in a two-phase mixture of dimethoxyethane (2 ml) and 2-molar aqueous Ma 2 CO3 (ml). The reaction mixture is blown with a stream of Mo for 15 minutes, Ra catalyst is added and the mixture is kept with heating at 857C for 16 hours. After that, the reaction mixture was cooled to room temperature and partitioned between water (10 ml) and EtOAc (75 ml). Layers

HF) are separated and the organic phase is washed with brine (20 ml), dried (MazO)), filtered and the solvent is removed to give a brown solid. After column chromatography, the product of XII is obtained as a beige solid.

The compound XII (0.5 mmol) is dissolved in 2 ml of anhydrous dioxane and NSI (2.5 mmol) is added. Solution 60 is stirred at room temperature for 16 hours. Next, diethyl ether (bml) is added to the resulting suspension and the mixture is cooled to 0"C. After neutralization with aqueous MasOH and filtration, 4-(b-(morpholin-4-ylmethyl)pyridin-3-yl|-1-aminonaphthalene (XO) is obtained in the form of a light brown solid substance (10 Ωg).

Method B - yati, 1usiclchloroformate a. ; in Y, shchy nni oyanaya she

WITH

17

A mixture of 2-tert-butyl-6-chloro-5-methylpyridine-4-carboxylic acid methyl ether (2.27g, 9.39mmol) and PON monohydrate (2.36g, 56.mmol) in Meon (30ml) and water ( 1 Oml) are stirred at room temperature for 24 hours. Then the reaction mixture is concentrated and purified by chromatography on silica gel (eluent: 595

TFUK in dichloromethane) to obtain the corresponding carboxylic acid (1.41 g, 66.3905).

Ethyl chloroformate (0.34 ml,

With, 51 mmol). The resulting mixture is stirred at 07"C for an hour. After that, a solution of sodium azide (0.40 g, b.Omol) in water (2 ml) is added and the stirring is continued for another hour. The mixture is extracted with toluene.

The organic phases are separated, dried with sodium sulfate and concentrated to a volume of 15 ml. The concentrate is heated under reflux for 2 hours, which is accompanied by the formation of an isocyanate precipitate, and then a solution of the compound XO! (0.39 g, 1.2 mmol) in dichloromethane (bml). The reaction mixture was stirred at room temperature overnight. After concentration and chromatography on silica gel (eluent: EtOAc), the title compound 17 was obtained (0.60, 89.9905). Go)

18

Vg -

Donu sch

VG Oh my. z-M she oyu hom x o7 /y F -e 7 Her. 5 o'clock M

From Tue and Thu 1) RR) - -

WITH . or 2 M Mazhbo,, DME o what s 2) oi Fo u t " Vg nin " ho hom - s / a yi Hm, :z" hom o ye gi

Mn; what are you mon -| 18 - 2,5-dibromopyridine (10Omg) is heated in a hermetically sealed tube to 1157C in the presence

of 3-methoxypropyl-1-methylamine (2 ml) for 48 hours to obtain the compound XSIM. After the union reaction

Suzuki (Zygiki) compound XSIM with compound XSI and extraction of tert-butyl carbamate (similarly described in 1 50 example 17 of the process) obtain the target naphthylamine XSU. "from B-tert-butyl-2-methylaniline (0.5 mmol) is dissolved in dichloromethane (200 ml). After that, an equal volume of saturated aqueous sodium bicarbonate is added and the two-phase solution is cooled to 0"C. During the addition of phosgene (1.93 M in toluene, 0.8O0ml) and stop stirring. Immediately after this, stirring is resumed and continued for 15 min with the reaction mixture at 07C. The layers are separated, the organic phases are dried over solid magnesium sulfate, and the solution is concentrated to a volume of approximately bml. Then they add

GF) necessary naphthylamine (HCMI, 0.47 mmol) in 5 ml of dichloromethane. The reaction mixture is stirred at room temperature for 1 hour. After flash chromatography using 79th Meon/EUdAs as an eluent and subsequent trituration with ether, the title compound 18 is obtained.

Example 19 60 1-(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|-3-(3--fluoromethylphenyl)urea b5

GOD and: ; RMOSOSI and o and MN, ot hom kore shshch

Hei y t So

Method G 7 and a n n so 19

A stirred solution of 3-trifluoromethylaniline (4.7 mmol) in dry THF (30 mL) is treated with phenyl chloroformate (4.8 mmol) at °C. After 2 hours, the reaction is stopped by adding a saturated aqueous solution of sodium bicarbonate and extracted with EtOAc. The combined organic layers are washed with aqueous saturated sodium bicarbonate solution and brine and dried over solid M950. After concentration, the carbamate XMI (97906) is obtained. After that, a mixture of the compound XMI (Example 17) (0.0 bmmol) and the indicated carbamate (0.05 mmol) is heated for 2 days in a hermetically sealed tube. Then the reaction mixture is cooled to room temperature. Next, R3-trisamine (100 mg, Agdopac company) and R3-isocyanate polymers (150 mg, Agdopac company) are added and the reaction mixture is shaken for 3 days. After that, the reaction mixture is filtered and concentrated with obtaining the compound indicated in the title 19. i)

Examples 20-25 illustrate the synthesis of aryl- and heteroarylamines, which can be used as an intermediate product of IM in methods B (section "General methods of synthesis") to obtain compounds of formula II or PI.

Example 20 c zo 1-(B-tert-butyl-2-(1H-pyrazol-4-iluphenyl|amine) - y. , syu 0 humor But with h:

С Mem -- Me, сО, Me son RE; -

HOM and

LANGUAGE, C RIS X « mesm ; With MchN, So, N o s 40 o -- chno, he X -nn, - and I sa

And" d - those that n 20

Methyl-4-tert-butylphenylacetate (200 mmol) is dissolved in MeonH (160 ml) and treated with water (40 ml) and PON monohydrate (20 mmol). After that, the reaction mixture is left to stir at room temperature overnight. Then, volatile components are removed under reduced pressure, the resulting residue is diluted with water and neutralized to p 4 with the help of others. sulfuric acid. The obtained solid substance (Ce) is filtered, washed with water and dried to obtain 4-tert-butylphenylacetic acid in the form of not sl 50 completely white solid substance (3.8g, 99905).

Anhydrous DMF (139 mmol) is cooled to 0"C and treated with ROSI with (79.bmmol). After 5 minutes, 4-tert-butylphenylacetic acid (19.9 mmol) is added and the reaction vessel is placed in an oil bath with a temperature of 11070. The reaction mixture is stirred within 2 hours, while all solids dissolve. After cooling to room temperature, the reaction mixture is poured into a stirred solution of MaPE (19.8 mmol) in water (200 ml). The precipitate is filtered off, washed with water and dried to obtain the compound XMII (7.8 g, 9796). o The HSMI! compound (5 mmol) is dissolved in EN (5 Oml) and the resulting suspension is treated with hydrazine hydrate (Ime) (bBmmol). After that, the reaction vessel is placed in an oil bath with a temperature of 90"7C and the reaction mixture is stirred while heating under reflux for 2 hours After cooling the reaction mixture to 60 room temperature, the volatile components are removed under reduced pressure. The residue is dissolved in ice water, the solid is filtered off, washed with water and dried, obtaining 4-(4-tert-butylphenyl)pyrazole (97Zmg, 9796).

This 4-(4-tert-butylphenyl)pyrazole (0.5 mmol) is suspended in Mesm (2 ml), cooled to 0"C and treated

MO»2BE, (0.bmmol). The reaction mixture is allowed to slowly warm to room temperature and stirred at 65 room temperature (RT) for 2 hours. After stopping the reaction by adding aqueous MnSO, the volatile components are removed under reduced pressure. The residue is dissolved in water and extracted with СНоСи». The organic phases are combined, dried over Mo5O, and concentrated to give a yellow oil, which is chromatographed on silica gel (eluent: SNCl/EtOAc in the ratio 6:4) to give 4-(4-tert-butyl-2-nitrophenyl) pyrazole as a yellow crystalline solid (71mg, 5895). 4-(4-tert-butyl-2-nitrophenyl)pyrazole (0.27 mmol) is dissolved in EN (3 ml) and treated with 1095 Pa/sC (O2 equiv. based on the weight of the nitro compound), and then MNACOOH (2.7 mmol ). Through ZOkhv, the catalyst is filtered through a layer of diatomaceous earth and the filtrate is concentrated under reduced pressure. The residue was dissolved in water, the solid formed was filtered off, washed with water and dried (54 mg, 9395) to give the title compound 20. 70 Example 21

Z-amino-2-methoxy-5-tert-butylpyridine (o) mn,on Ge) soy, ni saw,

Mo AISI,, MO, Me, 0 es from writing kt

U Z ra AL Tu Vi --- - - - ---

Mo MS article 6) uy on o tskyoto, RSIB, ROS; y br termievyunt no LO le MO poto, mo, (9) si "o

MaoMe, Meon r. ras, NSO, MN,, village

EE in February o 652 M EUN, 50C M t mo, mn,

OMe OMe 21

To ammonium hydroxide (25 ml, 11905) add ethyl nitroacetate (3.3 ml, 4.0 g, 29.7 mmol) and stir overnight, as described in A.M. Atheis and others, Kizziap Spetis! VyPesip, 1996, 45(2), 393-398. Next, the reaction mixture is alkalized with 4N. hydrochloric acid, extracted with simple ether (3x25ml), and then EtOAc (3x100ml). United and

EAs extracts are dried (magnesium sulfate), filtered and evaporated to dryness to give nitroacetamide as F) as a pale yellow solid (1.7g, 16.3mmol 5590). -

Trichloroaluminum (45.5 g, 34-1 mmol) is slowly added to 100 ml of ice-cooled nitromethane under a nitrogen atmosphere. After that, a solution of malononitrile (21.5 ml, 22.6 g, 341 mmol) in 50 ml of nitromethane is added dropwise over the course of an hour, maintaining the temperature below 10"7C. Then, a solution of tert-butyl chloride (88 ml, 74.9 g) is slowly added over 2.5 hours , 809 mmol) in 25 ml of nitromethane, maintaining the temperature below 107C.

The reaction mixture is closed and placed in a freezer for an hour. After that, saturated aqueous sodium bicarbonate (500 ml) is added dropwise to the reaction mixture for 4 hours to suppress the intensive course of the reaction, keeping the temperature below 107C. Then the heterogeneous mixture is neutralized with solid sodium bicarbonate (50 g). The layers are separated and the aqueous layer is extracted with methylene chloride (3x25Oml). The combined organic extracts were dried (magnesium sulfate) and concentrated in vacuo to give 42 g of partially crystalline brown oil. The residue was distilled in vacuo at 100°C. The first fraction is collected, after which solid formation begins in the condenser. Then the cooling water supply is turned off and the condenser is heated using a heat gun to melt the solid substance. This fraction is collected until the formation of a solid substance stops in the condenser when cooling water is passed through it, resulting in the target dinitrile as a cream-colored solid that melts at a low temperature (19g, 155 mmol, 46905). (Ce) A solution of this dinitrile (961 mg, 7.9 mmol) in anhydrous hexanes (500 mL) was cooled under nitrogen to 500-707 °C in a dry ice/acetone bath. After that, diisobutylaluminum hydride (DIBAG) (17.5 ml, 1.0 M in cyclohexane) is added dropwise for 20 minutes. The mixture is stirred at -70"C for 45 minutes, and then at room temperature for 5 hours. The reaction mixture is cooled to 0"C, after which a 2-molar aqueous solution of hydrochloric acid (45 ml) is slowly added, maintaining the temperature below 10"C The mixture is stirred at room temperature for 15 hours. The layers are separated and the aqueous layer is extracted with ether (3 x 25 ml).

The combined organic extracts were dried (magnesium sulfate), filtered and evaporated to dryness to give the target dialdehyde as a viscous yellow oil (bO0Omg, 4.6v8mmol, 60905). o A solution of this aldehyde (271mg, 2.11mmol), nitroacetamide (22mg, 2.14mmol) and piperidine (2095th in EN) (250μl, 0.5mmol) in absolute EUN (3ml) is maintained with heating at 657С for According to After cooling to room temperature, the reaction mixture is concentrated in vacuo. The residue is purified by 6o express chromatography on silica gel (E(UAs) to obtain the target nitropyridone M as a yellow solid (28Omg, 1.4Zmmol, 6790).

A mixture of this nitropyridone (15Omg.O,/bmmol), phosphorus pentachloride (199mg, 0.9bmmol) and phosphorus oxychloride (1 drop) is heated to the distillation temperature in a hermetically sealed tube. After 2 hours, phosphorus oxychloride is removed under vacuum and the residue is stirred in ice water (1 Oml) for 18 hours. After 65 minutes, the target product was collected as a brown solid (95 mg, 0.44 mmol, 58965).

A solution of sodium methoxide (1.57 g of sodium in 40 ml of anhydrous Meon) (85 μl, 0.14 mmol). The reaction mixture is heated overnight in a hermetically sealed tube in an oil bath with a temperature of 80-907C. After that, the volatile components are removed under vacuum, the residue is dissolved in E(Ac (15 ml), washed with water (1 Oml) and

Brine (1 Oml), dried (magnesium sulfate), filtered and evaporated to dryness. After flash chromatography of the residue on silica gel (10906th EtOAc in hexanes), the target 2-methoxy-3-nitro-5-tert-butylpyridine was obtained as a glassy yellow solid (12mg, 0.057mmol, 41905).

Ammonium formate (22 mg, 0.35 mmol) is added to a suspension of the intermediate product obtained at the previous stage (12 mg, 0.057 mmol) and Ra/sC (10905-th, 14 mg) in absolute EUN (ml) and the mixture is heated to 507С for an hour. 7/0 After cooling, the reaction mixture is filtered through diatomaceous earth and washed with Meon. The filtrate was evaporated to dryness to give the title compound 21 as a brown solid (1mg, 0.055mmol, 10096).

Example 22

M-acetyl-5-amino-3,3-dimethylindoline - Me! sk: Sam M 5. 5-7 zinvo, Sto» pev, sha BD with in! še de M no s nn fo no zl, "St o - re m -o sce

A solution of oxindole (5.0 g, 37.5 mmol) in acetic anhydride (7.1 mL, 75.1 mmol) and acetic acid (25 mL) was heated under reflux for 20 hours. After cooling to room temperature, the reaction mixture was diluted with water (200 ml). The resulting solid was filtered, washed with water and dried to give M-acetyloxindole as a white solid (5.2 g, 7990). Me

A mixture of this M-acetyloxindole (2.0g, 11.4mmol), iodomethane (1.5bml, 25.1mmol) and potassium carbonate (3.1g, 22.8mmol) in DMSO (20ml) was stirred at room temperature for 20h . After that, the reaction mixture

Dilute with water. The obtained solid substance is filtered, washed with water and dried to obtain -

M-acetyldimethyloxindole in the form of a yellow-hot solid (1.9 g, 84965).

A solution of this M-acetyldimethyloxindole (50 mg, 2.5 mmol) in Zn. a solution of sulfuric acid (/ml) and THF (7ml) is heated under reflux for 4 hours. After cooling to room temperature, the reaction mixture is diluted with ether. The ether layer is washed with water and brine, dried (magnesium sulfate), filtered and concentrated in vacuo. The residue was purified by express chromatography on silica gel (eluent 3095th with EtOAc in hexanes) to obtain dimethyloxindole as a red solid (228mg, 57965). "» A solution of this dimethyloxindole (220mg, 1.4mmol) in toluene (bml) is treated with a 6595th solution of Kead-AI in n H ... toluene (0.b4ml, 2.05mmol) at 80"С. After stirring at 1007C for 4 hours, the reaction is stopped by adding 1N. sodium hydroxide solution. The organic layer is separated, washed with water and brine, dried (sodium sulfate), filtered and concentrated in vacuo. The residue is purified by express chromatography on - silica gel (eluent: 2596th EtOAc in hexanes) to obtain dimethylindoline in the form of a clear blue oil - (121mg, 6096).

A solution of this dimethylindoline (bomg, 0.44 mmol) and triethylamine (0.12 mL, 0.8–8 mmol) in dry dichloromethane (3 mL) is treated with acetyl chloride (0.05 mL, 0.5 mmol) at 0°C. The mixture is allowed to warm to room temperature. 20 temperature and stirred for 16 hours. Then the reaction is stopped by adding water and the product is extracted with ether. The organic layer is washed with water and brine, dried (sodium sulfate), filtered and concentrated in vacuo. The residue is purified by express chromatography on silica gel (eluent: Z096 EtOAc in hexanes) to give M-acetnldimethylindoline as a light yellow oil (b8mg, 8290).

A solution of this M-acetyldimethylindoline (b5 mg, 0.34 mmol) in acetic acid (2 mL) is treated with fuming nitric acid (24 μL, 0.57 mmol) at room temperature and the resulting mixture is stirred for

GF) 1 hour After that, the reaction is stopped by adding a saturated solution of sodium bicarbonate and the product is extracted

EUAs. The organic layer was washed with water and brine, dried (sodium sulfate), filtered and concentrated in vacuo. The residue is purified by flash chromatography on silica gel (eluent: EtOAc 5090 in hexanes) to obtain the target nitrated indoline as a bright yellow-hot solid (ppm, 67905). 6o A mixture of M-acetyl-3,3-dimethyl-5-nitroindoline (b4mg, 0.27mmol), ammonium formate (8bmg, 1.30mmol) and 10905 palladium on carbon (mg) in MeonN (5ml) is stirred at room temperature temperature for 2 hours. The reaction mixture is filtered through a short plug of diatomaceous earth. Then this filtrate is concentrated in a vacuum. The residue was purified by flash chromatography on silica gel (eluent: 50905% EtOAc in hexanes) to give the title compound 22 as a white solid (48mg, 8790). because Example 23

8-amino-b6-tert-butyl-3-oxo-4-M-methylbenzoxazine c J o sha p writes TO noya and that -4 7 ROS nia manso" pod m

Ow o aty pu o m oy? 9 Shchi Man Mei! Ff dMmF pozh" lan "b. 07529000 same oi po hol-koM 23 t To a solution of 4-tert-butyl-2,6-dinitrophenol (3.15g, 13.133mmol) in 100ml of acetonitrile add ammonium formate (5.0g, 78.8mmol) and 10956 palladium on charcoal (1.0 g). The mixture is heated under reflux for 20 minutes, then allowed to cool and filtered through diatomaceous earth. The residue is washed with EtOAc and the combined organic phases are evaporated in vacuo. The residue is dissolved in dichloromethane and filtered through a porous plug of silica gel. After removing the solvent in vacuo, 20 2-amino-4-ter-buty-b-nitrophenol is obtained as a red solid (4.8 bmmol, yield 3790).

To a solution of this 2-amino-4-ter-buty-b-nitrophenol (258 mg, 1.2 mmol) and benzyltriethylammonium chloride (BTEA) (280 mg, 1.23 mmol) in 5 ml of chloroform is added finely divided Manso with (41 mg, 4.92 mmol) . The mixture is cooled to 0"C and a-chloroacetyl chloride (0.12ml, 1.47mmol) in 1.5ml of chloroform is added dropwise using a syringe over 15 minutes. After the addition, the mixture is left to stir at 0"C for an hour. сч 25 Then the mixture is allowed to warm up to ambient temperature and finally heated gently under reflux for 2 hours. The resulting crude yellow-hot mixture is allowed to cool, after which it is filtered through diatomaceous earth to separate the white precipitate, which is thoroughly washed with a large amount of chloroform.

After removing the solvent in a vacuum, the oily residue is treated with water (40 ml) and mixed with a spatula, as a result of which a yellow precipitate is formed. This pure b-tert-butyl-8-nitro-3-oxobenzoxazine was filtered and cm 3o dried first in air and then in vacuum (1.05 mmol, 85905). iv)

To a solution of this b-tert-butyl-8-nitro-3-oxobenzoxazine (51 mg, 0.20 mmol) in 3.5 ml of DMF at 07C, sodium hydride (1 mg, 6095th dispersion in mineral oil, 0.24 mmol) is added in one portion. . After 20 minutes, methyl iodide (20 μl, 0.24 mmol) is added using F syringe. The mixtures are allowed to slowly warm to ambient temperature h- overnight. A saturated aqueous solution of ammonium chloride is added to the curd mixture to stop the reaction and extracted with EtOAc (33x10ml). The combined organic phases are washed with water and then with brine, after which they are dried over sodium sulfate. After filtration and removal of solvents in a vacuum, b-tert-butyl-8-nitro-3-oxo-4-M-methylbenzoxazine (10090) is obtained.

This b-tert-butyl-8-nitro-3-oxo-4-N-methylbenzoxazine (53 mg, 0.2 mmol) was dissolved in 12.5 mL of acetonitrile. After that, cyclohexene (0.20 ml, 2.0 mmol) and 1096 palladium on charcoal (75 mg) are added. The mixture is refluxed for 1 h, then cooled to ambient temperature and filtered through diatomaceous earth. The residue is washed with EtOAc and the combined organic phases are evaporated in vacuo to give the title compound 23 (10096).

Example 24 7-amino-5-tert-butyl-ZN-benzoxazol-2-one

OM yah our t X M, o SO - | syu ' soyu nyk, pyridine nyu, Ra nm mn, (Se) not? M-9 )-9 sl 70 9 924

4-nitrophenyl chloroformate (280 mg, 1.39 mmol) was added to a solution of 2-amino-4-ter-butyl-b-nitrophenol (300 mg, 1.4 mmol) and pyridine (0.30 mL) in methylene chloride (0.0 mL). The mixture is stirred for 24 hours. The obtained solution is washed with aqueous sodium bicarbonate (2x20 ml), dried over solid magnesium sulfate and concentrated to obtain a yellow-hot solid. After column chromatography (silica gel, eluent: 50 4095-th EtOAc/petroleum ether) 5-tert-butyl-7-nitro-ZN-benzoxazol-2-one (7096) is obtained.

HF) This 5-tert-butyl-7-nitro-ZN-oenzoxazol-2-one (200mg, 0.U9mmol) was dissolved in EN (1Oml). After that add cyclohexene (4ml) and 1096th palladium on charcoal (HOmg). The mixture is heated under reflux for 10 minutes, then cooled to ambient temperature and filtered through diatomaceous earth. After column chromatography (silica gel, eluent: 25950 EtOAc/petroleum ether), the title compound 24 (7096) was obtained.

Example 25 7-amino-5-tert-butyl-2-methylbenzoxazole b5 nsOoZhn, triethylorthoacetate and i Pa-C ЮН in, ? ro z v, on /-9 75. Dissolve 2-amino-4-ter-buty-b6-nitrophenol in triethylorthoacetate (1 Oml). The reaction mixture is stirred overnight at 1007"C. After evaporation of the volatile components in a vacuum, we obtain

B-tert-butyl-2-methyl-7-nitrobenzoxazole (110mg).

This 5-tert-butyl-2-methyl-7-nitrobenzoxazole (100 mg, 0.4 mmol) was dissolved in EHN (20 L). After that, a catalyst is added (1096th Ra/C, 10Omg), and then ammonium formate (1bOmg, 0.3mmol). The obtained heterogeneous mixture is stirred at 1007C for an hour. After filtration and subsequent evaporation, the title compound 25 (85 mg) is obtained.

Examples 26-29 consider the synthesis of four heteroarylamines, which can be used as an intermediate product of IM in methods B (section "General methods of synthesis") to obtain compounds of formula I or Ia. Example 26 5-(5-amino-3-tert-butylpyrazol-1-yl)-2-methylbenzamide

MA, no re

Ivas, NS with EYUN, NS

And I r o to (SsMu Raye M | menu v. o

DMF A A a, p c 26 and y 3-iodo-4-methylphenylamine (10 g, 4 mmol) is dissolved in b.n. HCl (40 ml) and cooled to 0"C, stirring vigorously throughout this process. Sodium nitrite (2.9 g, 1.0 Seq.) is dissolved in water (ml) and this solution is added dropwise to the reaction mixture. Through ЗОхв with the help of a dropper add dihydrate

From stannous chloride!) (22.8 g, imol) in bn. HCl (100 ml) and the reaction suspension are stirred at room temperature for uh-

After this, the value of p is set to 14 with the help of 4095th aqueous solution of sodium hydroxide and the aqueous mixture is extracted with E(OAc (bx5Oml), dried (M9504) and concentrated to obtain 3-iodo-4-methylphenylhydrazine (7g, 5796). This material used directly in the next reaction without additional purification.

A solution of the above-mentioned phenylhydrazine (5.08g, 22mmol) and 4,4-dimethyl-3-oxopentannitrile (3,06g, 1, Leq.-) in EYN (100ml) containing conc. NS (Zml), heat under reflux for 17 hours, C s after which it is cooled to room temperature. The value of P is set to 14 with the help of a 4095th aqueous solution of sodium hydroxide "" methylphenyl)-2H-pyrazol-3-ylamine (6.3 g, 8695). This material is used directly in the next reaction without additional purification.

B-tert-butyl-2-(3-iodo-4-methylphenyl)-2H-pyrazole-3-ylamine (2g, 5.bmmol) is combined with zinc cyanide - (397mg, 0.eq.) and tetrakis( triphenylphosphine)palladium(0) (325mg, 5ml. 90) in deoxygenated dimethylformamide - (1Oml). The resulting yellow suspension is kept with heating at 1007C for 4 hours, cooled to room temperature, and then diluted with brine and 2N. NSI The aqueous mixture was extracted with EtOAc (bH1Oml), dried (M9503) and concentrated. The residue is purified by express chromatography, eluting with a mixture of 2095-th with 20 EUds/petroleum ether, to obtain 1.3 g (9195) of the target nitrile.

This nitrile (150 mg, 0.5 mmol) is heated to 1007C in the presence of TOn for 2 hours in EUN (5 ml). Mmaon. g" After that, the reaction mixture is cooled to room temperature, neutralized with 5095th NSI, extracted

EtOAc (6x10ml), dried (M950O), and concentrated to give the title compound 26 (130mg, 80905).

Example 27 what

Zh. c) o Te 1 Mother, her z Kk or ko j pany nn M 1

And 2. just 0.27 5-amino-2-methoxypyridine (5.0 g, 4 mmol) is dissolved in B.N. HCl (1 Oml) and cooled to 0°C, stirring vigorously throughout this process. Sodium nitrite (2.8 g, 41 mmol) is dissolved in water (1 Oml) and this solution is added to the reaction solution. ) (52 g, 230 mmol) in bn.

NH (20 ml) and the reaction suspension are stirred at 0"C for 2.5 hours. The value of p is set to 13 using a 4095 aqueous solution of sodium hydroxide. After that, ethyl ether is added and the mixture is extracted

EtOAc (4x7Oml), dried (M950,) and concentrated to give 5-hydrazino-2-methoxypyridine as a yellow-brown solid (5.1g).

A solution of 5-hydrazino-2-methoxypyridine (2.5 g, 18 mmol) and 4,4-dimethyl-3-oxopentannitrile (2.3 g, 18 mmol) in toluene (5 mL) is heated under reflux for 17 h in a flask equipped with a trap

Dean-Stark, and then cooled to room temperature. After that, the reaction mixture is concentrated and the residue is purified by column chromatography on silica gel, eluting with a mixture of SO96 EtOAc/petroleum ether, to obtain the title compound 27 as a yellowish-brown solid (3.5 g, 8096).

Example 28 5-amino-3-tert-butyl-1-(2-pyridon-5-yl)pyrazole

fashion tn,

NVg "NOde" 7 and y: p. MA and 28

To the solution of the product obtained in example 27 (0.6bg, 2.4mmol) in acetic acid (Zml) add 48965th HBg in acetic acid (Zml). The reaction mixture is heated to 1207C for 15 minutes, cooled to room temperature, and then the p value is set to 7.5 using a 1095 aqueous solution of sodium hydroxide. c The aqueous mixture is extracted with EtOAc (4x15 ml), dried (Mo5O)) and concentrated to obtain a yellowish-brown d) solid. The title compound 28 (0.46 g, 8290) was obtained after recrystallization from ether.

Example 29 5-amino-3-tert-butyl-1-(2-cyanoethyl)pyrazole

M (22) from

Mn, "-

SM m.

CM 29

A solution of 2-cyanoethylhydrazine (3.0 g, 35 mmol) and 4,4-dimethyl-3-oxopentannitrile (4.2 g, 34 mmol) in toluene (5 mL) is heated under reflux for 17 hours in a flask equipped with a Dean-Stark trap, and then cooled to room temperature. The suspension is filtered and the filtrate is concentrated. Column C with chromatography of the residue on silica gel eluting with a mixture of 5095th E(Ac/petroleum ether) gives "» the title compound 29 in the form of a colorless solid (2.6 g, 4090). " Example 30 1-Ib-tert-butyl -2-(2-methylthiopyrimidin-5-yl)-2H-pyrazol-3-yl|-3-14-I(b-«(morpholin-4-ylmethyl)pyridin-3-yl|Inaftadlin-1-ylurea -I - se) with 50

Co.)

Ф) име) 60 b5 o z i-tmde o 1) koiVy - also Shetipoxalate dmso and zu o rpdyait MM sov vtrobutit MA sov

NOAs, 907S I bromanetag M sov» lk still 1» LLMF. RUSSIA, still

We still live in MA soda

M? 2) Mare, BUT Mov shchy Medi--lb. there is

RE hom us (changeable; ra tson ru na meonto y

Ma M MU M hom 1 DFFA, ME still o t z nyaneb, and S IF zh No ch by

ZMe zo

Pinacoline (10 mmol) and diethyl oxalate (120 mmol) are dissolved in THF (200 ml), cooled to -787C and treated with lithium hexamethyldisilazide (II I-GMDS, 120 mmol, 1-molar solution in THF). After that, the ice bath is removed and the reaction mixture is allowed to warm to room temperature. After 2 hours, the volatile components are removed and the crude residue is dissolved in ice-cold NOAc (200 ml). Then hydrazine monohydrate (110 mmol) is added, the reaction mixture is placed in an oil bath with a temperature of 907C and stirred overnight. After that, NOAc is removed under reduced pressure and the crude residue is dissolved in aqueous ManSO»z, obtaining «M solution with р b. Next, the solid substance is filtered, washed with water and dried to obtain the target pyrazole ether (12.9 g, 66905). yu

KO-tert-Vy (6–7 mmol) is dissolved in DMSO (120 ml). Next, the pyrazole ether obtained in the previous (0) stage (12g, b1mmol) is added in one portion and the reaction mixture is stirred for 15 minutes. After that, tert-butyl bromoacetate (92 mmol) was added and the reaction mixture was stirred at room temperature for 45 min. Then -- DMSO is removed under reduced pressure and the crude residue is diluted with ice water and extracted with CH axis." uh-

The organic phases are combined, dried over Mo95O, and concentrated to obtain an isomeric mixture of pyrazoles in the form of a yellow-hot oil (21g). The target isomer is isolated as an oil by chromatography on silica gel, eluting with SNeoSi" (13, Zg, 70905). "

Pyrazole diester (13.3 g, 4 mmol) is dissolved in pure TFC (150 ml) and stirred at room temperature for 1 h. After that, the volatile components are removed and the crude residue is diluted with ice water and extracted with СНоСі». The organic phases were combined, washed with water, dried over Ma 5 O, and concentrated to give the target carboxylic acid as a thick oil that partially crystallized (10.2 g, 9490). "» Anhydrous DMF (282 mmol) is cooled to 0"C and treated with ROSI from (161 mmol). After 5 minutes, the pyrazole derivative of acetic acid obtained at the previous stage (10.2 g, 40 mmol) is added and the suspension is placed in an oil bath with a temperature of 1107C. After that, the reaction mixture is stirred for 2 hours, while all the solid matter is dissolved. After cooling to room temperature, the reaction mixture is poured into - a stirred solution of MaREBv (8 mmoles) in water (400 ml). The precipitate is filtered off, washed with water and dried, obtaining the target vinamidinium salt of HSMII (14.6 bg, 7890). (Se) This salt of HSMI (23Zmg, 0.5mmol) is dissolved in DMSO (10ml) and treated with 5-methylisothiourea sulfate sl 50 (0.25mmol) and KSO" (0.25mmol). After that, the reaction mixture is placed in an oil bath with a temperature of 90"C and stirred for 2 hours. After cooling the reaction mixture to room temperature, the volatile components are removed under reduced pressure. The residue is dissolved in ice water and extracted with diethyl ether.

The organic phases were combined, dried over Mo95O, and concentrated to give a brown resin. The target ethyl ether was purified by chromatography on a silica gel column, eluting with a 1:1 mixture of СНоСИЛЕЮАС to give a yellow oil that crystallized on standing (157mg, 9895).

The ether obtained at the previous stage (15Omg, 0.47 mmol) was dissolved in ME (4 ml) and water (1 ml), treated with GION monohydrate (0.7 mmol) and stirred at room temperature overnight. After that, volatile components are removed and the residue is diluted with water and neutralized to p 4 with the help of In. sulfuric acid. The solid substance is filtered, washed with water and dried (11Zmg, 82905). 60 The obtained carboxylic acid (105mg, 0.3bmmol) is suspended in benzene (4ml) and treated with triethylamine (0.6bmmol). The resulting solution is treated with diphenylphosphoryl azide (DFFA) (0.54 mmol) and left to stir at room temperature for 2 hours. The organic phases are washed with aqueous Manso»z and water, dried over Mo5O, and filtered. The resulting solution is treated with the compound XXXXIM (Example 4) (115 mg, 0O, Zbmmol) and the reaction mixture is placed for an hour in an oil bath with a temperature of 90"C. After that, the volatile components are removed and the crude residue is purified by preparative thin-layer chromatography on two plates, eluting with the mixture СНоСИ./Меон in a ratio of 9:1 to give the title compound

30 in the form of an off-white solid (b1mg, 2895).

By replacing the 3-methylisothiourea sulfate used in the reaction with the compound XCMIII, other substituted pyrimidines corresponding to the formula XCMIII can be obtained. So, for example, using acetamide hydrochloride, it is possible to obtain a 2-methylpyrimidine analogue of the compound ХСМИМ. Use of sulfate

O-methylisothiourea and guanidine carbonate allows to obtain 2-methoxypyrimidine and 2-aminopyrimidine analogues, respectively. When replacing Z-methylisothiourea sulfate with shydrazine monohydrate or

M-methylhydrazine can be used to obtain, respectively, a pyrazol-4-yl or 1-methylpyrazol-4-yl ring instead of a substituted pyrimidine in the HCMIM compound. Each of these analogs of the compound HCMIM can be used in the 7/0 methods described above to obtain the corresponding analogs of compound 30.

Examples 31-36 describe the synthesis of substituted naphthylamines that can be used as intermediate MI (0'-MH»o), as described for methods B and B in the section "General methods of synthesis", to obtain various compounds of the invention.

Example 31 5-(4-aminonaphthalen-1-yl)-2-pyridin-3-ylmethylphenol and Manso, (c)

No g Y -ee vn g o s dmFo SM Ff n 1509С M o

Vos-anhydride scha scha o r - de o sho Sho 5; heating with HOP-KOM 2) TFUK-DHM

Eh s o is s!

CC yu in FF 31 "-

1.75 ml is added to a tube with a solution of 2.0 g of 1-amino-4-bromonaphthalene (9U.00 mmol, Teq.) in 7 Oml of DMF

From 2-cyclohexen-1-one (18.0 mmol, 2.Eq.), 2.3 g of sodium bicarbonate (27.0 mmol, 3.Eq.;) and 186 mg of 1,3-bisidiphenylphosphino)propane (DFFP, 0 ,45 mmol, O, Obekv.). The mixture is bubbled with dry nitrogen gas for 15 minutes, after which 31 mg of bis(triphenylphosphino)palladium chloride (0.45 mmol, 0.OBeq.) is added and the tube is hermetically sealed. The mixture is kept with heating at 1507C for 8 hours, and then it is cooled to ambient temperature, diluted with EtOAc (15 Oml) and filtered through diatomaceous earth.

The mixture is washed with water, and then with brine. The organic layer is dried (Mo95O3), filtered and concentrated. From c The crude oil is purified by column chromatography on 5i", using from 10 to 50906 E(OAc in mixtures of "» hexanes as eluents, with the receipt of 2.0 g of a thick liquid containing 3-(4-aminonaphthalen-1-yl)ucyclohex- 2-enone and DMF (respectively, in a molar ratio of 1:2, 5.22 mmol of naphthylamine, yield 5895 from the theoretical).

2.72 g of di-tert-butyl dicarbonate (12 .5 mmol, 1.2 equiv.) and 1.5 ml of triethylamine (10.4 mmol, Equiv.). The mixture is kept with heating at 1007°C overnight, after which it is cooled to ambient temperature. Next, the reaction mixture is washed with 0.195 aqueous HCl (2 x 50 ml), water and brine, dried (Mao50), filtered and concentrated. The crude product precipitated and washed with 1095% EAs in hexane, obtaining after filtration 2.5g of the target tert-butylcarbamate (74mmol, yield 71905 from theoretical). s 20 To a solution of 18bmg of tert-butylnaphthylcarbamate obtained at the previous stage (0.55mmol, Teq. ) to 1.bml of anhydrous tert-butanol add 52 μl of pyridine-3-carboxaldehyde (0.55 mmol, Teq.) and 1.6 bml of a solution of g" potassium tert-butoxide (1.0M, 1.32 mmol, Teq.). This mixture heated to reflux overnight and then cooled.Meon (5 mL) and a solution of HCl in dioxane (4.0 M) were then added until the p value was about 1, after which the reaction mixture was stirred for 1.5 h at ambient 22 Then saturated is added to the mixture to stop the reaction and an aqueous solution of Manso with and extracted

HF) EUAs (2x50ml). The water layer is processed 4n. with Mahon's aqueous solution until the p value is set to about 12, and then extracted twice more. The combined organic extracts are washed with brine, dried (M95O), filtered and concentrated to give a mixture of crude products containing naphthylamine in the form of the still protected carbamate. Then this residue is dissolved in dichloromethane (Zml), treated with 2 mol of TFUK and left to stir for days off at ambient temperature. Then the reaction in the mixture is stopped and the mixture is neutralized with saturated aqueous ManHsSoOz, extracted with dichloromethane (3x5Oml), dried (Mo5o)) and filtered. Further, the volatile components are removed under vacuum and the crude product is purified by column chromatography on 5i, using from 50 to 10095 E(OAc in mixtures of hexanes as an eluent, with the receipt of 35 mg of the title compound 31 (0.11 mmol, yield 20905 from theoretical). bo Example 32

5-(4-aminonaphthalen-1-yl)-2-(tetrahydrofuran-3-ylmethyl)phenol o nn v o otelya o ee duk, ME r -ives va o shen o o o a AD

A list of references about F and F habits"

ZV. hol-kom 32 2» TFUK-DXM ke t To a solution of 3.16 g of tetrahydro-3-furanic acid (27 mmol, Teq.) in 25 ml of anhydrous dichloromethane, add 7.85 g of dicyclohexylcarbodiimide (DCC, Zvmmol, 1.4 equiv.) and 4, 54 ml of triethylamine (32.bmmol, 1.2 equiv.).

After that, M-methylmethanolamine hydrochloride is added, followed by DMAP ((4-dimethylamino)pyridine). At the same time, an exothermic reaction occurs, and therefore another 25 ml of dichloromethane is added. The mixture is stirred at ambient temperature overnight, then filtered through diatomaceous earth and concentrated. The residue is treated with ether, the white solid is filtered off and discarded. The solvent was removed from the mother liquor and the residue was purified by column chromatography on Z 1 using 15-25956 of EtOAc in hexanes as the eluent mixture to give the target amide as a colorless oil (yield 5595 of theory) still containing 1095 of dicyclohexylurea. This product is used in the next reaction without further purification. high school

To a solution of 1.0 g of the above-mentioned amide (6.28 mmol, eq.) in bbml of anhydrous THF at -78"С dropwise, with the help of a syringe, add 12.bml of a 1.0-molar solution of DIBAG in toluene (12.bmmol, 2.O0eq .).After

After 30 minutes of stirring at -787C, 500 ml of Meon is added to the reaction mixture to recolor the reaction and

B5Oml of water. The reaction mixture is transferred to a separatory funnel and 250 ml of ether is added. After that, add 1n. aqueous solution of NSII until all the solid substance is dissolved. The layers are separated and the aqueous phase is additionally extracted twice with ether in portions of 100 ml. The combined organic phases are washed with a saturated aqueous solution of ManHsSOOz, and then with brine, dried over Ma»5O), filtered and concentrated. The crude product is purified by chromatography on silica gel using 0-5906 Meon in dichloromethane as a mixture of eluents. F

In this way, the target 3-tetrahydrofuran aldehyde is obtained in the form of a volatile, impure, colorless oil (20 mg).

To a solution of 200 mg of tert-butyl naphthylcarbamate (0.59 mmol, equiv.) in 1.6 ml of anhydrous tert-butanol, add - 200 mg of 3-tetrahydrofuranaldehyde obtained at the previous stage (in excess) and 1.78 ml of a solution of potassium tert-butoxide in tert-butanol (1.0 M, 1.78 mmol, Zeq.). The mixture is kept with heating at 407C overnight, after which it is cooled and the reaction is stopped by adding a saturated aqueous solution of MH 4cIi. The obtained product is extracted with a mixture of dichloromethane and methanol (3x10 ml). The combined extracts are washed with brine, dried over Ma5O,; and concentrate. At the same time, according to the data of "H-NMR-analysis, only 1095 enone is consumed. The residue (300 mg) is dissolved in 4.0 ml of dichloromethane and treated with 4 ml of a mixture of :c" dichloromethane with TFUK in a ratio of 1:11. The reaction mixture is stirred for 1.5 hours , then neutralized with a saturated aqueous solution of MnHsSOOz, basified with a 4N solution of MnN and extracted with dichloromethane/methanol (3x100 ml). The combined organic extracts were washed with brine, dried (Ma5O)), - filtered and concentrated. The crude product was purified by column chromatography on silica gel, using from 10 to 5095 E(OAc in hexanes as a mixture of eluents, obtaining the title compound 32 (35 mg, 0.11 mmol, yield 1995 from theoretical). o Example 33 4-15-(4-aminonaphthalen-1-yl )pyridin-2-yloxy|butyronitrile 1 d- more) vet zshtmdsltye 0

TA co. Y po pi no cm RFRRN,;), 909 52 - s show o rya tibilnyut rn ko 33

1 M sodium hexamethyldisilazide (Ma-GMDS, 2.1 ml, 2, 1 mmol). After that, the reaction mixture is stirred at room temperature overnight. Next, EtOAc is added to the reaction mixture and the mixture is washed with water (2x10ml). The EFCOAs fraction is dried over anhydrous sodium sulfate and evaporated on a rotary evaporator. The crude product was purified by express column chromatography on silica gel using a mixture of 4096 E(dAs/hexane) to give 200 mg of 5-bromo-2-cyanopropyloxypyridine as a pale yellow solid (39,390).

2- molar solution of sodium carbonate (2 ml). The solution is purged with nitrogen for T7Ohv and then tetrakistriphenylphosphine palladium (2Omg) is added. The reaction mixture is kept with heating at 907C for 48 hours, after which it is cooled to room temperature. Next, EIAs is added to the reaction mixture and the mixture is washed with water (2 x 10 ml). The EA fraction is dried over anhydrous sodium sulfate, filtered and concentrated. The crude product is purified by column express chromatography on silica gel, eluting with a mixture of 4095th E(OAc/hexane, with the receipt of 7Omg of product (3990).

7/0 Cyclohexene (263mg, 3.2mmol) and 10906th Ra/C (20mg) are added to the product of the unification reaction obtained at the previous stage (7Omg, O0.1bmmol) in EUN (5ml). The reaction mixture is kept with heating in a nitrogen atmosphere overnight and cooled to room temperature. After that, the reaction mixture is filtered through diatomaceous earth, washed with MeOH and concentrated. The crude product is purified by express column chromatography on silica gel, eluting with a mixture of 5095th E(OAc/hexane), to obtain 15 mg of the title compound 33 (3195).

Example 34

Dihydrochloride of 1|5-(4-aminonaphthalen-1-yl)pyridin-2-yl|-(tetrahydrothiopyran-4-yl)amine o g mesh

Fe Mnon Z PAN, ! along the way Service station,

With EON 5 With what and -th century

Hi what lo PS lioksai

DME, 2M Ma?2SO» F, Ha (RRNZRAS', 900S uXxh o vom o, vd and NS for s

To tetrahydro-1,4-thiopyrone (2.0 g, 17.2 mmol) and hydroxylamine hydrochloride (2.0 g, 28./7/mmol) in EYN and (1 Oml) add sodium acetate trihydrate (4.0 g, 294 mmol) in 20 ml of water. The reaction mixture is heated with (o) a reflux condenser for hours, cooled to room temperature and concentrated on a rotary evaporator to a volume of 15 ml. The residue is cooled in an ice bath and filtered to obtain 2.0 g of the oxime product as a white solid with a Gl of 80-837C (88.7905). -

In a dry flask containing THF (20 ml) and 1M lithium aluminum hydride (LiH) in diethyl ether (19 ml) at room temperature, add the oxime obtained at the previous stage (500 Ωg, 3.82 mmol). The reaction mixture is heated under reflux for 2 hours, cooled to room temperature, and the reaction of excess AHL is stopped by adding a mixture of ice and water. After extraction with EtOAc and concentration, 340 mg (7690) of the target 4-aminotetrahydrothiopyran is obtained. - c 2,5-dibromopyridine (25Omg, 1.1 mmol) is added to the amine obtained in the previous stage (17O0mg, 1.4mmol) in dry pyridine (Iml), after which the reaction mixture is kept with heating at 110-120" "» within 5 days. Then the reaction mixture is extracted with EtOAc, washed with water, dried over anhydrous sodium sulfate and concentrated to obtain a crude product. This crude product is purified by express column chromatography on silica gel, using a mixture of 3096th E(Ac/hexanes as eluent, with the receipt of 10mg of pure product (33.390). - To the intermediate product obtained in the previous stage (8mg, 0.293mmol) and BOSC-protected naphthylboronic acid XCI (Example 17) (14mg, 0.48v8mmol) in DME (4ml) add 2M sodium carbonate (2ml) and bis(triphenylphosphine)palladium (Ce) chloride (15mg). The reaction mixture is kept with heating at 90"C in an atmosphere of 50 ml of nitrogen for 18 hours and cooled to room temperature. After that, the reaction mixture is extracted with E(OAc), washed with water, dried over anhydrous sodium sulfate and concentrated to obtain a crude product. This crude product is purified by express column chromatography on silica gel using a mixt

3090th E(OAc/hexanes as eluent, with the receipt of 110 mg of pure product HSC (86,090)

A mixture of 4M Nei/dioxane (0O0.bml) was added to the compound XH (35mg, 0.08mmol) in dioxane (1ml). Then the reaction mixture is stirred at room temperature for 48 hours. After addition of diethyl ether, the product is obtained in the form of hydrochloride, which is filtered to give 18 mg (5595) of the title compound 34.

IF) Example 35 name) Dihydrochloride of 1|5-(4-aminonaphthalen-1-yl)pyridin-2-yl|-(tetrahydropyran-4-yl)amine

Ve. and Hsi -h and o o 60 A DME om maso, to" sho (Ra Rosi, F mavn(oAsi hoh - -o -o u rzvya -SU UKISN,SI, nya i U bo Ho 35

2M sodium carbonate (2.5ml) and bis(triphenylphosphine) chloride are added to 2-amino-5-bromopyridine (25mg, 1.44mmol) and BOC-protected naphthylboronic acid XCI (example 17) (688mg, 2.4mmol) in bml DME ) palladium (ZOmg).

The reaction mixture is kept with heating at 907C in a nitrogen atmosphere for 18 hours and cooled to room temperature. Then the reaction mixture is extracted with E(OAc), washed with water, dried over anhydrous sodium sulfate and concentrated. The residue is purified by express column chromatography on silica gel, eluting with a mixture of 4095 E(OAc/hexanes, with the receipt of 370 mg of the product of the reaction of the combination of CXH (76.496 ).

To this intermediate (200mg, 0.597mmol) and tetrahydropyranone (120mg, 1.19mmol) in dichloroethane (bml) are added acetic acid (0.2ml, 3.5v8mmol) and sodium triacetoxyborohydride (38mg, 1.79mmol). 70 The reaction mixture is stirred at room temperature for 48 hours, and then extracted with EtOAc, washed with water, dried over anhydrous sodium sulfate and concentrated. The residue is purified by express column chromatography on silica gel, eluting with a mixture of 5095th E(Ac/hexanes as an eluent, with the receipt of 12 Ω of the compound ХСХИ (48,095).

The obtained at the previous stage, the compound Chskhi is dissolved in dichloromethane (3ml) and treated with trifluoroacetic acid 7/5 KI (ml). The reaction mixture was stirred for 1 h and concentrated. The residue is dissolved in EtOAc (20 ml), washed with sodium bicarbonate solution, dried over anhydrous sodium sulfate and concentrated to obtain 9 mg of the title compound 35 (98.5965).

Example 36

I5-(4-aminonaphthalen-1-yl)pyridin-2-yl|-(1-methylpiperidin-4-yl)amine -x B; Sh -03- ke vol "y Mavnioas), XX and hoch - s teUk/SNOSY, nim -- I-5 o la Sk o zv

Glacial acetic acid (120mg, 2.00mmol) and sodium triacetoxyborohydride are added to a mixture of the compound ХСХ (example 35) (110mg, 0.33mmol) and 1-methyl-4-piperidone (8mg, 0.1mmol) in dichloroethane (bml). (22Omg, with 1.0Zmmol). The reaction mixture is stirred at room temperature for 9 hours, and then extracted with EtOAc, washed with water, dried over anhydrous sodium sulfate and concentrated. The residue was purified by flash column chromatography on silica gel, using a mixture of 1095 Meon/CH2Cl2, 190 TEA (triethanolamine) as Me eluent, to give a bomg of pure product (42.095). -

The product obtained at the previous stage is dissolved in dichloromethane (3 ml) and treated with trifluoroacetic acid (1 ml). The reaction mixture was stirred for 2.5 hours and concentrated to obtain 94 mg of compound 36 (100905) indicated in the title.

Example 37

Example 37 illustrates the synthesis of the compound of the formula ЕІІ, in which E means 0. "

3-tert-butylphenyl ether (4-(b-morpholin-4-ylmethylshridin-3-yl)naphthalen-1-yl)carbamic acid. St t de z M So zho 0. sho p on phosgsya oh om n ze Z - 15 Compound ХХХХХМ (example 4) (100 mg, 0.3 mmol) is dissolved in dichloromethane (200 ml). After that, an equal volume of saturated aqueous sodium bicarbonate is added and the two-phase solution is cooled to 0"C. Then, for a while, phosgene (1.93M in toluene, 0.4O0ml) is added, and the stirring is stopped. Immediately after this stirring, the reaction mixture is restored and continue for 15 min at 07 C. After that, the layers are separated, the organic phases are dried over solid magnesium sulfate, and the solution is concentrated to a volume of approximately bml. Then 1 50 3-tert-butylphenol (100 mg, 0.b7 mmol) in dichloromethane (bml) is added. The reaction mixture is stirred at room temperature for 19 hours. After express chromatography using EtOAc as an eluent, 71 mg of the title compound 37 was obtained.

Example 38

In example 38, the synthesis of the compound of formula I, in which E stands for CH, is illustrated. 2-(5-tert-butyl-2-methoxyphenyl)-M-I(4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalene-1-ilyacetamide

F) i still seg ka ry om r. ochi i So

SCHHIH moose Fri at 60 years old writes) call

Compound I XXXIM (example 4) (10mg, 0.4mmol) and the sodium salt of 5-tert-butyl-2-methoxyphenylacetic acid (154mg, 0.4mmol) were dissolved in dichloromethane (15ml). Next, 1-(3-dimethylaminopropyl)-33-ethylcarbodiimide hydrochloride (172 mg, 0.9 mmol) is added and the reaction mixture is stirred at ambient temperature of 65 °C for 16 h. After purification by high-performance liquid chromatography (HPLC), the

ZOmg of the title compound 38.

Similarly to the methods described above, the following compounds are also obtained: 1-(2-tert-butyl-5-methylpyridin-4-yl)-3-14-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl| Urea, 1-(5-tert-butyl-2-methylphenyl)-3-14-Ib-(morpholin-4-ylmethyl)pyridin-3-yl|naphthalen-1-yl)urea, 1-(3, 3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea , 1-(3-amino-5-tert-butyl-2-methoxyphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1-(3-tert -butylphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 1-(4-methylbiphenyl-3-yl)-3-I4-(6-morpholin- 4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 70 1-(4-tert-butylbiphenyl-2-yl)-3-I4--b-morpholin-4-ylmethylpyridin-3-yl)naphthalene- 1-yl)urea, 1-(5-4-13-(5-tert-butyl-2-methoxyphenyl)ureido|naphthalen-1-yl)pyridin-2-ylmethyl)piperidine-3-carboxylic acid amide, 1- (5-isopropyl-2-methylphenyl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(5-tert-butyl-2-methoxyphenyl)- 3-I4-(b-morph olin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 1-(5-tert-butyl-2-methoxymethylphenyl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl) naphthalene-1-yl|urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-(4-16-((tetrahydrofuran-3-ylamino)-methyl|pyridin-3-ylnaphthalene-1-yl) wine urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-(4-16-14-(3-methoxyphenyl)piperazin-1-ylmethyl|pyridin-3-ylnaphthalen-1-yl) urea, 1 -(5-tert-butyl-2-methoxyphenyl)-3-I4-5-morpholin-4-ylmethylpyrazin-2-yl)naphthalen-1-yl)urea, 1-(5-tert-butyl-2-methoxyphenyl) )-3-I4-(6-4(2-cyanoethyl)-(tetrahydro-furan-2-ylmethyl)amino|methyl)pyridin-3-yl)unanaphthalen-1-yl|Urea, 1-(5-tert- butyl-2-methoxyphenyl)-3-I4-(6-4(2-cyanoethyl)pyridin-3-ylmethylamino|methyl)pyridin-3-yl)naphthalen-1-yl|Urea, sc 1-(5-tert- butyl-2-methoxyphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-I4- (b-thiomorpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, and) 1-(5-tert-butyl-2-methoxyphenyl)-3-74-(6-(1-oxo-I14) -thiomorpholine -4-ylmethyl)pyridin-3-yl|Inaphtalin-1-yl)usecuine, 1-(5-tert-butyl-2-methoxyphenyl)-3-74-(6-(1-oxotetrahydrothiopyran-4-ylamino) Pyridin-3-yl|Inaphthalin-1-yl)urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(6-(-2,6-dimethylmorpholin-4-ylmethyl) -pyridin-3-yl|Inaphthalin-1-yl)urea o y, 1-(5-tert-butyl-2-methoxyphenyl)-3-(4-I(6-(2,6-dimethylpiperidin-1-ylmethyl) )pyridin-3-yl|Inaphthalin-1-yl)isopheny o

U, "- 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(6-(2-methoxymethylmorpholin-4-ylmethyl)pyridin-3-ylInaphthalin-1-yl)usechovin, 1 -(5-tert-butyl-2-methoxyphenyl)-3-4-(6-(2-methyl-3-oxopiperazin-1-ylmethyl)pyridin-3-yl|naphthalen-1-yl) truncated wine, 1- (5-tert-butyl-2-methoxyphenyl)-3-74-(6-(2-oxa-5-azabicyclo|2.2.1)hept-5-ylmethyl)pyridin-3-ylInaphthalen-1-"yl)urea , with c 1-(5-tert-butyl-2-methoxyphenyl)-3-74-(6-(2-thia-5-azabicyclo|2.2.1)hept-5-ylmethyl)pyridin-3-ylInaphthalene-1 - and timber, ; » 1-(5-tert-butyl-2-methoxyphenyl)-3-74-(6-(3-oxopiperazin-1-ylmethyl)pyridin-3-yl|Inaphthalin-1-yl)uretate, 1-(5- tert-butyl-2-methoxyphenyl)-3-4-(6-(4-methylpiperazin-1-ylmethyl)pyridin-3-yl|naphthalen-1-yl)uretate, 1-(5-tert-butyl-2- methoxyphenyl)-3-74-(6-(4-pyridin-2-ylpiperazin-1-ylmethyl)pyridin-3-yl|Inaphthalen-1-yl)isocho -I wine, 1-(5-tert-butyl-2 -methoxyphenyl)-3-4-(b-(morpholine-4-carbonyl)pyridin-3-yl|Inaphthalen-1-yl)uretate, - 1-(5-tert-butyl-2-methoxyphenyl)-3-4 -(6b-(pyridin-3-yloxy)pyridin-3-yl|Inaphthalin-1-yl)urea,

Ge) 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(b-(tetrahydropyran-4-ylamino)pyridin-3-yl|Inaphthalin-1-yl)uretate, 1-(5-tert -butyl-2-methylphenyl)-3-(4-16-((3-methoxypropyl)methylamino|pyridin-3-ylnaphthalen-1-yl)uretate, o 1-(5-tert-butyl-2-methylphenyl)- 3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea,

Ge 1-(5-tert-butyl-2-methylpyridin-3-yl)-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1-(b-tert -butyl-3-oxo-3,4-dihydro-2H-benzo|1,oxazin-8-yl)-3-(4--6-morpholin-4-ylmethylpyridin-3-yl)naphthalene-1-yl )urea, 1-I4-(6-TIbis(2-cyanoethyl)amino|methyl)pyridin-3-yl)naphthalen-1-ylI|-3-(5-tert-butyl-2-methoxyphenyl)urea, 1- (5-(1,1-dimethylpropyl)-2-methoxyphenyl|-3-14-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea,

F) 1-(b-tert-butyl-2-(1H-pyrazol-4-yl)phenyl)|-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl| Isechovin, ka 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)phenyl/1-3-14-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl| urea, in 1-Ib-tert-butyl-2-(3-hydroxypropyl)phenyl-1|-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1-( b-tert-butyl-2-(morpholin-4-carbonyl)phenyl1|-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea y,

M-(5-4-(3-(5-tert-butyl-2-methoxyphenyl)ureido|naphthalen-1-yl)pyridin-2-yl)acetamide,

M-(5-tert-butyl-2-methoxy-3-13-I4-(6-morpholin-4-ylmethylpyridin-3-yl)unaphthalin-1-yl)ureido)phenyl)acetamide, 65 M-(5- tert-butyl-2-methoxy-3-13-14-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-ylureido)phenyl)-H-methylacetamide,

M-(5-tert-butyl-2-methoxy-3-13-14-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)ureido)phenyl)-2,2,2-triph toracetamide,

M-(5-tert-butyl-2-methoxy-3-13-14-(6-morpholin-4-ylmethylpyridin-3-yl)unaphthalin-1-yl)ureido)phenyl)methanesulfonamide.

Assessment of biological properties

Inhibition of TME production in TNR cells

Inhibition of cytokine production can be assessed by measuring inhibition of TMERa in lipopolysaccharide-stimulated TNR cells (see, for example, MU. Rgispei et al., 9. IpShattayiop, 45, 97, 70 1995). All cells and reagents were diluted with KRMI 1640 medium containing phenol red and I-glutamine with the addition of another portion of I-glutamine (total: 4MM), penicillin and streptomycin (50 units/ml each) and fetal bovine serum (FBS, 390 ) (SIVSO company, all concentrations are final concentrations).

The analysis was performed under sterile conditions; only the preparation of the tested compound was carried out under non-sterile conditions.

The original mother solutions were prepared in DMSO, and then diluted with KRMI 1640 medium to reach a 7/5 concentration, which is 2 times the final concentration required for analysis. Confluent

TNR.1 cells (final concentration 2x10 Ucells/ml, Ategisap Toure Siyshge Sotrapu, Rockville, Maryland) were introduced into 96-well polypropylene round-bottom plates for cultivation (type Soviag 3790; sterile) containing 125 μl of the tested compound (2- multiple concentration) or the carrier, which is DMSO (controls, pure). The final concentration of DMSO did not exceed 0.295. The mixture containing the cells was pre-incubated for 30 minutes at 37°C, 5956°C, before stimulation with lipopolysaccharide (LPS; final concentration μg/ml; Zida 1/-2630, from serotype 0111.84 E. soy; stored at - 80"C in the form of a mother solution with a concentration of mg/ml in distilled NO with constant monitoring of the presence of endotoxin).

A carrier, which is H 20, was added to the control samples (unstimulated); the final volume for incubation was 25 Ωcl. Incubation during the night (18-24 hours) was carried out according to the method described above. The Ga process was stopped by centrifuging the tablets at 1600 rpm (400 x ) for 5 min at room temperature; the supernatants were transferred to clean 9b-well plates and stored at -80"С until the analysis of 9) human TMR using a commercially available kit for EPGIZA (type Viozoshgse ЯКНСЗ015, Camarillo, pcs.

California). The data were analyzed by the method of nonlinear regression (using the Hill equation), obtaining the dependence of the response on the dose using the mathematical support of ZAZ Zoimage Zuviet (Institute of ZAZ, Ips., Ge Cary, North Carolina). The calculated IC»50 value is the concentration of the tested compound, which leads to a 5095th decrease in the production of TMRa compared to the maximum value. at

Using this method of analysis, the best compounds were evaluated, including the compounds given in Fd) examples of synthesis, and it was found that for them the ISvo is less than 1ΩμM.

Inhibition of other cytokines --

Analogous methods using peripheral blood monocyte cells, appropriate stimuli, and - commercially available kits for EGISA (or using another detection method, such as radioimmunoassay), suitable for a specific cytokine, can demonstrate inhibition of II -Ir, ZM-C5E, 1 -6 and 1/-8 (see, for example, -).S. And ee and others, Ipi. 9. Ittiporpagtasoi., 10, 835, 1988). "

Claims (1)

70 The formula of the invention as c ;z» 1. The compound of formula (1): di , - х- я'5 -- - am dumi zhya t - nn i-o () c 50 in which Agi is selected from the group that includes pyrrole , pyrrolidine, pyrazole, imidazole, oxazole, thiazole, furan and thiophene, where Ag can be replaced by one or more groups K., K» or Kz, Ago means phenyl, naphthyl, quinoline, isoquinoline, tetrahydronaphthyl, tetrahydroquinoline, tetrahydroisoquinoline , benzimidazole, benzofuran, indanyl, indenyl or indole, each of which is optionally substituted by 0-3 Co groups, and X means - Сb; S-cycloalkyl or cycloalkenyl, optionally substituted with 0-2 oxo groups or 0-3 branched or unbranched C.i-C.alkyl, C--C;. . . . . . . . . . . . . , thiophene, pyrrole, imidazolyl, pyridine, pyrimidine, pyridinone, dihydropyridinone, maleimide, 60 dihydromaleimide, piperidine, piperazine, or pyrazine, each of which is independently optionally substituted with 0-3 substituents selected from the group consisting of branched or unbranched C .4-C,alkyl, C.-C.Alkoxy group, hydroxy group, nitrile, mono- or di(C-i-Salkylamino group, group C.--Salkyl- (OO) or halogen, M means a bond or saturated or unsaturated branched or unbranched C 1- A carbon chain is optionally partially or fully halogenated, while one or more methylene groups are optionally replaced by О, МН, (0), 5(О0)» or 5, and U is optionally independently substituted 0-2 oxo groups and one or more branched or unbranched C.i.C., alkyl groups that can be substituted by one or more halogen atoms, 2 means - phenyl, pyridine, pyrimidine, pyridazine, imidazole, furan, thiophene, pyran, which optionally substituted with 1-3 substituents selected from the group consisting of halogen, C 4-Salkyl, C-Salkyl, hydroxy, mono- or di(C 4-Salkyl)amino group, C-Salkyl-Z(O) group t, a COOH group and a phenylamino group, while the phenyl ring is optionally substituted with 1-2 substituents selected from halogen, C4-Salkyl and C-Salkyloxy groups and, - tetrahydropyran, tetrahydrofuran, 1,3-dioxolanone, 1,3-dioxanone, 1,4-dioxane, morpholine, thiomorpholine, 70 thiomorpholine sulfoxide, piperidine, piperidinone, piperazine, tetrahydropyrimidone, cyclohexanone, cyclohexanol, pentamethylene sulfide, pentamethylene sulfoxide, pentamethylene sulfone, tetramethylene sulfide, tetramethylene sulfoxide or tetramethylene sulfone, optionally substituted with 1-3 substituents selected from nitrile, C.--Salkyl, C.i-Salkyloxy, hydroxy group, mono- or di(C.i-Salkyl)amino-C.- Salkyl, phenylamino-C4-Salkyl and C4-Salkoxy-C-4-Salkyl, - C-Salkoxy group, secondary or tertiary amine, where the amine nitrogen is covalently bound to groups selected from the series that includes C /-Salkyl, C .i-Caloxyalkyl, pyridinyl-C.-Calkyl, imidazolyl-C.-Calkyl, tetrahydrofuranyl-C 1-Calkyl, phenylamino group, where the phenyl ring is optionally substituted by 1-2 halogen atoms, C.i-Calkoxy groups, hydroxy groups or mono - or di(S.--Szalkil)daminogroups, group S.-Svalkyl-B(O) t and the phenyl-5(O)m group, in which the phenyl ring is optionally substituted by 1-2 halogen atoms, C1-Svalkoxy groups, hydroxy groups or mono- or di (S.-Svalkyl) amino groups, K. means - branched or unbranched C3-C4alkyl, which is optionally partially or fully halogenated and optionally substituted with 1-3 phenyl, naphthyl or heterocyclic groups selected from the group that includes pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, imidazolyl, pyrazolyl, thienyl, furyl, isoxazolyl, and isothiazolyl, wherein each such phenyl, naphthyl, or heterocycle selected from the series described above in this paragraph is substituted with 0-5 substituents selected from the group consisting of halogen, branched or an unbranched C 1 -C alkyl, which is optionally partially or fully halogenated, C 3 C -C 8 cycloalkyl, C 5 -C 8 cycloalkenyl, a hydroxy group, a nitrile, a C 1 -C 6 alkyloxy group, which is optionally partially or fully halogenated, a MNHS(O) group and di(Ci-C3)alkylaminocarbonyl, c - C53-Ccycloalkyl selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, bicyclopentanyl, bicyclohexanyl and bicycloheptanyl, each of which is necessarily partially or fully halogenated and optionally substituted with 1-3 C-alkyl groups, or an analogue of a similar /F) cycloalkyl group, in which 1-3 ring methylene groups are replaced by groups independently of each other "- selected from the series , which includes 0.5, CHOH, »2С-0, 2-51 МН, - branched C3-C-ralkenyl, which is optionally partially or fully halogenated and optionally in substituted with 1-3 substituents selected from branched or unbranched C1-alkyl, phenyl, naphthyl, or heterocyclic groups, each such heterocyclic group being independently selected from the group consisting of pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, imidazolyl, pyrazolyl , thienyl, furyl, isoxazolyl and isothiazolyl, and each of said phenyl, naphthyl or heterocyclic groups is substituted with 0-5 substituents selected from the group consisting of halogen, branched or unbranched C 4-alkyl, which is optionally partially or fully halogenated, cyclopropyl, cyclobutyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, h» bicyclopentanyl, bicyclohexanyl, bicycloheptanyl, hydroxy group, nitrile, C--Szalkoxy group, which is not necessarily "partially or fully halogenated, MNHS(O) group and mono- or di (C.4-C3)alkylaminocarbonyl, - CbC5-C, cycloalkenyl, selected from the group that includes cyclopentenyl, cyclohexenyl, cyclohexadienyl, cycloheptenyl, cycloheptadienyl, bicyclohexenyl and bicycloheptenyl, while each such cycloalkenyl group is optionally substituted by 1-3 C.i.C.alkyl groups, - - nitrile or - branched or unbranched C.i.C.alkyloxycarbonyl, branched or unbranched and) C.-C.alkylaminocarbonyl, branched or unbranched C.-Salkylcarbonylamino-C 1-Salkyl, sl 50 Ko means branched or unbranched C.-Salkyl, which is optionally partially or fully halogenated, acetyl, aroyl, branched or unbranched C. and C. alkoxy group, which is optional necessarily partially IR) or fully halogenated, halogen, methoxycarbonyl or phenylsulfonyl, Ez means - a phenyl, naphthyl or heterocyclic group selected from the group consisting of pyridinyl, pyrimidinyl, 22 pyrazinyl, pyridazinyl, pyrrolyl, imidazolyl, pyrazolyl, thienyl, furyl, tetrahydrofuryl , isoxazolyl, Ge! isothiazolyl, quinolinyl, isoquinolinyl, indolyl, benzimidazolyl, benzofuranyl, benzoxazolyl, benzisoxazolyl, benzpyrazolyl, benzothiofuranyl, cinolinyl, pterindinyl, phthalazinyl, naphthylpyridinyl, quinoxalinyl, where quinazolinyl, purinyl, and indazolyl, such a phenyl, naphthyl, or heterocyclic group is optional 1-5 substituents selected from the group consisting of phenyl, naphthyl, heterocycle selected from described 60 above in this paragraph of the series, branched or unbranched C .-Salkyl, which is optionally partially or fully halogenated, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, bicyclopentyl, bicyclohexyl, bicycloheptyl, phenyl-C.i-Svalkyl, naphthyl-C--Svalkyl, halogen, hydroxy group, nitrile, C.-C alkyloxy group, which may optionally be partially or fully halogenated, phenyloxy group, naphthyloxy group, heteroaryloxy group, where the heterocyclic fragment is selected from the series described above in this b5 paragraph, nitro group, amino group, mono- or di(C 4-C 3 )alkylamino group , a phenylamino group, a naphthylamino group, a heterocyclylamino group, where the heterocyclyl fragment is selected from the series described above in this paragraph, a group MNHS(O), mono- or di(C.4-C3)alkylaminocarbonyl, C.4-Salkyl-C(O0)-C.i-C.alkyl, amino-Ci-Salkyl, mono- or di(C4i- C3)alkylamino-C 1-Svalkyl, group amino-5(0)", group di(Ci-Salkylamino-Z(O)", C.-C4-Svalkyl, C5-Si-Svalkoxy group, Ka-FK(0) -C.4-Salkyl, group K,-C.-Salkyl(Ka)M, carboxy-mono- or di-C4-Salkylamino group, - condensed aryl selected from the group that includes benzocyclobutanyl, indanyl, indenyl, dihydronaphthyl, tetrahydronaphthyl , бензоциклогептаніл і бензоциклогептеніл, або конденсований гетероцикліл, вибраний із групи, яка включає циклопентенопіридин, циклогексанопіридин, циклопентанопіримідин, циклогексанопіримідин, циклопентанопіразин, циклогексанопіразин, циклопентанопіридазин, циклогексанопіридазин, 70 циклопентанохінолін, циклогексанохінолін, циклопентаноізохінолін, циклогексаноізохінолін, циклопентаноіндол, циклогексаноіндол, циклопентанобензімідазол, циклогексанобензімідазол, циклопентанобензоксазол, cyclohexanobenzoxazole, cyclopentanoimidazole, cyclohexanoimidazo l, cyclopentanothiophene and cyclohexanothiophene, wherein said fused aryl or fused heterocyclyl ring is substituted with 0-3 substituents selected from the group consisting of phenyl, naphthyl and heterocyclyl selected from the group consisting of pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl . , a naphthyloxy group, a heterocyclyloxy group, in which the heterocyclyl fragment is selected from the group described above in this paragraph, a nitro group, an amino group, a mono- or di(C.i.i.-C3)alkylamino group, a phenylamino group, a naphthylamino group, a heterocyclylamino group, in which the heterocyclyl fragment is selected from the group described above in in this paragraph, the group, the group MNHcC(O), mono- or di(C--C3)alkylaminocarbonyl, the group C.-Alkyl-OC(O), branched or unbranched C.-Salkyl-C(0)-C.-C;alkyl, amino-C--Salkyl, mono- or di(C4i-C3)alkylamino-C 1 - Svalkyl, Kye-Si-Svalkyl, Kio-C4-Svalkoxy group, K4-F(0)-C.4-Svalkyl and the group K/2-C4-Svalkyl(K 45) M, Ha - cycloalkyl selected from the group, which includes cyclopentyl, cyclohexyl, cycloheptyl, bicyclopentyl, bicyclohexyl and bicycloheptyl, while such cycloalkyl is optionally partially or fully halogenated and i) optionally substituted by 1-3 C-C alkyl groups, - b5-C, cycloalkenyl selected from the group , which includes cyclopentenyl, cyclohexenyl, cyclohexadienyl, cycloheptenyl, cycloheptadienyl, bicyclohexenyl and bicycloheptenyl, while such cycloalkenyl group c zo is optionally substituted with 1-3 C-C alkyl groups, - acetyl, aroyl, alkoxycarbonylalkyl or phenylsulfonyl or o - branched or unbranched S.-Svalkyl, which is not necessarily partially or fully halogenated, or b Ku and KB" together can optionally form a condensed phenyl a for the pyridinyl ring, Kv and Kz are each independently selected from the group consisting of hydrogen and branched or unbranched C.-C. alkyl, which is optionally partially or fully halogenated, Ku, Kv, Kv, KU , Co, Co, K44 And Ki" each independently selected from the group consisting of morpholine, piperidine, piperazine, imidazole and tetrazole, "t means 0, 1 or 2, in c M/ means O or 5, and its pharmaceutically acceptable derivatives. of 2. The compound according to claim 1, in which Ago is naphthyl, tetrahydronaphthyl, indanyl or indenyl, and MU is 0. 3. The compound according to claim 1, in which Ag is selected from thiophene and pyrazole, - and X means C5-Ccycloalkyl or C5-Ccycloalkenyl, optionally substituted by 0-2 oxo groups or 0-3 branched or unbranched C.-C.alkyl groups , C.-C. alkoxy groups or - C.-C. alkylamino groups, or X means phenyl, pyridine, tetrahydropyridine, pyrimidine, furan or thiophene, each of which is independently optionally substituted with 0-3 substituents selected from the group that includes branched or unbranched C .-C;alkyl, C.i.-C.alkoxy group, hydroxy group, nitrile, mono- or di(C4-Salkyl)amino group, C--Salkyl-Z(O) group and halogen, He Ku means branched or unbranched C.-C.alkyl, cyclopropyl or cyclohexyl, which are optionally partially or fully halogenated and optionally substituted by 1-3 C-C-alkyl groups, Ez means 5B - branched or unbranched optionally partially or fully halogenated C.-C.alkyl , - phenyl, pyrimidinyl, pyrazolyl or pyridinyl, each of which is optionally substituted with 1-5 substituents, F) selected from the group that includes phenyl, naphthyl, pyrimidinyl, pyrazolyl, pyridinyl, branched or unbranched S.-Svalkil, which optionally partially or fully halogenated, cyclopropyl, cyclobutyl, cy clopentyl, cyclohexyl, cycloheptyl, bicyclopentyl, bicyclohexyl, bicycloheptyl, phenyl-C.-Salkyl, because naphthyl-C.-Salkyl, halogen, hydroxy group, nitrile, C.-Salkyl, which may optionally be partially or fully halogenated, a phenyloxy group, a naphthyloxy group, a heteroaryloxy group, in which the heterocyclic fragment is pyrimidinyl, pyrazolyl, or opyridinyl, a nitro group, an amino group, a mono- or di(C4-C3)alkylamino group, a phenylamino group, a naphthylamino group, a heterocyclylamino group, in which the heterocyclic fragment is pyrimidinyl, pyrazolyl, or pyridinyl , group МН 2Б(О0), mono- or 65 di(C--C3)alkylaminocarbonyl, C.-Salkyl-C(O)-C.-Salkyl, amino-C.-Salkyl, mMono- or di(C4i- C3)alkylamino-C 1-Svalkyl, group amino-5(0)", group di(C4-C3)alkylamino-5(0O)2, C.-C.4-Svalkyl, K5-Ci-Svalkoxy group, Ke-FK(0)-C.4-Svalkyl, group K,-C.4-Svalkyl(Ka)M and carboxy-mono- or di(C4-Cv)alkylamino group, - alkoxycarbonylalkyl or - cyclopropyl or cyclopentyl, each of which is optionally partially or fully halogenated and optionally substituted with 1-3 C-C alkyl groups. 4. The compound according to claim 3, in which Ar represents pyrazole and X represents cyclopentenyl, cyclohexenyl or cycloheptenyl, optionally substituted by an oxo group or 0-3 /o substituents selected from the group that includes branched or unbranched C.4-C;alkyl , a C1-C4 alkoxy group and a C1-C4 alkylamino group, or X represents phenyl, pyridine, furan or thiophene, each of which is independently optionally substituted with 0-3 substituents selected from the group consisting of branched or unbranched C.-C;alkyl, C.-C;, alkoxy group, hydroxy group, nitrile, mono- or di(C.i.-C.alkyl)amino group, C-Salkyl-Z(O)n group and halogen. 5. The compound according to claim 4, in which M means -CH»-, -CHNOCH»-, -CHNOMH-, -CHNOCHNOMH- or a bond and 2 means phenyl, imidazole, furan, piperazine, tetrahydropyran, morpholine, thiomorpholine, thiomorpholine sulfoxide , piperidine, pyridine, secondary or tertiary amine, where the amine nitrogen is covalently bonded to groups selected from the group consisting of C 4 -C 4 alkyl and C 1 -C 4 -alkyloxyalkyl, or further means a phenylamino group in which the phenyl ring is optionally substituted 1-2 substituents selected from halogen, C.-Salkyloxy groups, hydroxy groups and mono- or di(C.i-Salkyl)amino groups, C.-Salkyl-Z(O)2t group and phenyl-B(O)»t group, in which the phenyl ring is optionally substituted 1-2 substituents selected from halogen, C.-Calkoxy groups, hydroxy groups and mono- or di(C.4-C.alkyl)amino groups. 6. The compound according to claim 5, in which C Ag means 5-tert-butylpyrazol-3-yl, where the pyrazole ring can be replaced by a Kz group, while Ez means i) - branched or unbranched optionally partially or fully halogenated C. -- Sualkyl, - phenyl, pyrimidinyl, pyrazolyl or pyridinyl, each of which is optionally substituted with 1-5 substituents selected from the group consisting of phenyl, naphthyl, pyrimidinyl, pyrazolyl, pyridinyl, branched or unbranched S.-- Svalky, which is optionally partially or fully halogenated, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, bicyclopentyl, bicyclohexyl, bicycloheptyl, phenyl-C.4-Svalky, o naphthyl-C.-Svalky, halogen, hydroxy, nitrile, C --Szalkoxygroup, which can optionally be partially or Ge! fully halogenated, phenyloxy group, naphthyloxy group, heteroaryloxy group, in which the heterocyclic fragment is pyridinyl, nitro group, amino group, mono- or di(C 4-C3)alkylamino group, -- phenylamino group, naphthylamino group, heterocyclylamino group, in which the heterocyclic fragment is pyridinyl , group МНосС(О), mono- or di(C.4-C3)alkylaminocarbonyl, C.i-Salkyl-C(0)-C.4-Salkyl, amino-C.--Salkyl, MOono- or di( C4-C3)alkylamino-C -Salkyl, amino-5(0) group, di(C4-C3)alkylamino-5(O)2 group, K/-C4-Salkyl, K5-Si-Salkyloxy group, Ke-C (0)-C4-Salkyl, group, K,-C4-Salkyl(Ka)M, carboxy-mono- or di(C.4-C)-alkylamino group, « - alkoxycarbonylalkyl or c - cyclopropyl or cyclopentyl, each of which are optionally partially or fully halogenated and optionally substituted with 1-3 C.-Alalkyl groups. of 7. The compound according to claim 6, in which X is pyridinyl. 8. The compound according to claim 7, in which pyridinyl is attached to Ag. in the 3rd position of pyridinyl. 9. The compound of formula (Ia): - mu 10, Czech Republic 1 IC (se) si NN (Iv) ki" in which Ag. means pyrrole, pyrrolidine, pyrazole, imidazole, oxazole, thiazole, furan and thiophene, while Ag. optionally substituted by one or more groups K., KE" or Kz, 25 Ago means phenyl, naphthyl, quinoline, isoquinoline, tetrahydronaphthyl, tetrahydroquinoline, Ge! tetrahydroisoquinoline, benzimidazole, benzofuran, indanyl, indenyl and indole, each of which is optionally substituted by 0-3 Co groups, where X means - C5-Cvcycloalkyl or cycloalkenyl, optionally substituted by 1-2 oxo groups or 1-3 C -- C/C-alkyl, because C-C-Alkoxy or C-C-Alkylamino chains, each of which is branched or unbranched, - phenyl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, pyridinyl, tetrahydropyridinyl, pyrimidinyl, pyridinonyl . -C;alkyl, C-C-Alkoxy group, hydroxy group, b5 nitrile, amino group, mono- or di(C-C-C alkyl)amino group, mono- or di(C-4-C alkylamino)carbonyl, MNHS(O) group, group C--Svalkyl-Z(O) t and halogen, M means a bond or a saturated or unsaturated branched or unbranched C 4-C carbon chain, which is optionally partially or fully halogenated, with one or more C atoms optionally replaced by O, M or 5(O ) same, and M in each case is independently optionally substituted by 1-2 oxo groups, nitrile, phenyl, hydroxy group or one or more C.-C. alkyl groups, optionally substituted by one or more halogen atoms, 2 means aryl, indanyl , heteroaryl selected from benzimidazolyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, furanyl, thienyl and pyranyl, heterocycle, 70 selected from piperazinyl, tetrahydropyrimidonyl, cyclohexanonyl, cyclohexanolyl, 2-oxa- or 2-thia -5-azabicyclo|2.2.1|heptanyl, pentamethylene sulfidyl, pentamethylene sulfoxidyl, pentamethylene sulfonyl, tetramethylene sulfidyl, tetramethylene sulfoxidyl or tetramethylene sulfonyl, tetrahydropyranyl, tetrahydrofuranyl, 1,3 3-dioxolanonyl, 1,3-dioxanonyl, 1,4-dioxanyl, morpholino group, thiomorpholino group, thiomorpholinosulfoxidyl, thiomorpholinosulfonyl, piperidinyl, piperidinonyl, pyrrolidinyl and dioxolanyl, while each of the 7 groups mentioned above is optionally substituted with 1-3 substituents, selected from the group consisting of halogen, C1-Salkyl, C1-Salkoxy, C1-4-Salkoxy-C1-Salkyl, C-Salkoxycarbonyl, aroyl, heteroaroyl, heterocycleC1-Szacyl, wherein heteroaryl and heterocycle have the above in this paragraph meaning, (F 1-Szacyl, oxo group, hydroxy group, pyridinyl-C-Szalkyl, imidazolyl-C4-Szalkyl, 2o Ttetrahydrofuranyl-C /-Szalkyl, nitrile-S--Szalkyl, nitrile, carboxy group, phenyl, and the phenyl ring optionally substituted with 1-2 substituents selected from the group consisting of halogen, C 4 -C 4 -Sulfoxy group, hydroxy group and mono- or di(C-i-Salkyl)amino group, amino-5(O)t group, C.i group - Svalkyl-Z(O)t and the group phenyl-B(O),t, where the phenyl ring is optionally replaced by 1-2 halogen atoms, С -- Св alkoxy groups, hydroxy groups or mono- or di(C.4-C-C alkyl)amino groups, ch or 7 is optionally substituted with 1-3 substituents selected from the group consisting of an amino group, aminocarbonyl and amino-C.-C-C alkyl, where the M atom independently optionally mono- or disubstituted aminoC with 4-Svalkyl, (8) C-Salkyl, arylCo-Salkyl, C4-Salkyl, C4-Salkyl, C-Salkyl, aroyl, C-Sacyl, group C.-Salkyl-B(O)t- or the group arylCo-Salkyl-C(O)»t-, while each of the above alkyls and aryls attached to the amino group is optionally substituted with 1-2 substituents selected from the group , which includes c zo Halogen, C -Salkyl, C-Salkyloxy, hydroxy and mono- or di(C1-Salkyl)amino group, or 7 is optionally substituted with 1-3 substituents selected from the group consisting of aryl, heterocycle or o heteroaryl, as they are defined above in this paragraph, while each of the specified substituents, in turn, is optionally substituted by a halogen, C4-Salkyl, or a C4-Salkyloxy group, or 7 means a hydroxy group, hydroxyC-Salkyl, halogen, nitrile, an amino group, where the M-atom independently ("7 is optionally mono- or disubstituted by Co 4-Salkyl, aminoC.-Salkyl, arylCo-Salkyl, M C.4-SalkoxyCi-Salkyl, C.i-Salkoxy group, aroyl, C.--Szacyl, C.i-Salkyl-3(O)»t- group, arylCo-Salkyl-3(O)t- group, nitrileC -C,alkyl or C.i-SalkoxyC--Cialkyl, while each of the above-mentioned alkyls and aryls attached to the amino group is optionally substituted with 1-2 substituents selected from the group that includes halogen, C.i-Salkyl, C.i-C3-alkyloxy group, hydroxy group and mono- or di(C.--C3 alkyl)amino group, " 40. C1-SalkoxyheteroarylC0-C6 alkyl, heteroarylC0-C6 alkyl or heterocycleC0-C6 alkyl, where heteroaryl and /7-C heterocycle have the above meanings in this paragraph, . or 7 means a branched or unbranched C.-Svalkyl, C--Svaloxy group, C.--Szacylamino group, and? nitrileC.-C;alkyl, C4i-Salkyl-Z(O)»t and phenyl-(O)»4, where the phenyl ring is optionally substituted by 1-2 halogen atoms, C-Salkyloxy groups, hydroxy groups or mono- or di( C4-C3 alkyl)amino groups, K. means -I - branched or unbranched C.-C.alkyl, which is optionally partially or fully halogenated and optionally substituted by 1-3 substituents selected from the group that includes phenyl, naphthyl and heterocyclic groups, - selected from a series that includes pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, imidazolyl, pyrazolyl, He)thienyl, furyl, isoxazolyl, and isothiazolyl, wherein each of said phenyl, naphthyl, or 5or heterocyclic groups selected from the above series is substituted with 0- 5 substituents selected from the group consisting of halogen, branched or unbranched C1-6alkyl, which is optionally partially or fully halogenated, C3-C3-cycloalkyl, C1-C3-cycloalkenyl, hydroxy group, nitrile, C3-C6alkyloxy group, which is optional necessarily partially or fully halogenated, the group MnC(O) and di(C--C3)alkylaminocarbonyl, - C3-C, cycloalkyl selected from the group that includes cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, bicyclopentyl, bicyclohexyl and beat cycloheptyl, each of which is optionally partially or fully halogenated and optionally substituted with 1-3 C and -C alkyl groups, or an analog of a similar cycloalkyl F) group in which 1-3 ring methylene groups are replaced by groups independently of each other selected from the series that includes 0.5, CHOH, »2С-0, 20-51 МН, - branched C3-Siralkenyl, which is optionally partially or fully halogenated and optionally substituted with 1-3 substituents selected from groups that include branched or unbranched C 4-Salkyl, phenyl, naphthyl, and heterocyclic groups, wherein each such heterocyclic group is independently selected from the group consisting of pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, imidazolyl, pyrazolyl, thienyl, furyl, isoxazolyl and isothiazolyl, and each of such phenyl, naphthyl or heterocyclic groups is substituted with 0-5 substituents selected from the group consisting of halogen, branched or unbranched C 1 -alkyl, which is optionally partially or fully halogenated, cyclo propyl, cyclobutyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, bicyclopentanyl, bicyclohexanyl, bicycloheptanyl, a hydroxy group, a nitrile, a C-S-alkoxy group, which is optionally partially or fully halogenated, a group MNoC(O) and mono- or di(C.--Cz) alkylaminocarbonyl, - СбС5-С,cycloalkenyl, selected from the group that includes cyclopentenyl, cyclohexenyl, cyclohexadienyl, cycloheptenyl, cycloheptadienyl, bicyclohexenyl and bicycloheptenyl, while each such cycloalkenyl group is optionally substituted with 1-3 C.i-C alkyl groups, - nitrile or - branched or unbranched C.i-Caloxycarbonyl, branched or unbranched C.-Salkylaminocarbonyl, branched or unbranched C.-Salkylcarbonylamino-C 1-Salkyl, Ko means branched or unbranched C.-Salkyl, which is optionally partially or fully 7/o hapogenated and optionally substituted with a nitrile, or Ko means acetyl . . and indazolyl, wherein such phenyl, naphthyl or heterocyclic group is optionally substituted with 1-5 substituents selected from the group including is phenyl, naphthyl, heterocycle selected from 2o above in this paragraph of the series, branched or unbranched C /-C alkyl, which is optionally partially or fully halogenated, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, bicyclopentyl, bicyclohexyl, bicycloheptyl, phenyl-C.--Salkyl, naphthyl-C.-Salkyl, halogen, hydroxy group, oxo group, nitrile, C.-Salkoxy group, which is not necessarily partially or fully halogenated, C /4-SalkoxyS-Svalkyl, C.-Czthioalkyl, C.-CzthioalkylC--Salkyl, phenyloxy group, naphthyloxy group, heteroaryloxy group, in which the heterocyclic fragment is selected from the series described above in this paragraph, nitro group, amino group, mono- or di(C4-C3)alkylamino group, phenylamino group , a naphthylamino group, a heterocyclylamino group, in which the heterocyclyl i) fragment is selected from the series described above in this paragraph, the group МН 2С(О0), mono- or di(С--С3)alkylaminocarbonyl, C.-Salkyl-С(О)-С .-Sualkyl, amino-C.-Sualkyl, mMono- or di(C4i-C3)alkylamino-C 1-Sualkyl, amino-5(0) group, di(C4-C3)alkylamino-5(0O)2 group . (C1-C8)alkylamino group, o - condensed aryl selected from the group that includes benzocyclobutanyl, indanyl, indenyl, dihydronaphthyl, Ge! тетрагідронафтил, бензоциклогептаніл і бензоциклогептеніл, або конденсований гетероцикліл, вибраний із групи, яка включає циклопентенопіридин, циклогексанопіридин, циклопентанопіримідин, циклогексанопіримідин, -- Зз5 циклопентанопіразин, циклогексанопіразин, циклопентанопіридазин, циклогексанопіридазин, р. циклопентанохінолін, циклогексанохінолін, циклопентаноізохінолін, циклогексаноізохінолін, циклопентаноіндол, циклогексаноіндол, циклопентанобензімідазол , cyclohexanobenzimidazole, cyclopentanobenzoxazole, cyclohexanobenzoxazole, cyclopentanoimidazole, cyclohexanoimidazole, cyclopentanothiophene, and cyclohexanothiophene, wherein the fused aryl or fused heterocyclyl ring " is substituted with 0-3 substituents independently selected from the group consisting of phenyl, naphthyl, and c heterocyclyl, selected from the group consisting of pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, . imidazolyl, pyrazolyl, thienyl, furyl, isoxazolyl, and isothiazolyl, branched or unbranched C.-Svalkyl, which is optionally partially or fully halogenated, halogen, nitrile, C i-Salkoxy group, which is optionally partially or fully halogenated, phenyloxy group, naphthyloxy group, heterocyclyloxy group, in which the heterocyclyl fragment is selected from the series described above, nitro group, amino group, mono- or -I di(C1-C3)alkylamino group, phenylamino group, naphthylamino group, heterocyclylamino group, in which the heterocyclyl fragment is selected from the series described above, group МН 5С (0), mono- or di(C.4-C3)alkylaminocarbonyl group - C.-Alkyl-OC(O), branched or unbranched C.-Salkyl-C(0)-C.-C;alkyl, amino-C--Salkyl, mono- or He) di(C4i-C3)alkylamino -C 1-Swallyl, Ky-C-Swallyl, Kio-C4-Swalloxy group, K4-F(0)-C.4-Swallyl and the group K/2-C4-Swallyl(K 45) M, o - cycloalkyl, selected from the group that includes cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, bicyclopentyl, bicyclohexyl and bicycloheptyl, while such cycloalkyl is optionally partially or fully halogenated and optionally substituted by 1-3 C.-C alkyl groups, - СбС5- C, cycloalkenyl, selected from the group that includes cyclopentenyl, cyclohexenyl, cyclohexadienyl, dv Cycloheptenyl, cycloheptadienyl, bicyclohexenyl and bicycloheptenyl, while this cycloalkenyl group is optionally substituted with 1-3 C-C alkyl groups, F) - acetyl, aroyl, C --Svalkoxycarbonyl 4-Svalkyl or phenylsulfonyl or ka - branched or unbranched S.--Svalkyl, which is optionally partially or fully halogenated, or in Ku and Kb" together is not required necessarily form a fused phenyl or pyridinyl ring, Kv and Kz are each independently selected from the group consisting of hydrogen and branched or unbranched C, C, alkyl, which is optionally partially or fully halogenated, 65 Ku, K5, Ke, KU, Ke, Ko, Kch44 and Kl" are each independently selected from the group consisting of morpholine, piperidine, piperazine, imidazole and tetrazole, t means 0, 1 or 2, M/ means O or 5, while X is directly attached to one or two groups -Y-7, and its pharmaceutically acceptable derivatives. 10. The compound according to claim 9, in which Ago is naphthyl, tetrahydronaphthyl, indanyl or indenyl and M is 0. 11. The compound according to claim 10, in which 70 Ag means thiophene or pyrazole, each of which is independently substituted by 1-3 Ku, Bo or E groups, X means - C5-Ccycloalkyl or cycloalkenyl, optionally substituted by 1-2 oxo groups or 1-3 C -C.alkyl, C 1 -Slalkoxy or C 1 -C 6 alkylamino chains, each of which is branched or unbranched - phenyl, indanyl, furanyl, thienyl, imidazolyl, pyridinyl, pyrazinyl, tetrahydropyridinyl, pyrimidinyl, pyridinonyl, piperidinyl, benzimidazole or piperazinyl, each of which, independently of each other, are optionally substituted with 1-3 substituents selected from the group consisting of C 1 -C 6 alkyl, C 1 -C 6 alkoxy, hydroxy, nitrile, amino, mono- or di(C 1 -C 6 alkyl )amino group, mono- or di(C-i-Salkylamino)carbonyl, MNHS(O) group, C--Salkyl-Z(O) group and halogen, M means a bond or saturated or unsaturated branched or unbranched C 4 - C.-carbon chain, which is optionally partially or fully halogenated, while one or more C atoms are optionally replaced by O or M, and M in each case is independently optionally replaced by 1-2 oxo groups, nitrile, phenyl, a hydroxy group or one or more C.4-C, alkyl groups, optionally substituted by one or more atoms of halogen, c 2 means - phenyl, heteroaryl selected from pyridinyl, imidazolyl, furanyl and thienyl, heterocycle selected from i) piperazinyl, (2-oxa-5-azabicyclo|2.2.1)heptanyl, pentamethylene sulfidyl, pentamethylene sulfoxidyl, pentamethylene sulfonyl, tetrahydrofuranyl , morpholino group, thiomorpholino group, and piperidinyl, while each of the above-mentioned 7 groups is optionally substituted with 1-3 substituents selected from the c zo group, which includes halogen, C/-Salkyl, C-Salkyloxy, C4-Salkoxy-C4i- Szalkyl, C4-Swalkoxycarbonyl, aroyl, morpholinocarbonyl, C.--Szacyl, oxo group, hydroxy group, pyridinyl-C--Szalkyl, imidazolyl-S.--Szalkyl, o tetrahydrofuranyl-S.-Szalkyl, nitrile-S.-Szalkyl, nitrile, carboxy group, phenyl, where the phenyl ring is Ge! optionally substituted by 1-2 halogen atoms, C-Salkyloxy groups, hydroxy groups or mono- or di(C.4-Salkyl)amino groups, amino-Z(O)t group, C-Salkyl-B(O)t group and the phenyl-Z(O)t group, where the phenyl ring 87 is optionally substituted by 1-2 halogen atoms, C-S-alkyloxy groups, hydroxy groups or mono- or idi(C4i-Salkyl)amino groups, or 7 is optionally substituted by 1 -3 substituents selected from the group that includes an amino group, aminocarbonyl and amino-C.-Salkyl, where the M-atom in each case is independently optionally mono- or disubstituted by aminoC.--Salkyl, C.--Salkyl, arylCo- Szalkyl, C.i-SwaloxyC--Szalky, S.--Swalkoxy group, aroyl, C-Szacyl, C.-Szalkyl-(O)t- group or arylCo-Szalkyl-Z(O) group, and, at the same time each of the specified alkyl and aryl groups attached to the amino group is optionally substituted with 1-2 substituents selected from . group, which includes halogen, S.-Svalkyl and C.-Svalkoxy group, and? or 7 is optionally substituted with 1-3 aryl, heterocyclic or heteroaryl groups as specified above in this paragraph, each of which is in turn optionally substituted with halogen, C 1 -Salkyl or C 1 -Salkyl, -I or 7 means a hydroxy group, hydroxyC-Salkyl, halogen, nitrile, amino group, where the M-atom in each case is independently optionally Mmono- or disubstituted by aroyl, Sb o 4-Szacyl, S.-Salkyl, - C-C-C-alkyl, pyridinylC-C-alkyl, tetrahydrofuranylC-C-alkyl, nitrileC-C-alkyl or He) phenyl, while the phenyl ring is optionally substituted with 1-2 substituents selected from the group that includes 5 Halogen, C-Salkyloxy group, hydroxy group and mono- or di(Ci-Salkyl)amino group, o or 7 means branched or unbranched C.--Salkyl, C--Salkyloxy group or nitrilos.-Su,alkyl, He K. means - branched or unbranched, optionally partially or fully halogenated C.-Alalkyl, - cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, which are optionally partially or fully halogenated and optionally substituted with 1-3 C.-Alalkyl groups, or an analogue such a cycloalkyl group, in which 1-3 ring methylene groups are replaced by groups, independently of each other, selected from О, З and МН, Ф) - branched C3-C-iralkenyl, which is optionally partially or fully halogenated and optionally ka replaced by 1-3 branched or unbranched S.i-Svalkilny by groups, - cyclopentenyl and cyclohexenyl, optionally substituted by 1-3 C.-Salkyl groups, 60 Ko means branched or unbranched C.-Salkyl, which is optionally partially or fully halogenated and optionally substituted by nitrile, Ez means - a phenyl or heterocyclic group selected from the group consisting of pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl and pyrazolyl, wherein such phenyl or heterocyclic group is optionally substituted with 1-5 65 substituents selected from the group consisting of phenyl, heterocycle selected from of the series described above in this paragraph, branched or unbranched C .-Svalkyl, which is optionally partially or fully halogenated, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, bicyclopentyl, bicyclohexyl, bicycloheptyl, phenyl-C--C-alkyl, naphthyl-C--C-alkyl, halogen, hydroxy group, oxo group, nitrile, C-C-C-alkyl, which is optionally partially or fully halogenated, Cbo4-Szalkoxys.--Svalkyl, S.-Szthioalkyl, C-C3-thioalkylC-C-alkyl, phenyloxy group, naphthyloxy group, heteroaryloxy group in which the heterocyclic fragment is selected from the series described above in this paragraph, nitro group, amino group, mono- or di(C4-C3)alkylamino group, phenylamino group, naphthylamino group, heterocyclylamino group in which heterocyclyl fragment selected from the series described above in this paragraph, group MH 2C(0), mono- or di(C41-C3)alkylaminocarbonyl, C.-Salkyl-C(O0)-C.-Salkyl, amino-C.--Salkyl , mMono- or 7/0. VKS4-C3)alkylamino-C 1-Svalkyl, amino-5(0) group", di(C4-C3)alkylamino-5(0O)2 group, C.-C.4-Svalkyl, C5-Ci-Svalkoxy group, Ke-FK(0)-C.4-Salkyl, group K,-C.4-Salkyl(Ka)M and carboxy-mono- or di(C4-C)-alkylamino group, - condensed aryl selected from the group which includes benzocyclobutanyl, indanyl, indenyl, wherein such fused aryl is substituted with 0-3 substituents independently selected from the group consisting of 7/5 phenyl, naphthyl, and heterocyclyl selected from pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, imidazolyl , pyrazolyl, thienyl, furyl, isoxazolyl and isothiazolyl, branched or unbranched C-Salkyl, which is optionally partially or fully halogenated, halogen, nitrile, C 4-Salkoxy, which is optionally partially or fully halogenated, phenyloxy, naphthyloxy, heterocyclyloxy, in which the heterocyclyl moiety is selected from the group described above in this paragraph , a nitro group, an amino group, a mono- or di(C.i-C3) alkylamino group, a phenylamino group, a naphthylamino group, a heterocyclylamino group, in which the heterocyclyl fragment is selected from the group described above in this paragraph, the group МНБС(О), and mono- or di(C --C3)alkylaminocarbonyl, group C.-C.alkyl-OS(O), branched or unbranched C.-Svalkyl-C(0)-C.-C,alkyl, amino-Si--Svalkyl, mono- or di(C--C3)alkylamino-C--Svalkyl, Ke-S.i-Svalkyl, Ko -C4-Salkyloxy group, K44-C(0)-C.4-Salkyl and the group Ki2-C4-Salkyl(K45)M, ch - cycloalkyl selected from the group that includes cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, when this cycloalkyl is not necessarily partially or fully halogenated and is not necessarily i) substituted by 1-3 C.-Salkyl groups, - C-Salkyloxycarbonyl 1-Salkyl, or C. and Co together optionally form a condensed phenyl or pyridinyl ring, c zo Kv and Kz are each independently selected from the group consisting of hydrogen and branched or unbranched C.--C;alkyl, which is optionally partially or fully halogenated, and b Ku, K5, Ke, KU, Ke , Ko, Kch44 and Kl" are each independently selected from the group consisting of morpholine, piperidine, piperazine, imidazole and tetrazole, wherein X is directly attached to one -Y-7 group. uh- 12. The compound according to claim 11, in which Agi means pyrazole, X means - cyclopentenyl, cyclohexenyl, cycloheptenyl, optionally substituted by an oxo group or 1-3 C.-C; alkyl, " 40. C1-Slalkoxy- or C.4-C.alkylamino chains, each of which is branched or unbranched, with c - phenyl, furanyl, thienyl, pyridinyl, pyrazinyl, piperidinyl or pyrimidinyl, each of which is independently . optionally substituted with 1-3 substituents selected from the group consisting of C--Soalkyl, C-1-Soalkyl, and hydroxy group and halogen, 2 means phenyl, heteroaryl selected from pyridinyl, imidazolyl and furanyl, heterocycle selected from -I 2-oxa-5-azabicyclo|2.2.1)heptanyl, pentamethylenesulfidyl, pentamethylenesulfoxidyl, pentamethylenesulfonyl, tetrahydrofuranyl, tetrahydropyranyl, piperazinyl, morpholino group, - thiomorpholino group, thiomorpholinosulfoxide and piperidinyl, while each of the above-mentioned 7 groups is optionally substituted with 1-3 substituents selected from the group that includes halogen, C/-Salkyl, C-Salkyloxy, C4-Salkoxy-C4i -Szalkyl, C4-Swalkoxycarbonyl, o aroyl, morpholinocarbonyl, C.--Szacyl, oxo group, hydroxy group, pyridinyl-C-i-Szalkyl, imidazolyl-S.--Szalkyl, He tetrahydrofuranyl-S.-Szalkyl, nitrile-S. -Salkyl, nitrile, carboxy group, phenyl, where the phenyl ring is optionally substituted by 1-2 halogen atoms, C the C--Svalkyl-Z(O) group and the phenyl-Z(O)y group, where phenyl the ring is optionally substituted by 1-2 halogen atoms, C -- C-alkyloxy groups, hydroxy groups or mono- or di(C4i-Salkyl)amino groups, F) or 7 optionally substituted by 1-3 amino groups, aminocarbonyl groups or amino-C /- C-alkyl groups, where the M-atom is not necessarily in each case independently mono- or disubstituted by amino-C 1-C alkyl, C-C alkyl, arylCo-C alkyl, C-4-C alkyl, C-C alkyl, C-C alkyl , aroyl, C.-Szacyl, because the group C.-Szalkyl-Z(O) n-, pyridinyl-Cz-Szalkyl, tetrahydrofuranyl-Cz-Szalkyl or the group arylCo-Szalkyl-Z(O)1-, while each of of the above-mentioned alkyls and aryls attached to the amino group, optionally substituted by 1-2 halogen atoms, C41-Salkyl groups or C.-Salkyloxy groups, or 7 means a hydroxy group, hydroxyC-Salkyl, halogen, nitrile, amino group, where the M atom is not necessarily in each case independently Mmono- or disubstituted by C-Svalky, pyridinylso-Szalky, 65 tetrahydrofuranylC o-Szalky, Si-Svalkoxys-Szalky, Si-Szacyl m, nitrileC-C.alkyl or phenyl, while the phenyl ring is optionally substituted by 1-2 halogen atoms, C-C-C alkyloxy groups, hydroxy groups or mono- or di(C.I-C.Alkyl)amino groups, or 7 means branched or unbranched C .--Alkyl, C--Alkoxy group or nitrileOS.-Su,alkyl, K. means - branched or unbranched C, C, alkyl, which is not necessarily partially or fully halogenated, - cyclopropyl, cyclobutyl, cyclopentanyl, cyclohexanyl and cycloheptanyl, which are not necessarily partially or fully halogenated and optionally substituted 1-3 C.-C alkyl groups, or an analogue of such a cycloalkyl group, in which 1-3 ring methylene groups are replaced by groups independently selected from O, C and MH, - branched C3-Siralkenyl, which is optionally partially or fully halogenated and optionally necessarily 70 substituted by 1-3 branched or unbranched C. and C. alkyl groups, - cyclopentenyl and cyclohexenyl, optionally substituted by 1-3 C. - C. alkyl groups, Ko means branched or unbranched C. - C. alkyl, which is not necessarily partially or completely halogenated and optionally substituted with a nitrile, Ez means a phenyl or heterocyclic group selected from the group consisting of pyridinyl, pyrimidinyl, pyridazinyl and pyrazolyl, wherein such phenyl or heterocyclic group upa is optionally substituted with 1-5 substituents selected from the group consisting of phenyl, a heterocycle selected from the group described above in this paragraph, branched or unbranched C.-alkyl, which is optionally partially or fully halogenated, phenyl-C. -Salkyl, halogen, hydroxy group, oxo group, nitrile, C--Salkoxy group, which is not necessarily partially or 2o fully halogenated, C--Sthioalkyl, C4-SthioalkylC1-Salkyl, amino group, mono- or di(C--C3) an alkylamino group, a MNHS(O) group, or a mono- or di(C.--C3)alkylaminocarbonyl, - C-C-Salkyloxycarbonyl 1-Salkyl, or Kz means cyclopropyl or cyclopentyl, each of which is optionally partially or fully halogenated and optionally substituted by 1-3 C.-Alkyl groups, or with Ku and KB" together optionally form a condensed phenyl or o pyridinyl ring. 13. The compound according to claim 12, in which M means -СНо-, -ОО-(СНо)оз-, -СНоСН»о-, -СНОМН-, -СНо.СнНо-МН-, МН-СНСН»-, -СН .-МН-СНо-, --МН-, -МН-С(О0)-, -С(0)-, -СН(ОН)-, -СН(СНоСН»)- or a bond, с з Х means - cyclohexenyl, optionally substituted by an oxo group or 1-3 C --Slalkyl, C.--Slalkoxy- or o C.-C.alkylamino chains, each of which is branched or unbranched, b - phenyl, pyridinyl, pyrazinyl, piperidinyl or pyrimidinyl, each of which is optionally independently substituted with 1-3 substituents selected from the group consisting of C.-S.alkyl , C--Soalkoxy group, hydroxy group and 007 zv Halogen, part 2 means - phenyl, heteroaryl selected from pyridinyl, imidazolyl and furanyl, heterocycle selected from 2-oxa-5-azabicyclo|2.2.1)heptanyl, pentamethylene sulfidyl, pentamethylene sulfoxidyl, pentamethylenesulfonyl, tetrahydrofuranyl, tetrahydropyranyl, piperazinyl, morpholino group, thiomorpholino group, thiomorpholinosulfoxide and piperidinyl, with c, while each of the 7 groups specified above is optionally substituted with 1-3 substituents selected from . a group that includes halogen, C 1-Salkyl, C-Salkyl, C.4-Salkyl, C-Salkyl, and? aroyl, morpholinocarbonyl, C.--Szacyl, oxo group, hydroxy group, pyridinyl-C-and-Szalkyl, imidazolyl-C.--Szalkyl, tetrahydrofuranyl-C.-Szalkyl, nitrile-C--Szalkyl, nitrile, carboxy group, phenyl, where the phenyl ring is optionally substituted by 1-2 halogen atoms, C-Salkyloxy groups, hydroxy groups or mono- or -I di(C4i-Salkyl)amino groups, the amino-5(O)»t group, the C--Salkyl-Z group (O) t and the phenyl-Z(O)y group, where the phenyl ring is optionally substituted by 1-2 halogen atoms, C--C-S-alkyloxy groups, hydroxy groups or mono- or -di(C4i-S-alkyl)amino groups, co or 7 neoob necessarily substituted by 1-3 amino groups or aminocarbonyl groups, where the M-atom is optional In each case independently mono- or disubstituted by aminoC. o S.-SvaloxyC-S-alkyl, C-Svaloxy, aroyl, C--Szacyl, C.--Salkyl-Z(O)»t- group or He group arylCo-Szalkyl-Z(O)1-, while each of the above-mentioned alkyls and aryls attached to the amino group, optionally substituted by 1-2 halogen atoms, C41-Salkyl groups or C.-Salkyloxy groups, or 7 means a hydroxy group, hydroxyC-Salkyl, halogen, nitrile, amino group, where the M atom optional in In each case independently Mmono- or disubstituted by C.-C alkyl, pyridinyl-C alkyl, tetrahydrofuranyl 4-C alkyl, C.--C alkyl, C.-C alkyl, nitrileC.-C alkyl, phenyl , while Ф) the phenyl ring is optionally substituted by 1-2 halogen atoms, C 1-Salkyloxy groups, hydroxy groups or mono- or di(Ci-Salkyl)amino groups, or 7 means branched or unbranched C.-Salkyl, C- -Salkoxy group or nitriloC.-C.sub.alkyl, 60 Ki means branched or unbranched C.-C.alkyl, which is optionally partially or fully halogenated, Ko means branched or unbranched C-C alkyl, which is optionally partially or fully halogenated and optionally substituted with a nitrile, Ez means 65 - phenyl or heterocyclic group selected from the group consisting of pyridinyl, pyrimidinyl and pyrazolyl, wherein such phenyl or heterocyclic group is optional is necessarily substituted by 1-5 substituents selected from the series that includes a branched or unbranched C.i.sub.Alkyl, which is optionally partially or fully halogenated, a C.--S.Alkoxy group, which is optionally partially or fully halogenated, C 4- sthioalkyl, C.-C3thioalkylC 1-Cylalkyl, an amino group or a group MNHS(O), - C-C3alkyloxycarbonyl, or Cz means cyclopropyl or cyclopentyl, each of which is optionally partially or fully halogenated and optionally substituted by 1-3 C.-C3alkyl in groups 14. The compound according to claim 13, in which Agi means 5-tert-butylpyrazol-3-yl, where the pyrazole ring is in each case independently substituted by 1-2 7/0 groups K" or Kz, X means - cyclohexenyl, - phenyl, pyridinyl . )heptanyl, pentamethylene sulfidyl, pentamethylene sulfoxidyl, tetrahydrofuranyl, piperazinyl, morpholino group, thiomorpholino group, and piperidinyl, while each of the above 7 groups is optionally substituted with 1-3 substituents selected from the Group, which includes C.i.sub.6alkyl, C.sub.4-Szalkoxy group , an oxo group, a hydroxy group and a group МНБС(О)-, or 7 means hydroxyC--Salkyl, an amino group, where the M-atom is not necessarily mono- or disubstituted in each case independently by pyridinylmethyl, tetrahydrofuranylmethyl, C.4-SalkoxyC-Salkyl, Si -- Szacylom or nitrileC -C.alkyl, or 7 means nitrileC.-C,alkyl, ch Ez means - phenyl or a heterocyclic group selected from the series that includes pyridinyl, pyrimidinyl and pyrazolyl, while i) such a phenyl or heterocyclic group is optionally substituted 1 -2 substituents selected from the group that includes C.sub.-Soalkyl, which is optionally partially or fully halogenated, C.sub.4-Soalkyl, which is optionally partially or fully halogenated, C.sub.1-Sothioalkyl, C.sub.4-SothioalkylC-Ssubalkyl, amino group and the group c zo МНХС(О), - C-Szalkoxycarbonyl, o or Kz means cyclopropyl or cyclopentyl, each of which is optionally partially or fully halogenated and optionally substituted with 1-3 C.-Szalkyl groups. 15. The compound according to claim 14, in which X is pyridinyl. -- 16. The compound according to claim 15, in which pyridinyl is attached to Ag. in the 3rd position of pyridinyl. uh- 17. Compound of formula (11): ШЧИ , v ry KE « | I - s n Nn h I! we where o means - an aromatic C3-C-ocarbocycle or a saturated or unsaturated unsaturated C3-C-ocarbocycle, - and - a 6-10-membered heteroaryl containing one or more heteroatoms selected from C, Mi 5, - - B-8 - lene monocyclic heterocycle, which contains one or more heteroatoms selected from 0, M and 5, or - 8-11--lene bicyclic heterocycle, which contains one or more heteroatoms selected from zo, M and 5, is), with this C is substituted by one or more groups K., K» or Kz, c 20 Ag means phenyl, naphthyl, quinolinyl, isoquinolinyl, tetrahydronaphthyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, benzimidazolyl, benzofuranyl, dihydrobenzofuranyl, indolinyl, benzothienyl, Co) dihydrobenzothienyl, indanyl, indenyl or indolyl, each of which is optionally substituted by one or more groups K, or Kv, X means 22 - Cb-Cv cycloalkyl or cycloalkenyl, optionally substituted by 1-2 oxo groups or 1-3 C -C; alkyl, Ge! C.-C.Alkoxy- or C.-C.Alkylamino chains, - phenyl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, pyridinyl, pyrimidinyl, pyridinonyl, co dihydropyridinonyl, maleimidyl, dihydromaleimidyl, piperidinyl, benzimidazole, ZH-imidazo|4 ,5-b|pyridine, piperazinyl, pyridazinyl or pyrazinyl, 60 M means a bond or saturated or unsaturated branched or unbranched C 4-C; a carbon chain that is optionally partially or fully halogenated, wherein one or more methylene groups are optionally substituted with O, M, or 5(O), and M is optionally independently substituted with 1-2 oxo groups, phenyl, or one or by several C. and C. alkyl groups, optionally substituted by one or more halogen atoms, 65 27 means - phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, furanyl, thienyl, pyranyl, each optionally substituted with 1-3 substituents selected from the group consisting of halogen, C-Salkyl, C-Salkyl, hydroxy, amino, mono- or di(C-Salkyl)amino , C.-Svalkyl-B(O)t group, SM group, SOMNo group, COOH group and phenylamino group, where the phenyl ring is optionally substituted by 1-2 halogen atoms, C41-Svalkyl groups or C.-Svaloxy groups, - tetrahydropyranyl . or tetramethylenesulfonyl, 70 each of which is optionally substituted with 1-3 substituents selected from the group consisting of nitrile, C 4-Cylalkyl, C.-Salkoxy group, hydroxy group, amino group, mono- or di(C.-Salkyl)amino-C-Salkyl, SOMN group, phenylamino-C-Salkyl and C4-Salkoxy-S.-Salkyl, - halogen, S. -C; alkyl, nitrile, amino group, hydroxy group, C-C-C-C alkyloxy group, MNHS(O) group, mono- or di(C4-C alkyl)aminocarbonyl, mono- or di(C-C alkyl)damino group, secondary or tertiary amine, when this /5 amine nitrogen is covalently bound to C -Salkyl or C.Swaloxyalkyl, pyridinyl-C.S-alkyl, imidazolyl-S.i-Salkyl, tetrahydrofuranyl-C.S-alkyl, nitrile-C-Salkyl, carboxamide-C --Salkyl, phenyl, where the phenyl ring is optionally substituted by 1-2 halogen atoms, C--Salkyloxy groups, hydroxy groups or mono- or di(C.i-Salkyl)amino groups, the group S.-Salkyl-Z3(O)2t or the phenyl-5(O)4 group, where the phenyl ring is optionally substituted by 1-2 halogen atoms, C-C-C alkyloxy groups, hydroxy groups or mono- or B(Ci-C alkyl)amino groups, - Si-Svalkyl-B(O)»t and phenyl-5(O)2, where the phenyl ring is optionally substituted by 1-2 halogen atoms, C.-Salkyloxy groups, hydroxy groups or mono- or di(C.4-Salkyl)amino groups, Ki in each case independently means - C.-Siralalkyl, which is optionally partially or fully halogenated and optionally substituted by 1-3 c ov Substituents selected from the group that includes C 3-C.iocycloalkanyl, hydroxy group, phenyl, naphthyl, pyridinyl, pyrimidinyl, pyrazinyl , pyridazinyl, pyrrolyl, imidazolyl, pyrazolyl, thienyl, furyl, isoxazolyl. (| (8) isothiazolyl, while each of the above substituents is optionally substituted by 1-5 substituents selected from halogen, C.sub.1-alkyl, which is optionally partially or fully halogenated, C.sub.3-C.sub.cycloalkanyl, C.sub.5-C.sub.cycloalkenyl, a hydroxy group, a nitrile, a C-C-C alkyloxy group, which is optionally partially or fully halogenated, a MNHS(O) group, a mono- or di(C-C-C alkyl)amino group and a mono- or di(C 4-C alkyl)aminocarbonyl , - a cyclopropyloxy group, a cyclobutyloxy group, a cyclopentyloxy group, a cyclohexyloxy group or a cycloheptyloxy group, each of which is optionally partially or fully halogenated and optionally substituted with (33 1-3 substituents selected from the group that includes C 4-Salkyl, which is optionally partially or fully halogenated, the SM group, hydroxyCi-Salkyl and aryl, or an analogue of such a cycloalkyl group, in which 1-3 ring methylene groups are independently replaced by 0.5(O)»4, CHOH, »C-0.2 -5 or МН, и- - a phenyloxy group or a benzyloxy group, each of which is optional o partially or fully halogenated and optionally substituted with 1-3 substituents selected from the group that includes C 4-C alkyl, which is optionally partially or fully halogenated, the CM group, hydroxyC-C alkyl and aryl, or an analogue of such a cycloaryl group , in which 1-2 ring methylene groups are independently replaced by M, " - cyclopropanyl, cyclobutanyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, bicyclopentanyl, not) bicyclohexanyl or bicycloheptanyl, each of which is optionally partially or fully halogenated and optionally substituted 1-3 substituents selected from the group that includes C 4-Salkyl, which is optionally partially or fully halogenated, the CM group, hydroxyC-Salkyl and aryl, or an analogue of such a cycloalkyl group, in which 1-3 ring methylene groups are independently replaced by O, 5(O)t, CHOH, »C-0, 2-5 or MH, - branched or unbranched C3-Siralkenyl, which in each case is optionally partially or -I fully halogenated and optionally replaced by 1-3 substitutes we selected from the group which includes branched or unbranched S-Svalkyl, phenyl, naphthyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, - pyrrolyl, imidazolyl, pyrazolyl, thienyl, furyl, isoxazolyl and isothiazolyl, while each of these Ge) substituents are substituted with 1-5 substituents selected from the group consisting of halogen, C.i.alkyl, which is optionally partially or fully halogenated, cyclopropanyl, cyclobutanyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, bicyclopentanyl, bicyclohexanyl and bicycloheptanyl, a hydroxy group, nitrile, a C-C alkyloxy group, He which is optionally partially or fully halogenated, a MH C(O) group and a mono- or di(C-C alkyl)aminocarbonyl, while such a branched or unbranched C 3-Siralkenyl is optionally interrupted by one or several heteroatoms selected from 0, M and (OO) t, - cyclopentenyl, cyclohexenyl, cyclohexadienyl, cycloheptenyl, cycloheptadienyl, bicyclohexenyl or bicycloheptenyl, while such a cycloalkenyl group is not is substituted by 1-3 C. and C. alkyl groups, (F) - nitrile, halogen, ka - methoxycarbonyl, ethoxycarbonyl and propoxycarbonyl, - silyl, which contains three C. - C. alkyl groups, which are not necessarily partially or fully halogenated , 60 - C4-Alkynyl branched or unbranched carbon chain, which is optionally partially or fully halogenated, while one or more methylene groups are optionally replaced by О, МН or З(О)т, and the specified alkynyl group is optionally independently substituted by 1-2 oxo groups, pyrrolidinyl, pyrrolyl, one or more C.--C; alkyl groups, optionally substituted by one or more halogen atoms, nitrile, morpholino group, piperidinyl, piperazinyl, imidazolyl, phenyl, 65 pyridinyl, tetrazolyl or a mono- or di(C.i-Salkyl)uamino group, optionally substituted by one or more halogen atoms, EC", RK. and K5 each means - a branched or unbranched C.--alkyl, which is optionally partially or fully halogenated, acetyl, aroyl, a branched or unbranched C.i.-C.alkyloxy group, which in each case is optionally partially or fully halogenated, halogen, methoxycarbonyl, C1-C6alkyl-Z(O)t group, which is optionally partially or fully halogenated, or phenylsulfonyl, - C1-C6oxy, hydroxy group, amino group, mono- or di(C1-C6 alkyl)amino group , nitrile or halogen, - group OK", - nitro group or 70 - group mono- or di(C.4-C.alkyl)lamino-B(O)", which is not necessarily partially or fully halogenated, or the group NaM5O" , Ez in each case independently means - phenyl, naphthyl, morpholinyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, pyrrolidinyl, imidazolyl, pyrazolyl, thiazolyl, oxazolyl, triazolyl, tetrazolyl, thienyl, furyl, tetrahydrofuryl, isoxazolyl, isothiazolyl, quinolinyl, isoquinolinyl, indolyl, benzimidazolyl, benzofuranyl, benzoxazolyl, benzisoxazolyl . which are described above in this paragraph, branched or unbranched C.i-Svalkyl, which is optionally partially or fully halogenated, cyclopropanyl, cyclobutanyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, bicyclopentanyl, bicyclohexanyl, bicycloheptanyl, phenyl-C.-Svalkyl, naphthyl- C-C alkyl, halogen, hydroxy group, oxo group, nitrile, C-C alkyloxy group, which is optionally partially or fully halogenated, phenyloxy group, naphthyloxy group, heteroaryloxy group and heterocyclooxy group, where the heterocyclic or heteroaryl moiety is described above in this paragraph, nitro group, amino group, mono- or s ov DY(C1-Salkyl)amino group, phenylamino group, naphthylamino group, heteroarylamino group or heterocyclamino a group where the heteroaryl or heterocyclic fragment is described above in this paragraph, the group MNHS(O), mono- or i) di(C4-Calkyl)aminocarbonyl, C4-Salkyl-C(O)-C.-Salkyl, amino-C. -Svalkyl, MOono- or di(C4i-Szalkyl)amino-C -Svalkyl, group amino-5(0)", group di(C--Szalkyl)amino-5(0)2, K.,-S.- Svalkyl, Ka-C--Svalkoxy group, Kea-C(0)-C.4-Svalkyl, Kio-C4-Svalkyl(K44)M group and carboxy-mono- or sizo VKS4-Svalkyl)amino group, - kCondensed aryl, вибраний з бензоциклобутанілу, інданілу, інденілу, дигідронафтилу, що) тетрагідронафтилу, бензоциклогептанілу і бензоциклогептенілу, або конденсований гетероарил, вибраний з ду циклопентенопіридинілу, циклогексанопіридинілу, циклопентанопіримідинілу, циклогексанопіримідинілу, циклопентанопіразинілу, циклогексанопіразинілу, циклопентанопіридазинілу, циклогексанопіридазинілу, (7 циклопентанохінолінілу, циклогексанохінолінілу, циклопентаноізохінолінілу, циклогексаноізохінолінілу , i- cyclopentanoindolyl, cyclohexanoindolyl, cyclopentanobenzimidazolyl y, cyclohexanobenzimidazolyl, cyclopentanobenzoxazolyl, cyclohexanobenzoxazolyl, cyclopentanoimidazolyl, cyclohexanoimidazolyl, cyclopentanothienyl, and cyclohexanothienyl, wherein the fused aryl or fused heteroaryl ring is independently substituted with 0-3 substituents selected from the group consisting of phenyl, naphthyl, pyridinyl, "pyrizinyl, pyrimidinyl, pyrrolyl, imidazolyl, pyrazolyl, thienyl, furyl, isoxazolyl, isothiazolyl, etc.") c C 1-C alkyl, which is optionally partially or fully halogenated, halogen, nitrile, C 1-C alkyloxy, which is optionally partially or fully halogenated, phenyloxy, naphthyloxy, heteroaryloxy, or a heterocyclooxy, where the heteroaryl or heterocyclic moiety is as described above in this paragraph, a nitro group, an amino group, a mono- or di(C--Salkyl)amino group, a phenylamino group, a naphthylamino group, a heteroarylamino group, or a heterocyclamino group, where the heteroaryl or heterocyclic moiety is described above in this paragraph, the group МНЬС(О), mono- or di(C.i-Salkyl)aminocarbonyl, C.-C; alkyl-OS(O) group, and C.4-Salkyl-C(O0)-C.-Salkyl, amino-C.-Salkyl, mono- or di(Ci-C3)alkylamino-C-Salkyl, Ki2-C4-Salkyl, C.3-C4-Svaloxy group, C414-C(0)-C.4-Svalkyl and group K/5-C1.Svalkyl(Kv)M, He) - cyclopropanil, cyclobutanil, cyclopentanil, cyclohexanil, cycloheptanil, bicyclopentanil, bicyclohexanil or bicycloheptanyl, each of which is optionally partially or fully halogenated and optionally substituted with 1-3 C /-C alkyl groups, or an analogue of such a cycloalkyl group in which 1-3 Ge ring methylene groups are independently replaced by 0.5, СНОН, 2С-0, 2-5 or МН, - cyclopentenyl, cyclohexenyl, cyclohexadienyl, cycloheptenyl, cycloheptadienyl, bicyclohexenyl or bicycloheptenyl, each of which is optionally substituted with 1-3 C.-C alkyl groups, - C4-C.alkylphenyl- C(0)-C4-Alkyl-, C4-C;alkyl-C(O)-C.-C;alkyl- or C4-C,alkylphenyl-5(O) t-C4-Sulalkyl-, - C.-Svalkyl group or branched or unbranched C-Svalkoxy group, each of which is optional (F, partially or fully halogenated or optionally substituted by K-7 group, ka - OK.v or S.-Svalkyl, optional necessarily substituted by the group OKv, - amino group or mono- or di(C.4-Salkyl) amino group, optionally substituted by the group Kch9, в - Koos(O)M(K 21)-, K20- or KozkK24MS(O)-, Ков(СНо)тС(ОМ(К214)- or КоС(ОХСН») PiК), - С2-Svalkenyl, substituted by the group KozКо4МС(О)-, - S.-Alkynyl branched or unbranched carbon chain, which is optionally partially or fully halogenated, while one or more methylene groups are optionally replaced by 0, МН, З(О)т, and the specified alkynyl group is optionally independently substituted by 1-2 oxo groups, pyrrolidinyl, 65 pyrrolyl, morpholinyl, piperidinyl, piperazinyl, imidazolyl, phenyl, pyridinyl, tetrazolyl, one or more C.-C; alkyl groups, optionally substituted by one or more halogen atoms, nitrile, morpholino group , piperidinyl, piperazinyl, imidazolyl, phenyl, pyridinyl, tetrazolyl or mono- or di(C.4-C.alkyl)amino group, which can be substituted by one or more halogen atoms, or - aroyl, Kv means C.-C.alkyl , which is optionally partially or fully halogenated and optionally substituted by the group Kev, k,, EB, Ko, Ko, EK", Kz, EK, GE, Ku", Kv, ov and Kov each independently of one another means nitrile , phenyl, morpholino group, piperidinyl, piperaz ynyl, imidazolyl, pyridinyl, 7/0 tetrazolyl, an amino group or a mono- or di(C.i-C.alkyl)amino group which is optionally partially or fully halogenated, Ku and Kv each independently represent hydrogen or C. -C,alkyl, which is optionally partially or fully halogenated, Kv in each case independently means hydrogen or C.4-C;alkyl, which is optionally independently substituted by a 7/5 oxo group or a Kov group, Koo in each case independently means C.-C-alkyl, which is optionally partially or fully halogenated, phenyl or pyridinyl, C2i in each case independently means hydrogen or C.4-C.alkyl, which is optionally partially or fully halogenated, Co", Coz, and Cod each independently of each other means hydrogen, C. and Svalkyl, which is not necessarily partially or fully halogenated, and C 4-Svalkyl is indicated. optionally interrupted by one or more atoms o, M or 5, as well as independently optionally substituted by mono- or di(C--Salkyl)aminocarbonyl, phenyl, pyridinyl, amino group or mono- or di(C.--C; alkyl)amino group, while each of the specified substituents is optionally partially or fully halogenated and optionally substituted with a mono- or di(C.-S-alkyl)amino group, or Coz and Cod together optionally form a heterocyclic or heteroaryl i) ring , t means 0, 1 or 2 and M/ means O or 5, c zo and its pharmaceutically acceptable derivatives. 18. Compound according to claim 17, in which what) o means Ge! - phenyl, naphthyl, benzocyclobutanyl, dihydronaphthyl, tetrahydronaphthyl, benzocycloheptanyl, benzocycloheptenyl, indanyl, indenyl, -- - pyridinyl, pyridonyl, quinolinyl, dihydroquinolinyl, tetrahydroquinoyl, isoquinolinyl, tetrahydroisoquinoyl, y- pyridazinyl, pyrimidinyl, pyrazinyl, benzimidazolyl, benzothixyl benzofuranyl, benzothiophenyl, benzpyrazolyl, dihydrobenzofuranyl, dihydrobenzothiophenyl, benzooxazolonyl, benzo|1,Zoxazin-3-onyl, benzodioxolyl, benzo|1,3|dioxol-2-onyl, benzofuran-Z-onyl, tetrahydrobenzopyranyl, indolyl, indolinyl, indolonyl, Indolinonyl, phthalimidyl, chromoyl, «-oxetanyl, pyrrolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, piperidinyl, piperazinyl, morpholinyl, stv) with tetrahydropyranyl, dioxanyl, tetramethylenesulfonyl, tetramethylenesulfoxidyl, oxazolinyl, thiazolinyl, imidazolinyl, tetrahydropyridinyl, homopiperidinyl, pyropyrlinyl, tetrahydrinyl, decahydrinyl decahydroisoquinolinyl, thiomorpholinyl, thiazolidinyl, dihydrooxazinyl, dihyde ropyranil, oxocanil, heptacanil, thioxanil or dithianil, while C is replaced by one or more groups K., K» or Ku. - And 19. The compound according to claim 18, in which b means phenyl, pyridinyl, pyridonyl, naphthyl, quinolinyl, isoquinolinyl, pyrazinyl, benzimidazolyl, - benzoxazolyl, benzofuranyl, benzothiophenyl, benzpyrazolyl, dihydrobenzofuranyl, dihydrobenzothiophenyl, Ge) indanyl, indenyl, indolyl, indolinyl, indolonyl, or indolinonyl, while being substituted by one or more Ku, K" or Ku groups, 1 Ag means naphthyl, quinolinyl, isoquinolinyl, tetrahydronaphthyl, tetrahydroquinolinyl, He tetrahydroisoquinolinyl, indanyl, indenyl, or indolyl, each of which is optionally substituted by one or more groups K, or Kv, X means phenyl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, pyridinyl, pyrimidinyl, pyridinonyl, dihydropyridinonyl, maleimidyl, dihydromaleimidyl, piperidinyl, piperazinyl, pyridazinyl or pyrazinyl, M means a bond or saturated or an unsaturated C /-C.-carbon chain, while one of the F) carbon atoms is optionally replaced by O, M or 5(O) t, and U is optionally independently substituted by 1-2 ox groups, such as phenyl or one or more C.i.C., alkyl groups, optionally substituted by one or more halogen atoms, in 7 means - phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, imidazolyl, furanyl, thienyl, dihydrothiazolyl, dihydrothiazolylsulfoxidyl . and the OH group, 65 - tetrahydropyranyl, tetrahydrofuranyl, 1,3-dioxolanonyl, 1,3-dioxanonyl, 1,4-dioxanyl, morpholinyl, thiomorpholinyl, thiomorpholinosulfoxidyl, piperidinyl, piperidinonyl, piperazinyl, tetrahydropyrimidonyl, pentamethylenesulfidyl, pentamethylenesulfoxidyl, pentamethylenesulfonyl, tetramethylenesulfidyl, tetramethylenesulfoxidyl, or tetramethylenesulfonyl, which are optionally substituted with 1-3 substituents selected from the group consisting of nitrile, C 4-C alkyl, C 4-C 6-alkyl, amino, mono- or di(C 4- Salkyl)amino group, SOMN" group and OH group, - nitrile, C.--Salkyl-B(O)t, halogen, hydroxy group, C.i-C.alkyl group, amino group, mono- or di(C--Salkyl) an amino group, a mono- or di(C4i-Salkyl)aminocarbonyl or a MNHS(O) group, Ki in each case independently means - C3-Salkyl, which is optionally partially or fully halogenated and optionally substituted with 1-3 /o substituents, selected from the group that includes C 5-Seccycloalkyl, phenyl, thienyl, furyl, isoxazolyl and isothiazolyl, where each of the specified substituents is optionally substituted with 1-3 substituents selected from halogen, S.-Szalkyl, which is not necessarily partially or fully halogenated, hydroxy groups, nitrile and C.-Csalkoxy group, which is optionally partially or fully halogenated, - cyclopropyl, cyclobutyl, cyclopentanyl, cyclohexanyl, bicyclopentanyl or bicyclohexanyl, each of y/5 WHICH is optionally partially or fully halogenated and optionally substituted with 1-3 substituents, selected from the group consisting of C 4 -S alkyl, which is optionally partially or fully halogenated, a CM group, hydroxy-C 4 -S alkyl and phenyl, or an analogue of such a cycloalkyl group in which 1-3 ring methylene groups are independently replaced by 0 , 5, СНОН, »С-0, 2-5 or МН, or - silyl, which contains three C.-C, alkyl groups, which are not necessarily partially or fully halogenated, Ko in each case independently means halogen, С. -Salkoxy group, C.i.S.alkyl-Z(O)t group, which is not necessarily partially or fully halogenated, phenylsulfonyl or nitrile, Ez in each case independently means - phenyl, morpholino group, pyridinyl, pyrimidinyl, pyrazinyl, pyrrolyl, pyrrolidinyl, imidazolyl, pyrazolyl, each of which is optionally substituted substituted with 1-3 substituents selected from the group consisting of phenyl, naphthyl, sz ov Heterocycle or heteroaryl, which are described above in this paragraph, C /-Salkyl, which is optionally partially or fully halogenated, cyclopropanyl, cyclobutanyl, cyclopentanyl, cyclohexanyl , cycloheptanyl, and) bicyclopentanyl, bicyclohexanyl, bicycloheptanyl, phenyl-C--Salkyl, naphthyl-C-Salkyl, halogen, oxo group, hydroxy group, nitrile, C.-Salkyloxy group, which is optionally partially or fully halogenated, phenyloxy group, a naphthyloxy group, a heteroaryloxy group, or a heterocyclooxy group, where the heteroaryl or suso heterocyclic moiety is described above in this paragraph, a nitro group, an amino group, a mono- or di(C4-C4-alkyl)amino group, a phenylamino group, a naphthylamino group, a heteroarylamino group, or a heterocyclamino group, where the heteroaryl or heterocyclic moiety is described above in this paragraph, the group MNHS(O), mono- or di(C--Salkyl)aminocarbonyl, C.i-Salkyl-C(O)-C.-C;.alkyl, mono- or di(C.- i-Szalkyl) amino group, mono - or di(C4-C3)alkylamino-C 1-Salkyl, mono- or di(C-4-Salkyl)amino-5(0)", K-C-Salkyl, Ka-C-Salkyloxy group, - - Ka-C(0)-C4-Salkyl, Kio-C4-Salkyl(K.4)M group and carboxy-mono- or di(C4-C) alkyl-amino group, i- - a C.-Salkyl group or a C.i-C,alkyl group, each of which is optionally partially or completely halogenated or optionally substituted by a K.7 group, - OK.v or C.-Salkyl, optionally substituted by a group OKv, - an amino group or a mono- or di(C.4-Svalkyl) amino group, optionally substituted by a Kch9 group, « - Kos(O)(K 21)-, K220-, KazCoaMS(O0)-, KovSNoS(O) М(А21)- or КовС(О)СНоМ(К21)-, - с - С--С.alkenyl, substituted by the Kozko4МС(О)- group, or - C.-C.alkynyl branched or unbranched carbon chain, which is not necessarily partially or;" fully halogenated and optionally independently substituted by 1-2 oxo groups, pyrrolidinyl, pyrrolyl, morpholinyl, piperidinyl, piperazinyl, imidazolyl, phenyl, pyridinyl, tetrazolyl, or one or more C.4-C, alkyl groups, which are optionally substituted by one or by several halogen atoms, and -I Koz and Kod together optionally form an imidazolyl, piperidinyl, morpholinyl, piperazinyl or pyridinyl ring. - 20. The compound according to claim 19, in which Ge) b means phenyl, pyridinyl, pyridonyl, naphthyl, quinolinyl, isoquinolinyl, pyrazinyl, benzothiophenyl, dihydrobenzofuranyl, dihydrobenzothiophenyl, indanyl, indolyl, indolinyl, indolonyl or indolinonyl, while 1 Co is substituted by one or by several groups K., RK" or Kz, Ge Ag means naphthyl, X means phenyl, imidazolyl, pyridinyl, pyrimidinyl, piperidinyl, piperazinyl, pyridazinyl or pyrazinyl, each of which is optionally independently substituted with 1-3 substituents selected from the group , which includes two C1-Slalkyl, a C1-C6-alkyl group, a hydroxy group, a nitrile, an amino group, a mono- or di(C--Salkyl)amino group, a mono- or di(C-Salkylamino)carbonyl, a MNHS(O) group, group C--Svalkyl-5(O) and halogen, F) U means a bond or a saturated C.4-C.-carbon chain, while one of the carbon atoms is optionally replaced by 0, M or 5 , and U is optionally independently substituted by an oxo group, 2 means ω - phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, imidazolyl, dihydro iazolyl, dihydrothiazolyl sulfoxide, pyranyl or pyrrolidinyl, which are optionally substituted with 1-2 C.-Soalkyl groups or C.i-Soalkoxy groups, - tetrahydropyranyl, morpholinyl, thiomorpholinyl, thiomorpholinosulfoxidyl, piperidinyl, piperidinonyl, piperazinyl or tetrahydropyrimidonyl, which are optionally substituted by 1-2 C 4-Soalkyl groups or 65 C1-Coalkoxy groups, or - C-Salkoxy group, Ki in each case independently means - C 43 -C alkyl, which is optionally partially or fully halogenated and optionally substituted with phenyl substituted with 0-3 substituents selected from the group consisting of halogen, C 43 -C alkyl, which is optionally partially or fully halogenated, a hydroxy group, a nitrile, and a C-C 6 -C 600 hydroxy group, which is optionally partially or fully halogenated, - cyclopropyl, cyclobutyl, cyclopentanyl, cyclohexanyl, bicyclopentanyl or bicyclohexanyl, each of which is optionally partially or fully halogenated and optionally substituted 1 -3 substituents selected from the group that includes C 4-C alkyl, which is optionally partially or fully halogenated, the CM group, /o hydroxyC-C alkyl and phenyl, or an analog of cyclopropyl, cyclobutyl, cyclopentanyl, cyclohexanyl, bicyclopentanyl or bicyclohexanyl where one ring methylene group is replaced by 0, or - silyl, which independently contains three C 4-Soalkyl groups, which are not necessarily partially or fully halogenated, E" in ko in each case independently means bromine, chlorine, fluorine, methoxy group, methylsulfonyl or nitrile, Ez in each case independently means - phenyl, morpholino group, pyridinyl, pyrimidinyl, pyrrolidinyl, 2,5-pyrrolidinedionyl, imidazolyl, pyrazolyl, while each of the specified radicals is optionally substituted with 1-3 substituents selected from the group consisting of C1-C6alkyl, which is optionally partially or fully halogenated, halogen, oxo, hydroxy, nitrile and C1-C6alkyloxy, which is optionally partially or fully halogenated, - C.-Szalkyl group or C-Szalkoxy group, which is optionally partially or completely halogenated or optionally substituted by group K.7, - OK.c or C.-Szalkyl group, optionally substituted by group OKv, - amino group or mono- or di(C.4-Salkyl) amino group, optionally substituted by the Kch9 group, - Kos(O)(K 21)-, K220-, KazCoaMS(O0)-, KovSNoC(O)M(A21)- or КовС(О)СНоМ(К21)-, сч - С--С.alkenyl, substituted by the Kozko4МС(О)- group, or - C.-C.alkynyl substituted by pyrrolidinyl or pyrrolyl, and (8) Koz and K24 together optionally form a morpholino group. 21. The compound according to claim 20, in which b means phenyl, pyridinyl, pyridonyl, naphthyl, quinolinyl, isoquinolinyl, dihydrobenzofuranyl, indanyl, c zo indolinyl, indolonyl or indolinonyl, while C is substituted by one or more groups K., K» or Ku , Ag is 1-naphthyl, which) X is phenyl, imidazolyl, pyridinyl, pyrimidinyl, piperidinyl, piperazinyl, pyridazinyl or pyrazinyl, Ge! U means a bond or -CH»o-, -CHNoCH»-, -С(0)-, -О-, -5-, -МН-СНоСНХСН»-, -МЩ(СНе)- or -МН-, Ki in each case independently represents -- - C3-Salkyl, which is optionally partially or fully halogenated and optionally substituted with phenyl, or - cyclopropyl, cyclopentanyl, cyclohexanyl or bicyclopentanyl, optionally substituted with 1-3 substituents selected from the group , which includes methyl, which is optionally partially or fully halogenated, the CM group, hydroxymethyl and phenyl, or 2-tetrahydrofuranyl substituted with methyl, or - trimethylsilyl, "Ez in each case independently means in c - phenyl, morpholinyl, pyridinyl, pyrimidinyl . - C.i-Szalkyl group or C.--Szalkoxy group, each of which is optionally partially or fully halogenated or optionally substituted by a diethylamino group, -I - OK.c or C.-Szalkyl, optionally substituted by a group OKv, - an amino group or a mono- or di(C.4-Salkyl)amino group, optionally substituted by a Kch9 group, - - СН3С(О)МН-, Ко20-, КозК24МС(О)-, КобСНоС(ОМ(К21)- or КовС (O)СНоМ(К21)-, со - С--С.alkenyl, substituted by the Kozko4МС(О)- group, or - C.-C.alkynyl, substituted by pyrrolidinyl or pyrrolyl, where Coz and Cod mean H or Coz and K24 together optionally form a Ge morpholino group and Eov means a morpholino group. 22. The compound according to claim 21, in which b means phenyl, pyridinyl or naphthyl, while C is replaced by one or more groups K., Ko or Kz, (Ф) X means imidazolyl or pyridinyl, and M means -СНо-, -МН -СНСНОСН»- or -МН-, 27 means a morpholino group, 60 Ku in each case independently means tert-butyl, sec-butyl, tert-amyl or phenyl, ER" means chlorine and Kz in each case independently means methyl, methoxy group, methoxymethyl , hydroxypropyl, acetamide, morpholino group or morpholinocarbonyl. 23. The compound according to claim 22, in which X is pyridinyl. 65 24. The compound according to claim 23, in which pyridinyl is attached to Ag in the 3rd position of pyridinyl. 25. Compound of the formula (PP): AG, b. TO oA-X-th ZE as well as H (1) in which E means carbon or a group that contains a heteroatom selected from -O-, -MH- and -5-, o means - aromatic Sv-Siocarbocycle or saturated or an unsaturated non-aromatic C3-C:iocarbocycle, - a 6-14-membered monocyclic, bicyclic or tricyclic heteroaryl, which contains one or more heteroatoms selected from 3O, M and 5, - a 6-8-membered monocyclic heterocycle, which contains one or more heteroatoms selected from zo, Mi5, or an 8-11-membered bicyclic heterocycle containing one or more heteroatoms selected from O, Mi5, while C is optionally substituted by one or more groups K, K »o or Kz, Ag means phenyl, naphthyl, quinolinyl, isoquinolinyl, tetrahydronaphthyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, benzimidazolyl, benzofuranyl, dihydrobenzofuranyl, indolinyl, benzothienyl, dihydrobenzothienyl, indanyl, indenyl or indolyl, each optionally substituted with one or more groups K, or Kv, X means - C5-Cvcycloalkyl or cyclo alkenyl, optionally substituted with 1-2 oxo groups or 1-3 C -C.alkyl, C.i-Slalkoxy- or C.-C.alkylamino chains, each of which is branched or unbranched, c - aryl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, pyridinyl, pyrimidinyl, pyridinonyl, o dihydropyridinonyl, maleimidyl, dihydromaleimidyl, piperidinyl . ralkoxy group, hydroxy group, nitrile, amino group, mono- or di(C4-Salkyl)damino group, mono- or di(C-Salkylamino)carbonyl, MNoC(O) group, C.-Salkyl-3(O)pt group and EM halogen, ю M means a bond or a saturated or unsaturated branched or unbranched C 4-C carbon chain, which is optionally partially or fully halogenated, while one or more C atoms (o) are optionally replaced by O, M or 5(O) t, and U is optionally independently substituted by 1-2 oxo groups, nitrile, "- phenyl or one or more C. and C. alkyl groups rups, which are optionally substituted by one or more halogen atoms, - 2 means aryl, heteroaryl selected from pyridinyl, piperazinyl, pyrimidinyl, pyridazinyl, pyrazinyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, furanyl, thienyl and pyranyl, heterocycle selected from "tetrahydropyrimidonyl, cyclohexanonyl, cyclohexanolyl, 2-oxa- or 2-thia-5-azabicyclo|2.2.1)heptanyl, pentamethylenesulfidyl, pentamethylenesulfoxidyl, pentamethylenesulfonyl, tetramethylenesulfidyl, tetramethylenesulfoxidyl or tetramethylenesulfonyl, tetrahydropyranil, tetrahydrofuranyl, part" 1,3- dioxolanonyl, 1,3-dioxanonyl, 1,4-dioxanyl, morpholino group, thiomorpholino group, "thiomorpholinosulfoxidyl, thiomorpholinosulfonyl, piperidinyl, piperidinonyl, pyrrolidinyl and dioxolanyl, while each of the above 7 groups is optionally substituted with 1-3 substituents selected from the group that includes halogen, C --Svalkyl, C-Svalkoxy group, C.--Szalkoxy-C--Szalkyl, S.i-Svalkoxy rbonyl, - aroyl, C.-Szacyl, oxo group, hydroxy group, pyridinyl-C.-Szalkyl, imidazolyl-C.-Szalkyl, - tetrahydrofuranyl-C.-Szalkyl, nitrile-S.-Szalkyl, nitrile, carboxy group, phenyl, where the phenyl ring optionally substituted by 1-2 halogen atoms, C-Salkyloxy groups, hydroxy groups or mono- or is), di(C-Salkyl)amino groups, C-Salkyl-Z(O)t1 group and phenyl-5(O) group y, where the phenyl ring is optionally substituted with 20 by 1-2 halogen atoms, C.-Chaloxy groups, hydroxy groups or mono- or di(C4i-Salkyl)amino groups, IR) or 7 is optionally substituted by 1-3 amino groups or amino- With i-Salkyl groups, while the M-atom is not necessarily independently mono- or disubstituted aminoC -Salkyl, C.i-Salkyl, arylCo-Salkyl, C-SalkyloxyC 1-Salkyl, C-Salkyl, aroyl, C4- -Szacyl, the group C.4-Salkyl-Z(O)»t- or the group arylCo-Szalkyl-Z(O)n-, while each of the indicated alkyls and aryls attached to the amino group, Ge! optionally substituted by 1-2 halogen atoms, C41-Salkyl groups or C.-Salkyloxy groups, or 7 optionally substituted by 1-3 aryl groups, heterocyclic or heteroaryl groups, which are described above in this paragraph, while each of the specified groups, in turn, is optionally substituted by halogen, C.-Swalkyl or C.-Swalkoxy group, 60 or 7 means a hydroxy group, halogen, nitrile, amino group, where the M atom is not necessarily independently mono- or disubstituted by C.-i-Szacyl, C--Swalkyl or C.-SzalkoxyS .-i-Szalkilom, branched or unbranched C.-Salkyl, C--Salkyloxy, C.i-Szacylamino group, nitrileC.i-C;alkyl, group C.--Salkyl-Z(O)t or group phenyl-B(O),t, where the phenyl ring optionally substituted by 1-2 halogen atoms, C --Salkoxy groups, hydroxy groups or mono- or di(C.4-Salkyl)amino groups, 65 Ki in each case independently means branched or unbranched C.--Siralalkyl, which is optionally partially or fully halogenated, at the same time, one or more C atoms are not necessarily independently replaced by O, M or 5(0O) 1, and the indicated C-Cialkyl is optionally substituted with 1-3 substituents selected from the group consisting of C 3-Ci-ocycloalkyl, hydroxy, oxo, phenyl, naphthyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, pyrrolidinyl, imidazolyl, pyrazolyl . Swacycloalkenyl, hydroxy group, nitrile, C-C-C-alkyloxy group, which is optionally partially or fully halogenated, MH 5C(0) group, mono- or di(C--C-C alkyl)amino group and mono- or di(C-C-C-C alkyl)aminocarbonyl , 70 or Ku means - a cyclopropyloxy group, a cyclobutyloxy group, a cyclopentyloxy group, a cyclohexyloxy group, or a cycloheptyloxy group, each of which is optionally partially or fully halogenated and optionally substituted with 1-3 substituents selected from the group that includes C 4-Salkyl, which is optionally necessarily often valent or fully halogenated, nitrile, hydroxyC--Salkyl and aryl, or an analogue of such a cycloalkyl group in which 1-3 ring methylene groups are independently replaced by OO, 5(O)t, CHOH, 2C-0, 2-5 or MH , - a phenyloxy group or a benzyloxy group, each of which is optionally partially or fully halogenated and optionally substituted with 1-3 substituents selected from the group that includes C 4-Salkyl, which is optionally partially or fully halogenated, nitrile, hydroxyC- - Szalkyl and aryl, or an analogue of such a cycloaryl group, in which 1-2 ring methylene groups are independently replaced by M, - cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, bicyclopentanyl, bicyclohexanyl or bicycloheptanyl, each of which is optional partially or completely halogenated and optionally substituted with 1-3 substituents selected from the group consisting of C 4-C alkyl, which is optionally partially or fully halogenated, nitrile, hydroxyC-C alkyl and aryl, or an analog of such a cycloalkyl group in which 1- 3 rings and methylene groups are independently replaced by ОО, 5(О)т, СНОН, 2С-0, 2-5 or МН, сч - branched or unbranched C3-Siralkenyl, which in each case is optionally partially or fully halogenated and optionally substituted with 1-3 substituents selected from the group that includes i) branched or unbranched C-Svalkyl, phenyl, naphthyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, imidazolyl, pyrazolyl, thienyl, furyl, isoxazolyl and isothiazolyl, while each of said substituents is substituted with 1-5 substituents selected from the group consisting of halogen, C1-alkyl, optionally partially or fully halogenated, cyclopropanyl, cyclobutanyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, bicyclopentanyl, bicyclohexanyl, or bicycloheptanyl , hydroxy group, nitrile, o C.-Salkyloxy group, which is not necessarily partially or fully halogenated, the group MH 2C(O) and mono- or Ge! di(C--Salkylaminocarbonyl, while the specified branched or unbranched /C3-Cyralkenyl is optionally interrupted by one or more heteroatoms selected from 0, M and (OO) t, -- - cyclopentenyl, cyclohexenyl, cyclohexadienyl, cycloheptenyl, cycloheptadienyl, bicyclohexenyl or bicycloheptenyl, while such a cycloalkenyl group is optionally substituted by 1-3 C. and C. alkyl groups, - an oxo group, nitrile, halogen, - silyl, which contains three C. - C. alkyl groups, which are not necessarily partially or fully halogenated, or - C4-Svalkynyl branched or unbranched carbon chain, which is optionally partially or fully halogenated, while one or more methylene groups are optionally replaced by O, MH or sv) with З(О) t, and the indicated alkynyl group is not necessarily independently substituted by 1-2 oxo groups, a hydroxy group, . pyrrolidinyl, pyrrolyl, tetrahydropyranyl, one or more C. and C. alkyl groups, optionally substituted by one or more halogen atoms, nitrile, morpholino group, piperidinyl, piperazinyl, imidazolyl, phenyl, pyridinyl, tetrazolyl, or mono- or di(C.-4-Salkyl)amino group, optionally substituted by one or more halogen atoms, -I EC ", RK. and K5 each means - branched or unbranched C.--Svalkyl, which is not necessarily partially or fully halogenated, - C.-Svacyl, aroyl, branched or unbranched C.i.-C.alkoxy group, which in each case is not necessarily He) partially or fully halogenated, halogen, methoxycarbonyl, group C--Szalkyl-Z(O)»t, which is not necessarily partially or fully halogenated, or a phenyl-Z(O) t, o - Ohm» group, a Si-Sulfoxy group, a hydroxy group, a nitrile, a nitro group, a halogen or He - an amino-5(O),1-, where the M-atom is optionally independently mono- or disubstituted by C--Salkyl or arylCo-Salkyl, or an amino group where the M-atom is optionally independently mono- or disubstituted by C-Salkyl, arylCo-Salkyl, C--Svacyl, group C-Salkyl-(O).1- or group arylCo-Salkyl-Z(O)»y-, while each of the alkyls and aryls specified in this paragraph is optionally partially or fully halogenated and optionally substituted 1 -2 C-Svalky groups or C.-Svaloxy groups, (F, Ez in each case independently means ka - phenyl, naphthyl, morpholino group, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, pyrrolidinyl, imidazolyl, pyrazolyl, thiazolyl, oxazolyl, (|1,3,Sxoxadiazole, triazolyl, tetrazolyl, thienyl, furyl, o tetrahydrofuryl, isoxazolyl, isothiazolyl, quinolinyl, isoquinolinyl, indolyl, benzimidazolyl, benzofuranyl, benzoxazolyl, benzisoxazolyl, benzpyridazolyl, benzothiofuranyl, pterinyl, . or unbranched C-Svalkyl, which is optionally partially or fully halogenated, cyclopropanyl, cyclobutanyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, bicyclopentanyl, bicyclohexanyl, bicycloheptanyl, phenyl-C--Svalkyl, naphthyl-C-Svalkyl, halogen, a hydroxy group, an oxo group, a nitrile, a C 1 -C 6 alkoxy group, which is optionally partially or fully halogenated, a phenyloxy group, a naphthyloxy group, a heteroaryloxy group, or a heterocyclooxy group, wherein the heterocyclic or heteroaryl moiety is described above in this paragraph, a nitro group, an amino group, a mono- or di(C1 -Salkyl)amino group, phenylamino group, naphthylamino group, heteroarylamino group or heterocyclamino group, where the heterocyclic or heteroaryl fragment is described above in this paragraph, the MNHS(O) group, mono- or di(C--Salkyl)iaminocarbonyl, C.-Salkyl-C(0 )-C4-C, alkyl, amino-C.-Salkyl, mono- or di(C.-4-Salkyl) amino group, mono- or di(C.-Salkyl) amino-C4-Salkyl, amino-5 group ( 0)5, group di(Si-Salkyl)lamino-5(0)»5, K.-C.4-Svalkyl, Ka-C--Svalkoxy group, Kea-C(0)-C.4-Svalkyl, group Kio-C4-Svalkyl(K44)M and carboxy-mono-or 7/0. В(С4-Свалкіл)аміногрупу, - кКонденсований арил, вибраний з бензоциклобутанілу, інданілу, інденілу, дигідронафтилу, тетрагідронафтилу, бензоциклогептанілу і бензоциклогептенілу, або конденсований гетероарил, вибраний з циклопентенопіридинілу, циклогексанопіридинілу, циклопентанопіримідинілу, циклогексанопіримідинілу, циклопентанопіразинілу, циклогексанопіразинілу, циклопентанопіридазинілу, циклогексанопіридазинілу, /5 циклопентанохінолінілу, циклогексанохінолінілу, циклопентаноізохінолінілу, циклогексаноізохінолінілу, циклопентаноіндолілу, циклогексаноіндолілу, циклопентанобензімідазолілу, циклогексанобензімідазолілу, циклопентанобензоксазолілу, циклогексанобензоксазолілу, циклопентаноімідазолілу, циклогексаноімідазолілу, циклопентанотієнілу і циклогексанотієнілу, при цьому вказане конденсоване арильне або конденсоване гетероарильне кільце незалежно заміщено 0-3 замісниками, вибраними з групи, which includes phenyl, naphthyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, imidazolyl , pyrazolyl, thienyl, furyl, isoxazolyl, isothiazolyl, C.-Svalkyl, which is optionally partially or fully halogenated, halogen, nitrile, C-C alkyloxy group, which is optionally partially or fully halogenated, phenyloxy group, naphthyloxy group, heteroaryloxy group or heterocyclooxy group, where the heteroaryl or heterocyclic moiety is described above in this paragraph, nitro group, amino group, mono- or di(C 1-C alkyl)amino group, a phenylamino group, a naphthylamino group, a heteroarylamino group or a heterocyclamino group, where the heteroaryl or heterocyclic fragment is described above in this paragraph, the MNHS(O) group, mono- or di(C.i-Salkyl)aminocarbonyl, the C.-C;alkyl-OC( Oh), and) C.i-Salkyl-C(0)-Ci-Slalkyl, amino-C--Salkyl, mono- or di(C.-4-C3)alkylamino-C.4-Salkyl, K412-C4-Salkyl, K/ 3-C4-Svalkoxy group, K414-C(0)-C.4-Svalkyl and the group Kiv-C4-Svalkyl(K4v)M, - cyclopropanil, cyclobutanil, cyclopentanil, cyclohexanyl, cycloheptanil, bicyclopentanil, c bicyclohexanil or bicycloheptanil, each of which is optionally partially or fully halogenated and optionally substituted with 1-3 C-C alkyl groups, or an analogue of such a cycloalkyl group, in which the 1-3 ring methylene groups are independently replaced by 0.5, CHOH, 2C-0.2 -5 or MN, Gee! - cyclopentenyl, cyclohexenyl, cyclohexadienyl, cycloheptenyl, cycloheptadienyl, bicyclohexenyl or bicycloheptenyl, each of which is optionally substituted with 1-3 C.-Salkyl groups, -- - C4-C.alkylphenyl-C(0)-C4-Salkyl-, C4-C; alkyl-C(O)-C.-C; alkyl- or C4-C, alkylphenyl-5(O) t-C4-Sualkyl-, i- - C.-Svalkyl group or branched or unbranched C-Svalkoxy group, each of which is optionally partially or fully halogenated or optionally substituted by group K.7, - OK.v or C.-Svalkyl, optionally substituted by group OKv , - an amino group or a mono- or di(C.4-Salkyl)amino group, optionally substituted by a Kch9 group, « - Koob(O)MZh(K»21)-, Ko20-, KozKo4MO(O)-, Kob(СНо )pC(O)MZh(K»21)-, Koza MC(O0)-S.-Czalkoxy group or with KovS(OHCHN)t(Kat)-Y . - So--Svalkenil, replaced by the KozKodMS(O)- group, and?" - S.-Alkynyl branched or unbranched carbon chain, which is optionally partially or fully halogenated, while one or more methylene groups are optionally replaced by 0, МН, З(О)т and the indicated alkynyl group is optionally independently substituted 1-2 oxo groups, pyrrolidinyl, -I pyrrolyl, morpholino group, piperidinyl, piperazinyl, imidazolyl, phenyl, pyridinyl, tetrazolyl, one or more C. and C. alkyl groups, which are optionally substituted by one or more atoms - halogen, nitrile , morpholino group, piperidinyl, piperazinyl, imidazolyl, phenyl, pyridinyl, Ge) tetrazolyl or mono- or di(Ci-C.alkylamino group, optionally substituted by one or more 50p halogen atoms, o - Si--Svacyl or aroyl, From Kv means C.-C.alkyl, which is optionally partially or fully halogenated and optionally substituted by the group Kev, k,, EB, Ko, Ko, EK", Kz, EK, GE, Ku", Kv, ov and Kov each independently means nitrile, phenyl, m an orfolino group, piperidinyl, piperazinyl, imidazolyl, pyridinyl, tetrazolyl, an amino group, or a mono- or di(C.--C, alkyl)amino group, which is optionally partially or fully (F, halogenated, Ka Ku and Kv each independently of one another means hydrogen or C.-C.alkyl, which is optionally partially or fully halogenated, in Kv in each case independently means hydrogen or C.-C.alkyl, which is optionally independently substituted by an oxo group or a Kov, Koo group in each case independently means C.-C-alkyl, which is optionally partially or fully halogenated, phenyl or pyridinyl, C2i in each case independently means hydrogen or C.4-C.alkyl, which is optionally partially or fully 65 halogenated, Co», Coz and Code each independently of each other means hydrogen, S.i-Svalkil, which is not necessarily partially or fully halogenated, while the indicated C 4-Salkyl is optionally interrupted by one or more o, M or 5 atoms, and is also independently optionally substituted by mono- or di(C-Salkyl)aminocarbonyl, phenyl , pyridinyl, an amino group or a mono- or di(C-C alkyl)amino group, and each of the specified radicals is optionally partially or fully halogenated and optionally substituted with a mono- or di(C-C alkyl)amino group, or Koz and Cod together optionally form a heterocyclic or heteroaryl ring, t means 0, 1 or 2, 70 M/ means O or 5, and pharmaceutically acceptable derivatives thereof. 26. The compound according to claim 25, in which E means -CH»o-, -MH- or -O-, M means O and o means - phenyl, naphthyl, benzocyclobutanyl, dihydronaphthyl, tetrahydronaphthyl, benzocycloheptanyl, benzocycloheptenyl, indanyl, indenyl, - pyridinyl, pyridonyl, quinolinyl, dihydroquinolinyl, tetrahydroquinoyl, isoquinolinyl, tetrahydroisoquinoyl, pyridazinyl, pyrimidinyl, pyrazinyl, benzimidazolyl, benzthiazolyl, benzooxazolyl, benzofuranyl, benzothiophenyl, benzpyrazolyl, dihydrobenzofuranyl, dibenzofuranyl, dihydrobenzothiophenyl, oxazolone-3 ) tetrahydrothiophenyl, piperidinyl, piperazinyl, morpholino, tetrahydropyranyl, dioxanil, tetramethylenesulfonyl, tetramethylenesulfoxidyl, oxazolinyl, 3,4-dihydro-2H-benzo|1,oxazinyl, thiazolinyl, imidazolinyl, tetrahydropyridinyl, homopipe eridinyl, pyrrolinyl, tetrahydropyrimidinyl, decahydroquinolinyl, decahydroisoquinolinyl, thiomorpholino group, thiazolidinyl, (8) dihydrooxazinyl, dihydropyranyl, oxocanyl, heptacanyl, thioxanyl or dithianyl, while C is optionally substituted by one or more groups K., K»o or Kz. 27. The compound according to claim 26, in which c zo E means -MH-, b means phenyl, pyridinyl, pyridonyl, naphthyl, quinolinyl, isoquinolinyl, pyrazinyl, benzimidazolyl, which) benzooxazolyl, benzooxazolonyl, benzofuranyl, benzothiophenyl, benzopyrazolyl, dihydrobenzofuranyl, ( from dihydrobenzothiophenyl, 3,4-dihydro-2H-benzo|1,Shoxazinyl, indanyl, indenyl, indolyl, indolinyl, indolonyl, 2,3-dihydro-1H-indolyl or indolinonyl, while optionally substituted by one or more groups -- , Bo or r, rch- Ag means naphthyl, quinolinyl, isoquinolinyl, tetrahydronaphthyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, indanyl, indenyl or indolyl, each of which is optionally substituted by one or more groups K, or Kv, X means phenyl, furanyl , thienyl, pyrrolyl, pyrazolyl, imidazolyl, pyridinyl, pyrimidinyl, pyridinonyl, "dihydropyridinonyl, maleimidyl, dihydromaleimidyl, piperidinyl, piperazinyl, pyridazinyl or pyrazinyl, pt"), each of which is optionally independently substituted with 1-3 substituents selected from group that includes . C-C alkyl, C-C alkyl, hydroxy group, nitrile, amino group, mono- or di(C-4-C alkyl) amino group, mono- or di(C--Salkylamino)carbonyl, MNHS(O) group, C--Salkyl-5(O) group and halogen, U means a bond or a saturated or unsaturated C.-C.-carbon chain, where one or several C atoms are optionally replaced by O, M or 5(O) t, and U is optionally independently substituted by 1-2 oxo groups, nitrile, -I phenyl or one or more C.i.C.alkyl groups, optionally necessarily substituted by one or more halogen atoms, - 27 means He) phenyl, heteroaryl selected from pyridinyl, piperazinyl, pyrimidinyl, pyridazinyl, pyrazinyl, 5o imidazolyl, furanyl, thienyl and pyranyl, heterocycle selected from 2-oxa-5-azabicyclo |2.2.1|heptanyl, o tetrahydropyrimidonyl, pentamethylene sulfidyl, pentamethylene sulfoxidyl, pentamethylene sulfonyl, He tetramethylene sulfidyl, tetramethylene sulfoxidyl, tetramethylene sulfonyl, tetrahydropyranyl, tetrahydrofuranyl, 1,3-dioxolanonyl, 1,3-dioxanonyl, 1,4-dioxanyl, morpholino group, thiomorphol oxide, thiomorphol , piperidinyl, piperidinonyl , dihydrothiazolyl, dihydrothiazolylsulfoxidyl, dipyrrolidinyl, and dioxolanyl, each of which is optionally substituted with 1-3 substituents selected from the group consisting of nitrile, C.4-Salkyl, C.sub.6-Salkoxy, amino, mono- or di(C-- C alkyl)amino group, the group COMNH" and F) the group OH, ka or 7 is optionally substituted with phenyl, heterocycle or heteroaryl as defined above in this paragraph, each of which in turn is optionally substituted with halogen, C4-C alkyl or C.-Salkyloxy group, vo or 7 means nitrile, nitrileC.--Salkyl, group C.--Salkyl-Z(O)»t, halogen, hydroxy group, C.-Salkyl, C.-Szacylamino group, C.-C.-alkyl group, amino group, mono- or di(C--Salkyl)aminocarbonyl or amino group, mono- or disubstituted amino-C--Salkyl or C.-Szaloxy-C.--Salkyl, Ki y in each case independently means - branched or unbranched C.--Svalkyl, which is not necessarily partially or completely halogenated, 65 while one or more C atoms are not necessarily independently replaced by O, M or 5(0O) t, and the indicated C-Salkyl is optionally substituted with 1-3 substituents selected from the group consisting of C 3-Seccycloalkyl, an oxo group, phenyl, dioxolanyl, pyrrolidinyl, furyl, isoxazolyl or isothiazolyl, each of which is optionally substituted with 1-3 substituents selected from the group consisting of halogen, C 1 -Salkyl, which is optionally partially or fully halogenated, hydroxy, a nitrile and a C-Salkoxy group, which is optionally partially or fully halogenated, - cyclopropyl, cyclobutyl, cyclopentanyl, cyclohexanyl, bicyclopentanyl or bicyclohexanyl, each of which is optionally partially or fully halogenated and optionally substituted with 1-3 C 4-Salkyl groups, which are not necessarily partially or fully halogenated, nitrile, hydroxyC i-Salkyl or phenyl, or an analogue of such a cycloalkyl group, in which 1-3 ring methylene groups are independently replaced by o, 5, 7/0 CHOH, »С-0 , 0-5 or MH, - an oxo group, - C4-Svalkynyl branched or unbranched carbon chain, which is optionally partially or fully halogenated, while one or more methylene groups are optionally replaced by O, МН or 5З(О)т, and the indicated alkynyl group is optionally independently substituted by 1-2 oxo groups, a hydroxy group, pyrrolidinyl, pyrrolyl, tetrahydropyranyl, C.i.C.alkyl, which is optionally substituted by one or more halogen atoms, nitrile , a morpholino group, piperidinyl, piperazinyl, imidazolyl, phenyl, pyridinyl, tetrazolyl, or a mono- or di(C.-i-Salkyl)uamino group, which is optionally substituted by one or more halogen atoms, or - silyl, which contains three C.- C, alkyl groups, which are not necessarily partially or fully halogenated, E" in each case independently means - branched or unbranched C.--Svalkyl, which is not necessarily partially or fully halogenated, acetyl, aroyl, branched or unbranched C. and -C.alkyloxy group, which in each case is not necessarily partially or fully halogenated, halogen, methoxycarbonyl, the C.--Soalkyl-3(O)»t group, which is not necessarily partially or fully halogenated, or the phenyl-3( O) t, sch - Si-Szalkoxygroup, hydro xy group, nitrile, nitro group, halogen or - amino-5(O),1- group, where the M-atom is not necessarily independently mono- or di-substituted by C--Salkyl or i) arylCo-Salkyl, or an amino group where the M-atom optionally independently mono- or disubstituted by C 1 -C alkyl, arylC 1 -C alkyl, C 1 -C acyl, C 1 -C 4 -alkyl-(O)1- group or arylCo -C 3 alkyl-C(O)»y- group , while each of the alkyls and aryls specified in this paragraph is not necessarily partially or fully halogenated and zo is optionally substituted by 1-2 C. and C. - C. alkyl groups or C. - C. - alkyloxy groups, Ez in each case independently means yu - phenyl , morpholino group, pyridinyl, pyrimidinyl, pyrazinyl, pyrrolyl, pyrrolidinyl, imidazolyl, Ge! 1,3,Shoxadiazole, pyrazolyl, each of which is optionally substituted with 1-3 substituents selected from the group consisting of phenyl, naphthyl, heterocycle or heteroaryl as described above in this paragraph, C -alkyl, which is necessarily partially or fully halogenated, cyclopropanyl, cyclobutanyl, cyclopentanyl, cyclohexanyl, cycloheptanyl, bicyclopentanyl, bicyclohexanyl, bicycloheptanyl, phenyl-C.-Salkyl, naphthyl-C.-Salkyl, halogen, oxo group, hydroxy group, nitrile, C-Salkyloxy group, which is optionally partially or fully halogenated, a phenyloxy group, a naphthyloxy group, a heteroaryloxy group, or a heterocyclooxy group, where the heteroaryl or heterocyclic moiety is described above in this paragraph, a nitro group, an amino group, a mono- or di(C4i-C6alkyl)amino group, a phenylamino group, a naphthylamino group, a heteroarylamino group, or C is a heterocyclamino group, where the heteroaryl or heterocyclic fragment is described above in this paragraph, the group is МНоС(О), mMono- or di(C4-Salkyl)aminocarbonyl, C.4-Salkyl-C(0 )-S.-Su,alkyl, mMo- or y?" di(C4-Salkyl)amino group, MOono- or di(C4i-C3)alkylamino-C.-Salkyl, group MOono- or di(Ci-Salkyl)amino-5(O)", K-C4-Salkyl, Ka- C4-Salkyloxy group, Ke-C(0)-C4-Salkyl, K/o-C41-Salkyl(K44)M 1 carboxy-mono- or di(C4-C)-alkylamino group, -I - C.-Salkyl group or a C.i-C.alkoxy group, each of which is optionally partially or fully halogenated or optionally substituted by a group K.7, - - OK.v or C.-Svalkyl, optionally substituted by a group OKv, Ge) - an amino group or a mono- or di(C.4-Salkyl)amino group, optionally substituted by a Kch9 group, - Koos(O)M(Koya4)-, Kogo-, Kozk2AMS(O)-, KovSNoSO)M(Koya4)-, Kozk2АМС(О)-С4-Sialkoxygroup or n BovС(О)СНо МВ) -, Ge - С.-С.alkenyl, substituted by the group KozКо4МС(О)-, - C.-C.alkynyl branched or unbranched carbon chain, which is optionally partially or fully halogenated, while one of the methylene groups is optionally replaced by 0, and optionally substituted by 1-2 oxo groups, pyrrolidinyl, pyrrolyl , a morpholino group, piperidinyl, piperazinyl, imidazolyl, phenyl, pyridinyl, tetrazolyl or one or more C.i.C.; The code together optionally forms an imidazolyl, piperidinyl, morpholine, piperazinyl or pyridinyl ring. 28. The compound according to claim 27, in which o is phenyl, pyridinyl, pyridonyl, naphthyl, quinolinyl, isoquinolinyl, pyrazinyl, 3,4-dihydro-2H-benzo|1, coxazinyl, benzothiophenyl, dihydrobenzofuranyl, dihydrobenzothiophenyl, benzoxazolyl, indanyl, indolyl , indolinyl, indolonyl or indolinonyl, while C is optionally substituted by one or more Ku, K»o or Kz groups, Ag means naphthyl, X is phenyl, imidazolyl, pyridinyl, pyrimidinyl, piperidinyl, piperazinyl, pyridazinyl or pyrazinyl, each of which is optionally independently substituted with 1-3 substituents selected from the group consisting of C.-Alkyl, C-C; alkoxy group, hydroxy group, nitrile, amino group, mono- or di(C-4-C alkyl)amino group, mono- or di(C-C alkylamino)carbonyl, MNHS(O) group, C group -- Svalkyl-5(O) t and halogen, U means a bond or a saturated C.-C.-carbon chain, where one or more C-atoms are optionally replaced by 0, M or 5, and U is optional optionally independently substituted with a nitrile or oxo group, 27 means phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, imidazolyl, dihydrothiazolyl, dihydrothiazolyl sulfoxide, pyranyl, pyrrolidinyl, phenylpiperazinyl, tetrahydropyranyl, tetrahydrofuranyl, 7/o dioxolanyl, 2-oxa-5-azabicyclo|2.2. 1) heptanyl, morpholino group, thiomorpholino group, thiomorpholinosulfoxidyl, piperidinyl, piperidinonyl, piperazinyl or tetrahydropyrimidonyl, each of which is optionally substituted 1-2 C.-Soalkyl groups or C.-Soalkyl groups, or 2 means a hydroxy group, C.i-Salkyl, C.--Szalkoxy group, C.--Szacylamino group, C.i-Salkylsulfonyl, nitrile-C.4-Salkyl or an amino group, mono- or disubstituted C.--SzalkoxyC.4-Salkyl, Ki in each case independently means - branched or unbranched C.--Salkyl, which is optionally partially or fully halogenated, while one or more C-atoms are optional independently replaced by O, M or 5(0O) 1, and indicated C-Salkyl is optionally substituted with oxo, dioxolanyl, pyrrolidinyl, furyl, or phenyl, each of which is optionally substituted with 1-3 substituents selected from the group consisting of halogen, C 4-Salkyl, which is optionally partially or fully halogenated, a hydroxy group, a nitrile, and a C 4-Salkoxy group, which is optionally partially or fully halogenated, - cyclopropyl, cyclobutyl, cyclopentanyl, cyclohexanyl, bicyclopentanyl or bicyclohexanyl, each of which is optionally partially or fully halogenated and optionally substituted with 1- 3 C 4-C alkyl groups, which are optionally partially or fully halogenated, nitrile, hydroxyC 1-C alkyl, or phenyl, or an analog of cyclopropyl, cyclobutyl, cyclopentanyl, cyclohexanyl, bicyclopentanyl, or bicyclohexanyl, in which one ring methylene group is replaced by o , i) - an oxo group, - Co-C.alkynyl, which is optionally partially or completely halogenated, while one or more methylene groups are optionally replaced by n and OO, and optionally independently substituted by 1-2 oxo groups, with zo a hypohydroxy group, pyrrolidinyl, pyrrolyl, tetrahydropyranyl, C.-sualalkyl, which is optionally substituted by one or more halogen atoms, nitrile, morpholino group, piperidinyl, piperazinyl, which) imidazolyl, phenyl, pyridinyl, tetrazolyl or mono- or di(C.i-Szalkyl) amino group, which is not necessarily Ge! substituted by one or more halogen atoms, or - silyl, which contains three C.--Soalkyl groups, which are not necessarily partially or fully halogenated, -- Ko in each case independently means C.i.-C,alkyl, which is not necessarily partially or fully halogenated, C1-Slalkoxy group, which is optionally partially or fully halogenated, bromine, chlorine, fluorine, methoxycarbonyl, methyl-3(O)" or ethyl-5(O)" group, each of which optionally partially or fully halogenated, or a phenyl-Z(O)t group, or Ko means a mono- or di-Szacylamino group, an amino-(O)t group or (0) p-amino group, where the M atom is mono- " or disubstituted by C-Szalkyl or phenyl, nitrile, nitro group or amino group, in c Ez in each case independently means . - phenyl, morpholino group, pyridinyl, pyrimidinyl, pyrrolidinyl, 2,5-pyrrolidinedionyl, imidazolyl, and? 1,3,Shoxadiazole, pyrazolyl, each of which is optionally substituted with 1-3 substituents selected from the group consisting of C-Salkyl, which is optionally partially or fully halogenated, halogen, oxo, hypohydroxy, nitrile and C.- C-Salkoxy group, which is optionally partially or completely halogenated, -I - C.-Szalkyl group or C-Szalkoxy group, which is optionally partially or completely halogenated or optionally substituted by group K.7, - - OK.v or C. - Szalkyl, optionally substituted by the group OKv, He) - amino group or mono- or di(C.4-Szalkyl) amino group, optionally substituted by the group Kch9, - KoosS(OM(Koch)-, Kkogo-, KozkKoaMO(O )-, РовСНоС(ОМ(Коая4)-, МНЖС(О)methoxy group or КовС(О)СНоМ(Ко)-, о - С.-С. .alkynyl substituted by pyrrolidinyl or pyrrolyl, or - C-Zacyl and Coz and Cod together optionally form a morpholino group. 5B 29. A compound according to claim 28, in which b means phenyl, pyridinyl, pyridonyl, 2-naphthyl, quinolinyl, isoquinolinyl, dihydrobenzof uranyl, indanyl, (F) 5B-indolyl, 3Z-oxo-3,4-dihydro-2H-benzo|1,Zoxazin-8-yl, benzooxalolyl, 2,3-dihydrobenzooxazol-7-yl, ka 2-oxo- 2,3-dihydro-1H-indol-b-yl, indolinyl, indolonyl or indolinonyl, while b is optionally substituted by one or more groups K., K» or Kz, where Ag means 1-naphthyl, X means phenyl, imidazolyl, pyridinyl, pyrimidinyl, piperidinyl, piperazinyl, pyridazinyl or pyrazinyl, U means a bond or -CH»-, -CHNoCH»-, -C(0)-, -O-, -5-, -MUN-СНХСНХ» -, -МЩ(СНаз)-, СНАСМ)СНо-МН-СНо or -МН-, 7 means a morpholino group, dioxolanil, tetrahydrofuranil, pyridinyl, 2-oxa-5-azabicyclo|2.2.1)heptanil, 65 S.i- Szalkoxyphenylpiperazinyl, hydroxy group, S.-Szalkyl, M, M-dis--Szalkoxy-S.-Szalkylamino group, C.-Szacylamino group, C-Szalkylsulfonyl or nitrilos.-Szalkyl, Ki in each case independently means - C-Svalkyl, which is optionally partially or fully halogenated, while one or more C-atoms are optionally independently replaced by O or M, and the specified C.-Svalkyl is optionally substituted by an oxo group, dioxolanil, pyrrolidinyl, furyl or phenyl, optionally substituted by a C.-Salkoxy group, - cyclopropyl, cyclopentanyl, cyclohexanyl and bicyclopentanyl, optionally substituted by 1-3 methyl groups, which are optionally partially or fully halogenated, nitrile, hydroxymethyl or phenyl . - amino group, where the M-atom is mono- or disubstituted by C--C alkyl or phenyl, bromine, chlorine, fluorine, nitrile, nitro group, amino group, methylsulfonyl, which is optionally partially or fully halogenated, or phenylsulfonyl, Ez in each case not independently means - phenyl, morpholino group, pyridinyl, pyrimidinyl, pyrrolidinyl, 2,5-pyrrolidinyldionyl, imidazolyl, 1,3,Shoxadiazole or pyrazolyl, each of which is optionally substituted with C 4-Soalkyl, which is optionally partially or fully halogenated, - C.-Szalkyl group or C.i-Szalkoxy group, each of which is optionally partially or completely halogenated or optionally substituted by a diethylamino group, - OK.c or C.-Szalkyl, optionally substituted by a group OKv, - an amino group or a mono- or di(C.4-Salkyl) amino group, optionally substituted by a Kch9 group, - snNUFfomMnH-, Eogo-, KozKoMO(O)-, RovSNoS(OMKa34)-, MNHS(O)methoxy group or KovS(O)СНо M (Co), - C--C.alkenyl, substituted by the group Kozko4MS(O)-, or - C.-C.alkynyl, substituted by pyrrolidinyl or pyrrolyl, ch - C4-Soacyl; and Koz and Kod mean H or Koz and K24 together optionally form i) a morpholino group and Eov means a morpholino group. 30. The compound according to claim 29, in which c or b means phenyl, pyridinyl, 5-indolyl, 3-oxo-3,4-dihydro-2H-benzo|1,Coxazin-8-yl, benzooxalolyl, 2,3-dihydrobenzooxazole -7-yl, 2-oxo-2,3-dihydro-1H-indol-b-yl or 2-naphthyl, while (it is not necessary that) substituted by one or more groups K., K»o or Kz, b X means imidazolyl, pyridinyl, pyrimidinyl or pyrazinyl, Y means a bond, СНА«(СМ)СНо-МН-СН», -СНо-, -«МН-СНоСНХБСН»- or -МН-, -- 7 means morpholine -4-yl, dioxolan-2-yl, tetrahydrofuranyl, pyridinyl, y-2-oxa-5-azabicyclo|2.2.1|hept-5-yl, methoxyphenylpiperazinyl, hydroxy group, methyl, M,M-dimethoxyethylamino group, acetylamino group, methylsulfonyl or cyanoethyl, K in each case independently means tert-butyl, sec-butyl, tert-amyl, phenyl, tetrahydropyran-2-yloxypropynyl, hydroxypropynyl, trihalomethyl, 2,2-diethylpropionyl or cyclohexanyl, " Ko means chlorine, nitro, amino, nitrile, methylsulfonylamino group, diacetylamino group, stv) with phenylsulfonylamino group, M,M-di(meth ylsulfonyl)amino group, methylsulfonyl or trihalomethylsulfonyl, and Kz in each case independently means methyl, C1-C6alkoxy group, methoxymethyl, hydroxypropyl, and? dimethylamino group, C.4-C; alkylamino group, MNoC(O)methoxy group, acetyl, pyrrolidinyl, imidazolyl, pyrazolyl, morpholino group or morpholinocarbonyl. 31. The compound according to item 30, in which X is pyridinyl. -I 32. The compound according to claim 31, in which pyridinyl is attached to Ag in the 3rd position of pyridinyl. 33. The compound according to claim 1, selected from the group that includes: - 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-I(4-(4-(morpholine -4-yl-methyl)phenyl)naphthalen-1-yl|Urea, Ge) 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(4 -(-2-(morpholin-4-yl)ethyl)phenyl)naphthalen-1-yl|Urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3- I(4-(3-(morpholin-4-yl-methyl)phenyl)naphthalen-1-yl|Urea, o 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl| -3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, Ge 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl) |-3-(4-(5-morpholin-4-ylmethylpyridin-2-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl) |-3-(4-(5-morpholin-4-ylmethylfur-2-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H -pyrazol-3-ylI-3-I4-(6b-morpholin-4-ylmethylpyridin-3-yl)naphthalene-1 diylurea, 1-(b-tert-butyl-2-methyl-2H-pyrazol-3-yl |-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|)urea, F) 1-(b-tert-butyl-2-p-tolyl-2H-pyrazole-3 -ylI|-3-I(4-(5-(morpholin-4-ylmethyl) pyridin-2-yl)naphthalen-1-yl)urea, ka 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylI|-3-I(4-(6--« morpholin-4-ylmethyl)pyridin-3-yl)naphthalen-1-yl)urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-yl)- 3-I4-(3-(2-(pyridin-2-yl)ethylamino)cyclohexenyl)bonaphthalen-1-yl)urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazole-3 -yl|-3-I(4-(4-(pyridin-3-ylmethylaminomethyl)phenyl)naphthalen-1-yl|urea NU, 1-(b-tert-butyl-2-(b-methyl-pyridin-3 -yl)-2H-pyrazol-3-ylI-3-I(4-(4-(morpholin-4-yl-methyl)phenyl)naphthalen-1-yl urea, 65 1-Ib-tert-butyl-2- (b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I(4-(6-(4-hydroxybutylamino)pyridin-3-yl)naphthalin-1-yl|urea, 1-(b-tert-butyl-2-(4-methyl-3-carbamylphenyl)-2H-pyrazol-3-ylI-3-I4-(6-"morpholin-4-ylmethyl)pyridin-3-yl)unapht alin-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I(4-(4-(3-hydroxypiperidine -1-ylmethyl)phenyl)naphthalin-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I(4 -(4-(4-Hydroxymorpholin-4-ylmethyl)phenyl)naphthalene-1-yl)urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3 -ylI-3-I4-(3-"morpholin-4-ylmethyl)cyclohexenyl)naphthalene-1-yl|urea, 70 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)- 2H-pyrazol-3-ylI-3-I4-(4-(tetrahydrofuran-3-ylmethyl)-3-hydroxyphen yl)unanaphthalen-1-yl|Urea, 1-(b-tert-butyl-2-(b- methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(4-(M,M-di(2-methoxyethyl)aminomethyl)phenyl)na phthalin-1-yl|urea, 1-(b -tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(6-(3-cyanopropoxy)pyridin-3-yl)naphthalene-1-7/5 yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-(4-(4-morpholin-4-ylmethylpiperidinyl)naphth alin-1-yl|Urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I(4-(4-(M,M -di(2-cyanoethyl)aminomethyl)phenyl)naphthalin-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3 -I4-(4-(furan-2-ylmethyl)-3-hydroxyphenyl)naphthalene-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H- pyrazol-3-ylI-3-I4-(4-(thiomorpholin-4-ylmethyl)phenyl)naphthalene-1-lysine, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)- 2H-pyrazol-3-ylI-3-I4-(4-(3-carboxamidopiperidin-1-ylmethyl)phenyl) naphthalene-1-yl)urea, 1-(b-tert-butyl-2-(b- methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(4--2-methyl-3-oxopiperazin-1-ylmethyl)phenyl) and) naphthalene-1-yl|urea, 1-( b-tert-butyl-2-(2-methylpyrimidin-5-yl)-2H-pyrazol-3-yl|-3-(4-(6--«morpholin-4-ylmethyl)pyridin-3-yl)unaphthal yn-1-yl|urea, c zo 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I(4-(6-(4 -hydroxybutyloxy)pyridin-3-yl)naphthalene n-1-yl|Urea, o 1-(3-tert-butyl-1 H-/1,4bipyrazol-5-ylI|-3-I(4-(6- -"morpholin-4-ylmethyl)pyr idyn-3-yl)naphthalene-1-yl)urea, Ge! 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-yl)-3-I4-(b-(tetrahydrothiopyran-4-ylamino)pyridin-3-yl) )naphthalen-1-yl|urea, -- 1-(b-tert-butyl-2-(2-cyanoethyl)-2H-pyrazol-3-ylI|-3-I(4-(6--"morpholine- 4-ylmethyl)pyridin-3-yl)naphthalen-1-yl)urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI- 3-I4-(6-(-2,6-dimethylmorpholin-4-ylmethyl)pyridin-3-yl)unaphthalin-1-yl|Urea, 1-(b-tert-butyl-2-(2-methoxypyridin-5 -yl)-2H-pyrazol-3-yl|-3-(4-(6--"morpholin-4-ylmethyl)pyridin-3-yl)unaphthal" In-1-yl|urea, with c 1-( b-tert-butyl-2-(2-aminopyridin-5-yl)-2H-pyrazol-3-ylI|-3-I4-(6-(morpholin-4-ylmethyl)pyridin-3-yl)naphthalene-1 -yl)urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(6-(morpholin-4-yl- 4-carbonyl)pyridin-3-yl)na phthalin-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3- I(4-(6-(2-oxa-5-azabicyclo|2.2.1)hept-b--ylmethyl-I)pyridin-3-yl)unaphtalin-1-yl|Urea, 1-(b-tert- butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I( 4-(4-(M-(2-cyanoethyl)-M-(pyridin-3-ylmethyl)aminomethyl)phenyl)naphthalen-1-yl|urea, Ge) 1-(b-tert-butyl-2- (b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-(4-(4-(M-(2-cyanoethyl)-M-(tetrahydrofuran-2-yl)ethyl)aminomethyl)phenyl) naphthalene-1-yl|urea, o 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(6-(morpholine-4- ylmethyl)-4-methoxypyridin-3-yl hel)naphthalene-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI- 3-I4-(6-(1-morpholin-4-lpropyl)pyridin-3-yl)unaphthalin-1-yl|urea, 1-III-tert-butyl-1"-methyl-1H-(/1 ,4Dbipyrazol-5-yl|-3-I(4-(6--«morpholin-4-ylmethyl)pyridin-3-yl)naphthalen-1-yl)urea, F) 1-(b-tert-butyl- 2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I(4-(6-(1-oxo-tetrahydrothiopyran-4-ylamino)pyrikadin-3-yl)naphthalene- 1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4-(6-(tetrahydropyran-4-ylamino)pyridine -3-yl)nbo aphthalin-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I(4- (5-(tetrahydrothiopyran-4- ylamino)pyrazin-2-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(b-methylpyridin-3-yl)-2H-pyrazol-3-ylI-3-I4- (6-(methylcarbonylamino)pyridin-3-yl)naphthalene-1-yl)urea, 65 1-3-tert-butyl-1-(3-methylsulfanylpropyl)-1'H-/1,4bipyrazol-5-yl 3-I4-(6-(morpholin-4-ylmethyl)pyridin-3-yl)unaphtalin-1-yl|urea, 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)-2H-pyrazol-3-yl1|-3-(4-(6-(1-oxothiomorpholin-4-ylmethyl)pyridin-3 - yl)unaphtalin-1-yl|Urea, 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)-2H-pyrazol-3-ylI|-3-(4-(6-( tetrahydropyran-4-ylamino)pyridin-3-yl)naphthalen-1-yl)urea, 1-(b-tert-butyl-2-(2-methylthiopyrimidin-5-yl)-2H-pyrazol-3-yl|- 3-I(4-(6--"morpholin-4-ylmethyl)pyridin-3-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-2-(2-aminopyrimidin-5- yl)-2H-pyrazol-3-ylI-3-I4-(6-"morpholin-4-ylmethyl)pyridin-3-yl)naphthalin-1-yl|urea, 70 1-(3-tert-butyl- 1"-methyl-1' H-(1,4Dbipyrazol-5-yl|-3-I4-(6--"morpholin-4-ylmethyl)phenyl)naphthalen-1-yl|urea, 1-(b-tert -butyl-2-p-tolyl-2H-pyrazol-3-ylI-3-(4-(6-(1-oxotetrahydrothiopyran-4-ylamino)pyridin-3-yl)naphthalin-1-yl|urea, 1 -(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(6-(thiomorpholin-4-ylmethyl)pyridin-3-yl)naphthalen-1-yl| urea, 1-(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-I(4-(2-(morpholin-4-ylcarbonyl)pyrimidin-5-yl)naphthalene- 1-il|Sec /5 VINU, 1-(b-tre t-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-I(4-(2-(morpholin-4-ylmethyl)pyrimidin-5-yl)naphthalen-1-yl|Urea, 1 -(b-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl|-3-(4-(6-(1-oxothiomorpholin-4-ylmethyl)pyridin-3-yl)naphthalene-1- yl urea, 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)-2H-pyrazol-3-yl|-3-I(4-(2-(morpholin-4-ylmethyl)pyrimidine -5-yl)naphtho-2oalin-1-yl|urea, 1-(2-tert-butyl-5-methylpyridin-4-yl)-3-14-(6-morpholin-4-ylmethylpyridin-3-yl) Naphthalin-1-yl|Urea, 1-(3-tert-butylphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalin-1-yl)urea, 1-(4-methylbiphenyl- 3-yl)-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(4-tert-butylbiphenyl-2-yl)-3-(4-( 6b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, sc 1-(5-isopropyl-2-methylphenyl)-3-I(4-(b-morpholin-4-ylmethylpyridin-3- yl)naphthalen-1-yl|urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-14-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, and ) 1-(5-tert-butyl-2-methoxymethylphenyl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalene-1 -yl|urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 1-(5-tert -butyl-2-methylphenyl)-3-(4-16-((3-methoxypropyl)methylamino|pyridin-3-ylnaphthalen-1-yl)urea, c zo 1-(5-tert-butyl-2-methylphenyl) -3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1-(5-tert-butyl-2-methylpyridin-3-yl)-3-I4-(6 -morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, o 1-(5-(1,1-dimethylpropyl)-2-methoxyphenyl|-3-(4-(6-morpholin-4- ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, Ge! 1-(b-tert-butyl-2-(1H-pyrazol-4-yl)phenyl)|-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1-(b-tert-butyl-2-(2-methylpyrimidin-5-yl)phenyl/1-3-14-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea -- ZB MNU, i- 1-Ib-tert-butyl-2-(3-hydroxypropyl)phenyl1|-3-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1- (b-tert-butyl-2-(morpholin-4-carbonyl)phenyl1|-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea y, M-(5- tert-butyl-2-methoxy-3-13-14-(6-morpholin-4-ylmethylpyridin-3-yl)unaphthalin-1-yl)ureido)phenyl)acetamide, "1-(3-methylnaphthalen-2-yl) )-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, with M-(5-tert-butyl-2-methoxy-3-13-I4-(6 -morpholin-4-ylmethylpyridin-3-yl)unaphtalin-1-yl)ureido)phenyl)acetamide, . 1-(b-tert-butyl-3-(2,3-dihydroxypropyl)-2-hydroxyphenyl|-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalene)? 1- yl|urea, 1--2,3-dimethyl-1H-indol-5-yl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-- 5-tert-butyl-2-methyl-3-III-(tetrahydropyran-2-yloxy)prop-1-ynyl|phenyl)-3-I(4-(b-morpholin-4-ylmethylpyrides -I n-3- yl)unaphtalin-1-yl|urea, 1--2-methoxy-5-trifluoromethylphenyl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, - 1 -(5--2,2-dimethylpropionyl)-2-methylphenyl/|-3-I4-(b6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, Ge) 1-(b- tert-butyl-3-(3-hydroxyprop-1-ynyl)-2-methylphenyl|-3-14-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-5or ylurea, o 1-(b -tert-butyl-2-(3-hydroxyprop-1-ynyl)uphenyl|-3-I(4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 1- (b-tert-butyl-3-(2,2-dimethyl-|1,3|dioxolan-4-ylmethyl)-2-methoxyphenyl/|-3-(4-(6-morpholin-4-ylmethylpyridin-3- yl)unnaphthalen-1-yl|urea, 1-(b-tert-butyl-3-(2,3-dihydroxyprop 1)-2-methoxyphenyl/i-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, F) 1-(5-tert-butoxy-2-methoxyphenyl )-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, ka 1-I(5-(1-cyanocyclopropyl)-2-methoxyphenyl|-3-(4 -(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(b-tert-butyl-3-(2-diethylaminoethyl)-2-methoxyphenyl|-3-I4-(b -morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl bo Esechovin, 1-(5-tert-butyl-2-methoxyphenyl)-3-I(4-(6-(1,3|dioxolane-2 -ylpyridin-3-yl)naphthalen-1-yl)urea, 1-(5-tert-butyl-2-pyrrolidin-1-ylphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl) naphthalene-1-yl|Urea, 1-(5-tert-butyl-2-dimethylaminophenyl)-3-I(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalene-1-yl)urea, 1 -(5-tert-butyl-2-propoxyphenyl)-3-I(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 65 1-(5-tert-butyl- 2-methoxyphenyl)-3-I4-(b-hydroxymethylpyridin-3-yl)naphthalen-1-yl)urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(6-(-2 ,6-Dimethylmorpholin-4-ylmethyl)pyridin-3-yl|Inaphthalene -1-il) section 1-(5-cyclohexyl-2-methoxyphenyl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1--2,4-dimethoxy-5-trifluoromethylphenyl )-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(5-tert-butyl-2-methoxy-33-nitrophenyl)-3-I4- (b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 1-(3-amino-5-tert-butyl-2-methoxyphenyl)-3-I(4-(b-methylpyridin- 3-yl)naphthalen-1-yl)urea, M-acetyl-M-(5-tert-butyl-2-methoxy-3-13-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalene- 1-yl)/ureido)phenyl)acetamide, 1-(b-tert-butyl-4-methyl-3-oxo-3,4-dihydro-2H-benzo|1,Zoxazin-8-yl)-3- I4-(b-morpholin-4-ylmethylpyridin-3-7/yl)naphthalen-1-yl|urea, 1-(5-tert-butyl-2-ethoxyphenyl)-3-I4-(6-morpholin-4 -ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, 1-(5-tert-butyl-2-isopropoxyphenyl)-3-I(4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalene- 1-yl)urea, 1-(5-tert-butyl-2-imidazol-1-ylphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 1 -(5-tert-butyl-3-ethylamino-2-methoxyphenyl)-3-I4-(6-morphol n-4-ylmethylpyridin-3-yl)naphthalen-1-yl|Urea, M-(5-tert-butyl-2-methoxy-3-13-I4-(6-morpholin-4-ylmethylpyridin-3-yl) naphthalene-1-yl)ureido)phenyl)bis(methanesulfon)amide, 1-(b-tert-butyl-2-(1-methyl-1H-pyrazol-4-yl)phenyl)1-3-I4-(b- morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl, 1--2-methanesulfinyl-5-trifluoromethylphenyl)-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl) naphthalene-1-yl|urea, 1-I4-(6-Tbis(2-methoxyethyl)amino|methyl)pyridin-3-yl)naphthalene-1-yl|-3-(5-tert-butyl-2-methoxyphenyl) )urea, IM-(11-(5-4-(3-(5-tert-butyl-2-methoxyphenyl)ureido|naphthalen-1-yl)upyridin-2-ylmethyl)pyrrolidin-3-ilyacetamide, 1-- 1-acetyl-3,3-dimethyl-2,3-dihydro-1H-indol-5-yl)-3-I(4-(β6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl| )urea, M-(5-tert-butyl-2-methoxy-3-13-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-ylIureido)phenyl)propionamide, sc 1-( 5-tert-butyl-2-methyl-benzoxazol-7-yl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, 1-(4-(b -morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|-3--Z -trifluoromethanesulfonylphenyl)urea, and) M-(5-tert-butyl-2-methoxy-3-13-I4-(6-morpholin-4-ylmethylpyridin-3-yl)unaphtalin-1-yl)ureido)phenyl)isobutyrami d, 2-(4-tert-butyl-2-13-14-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)ureido)phenoxy)acetamide, c zo 1-(5-tert -butyl-2-oxo-2,3-dihydrobenzooxazol-7-yl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl urea, 1-(5-tert- butyl-3-cyano-2-methoxyphenyl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, Ge! 1-(5-tert-butylbenzoxazol-7-yl)-3-I(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, M-(5-tert-butyl- 2-Methoxy-3-13-I4-(6-morpholin-4-ylmethylpyridin-3-yl)unaphthalin-1-yl)ureido)phenyl)benzenesul --fonamide, i-(5-tert-butyl-2-methoxy -3-(3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)ureido)phenyl)amide of ethanesulfonic acid, 1-(5-tert-butyl-2-methoxyphenyl)-3 -I(4-(2-morpholin-4-ylmethylpyrimidin-5-yl)naphthalen-1-yl|urea, 1-(5-tert-butyl-2-methylsulfanylphenyl)-3-I(4-(b-morpholine -4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, « 1-(5-tert-butyl-2-methoxypyridin-3-yl)-3-14-(b-morpholin-4-ylmethylpyridin-3 -yl)naphthalen-1-yl)urea, with (5-tert-butyl-2-methoxy-3-(3-14-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl) ureido)phenyl)amide . 2,2,2-trifluoroethanesulfonic acid, and? M-(5-4-(3-(5-tert-butyl-2-methylphenyl)ureido|naphthalen-1-yl/pyrazin-2-yl)umethanesulfonamide, 1-I4-(6-Tibis(2-cyanoethyl) amino|methyl)pyridin-3-yl)naphthalen-1-ylI|-3-(5-tert-butyl-2-methoxyphenyl)urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-4- (6-(4-methylpiperazin-1-ylmethyl)pyridin-3-yl|naphthalen-1-yl)uretate, -I 1-(5-tert-butyl-2-methoxyphenyl)-3-I4-(b-thiomorpholine -4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, and 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(6-(2,6-dimethylpiperidin-1-ylmethyl) -pyridin-3-yl|Inaphthalin-1-yl)usechovy NU, Ge) 1-(5-tert-butyl-2-methoxyphenyl)-3-74-(6-(1-oxotetrahydrothiopyran-4-ylamino)pyridine- 3-yl|Inaphthalin-1-yl) urine OVINU, about 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(b-(tetrahydropyran-4-ylamino)pyridin-3-yl|Inaphthalin- 1-yl)uretate, Ge 1-(5-tert-butyl-2-methoxyphenyl)-3-I4-(6-4(2-cyanoethyl)-(tetrahydrofuran-2-ylmethyl)amino)methyl)pyridin-3- i) naphthalene-1-yl|urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(6-(2-methoxymethylmorpholin-4-ylmethyl)-pyridin-3-yl|Inaphthalene- 1-il)usecho B VINU, 1-(5 -tert-butyl-2-methoxyphenyl)-3-14-(6-(2-methyl-3-oxopiperazin-1-ylmethyl)-pyridin-3-ylInaphthalin-1-yl)urea (F, ovinu, ka amide 1 -(5-4-I3-(5-tert-butyl-2-methoxyphenyl)ureido|naphthalen-1-yl)pyridin-2-ylmethyl)piperidine-3-carboxylic acid, in 1-(5-tert-butyl- 2-methoxyphenyl)-3-74-(6-(1-oxo-114-thiomorpholin-4-ylmethyl)pyridin-3-yl|naphthalen-1-yl)urea, 1-(3,3-dimethyl-2 -oxo-2,3-dihydro-1H-indol-5-yl)-3-(4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)urea, 1-(5 -tert-butyl-2-methoxyphenyl)-3-74-(6-(3-oxopiperazin-1-ylmethyl)pyridin-3-yl|Inaphthalin-1-yl)uretic, 65 1-(5-tert-butyl- 2-Methoxyphenyl)-3-(4-16-((Tetrahydrofuran-33-ylamino)methylpyridin-3-ylenenaphthalen-1-yl)usecuine, 1-(5-tert-butyl-2-methoxyphenyl)-3-I4-(6-4(2-cyanoethyl)pyridin-3-ylmethylamino|methyl)pyridin-3-yl)naphthalen-1-yl|Urea, 1 -(5-tert-butyl-2-methoxyphenyl)-3-74-(6-(2-oxa-5-azabicyclo|2.2.1)hept-5--ylmethyl)pyridin-3-ylInaphthalin-1-yl) urea, 1-(5-tert-butyl-2-methoxyphenyl)-3-4-(6-(-2,6-dimethylmorpholin-4-ylmethyl)pyridin-3-yl|Inaphthalin-1-yl)urea 1- (5-tert-butyl-2-methoxyphenyl)-3-(4-16-14-(3-methoxyphenyl)piperazin-1-ylmethyl|-pyridin-3-ylnaphthalen-1-yl)urea, 70 1-(5 -tert-butyl-2-methoxyphenyl)-3-4-(b-(morpholine-4-carbonyl)pyridin-3-yl|Inaphthalen-1-yl)erucine, 1-(5-tert-butyl-2-methoxyphenyl )-3-I4--5-morpholin-4-ylmethylpyrazin-2-yl)naphthalen-1-yl)urea, 1-(b-tert-butyl-3-oxo-3,4-dihydro-2H-benzo| 1,oxazin-8-yl)-3-(4--6-morpholin-4-ylmethylpyridin-3-yl)naphthalene-1-yl)urea, 1-(3-amino-5-tert-butyl-2 -methoxyphenyl)-3-I4-(b-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl|urea, M-(5-4-(3-(5-tert-butyl-2-methoxyphenyl) ureido|naphthalen-1-yl)pyridin-2-yl)acetamide, M-(5-tert-butyl-2-me toxy-3-13-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-ylIureido)phenyl)-M-methylacetamide, M-(5-tert-butyl-2-methoxy-3- 13-I4-(6-morpholin-4-ylmethylpyridin-3-yl)naphthalen-1-yl)ureido)phenyl)-2,2,2-tri toracetamide, 1-(5-tert-butyl-2-methoxyphenyl) -3-4-(6b-(pyridin-3-yloxy)pyridin-3-yl|Inaphthalin-1-yl)urea, 3-tert-butylphenyl ether (4-(b-morpholin-4-ylmethylpyridin-3-yl )naphthalen-1-yl|carbamic acid, M-(5-tert-butyl-2-methoxy-3-13-14-(6-morpholin-4-ylmethylpyridin-3-yl)unanaphthalen-1-yl)ureido) phenyl)methanesulfonamide, and their pharmaceutically acceptable derivatives. high school 34. A pharmaceutical composition containing a pharmaceutically effective amount of a compound according to any one of claims 1, 9, 17 or 25. o 35. A method of treating a cytokine-mediated disease, comprising administering to a patient in need thereof a therapeutically effective amount of a compound according to any one of claims 1, 9, 17 or 25. 36. The method according to claim 35, wherein said cytokine-mediated disease is a disease selected from the group consisting of rheumatoid arthritis, osteoarthritis, Crohn's disease, nonspecific ulcerative colitis, multiple sclerosis, Guillain-Barré syndrome, psoriasis, graft-versus-host disease host", systemic lupus erythematosus, diabetes, toxic shock, osteoporosis, Alzheimer's disease, acute and chronic pain, contact dermatitis and atherosclerosis. 37. A method of treatment of a disease mediated by neutrophils, selected from the group that includes shock, myocardial infarction, thermal burn, adult respiratory distress syndrome (RDS), multiple injuries in the gut as a result of trauma, acute glomerulonephritis, dermatosis accompanied by acute inflammatory processes, acute purulent meningitis, hemodialysis, leukopheresis, granulocyte transfusion-related syndromes and necrotizing enterocolitis, which consists in administering to a patient in need of such treatment a therapeutically effective amount of a compound according to any one of claims 1, 9, 17 or 25. Official Bulletin "Industrial Property". Book 1 "Inventions, useful models, topographies of integrated microcircuits", 2005, M 1, 15.01.2005. The State Department of Intellectual Property of the Ministry of Education and Science? of Sciences of Ukraine. -I - se) c 50 Ko) F) ime) 60 b5