Therapeutic compounds and their uses

Abstract

The present invention relates to the field of therapeutic compounds in general. More specifically, the present invention relates to certain biarylamide compounds of the following formula (also referred to here as “BAA compounds”) that inhibit the protein kinase, membrane-bound tyrosine / threonine 1 (PKMYT1). The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds and compositions both in vitro and in vivo for inhibiting PKMYT1 kinase; for treating disorders (e.g., diseases) that are improved by inhibition of PKMYT1 kinase; and for treating proliferative disorders, cancer, and the like. TIFF2026510369000585.tif2338

Description

[Technical Field]

[0001] Technical field The present invention relates to the field of therapeutic compounds in general. More specifically, the present invention relates to certain biarylamide compounds (hereinafter also referred to as "BAA compounds") that inhibit the protein kinase, membrane-bound tyrosine / threonine 1 (PKMYT1). The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds and compositions for inhibiting PKMYT1 kinase in vitro and in vivo; for treating disorders (e.g., diseases) that are improved by inhibition of PKMYT1 kinase; and for treating proliferative disorders, cancer, and the like. [Background technology]

[0002] background To more fully describe the state of the art in the field to which this invention relates, publications are referenced. Each of these references is incorporated into this disclosure by reference to the same extent that each individual reference is shown to be incorporated by specific and individual reference.

[0003] Throughout this specification, including the claims set forth below, unless otherwise specified, the terms “including,” and variations thereof such as “including,” and “including,” are understood to encompass the integers or processes or groups of integers or processes described, but not to exclude any other integers or processes or groups of integers or processes.

[0004] It should be noted that, as used herein and in the appended claims, singular expressions include plural subjects unless the context clearly indicates otherwise. Therefore, for example, the description of “pharmaceutical carrier” includes a mixture of two or more such carriers.

[0005] Ranges are often expressed as "approximately" from one specific value to / or "approximately" the other specific value. When such an expression is used, the other embodiment includes from one specific value to / or the other specific value. Similarly, when a value is expressed as an approximation by the use of the antecedent "approximately," it is understood that the specific value forms the other embodiment.

[0006] This disclosure may contain information useful for understanding the present invention. It does not constitute an endorsement that any information provided herein is prior art or relating to the present invention, nor does it endorse any publication expressly or implicitly cited herein as prior art.

[0007] Protein kinase, membrane-bound tyrosine / threonine 1 (PKMYT1) A key characteristic of cancer is that cancer cells disable cell cycle control that prevents them from participating in division until the appropriate conditions are met. When the conditions are right, the cell passes through a decisive point in the cell division cycle, known as a "limiting point," through the activation of the Cdk4 / 6-cyclin D complex. After passing this point of no return, the cell activates Cdk2-cyclin E to drive DNA replication, and this DNA is sequestered into two daughter cells in the late cell cycle by Cdk1-cyclin B.

[0008] To enable illogical proliferation, cancer cells either inadvertently boost the kinase activity of the Cdk4 / 6-cyclin D complex or bypass the need for Cdk4 / 6-cyclin D activation by activating the downstream Cdk2-cyclin E complex, independently of any input from Cdk4 / 6-cyclin D. By implementing either of these two approaches, cancer can evade the normal controls that maintain a balance between proliferation and homeostasis in the body. Consequently, cancer growth becomes uncontrolled.

[0009] Drugs that inhibit the Cdk4 / 6-cyclin D complex have had a significant impact on the treatment of hormone-responsive HER2-negative breast cancer (HER2-ER+) and are currently in clinical trials for a variety of other cancers.

[0010] In contrast, counteracting Cdk2-cyclin E hyperactivation was considered drug-ineffective until a recent study reported that a WEE1 family kinase, referred to as PKMYT1, is only required when cyclin E levels are abnormally high (Gallo et al., 2022). Importantly, they found that PKMYT1 loss does not kill normal cells.

[0011] The same study showed that PKMYT1 loss is synthetically lethal in the presence of cyclin E (CCNE1) overexpression; CCNE1 overexpression drives cyclin B transcription, increasing cyclin B levels, and all available Cdk1 inhibitory activity is required to suppress Cdk1-cyclin B, leading to the production of large amounts of Cdk1-cyclin B so that catastrophic mitosis is prevented. Therefore, CCNE1 overproduction leads to PKMYT1 dependence.

[0012] FBXW7 is a gene that encodes E3 ligase, which degrades cyclin E. FBXW7 loss has also been shown to be synthetically lethal in the presence of PKMYT1 inhibitors (Durocher et al., 2021), suggesting that PKMYT1 drugs may be a potential first-line therapy for several types of cancer.

[0013] CCNE1 amplification has been reported in several cancer types, including endometrial, ovarian, breast, and gastric cancers, with frequencies ranging from 5% to 40%. CCNE1 amplification and / or FBXW7 mutations occur in >60% of uterine carcinosarcomas, >20% of uterine cancers, about 20% of ovarian cancers, about 18% of gastric cancers, about 14% of colorectal cancers, about 12% of bladder cancers, 11.5% of esophageal cancers, about 11% of cervical cancers, 7.5% of sarcomas, and about 7% of lung squamous cell carcinomas (Durocher et al., 2021). CCNE1 also occurs at low levels in other cancers such as adenoid cystic carcinoma, pancreatic cancer, mesothelioma, lung adenocarcinoma, head and neck cancers, diffuse large B-cell lymphoma, liver cancer, and others (Gorski et al., 2020). Furthermore, CCNE1-overexpressing ovarian cancers represent a 50% subset that is recombinant and does not benefit from PARP inhibitors (Gorski et al., 2020), highlighting the unmet need in these indications.

[0014] CCNE1 amplification is observed in more invasive subtypes, including uterine carcinosarcoma (UCS; approximately 40%), serous uterine carcinoma (USC; approximately 25%), high-grade serous ovarian cancer (HGSOC; approximately 20%), and triple-negative breast cancer (TNBC; approximately 8%). CCNE1 overexpression in tumor biopsies is associated with lower overall survival compared to patients with normal cyclin E1 levels. HGSOC patients with CCNE1 overexpression have a low response rate to current standard treatment, cisplatin.

[0015] Similarly, FBXW7 frequently mutates in several cancer types, including uterine carcinosarcoma, endometrial, colorectal, cervical, bladder, head and neck, gastric, and lung squamous cell carcinoma, with frequencies ranging from 5% to 39%. Similar to CCNE1 overexpression, FBXW7 driver mutations are observed in more invasive subtypes of endometrial cancer, including UCS and USC.

[0016] Elevated Cdk2-cyclin E activity via various means is also associated with resistance to Cdk4 / 6 inhibitors (Fassl et al., 2022); this also suggests that PKMYT1 inhibition constitutes a robust second-line treatment in a cohort of HER2-ER+ breast cancer patients treated with Cdk4 / 6 inhibitors, who generally acquire resistance approximately two years after treatment.

[0017] A recently discovered inhibitor of PKMYT1, RP-6306 (Szychowski et al., 2022), has shown efficacy in vivo, either alone or in combination with gemcitabine, in breast and ovarian cancer models overexpressing CCNE1, as well as in pancreatic PDX models with increased CCNE1 expression (Gallo et al., 2022).

[0018] Synthetic lethality has been suggested to occur in cancer cells between PKMYT1 inhibition and deficiency of protein phosphatase 2 (PP2A), particularly the regulatory subunit B-alpha (PPP2R2A) (Yost et al., 2021). PPP2R2A inactivation is present in 15% of prostate adenocarcinomas and >5% of ovarian serous adenocarcinoma, rectal adenocarcinoma, bladder urothelial carcinoma, colorectal adenocarcinoma, invasive breast carcinoma, endometrioid carcinoma of the uterine body, carcinosarcoma of the uterus, hepatocellular carcinoma of the liver, squamous cell carcinoma of the lung, and lung adenocarcinoma.

[0019] PKMYT1 is a cell cycle regulatory kinase, part of the WEE1 family of kinases, which also includes WEE1 and WEE2. WEE2 is limited to the gonads because it regulates meiosis. In contrast, both PKMYT1 and WEE1 are expressed ubiquitously. PKMYT1 is primarily localized to the endoplasmic reticulum and Golgi complex, while WEE1 is primarily a nucleoprotein. PKMYT1 is involved in the negative regulation of the CDK1-cyclin B complex, which facilitates the progression of the cell cycle from G2 phase to mitotic phase (M phase). The biology of cyclin E overproduction necessitates PKMYT1, which is otherwise not essential. Cyclin E accumulation boosts the transcription of cyclin B1; the likelihood of forming active Cdk1-cyclin B is greatly enhanced by CCNE1 overexpression. This places a much greater demand on the Cdk1-cyclin B inhibitory activity of both WEE1 and PKMYT1, making PKMYT1 essential. Furthermore, CCNE1 overproduction stimulates abnormally high levels of DNA replication, which depletes the nucleotide pool and leads to DNA damage (Jones et al, 2013). DNA damage caused by cyclin E accumulation is not lethal in itself because cells have a G2 / M checkpoint that suppresses their involvement in genome segregation in mitosis until all damage is repaired. These checkpoint pathways boost the activity of Wee1 family kinases WEE1 and PKMYT1 and suppress division by phosphorylating Cdk1 kinase to block Cdk1-cyclin B activity. Damage persists, but WEE1 and PKMYT1 activity remains high, and the cell cannot divide. Therefore, WEE1 or PKMYT1 inhibition kills damaged cells by causing them to divide when the DNA is still damaged and / or non-replicating. This places a great demand on WEE1 and PKMYT1's ability to suppress CDK1-cyclin B activity in order to maintain cell viability.

[0020] PKMYT1 can be removed from non-transformed cells because the need for suppressing CDK1-cyclin B1 activity can be met by WEE1 alone. PKMYT1 activity becomes essential only when abnormally high levels of DNA damage create a significant need for CDK1-cyclin B inhibition.

[0021] The WEE1 inhibitor adavocertib has progressed to clinical trials in several solid tumors (clinicaltrials.gov) but has shown significant toxicity. WEE1 inhibitory toxicity is most likely due to its ability to inhibit both the CDK2 and CDK1 complexes. CDK2-cyclin E and CDK2-cyclin A control the initiation and progression of DNA replication. The release of excessive levels of CDK2-cyclin activity leads to DNA damage in a phenomenon known as oncogene-induced replication senescence. PKMYT1 inhibition, unlike WEE1, phosphorylates CDK1 and is therefore less likely to exhibit similar S-phase toxicity (Booher et al., 1997; Liu et al., 1997).

[0022] In summary, due to the significant reduction in toxicity to normal tissue resulting from PKMYT1 dependence and restricted CDK1 regulation brought about by excessive Cdk2-cyclin E activity in cancer cells, PKMYT1 is a highly attractive target for inhibition in patients whose tumors proliferate inappropriately due to enhanced Cdk2-cyclin E activity.

[0023] Overexpression of PKMYT1 has been observed in various cancers, including lung squamous cell carcinoma, lung adenocarcinoma, endometrioid carcinoma of the uterine body, invasive breast cancer, hepatocellular carcinoma, renal clear cell carcinoma, chromophobic renal cell carcinoma, renal papillary cell carcinoma, head and neck squamous cell carcinoma, colon adenocarcinoma, gastric adenocarcinoma, thyroid cancer, and prostate adenocarcinoma (compared to normal tissue). Elevated PKMYT1 expression is associated with poor prognosis in adrenocortical carcinoma, renal chromophobic cell carcinoma, renal clear cell carcinoma, renal papillary cell carcinoma, low-grade glioma, hepatocellular carcinoma of the liver, lung adenocarcinoma, mesothelioma, pancreatic adenocarcinoma, prostate adenocarcinoma, cutaneous melanoma, uveal melanoma (Shao et al., 2021), and breast cancer (Liu et al., 2020).

[0024] PKMYT1 is found in many solid tumors, such as non-small cell lung cancer (Zhang et al., 2022; He et al., 2021; Sun et al., 2019), osteosarcoma (Luo et al., 2022), clear cell renal carcinoma (Chen et al., 2020; Chen et al., 2021), oral squamous cell carcinoma (Cai et al., 2022), gastric cancer (Hu et al., 2022; Zhang et al., 2020), prostate cancer (Wang et al., 2020), esophageal squamous cell carcinoma (Zhang et al., 2019), colorectal cancer (Jeong et al., 2018), hepatocellular carcinoma (Liu et al., 2017), and ovarian cancer (Xuan et al., PKMYT1 is involved in the progression, invasion, and / or metastasis of neuroblastoma (especially with MYCN amplification) (Chayka et al., 2015) and glioblastoma (Toledo et al., 2015). PKMYT1 is essential for survival in some hematological malignancies, such as acute lymphoblastic leukemia and multiple myeloma (Ghelli Luserna di Rora et al., 2020).

[0025] PKMYT1 may have indications for addressing resistance to treatment or improving the effectiveness of cancer treatment agents. Elevated PKMYT1 has been reported as a resistance mechanism for sustained WEE1 inhibition (Lewis et al., 2019). PKMYT1 inhibitors may also be useful as a second-line treatment complementing emerging WEE1i-based therapies.

[0026] Knockdown of PKMYT1 can eliminate radiation-induced G2 / M arrest and reduce the survival rate of cells receiving radiotherapy, making it a promising target for improving the radiosensitivity of lung adenocarcinoma (Long et al., 2020). PKMYT1 may also be useful in enhancing the efficacy of anti-microtubule cancer drugs (Visconti et al., 2017).

[0027] PKMYT1 also plays a role in viral infections. Knockdown of PKMYT1 reduces the number of cells supporting Kaposi's sarcoma herpesvirus (KSHV) lytic infection during the S phase of the cell cycle (Bryan et al., 2006). KSHV is the cause of Kaposi's sarcoma, primary exudative lymphoma (PEL), and the plasmablastic subtype of multicentric Castleman disease.

[0028] There is a clear need for PKMYT1 selective inhibitors that have minimal or no toxicity, are suitable for oral administration, and possess good pharmacokinetic properties. [Overview of the Initiative] [Problems that the invention aims to solve]

[0029] The present invention provides compounds and compositions that selectively inhibit PKMYT1 for treating cancer. [Means for solving the problem]

[0030] Summary of the Invention One aspect of the present invention relates to certain biarylamide compounds (also referred to herein as "BAA compounds") that inhibit the protein kinase, membrane-bound tyrosine / threonine 1 (PKMYT1), as described herein.

[0031] Another aspect of the present invention relates to a composition (e.g., a pharmaceutical composition) comprising the BAA compound described herein and a pharmaceutically acceptable carrier or diluent.

[0032] Another aspect of the present invention relates to a method for producing a composition (e.g., a pharmaceutical composition) comprising mixing the BAA compound described herein with a pharmaceutically acceptable carrier or diluent.

[0033] Another aspect of the present invention relates to a method for inhibiting PKMYT1 in vitro or in vivo (e.g., inhibiting, reducing, or blocking the activity or function of PKMYT1), comprising contacting PKMYT1 with an effective amount of one of the BAA compounds described herein.

[0034] Another aspect of the present invention relates to a method for inhibiting PKMYT1 in cells in vitro or in vivo (e.g., inhibiting, reducing, or blocking the activity or function of PKMYT1), comprising contacting cells with an effective amount of the BAA compound described herein.

[0035] Another aspect of the present invention relates to the BAA compounds described herein for use in methods of treating human or animal bodies by therapeutic means, for example, in methods of treating the disorders (e.g., diseases) described herein.

[0036] Another aspect of the present invention relates to the use of the BAA compounds described herein in methods of treating human or animal bodies in the treatment of, for example, the disorders (e.g., diseases) described herein.

[0037] Another aspect of the present invention relates to the use of the BAA compounds described herein in the manufacture of pharmaceuticals, for example, for use in a method of treatment, for example, for use in a method of treatment of the disorders (e.g., diseases) described herein.

[0038] Another aspect of the present invention relates to a method of treatment, for example, a method of treatment for a disorder (e.g., a disease) described herein, comprising administering a therapeutically effective amount of the BAA compound described herein to a subject requiring treatment, preferably in the form of a pharmaceutical composition.

[0039] In one embodiment, the disorder is one that is improved by inhibiting PKMYT1 (for example, by inhibiting, reducing, or blocking the activity or function of PKMYT1).

[0040] In one embodiment, the disorder is one of those described herein, such as a proliferative state or cancer.

[0041] Other aspects of the present invention relate to (a) the BAA compounds described herein, preferably provided as a composition (e.g., a pharmaceutical composition) in a suitable container and / or in suitable packaging; and (b) a kit, including instructions for use, e.g., instructions on how to administer the compounds, in a method of treating, for example, a disorder (e.g., a disease) described herein.

[0042] Another aspect of the present invention relates to BAA compounds that can be obtained by the synthesis method described herein or by a method comprising the synthesis method described herein.

[0043] Another aspect of the present invention relates to BAA compounds obtained by the synthesis method described herein or by a method comprising the synthesis method described herein.

[0044] Another aspect of the present invention relates to novel intermediates described herein that are suitable for use in the synthesis methods described herein.

[0045] Another aspect of the present invention relates to the use of the novel intermediates described herein in the synthetic methods described herein.

[0046] As will be recognized by those skilled in the art, the characteristics and preferred embodiments of one aspect of the present invention also relate to other aspects of the present invention.

BRIEF DESCRIPTION OF THE INVENTION

[0047] Detailed description compound One aspect of the present invention is a compound of the following formula, or a pharmaceutically acceptable salt or solvate thereof, wherein ring A and ring B are as defined herein (for convenience, collectively referred to herein as "biaryl amide compound" or "BAA compound"):

CHEMICAL FORMULA

[0048] Certain embodiments include the following: (1) The following formula:

CHEMICAL FORMULA

CHEMICAL FORMULA

[0049] (2) The following equation: [ka] Compounds of or pharmaceutically acceptable salts or solvates thereof (e.g., or pharmaceutically acceptable salts thereof); Here: Ring A is: [ka] And here: -RA1 ha-R A11 and; -R A11 ha-R A111 , -F, -Cl, -Br, -I, -CF3, -CHF2, -OH, -OR A111 -OCF3, -NH2, -NHR A111 , -NR A111 2, -CN, -C(=O)R A111 -C(=O)OH, -C(=O)OR A111 -C(=O)NH2, -C(=O)NHR A111 -C(=O)NR A111 2, or -S(=O)2R A111 and; Each-R A111 These are independently linear or branched saturated C 1-4 It is alkyl; -R A2 ha-R A22 and; -R A22 ha-R A222 , -F, -Cl, -Br, -I, -CF3, -CHF2, -OH, -OR A222 -OCF3, -NH2, -NHR A222 , -NR A222 2, -CN, -C(=O)R A222 -C(=O)OH, -C(=O)OR A222 -C(=O)NH2, -C(=O)NHR A222 -C(=O)NR A222 2, or -S(=O)2R A222 and; Each-R A222 These are independently linear or branched saturated C 1-4 It is alkyl; -R A3 is -H or -R A33 and; -R A33 ha-R A333 , -F, -Cl, -Br, -I, -CF3, -OH, -OR A333 , or -OCF3; Each-R A333 These are independently linear or branched saturated C 1-4 It is alkyl; -RA4 is -H or -R A44 and; -R A44 ha-R A444 , -F, -Cl, -Br, -I, -CF3, -OH, -OR A444 , or -OCF3; Each-R A444 These are independently linear or branched saturated C 1-4 It is alkyl; and: Ring B is: [ka] Selected from, here: Y 1 S, O, NH, NR Y1 and; Y 2 CH, CR Y2 , or N; Y 3 is N, CH, or CR Y3 and; Y 4 is N, CH, or CR Y4 and; Y 5 S, O, NH, NR Y5 and; Y 6 is N, CH, or CR Y6 and; Y 7 is N, CH, or CR Y7 and; Y 8 is N, CH, or CR Y8 and; Y 9 S, O, NH, NR Y9 and; Here: Each-R Y2 And, -R Y3 And, -R Y4 And, -R Y6 And, -R Y7 , and -R Y8 These are independently -H, -F, -Cl, -Br, -I, and -R YY -CF3, -OH, -ORYY -OCF3, -NH2, -NHR YY , or -NR YY It is 2; Each-R YY These are independently linear or branched saturated C 1-4 It is alkyl; and: Each-R Y1 And, -R Y5 , and -R Y9 -R is independent YYN -C(=O)R YYN , -C(=O)OR YYN -C(=O)NH2, -C(=O)NHR YYN -C(=O)NR YYN 2, or -S(=O)2R YYN and; Each-R YYN These are independently linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 Heteroaryl, or C 5-6 Heteroaryl-C 1-3 It is alkyl, and here, C 1-4 Alkyl groups are optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; and: -Q is -Q 1 , -L Q1 -Q 1 ,-Q 2 , -L Q2 -Q 2 ,-Q 3 , -L Q3 -Q 3 ,-Q 4 , -L Q4 -Q 4 ,-Q 5 , or -H; Here: Q 1 is C 5-10 It is a heteroaryl; and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and If desired, if present, add one or more secondary nitrogen atoms to the -R group. Q1N It has been replaced with; -L Q1 - indicates a straight-chain or branched saturated C 1-4 It is alkylene; Q 2 is non-aromatic C 3-7 It is a heterocycline; and: If desired, if present, sulfur is substituted with one or two oxygen groups; If desired, one or more carbon atoms are added as a group -R Q2C It is replaced by; and If desired, if present, add one or more secondary nitrogen atoms to the -R group. Q2N It has been replaced with; -L Q2 - indicates a straight-chain or branched saturated C 1-4 It is alkylene; Q 3 is phenyl or naphthyl; And, if desired, one or more base-R Q3C It has been replaced with; -L Q3 - indicates a straight-chain or branched saturated C 1-4 It is alkylene; Q 4 is C 3-7 It is a cycloalkyl; And, if desired, one or more base-R Q4C It has been replaced with; -L Q4 - indicates a straight-chain or branched saturated C 1-4 It is alkylene; Q 5 is a linear or branched saturated C 1-6 It is alkyl; And, if desired, one or more base-R Q5C It has been replaced with; and: Each -R Q1C is independently: -F, -Cl, -Br, -I, -R Q1CC , -R Q1CX , -OR Q1CX , -OH, -OR Q1CC , -L Q1C -OH, -L Q1C -OR Q1CC , -NH2, -NHR Q1CC , -NR Q1CC 2, and -R Q1CM , -L Q1C -NH2, -L Q1C -NHR Q1CC , -L Q1C -NR Q1CC 2, -L Q1C -R Q1CM , -NHC(=O)R Q1CC , -NHC(=O)OR Q1CC , -L Q1C -NHC(=O)R Q1CC , -L Q1C -NHC(=O)OR Q1CC , -C(=O)NH2, -C(=O)NHR Q1CC , -C(=O)NR Q1CC 2, -C(=O)R Q1CM , -L Q1C -C(=O)NH2, -L Q1C -C(=O)NHR Q1CC , -L Q1C -C(=O)NR Q1CC 2, -L Q1C -C(=O)R Q1CM , -C(=O)OH, -C(=O)OR Q1CC , -OC(=O)R Q1CC , -OC(=O)NH2, -OC(=O)NHR Q1CC , -OC(=O)NR Q1CC 2, -OC(=O)R Q1CM , -S(=O)2R Q1CC 、 -S(=O)2NH2, -S(=O)2NHR Q1CC 、-S(=O)2NR Q1CC 2, -S(=O)2NR Q1CM 、 -CN, or -NO2 and; where two adjacent -R Q1C if present, combine to form -(CH2) n1 -O-(CH2) m1 - or -O-(CH2) p1 -O- where: n1 is 0, 1, 2, or 3; m1 is 0, 1, 2, or 3; and p1 is 1 or 2; provided that m1 + n1 is 2 or 3; where: each -R Q1CC is independently a straight or branched chain saturated C 1-4 alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 alkyl, C 3-7 heterocyclyl, phenyl, phenyl-C 1-3 alkyl, C 5-6 heteroaryl, or C 5-6 heteroaryl-C​​​​​​​​​​​​​​​​​​​​​It is a heterocycline; and: If desired, one or more carbon atoms are added as a group -R Q1CMM It has been replaced with; If desired, if present, sulfur is substituted with one or two =O groups; and Upon request, if available, secondary nitrogen, -R Q1CMM -C(=O)R Q1CMM , -C(=O)OR Q1CMM -C(=O)NH2, -C(=O)NHR Q1CMM -C(=O)NR Q1CMM 2, and -S(=O)2R Q1CMM It is substituted with a group selected from; and Each-R Q1CMM These are independently linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 Heteroaryl, or C 5-6 Heteroaryl-C 1-3 It is alkyl, and here, C 1-4 Alkyl groups are optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; and: Each-R Q1N Independently: -R Q1NC , -R Q1NX , -R Q1Nhet , -L Q1N -R Q1Nhet , -L Q1N -OH, -L Q1N -OR Q1NC , -L Q1N -C(=O)R Q1NC , -L Q1N-C(=O)OH, -L Q1N -C(=O)OR Q1NC , -L Q1N -C(=O)NH2, -L Q1N -C(=O)NHR Q1NK , -L Q1N -C(=O)NR Q1NC 2, -L Q1N -C(=O)R Q1NP , -L Q1N -NH2, -L Q1N -NHR Q1NC , -L Q1N -NR Q1NC 2, -L Q1N -R Q1NM , or -L Q1N -NHC(=O)OR Q1NC ; and where: each -R Q1NC is independently a straight or branched chain saturated C 1-4 alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 alkyl, phenyl, phenyl-C 1-3 alkyl, C 5-6 heteroaryl, or C 5-6 heteroaryl-C 1-3 alkyl, where each cycloalkyl, phenyl and heteroaryl is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; each -R Q1NX is independently a straight or branched chain saturated C 1-4 haloalkyl; each -L Q1N - is independently a straight or branched chain saturated C 1-4 alkylene; each -R Q1NM is independently a non-aromatic C 3-7 heterocyclyl having at least one N ring atom and bonded through said N ring atom; and: If desired, one or more carbon atoms are added as a group -R Q1CMM It has been replaced with; If desired, if present, sulfur is substituted with one or two =O groups; and Upon request, if available, secondary nitrogen, -R Q1NMM -C(=O)R Q1NMM , -C(=O)OR Q1NMM -C(=O)NH2, -C(=O)NHR Q1NMM -C(=O)NR Q1NMM 2, and -S(=O)2R Q1NMM It is substituted with a group selected from; and Each-R Q1NMM These are independently linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 Heteroaryl, or C 5-6 Heteroaryl-C 1-3 It is alkyl, and here, C 1-4 Alkyl groups are optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; and: Each-R Q1Nhet These are independently non-aromatic C 3-7 It is a heterocycline; and: If desired, if present, sulfur is substituted with one or two oxygen groups; If desired, one or more carbon atoms are added as a group -R Q1NHH Or it is replaced by =O; and Upon request, if available, secondary nitrogen, -R Q1NHH -C(=O)R Q1NJJ , -C(=O)OR Q1NHH -C(=O)NH2, -C(=O)NHR Q1NHH -C(=O)NR Q1NHH2, and -S(=O)2R Q1NHH It is substituted with a group selected from; Here: Each-R Q1NHH These are independently linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, C 3-7 Heterocyclyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 Heteroaryl, or C 5-6 Heteroaryl-C 1-3 It is alkyl, and here, C 1-4 Alkyl groups are optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; and: -R Q1NJJ ha-R J1 And, -R J2 , -L J -R J2 And, -R J3 , -L J -R J3 And, -R J4 , -L J -R J4 And, -R J5 , or -L J -R J5 and; -R J1 is a linear or branched saturated C 1-6 Alkyl; and optionally -F, -OH, -OR JJ -O-phenyl, -C(=O)OH, -C(=O)OR JJ -NH2, -NHR JJ , and -NR JJ Substituted with one or more elements selected from 2; Each-R J2 C is independent 3-6 It is cycloalkyl; and optionally -F and -RJJ -CF3, -OH, -OR JJ -NH2, -NHR JJ , and -NR JJ Substituted with one or more elements selected from 2; Each-R J3 These are independently non-aromatic C 3-7 It is a heterocycline; and: If desired, if present, sulfur is substituted with one or two oxygen groups; Carbon is -F and -R as desired. JJ -CF3, -OH, -OR JJ -NH2, -NHR JJ , and -NR JJ It is replaced by one or more elements selected from 2; and Upon request, if available, secondary nitrogen, -R JJ -C(=O)R JJ , -C(=O)OR JJ , and -S(=O)2R JJ It is substituted with a group selected from; Each-R J4 is phenyl; and optionally -F, -Cl, and -R JJ -CF3, -OH, -OR JJ -NH2, -NHR JJ , and -NR JJ Substituted with one or more elements selected from 2; Each-R J5 C is independent 5-6 It is a heteroaryl; and: Carbon is -F and -R as desired. JJ -CF3, -OH, -OR JJ -NH2, -NHR JJ , and -NR JJ It is replaced by one or more elements selected from 2; and Upon request, if available, secondary nitrogen, -R JJ -C(=O)R JJ , -C(=O)OR JJ , and -S(=O)2R JJ It is substituted with a group selected from; Each-LJ - is independently linear or branched saturated C 1-4 It is an alkylene and optionally substituted with one or more -F groups; Each-R JJ is a linear or branched saturated C 1-4 It is alkyl; and: -R Q1NK ha-R K1 And, -R K2 , -L K -R K2 And, -R K3 , -L K -R K3 And, -R K4 , -L K -R K4 And, -R K5 , or -L K -R K5 and; -R K1 is a linear or branched saturated C 1-7 Alkyl; and optionally -F, -OH, -OR KK -OCH2CH2OCH3, -O-phenyl, -C(=O)OH, -C(=O)OR KK -NH2, -NHR KK , and -NR KK Substituted with one or more elements selected from 2; Each-R K2 C is independent 3-6 It is cycloalkyl; and optionally -F and -R KK -CF3, -OH, -OR KK -NH2, -NHR KK , and -NR KK Substituted with one or more elements selected from 2; Each-R K3 These are independently non-aromatic C 3-7 It is a heterocycline; and: Carbon is -F and -R as desired. KK -CF3, -OH, -OR KK -NH2, -NHR KK , and -NR KK It is replaced by one or more elements selected from 2; and Upon request, if available, secondary nitrogen, -R KK -C(=O)R KK , -C(=O)OR KK , and -S(=O)2R KK It is substituted with a group selected from; Each-R K4 is phenyl; and optionally -F, -Cl, and -R KK -CF3, -OH, -OR KK -NH2, -NHR KK , and -NR KK Substituted with one or more elements selected from 2; Each-R K5 C is independent 5-6 It is a heteroaryl; and: Carbon is -F and -R as desired. KK -CF3, -OH, -OR KK -NH2, -NHR KK , and -NR KK It is replaced by one or more elements selected from 2; and Upon request, if available, secondary nitrogen, -R KK -C(=O)R KK , -C(=O)OR KK , and -S(=O)2R KK It is substituted with a group selected from; Each-L K - indicates a straight-chain or branched saturated C 1-4 It is an alkylene, optionally substituted with one or more -F groups; Each-R KK is a linear or branched saturated C 1-4 It is alkyl; and: -R Q1NP It has at least one N-ring atom, and C is bonded via the N-ring atom. 3-11 It is a heterocycline; and: If desired, if present, sulfur is substituted with one or two =O groups; Carbon can be added as desired -R Q1NPP -F, -OH, -OR Q1NPP, and are substituted with one or more bases selected from =O; and Upon request, if available, secondary nitrogen, -R Q1NPP And, -R Q1NPPX -C(=O)R Q1NPP , -C(=O)OR Q1NPP -C(=O)NH2, -C(=O)NHR Q1NPP -C(=O)NR Q1NPP 2, and -S(=O)2R Q1NPP It is substituted with a group selected from; Each-R Q1NPP These are independently linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 Heteroaryl, or C 5-6 Heteroaryl-C 1-3 It is alkyl, and here, C 1-4 Alkyl groups are optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; -R Q1NPPX is a linear or branched saturated C 1-4 It is a haloalkyl; and: Each-R Q2C Independently: -F, -R Q2CC ,-R Q2CX , -OH, -OR Q2CC , -OR Q2CX , -NH2, -NHR Q2CC , -NR Q2CC 2, -R Q2CM , -NHC(=O)R Q2CC , -NHC(=O)OR Q2CC , -C(=O)NH2, -C(=O)NHR Q2CC -C(=O)NR Q2CC 2. -C(=O)R Q2CM , -C(=O)OH, -C(=O)OR Q2CC , -OC(=O)R Q2CC , -OC(=O)NH2, -OC(=O)NHR Q2CC -OC(=O)NR Q2CC 2. -OC(=O)R Q2CM ,or =O and; Here: Each-R Q2CC These are independently linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, phenyl, C 3-7 Heterocyclyl, phenyl-C 1-3 Alkyl, C 5-6 Heteroaryl, or C 5-6 Heteroaryl-C 1-3 It is alkyl, and here, C 1-4 Alkyl groups are optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; Each-R Q2CX These are independently linear or branched saturated C 1-4 It is a haloalkyl; Each-R Q2CM Each independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C 3-11 It is a heterocycline; and: If desired, one or more carbon atoms are added as a group -R Q2CMM It has been replaced with; If desired, if present, sulfur is substituted with one or two =O groups; and Upon request, if available, secondary nitrogen, -RQ2CMM -C(=O)R Q2CMM , -C(=O)OR Q2CMM -C(=O)NH2, -C(=O)NHR Q2CMM -C(=O)NR Q2CMM 2, and -S(=O)2R Q2CMM It is substituted with a group selected from; and Each-R Q2CMM These are independently linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 Heteroaryl, or C 5-6 Heteroaryl-C 1-3 It is alkyl, and here, C 1-4 Alkyl groups are optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; and: Each-R Q2N Independently: -R Q2NC , -C(=O)R Q2NC , -C(=O)-L Q2N -OH, -C(=O)-L Q2N -OR Q2NC , -C(=O)-L Q2N -NH2, -C(=O)-L Q2N -NHR Q2NC -C(=O)-L Q2N -NR Q2NC 2. -C(=O)-L Q2N -R Q2NM , -C(=O)OR Q2NC , -L Q2N -NH2, -L Q2N -NHR Q2NC , -L Q2N -NRQ2NC 2, -L Q2N -R Q2NM , -C(=O)NH2, -C(=O)NHR Q2NC -C(=O)NR Q2NC 2. -C(=O)R Q2NM , -L Q2N -C(=O)NH2, -L Q2N -C(=O)NHR Q2NC , -L Q2N -C(=O)NR Q2NC 2, -L Q2N -C(=O)R Q2NM ,or -S(=O)2R Q2NC and; Here: Each-R Q2NC These are independently linear or branched saturated C 1-6 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 Heteroaryl, or C 5-6 Heteroaryl-C 1-3 It is alkyl, and here, C 1-6 Alkyl groups are optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; Each-L Q2N - is independently linear or branched saturated C 1-4 It is alkylene; Each-R Q2NM Each independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C 3-11 It is a heterocycline; and: If desired, one or more carbon atoms are added as a group -R Q2NMM It has been replaced with; If desired, if present, sulfur is substituted with one or two =O groups; and Upon request, if available, secondary nitrogen, -R Q2NMM -C(=O)R Q2NMM , -C(=O)OR Q2NMM -C(=O)NH2, -C(=O)NHR Q2NMM -C(=O)NR Q2NMM 2, and -S(=O)2R Q2NMM It is substituted with a group selected from; and Each-R Q2NMM These are independently linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 Heteroaryl, or C 5-6 Heteroaryl-C 1-3 It is alkyl, and here, C 1-4 Alkyl groups are optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; and: Each-R Q3C Independently: -F, -Cl, -Br, -I, -R Q3CC , -R Q3CX , -OR Q3CX , -OH, -OR Q3CC , -L Q3C -OH, -L Q3C -OR Q3CC , -NH2, -NHR Q3CC , -NR Q3CC 2, -R Q3CM , -L Q3C -NH2, -L Q3C -NHR Q3CC , -L Q3C -NR Q3CC 2, -LQ3C -R Q3CM , -NHC(=O)R Q3CC , -NHC(=O)OR Q3CC , -L Q3C -NHC(=O)R Q3CC , -L Q3C -NHC(=O)OR Q3CC , -C(=O)NH2, -C(=O)NHR Q3CC -C(=O)NR Q3CC 2. -C(=O)R Q3CM , -L Q3C -C(=O)NH2, -L Q3C -C(=O)NHR Q3CC , -L Q3C -C(=O)NR Q3CC 2, -L Q3C -C(=O)R Q3CM , -C(=O)OH, -C(=O)OR Q3CC , -OC(=O)R Q3CC , -OC(=O)NH2, -OC(=O)NHR Q3CC -OC(=O)NR Q3CC 2. -OC(=O)R Q3CM , -CN, or -NO2 and; Two adjacent -R Q3C If it exists, then it will be united as one (CH2) n3 -O-(CH2) m3 -or -O-(CH2) p3 -O- is formed, where n3 is 0, 1, 2, or 3; m3 is 0, 1, 2, or 3; and p3 is 1 or 2; however m3+n3 is 2 or 3; Here: Each-R Q3CC These are independently linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, C 3-7Heterocyclyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 Heteroaryl, or C 5-6 Heteroaryl-C 1-3 It is alkyl, and here, C 1-4 Alkyl groups are optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; Each-R Q3CX These are independently linear or branched saturated C 1-4 It is a haloalkyl; Each-L Q3C - is independently linear or branched saturated C 1-4 It is alkylene; Each-R Q3CM Each independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C 3-11 It is a heterocycline; and: If desired, one or more carbon atoms are added as a group -R Q3CMM It has been replaced with; If desired, if present, sulfur is substituted with one or two =O groups; and Upon request, if available, secondary nitrogen, -R Q3CMM -C(=O)R Q3CMM , -C(=O)OR Q3CMM -C(=O)NH2, -C(=O)NHR Q3CMM -C(=O)NR Q3CMM 2, and -S(=O)2R Q3CMM It is substituted with a group selected from; and Each-R Q3CMM These are independently linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 Heteroaryl, or C 5-6 Heteroaryl-C 1-3It is alkyl, and here, C 1-4 Alkyl groups are optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; and: Each-R Q4C Independently: -F, -R Q4CC And, -R Q4CX , -OH, -OR Q4CC , -OR Q4CX , -NH2, -NHR Q4CC , -NR Q4CC 2, -R Q4CM , -NHC(=O)R Q4CC , -NHC(=O)OR Q4CC , -C(=O)NH2, -C(=O)NHR Q4CC -C(=O)NR Q4CC 2. -C(=O)R Q4CM , -C(=O)OH, -C(=O)OR Q4CC , -OC(=O)R Q4CC , -OC(=O)NH2, -OC(=O)NHR Q4CC -OC(=O)NR Q4CC 2. -OC(=O)R Q4CM ,or =O and; Here: Each-R Q4CC These are independently linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, C 3-7 Heterocyclyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 Heteroaryl, or C 5-6 Heteroaryl-C1-3 It is alkyl, and here, C 1-4 Alkyl groups are optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; Each-R Q4CX These are independently linear or branched saturated C 1-4 It is a haloalkyl; Each-R Q4CM Each independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C 3-11 It is a heterocycline; and: If desired, one or more carbon atoms are added as a group -R Q4CMM It has been replaced with; If desired, if present, sulfur is substituted with one or two =O groups; and Upon request, if available, secondary nitrogen, -R Q4CMM -C(=O)R Q4CMM , -C(=O)OR Q4CMM -C(=O)NH2, -C(=O)NHR Q4CMM -C(=O)NR Q4CMM 2, and -S(=O)2R Q4CMM It is substituted with a group selected from; Each-R Q4CMM These are independently linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 Heteroaryl, or C 5-6 Heteroaryl-C 1-3 It is alkyl, and here, C 1-4 Alkyl groups are optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; and: Each-R Q5C Independently: -F, -OH, -OR Q5CC , -OCF3, -NH2, -NHR Q5CC , -NR Q5CC 2, -R Q5CM , -NHC(=O)R Q5CC , -NHC(=O)OR Q5CC , -C(=O)NH2, -C(=O)NHR Q5CC -C(=O)NR Q5CC 2. -C(=O)R Q5CM , -C(=O)OH, -C(=O)OR Q5CC , -OC(=O)R Q5CC , -OC(=O)NH2, -OC(=O)NHR Q5CC -OC(=O)NR Q5CC 2, or -OC(=O)R Q5CM and; Here: Each-R Q5CC These are independently linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, C 3-7 Heterocyclyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 Heteroaryl, or C 5-6 Heteroaryl-C 1-3 It is alkyl, and here, C 1-4 Alkyl groups are optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; Each-R Q5CM Each independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C 3-11It is a heterocycline; and: If desired, one or more carbon atoms are added as a group -R Q5CMM It has been replaced with; If desired, if present, sulfur is substituted with one or two =O groups; and Upon request, if available, secondary nitrogen, -R Q5CMM -C(=O)R Q5CMM , -C(=O)OR Q5CMM -C(=O)NH2, -C(=O)NHR Q5CMM -C(=O)NR Q5CMM 2, and -S(=O)2R Q5CMM It is substituted with a group selected from; Each-R Q5CMM These are independently linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 Heteroaryl, or C 5-6 Heteroaryl-C 1-3 It is alkyl, and here, C 1-4 Alkyl groups are optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2. A compound or its pharmaceutically acceptable salt or solvate.

[0050] To avoid suspicion: The central amide group, -NH-C(=O)-, linking rings A and B is intended to have an unsubstituted nitrogen atom.

[0051] The meta-OH substituent on ring A is intended to be unsubstituted.

[0052] It is intended that ring B does not condense with any other ring.

[0053] "C 9-10 "Heteroaryl", "C 3-7 The exponent "C" in terms such as "heterocycline" x-y "C6" refers to the number of ring atoms, which may be carbon atoms or heteroatoms (e.g., N, O, S depending on the case). For example, pyridyl is an example of a C6 heteroaryl group, and piperidino is an example of a C6 heterocyclyl group.

[0054] The term "heteroaryl" refers to a group that is bonded to the rest of a molecule by an atom that is part of an aromatic ring, where the aromatic ring is part of an aromatic ring system, and the aromatic ring system has one or more heteroatoms (e.g., N, O, S, as may be the case). Unless otherwise specified, heteroaryls can be bonded via a ring carbon or ring nitrogen atom. For example, pyridyl is an example of a C6 heteroaryl group, and quinolyl (e.g., quinoline-2-yl, quinoline-7-yl, etc.) is C 10 Examples of heteroaryl groups. Furthermore, aromatic ring systems can be condensed with one or more non-aromatic rings, which may optionally contain only one or more heteroatoms (e.g., N, O, S) or only carbon atoms. For example, 4,5,6,7-tetrahydro-1H-indole-2-yl is an example of a C9 heteroaryl group; 4,5,6,7-tetrahydro-1H-pyrrolo[2,3-b]pyridine-2-yl is an example of a C9 heteroaryl group. Pyridyl and furan are C 5-6 This is an example of a heteroaryl compound.

[0055] The term "heterocyclyl" refers to a group comprising at least one non-aromatic ring system comprising one or more heteroatoms (e.g., optionally N, O, S), bonded to the rest of the molecule by an atom that is part of a non-aromatic ring system comprising one or more heteroatoms (e.g., optionally N, O, S). Unless otherwise specified, heterocyclyls may be bonded via a ring carbon or ring nitrogen atom. In some embodiments, the term "heterocyclyl" refers to a group bonded to the rest of the molecule via an atom that is part of a non-aromatic ring, where the non-aromatic ring is part of a non-aromatic ring system, and the non-aromatic ring system has one or more heteroatoms (e.g., optionally N, O, S). Unless otherwise specified, the sulfur ring atom may be substituted with one or two oxo (=O) groups (e.g., as in 1,1-dioxo-1,4-thiadinani-4-yl). Unless otherwise specified, "heterocyclyl" refers to monocyclic heterocyclyls (e.g., piperidinyl, an example of a monocyclic C6 heterocyclyl), condensed heterocyclyls (e.g., 3-azabicyclo[3.1.0]hexyl, an example of a condensed C6 heterocyclyl; decahydroquinolinyl, a condensed C6 heterocyclyl) 10 Examples of heterocyclils include cross-linked heterocyclils (e.g., 6-azabicyclo[3.1.1]heptanil and 2,5-diazabicyclo[2.2.1]heptane, examples of cross-linked C7 heterocyclils; 3,8-diazabicyclo[3.2.1]octanil, an example of a cross-linked C8 heterocyclil), and spiroheterocyclils (2,6-diazaspiro[3.3]heptane, an example of a spiroC7 heterocyclil; 7-azaspiro[3.5]nonyl, an example of a spiroC9 heterocyclil; 2,8-diazaspiro[4.5]decane, spiroC 10 Includes examples of heterocyclines. Tetrahydropyran and pyrrolidine are C 3-7 Examples of heterocyclyls are shown. Furthermore, non-aromatic ring systems can optionally be condensed with one or more aromatic rings that may contain only one or more heteroatoms (e.g., N, O, S) or carbon atoms. For example: 4,5,6,7-tetrahydro-1H-pyrrolo[2,3-b]pyridine-5-yl is an example of a C9 heterocyclyl group; 1,2,3,4-tetrahydroisoquinoline-3-yl is C 10Examples of heterocyclyl groups. 2,3-Dihydro-1-benzofuran is an example of a C9 heterocyclyl group in which a non-aromatic ring system is condensed with an aromatic ring. 3,4-Dihydro-2H-1,4-Benzoxazine and 2,3-Dihydro-1,4-Benzodioxin are examples of C9 heterocyclyl groups in which a non-aromatic ring system is condensed with an aromatic ring. 10 An example of a heterocyclyl group: "Non-aromatic C 3-7 Examples of "heterocyclines" include oxetanil, piperidine, pyrrolidine, tetrahydrofuran, tetrahydropyran, pyrrolidine, morpholinil, azetidine, and tetrahydrothiophene.

[0056] "A non-aromatic carbon having at least one N-ring atom and bonded via the N-ring atom" 3-11 A "heterocyclyl" comprises at least one non-aromatic ring system containing at least one N-ring atom, which is bonded to the rest of the molecule by the N-ring atom and may optionally contain one or more further heteroatoms (e.g., optionally N, O, S). Furthermore, the non-aromatic ring system may optionally condense with one or more aromatic rings which may contain only one or more heteroatoms (e.g., optionally N, O, S) or only carbon atoms. In one embodiment, the term "a non-aromatic C having at least one N-ring atom and bonded via the N-ring atom" is used. 3-11 A "heterocyclyl" is a heterocyclyl group that is bonded via an N-ring atom, but may have additional N-ring atoms. Examples include azilidino, azetidino, pyrrolidino, piperidino, piperazino, morpholino, thiomorpholino, azepano, and diazepano.

[0057] The term "carbocyclyl" refers to a ring system containing at least one non-aromatic carbon ring and consisting only of carbon atoms. Unless otherwise specified, "carbocyclyl" includes monocyclic carbocyclyls (e.g., cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl), bicyclic carbocyclyls (e.g., 2,3-dihydro-1H-indene), condensed carbocyclyls (e.g., 7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene, the core scaffold of estradiol), cross-linked carbocyclyls (e.g., 1,2,3,4-tetrahydro-1,4-methanonaphthalene), and spirocarbocyclyls (e.g., 3',4'-dihydro-2'H-spiro[cyclopentane-1,1'-naphthalene]).

[0058] The term "haloalkyl" refers to an alkyl group substituted with one or more halo groups (e.g., -F, -Cl, -Br, -I). The term "fluoroalkyl" refers to an alkyl group substituted with one or more -F groups. For example, -CF3 and -CHF2 are examples of C1 fluoroalkyl groups; -CH2CF3 and -CH2CHF2 are examples of C2 fluoroalkyl groups.

[0059] The term “C 1-4 "Alkylene" refers to an alkyl group having two bonding points. For example, -CH2- is an example of a C1 alkylene group; -CH2CH2- and -CH(CH3)- are examples of C2 alkylene groups; and -CH2CH2CH2- and -CH(CH3)2- are examples of C3 alkylene groups.

[0060] C 1-7 Alkyl, C 1-6 Alkyl and C 1-4 Examples of alkyl groups include methyl, ethyl, propyl, isopropyl, and butyl. 3-6 Examples of cycloalkyl groups include cyclopropyl and cyclohexyl. 3-6 Cycloalkyl-C 1-3 Examples of alkyl groups include cyclopropylmethyl and cyclohexylethyl. Phenylen-C 1-3Examples of alkyl groups include benzyl and 2-phenylpropyl. 5-6 Heteroaryl-C 1-3 Examples of alkyl groups include pyrimidine-2-ylmethyl and thiazole-4-ylethyl. 2-6 Examples of alkenyls include ethenyl and propenyl.

[0061] The term "one or more groups" in the context of arbitrary substituents (e.g., "one or more groups - R") AR1C The group(s) are necessarily constrained by the parent moiety and the number of suitable substitution positions present on it. In one parent moiety (e.g., tetrazolyl), only one substitution position is available. However, in another parent moiety, there may be several positions (e.g., phenyl has five). Except when constrained by the parent moiety, the group(s) may be, for example, one, two, three, four, etc., but more preferably one, two, or three, even more preferably one or two, and still more preferably one.

[0062] The term "carbon substituent" is intended to refer to a substituent bonded to a carbocyclic atom. Similarly, the term "secondary nitrogen substituent" is intended to refer to a substituent bonded to a nitrogen ring atom that, in the absence of a substituent, is a secondary nitrogen ring atom (i.e., -NH-). Consequently, as shown in the figure below, the pyridyl group can only have "carbon substituents," while 1H-pyrrole can have both "carbon substituents" and "secondary nitrogen substituents." [ka]

[0063] Similarly, as shown in the figure below, a piperidino group can only have a "carbon substituent," while piperidino can have both a "carbon substituent" and a "secondary nitrogen substituent." [ka]

[0064] Some groups, despite having a carbocyclic atom, may not have any carbocyclic atoms available for substitution. For example, as shown in the figure below, a tetrazolyl group may only be able to have a "carbon substituent" or only a "secondary nitrogen substituent." [ka]

[0065] Unless otherwise specified, when a compound having one or more chiral centers and capable of two or more stereoisomers is shown or described, all such stereoisomers are disclosed and included individually (e.g., as isolates from other stereoisomers) and in mixtures (e.g., equimolar or equomolar mixtures of two or more stereoisomers). For example, unless otherwise specified, when a compound has one chiral center, both the (R) and (S) enantiomers are disclosed and included individually (e.g., as isolates from other enantiomers) and in mixtures (e.g., equimolar or equomolar mixtures of two enantiomers). For example, when the first carbon atom of a side-chain sec-butyl group, -CH(CH3)CH2CH3, is usually chiral and therefore the only chiral center, stereoisomers, e.g., (R) and (S) enantiomers, are produced, each of which is disclosed and included.

[0066] Group-R A11 (3) A compound of (1) or (2), wherein: -R A11 ha-R A111 , -F, -Cl, -Br, -I, -CF3, -CHF2, -OH, -OR A111 It is either -OCF3 or -CN.

[0067] (4) A compound of (1) or (2), wherein: -R A11 ha-R A111 , -F, -Cl, -Br, -I, -CF3, -CHF2, -OH, -OR A111 , or -OCF3.

[0068] (5) A compound of (1) or (2), wherein: -R A11 ha-R A111 , -F, -Cl, -Br, -I, -CF3, -OH, -OR A111 , or -OCF3.

[0069] (6) A compound of (1) or (2), wherein: -R A11 ha-R A111 -F, -Cl, -Br, -I, -OH, or -OR A111 That is the case.

[0070] (7) A compound of (1) or (2), wherein: -R A11 ha-R A111 It is -F, -Cl, -Br, -I, or -OH.

[0071] (8) A compound of (1) or (2), wherein: -R A11 ha-R A111 It is -F, -Cl, or -OH.

[0072] (9) A compound of (1) or (2), where: -R A11 ha-R A111 It is -F or -Cl.

[0073] (10) A compound of (1) or (2), where: -R A11 ha-R A111 That is the case.

[0074] (11) A compound of (1) or (2), where: -R A11 ha-R A111 It is -F, -Cl, or -Br.

[0075] (12) A compound of (1) or (2), where: -RA11 It is -F.

[0076] (13) A compound of (1) or (2), where: -R A11 It is -Cl.

[0077] (14) A compound of (1) or (2), where: -R A11 It is -Br.

[0078] (11) (15) A compound of (1) or (2), where: -R A11 ha-R A111 , or -Br.

[0079] Group-R A111 (16) Any compound from (1) to (15), where: -R A111 The options are -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0080] (17) A compound of any of (1) to (15), where: -R A111 The options are -Me, -Et, -nPr, or -iPr.

[0081] (18) A compound of any of (1) to (15), where: -R A111 is either -Me or -Et.

[0082] (19) A compound of any of (1) to (15), where: -R A111 It is -Me.

[0083] (20) A compound of any of (1) to (15), where: -R A111 is -Et.

[0084] Group-R A22 (21) A compound of any of (1) to (20), where: -R A22 ha-R A222 , -F, -Cl, -Br, -I, -CF3, -CHF2, -OH, -OR A222 It is either -OCF3 or -CN.

[0085] (22) A compound of any of (1) to (20), where: -R A22 ha-R A222 , -F, -Cl, -Br, -I, -CF3, -CHF2, -OH, -OR A222 , or -OCF3.

[0086] (23) A compound of any of (1) to (20), where: -R A22 ha-R A222 , -F, -Cl, -Br, -I, -CF3, -OH, -OR A222 , or -OCF3.

[0087] (24) Any compound from (1) to (20), where: -R A22 ha-R A222 -F, -Cl, -Br, -I, -OH, or -OR A222 That is the case.

[0088] (25) Any compound from (1) to (20), where: -R A22 ha-R A222 It is -F, -Cl, -Br, -I, or -OH.

[0089] (26) Any compound from (1) to (20), where: -R A22 ha-R A222 It is -F, -Cl, or -OH.

[0090] (27) Any compound from (1) to (20), where: -R A22 ha-R A222 It is -F or -Cl.

[0091] (28) Any compound from (1) to (20), where: -R A22 ha-R A222 That is the case.

[0092] (29) Any compound from (1) to (20), where: -R A22 It is -Cl.

[0093] (30) A compound of any of (1) to (20), where: -R A22 ha-R A222 It is -F, -Cl, or -Br.

[0094] (31) Any compound from (1) to (20), where: -R A22 It is -F.

[0095] (32) Any compound from (1) to (20), where: -R A22 It is -Br.

[0096] Group-R A222 (33) A compound of any of (1) to (32), where: Each-R A222 If it exists, then linear saturated C 1-4 It is alkyl.

[0097] (34) Any compound from (1) to (32), where: Each-R A222 If they exist, they are -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0098] (35) A compound of any of (1) to (32), where: Each-R A222 If they exist, they are -Me, -Et, -nPr, or -iPr.

[0099] (36) Any compound from (1) to (32), where: Each-R A222 If it exists, it is either -Me or -Et.

[0100] (37) A compound of any of (1) to (32), where: Each-R A222 If it exists, it is -Me.

[0101] Group-R A3 (38) Any compound from (1) to (37), where: -R A3 is -H.

[0102] (39) A compound of any of (1) to (37), where: -R A3 ha-R A33 That is the case.

[0103] Group-R A33 (40) A compound of any of (1) to (37), where: -R A33 If it exists: -R A333 -F, -Cl, -Br, -I, -OH, or -OR A333 That is the case.

[0104] (41) A compound of any of (1) to (37), where: -R A33 If it exists: -R A333 It is -F, -Cl, -Br, -I, or -OH.

[0105] (42) Any compound from (1) to (37), where: -R A33 If it exists: -R A333 It is -F, -Cl, or -OH.

[0106] (43) A compound of any of (1) to (37), where: -R A33 If it exists: -R A333 It is -F or -Cl.

[0107] (44) A compound of any of (1) to (37), where: -R A33 If it exists: -R A333 That is the case.

[0108] (45) A compound of any of (1) to (37), where: -R A33 If it exists: It is -Cl.

[0109] (46) A compound of any of (1) to (37), where: -R A33 If it exists: -Br

[0110] Group-R A333 (47) A compound of any of (1) to (37), where: Each-R A333 If they exist, they are -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0111] (48) Any compound from (1) to (37), where: Each-R A333 If they exist, they are -Me, -Et, -nPr, or -iPr.

[0112] (49) A compound of any of (1) to (37), where: Each-R A333 If it exists, it is either -Me or -Et.

[0113] (50) A compound of any of (1) to (37), where: Each-R A333 If it exists, it is -Me.

[0114] Group-R A4 (51) A compound of any of (1) to (50), where: -R A4 is -H.

[0115] (52) Any compound from (1) to (50), where: -R A4 ha-R A44 That is the case.

[0116] Group-R A44 (53) A compound of any of (1) to (52), where: -R A44 If it exists: -R A444 -F, -Cl, -Br, -I, -OH, or -OR A444 That is the case.

[0117] (54) A compound of any of (1) to (52), where: -R A44 If it exists: -R A444 It is -F, -Cl, -Br, -I, or -OH.

[0118] (55) Any compound from (1) to (52), where: -R A44 If it exists: -R A444It is -F, -Cl, or -OH.

[0119] (56) Any compound from (1) to (52), where: -R A44 If it exists: -R A444 It is -F or -Cl.

[0120] (57) A compound of any of (1) to (52), where: -R A44 If it exists: -R A444 That is the case.

[0121] (58) A compound of any of (1) to (52), where: -R A44 If it exists: It is -Cl.

[0122] (59) A compound of any of (1) to (52), where: -R A44 If it exists: -R A444 It is -Cl or -Br.

[0123] Group-R A444 (60) A compound of any of (1) to (59), where: Each-R A444 If it exists, then linear saturated C 1-4 It is alkyl.

[0124] (61) A compound of any of (1) to (59), where: Each-R A444 If they exist, they are -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0125] (62) Any compound from (1) to (59), where: Each-R A444If they exist, they are -Me, -Et, -nPr, or -iPr.

[0126] (63) Any compound from (1) to (59), where: Each-R A444 If it exists, it is either -Me or -Et.

[0127] (64) Any compound from (1) to (59), where: Each-R A444 If it exists, it is -Me.

[0128] Ring B (65) Any compound from (1) to (64), where: Ring B is: [ka] That is the case.

[0129] (66) Any compound from (1) to (64), where: Ring B is: [ka] That is the case.

[0130] (67) Any compound from (1) to (64), where: Ring B is: [ka] That is the case.

[0131] (68) Any compound of (1) to (64), where: Y 1 If it exists, it is S, O, or NH; Y 2 If it exists, it is CH or N; Y 3 If it exists, it is N or CH; Y4 If it exists, it is N or CH; Y 5 If it exists, it is S, O, or NH; Y 6 If it exists, it is N or CH; Y 7 If it exists, it is N or CH; Y 8 If it exists, it is N or CH; and Y 9 If it exists, it is S, O, or NH.

[0132] For example, ring B is: [ka] Selected from.

[0133] (69) Any compound from (1) to (64), where: Y 1 If it exists, then it is S; Y 2 If they exist, then CH, CR Y2 , or N; Y 3 If present, N, CH, or CR Y3 and; Y 4 If present, N, CH, or CR Y4 and; Y 5 If it exists, then it is S; Y 6 If present, N, CH, or CR Y6 and; Y 7 If present, N, CH, or CR Y7 and; Y 8 If present, N, CH, or CR Y8 and Y 9 If it exists, then it is S.

[0134] (70) A compound of any of (1) to (64), where: Y 1 If it exists, then it is S; Y 2 If it exists, it is CH or N; Y 3 If it exists, it is N or CH; Y 4 If it exists, it is N or CH; Y 5 If it exists, then it is S; Y 6 If it exists, it is N or CH; Y 7 If it exists, it is N or CH; Y 8 If it exists, it is N or CH; and Y 9 If it exists, then it is S.

[0135] (71) A compound of any of (1) to (64), where: Y 1 If it exists, then it is S; Y 2 If they exist, then CH, CR Y2 , or N; Y 3 If present, N, CH, or CR Y3 and; Here, Y 2 and Y 3 Only one of them is N; Y 4 If present, N, CH, or CR Y4 and; Y 5 If it exists, then it is S; Y 6 If present, N, CH, or CR Y6 and; Here, Y 4 and Y 6 Only one of them is N; Y 7 If present, N, CH, or CR Y7 and; Y 8 If present, N, CH, or CR Y8 and; Y 9 If it exists, then it is S; and Here, Y 7 and Y 8 Only one of these is N.

[0136] (72) A compound of any of (1) to (64), where ring B is: [ka] That is the case.

[0137] (73) Any compound from (1) to (64), where: Y 1 If it exists, then it is S; Y 2 If they exist, then CH, CR Y2 , or N; Y 3 If present, N, CH, or CR Y3 and; Here, Y 2 and Y 3 Only one of them is N; Y 4 If it exists, then it is N; Y 5 If it exists, then it is S; Y 6 If present, CH or CR Y6 and; Y 7 If it exists, then it is N; Y 8 If present, CH or CR Y8 and Y 9 If it exists, then it is S.

[0138] (74) A compound of any of (1) to (64), where ring B is: [ka] That is the case.

[0139] (75) Any compound from (1) to (64), where: Y 1 If it exists, then it is S; Y 2 If they exist, then CH, CR Y2 , or N; Y 3 If present, N, CH, or CR Y3 and Here, Y 2 and Y 3 Only one of these is N.

[0140] (76) A compound of any of (1) to (64), where ring B is: [ka] That is the case.

[0141] (77) Any compound from (1) to (64), where: Y 1 If it exists, then it is S; Y 2 If present, CH or CR Y2 and; Y 3 If it exists, then it is N.

[0142] (78) A compound of any of (1) to (64), where ring B is: [ka] That is the case.

[0143] (79) Any compound from (1) to (64), where: Ring B is: [ka] Here: Y 1 is S or O; Y 2 CH, CR Y2 , or N; Y 3 It is N.

[0144] (80) A compound of any of (1) to (64), where: Ring B is: [ka] And here: Y 1 is S or O; Y 2 is CH or N; Y 3 It is N.

[0145] Group-R Y2 And, -R Y3 etc. (81) A compound of any of (1) to (80), where: Each-R Y2 And, -R Y3 And, -R Y4 And, -R Y6 And, -R Y7 , and -R Y8 If they exist, they exist independently: -F, -Cl, -Br, -I, and -R YY -CF3, -OH, -OR YY It is either -OCF3 or -NH2.

[0146] (82) A compound of any of (1) to (80), where: Each-R Y2 And, -R Y3 And, -R Y4And, -R Y6 And, -R Y7 , and -R Y8 If they exist, they exist independently: -F, -Cl, -Br, -I, and -R YY , or -NH2.

[0147] (83) A compound of any of (1) to (80), where: Each-R Y2 And, -R Y3 And, -R Y4 And, -R Y6 And, -R Y7 , and -R Y8 If they exist, they exist independently: -F, -Cl, and -R YY , or -NH2.

[0148] (84) Any compound from (1) to (80), where: Each-R Y2 And, -R Y3 And, -R Y4 And, -R Y6 And, -R Y7 , and -R Y8 If they exist, they exist independently: -H

[0149] (85) A compound of any of (1) to (80), where: Each-R Y2 And, -R Y3 And, -R Y4 And, -R Y6 And, -R Y7 , and -R Y8 If they exist, they exist independently: -F, -Cl, or -R YY That is the case.

[0150] (86) Any compound from (1) to (80), where: Each-R Y2 It is -NH2.

[0151] Group-R YY (87) A compound of any of (1) to (86), where: Each-R YY If it exists: The options are -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0152] (88) A compound of any of (1) to (86), where: Each-R YY If it exists: The options are -Me, -Et, -nPr, or -iPr.

[0153] (89) A compound of any of (1) to (86), where: Each-R YY If it exists: -Me or -Et

[0154] (90) A compound of any of (1) to (86), where: Each-R YY If it exists: -Me

[0155] Group-R Y1 And, -R Y5 , and -R Y9 (91) A compound of any of (1) to (90), where: Each-R Y1 And, -R Y5 , and -R Y9 If they exist, they exist independently: -R YYN Or -C(=O)R YYN That is the case.

[0156] (92) Any compound from (1) to (90), where: Each-R Y1 And, -R Y5 , and -RY9 If they exist, they exist independently: -R YYN That is the case.

[0157] Group-R YYN (93) A compound of any of (1) to (92), where: Each-R YYN If present, then independently of linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 The alkyl group is wherein each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0158] (94) Any compound from (1) to (92), where: Each-R YYN If present, then independently of linear or branched saturated C 1-4 The group is alkyl, phenyl, or phenyl-CH2-, where each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0159] (95) A compound of any of (1) to (92), where: Each-R YYN If present, then independently of linear or branched saturated C 1-4 It is alkyl, phenyl, or benzyl.

[0160] (96) A compound of any of (1) to (92), where: Each-R YYN If present, then independently of linear or branched saturated C 1-4 It is alkyl.

[0161] (97) A compound of any of (1) to (92), where: Each-R YYN If it exists, it is -Me.

[0162] Group-Q (98) A compound of any of (1) to (97), where: -Q is -Q 1 , -L Q1 -Q 1 ,-Q 2 , -L Q2 -Q 2 ,-Q 3 , -L Q3 -Q 3 ,-Q 4 , -L Q4 -Q 4 , or -Q 5 That is the case.

[0163] (99) A compound of any of (1) to (97), where: -Q is -Q 1 , -L Q1 -Q 1 ,-Q 2 , or -L Q2 -Q 2 That is the case.

[0164] (100) A compound of any of (1) to (97), where: -Q is -Q 1 or -L Q2 -Q 2 That is the case.

[0165] (101) A compound of any of (1) to (97), where: -Q is -Q 1 That is the case.

[0166] (102) A compound of any of (1) to (97), where: -Q is -L Q1 -Q 1 That is the case.

[0167] (103) A compound of any of (1) to (97), where: -Q is -Q 2 That is the case.

[0168] (104) (84) (1)~(97) is a compound of any of the above, where: -Q is -L Q2 -Q 2 That is the case.

[0169] (105) A compound of any of (1) to (97), where: -Q is -Q 3 That is the case.

[0170] (106) A compound of any of (1) to (97), where: -Q is -L Q3 -Q 3 That is the case.

[0171] (107) A compound of any of (1) to (97), where: -Q is -Q 4 That is the case.

[0172] (108) Any compound from (1) to (97), where: -Q is -L Q4 -Q 4 That is the case.

[0173] (109) A compound of any of (1) to (97), where: -Q is -Q 5 That is the case.

[0174] (110) Any compound from (1) to (97), where: -Q is -H

[0175] Group-Q 1 (111) A compound of any of (1) to (110), where: -Q 1 If it exists, C 5-9It is a heteroaryl; and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and If desired, and if available, secondary nitrogen is used as the base-R Q1N It has been replaced with.

[0176] (112) A compound of any of (1) to (110), where: -Q 1 If it exists, C 5-6 It is a heteroaryl; and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and If desired, and if available, secondary nitrogen is used as the base-R Q1N It has been replaced with.

[0177] (113) A compound of any of (1) to (110), where: -Q 1 If it exists, it is a C5 heteroaryl, and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and Upon request, secondary nitrogen is used as the base-R Q1N It has been replaced with.

[0178] (114) A compound of any of (1) to (110), where: -Q 1 If present, these are pyrazolyl, pyrrolyl, imidazolyl, triazolyl, tetrazolyl, furanyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, oxadiazolyl, or thiadiazolyl; and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and If desired, and if available, secondary nitrogen is used as the base-R Q1N It has been replaced with.

[0179] (115) A compound of any of (1) to (110), where: -Q 1 If present, these are pyrazolyl, pyrrolyl, imidazolyl, furanyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, oxadiazolyl, or thiadiazolyl; and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and If desired, and if available, secondary nitrogen is used as the base-R Q1N It has been replaced with.

[0180] (116) A compound of any of (1) to (110), where: -Q 1 If present, these are pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, oxadiazolyl, or thiadiazolyl; and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and If desired, and if available, secondary nitrogen is used as the base-R Q1N It has been replaced with.

[0181] (117) A compound of any of (1) to (110), where: -Q 1 If present, it is pyrazolyl (e.g., 1H-pyrazole-3-yl, 1H-pyrazole-4-yl, 1H-pyrazole-5-yl, or pyrazole-1-yl); and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and If desired, and if available, secondary nitrogen is used as the base-R Q1N It has been replaced with. [ka]

[0182] (118) Compounds of (1) to (110), where, -Q 1 If it exists, it is pyrazole-1-yl; Furthermore, if desired, one or more carbon atoms are added to any of the -R groups. Q1C It has been replaced with.

[0183] (119) Compounds of (1) to (110), where, -Q 1 If present, it is 1H-pyrazole-3-yl; and: If desired, one or more carbon atoms can be added to any of the -R groups. Q1C It is replaced by; and Upon request, secondary nitrogen is used as the base-R Q1N It has been replaced with.

[0184] (120) Compounds of (1) to (110), where, -Q 1 If present, it is 1H-pyrazole-4-yl; and: If desired, one or more carbon atoms can be added to any of the -R groups. Q1C It is replaced by; and Upon request, secondary nitrogen is used as the base-R Q1N It has been replaced with.

[0185] (121) Compounds of (1) to (110), where, -Q 1 If it exists, it is 1H-pyrazole-5-yl; and: If desired, one or more carbon atoms can be added to any of the -R groups. Q1C It is replaced by; and Upon request, secondary nitrogen is used as the base-R Q1N It has been replaced with.

[0186] (122) A compound of any of (1) to (110), where: -Q 1 If it exists, it is a C9 heteroaryl; and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and If desired, and if available, secondary nitrogen is used as the base-R Q1N It has been replaced with.

[0187] (123) A compound of any of (1) to (81105), where: -Q 1 If it exists, it is a C9 heteroaryl; Here, the C9 heteroaryl is a 5:6-condensed heteroaryl; and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and If desired, and if available, secondary nitrogen is used as the base-R Q1N It has been replaced with.

[0188] (124) A compound of any of (1) to (110), where: -Q 1 If present, these are indolyl, indazolyl, benzimidazolyl, benzoxazolyl, pyrazolopyridinyl, pyrazolopyridinyl, imidazopyridinyl, or pyrrolopyridinyl; and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and Upon request, secondary nitrogen is used as the base-R Q1N It has been replaced with.

[0189] (125) A compound of any of (1) to (110), where: -Q 1 If it exists, it is indole-2-yl or indole-3-yl; and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and Upon request, secondary nitrogen is used as the base-R Q1N It has been replaced with. [ka]

[0190] (126) A compound of any of (1) to (110), where: -Q 1 If present, it is 2H-indazole-3-yl or 1H-indazole-3-yl; and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and Upon request, secondary nitrogen is used as the base-R Q1N It has been replaced with. [ka]

[0191] (127) A compound of any of (1) to (110), where: -Q 1 If it exists, it is benzimidazole-2-yl; and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and Upon request, secondary nitrogen is used as the base-R Q1N It has been replaced with.

[0192] [ka] (128) A compound of any of (1) to (110), where: -Q 1 If it exists, it is benzoxazole-2-yl; and: If desired, one or more carbon atoms are added as a group -R Q1C It has been replaced with. [ka]

[0193] (129) A compound of any of (1) to (110), where: -Q 1 If present, it is pyrazolo[1,5-a]pyridine-2-yl or pyrazolo[1,5-a]pyridine-3-yl; and: If desired, one or more carbon atoms are added as a group -R Q1C It has been replaced with. [ka]

[0194] (130) A compound of any of (1) to (110), where: -Q 1 If present, it is 1H-pyrazolo[3,4-b]pyridine-3-yl, 1H-pyrazolo[3,4-c]pyridine-3-yl, 1H-pyrazolo[4,3-c]pyridine-3-yl, or 1H-pyrazolo[4,3-b]pyridine-3-yl; and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and Upon request, secondary nitrogen is used as the base-R Q1N It has been replaced with. [ka]

[0195] (131) A compound of any of (1) to (110), where: -Q 1 If present, it is imidazo[1,2-a]pyridine-2-yl or imidazo[1,2-a]pyridine-3-yl; and: If desired, one or more carbon atoms are added as a group -R Q1C It has been replaced with. [ka]

[0196] (132) A compound of any of (1) to (110), where: -Q 1 If present, it is 1H-pyrrolo[3,2-b]pyridine-2-yl or 1H-pyrrolo[3,2-b]pyridine-3-yl; and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and Upon request, secondary nitrogen is used as the base-R Q1N It has been replaced with. [ka]

[0197] (133) A compound of any of (1) to (110), where: -Q 1 If present, it is either 1H-pyrrolo[3,2-c]pyridine-2-yl or 1H-pyrrolo[3,2-c]pyridine-3-yl; and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and Upon request, secondary nitrogen is used as the base-R Q1N It has been replaced with. [ka]

[0198] (134) A compound of any of (1) to (110), where: -Q 1 If present, it is 1H-pyrrolo[2,3-c]pyridine-2-yl or 1H-pyrrolo[2,3-c]pyridine-3-yl; and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and Upon request, secondary nitrogen is used as the base-R Q1N It has been replaced with. [ka]

[0199] (135) A compound of any of (1) to (110), where: -Q 1 If present, it is pyrazolo[1,5-c]pyrimidine-2-yl, pyrazolo[1,5-c]pyrimidine-3-yl, pyrazolo[1,5-a]pyrimidine-2-yl, or pyrazolo[1,5-a]pyrimidine-3-yl; and: If desired, one or more carbon atoms are added as a group -R Q1C It has been replaced with. [ka]

[0200] (136) A compound of any of (1) to (110), where: -Q 1 If present, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, thiophenyl, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 6,7-dihydro-4H-pyrano[4,3-d]thiazolyl, imidazolyl, 1,3-benzoxazolyl, pyrazolo[1,5-a]pyridinyl, indazolyl, pyrazolo[4,3-b]pyridinyl, pyrimidinyl, pyrazolo[3,4-b]pyridinyl, pyrazolo[3,4-c]pyridinyl, 4,5,6,7-tetrahydro-1H-indazolyl, 1,4,5,6-tetrahydrocyclopenta [c]pyrazolyl, pyrazolo[4,3-c]pyridinyl, 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridinyl, 1,2,4-triazolyl, pyridinyl, pyrimidinyl, quinolinyl, isoquinolinyl, quinazolinyl, 1,8-naphthilidinyl, pyridadinyl, indolyl, 7H-pyrrolo[2,3-d]pyrimidinyl, 1,3-benzothiazolyl, thieno[2,3-d]pyrimidinyl, pyrrolo[2,1-f][1,2,4]triazinyl, benzofuranil, 1,5-naphthilidinyl, 1,7-naphthilidinyl, 2,7-naphthilidinyl, or 1,6-naphthilidinyl; and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and If desired, if present, add one or more secondary nitrogen atoms to the -R group. Q1N It has been replaced with.

[0201] Group-L Q1 - (137) A compound of any of (1) to (136), where: -L Q1 If it exists, -CH2-, -C(CH3)2-, -CH2CH2-, or -CH2CH2CH2-.

[0202] (138) A compound of any of (1) to (136), where: -L Q1 -If it exists, it is -CH2-, -CH2CH2-, or -CH2CH2CH2-.

[0203] (139) A compound of any of (1) to (136), where: -L Q1 -If it exists, it is -CH2-.

[0204] (140) A compound of any of (1) to (136), where: -L Q1 -If it exists, then it is -CH2CH2-.

[0205] (141) A compound of any of (1) to (136), where: -L Q1 -If it exists, then it is -CH2CH2CH2-.

[0206] Group-Q 2 (142) A compound of any of (1) to (141), where: -Q 2If present, these are azetidinil, pyrrolidinil, piperidinil, piperazinil, morpholinil, thiomorpholinil, azepanil, or diazepanil; and: If desired, if present, sulfur is substituted with one or two oxygen groups; If desired, one or more carbon atoms are added as a group -R Q2C It is replaced by; and If desired, if present, one or more secondary nitrogen atoms -R Q2N It has been replaced with.

[0207] (143) A compound of any of (1) to (141), where: -Q 2 If present, these are pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, or thiomorpholinyl; and: If desired, if present, sulfur is substituted with one or two oxygen groups; If desired, one or more carbon atoms are added as a group -R Q2C It is replaced by; and If desired, and if available, secondary nitrogen is used as the base-R Q2N It has been replaced with.

[0208] (144) A compound of any of (1) to (141), where: -Q 2 If present, it is piperidinyl or piperazinyl; and: If desired, one or more carbon atoms are added as a group -R Q2C It is replaced by; and If desired, and if available, secondary nitrogen is used as the base-R Q2N It has been replaced with.

[0209] (145) A compound of any of (1) to (141), where: -Q 2If present, it is piperidinyl (e.g., piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl); and: If desired, one or more carbon atoms are added as a group -R Q2C It is replaced by; and If desired, and if available, secondary nitrogen is used as the base-R Q2N It has been replaced with. [ka]

[0210] (146) A compound of any of (1) to (141), where: -Q 2 If present, it is piperidine-4-yl; and: If desired, one or more carbon atoms are added as a group -R Q2C It is replaced by; and Upon request, secondary nitrogen is used as the base-R Q2N It has been replaced with.

[0211] (147) A compound of any of (1) to (141), where: -Q 2 If it exists, it is piperazinyl (e.g., piperazine-1-yl, piperazine-2-yl); and: If desired, one or more carbon atoms are added as a group -R Q2C It is replaced by; and Upon request, secondary nitrogen is used as the base-R Q2N It has been replaced with. [ka]

[0212] (148) A compound of any of (1) to (141), where: -Q 2 If it exists, it is piperazine-1-yl; and: If desired, one or more carbon atoms are added as a group -R Q2C It is replaced by; and Upon request, secondary nitrogen is used as the base-R Q2N It has been replaced with. [ka]

[0213] (149) A compound of any of (1) to (141), where: -Q 2 If present, these are pyrrolidinyl, morpholinyl, piperidinyl, thiomorpholinyl, piperazinyl, 2,3-dihydro-1,4-benzodioxynyl, 3,4-dihydro-2H-1,4-benzoxazinyl, or 2,3-dihydro-1-benzofuranyl; and: If desired, if present, sulfur is substituted with one or two oxygen groups; If desired, if present, one or more secondary nitrogen atoms -R Q2N It has been replaced with.

[0214] Group-L Q2 - (150) A compound of any of (1) to (149), where: -L Q2 If it exists, -CH2-, -C(CH3)2-, -CH2CH2-, or -CH2CH2CH2-.

[0215] (151) A compound of any of (1) to (149), where: -L Q2 -If it exists, it is -CH2-, -CH2CH2-, or -CH2CH2CH2-.

[0216] (152) A compound of any of (1) to (149), where: -L Q2 - is -CH2- or -CH2CH2CH2- if it exists.

[0217] (153) A compound of any of (1) to (149), where: -L Q2 -If it exists, it is -CH2-.

[0218] (154) A compound of any of (1) to (149), where: -L Q2 -If it exists, then it is -CH2CH2-.

[0219] (155) A compound of any of (1) to (149), where: -L Q2 -If it exists, then it is -CH2CH2CH2-.

[0220] Group-Q 3 (156) A compound of any of (1) to (155), where: -Q 3 If it exists, it is phenyl; And, if desired, one or more base-R Q3C It has been replaced with.

[0221] (157) A compound of any of (1) to (155), where: -Q 3 If it exists, it is naphthyl; And, if desired, one or more base-R Q3C It has been replaced with.

[0222] Group-L Q3 - (158) A compound of any of (1) to (157), where: -L Q3 If it exists, -CH2-, -C(CH3)2-, -CH2CH2-, or -CH2CH2CH2-.

[0223] (159) A compound of any of (1) to (157), where: -L Q3 -If it exists, it is -CH2-, -CH2CH2-, or -CH2CH2CH2-.

[0224] (160) A compound of any of (1) to (157), where: -L Q3 - is -CH2- or -CH2CH2- if it exists.

[0225] (161) A compound of any of (1) to (157), where: -L Q3 -If it exists, it is -CH2-.

[0226] (162) A compound of any of (1) to (157), where: -L Q3 -If it exists, then it is -CH2CH2-.

[0227] (163) A compound of any of (1) to (157), where: -L Q3 -If it exists, then it is -CH2CH2CH2-.

[0228] Group-Q 4 (164) A compound of any of (1) to (163), where: -Q 4 If present, these are cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl; And, if desired, one or more base-R Q4C It has been replaced with.

[0229] (165) A compound of any of (1) to (163), where: -Q 4 If present, it is cyclopropyl; And, if desired, one or more base-R Q4CIt has been replaced with.

[0230] (166) A compound of any of (1) to (163), where: -Q 4 If it exists, it is cyclobutyl; And, if desired, one or more base-R Q4C It has been replaced with.

[0231] (167) A compound of any of (1) to (163), where: -Q 4 If it exists, it is cyclopentyl; And, if desired, one or more base-R Q4C It has been replaced with.

[0232] (168) A compound of any of (1) to (163), where: -Q 4 If it exists, it is cyclohexyl; And, if desired, one or more base-R Q4C It has been replaced with.

[0233] (169) A compound of any of (1) to (163), where: -Q 4 If present, it is cyclopropyl or cyclohexyl; And, if desired, one or more base-R Q4C It has been replaced with.

[0234] Group-L Q4 - (170) A compound of any of (1) to (169), where: -L Q4 If it exists, -CH2-, -C(CH3)2-, -CH2CH2-, or -CH2CH2CH2-.

[0235] (171) A compound of any of (1) to (169), where: -LQ4 -If it exists, it is -CH2-, -CH2CH2-, or -CH2CH2CH2-.

[0236] (172) Any compound from (1) to (169), where: -L Q4 -If it exists, it is -CH2-.

[0237] (173) A compound of any of (1) to (169), where: -L Q4 -If it exists, then it is -CH2CH2-.

[0238] (174) A compound of any of (1) to (169), where: -L Q4 -If it exists, then it is -CH2CH2CH2-.

[0239] Group-Q 5 (175) A compound of any of (1) to (174), where: -Q 5 If present, these are -Me, -Et, -nPr, -iPr, -nBu, -iBu, -sBu, -tBu, n-pentyl, iso-pentyl, neo-pentyl, n-hexyl, isohexyl, or 3,3-dimethylbutyl; And, if desired, one or more base-R Q5C It has been replaced with.

[0240] (176) A compound of any of (1) to (174), where: -Q 5 If present, linear or branched saturated C 1-4 It is alkyl; And, if desired, one or more base-R Q5C It has been replaced with.

[0241] (177) A compound of any of (1) to (174), where: -Q5 If it exists, it is -Me, -Et, or -nPr; And, if desired, one or more base-R Q5C It has been replaced with.

[0242] (178) A compound of any of (1) to (174), where: -Q 5 If it exists, -CH2-R Q5C ,-CH2CH2-R Q5C , or -CH2CH2CH2-R Q5C That is the case.

[0243] (179) A compound of any of (1) to (174), where: -Q 5 If it exists, -CH2-R Q5C That is the case.

[0244] (180) A compound of any of (1) to (174), where: -Q 5 If it exists, then -CH2CH2-R Q5C That is the case.

[0245] (181) A compound of any of (1) to (174), where: -Q 5 If it exists, then -CH2CH2CH2-R Q5C That is the case.

[0246] (182) A compound of any of (1) to (174), where: -Q 5 If present, these are -Me, -Et, -nPr, or 3,3-dimethylbutyl; If desired, one or more base-R Q5C It has been replaced with.

[0247] Group-R Q1C (183) A compound of any of (1) to (182), where: Each-RQ1C If they exist, they exist independently: -F, -Cl, -Br, -I, -R Q1CC , -R Q1CX , -OR Q1CX , -OH, -OR Q1CC , -L Q1C -OH, -L Q1C -OR Q1CC , -NH2, -NHR Q1CC , -NR Q1CC 2, -R Q1CM , -L Q1C -NH2, -L Q1C -NHR Q1CC , -L Q1C -NR Q1CC 2, -L Q1C -R Q1CM , -C(=O)NH2, -C(=O)NHR Q1CC -C(=O)NR Q1CC 2. -C(=O)R Q1CM , -C(=O)OH, or -C(=O)OR Q1CC , -S(=O)2R Q1CC , or -CN and; Two adjacent -R Q1C If it exists, then it becomes one with -(CH2) n1 -O-(CH2) m1 -or -O-(CH2) p1 It can form -O-

[0248] (184) A compound of any of (1) to (182), where: Each-R Q1C If they exist, they exist independently: -F, -Cl, -Br, -I, -R Q1CC , -R Q1CX , -OR Q1CX , -OH, -OR Q1CC, -NH2, -NHR Q1CC , -NR Q1CC 2, -R Q1CM , -C(=O)NH2, -C(=O)NHR Q1CC -C(=O)NR Q1CC 2. -C(=O)R Q1CM , -C(=O)OH, or -C(=O)OR Q1CC That is the case.

[0249] (185) A compound of any of (1) to (182), where: Each-R Q1C If they exist, they exist independently: -R Q1CC , -R Q1CX , -NH2, -NHR Q1CC , -NR Q1CC 2, -R Q1CM , -C(=O)NH2, -C(=O)NHR Q1CC -C(=O)NR Q1CC 2. -C(=O)R Q1CM , -C(=O)OH, or -C(=O)OR Q1CC That is the case.

[0250] (186) A compound of any of (1) to (182), where: Each-R Q1C If they exist, they exist independently: -R Q1CC , -R Q1CX ,or -C(=O)OR Q1CC That is the case.

[0251] (187) A compound of any of (1) to (182), where: Each-R Q1C If it exists: -R Q1CC That is the case.

[0252] (188) A compound of any of (1) to (182), where: Each-R Q1C If they exist, they exist independently: -F, -Cl, -Br, -R Q1CC , -R Q1CX , -OR Q1CX , -OH, -OR Q1CC , -NH2, -NHR Q1CC , -NR Q1CC 2, -R Q1CM , -L Q1C -R Q1CM , -NHC(=O)R Q1CC , -N(R Q1CC )C(=O)R Q1CC , -NHC(=O)OR Q1CC , -C(=O)NH2, -C(=O)NHR Q1CC -C(=O)NR Q1CC 2. -C(=O)R Q1CM ,=O, -NHC(=O)NHR Q1CC , -L Q1C -C(=O)NR Q1CC 2 -C(=O)OH, -C(=O)OR Q1CC , -OC(=O)NH2, -S(=O)2R Q1CX , -S(=O)2R Q1CM , -NHS(=O)R Q1CC , -NHS(=O)2R Q1CC , -CN, or -C≡CH.

[0253] (189) A compound of any of (1) to (182), where: Each-R Q1C If they exist, they exist independently: -F, -Cl, -R Q1CC , -R Q1CX , -OR Q1CC , -NR Q1CC 2, -R Q1CM , -NHC(=O)R Q1CC ,or -L Q1C -C(=O)NR Q1CC The answer is 2.

[0254] Group-R Q1CC (190) A compound of any of (1) to (189), where: Each-R Q1CC If present, then independently of linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 The alkyl group is wherein each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0255] (191) A compound of any of (1) to (189), where: Each-R Q1CC If present, then independently of linear or branched saturated C 1-4 The group is alkyl, phenyl, or phenyl-CH2-, where each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0256] (192) A compound of any of (1) to (189), where: Each-R Q1CC If present, then independently of linear or branched saturated C 1-4 It is alkyl, phenyl, or benzyl.

[0257] (193) A compound of any of (1) to (189), where: Each-R Q1CC If present, then independently of linear or branched saturated C 1-4 It is alkyl.

[0258] (194) A compound of any of (1) to (189), where: Each-R Q1CC If they exist, they are independently -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0259] (195) A compound of any of (1) to (189), where: Each-R Q1CC If they exist, they are independently -Me, -Et, -nPr, or -iPr.

[0260] (196) A compound of any of (1) to (189), where: Each-R Q1CC If they exist, they are independently -Me or -Et.

[0261] (197) A compound of any of (1) to (189), where: Each-R Q1CC If it exists, it is -Me.

[0262] (198) A compound of any of (1) to (189), where: Each-R Q1CC If it exists, then it independently produces linearly saturated C 1-6 Alkyl, C 2-6 Alkenil, C 3-6 Cycloalkyl, C 3-7 Heterocyclyl, phenyl, or C 5-6 It is a heteroaryl, where C 1-6The alkyl group is optionally substituted with -OH, -CN, or -OCH3, and each phenyl and heteroaryl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CHF2, -CF3, and -OCH3.

[0263] (199) Any compound from (1) to (189), where: Each-R Q1CC If they exist, they are independently -Me, -Et, -iPr, -iBu, -t-Bu, -heptyl, C 2-6 The compounds are alkenyl, cyclopropyl, tetrahydropyran, phenyl, or pyrazolyl, pyrimidinyl, where -Me, -Et, -iPr, -iBu, -t-Bu, or -heptyl is optionally substituted with -OH, -CN, or -OCH3, and each phenyl, pyrazolyl, and pyrimidinyl is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CHF2, -CF3, and -OCH3.

[0264] (200) A compound of any of (1) to (189), where: Each-R Q1CC If they exist, then independently, linearly C 1-6 Alkyl, C 3-6 Cycloalkyl, phenyl, or C 5-6 These are heteroaryl compounds, where each cycloalkyl, phenyl, and heteroaryl is optionally -F, -Cl, or -C. 1-4 It is substituted with one or more groups selected from alkyl-CHF2, -CF3, and -OCH3.

[0265] -(CH 2 ) n1 -O-(CH 2 ) m1 - The indices "n1" and "m1" (201) A compound of any of (1) to (200), where: n1 is 0, 1, 2, or 3, if it exists; m1 is 0, 1, 2, or 3, if it exists; However, m1+n1 is either 2 or 3.

[0266] (202) A compound of any of (1) to (200), where: n1 is 0, 1, or 2, if it exists; m1 is 0, 1, or 2, if it exists; However, m1+n1 is either 2 or 3.

[0267] (203) A compound of any of (1) to (200), where: n1 is either 1 or 2, if it exists; m1 is either 1 or 2, if it exists; However, m1+n1 is either 2 or 3.

[0268] -O-(CH 2 ) p1 -O- exponent "p1" (204) A compound of any of (1) to (203), where: If p1 exists, then it is 1.

[0269] (205) A compound of any of (1) to (203), where: If p1 exists, then it is 2.

[0270] Group-R Q1CX (206) A compound of any of (1) to (203), where: Each-R Q1CX If present, then independently of linear or branched saturated C 1-4 It is a fluoroalkyl group.

[0271] (207) A compound of any of (1) to (203), where: Each-R Q1CXIf they exist, they are independently -CF3, -CHF2, -CH2CF3, or -CH2CHF2.

[0272] (208) A compound of any of (1) to (203), where: Each-R Q1CX If it exists, it is -CF3.

[0273] (209) A compound of any of (1) to (203), where: Each-R Q1CX If they exist, they are independently -CF3 or -CH2CF3.

[0274] Group-L Q1C - (210) A compound of any of (1) to (209), where: Each-L Q1C If it exists, it is independently -CH2-, -C(CH3)2-, -CH2CH2-, or -CH2CH2CH2-.

[0275] (211) A compound of any of (1) to (209), where: Each-L Q1C If they exist, - are independently -CH2-, -CH2CH2-, or -CH2CH2CH2-.

[0276] (212) Any compound from (1) to (209), where: Each-L Q1C -If it exists, it is -CH2-.

[0277] (213) Any compound from (1) to (209), where: Each-L Q1C -If it exists, then it is -CH2CH2-.

[0278] (214) Any compound from (1) to (209), where: Each-L Q1C-If it exists, then it is -CH2CH2CH2-.

[0279] Group-R Q1CM (215) A compound of any of (1) to (214), where: Each-R Q1CM If present, they are independently azetidino, pyrrolidino, piperidino, piperadino, morpholino, thiomorpholino, azepano, or diazepano, and: If desired, one or more carbon atoms are added as a group -R Q1CMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q1CMM -C(=O)R Q1CMM , -C(=O)OR Q1CMM -C(=O)NH2, -C(=O)NHR Q1CMM -C(=O)NR Q1CMM 2, and -S(=O)2R Q1CMM It is substituted with a group selected from the following.

[0280] (216) Any compound from (1) to (214), where: Each-R Q1CM If they exist, they are independently pyrrolidino, piperidino, piperazino, or morpholino, and: If desired, one or more carbon atoms are added as a group -R Q1CMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q1CMM -C(=O)R Q1CMM , -C(=O)OR Q1CMM -C(=O)NH2, -C(=O)NHR Q1CMM -C(=O)NR Q1CMM 2, and -S(=O)2R Q1CMM It is substituted with a group selected from the following.

[0281] (217) A compound of any of (1) to (214), where: Each-R Q1CMIf they exist, they are independently pyrrolidino, piperidino, piperazino, or morpholino, and: If desired, one or more carbon atoms are added as a group -R Q1CMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q1CMM -C(=O)R Q1CMM , and -C(=O)OR Q1CMM It is substituted with a group selected from the following.

[0282] (218) A compound of any of (1) to (214), where: Each-R Q1CM If present, it independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C 3-11 It is a heterocycline; and: If desired, one or more carbon atoms are added as a group -R Q1CMM It has been replaced with; If desired, secondary nitrogen, if available, -R Q1CMM It is substituted with a group selected from the following.

[0283] (219) A compound of any of (1) to (214), where: Each-R Q1CM If present, these are piperazinyl, piperidinyl, pyrrolidinyl, and morpholinyl, independently bonded via an N-ring atom; and: If desired, one or more carbon atoms are added as a group -R Q1CMM It has been replaced with; If desired, secondary nitrogen, if available, -R Q1CMM It is substituted with a group selected from the following.

[0284] (220) A compound of any of (1) to (214), where: Each-R Q1CM If present, and if desired, secondary nitrogen -R Q1CMM It is substituted with a group selected from the following.

[0285] Group-R Q1CMM (221) A compound of any of (1) to (220), where: Each-R Q1CMM If present, then independently of linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, phenyl, or phenyl-C 1-3 It is alkyl, and here, C 1-4 The alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl or phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0286] (222) A compound of any of (1) to (220), where: Each-R Q1CMM If present, then independently of linear or branched saturated C 1-4 Alkyl or phenyl-C 1-3 It is alkyl, and here, C 1-4 Alkyl groups are optionally substituted with -OH or -OCH3, and each cycloalkyl and phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; (223) A compound of any of (1) to (220), where: Each-R Q1CMM If present, then independently of linear or branched saturated C 1-4 Alkyl, phenyl, or phenyl-CH2-, where C 1-4 The alkyl group is optionally substituted with -OH or -OCH3.

[0287] (224) A compound of any of (1) to (220), where: Each-R Q1CMM If present, then independently of linear or branched saturated C 1-4It is alkyl, phenyl, or benzyl.

[0288] (225) A compound of any of (1) to (220), where: Each-R Q1CMM If present, then independently of linear or branched saturated C 1-4 It is alkyl and optionally substituted with -OH or -OCH3.

[0289] (226) A compound of any of (1) to (220), where: Each-R Q1CMM If present, then independently of linear or branched saturated C 1-4 It is alkyl.

[0290] (227) A compound of any of (1) to (220), where: Each-R Q1CMM If they exist, they are independently -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0291] (228) A compound of any of (1) to (220), where: Each-R Q1CMM If they exist, they are independently -Me, -Et, -nPr, or -iPr.

[0292] (229) A compound of any of (1) to (220), where: Each-R Q1CMM If they exist, they are independently -Me or -Et.

[0293] (230) A compound of any of (1) to (220), where: Each-R Q1CMM If it exists, it is -Me.

[0294] (231) A compound of any of (1) to (220), where: Each-R Q1CMM If they exist, they are independently -F, -NH2, and linearly saturated C.1-4 Alkyl, C 1-4 Alkyl OC(=O)NH-, or C 3-6 It is a cycloalkyl, where C 1-4 The alkyl group is optionally substituted with an -OH group.

[0295] (232) A compound of any of (1) to (220), where: Each-R Q1CMM If present, these are independently -F, -NH2, -Me, -Et, EtOC(=O)NH-, or cyclopropyl, where -Me or -Et is optionally substituted with -OH.

[0296] (233) A compound of any of (1) to (220), where: Each-R Q1CMM If present, these are independently -F, or linear or branched saturated C. 1-4 It is alkyl.

[0297] Group-R Q1N (234) A compound of any of (1) to (233), where: Each-R Q1N If they exist, they exist independently: -R Q1NC , -R Q1NX , -R Q1Nhet , -L Q1N -R Q1Nhet , -L Q1N -OH, -L Q1N -OR Q1NC , -L Q1N -C(=O)OH, -L Q1N -C(=O)OR Q1NC , -L Q1N -C(=O)NH2, -L Q1N -C(=O)NHR Q1NK , -L Q1N -C(=O)NR Q1NC 2, -L Q1N -C(=O)RQ1NP , -L Q1N -NH2, -L Q1N -NHR Q1NC , -L Q1N -NR Q1NC 2, -L Q1N -R Q1NM , -L Q1N -NHC(=O)OR Q1NC That is the case.

[0298] (235) A compound of any of (1) to (233), where: Each-R Q1N If they exist, they exist independently: -R Q1NC , -L Q1N -C(=O)NR Q1NC 2, or -L Q1N -C(=O)R Q1NP That is the case.

[0299] (236) A compound of any of (1) to (233), where: Each-R Q1N If they exist, they exist independently: -R Q1Nhet or -L Q1N -R Q1Nhet That is the case.

[0300] (237) A compound of any of (1) to (233), where: Each-R Q1N If it exists: -R Q1Nhet That is the case.

[0301] (238) A compound of any of (1) to (233), where: Each-R Q1N If it exists: -L Q1N -C(=O)NH2, -L Q1N -C(=O)NHR Q1NK , -L Q1N -C(=O)NR Q1NC 2, or -L Q1N-C(=O)R Q1NP That is the case.

[0302] (239) A compound of any of (1) to (233), where: Each-R Q1N If it exists: -L Q1N -C(=O)NHR Q1NK , -L Q1N -C(=O)NR Q1NC 2, or -L Q1N -C(=O)R Q1NP That is the case.

[0303] (240) A compound of any of (1) to (233), where: Each-R Q1N If it exists: -L Q1N -C(=O)NHR Q1NK That is the case.

[0304] (241) A compound of any of (1) to (233), where: Each-R Q1N If it exists: -L Q1N -C(=O)R Q1NP That is the case.

[0305] (242) A compound of any of (1) to (233), where: Each-R Q1N If they exist, they exist independently: -R Q1NC , (243) A compound of any of (1) to (233), where: Each-R Q1N If they exist, they exist independently: -L Q1N -OH or -L Q1N -OR Q1NC That is the case.

[0306] (244) A compound of any of (1) to (233), where: Each-R Q1NIf they exist, they exist independently: -L Q1N -NH2, -L Q1N -NHR Q1NC , -L Q1N -NR Q1NC 2, or -L Q1N -R Q1NM That is the case.

[0307] (245) A compound of any of (1) to (233), where: Each-R Q1N If they exist, they exist independently: -R Q1NC , -L Q1N -R Q1NC , -R Q1NX , -R Q1Nhet , -L Q1N -R Q1Nhet , -L Q1N -OH, -L Q1N -OR Q1NC , -S(=O)2R Q1NC , -L Q1N -C(=O)OH, -L Q1N -C(=O)OR Q1NC , -L Q1N -C(=O)NH2, -L Q1N -C(=O)NHR Q1NK , -L Q1N -C(=O)NR Q1NC 2, -L Q1N -C(=O)R Q1NP , -L Q1N -NH2, -L Q1N -NR Q1NC 2. or -L Q1N -NHC(=O)OR Q1NC That is the case.

[0308] (246) Any compound from (1) to (233), where: Each-R Q1N If they exist, they exist independently: -RQ1NC , -R Q1NX , -R Q1Nhet , -L Q1N -R Q1Nhet , -S(=O)2R Q1NC , -L Q1N -C(=O)NR Q1NC 2, or -L Q1N -C(=O)R Q1NP That is the case.

[0309] Group-R Q1NC (247) A compound of any of (1) to (246), where: Each-R Q1NC If present, then independently of linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 The alkyl group is wherein each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0310] (248) Any compound from (1) to (246), where: Each-R Q1NC If present, then independently of linear or branched saturated C 1-4 The group is alkyl, phenyl, or phenyl-CH2-, where each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0311] (249) A compound of any of (1) to (246), where: Each-R Q1NC If present, then independently of linear or branched saturated C 1-4It is alkyl, phenyl, or benzyl.

[0312] (250) A compound of any of (1) to (246), where: Each-R Q1NC If present, then independently of linear or branched saturated C 1-4 It is alkyl.

[0313] (251) A compound of any of (1) to (246), where: Each-R Q1NC If they exist, they are independently -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0314] (252) Any compound of (1) to (246), where: Each-R Q1NC If they exist, they are independently -Me, -Et, -nPr, or -iPr.

[0315] (253) Any compound from (1) to (246), where: Each-R Q1NC If they exist, they are independently -Me or -Et.

[0316] (254) Any compound from (1) to (246), where: Each-R Q1NC If it exists, it is -Me.

[0317] (255) Any compound from (1) to (246), where: Each-R Q1NC If present, then independently of linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, phenyl, or C 5-6 It is a heteroaryl, where each C 1-4The alkyl group is optionally substituted with -F, -OH, -C≡N, -SO2-CH3, or -OCH3, where each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with -F, -Cl, -Br, linear or branched saturated C 1-4 These are alkyl, -CHF2, -CF3, -CH2-O-CH3, -OCH2CH3, and -C(=O)-NH-phenyl, where C 1-4 Alkyl and phenyl are independently substituted with -CH3 or -OH as desired, and are substituted with one or more groups selected from the above.

[0318] (256) Any compound from (1) to (246), where: Each-R Q1NC If present, these are independently methyl, ethyl, propyl, i-propyl, butyl, i-butyl, t-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl, pyrimidinyl, oxazolyl, pyridyl, thiazolyl, imidazolyl, or pyrazolyl, where each methyl, ethyl, propyl, i-propyl, butyl, i-butyl, or t-butyl is optionally substituted with -F, -OH, -C≡N, -SO2-CH3, or -OCH3, where each cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl, pyrimidinyl, oxazolyl, pyridyl, thiazolyl, imidazolyl, or pyrazolyl is optionally substituted with -F, -Cl, -Br, linear or branched saturated C 1-4 It is substituted with one or more groups selected from alkyl, -CHF2, -CF3, -CH2-O-CH3, -OCH2CH3, and -C(=O)-NH-phenyl, where C 1-4 Alkyl and phenyl are independently substituted with -CH3 or -OH as desired.

[0319] (257) Any compound from (1) to (246), where: Each-R Q1NC If present, then independently of linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, phenyl, or C5-6 It is a heteroaryl, where each C 1-4 The alkyl group is optionally substituted with -F, -OH, -C≡N, -SO2-CH3, or -OCH3, where each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from -F, -Cl, -CF3, and -OCH3.

[0320] Group-R Q1NX (258) A compound of any of (1) to (257), where: Each-R Q1NX If present, then independently of linear or branched saturated C 1-4 It is a fluoroalkyl group.

[0321] (259) A compound of any of (1) to (257), where: Each-R Q1NX If they exist, they are independently -CF3, -CHF2, -CH2CF3, or -CH2CHF2.

[0322] (260) A compound of any of (1) to (257), where: Each-R Q1NX If it exists, it is -CHF2.

[0323] (261) A compound of any of (1) to (257), where: Each-R Q1NX If they exist, they are -CH2CH2F, -CH2CHF2, -CH2CF3, and -CH2CH2Br.

[0324] Group-L Q1N - (262) A compound of any of (1) to (261), where: Each-L Q1N If it exists, it is independently -CH2-, -C(CH3)2-, -CH2CH2-, or -CH2CH2CH2-.

[0325] (263) A compound of any of (1) to (261), where: Each-L Q1N If they exist, - are independently -CH2-, -CH2CH2-, or -CH2CH2CH2-.

[0326] (264) Any compound from (1) to (226112), where: Each-L Q1N -If it exists, it is -CH2-.

[0327] (265) A compound of any of (1) to (261), where: Each-L Q1N -If it exists, then it is -CH2CH2-.

[0328] (266) A compound of any of (1) to (261), where: Each-L Q1N -If it exists, then it is -CH2CH2CH2-.

[0329] (267) A compound of any of (1) to (261), where: Each-L Q1N - is, if present, -CH2-, -C(CH3)2CH2--, -CH2CH2-, or -CH2CH2CH2-, where -CH2-, -C(CH3)2CH2--, -CH2CH2-, or -CH2CH2CH2- is optionally substituted with -OH or -OMe.

[0330] Group-R Q1NM (268) A compound of any of (1) to (267), where: Each-R Q1NM If present, they are independently azetidino, pyrrolidino, piperidino, piperadino, morpholino, thiomorpholino, azepano, or diazepano, and: If desired, one or more carbon atoms are added as a group -R Q1NMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q1NMM -C(=O)R Q1NMM , -C(=O)OR Q1NMM -C(=O)NH2, -C(=O)NHR Q1NMM -C(=O)NR Q1NMM 2, and -S(=O)2R Q1NMM It is substituted with a group selected from the following.

[0331] (269) A compound of any of (1) to (267), where: Each-R Q1NM If they exist, they are independently pyrrolidino, piperidino, piperazino, or morpholino, and: If desired, one or more carbon atoms are added as a group -R Q1NMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q1NMM -C(=O)R Q1NMM , -C(=O)OR Q1NMM -C(=O)NH2, -C(=O)NHR Q1NMM -C(=O)NR Q1NMM 2, and -S(=O)2R Q1NMM It is substituted with a group selected from the following.

[0332] (270) A compound of any of (1) to (267), where: Each-R Q1NM If they exist, they are independently pyrrolidino, piperidino, piperazino, or morpholino, and: If desired, one or more carbon atoms are added as a group -R Q1NMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q1NMM -C(=O)R Q1NMM , and -C(=O)OR Q1NMM It is substituted with a group selected from the following.

[0333] Group-R Q1NMM (271) A compound of any of (1) to (270), where: Each-RQ1NMM If present, then independently of linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 The alkyl group is wherein each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0334] (272) Any compound from (1) to (270), where: Each-R Q1NMM If present, then independently of linear or branched saturated C 1-4 The group is alkyl, phenyl, or phenyl-CH2-, where each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0335] (273) A compound of any of (1) to (270), where: Each-R Q1NMM If present, then independently of linear or branched saturated C 1-4 It is alkyl, phenyl, or benzyl.

[0336] (274) A compound of any of (1) to (270), where: Each-R Q1NMM If present, then independently of linear or branched saturated C 1-4 It is alkyl.

[0337] (275) A compound of any of (1) to (270), where: Each-R Q1NMM If it exists, it is -Me.

[0338] Group-R Q1Nhet (276) A compound of any of (1) to (275), where: Each-R Q1Nhet If present, these are independently azetidinil, oxetanil, pyrrolidinil, tetrahydrofuranil, piperidinil, piperazinil, tetrahydropyranil, morpholinil, thiomorpholinil, azepanil, or diazepanil; and: If desired, if present, sulfur is substituted with one or two oxygen groups; If desired, one or more carbon atoms are added as a group -R Q1NHH Or it is replaced by =O; and If desired, secondary nitrogen, if available, -R Q1NHH -C(=O)R Q1NJJ , -C(=O)OR Q1NHH -C(=O)NH2, -C(=O)NHR Q1NHH -C(=O)NR Q1NHH 2, and -S(=O)2R Q1NHH It is substituted with a group selected from the following.

[0339] (277) A compound of any of (1) to (275), where: Each-R Q1Nhet If present, these are independently oxetanil, pyrrolidinil, tetrahydrofuranil, piperidinil, piperazinil, tetrahydropyranil, or morpholinil; and: If desired, one or more carbon atoms are added as a group -R Q1NHH Or it is replaced by =O; and If desired, secondary nitrogen, if available, -R Q1NHH -C(=O)R Q1NJJ , -C(=O)OR Q1NHH -C(=O)NH2, -C(=O)NHR Q1NHH -C(=O)NR Q1NHH 2, and -S(=O)2R Q1NHH It is substituted with a group selected from the following.

[0340] (278) Any compound from (1) to (275), where: Each-R Q1Nhet If they exist, they are independently pyrrolidinil, piperidinil, or piperazinil; and: If desired, one or more carbon atoms are added as a group -R Q1NHH Or it is replaced by =O; and If desired, secondary nitrogen, if available, -R Q1NHH -C(=O)R Q1NJJ , -C(=O)OR Q1NHH -C(=O)NH2, -C(=O)NHR Q1NHH -C(=O)NR Q1NHH 2, and -S(=O)2R Q1NHH It is substituted with a group selected from the following.

[0341] (279) A compound of any of (1) to (275), where: Each-R Q1Nhet If they exist, they are independently pyrrolidinyl or piperidinyl; and: If desired, one or more carbon atoms are added as a group -R Q1NHH Or it is replaced by =O; and If desired, secondary nitrogen, if available, -R Q1NHH -C(=O)R Q1NJJ , -C(=O)OR Q1NHH -C(=O)NH2, -C(=O)NHR Q1NHH -C(=O)NR Q1NHH 2, and -S(=O)2R Q1NHH It is substituted with a group selected from the following.

[0342] (280) A compound of any of (1) to (275), where: Each-R Q1Nhet If it exists, it is pyrrolidinyl; and: If desired, one or more carbon atoms are added as a group -R Q1NHH Or it is replaced by =O; and If desired, secondary nitrogen, if available, -R Q1NHH -C(=O)R Q1NJJ , -C(=O)ORQ1NHH -C(=O)NH2, -C(=O)NHR Q1NHH -C(=O)NR Q1NHH 2, and -S(=O)2R Q1NHH It is substituted with a group selected from the following.

[0343] (281) A compound of any of (1) to (275), where: Each-R Q1Nhet If it exists, then it is an independent non-aromatic C 3-7 It is a heterocycline; and: The carbon atoms are optionally substituted with one or more groups = O; and If desired, secondary nitrogen, if available, -R Q1NHH -C(=O)R Q1NJJ , -C(=O)OR Q1NHH -C(=O)NHR Q1NHH , and -C(=O)NR Q1NHH It is substituted with a group selected from 2.

[0344] (282) Any compound from (1) to (275), where: Each-R Q1Nhet If present, these are independently oxetanil, piperidinil, pyrrolidinil, tetrahydrofuranil, tetrahydropyranil, morpholinil, azetidinil, or tetrahydrothiophenyl; and: The carbon atoms are optionally substituted with one or more groups = O; and If desired, secondary nitrogen, if available, -R Q1NHH -C(=O)R Q1NJJ , -C(=O)OR Q1NHH -C(=O)NHR Q1NHH , and -C(=O)NR Q1NHH It is substituted with a group selected from 2.

[0345] Group-R Q1NHH (283) A compound of any of (1) to (283), where: Each-RQ1NHH If present, then independently of linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 The alkyl group is wherein each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0346] (284) A compound of any of (1) to (283), where: Each-R Q1NHH If present, then independently of linear or branched saturated C 1-4 The group is alkyl, phenyl, or phenyl-CH2-, where each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0347] (285) A compound of any of (1) to (283), where: Each-R Q1NHH If present, then independently of linear or branched saturated C 1-4 It is alkyl, phenyl, or benzyl.

[0348] (286) A compound of any of (1) to (283), where: Each-R Q1NHH If present, then independently of linear or branched saturated C 1-4 It is alkyl.

[0349] (287) A compound of any of (1) to (283), where: Each-R Q1NHH If they exist, they are independently -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0350] (288) Any compound from (1) to (283), where: Each-R Q1NHH If they exist, they are independently -Me, -Et, -nPr, or -iPr.

[0351] (289) A compound of any of (1) to (283), where: Each-R Q1NHH If they exist, they are independently -Me or -Et.

[0352] (290) A compound of any of (1) to (283), where: Each-R Q1NHH If it exists, it is -Me.

[0353] (291) A compound of any of (1) to (283), where: Each-R Q1NHH If present, then independently of linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, or phenyl-C 1-3 It is alkyl.

[0354] (292) A compound of any of (1) to (283), where: Each-R Q1NHH If present, these are independently -Me, -Et, -tBu, cyclopropyl, benzyl, or phenylethyl.

[0355] Group-R Q1NJJ (293) A compound of any of (1) to (292), where: -R Q1NJJ If it exists, -R J1 , -L J -R J2 And, -R J3 , -L J -R J3 And, -R J4 , -L J -R J4 , or -LJ -R J5 That is the case.

[0356] (294) Any compound of (1) to (292), where: -R Q1NJJ If it exists, -R J1 , -L J -R J2 , -L J -R J3 , -L J -R J4 , or -L J -R J5 That is the case.

[0357] (295) A compound of any of (1) to (292), where: -R Q1NJJ If it exists, -R J1 , -L J -R J3 , -L J -R J4 , or -L J -R J5 That is the case.

[0358] (296) A compound of any of (1) to (292), where: -R Q1NJJ If it exists, -R J1 , -L J -R J4 , or -L J -R J5 That is the case.

[0359] (297) Any compound of (1) to (292), where: -R Q1NJJ If it exists, -R J1 or -L J -R J4 That is the case.

[0360] (298) A compound of any of (1) to (292), where: -R Q1NJJ If it exists, -L J -R J2, -L J -R J3 , -L J -R J4 , or -L J -R J5 That is the case.

[0361] (299) A compound of any of (1) to (292), where: -R Q1NJJ If it exists, -L J -R J3 , -L J -R J4 , or -L J -R J5 That is the case.

[0362] (300) Any compound from (1) to (292), where: -R Q1NJJ If it exists, -L J -R J4 or -L J -R J5 That is the case.

[0363] (301) A compound of any of (1) to (292), where: -R Q1NJJ If it exists, -L J -R J4 That is the case.

[0364] Group-R J1 (302) A compound of any of (1) to (301), where: -R J1 If present, linear or branched saturated C 1-6 Alkyl; and optionally, one or more -F, -OH, -OR JJ -O-phenyl, -C(=O)OH, -C(=O)OR JJ -NH2, -NHR JJ , and -NR JJ It is substituted with a group selected from 2.

[0365] (303) A compound of any of (1) to (301), where: -R J1 If present, linear or branched saturated C 1-4 Alkyl; and optionally, one or more -F, -OH, -OR JJ -O-phenyl, -C(=O)OH, -C(=O)OR JJ -NH2, -NHR JJ , and -NR JJ It is substituted with a group selected from 2.

[0366] (304) A compound of any of (1) to (301), where: -R J1 If present, linear or branched saturated C 1-4 Alkyl; and optionally one or more -F, -OH, or -OR groups. JJ It is substituted with a group selected from the following.

[0367] (305) A compound of any of (1) to (301), where: -R J1 If present, linear or branched saturated C 1-4 It is alkyl.

[0368] (306) A compound of any of (1) to (301), where: -R J1 If they exist, they are -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0369] (307) A compound of any of (1) to (301), where: -R J1 If they exist, they are -Me, -Et, -nPr, or -iPr.

[0370] (308) A compound of any of (1) to (301), where: -R J1 If it exists, it is either -Me or -Et.

[0371] (309) A compound of any of (1) to (301), where: -R J1 If it exists, it is -Me.

[0372] (310) A compound of any of (1) to (301), where: -R J1 If present, linear or branched saturated C 1-6 Alkyl; and optionally -F, -OR JJ -O-phenyl, and -C(=O)OR JJ It is replaced by one or more elements selected from the following.

[0373] (311) A compound of any of (1) to (301), where: -R J1 -Me, -Et, -iPr, -iBu; and optionally -F, -OR JJ -O-phenyl, and -C(=O)OR JJ It is replaced by one or more elements selected from the following.

[0374] Group-R J2 (312) A compound of any of (1) to (311), where: Each-R J2 If present, these are independently cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl.

[0375] (313) A compound of any of (1) to (311), where: Each-R J2 If present, it is cyclopropyl.

[0376] (314) A compound of any of (1) to (311), where: Each-R J2 If it exists, it is independently cyclobutyl.

[0377] (315) A compound of any of (1) to (311), where: Each-R J2 If it exists, it is independently cyclopentyl.

[0378] (316) A compound of any of (1) to (311), where: Each-R J2 If it exists, it is independently cyclohexyl.

[0379] Group-R J3 (317) A compound of any of (1) to (316), where: Each-R J3 If it exists, then it is an independent non-aromatic C 3-7 It is a heterocycline.

[0380] (318) A compound of any of (1) to (316), where: Each-R J3 If present, these are independently azetidinil, oxetanil, pyrrolidinil, tetrahydrofuranil, piperidinil, piperazinil, tetrahydropyranil, morpholinil, thiomorpholinil, azepanil, or diazepanil; and: If desired, if present, sulfur is substituted with one or two oxygen groups; Carbon is -F and -R as desired. JJ -CF3, -OH, -OR JJ -NH2, -NHR JJ , and -NR JJ It is replaced by one or more elements selected from 2; and If desired, secondary nitrogen, if available, -R JJ -C(=O)R JJ , -C(=O)OR JJ , and -S(=O)2R JJ It is substituted with a group selected from the following.

[0381] (319) A compound of any of (1) to (316), where: Each-R J3 If present, these are independently pyrrolidinyl, tetrahydrofuranil, piperidinyl, piperazinyl, tetrahydropyranil, or morpholinil; and: Carbon is -F and -R as desired. JJ -CF3, -OH, -OR JJ -NH2, -NHR JJ , and -NR JJ It is replaced by one or more elements selected from 2; and If desired, secondary nitrogen, if available, -R JJ -C(=O)R JJ , -C(=O)OR JJ , and -S(=O)2R JJ It is substituted with a group selected from the following.

[0382] (320) A compound of any of (1) to (316), where: Each-R J3 If present, these are independently pyrrolidinyl, tetrahydrofuranil, piperidinyl, piperazinyl, tetrahydropyranil, or morpholinil; and: Carbon can be -F and -R as desired. JJ It is replaced by one or more elements selected from; and If desired, secondary nitrogen, if available, -R JJ -C(=O)R JJ , -C(=O)OR JJ , and -S(=O)2R JJ It is substituted with a group selected from the following.

[0383] (321) A compound of any of (1) to (316), where: Each-R J3 If present, these are independently pyrrolidinyl, tetrahydrofuranil, piperidinyl, piperazinyl, tetrahydropyranil, or morpholinil; and: If desired, secondary nitrogen, if available, -R JJ -C(=O)R JJ , -C(=O)OR JJ , and -S(=O)2R JJ It is substituted with a group selected from the following.

[0384] (322) A compound of any of (1) to (316), where: Each-R J3 If present, it is independently tetrahydropyranil or piperidinil.

[0385] Group-R J4 (323) A compound of any of (1) to (322), where: Each-R J4 If present, it is phenyl; and optionally one or more -F, -Cl, and -R JJ -OH, -NH2, -NHR JJ , and -NR JJ It is substituted with a group selected from the following.

[0386] (324) A compound of any of (1) to (322), where: Each-R J4 If it exists, it is phenyl.

[0387] (325) A compound of any of (1) to (322), where: Each-R J4 is phenyl, if present; and optionally one or more -F, -OR JJ -NH2 and -NR JJ It is substituted with a group selected from 2.

[0388] Group-R J5 (326) A compound of any of (1) to (325), where: Each-R J5 If it exists, then independently C 5-6It is a heteroaryl compound.

[0389] (327) A compound of any of (1) to (325), where: Each-R J5 If present, they are independently pyrrolyl, furanyl, thienyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridinyl, pyrimidinyl, or pyrididinyl; and: Carbon is -F and -R as desired. JJ -CF3, -OH, -OR JJ -NH2, -NHR JJ , and -NR JJ It is replaced by one or more elements selected from 2; and If desired, secondary nitrogen, if available, -R JJ -C(=O)R JJ , -C(=O)OR JJ , and -S(=O)2R JJ It is substituted with a group selected from the following.

[0390] (328) A compound of any of (1) to (325), where: Each-R J5 If present, they are independently pyrrolyl, furanyl, thienyl, pyrazolyl, pyridinyl, pyrimidinyl, or pyrididinyl; and: Carbon is -F and -R as desired. JJ -CF3, -OH, -OR JJ -NH2, -NHR JJ , and -NR JJ It is replaced by one or more elements selected from 2; and If desired, secondary nitrogen, if available, -R JJ -C(=O)R JJ , -C(=O)OR JJ , and -S(=O)2R JJ It is substituted with a group selected from the following.

[0391] (329) A compound of any of (1) to (325), where: Each-RJ5 If present, it is independently thienyl, pyrazolyl, or pyridinyl; and: Carbon is -F and -R as desired. JJ -CF3, -OH, -OR JJ -NH2, -NHR JJ , and -NR JJ It is replaced by one or more elements selected from 2; and If desired, secondary nitrogen, if available, -R JJ -C(=O)R JJ , -C(=O)OR JJ , and -S(=O)2R JJ It is substituted with a group selected from the following.

[0392] (330) A compound of any of (1) to (325), where: Each-R J5 If present, these are independently thienyl, pyrazolyl, or pyridinyl.

[0393] Group-L J - (331) A compound of any of (1) to (330), where: Each-L J If they exist, - are independently -CH2-, -CF2-, -C(CH3)2-, -CH2CH2-, or -CH2CH2CH2-.

[0394] (332) A compound of any of (1) to (330), where: Each-L J - If present, independently of linear or branched saturated C 1-4 It is alkylene.

[0395] (333) A compound of any of (1) to (330), where: Each-L J If it exists, it is independently -CH2-, -C(CH3)2-, -CH2CH2-, or -CH2CH2CH2-.

[0396] (334) A compound of any of (1) to (330), where: Each-L J If they exist, - are independently -CH2-, -CH2CH2-, or -CH2CH2CH2-.

[0397] (335) A compound of any of (1) to (330), where: Each-L J -If it exists, it is -CH2-.

[0398] (336) A compound of any of (1) to (330), where: Each-L J -If it exists, then it is -CH2CH2-.

[0399] (337) A compound of any of (1) to (330), where: Each-L J -If it exists, then it is -CH2CH2CH2-.

[0400] (338) A compound of any of (1) to (330), where: Each-L J -, if present, is independently -CH2- or -CH2CH2- and optionally substituted with one or more -F groups.

[0401] Base- R JJ (339) A compound of any of (1) to (338), where: Each-R JJ If it exists: The options are -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0402] (340) A compound of any of (1) to (338), where: Each-R JJ If it exists: The options are -Me, -Et, -nPr, or -iPr.

[0403] (341) A compound of any of (1) to (338), where: Each-R JJ If it exists: -Me or -Et

[0404] (342) A compound of any of (1) to (338), where: Each-R JJ If it exists: -Me

[0405] Group-R Q1NK (343) A compound of any of (1) to (342), where: -R Q1NK If it exists, -R K1 And, -R K2 , -L K -R K2 And, -R K3 , or -L K -R K3 That is the case.

[0406] (344) A compound of any of (1) to (342), where: -R Q1NK If it exists, -R K1 And, -R K2 And, -R K3 , or -L K -R K3 That is the case.

[0407] (345) A compound of any of (1) to (342), where: -R Q1NK If it exists, -R K1 That is the case.

[0408] (346) Any compound from (1) to (342), where: -R Q1NKIf it exists, -R K2 That is the case.

[0409] (347) A compound of any of (1) to (342), where: -R Q1NK If it exists, -R K3 That is the case.

[0410] (348) Any compound from (1) to (342), where: -R Q1NK If it exists, -L K -R K3 That is the case.

[0411] Group-R K1 (349) A compound of any of (1) to (348), where: -R K1 If present, linear or branched saturated C 1-6 Alkyl; and optionally, one or more -F, -OH, -OR KK -O-phenyl, -C(=O)OH, -C(=O)OR KK -NH2, -NHR KK , and -NR KK It is substituted with a group selected from 2.

[0412] (350) A compound of any of (1) to (348), where: -R K1 If present, linear or branched saturated C 1-4 Alkyl; and optionally, one or more -F, -OH, -OR KK -O-phenyl, -C(=O)OH, -C(=O)OR KK -NH2, -NHR KK , and -NR KK It is substituted with a group selected from 2.

[0413] (351) A compound of any of (1) to (348), where: -R K1If present, linear or branched saturated C 1-4 Alkyl; and optionally one or more -F, -OH, or -OR groups. KK It is substituted with a group selected from the following.

[0414] (352) A compound of any of (1) to (348), where: -R K1 If present, linear or branched saturated C 1-4 It is alkyl.

[0415] (353) A compound of any of (1) to (348), where: -R K1 If they exist, they are -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0416] (354) A compound of any of (1) to (348), where: -R K1 If they exist, they are -Me, -Et, -nPr, or -iPr.

[0417] (355) A compound of any of (1) to (348), where: -R K1 If it exists, it is either -Me or -Et.

[0418] (356) Any compound from (1) to (348), where: -R K1 If it exists, it is -Me.

[0419] (357) A compound of any of (1) to (348), where: -R K1 If present, linear or branched saturated C 1-7 Alkyl; and optionally, one or more -OH, -OR groups. KK -OCH2CH2OCH3, and -NR KK It is substituted with a group selected from 2.

[0420] (358) A compound of any of (1) to (348), where: -R K1 If present, it is -Me, -Et, -nPr, -iPr, -tBu, or heptane; and optionally one or more -OH, -OR KK -OCH2CH2OCH3, and -NR KK It is substituted with a group selected from 2.

[0421] Group-R K2 (359) A compound of any of (1) to (358), where: Each-R K2 If it exists, then independently C 3-6 It is a cycloalkyl group.

[0422] (360) A compound of any of (1) to (358), where: Each-R K2 If present, these are independently cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl.

[0423] (361) A compound of any of (1) to (358), where: Each-R K2 If present, it is cyclopropyl.

[0424] (362) A compound of any of (1) to (358), where: Each-R K2 If it exists, it is independently cyclobutyl.

[0425] (363) A compound of any of (1) to (358), where: Each-R K2 If it exists, it is independently cyclopentyl.

[0426] (364) A compound of any of (1) to (358), where: Each-RK2 If it exists, it is independently cyclohexyl.

[0427] Group-R K3 (365) A compound of any of (1) to (364), where: Each-R K3 If it exists, then it is an independent non-aromatic C 3-7 It is a heterocycline; and: If desired, secondary nitrogen, if available, -R KK , and -C(=O)OR KK It is substituted with a group selected from the following.

[0428] (366) Any compound from (1) to (364), where: Each-R K3 If present, they are independently morpholinil, piperidinil, piperazinil, pyrrolidinil, or tetrahydropyranil; and: If desired, secondary nitrogen, if available, -R KK , and -C(=O)OR KK It is substituted with a group selected from the following.

[0429] (367) Any compound from (1) to (364), where: Each-R K3 If present, these are independently azetidinil, oxetanil, pyrrolidinil, tetrahydrofuranil, piperidinil, piperazinil, tetrahydropyranil, morpholinil, thiomorpholinil, azepanil, or diazepanil; and: If desired, if present, sulfur is substituted with one or two oxygen groups; Carbon is -F and -R as desired. KK -CF3, -OH, -OR KK -NH2, -NHR KK , and -NR KK It is replaced by one or more elements selected from 2; and If desired, secondary nitrogen, if available, -R KK -C(=O)R KK , -C(=O)OR KK , and -S(=O)2R KK It is substituted with a group selected from the following.

[0430] (368) Any compound from (1) to (364), where: Each-R K3 If present, these are independently pyrrolidinyl, tetrahydrofuranil, piperidinyl, piperazinyl, tetrahydropyranil, or morpholinil; and: Carbon is -F and -R as desired. KK -CF3, -OH, -OR KK -NH2, -NHR KK , and -NR KK It is replaced by one or more elements selected from 2; and If desired, secondary nitrogen, if available, -R KK -C(=O)R KK , -C(=O)OR KK , and -S(=O)2R KK It is substituted with a group selected from the following.

[0431] (369) Any compound from (1) to (364), where: Each-R K3 If present, these are independently pyrrolidinyl, tetrahydrofuranil, piperidinyl, piperazinyl, tetrahydropyranil, or morpholinil; and: Carbon can be -F and -R as desired. KK It is replaced by one or more elements selected from; and If desired, secondary nitrogen, if available, -R KK -C(=O)R KK , -C(=O)OR KK , and -S(=O)2R KK It is substituted with a group selected from the following.

[0432] (370) A compound of any of (1) to (364), where: Each-R K3 If present, these are independently pyrrolidinyl, tetrahydrofuranil, piperidinyl, piperazinyl, tetrahydropyranil, or morpholinil; and: If desired, secondary nitrogen, if available, -R KK -C(=O)R KK , -C(=O)OR KK , and -S(=O)2R KK It is substituted with a group selected from the following.

[0433] Group-R K4 (371) A compound of any of (1) to (370), where: Each-R K4 If present, it is phenyl; and optionally one or more -F, -Cl, and -R KK -CF3, -OH, and -OR KK It is substituted with a group selected from the following.

[0434] (372) A compound of any of (1) to (370), where: Each-R K4 If it exists, it is phenyl.

[0435] Group-R K5 (373) A compound of any of (1) to (372), where: Each-R K5 If present, they are independently pyrrolyl, furanyl, thienyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridinyl, pyrimidinyl, or pyrididinyl; and: Carbon is -F and -R as desired. KK -CF3, -OH, -OR KK -NH2, -NHR KK , and -NR KKIt is replaced by one or more elements selected from 2; and If desired, secondary nitrogen, if available, -R KK -C(=O)R KK , -C(=O)OR KK , and -S(=O)2R KK It is substituted with a group selected from the following.

[0436] (374) A compound of any of (1) to (372), where: Each-R K5 If present, they are independently pyrrolyl, furanyl, thienyl, pyrazolyl, pyridinyl, pyrimidinyl, or pyrididinyl; and: Carbon is -F and -R as desired. KK -CF3, -OH, -OR KK -NH2, -NHR KK , and -NR KK It is replaced by one or more elements selected from 2; and If desired, secondary nitrogen, if available, -R KK -C(=O)R KK , -C(=O)OR KK , and -S(=O)2R KK It is substituted with a group selected from the following.

[0437] (375) A compound of any of (1) to (372), where: Each-R K5 If present, these are independently pyrrolyl, furanyl, thienyl, pyrazolyl, pyridinyl, pyrimidinyl, or pyrididinyl.

[0438] Group-L K - (376) A compound of any of (1) to (375), where: Each-L K - If present, independently of linear or branched saturated C 1-4 Alkilen.

[0439] (377) A compound of any of (1) to (375), where: Each-L K If it exists, it is independently -CH2-, -C(CH3)2-, -CH2CH2-, or -CH2CH2CH2-.

[0440] (378) Any compound from (1) to (375), where: Each-L K If they exist, - are independently -CH2-, -CH2CH2-, or -CH2CH2CH2-.

[0441] (379) A compound of any of (1) to (375), where: Each-L K -If it exists, it is independently -CH2- or -CH2CH2-.

[0442] (380) A compound of any of (1) to (375), where: Each-L K -If it exists, it is -CH2-.

[0443] (381) A compound of any of (1) to (375), where: Each-L K -If it exists, then it is -CH2CH2-.

[0444] (382) A compound of any of (1) to (375), where: Each-L K -If it exists, then it is -CH2CH2CH2-.

[0445] Group-R KK (383) A compound of any of (1) to (382), where: Each-R KK If it exists: The options are -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0446] (384) A compound of any of (1) to (382), where: Each-R KK If it exists: The options are -Me, -Et, -nPr, or -iPr.

[0447] (385) A compound of any of (1) to (382), where: Each-R KK If it exists: -Me or -tBu.

[0448] (386) A compound of any of (1) to (382), where: Each-R KK If it exists: -Me or -Et

[0449] (387) A compound of any of (1) to (382), where: Each-R KK If it exists: -Me

[0450] Group-R Q1NP (388) A compound of any of (1) to (387), where: -R Q1NP If present, it independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C 3-11 It is a heterocycline; and: Carbon can be added as desired -R Q1NPP -F, -OH, -OR Q1NPP , and are substituted with one or more bases selected from =O; and If desired, secondary nitrogen, if available, -R Q1NPP And, -R Q1NPPX -C(=O)R Q1NPP , -C(=O)OR Q1NPP -C(=O)NR Q1NPP 2, and -S(=O)2R Q1NPP It is substituted with a group selected from the following.

[0451] (389) A compound of any of (1) to (387), where: -R Q1NP If present, is morpholinyl, piperazinyl, piperidinyl, pyrrolidinyl, 2,5-diazabicyclo[2.2.1]heptanyl, 2,6-diazaspiro[3.3]heptanyl, 2,8-diazaspiro[4.5]decanyl, 1,4-diazepanyl, azetidinyl, 3,8-diazabicyclo[3.2.1]octanyl, 3-azabicyclo[3.1.0]hexanyl, azetidinyl, 2-azaspiro[3.3]heptanyl, or 2,6-diazaspiro[3.3]heptanyl, independently bonded via an N-ring atom; and: Carbon can be added as desired -R Q1NPP -F, -OH, -OR Q1NPP , and are substituted with one or more bases selected from =O; and If desired, secondary nitrogen, if available, -R Q1NPP And, -R Q1NPPX -C(=O)R Q1NPP , -C(=O)OR Q1NPP -C(=O)NR Q1NPP 2, and -S(=O)2R Q1NPP It is substituted with a group selected from the following.

[0452] (390) A compound of any of (1) to (387), where: -R Q1NP If present, it can independently and as desired, remove carbon -R Q1NPP It is replaced by one or more elements selected from; and If desired, secondary nitrogen, if available, -R Q1NPP It is substituted with a group selected from the following.

[0453] (391) A compound of any of (1) to (387), where: -R Q1NP If they exist, they exist independently: Azetidinil, pyrrolidinil, piperidinil, piperazinil, morpholinil, thiomorpholinil, azepanil, diazepanil, 3-azabicyclo[3.1.0]hexanil, 3,6-diazabicyclo[3.1.1]heptanil, 3-azabicyclo[3.1.1]heptanil, 2,5-diazabicyclo[2.2.1]heptanil, 2-azabicyclo[2.2.1]heptanil, 3,8-diazabicyclo[3.2.1]octanil, 3-azabicyclo[3.2.1]octanil, 2- These are azaspiro[3.3]heptanyl, 2,6-diazaspiro[3.3]heptanyl, 6-azaspiro[3.4]octanyl, 2-azaspiro[3.4]octanyl, 2,7-diazaspiro[3.4]octanyl, 7-azaspiro[3.5]nonanyl, 2-azaspiro[3.5]nonanyl, 2,7-diazaspiro[3.5]nonanyl, 2,7-diazaspiro[4.4]nonanyl, 2,8-diazaspiro[4.5]decanyl, or 3,9-diazaspiro[5.5]undecanyl; and bonded via an N-ring atom; and: If desired, if present, sulfur is substituted with one or two =O groups; Carbon can be added as desired -R Q1NPP -F, -OH, -OR Q1NPP , and are substituted with one or more bases selected from =O; and If desired, secondary nitrogen, if available, -R Q1NPP And, -R Q1NPPX -C(=O)R Q1NPP , -C(=O)OR Q1NPP -C(=O)NH2, -C(=O)NHR Q1NPP -C(=O)NR Q1NPP 2, and -S(=O)2R Q1NPP It is substituted with a group selected from the following. [ka]

[0454] (392) A compound of any of (1) to (387), where: -R Q1NPIf they exist, they exist independently: Azetidinil, pyrrolidinil, piperidinil, piperazinil, 2-azaspiro[3.3]heptanil, These are morpholinil, thiomorpholinil, azepanil, or diazepanil; and bonded via an N-ring atom; and: If desired, if present, sulfur is substituted with one or two =O groups; Carbon can be added as desired -R Q1NPP -F, -OH, -OR Q1NPP , and are substituted with one or more bases selected from =O; and If desired, secondary nitrogen, if available, -R Q1NPP And, -R Q1NPPX -C(=O)R Q1NPP , -C(=O)OR Q1NPP -C(=O)NH2, -C(=O)NHR Q1NPP -C(=O)NR Q1NPP 2, and -S(=O)2R Q1NPP It is substituted with a group selected from the following.

[0455] (393) A compound of any of (1) to (387), where: -R Q1NP If they exist, they exist independently: These are azetidinil, pyrrolidinil, piperidinil, piperazinil, or morpholinil; and bonded via an N-ring atom; and: Carbon can be added as desired -R Q1NPP -F, -OH, -OR Q1NPP , and are substituted with one or more bases selected from =O; and If desired, secondary nitrogen, if available, -R Q1NPP And, -R Q1NPPX -C(=O)R Q1NPP , -C(=O)OR Q1NPP -C(=O)NH2, -C(=O)NHR Q1NPP -C(=O)NR Q1NPP 2, and -S(=O)2RQ1NPP It is substituted with a group selected from the following.

[0456] Group-R Q1NPP (394) A compound of any of (1) to (393), where: Each-R Q1NPP If present, then independently of linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, C 3-6 Cycloalkyl-C 1-3 Alkyl or phenyl, where C 1-4 The alkyl group is optionally substituted with -F, -OH, or -OCH3.

[0457] (395) A compound of any of (1) to (393), where: Each-R Q1NPP If present, these are independently -Me, -Et, -iPr, -iBu, -tBu, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, or phenyl, where -Me, -Et, -iPr, -iBu, or -tBu is optionally substituted with -F, -OH, or -OCH3.

[0458] (396) A compound of any of (1) to (393), where: Each-R Q1NPP If present, then independently of linear or branched saturated C 1-4 Alkyl or phenyl, where C 1-4 The alkyl group is optionally substituted with -F, -OH, or -OCH3.

[0459] (397) A compound of any of (1) to (393), where: Each-R Q1NPP If present, then independently of linear or branched saturated C 1-4The group is alkyl, phenyl, or phenyl-CH2-, where each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0460] (398) A compound of any of (1) to (393), where: Each-R Q1NPP If present, then independently of linear or branched saturated C 1-4 It is alkyl, phenyl, or phenyl-CH2-.

[0461] (399) A compound of any of (1) to (393), where: Each-R Q1NPP If present, then independently of linear or branched saturated C 1-4 It is alkyl.

[0462] (400) A compound of any of (1) to (393), where: Each-R Q1NPP If it exists: The options are -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0463] (401) A compound of any of (1) to (393), where: Each-R Q1NPP If it exists: The options are -Me, -Et, -nPr, or -iPr.

[0464] (402) Any compound from (1) to (393), where: Each-R Q1NPP If it exists: -Me or -Et

[0465] (403) A compound of any of (1) to (393), where: Each-R Q1NPP If it exists: -Me

[0466] Group-R Q1NPPX (404) A compound of any of (1) to (403), where: -R Q1NPPX If present, then independently of linear or branched saturated C 1-4 It is a fluoroalkyl group.

[0467] (405) A compound of any of (1) to (403), where: -R Q1NPPX If they exist, they are independently -CF3, -CHF2, -CH2CF3, or -CH2CHF2.

[0468] (406) A compound of any of (1) to (403), where: -R Q1NPPX If it exists, it is -CH2CF3.

[0469] Group-R Q2C (407) Any compound from (1) to (406), where: Each-R Q2C If they exist, they exist independently: -F, -R Q2CC ,-R Q2CX , -OH, -OR Q2CC , -OR Q2CX , -NH2, -NHR Q2CC , -NR Q2CC 2, -R Q2CM , -NHC(=O)R Q2CC , -NHC(=O)OR Q2CC ,or = O

[0470] (408) Any compound from (1) to (406), where: Each-R Q2C If they exist, they exist independently: -F, -R Q2CC ,-R Q2CX , -OH, -OR Q2CC , -OR Q2CX , -NH2, -NHR Q2CC , -NR Q2CC 2, or -R Q2CM That is the case.

[0471] (409) Any compound from (1) to (406), where: Each-R Q2C If they exist, they exist independently: -F, -R Q2CC ,-R Q2CX , -OH, -OR Q2CC , or -OR Q2CX That is the case.

[0472] Group-R Q2CC (410) A compound of any of (1) to (409), where: Each-R Q2CC If present, then independently of linear or branched saturated C 1-4 The group is alkyl, phenyl, or phenyl-CH2-, where each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0473] (411) Any compound from (1) to (409), where: Each-R Q2CC If present, then independently of linear or branched saturated C 1-4 It is alkyl, phenyl, or phenyl-CH2-.

[0474] (412) Any compound from (1) to (409), where: Each-R Q2CC If present, then independently of linear or branched saturated C 1-4It is alkyl.

[0475] (413) A compound of any of (1) to (409), where: Each-R Q2CC If it exists: The options are -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0476] (414) Any compound from (1) to (409), where: Each-R Q2CC If it exists: The options are -Me, -Et, -nPr, or -iPr.

[0477] (415) Any compound from (1) to (409), where: Each-R Q2CC If it exists: -Me or -Et

[0478] (416) Any compound from (1) to (409), where: Each-R Q2CC If it exists: -Me

[0479] Group-R Q2CX (417) A compound of any of (1) to (416), where: Each-R Q2CX If present, then independently of linear or branched saturated C 1-4 It is a fluoroalkyl group.

[0480] (418) Any compound from (1) to (341), where: Each-R Q2CX If they exist, they are independently -CF3, -CHF2, -CH2CF3, or -CH2CHF2.

[0481] (419) A compound of any of (1) to (416), where: Each-R Q2CX If it exists, it is -CF3.

[0482] Group-R Q2CM (420) A compound of any of (1) to (419), where: Each-R Q2CM If present, they are independently azetidino, pyrrolidino, piperidino, piperadino, morpholino, thiomorpholino, azepano, or diazepano, and: If desired, one or more carbon atoms are added as a group -R Q2CMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q2CMM -C(=O)R Q2CMM , -C(=O)OR Q2CMM -C(=O)NH2, -C(=O)NHR Q2CMM -C(=O)NR Q2CMM 2, and -S(=O)2R Q2CMM It is substituted with a group selected from the following.

[0483] (421) A compound of any of (1) to (419), where: Each-R Q2CM If they exist, they are independently pyrrolidino, piperidino, piperazino, or morpholino, and: If desired, one or more carbon atoms are added as a group -R Q2CMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q2CMM -C(=O)R Q2CMM , -C(=O)OR Q2CMM -C(=O)NH2, -C(=O)NHR Q2CMM , -C(=O)NR Q2CMM 2, and -S(=O)2R Q2CMM It is substituted with a group selected from the following.

[0484] (422) Any compound of (1) to (419), where: Each-R Q2CMIf they exist, they are independently pyrrolidino, piperidino, piperazino, or morpholino, and: If desired, one or more carbon atoms are added as a group -R Q2CMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q2CMM -C(=O)R Q2CMM , and -C(=O)OR Q2CMM It is substituted with a group selected from the following.

[0485] Group-R Q2CMM (423) A compound of any of (1) to (422), where: Each-R Q2CMM If present, then independently of linear or branched saturated C 1-4 The group is alkyl, phenyl, or phenyl-CH2-, where each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0486] (424) A compound of any of (1) to (422), where: Each-R Q2CMM If present, then independently of linear or branched saturated C 1-4 It is alkyl, phenyl, or phenyl-CH2-.

[0487] (425) Any compound from (1) to (422), where: Each-R Q2CMM If present, then independently of linear or branched saturated C 1-4 It is alkyl.

[0488] (426) Any compound of (1) to (422), where: Each-R Q2CMM If it exists: The options are -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0489] (427) Any compound of (1) to (422), where: Each-R Q2CMM If it exists: The options are -Me, -Et, -nPr, or -iPr.

[0490] (428) A compound of any of (1) to (422), where: Each-R Q2CMM If it exists: -Me or -Et

[0491] (429) Any compound of (1) to (422), where: Each-R Q2CMM If it exists: -Me

[0492] Group-R Q2N (430) A compound of any of (1) to (429), where: Each-R Q2N If they exist, they exist independently: -R Q2NC , =O, -C(=O)R Q2NC , C(=O)-L Q2N -R Q2NM , -C(=O)OR Q2NC , -L Q2N -C(=O)NR Q2NC 2, or -S(=O)2R Q2NC That is the case.

[0493] (431) A compound of any of (1) to (429), where: Each-R Q2N If they exist, they exist independently: -R Q2NC , -C(=O)R Q2NC , -C(=O)-L Q2N-OH, -C(=O)-L Q2N -OR Q2NC , -C(=O)-L Q2N -NH2, -C(=O)-L Q2N -NHR Q2NC -C(=O)-L Q2N -NR Q2NC 2. -C(=O)-L Q2N -R Q2NM , -C(=O)OR Q2NC , -C(=O)NH2, -C(=O)NHR Q2NC -C(=O)NR Q2NC 2. -C(=O)R Q2NM , -L Q2N -C(=O)NH2, -L Q2N -C(=O)NHR Q2NC , -L Q2N -C(=O)NR Q2NC 2, or -L Q2N -C(=O)R Q2NM That is the case.

[0494] (432) Any compound of (1) to (429), where: Each-R Q2N If they exist, they exist independently: -R Q2NC , -C(=O)R Q2NC , -C(=O)-L Q2N -OH, -C(=O)-L Q2N -OR Q2NC , -C(=O)-L Q2N -NH2, -C(=O)-L Q2N -NHR Q2NC -C(=O)-L Q2N -NR Q2NC 2. -C(=O)-L Q2N -R Q2NM , -C(=O)NH2, -C(=O)NHR Q2NC -C(=O)NR Q2NC 2, or -C(=O)R Q2NM That is the case.

[0495] (433) Any compound from (1) to (429), where: Each-R Q2N If they exist, they exist independently: -R Q2NC or -C(=O)R Q2NC That is the case.

[0496] (434) Any compound of (1) to (429), where: Each-R Q2N If it exists: -C(=O)R Q2NC That is the case.

[0497] Group-R Q2NC (435) A compound of any of (1) to (434), where: Each-R Q2NC If present, then independently of linear or branched saturated C 1-6 Alkyl, phenyl-C 1-3 Alkyl, or C 5-6 Heteroaryl-C 1-3 It is alkyl, and here, C 1-6 The alkyl groups are optionally substituted with -OH, and each phenyl and heteroaryl group is optionally substituted with one or more groups selected from -Cl and -OCH3.

[0498] (436) Any compound from (1) to (434), where: Each-R Q2NC If present, these are independently -Me, -Et, -t-Bu, t-pentyl, benzyl, or pyridylmethyl, where -Me, -Et, -t-Bu, and t-pentyl are optionally substituted with -OH, and each phenyl and pyridyl is optionally substituted with one or more groups selected from -Cl and -OCH3.

[0499] (437) A compound of any of (1) to (434), where: Each-RQ2NC If present, then independently of linear or branched saturated C 1-6 Alkyl, phenyl, phenyl-CH2-, pyridyl, or pyridyl-CH2-, where C 1-6 Alkyl groups are optionally substituted with -OH or -OCH3, and each phenyl and pyridyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; (438) Any compound from (1) to (434), where: Each-R Q2NC If present, then independently of linear or branched saturated C 1-4 The group is alkyl, phenyl, or phenyl-CH2-, where each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0500] (439) A compound of any of (1) to (434), where: Each-R Q2NC If present, then independently of linear or branched saturated C 1-4 It is alkyl, phenyl, or phenyl-CH2-.

[0501] (440) A compound of any of (1) to (434), where: Each-R Q2NC If present, then independently of linear or branched saturated C 1-4 It is alkyl.

[0502] (441) Any compound from (1) to (434), where: Each-R Q2NC If it exists: The options are -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0503] (442) Any compound from (1) to (434), where: Each-R Q2NC If it exists: The options are -Me, -Et, -nPr, or -iPr.

[0504] (443) Any compound from (1) to (434), where: Each-R Q2NC If it exists: -Me or -Et

[0505] (444) Any compound from (1) to (434), where: Each-R Q2NC If it exists: -Me

[0506] Group-L Q2N - (445) Any compound from (1) to (444), where: Each-L Q2N If it exists, it is independently -CH2-, -C(CH3)2-, -CH2CH2-, or -CH2CH2CH2-.

[0507] (446) Any compound from (1) to (444), where: Each-L Q2N If they exist, - are independently -CH2-, -CH2CH2-, or -CH2CH2CH2-.

[0508] (447) Any compound from (1) to (444), where: Each-L Q2N -If it exists, it is -CH2-.

[0509] (448) Any compound from (1) to (444), where: Each-L Q2N -If it exists, then it is -CH2CH2-.

[0510] (449) Any compound from (1) to (444), where: Each-L Q2N -If it exists, then it is -CH2CH2CH2-.

[0511] Group-R Q2NM (450) Any compound from (1) to (449), where: Each-R Q2NM If present, it independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C 3-11 It is a heterocycline.

[0512] (451) A compound of any of (1) to (449), where: Each-R Q2NM If present, these are pyrrolidinyl or morphilinyl molecules bonded independently via the N-ring atom.

[0513] (452) A compound of any of (1) to (449), where: Each-R Q2NM If present, they are independently azetidino, pyrrolidino, piperidino, piperadino, morpholino, thiomorpholino, azepano, or diazepano, and: If desired, one or more carbon atoms are added as a group -R Q2NMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q2NMM -C(=O)R Q2NMM , -C(=O)OR Q2NMM -C(=O)NH2, -C(=O)NHR Q2NMM -C(=O)NR Q2NMM 2, and -S(=O)2R Q2NMM It is substituted with a group selected from the following.

[0514] (453) Any compound from (1) to (449), where: Each-R Q2NMIf they exist, they are independently pyrrolidino, piperidino, piperazino, or morpholino, and: If desired, one or more carbon atoms are added as a group -R Q2NMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q2NMM -C(=O)R Q2NMM , -C(=O)OR Q2NMM -C(=O)NH2, -C(=O)NHR Q2NMM -C(=O)NR Q2NMM 2, and -S(=O)2R Q2NMM It is substituted with a group selected from the following.

[0515] (454) Any compound from (1) to (449), where: Each-R Q2NM If they exist, they are independently pyrrolidino, piperidino, piperazino, or morpholino, and: If desired, one or more carbon atoms are added as a group -R Q2NMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q2NMM -C(=O)R Q2NMM , and -C(=O)OR Q2NMM It is substituted with a group selected from the following.

[0516] Group-R Q2NMM (455) Any compound from (1) to (454), where: Each-R Q2NMM If present, then independently of linear or branched saturated C 1-4 The group is alkyl, phenyl, or phenyl-CH2-, where each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0517] (456) Any compound from (1) to (454), where: Each-R Q2NMMIf present, then independently of linear or branched saturated C 1-4 It is alkyl, phenyl, or phenyl-CH2-.

[0518] (457) A compound of any of (1) to (454), where: Each-R Q2NMM If present, then independently of linear or branched saturated C 1-4 It is alkyl.

[0519] (458) Any compound of (1) to (454), where: Each-R Q2NMM If it exists: The options are -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0520] (459) Any compound of (1) to (454), where: Each-R Q2NMM If it exists: The options are -Me, -Et, -nPr, or -iPr.

[0521] (460) Any compound from (1) to (454), where: Each-R Q2NMM If it exists: -Me or -Et

[0522] (461) Any compound from (1) to (454), where: Each-R Q2NMM If it exists: -Me

[0523] Group-R Q3C (462) A compound of any of (1) to (461), where: Each-R Q3C If they exist, they exist independently: -F, -R Q3CC , -RQ3CX , -OH, -OR Q3CC , -NHC(=O)R Q3CC , -C(=O)NHR Q3CC -C(=O)R Q3CM , -S(=O)2R Q3CC Or -S(=O)2R Q3CM and; Two adjacent -R Q3C If it exists, then it will be united as -NH-(CH2) q3 C(O)(CH2) v3 -O- is formed, where q3 is 0 and v3 is 1.

[0524] (463) A compound of any of (1) to (461), where: Each-R Q3C If they exist, they exist independently: -F, -Cl, -Br, -I, -R Q3CC , -R Q3CX , -OR Q3CX , -OH, -OR Q3CC , -NH2, -NHR Q3CC , -NR Q3CC 2, -R Q3CM , -NHC(=O)R Q3CC , -NHC(=O)OR Q3CC , -C(=O)NH2, -C(=O)NHR Q3CC -C(=O)NR Q3CC 2. -C(=O)R Q3CM , -C(=O)OH, -C(=O)OR Q3CC , -OC(=O)R Q3CC , -OC(=O)NH2, -OC(=O)NHR Q3CC -OC(=O)NR Q3CC 2. -OC(=O)R Q3CM , -CN, or -NO2 and; Two adjacent -R Q3C If it exists, then it becomes one with -(CH2) n3 -O-(CH2) m3 -or -O-(CH2) p3 -O can be formed.

[0525] (464) A compound of any of (1) to (461), where: Each-R Q3C If they exist, they exist independently: -F, -Cl, -Br, -I, -R Q3CC , -R Q3CX , -OR Q3CX , -OH, -OR Q3CC , -NH2, -NHR Q3CC , -NR Q3CC 2, or -R Q3CM and; Two adjacent -R Q3C If it exists, then it becomes one with -(CH2) n3 -O-(CH2) m3 -or -O-(CH2) p3 -O can be formed.

[0526] (465) A compound of any of (1) to (461), where: Each-R Q3C If they exist, they exist independently: -F, -Cl, -Br, -I, -R Q3CC , -R Q3CX , -OR Q3CX , -OH, or -OR Q3CC That is the case.

[0527] -(CH 2 ) q3 (C(O))-NH-(CH 2 )v3 - and -NH-(CH 2 ) q3 C(O)(CH 2 ) v3 -O-'s exponent "q3" (466) A compound of any of (1) to (465), where: If Q3 exists, then it is 0.

[0528] (467) Any compound from (1) to (465), where: If Q3 exists, then it is 1.

[0529] (468) Any compound from (1) to (465), where: If Q3 exists, then it is 2.

[0530] (469) A compound of any of (1) to (465), where: If Q3 exists, then it is 3.

[0531] -(CH 2 ) q3 (C(O))-NH-(CH 2 ) v3 - and -NH-(CH 2 ) q3 C(O)(CH 2 ) v3 -O- exponent "v3" (470) A compound of any of (1) to (469), where: v3 is 0 if it exists.

[0532] (471) A compound of any of (1) to (469), where: v3 is 1 if it exists.

[0533] (472) Any compound of (1) to (469), where: If v3 exists, it is 2.

[0534] (473) Any compound of (1) to (469), where: If v3 exists, it is 3.

[0535] Group-R Q3CC (474) A compound of any of (1) to (473), where: Each-R Q3CC If present, then independently of linear or branched saturated C 1-4 Alkyl, C 3-6 Cycloalkyl, or C 3-7 It is a heterocycline, and here, C 1-4 The alkyl group is optionally substituted with -F.

[0536] (475) A compound of any of (1) to (473), where: Each-R Q3CC If present, these are independently -Me, -Et, -iPr, -iBu, cyclopropyl, or 4,5-dihydro-1,3-oxazolyl, where -Me, -Et, -iPr, or -iBu is optionally substituted with -F.

[0537] (476) A compound of any of (1) to (473), where: Each-R Q3CC If present, then independently of linear or branched saturated C 1-4 The group is alkyl, phenyl, or phenyl-CH2-, where each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0538] (477) A compound of any of (1) to (473), where: Each-R Q3CC If present, then independently of linear or branched saturated C 1-4 It is alkyl, phenyl, or phenyl-CH2-.

[0539] (478) A compound of any of (1) to (473), where: Each-R Q3CC If present, then independently of linear or branched saturated C 1-4 It is alkyl.

[0540] (479) Any compound from (1) to (473), where: Each-R Q3CC If it exists: The options are -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0541] (480) A compound of any of (1) to (473), where: Each-R Q3CC If it exists: The options are -Me, -Et, -nPr, or -iPr.

[0542] (481) A compound of any of (1) to (473), where: Each-R Q3CC If it exists: -Me or -Et

[0543] (482) A compound of any of (1) to (473), where: Each-R Q3CC If it exists: -Me

[0544] Group-R Q3CX (483) A compound of any of (1) to (482), where: Each-R Q3CX If present, then independently of linear or branched saturated C 1-4 It is a fluoroalkyl group.

[0545] (484) Any compound from (1) to (482), where: Each-R Q3CXIf they exist, they are independently -CF3, -CHF2, -CH2CF3, or -CH2CHF2.

[0546] (485) A compound of any of (1) to (482), where: Each-R Q3CX If it exists, it is -CF3.

[0547] Group-L Q3C - (486) Any compound from (1) to (485), where: Each-L Q3C If it exists, it is independently -CH2-, -C(CH3)2-, -CH2CH2-, or -CH2CH2CH2-.

[0548] (487) A compound of any of (1) to (485), where: Each-L Q3C If they exist, - are independently -CH2-, -CH2CH2-, or -CH2CH2CH2-.

[0549] (488) Any compound from (1) to (485), where: Each-L Q3C -If it exists, it is -CH2-.

[0550] (489) Any compound from (1) to (485), where: Each-L Q3C -If it exists, then it is -CH2CH2-.

[0551] (490) Any compound from (1) to (485), where: Each-L Q3C -If it exists, then it is -CH2CH2CH2-.

[0552] Group-R Q3CM (491) A compound of any of (1) to (490), where: Each-R Q3CM If present, it independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C 3-11 It is a heterocycline; and: If desired, one or more carbon atoms are added to the -R group. Q3CMM It has been replaced with.

[0553] (492) Any compound from (1) to (490), where: Each-R Q3CM If present, it is independently bonded to pyrrolidinyl or 2-azabicyclo[2.2.1]heptyl and is via the N ring atom; and: If desired, one or more carbon atoms are added to the -R group. Q3CMM It has been replaced with.

[0554] (493) A compound of any of (1) to (490), where: Each-R Q3CM If present, they are independently azetidino, pyrrolidino, piperidino, piperadino, morpholino, thiomorpholino, azepano, or diazepano, and: If desired, one or more carbon atoms are added as a group -R Q3CMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q3CMM -C(=O)R Q3CMM , -C(=O)OR Q3CMM -C(=O)NH2, -C(=O)NHR Q3CMM -C(=O)NR Q3CMM 2, and -S(=O)2R Q3CMM It is substituted with a group selected from the following.

[0555] (494) A compound of any of (1) to (490), where: Each-R Q3CM If they exist, they are independently pyrrolidino, piperidino, piperazino, or morpholino, and: If desired, one or more carbon atoms are added as a group -RQ3CMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q3CMM -C(=O)R Q3CMM , -C(=O)OR Q3CMM -C(=O)NH2, -C(=O)NHR Q3CMM -C(=O)NR Q3CMM 2, and -S(=O)2R Q3CMM It is substituted with a group selected from the following.

[0556] (495) A compound of any of (1) to (490), where: Each-R Q3CM If they exist, they are independently pyrrolidino, piperidino, piperazino, or morpholino, and: If desired, one or more carbon atoms are added as a group -R Q3CMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q3CMM -C(=O)R Q3CMM , and -C(=O)OR Q3CMM It is substituted with a group selected from the following.

[0557] Group-R Q3CMM (496) Any compound from (1) to (495), where: Each-R Q3CMM If present, then independently of linear or branched saturated C 1-4 The group is alkyl, phenyl, or phenyl-CH2-, where each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0558] (497) A compound of any of (1) to (495), where: Each-R Q3CMM If present, then independently of linear or branched saturated C 1-4 It is alkyl, phenyl, or phenyl-CH2-.

[0559] (498) Any compound from (1) to (495), where: Each-R Q3CMM If present, then independently of linear or branched saturated C 1-4 It is alkyl.

[0560] (499) Any compound from (1) to (495), where: Each-R Q3CMM If it exists: The options are -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0561] (500) A compound of any of (1) to (495), where: Each-R Q3CMM If it exists: The options are -Me, -Et, -nPr, or -iPr.

[0562] (501) A compound of any of (1) to (495), where: Each-R Q3CMM If it exists: -Me or -Et

[0563] (502) Any compound from (1) to (495), where: Each-R Q3CMM If it exists: -Me

[0564] (503) Any compound from (1) to (495), where: Each-R Q3CMM If it exists: -F

[0565] -(CH 2 ) n3 -O-(CH 2 ) m3 -and-(CH 2 ) n3 -NH-(CH2 ) m3 - The indices "n3" and "m3" (504) A compound of any of (1) to (503), where: n3 is 0, 1, 2, or 3 if it exists; m3 is 0, 1, 2, or 3, if it exists; However, m3 + n3 is either 2 or 3.

[0566] (505) A compound of any of (1) to (503), where: n3 is 0, 1, or 2 if it exists; m3 is 0, 1, or 2, if it exists; However, m3 + n3 is either 2 or 3.

[0567] (506) A compound of any of (1) to (503), where: n3 is either 1 or 2, if it exists; m3 is either 1 or 2, if it exists; However, m3 + n3 is either 2 or 3.

[0568] -O-(CH 2 ) p3 -O- and -NH-(CH 2 ) p3 -NH- index "p3" (507) A compound of any of (1) to (503), where: p3 is 1 if it exists.

[0569] (508) A compound of any of (1) to (503), where: If p3 exists, then it is 2.

[0570] Group-R Q4C (509) A compound of any of (1) to (508), where: Each-R Q4CIf they exist, they exist independently: -F, -R Q4CC And, -R Q4CX , -OH, -OR Q4CC , -OR Q4CX , -NH2, -NHR Q4CC , -NR Q4CC 2, or -R Q4CM That is the case.

[0571] (510) A compound of any of (1) to (508), where: Each-R Q4C If they exist, they exist independently: -R Q4CC And, -R Q4CX , -OH, -OR Q4CC , or -OR Q4CX That is the case.

[0572] (511) A compound of any of (1) to (508), where: Each-R Q4C If they exist, they exist independently: -R Q4CC , -OH, or -OR Q4CC That is the case.

[0573] Group-R Q4CC (512) A compound of any of (1) to (511), where: Each-R Q4CC If present, then independently of linear or branched saturated C 1-4 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 Heteroaryl, or C 5-6 Heteroaryl-C 1-3 The alkyl groups are, where each phenyl and heteroaryl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0574] (513) A compound of any of (1) to (511), where: Each-R Q4CC If present, then independently of linear or branched saturated C 1-4 The group is alkyl, phenyl, or phenyl-CH2-, where each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0575] (514) A compound of any of (1) to (511), where: Each-R Q4CC If present, then independently of linear or branched saturated C 1-4 It is alkyl, phenyl, or phenyl-CH2-.

[0576] (515) A compound of any of (1) to (511), where: Each-R Q4CC If present, then independently of linear or branched saturated C 1-4 It is alkyl.

[0577] (516) A compound of any of (1) to (511), where: Each-R Q4CC If it exists: The options are -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0578] (517) A compound of any of (1) to (511), where: Each-R Q4CC If it exists: The options are -Me, -Et, -nPr, or -iPr.

[0579] (518) A compound of any of (1) to (511), where: Each-R Q4CC If it exists: -Me or -Et

[0580] (519) A compound of any of (1) to (511), where: Each-R Q4CC If it exists: -Me

[0581] Group-R Q4CX (520) A compound of any of (1) to (519), where: Each-R Q4CX If present, then independently of linear or branched saturated C 1-4 It is a fluoroalkyl group.

[0582] (521) A compound of any of (1) to (519), where: Each-R Q4CX If they exist, they are independently -CF3, -CHF2, -CH2CF3, or -CH2CHF2.

[0583] (522) A compound of any of (1) to (519), where: Each-R Q4CX If it exists, it is -CF3.

[0584] Group-R Q4CM (523) A compound of any of (1) to (522), where: Each-R Q4CM If present, they are independently azetidino, pyrrolidino, piperidino, piperadino, morpholino, thiomorpholino, azepano, or diazepano, and: If desired, one or more carbon atoms are added as a group -R Q4CMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q4CMM -C(=O)R Q4CMM , -C(=O)OR Q4CMM -C(=O)NH2, -C(=O)NHR Q4CMM -C(=O)NR Q4CMM 2, and -S(=O)2RQ4CMM It is substituted with a group selected from the following.

[0585] (524) A compound of any of (1) to (522), where: Each-R Q4CM If they exist, they are independently pyrrolidino, piperidino, piperazino, or morpholino, and: If desired, one or more carbon atoms are added as a group -R Q4CMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q4CMM -C(=O)R Q4CMM , -C(=O)OR Q4CMM -C(=O)NH2, -C(=O)NHR Q4CMM -C(=O)NR Q4CMM 2, and -S(=O)2R Q4CMM It is substituted with a group selected from the following.

[0586] (525) A compound of any of (1) to (522), where: Each-R Q4CM If they exist, they are independently pyrrolidino, piperidino, piperazino, or morpholino, and: If desired, one or more carbon atoms are added as a group -R Q4CMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q4CMM -C(=O)R Q4CMM , and -C(=O)OR Q4CMM It is substituted with a group selected from the following.

[0587] Group-R Q4CMM (526) A compound of any of (1) to (522), where: Each-R Q4CMM If present, then independently of linear or branched saturated C 1-4The group is alkyl, phenyl, or phenyl-CH2-, where each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0588] (527) A compound of any of (1) to (522), where: Each-R Q4CMM If present, then independently of linear or branched saturated C 1-4 It is alkyl, phenyl, or phenyl-CH2-.

[0589] (528) A compound of any of (1) to (522), where: Each-R Q4CMM If present, then independently of linear or branched saturated C 1-4 It is alkyl.

[0590] (529) A compound of any of (1) to (522), where: Each-R Q4CMM If it exists: The options are -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0591] (530) A compound of any of (1) to (522), where: Each-R Q4CMM If it exists: The options are -Me, -Et, -nPr, or -iPr.

[0592] (531) A compound of any of (1) to (522), where: Each-R Q4CMM If it exists: -Me or -Et

[0593] (532) A compound of any of (1) to (522), where: Each-R Q4CMM If it exists: -Me

[0594] Group-R Q5C (533) A compound of any of (1) to (532), where: Each-R Q5C If they exist, they exist independently: -OH, -OR Q5CC , -NHC(=O)R Q5CC , -NHC(=O)OR Q5CC , -C(=O)NH2, -C(=O)NHR Q5CC , or -C(=O)R Q5CM That is the case.

[0595] (534) A compound of any of (1) to (532), where: Each-R Q5C If they exist, they exist independently: -OH, -OR Q5CC , -NH2, -NHR Q5CC , -NR Q5CC 2, -R Q5CM , -NHC(=O)R Q5CC , -NHC(=O)OR Q5CC , -C(=O)NH2, -C(=O)NHR Q5CC -C(=O)NR Q5CC 2. -C(=O)R Q5CM , -OC(=O)NH2, -OC(=O)NHR Q5CC -OC(=O)NR Q5CC 2, or -OC(=O)R Q5CM That is the case.

[0596] (535) A compound of any of (1) to (532), where: Each-R Q5C If they exist, they exist independently: -OH, -OR Q5CC , -NH2, -NHR Q5CC , -NR Q5CC 2, -RQ5CM , -NHC(=O)R Q5CC , or -NHC(=O)OR Q5CC That is the case.

[0597] (536) A compound of any of (1) to (532), where: Each-R Q5C If they exist, they exist independently: -NH2, -NHR Q5CC , -NR Q5CC 2, -R Q5CM , -NHC(=O)R Q5CC , or -NHC(=O)OR Q5CC That is the case.

[0598] (537) A compound of any of (1) to (532), where: Each-R Q5C If they exist, they exist independently: -NHC(=O)R Q5CC or -NHC(=O)OR Q5CC That is the case.

[0599] Group-R Q5CC (538) A compound of any of (1) to (537), where: Each-R Q5CC If present, then independently of linear or branched saturated C 1-4 The group is alkyl, phenyl, or phenyl-CH2-, where each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0600] (539) A compound of any of (1) to (537), where: Each-R Q5CC If present, then independently of linear or branched saturated C 1-4 It is alkyl, phenyl, or phenyl-CH2-.

[0601] (540) A compound of any of (1) to (537), where: Each-R Q5CC If present, then independently of linear or branched saturated C 1-4 It is alkyl.

[0602] (541) A compound of any of (1) to (537), where: Each-R Q5CC If it exists: The options are -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0603] (542) A compound of any of (1) to (537), where: Each-R Q5CC If it exists: -Me, -Et, or -tBu.

[0604] (543) A compound of any of (1) to (537), where: Each-R Q5CC If it exists: The options are -Me, -Et, -nPr, or -iPr.

[0605] (544) A compound of any of (1) to (537), where: Each-R Q5CC If it exists: -Me or -Et

[0606] (545) A compound of any of (1) to (537), where: Each-R Q5CC If it exists: -Me

[0607] Group-R Q5CM (546) A compound of any of (1) to (545), where: Each-R Q5CMIf present, it independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C 3-11 It is a heterocycline.

[0608] (547) A compound of any of (1) to (545), where: Each-R Q5CM If present, they are independently azetidino, pyrrolidino, piperidino, piperadino, morpholino, thiomorpholino, azepano, or diazepano, and: If desired, one or more carbon atoms are added as a group -R Q5CMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q5CMM -C(=O)R Q5CMM , -C(=O)OR Q5CMM -C(=O)NH2, -C(=O)NHR Q5CMM -C(=O)NR Q5CMM 2, and -S(=O)2R Q5CMM It is substituted with a group selected from the following.

[0609] (548) A compound of any of (1) to (545), where: Each-R Q5CM If they exist, they are independently pyrrolidino, piperidino, piperazino, or morpholino, and: If desired, one or more carbon atoms are added as a group -R Q5CMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q5CMM -C(=O)R Q5CMM , -C(=O)OR Q5CMM -C(=O)NH2, -C(=O)NHR Q5CMM -C(=O)NR Q5CMM 2, and -S(=O)2R Q5CMM It is substituted with a group selected from the following.

[0610] (549) A compound of any of (1) to (545), where: Each-R Q5CMIf they exist, they are independently pyrrolidino, piperidino, piperazino, or morpholino, and: If desired, one or more carbon atoms are added as a group -R Q5CMM It is replaced by; and If desired, secondary nitrogen, if available, -R Q5CMM -C(=O)R Q5CMM , and -C(=O)OR Q5CMM It is substituted with a group selected from the following.

[0611] (550) A compound of any of (1) to (545), where: Each-R Q5CM If it exists, it is independently morpholino.

[0612] Group-R Q5CMM (551) A compound of any of (1) to (550), where: Each-R Q5CMM If present, then independently of linear or branched saturated C 1-4 The group is alkyl, phenyl, or phenyl-CH2-, where each phenyl group is optionally substituted with one or more groups selected from -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0613] (552) A compound of any of (1) to (550), where: Each-R Q5CMM If present, then independently of linear or branched saturated C 1-4 It is alkyl, phenyl, or phenyl-CH2-.

[0614] (553) A compound of any of (1) to (550), where: Each-R Q5CMM If present, then independently of linear or branched saturated C 1-4 It is alkyl.

[0615] (554) A compound of any of (1) to (550), where: Each-R Q5CMM If it exists: The options are -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[0616] (555) A compound of any of (1) to (550), where: Each-R Q5CMM If it exists: The options are -Me, -Et, -nPr, or -iPr.

[0617] (556) A compound of any of (1) to (550), where: Each-R Q5CMM If it exists: -Me or -Et

[0618] (557) A compound of any of (1) to (550), where: Each-R Q5CMM If it exists: -Me

[0619] A preferred combination (558) When applicable, any of the compounds from (1) to (557), where: -R A3 is -H; and -R A4 is -H.

[0620] For example, ring A is: [ka] That is the case.

[0621] (559) When applicable, any of the compounds from (1) to (557), where: -R A1 ha-R A11 And, -R A11 ha-R A111 And, -RA111 is -Me; -R A2 ha-R A22 And, -R A22 ha-R A222 And, -R A222 is -Me; -R A3 is -H; and -R A4 is -H.

[0622] For example, ring A is: [ka] That is the case.

[0623] (560) When applicable, any of the compounds from (1) to (557), where: Ring B is [ka] and; Y 1 is S; Y 2 is CH or CR Y2 and; Y 3 is N; -R A1 ha-R A11 And, -R A11 ha-R A111 And, -R A111 is -Me; -R A2 ha-R A22 And, -R A22 ha-R A222 And, -R A222 is -Me; -R A3 is -H; and -R A4 is -H.

[0624] For example, the compound has the following structural formula: [ka] It is a compound that has [a certain characteristic].

[0625] (561) When applicable, any of the compounds from (1) to (557), where: Ring B is [ka] and; -R A1 ha-R A11 And, -R A11 ha-R A111 And, -R A111 is -Me; -R A2 ha-R A22 And, -R A22 ha-R A222 And, -R A222 is -Me; -R A3 is -H; -R A4 is -H; and -Q is -Q 1 That is the case.

[0626] For example, the compound has the following structural formula: [ka] It is a compound that has [a certain characteristic].

[0627] (562) When applicable, any of the compounds from (1) to (557), where: Ring B is [ka] That's right; -R A1 ha-R A11 And, -R A11 ha-R A111 And, -R A111 is -Me; -R A2 ha-R A22 And, -R A22 ha-R A222And, -R A222 is -Me; -R A3 is -H; -R A4 is -H; -Q is -Q 1 and -Q 1 It is pyrazolyl and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and If desired, secondary nitrogen, if available, -R Q1N It has been replaced with.

[0628] (563) When applicable, any of the compounds from (1) to (557), where: Ring B is [ka] and; -R A1 ha-R A11 And, -R A11 ha-R A111 And, -R A111 is -Me; -R A2 ha-R A22 And, -R A22 ha-R A222 And, -R A222 is -Me; -R A3 is -H; -R A4 is -H; -Q is -Q 1 and -Q 1 is 1H-pyrazole-3-yl and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and Secondary nitrogen -R Q1N It has been replaced with.

[0629] For example, the compound has the following structural formula: [ka] It is a compound that has [a certain characteristic].

[0630] (564) When applicable, any of the compounds from (1) to (557), where: Ring B is [ka] and; -Q is -Q 1 and -Q 1 is pyridyl and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and Secondary nitrogen -R Q1N It has been replaced with.

[0631] (565) When applicable, any of the compounds from (1) to (557), where: Ring B is [ka] and; -R A1 ha-R A11 And, -R A11 ha-R A111 And, -R A111 is -Me; -R A2 ha-R A22 And, -R A22 ha-R A222 And, -R A222 is -Me; -R A3 is -H; -R A4 is -H; -Q is -Q 1 and -Q 1 is 1H-pyrazole-3-yl and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and Secondary nitrogen -RQ1N It has been replaced with; Here: -R Q1N ha-R Q1NC And, -R Q1Nhet , -L Q1N -C(=O)R Q1NP , or -L Q1N -C(=O)NR Q1NC The answer is 2.

[0632] (566) When applicable, any of the compounds from (1) to (557), where: Ring B is [ka] and; -R A1 ha-R A11 And, -R A11 ha-R A111 And, -R A111 is -Me; -R A2 ha-R A22 And, -R A22 ha-R A222 And, -R A222 is -Me; -R A3 is -H; -R A4 is -H; -Q is -Q 1 and -Q 1 is 1H-pyrazole-3-yl and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and Secondary nitrogen -R Q1N It has been replaced with; Here: -R Q1N ha-L Q1N -C(=O)R Q1NP and -L Q1N - is -CH2-.

[0633] For example, the compound has the following structural formula: [ka] It is a compound that has [a certain characteristic].

[0634] (567) When applicable, any of the compounds from (1) to (557), where: Ring B is [ka] and; -R A1 ha-R A11 And, -R A11 ha-R A111 And, -R A111 is -Me; -R A2 ha-R A22 And, -R A22 ha-R A222 And, -R A222 is -Me; -R A3 is -H; -R A4 is -H; -Q is -Q 1 and -Q 1 is 1H-pyrazole-3-yl and: If desired, one or more carbon atoms are added as a group -R Q1C It is replaced by; and Secondary nitrogen -R Q1N It has been replaced with; Here: -R Q1N ha-R Q1NC That is the case.

[0635] For example, the compound has the following structural formula: [ka] It is a compound that has [a certain characteristic].

[0636] (568) When applicable, any of the compounds from (1) to (557), where: Ring B is [ka] and; -R A1 ha-R A11 And, -R A11 ha-R A111 And, -R A111 is -Me; -R A2 ha-R A22 And, -R A22 ha-R A222 And, -R A222 is -Me; -R A3 is -H; -R A4 is -H; -Q is -Q 1 and -Q 1 is 1H-pyrazole-3-yl and: Secondary nitrogen -R Q1N It has been replaced with; Here: -R Q1N ha-R Q1Nhet That is the case.

[0637] For example, the compound has the following structural formula: [ka] It is a compound that has [a certain characteristic].

[0638] Some specific examples (569) Compound (1), selected from the compounds of the following formula and their pharmaceutically acceptable salts and solvates (e.g., and their pharmaceutically acceptable salts): [Table 1] [Table 2] [Table 3] Table 4 Table 5 Table 6 Table 7 Table 8 Table 9 Table 10 Table 11 Table 12 Table 13 Table 14 Table 15 Table 16 Table 17 Table 18 Table 19 Table 20 Table 21 [Table 22] [Table 23] [Table 24] [Table 25] [Table 26] [Table 27] [Table 28] [Table 29] [Table 30] [Table 31] [Table 32] [Table 33] [Table 34] [Table 35]

[0639] In one embodiment, the BAA compound can be obtained (or obtained) by the following method described in the experimental section.

[0640] In one embodiment, a BAA compound is provided according to any embodiment described herein (e.g., Embodiment (1), (2), or (3); or Claim 1), but any particular embodiment is individually excluded. For example, further properties are any of any embodiments described herein (e.g., Embodiment (1), (2), or (3); or Claim 1), but any of the compounds in the table above (e.g., any one, any two, or any three) are individually excluded.

[0641] In one embodiment, a BAA compound is provided according to any embodiment described herein (e.g., Embodiment (1), (2), or (3); or Claim 1), provided that any other embodiment described herein is not particularly precluded.

[0642] combination For clarity, it is acknowledged that certain properties of the present invention described in the context of separate embodiments may also be provided by combining them into a single embodiment. Conversely, for brevity, various properties of the present invention described in the context of a single embodiment may also be provided separately or in any suitable subcombination. All combinations of embodiments relating to chemical groups represented by variable groups (e.g., ring A, ring B, etc.) are concretely encompassed and disclosed herein as if each and all combinations were individually and explicitly disclosed, insofar as the combinations include compounds that are stable compounds (i.e., compounds that can be isolated, characterized, and tested for biological activity). In this context, it is readily apparent to those skilled in the art that combinations of certain groups (e.g., substituents) may result in compounds that are not readily synthesized and / or are chemically unstable. Furthermore, all subcombinations of chemical groups listed in embodiments describing such variable groups are also concretely encompassed and disclosed herein as if each and all of such subcombinations of chemical groups were individually and explicitly disclosed herein.

[0643] Substantially refined form Certain aspects of the present invention relate to the BAA compounds described herein in substantially purified form and / or in substantially contaminant-free form.

[0644] In certain embodiments, substantially purified form is at least 50% by weight, such as at least 60% by weight, such as at least 70% by weight, such as at least 80% by weight, such as at least 90% by weight, such as at least 95% by weight, such as at least 97% by weight, such as at least 98% by weight, such as at least 99% by weight.

[0645] Unless otherwise specified, substantially purified form refers to the compound in any stereoisomeric or enantiomeric form. For example, in certain embodiments, substantially purified form refers to a mixture of stereoisomers, i.e., purified relative to other compounds. In certain embodiments, substantially purified form refers to one stereoisomer, such as an optically pure stereoisomer. In certain embodiments, substantially purified form refers to a mixture of enantiomers. In certain embodiments, substantially purified form refers to an equimolar mixture of enantiomers (i.e., a racemic mixture, a racemate). In certain embodiments, substantially purified form refers to one enantiomer, such as an optically pure enantiomer.

[0646] In certain embodiments, contaminants are 50% by weight or less, such as 40% by weight or less, such as 30% by weight or less, such as 20% by weight or less, such as 10% by weight or less, such as 5% by weight or less, such as 3% by weight or less, such as 2% by weight or less, such as 1% by weight or less.

[0647] Unless otherwise specified, contaminants refer to other compounds, i.e., those other than stereoisomers or enantiomers. In certain embodiments, contaminants refer to other compounds and other stereoisomers. In certain embodiments, contaminants refer to other compounds and other enantiomers.

[0648] In certain embodiments, a substantially purified form is at least 60% optically pure (i.e., on a molar basis, 60% of the compound is the desired stereoisomer or enantiomer and 40% is the undesired stereoisomer or enantiomer), for example, at least 70% optically pure, for example, at least 80% optically pure, for example, at least 90% optically pure, for example, at least 95% optically pure, for example, at least 97% optically pure, for example, at least 98% optically pure, for example, at least 99% optically pure.

[0649] isomer Certain compounds may exist in one or more specific geometric, optical, enantiomeric, diastereoisomeric, epimeric, atropisomeric, stereoisomeric, tautomeric, conformational, or anomeric forms, including but not limited to cis- and trans-forms; E- and Z-forms; c-, t-, and r-forms; endo- and exo-forms; R-, S-, and meso-forms; D- and L-forms; d- and l-forms; (+) and (-) forms; keto-, enol-, and enolate-forms; syn- and anti-forms; synclinal- and anticlinal-forms; α- and β-forms; axial and equatorial forms; boat-, chair-, twist-, envelope-, and half-chair-forms; and combinations thereof, hereinafter collectively referred to as "isomers" (or "isomeric forms").

[0650] A description of a class of structures may adequately include the structural isomeric forms that fall within that class (e.g., C 1-6 Alkyl includes n-propyl and iso-propyl; butyl includes n-, iso-, sec-, and tert-butyl; methoxyphenyl includes ortho-, meta-, and para-methoxyphenyl).

[0651] However, descriptions of specific groups or substitution patterns are not intended to include other structures (or structural isomers) with different interatomic bonds, rather than spatial positions. For example, the description of a methoxy group, -OCH3, is not interpreted as the description of its structural isomer, a hydroxymethyl group, -CH2OH. Similarly, the specific description of ortho-chlorophenyl is not interpreted as the description of its structural isomer, meta-chlorophenyl.

[0652] The above exclusions do not apply to tautomer forms, such as the keto-, enol-, and enolate-forms in the following tautomer pairs: keto / enol (see diagram below), imine / enamine, amide / iminoalcohol, amidine / amidine, nitroso / oxime, thioketone / enthiol, N-nitroso / hydroxyazo, and nitro / aci-nitro. Here, the description of one tautomer is intended to encompass both tautomers. [ka]

[0653] For example, 1H-pyridine-2-on-5-yl and 2-hydroxyl-pyridine-5-yl (see figure below) are tautomers of each other. A description of one here is intended to include both. [ka]

[0654] It should be noted that the term "isomer" specifically refers to compounds that have one or more isotopic substitutions. For example, H is 1 H, 2 H(D), and 3 Any isotope containing H(T) is acceptable; C is 12 C, 13 C, and 14 Any isotope containing C is acceptable; O is 16 O and 18 Any isotope containing oxygen is acceptable; etc.

[0655] Unless otherwise specified, descriptions of a particular compound include all such isomers, including mixtures thereof (e.g., racemic mixtures). Methods for producing such isomers (e.g., asymmetric synthesis) and separating them (e.g., fractional crystallization and chromatographic means) can be readily obtained by applying known methods, methods taught herein, or known methods using known means.

[0656] Unless otherwise specified, descriptions of a particular compound include all such isomers, including mixtures thereof (e.g., racemic mixtures). Methods for producing such isomers (e.g., asymmetric synthesis) and separating them (e.g., fractional crystallization and chromatographic means) can be readily obtained by applying known methods, methods taught herein, or known methods using known means.

[0657] salt It may be convenient or desirable to manufacture, purify, and / or handle the corresponding salts of compounds, pharmaceutically acceptable salts. The term “salt” here refers to a solid complex comprising a first co-formation (e.g., a compound such as a BAA compound) and a second co-formation (e.g., a suitable Brønsted acid or base) where there is complete proton transfer from one substance to the other. An example of pharmaceutically acceptable salts is found in Berge et al., 1977, “Pharmaceutically Acceptable Salts,” J. Pharm. Sci. This is described in Vol. 66, pp. 1-19.

[0658] For example, a compound may be anionic or may have an anionic functional group (e.g., -COOH is -COO - If it has (possibly), then a suitable cation and salt can be formed. Examples of suitable inorganic cations are alkali metal ions, such as Na. + and K + , alkaline earth cations, for example, Ca 2+ and Mg 2+ , and other cations, such as Al 3+ Furthermore, ammonium ions (i.e., NH4)+ This includes, but is not limited to, ) and substituted ammonium ions (e.g., NH3R). + NH2R2 + NHR3 + NR4 + This includes, but is not limited to, ) and for example, here each R is independently linear or branched saturated C 1-18 Alkyl, C 3-8 Cycloalkyl, C 3-8 Cycloalkyl-C 1-6 Alkyl and phenyl-C 1-6 It is alkyl, where the phenyl group is optionally substituted. Some suitable substituted ammonium ions include: ethylamine, diethylamine, dicyclohexylamine, triethylamine, butylamine, ethylenediamine, ethanolamine, diethanolamine, piperazine, benzylamine, phenylbenzylamine, choline, meglumine, and tromethamine, as well as those derived from amino acids, such as lysine and arginine. A common example of a quaternary ammonium ion is N(CH3)4 + That is the case.

[0659] The compound is cationic, or has a functional group that can become cationic by protonation (e.g., -NH2 is -NH3). + If it has (which can be), then a suitable anion and salt can be formed.

[0660] For example, the parent structure contains cationic properties, or the functional group can become cationic through protonation (e.g., -NH2 is -NH3). + If it has a cationic group (e.g., -NMe2), then a suitable anion and salt can be formed. In the case of quaternary ammonium compounds, a counter-anion is generally always present for the equilibrium of positive charge. + , -NH3 + In addition to the above, if the compound also contains a group that can form an anion (e.g., -COOH), then an intramolecular salt (also called a zwitterion) may be formed.

[0661] Examples of suitable inorganic anions include, but are not limited to, those derived from the following inorganic acids: hydrochloric acid, hydrobromic acid, hydroiodic acid, sulfuric acid, sulfurous acid, nitric acid, nitrous acid, phosphoric acid, and phosphorous acid.

[0662] Examples of suitable organic anions include, but are not limited to, those derived from the following organic acids: 2-acetoxybenzoic acid, acetic acid, trifluoroacetic acid, ascorbic acid, aspartic acid, benzoic acid, camphorsulfonic acid, cinnamic acid, citric acid, edetic acid, 1,2-ethanedisulfonic acid, ethanesulfonic acid, fumaric acid, glucoheptonic acid, gluconic acid, glutamic acid, glycolic acid, hydroxymaleic acid, hydroxynaphthalenecarboxylic acid, isethionic acid, lactic acid, lactobionic acid, lauric acid, maleic acid, malic acid, methanesulfonic acid, mucic acid, oleic acid, oxalic acid, palmitic acid, pamoic acid, pantothenic acid, phenylacetic acid, phenylsulfonic acid, propionic acid, pyruvic acid, salicylic acid, stearic acid, succinic acid, sulfanilic acid, tartaric acid, toluenesulfonic acid, and valeric acid. Examples of suitable polymeric organic anions include, but are not limited to, those derived from the following polymeric acids: tannic acid, carboxymethylcellulose.

[0663] 4-Quaternary ammonium compounds (e.g., those having a -NMe2 + group) particularly suitable examples of suitable counterions include 1-adamantanesulfonic acid, benzenesulfonic acid, bisulfate, bromide, chloride, iodide, methanesulfonic acid, methyl sulfate, 1,5-naphthalene-bissulfonic acid, 4-nitrobenzenesulfonic acid, formic acid, tartaric acid, tosyl acid, trifluoroacetic acid, trifluoromethylsulfonic acid, sulfuric acid. Similarly, if the compound also contains a group capable of forming an anion (e.g., -COOH), an internal salt can be formed.

[0664] Unless otherwise specified, the description of a particular compound includes its salt forms.

[0665] In certain embodiments, the BAA compound is provided in salt form.

[0666] In one embodiment, the BAA compound is provided in a neutral form (e.g., as a free acid, free base, or zwitterion).

[0667] Solvates and hydrates It may be convenient or desirable to prepare, purify, and / or handle the corresponding solvates of compounds. The term “solvate” is used here in its conventional sense, referring to a complex of a solute (e.g., a compound, a salt of a compound) and a solvent. If the solvent is water, the solvate may for convenience be called a hydrate, e.g., monohydrate, dihydrate, acid hydrate, etc.

[0668] Unless otherwise specified, descriptions of specific compounds include their solvates and hydrates.

[0669] In one embodiment, the BAA compound is provided in the form of a solvate.

[0670] In one embodiment, the BAA compound is provided in the form of a hydrate.

[0671] In one embodiment, the BAA compound is provided in a non-solvated form.

[0672] Chemically protected form It may be convenient or desirable to prepare, purify, and / or handle compounds in a chemically protected form. The term “chemically protected form” is used here in its conventional chemical sense and refers to a compound in which one or more reactive functional groups are protected from undesirable chemical reactions under specific conditions (e.g., pH, temperature, radiation, solvent, reactive chemical reagent, etc.). In practice, this involves using well-known chemical methods to make a functional group that would otherwise be reactive reversibly unreactive under specific conditions. In a chemically protected form, one or more reactive functional groups are protected or in the form of protecting groups (or masked or masking groups or blocked or blocking groups). Protection of a reactive functional group allows reactions involving other unprotected reactive functional groups to be carried out without affecting the protected group; the protecting group is usually removed by subsequent fixation or the masking group is deformed, with substantially no effect on the rest of the molecule. See, for example, Protective Groups in Organic Synthesis (T. Green and P. Wuts; 4th Edition; John Wiley and Sons, 2006).

[0673] A wide variety of such "protection," "blocking," or "masking" methods are widely used and well-known in organic synthesis. For example, a compound having two non-equivalent reactive functional groups, both of which are reactive under specific conditions, can be derivatized to "protect" one of the functional groups, thereby making it unreactive under specific conditions; the thus protected compound can then be used as a reactant efficiently possessing only one of the reactive functional groups. After the desired reaction (involving the other functional group) is complete, the protected group can be "deprotected" to return it to its original functional group.

[0674] For example, the hydroxyl group can be protected as an ether (-OR) or ester (-OC(=O)R), e.g., t-butyl ether; benzyl, benzhydryl(diphenylmethyl), or trityl(triphenylmethyl) ether; trimethylsilyl or t-butyldimethylsilyl ether; or acetyl ester (-OC(=O)CH3, -OAc).

[0675] For example, the aldehyde or ketone group can be protected as an acetal (R-CH(OR)2) or ketal (R2C(OR)2), respectively, where the carbonyl group (>C=O) is converted to a 1,1-diether (>C(OR)2) by reaction with a primary alcohol, for example, in the presence of an acid. The aldehyde or ketone group is readily regenerated, for example, by hydrolysis using water in the presence of an acid.

[0676] For example, amine groups include amides (-NRCO-R), e.g., acetamide (-NHCO-CH3); or carbamates (-NRCO-OR), e.g., benzyloxycarbamate (-NHCO-OCH2C6H5, -NH-Cbz), t-butoxycarbamate (-NHCO-OC(CH3)3, -NH-Boc); 2-biphenyl-2-propoxycarbamate (-NHCO-OC(CH3)2C6H4C6H5, -NH-Bpoc), 9-fluorenylmethoxycarbamate (-NH-Fmoc), and 6-nitroveratril. They may be protected as oxycarbamates (-NH-Nvoc), 2-trimethylsilylethyloxycarbamate (-NH-Teoc), 2,2,2-trichloroethyloxycarbamate (-NH-Troc), allyloxyamide (-NH-Alloc), or 2(-phenylsulfonyl)ethyloxycarbamate (-NH-Psec); or, where appropriate (e.g., cyclic amines), nitrooxide radicals (>NO●); or, where appropriate (e.g., heterocyclic nitrogen), 2-trimethylsilylethoxymethyl (N-SEM).

[0677] For example, a carboxylic acid group is an ester, for example: C 1-7 Alkyl esters (e.g., methyl esters; t-butyl esters); C 1-7 Haloalkyl esters (e.g., 2,2,2-trihaloethyl esters); 2-tri(C 1-7 Alkyl)silyl-ethyl ester; or C 5-20 Aryl-C 1-7Alkyl esters (e.g., benzyl esters; nitrobenzyl esters); or amides or hydrazides, such as acetamide or N,N,N'-trimethylhydrazide, may be protected.

[0678] For example, the thiol group can be protected as a thioether (-SR), such as benzyl thioether; or acetamidomethyl ether (-S-CH2NHC(=O)CH3).

[0679] Prodrug It may be convenient or desirable to manufacture, purify, and / or handle compounds in the form of prodrugs. As used herein, “prodrug” refers to a compound that produces a desired active compound in vivo. Typically, prodrugs are inactive or less active than the desired active compound, but may offer advantageous handling, administration, or metabolic properties.

[0680] For example, some prodrugs are esters of active compounds (e.g., physiologically acceptable metabolically unstable esters). During metabolism, the ester group (-C(=O)OR) is cleaved to produce the active drug. Such esters may be formed, for example, by esterification with any carboxylic acid group (-C(=O)OH) of the parent compound, and, where appropriate, before protection of any other reactive groups present in the parent compound, and subsequently deprotected if necessary.

[0681] Furthermore, some prodrugs are enzymatically activated to produce active compounds, or compounds that produce active compounds through further chemical reactions (for example, in antibody-directed enzyme prodrug therapy (ADEPT), gene-directed enzyme prodrug therapy (GDEPT), ligand-directed enzyme prodrug therapy (LIDEPT), etc.). For example, prodrugs may be sugar derivatives or other glycoside conjugates, or amino acid ester derivatives.

[0682] composition Compositions (e.g., pharmaceutical compositions) comprising the BAA compounds described herein and pharmaceutically acceptable carriers, diluents, or additives are also described herein.

[0683] Methods for preparing compositions (e.g., pharmaceutical compositions) comprising mixing the BAA compounds described herein with pharmaceutically acceptable carriers, diluents, or additives are also described herein.

[0684] use The BAA compounds described herein inhibit PKMYT1 (for example, by inhibiting, reducing, or blocking the activity or function of PKMYT1).

[0685] Therefore, the BAA compounds described herein are useful for treating disorders (e.g., diseases) that are improved by inhibition of PKMYT1 (e.g., by inhibition, reduction, or blockade of PKMYT1 activity or function).

[0686] Use in PKMYT1 inhibition methods Methods for inhibiting PKMYT1 in vitro or in vivo (e.g., inhibiting, reducing, or blocking the activity or function of PKMYT1) are also described herein, comprising contacting PKMYT1 with an effective amount of one of the BAA compounds described herein.

[0687] Methods for inhibiting PKMYT1 in cells in vitro or in vivo (e.g., inhibiting, reducing, or blocking the activity or function of PKMYT1) are also described herein, which include contacting cells with an effective amount of the BAA compound described herein.

[0688] In one embodiment, the method is performed in vitro.

[0689] In one embodiment, the method is performed in vivo.

[0690] In one embodiment, the BAA compound is provided in the form of a pharmaceutically acceptable composition.

[0691] Those skilled in the art can readily determine whether a candidate compound inhibits PKMYT1 (e.g., inhibits, reduces, or blocks the activity or function of PKMYT1). For example, suitable assays are described herein and / or known in the art.

[0692] Those skilled in the art can readily determine whether a candidate compound inhibits PKMYT1 in cells (e.g., inhibits, reduces, or blocks the activity or function of PKMYT1). For example, a sample of cells can be grown in vitro, the compound can be brought into contact with the cells, and the effect of the compound on the cells can be observed. As an example of “effect,” the morphological status of the cells (e.g., viability, etc.) can be determined. If the compound is found to affect the cells, this can be used as a prognostic or diagnostic marker of the compound’s effectiveness in treating subjects (e.g., patients) possessing cells of the same cell type. As another example of “effect,” the direct interaction between the compound and its target in cells can be measured, for example, using colorimetric analysis, fluorescence, or luminescence readout information (e.g., “target binding assays”).

[0693] Uses in methods for inhibiting cell proliferation, etc. The BAA compounds described herein may, for example, (a) control (e.g., inhibit) cell proliferation; (b) inhibit cell cycle progression; (c) promote apoptosis; (d) reduce clonal capacity; (e) reduce tumor-like growth or self-renewal; (f) enhance the effects of DNA damaging agents in cytotoxicity; or (g) perform one or more of these in combination.

[0694] Therefore, also described herein are methods, either in vitro or in vivo, for controlling (e.g., inhibiting) cell proliferation, promoting cell cycle progression, promoting apoptosis, reducing clonal capacity, reducing tumor-like growth or self-renewal, or a combination thereof, comprising contacting cells with an effective amount of the BAA compound described herein.

[0695] In one embodiment, the method is performed in vitro.

[0696] In one embodiment, the method is performed in vivo.

[0697] In one embodiment, the BAA compound is provided in the form of a pharmaceutically acceptable composition.

[0698] It can treat or target any type of cell, including, for example, blood (e.g., neutrophils, eosinophils, basophils, lymphocytes, monocytes, red blood cells, platelets), lungs, digestive tract (e.g., intestines, colon), breasts (mammary glands), ovaries, prostate, liver (liver), kidney (kidney), bladder, pancreas, brain, and skin cells.

[0699] Those skilled in the art can easily determine whether a candidate compound controls (e.g., inhibits) cell proliferation. For example, assays that can be easily used to evaluate the activity provided by a particular compound are described herein and / or known in the art.

[0700] The BAA compounds described herein can inhibit cell migration and invasion, for example, inhibit metastasis.

[0701] The BAA compounds described herein may restore sensitivity to other agents in resistant cell populations.

[0702] The BAA compounds described herein may prevent cell populations from developing resistance to other agents.

[0703] The BAA compounds described herein may enhance the effects of other agents on DNA damage and subsequent cell elimination. Such agents may be therapeutic compounds that cause DNA damage or interfere with the DNA damage response.

[0704] Use in treatment methods Also described herein are BAA compounds for use in methods of treating human or animal bodies by therapeutic means, for example, for use in methods of treating the disorders (e.g., diseases) described herein.

[0705] Also described herein is the use of the BAA compounds described herein in methods of treating the human or animal body in the course of treatment, for example, in methods of treating the disorders (e.g., diseases) described herein.

[0706] Use in the manufacture of pharmaceuticals Also described herein are the use of the BAA compounds described herein in the manufacture of pharmaceuticals, for example, for use in methods of treatment, for example, for use in methods of treatment of the disorders (e.g., diseases) described herein.

[0707] In one embodiment, the pharmaceutical product contains a BAA compound.

[0708] Treatment method Also described herein are methods of treatment, for example, methods of treatment for the disorders (e.g., diseases) described herein, which include administering a therapeutically effective amount of the BAA compound described herein to an object requiring treatment, preferably in the form of a pharmaceutical composition.

[0709] Disorders treated - Disorders improved by inhibiting PKMYT1 In one embodiment (for example, a compound for use in a therapeutic method, use in a therapeutic method, use in the manufacture of a pharmaceutical product, or a treatment method), the treatment is the treatment of a disorder (e.g., a disease) that is improved by inhibition of PKMYT1 (e.g., by inhibition, reduction, or blockade of the activity or function of PKMYT1).

[0710] Disorders to be treated In one embodiment (for example, a compound for use in a therapeutic method, use in a therapeutic method, use in the manufacture of a pharmaceutical product, or treatment method), the treatment is the treatment of a disorder (e.g., a disease) described herein, such as proliferative disorders or cancer.

[0711] Proliferative disorder In one embodiment, the disorder is a proliferative disorder.

[0712] The term "proliferative disorder" as used herein refers to unwanted, excessive, or uncontrolled cell proliferation of abnormal cells, such as neoplasms or hyperplastic proliferation.

[0713] In one embodiment, proliferative disorders are characterized by benign, pre-malignant, malignant, pre-metastatic, metastatic, or non-metastatic cell proliferation, including, for example: neoplasms, hyperplasia, tumors (e.g., histiocytoma, glioma, astrocytoma, osteoma), cancer, psoriasis, bone diseases, fibroproliferative disorders (e.g., of connective tissue), pulmonary fibrosis, atherosclerosis, and smooth muscle cell proliferation of blood vessels such as stenosis or restenosis after angioplasty.

[0714] Disorders treated - Proliferative disorders In one embodiment (for example, use in a therapeutic method, use in the manufacture of a pharmaceutical product, or treatment method), the treatment is treatment for a proliferative disorder.

[0715] The term "proliferative disorder" as used herein refers to unwanted, excessive, or uncontrolled cell proliferation of abnormal cells, such as neoplasms or hyperplastic proliferation.

[0716] In one embodiment, the treatment is the treatment of a proliferative disorder characterized by benign, premalignant, or malignant cell proliferation.

[0717] In one embodiment, the treatment is the treatment of a proliferative disorder characterized or further characterized by inappropriate activity and / or expression of PKMYT1, CCNE1, FBXW7, or PPP2A or one of its subunits.

[0718] In one embodiment, the treatment is the treatment of a proliferative disorder characterized or further characterized by overexpression of PKMYT1 or CCNE1.

[0719] In one embodiment, the treatment is the treatment of a proliferative disorder characterized by or further characterized by overexpression of PKMYT1.

[0720] In one embodiment, the treatment is the treatment of a proliferative disorder characterized by or further characterized by overexpression of CCNE1.

[0721] In one embodiment, the treatment is a treatment for proliferative impairment characterized or further characterized by inactivation, reduced activity, or reduced expression of FBXW7 or PPP2R2A.

[0722] In one embodiment, the treatment is a treatment for a proliferative disorder characterized by or further characterized by the inactivation of FBXW7.

[0723] In one embodiment, the treatment is a treatment for a proliferative disorder characterized or further characterized by reduced activity or expression of PPP2R2A.

[0724] In one embodiment, the procedure is a cancer treatment.

[0725] Disorders treated - Cancer In one embodiment (for example, use in a treatment method, use in the manufacture of a pharmaceutical product, or treatment method), the treatment is a treatment for cancer.

[0726] Cancers, in particular, include: (1) Carcinomas including tumors originating from stratified squamous epithelium (squamous cell carcinoma) and tumors occurring within organs or glands (adenocarcinoma). Examples include breast, colon, lung, prostate, and ovary.

[0727] (2) Sarcomas including osteosarcoma and osteogenic sarcoma (bone); chondrosarcoma (cartilage); leiomyosarcoma (smooth muscle); rhabdomyosarcoma (skeletal muscle); mesosarcoma and mesothelioma (membranes lining body cavities); fibrosarcoma (fibrous tissue); angiosarcoma and hemangioendothelioma (blood vessels); liposarcoma (adipose tissue); glioma and astrocytoma (neuronal connective tissue found in the brain); myxosarcoma (primitive embryonic connective tissue); and mesenchymal and mixed mesodermal tumors (mixed connective tissue type).

[0728] (3) Myeloma.

[0729] (4) Myeloid and granulocytic leukemias (malignancies of the bone marrow and granulocytic leukocyte series), e.g., chronic myeloid leukemia (CML), acute myeloid leukemia (AML); lymphoid, lymphocytic, and lymphoblastic leukemias (malignancies of the lymphoid and lymphocytic blood cell series), e.g., acute lymphoblastic leukemia (ALL), chronic lymphocytic leukemia (CLL); hematopoietic malignancies, including polycythemia vera (malignancies of various blood cell products, but with a predominantly red blood cell population).

[0730] (5) Lymphomas, including Hodgkin and non-Hodgkin lymphomas.

[0731] (6) Mixed types including adenosquamous cell carcinoma; mixed mesodermal tumors; carcinosarcoma; and teratocarcinoma.

[0732] One argument is that cancer is: Bone or muscle sarcomas, e.g.: bone cancer; osteosarcoma; chondrosarcoma; Ewing's sarcoma; cardiac cancer; leiomyosarcoma; malignant fibrous histiocytoma of bone; osteosarcoma; or rhabdomyosarcoma; Brain and nervous system cancers, for example: Astrocyteoma; brain cancer; brainstem glioma; cerebellar astrocytoma; cerebral astrocytoma; ependymoma; glioblastoma; glioma; medulloblastoma; neuroblastoma; oligodendroglioma; pilocytic astrocytoma; pineal astrocytoma; pituitary adenoma; primitive neuroectodermal tumor; Schwannoma; or visual tract and hypothalamic glioma; Breast cancer, e.g.: breast cancer; invasive cribriform carcinoma; inflammatory breast cancer; invasive lobular carcinoma; medullary carcinoma; male breast cancer; phyllodes tumor; or tubular carcinoma; Endocrine cancers, e.g.: adrenal cancer; adrenocortical cancer; papillary thyroid cancer; follicular thyroid cancer; islet cell carcinoma; multiple endocrine neoplasia syndrome; parathyroid cancer; pheochromocytoma; thyroid cancer; or thyroid cancer; Eye cancers, for example: retinoblastoma; or uveal melanoma; Gastrointestinal cancers, for example: Anal cancer; appendiceal cancer; bile duct cancer; intestinal cancer; cholangiocarcinoma; colonic adenocarcinoma; colonic adenoma; colon cancer; exocrine pancreatic cancer; extrahepatic bile duct cancer; gallbladder cancer; stomach (gastric) cancer; digestive tract cancer; digestive tract carcinoid tumor; digestive tract carcinoid tumor; digestive tract stromal tumor (GIST); hepatocellular carcinoma; hepatoblastoma; kidney cancer; colorectal cancer; liver cancer; colorectal cancer; pancreatic cancer; rectal cancer; or small intestine cancer; Cancers of the genitourinary tract or gynecology, e.g.: bladder cancer; cervical cancer; endometrial cancer; extragonadal germ cell tumors; genitourinary cancers; gestational trophoblastic neoplasms; gynecology cancers; ovarian cancer; ovarian epithelial cancer; ovarian germ cell tumors; penile cancer; prostate cancer; renal cell carcinoma; transitional cell carcinoma of the renal pelvis and ureter; testicular epithelioma; teratoma; testicular cancer; transitional cell carcinoma of the ureter and renal pelvis; urethral cancer; uterine sarcoma; vaginal cancer; vulvar cancer; or Wilms' tumor; Head and neck cancers, e.g.: esophageal cancer; craniocervical cancer; squamous cell carcinoma of the head and neck; hypopharyngeal cancer; nasopharyngeal cancer; nasopharyngeal carcinoma; oral cancer; oropharyngeal cancer; sinus and nasal cavity cancer; pharyngeal cancer; or salivary gland cancer; Hematopoietic cancer, for example: Plasma cell neoplasms, such as plasmacytoma or multiple myeloma; Leukemia, for example: acute mixed leukemia; acute eosinophilic leukemia; acute lymphoblastic leukemia; acute myeloid dendritic cell leukemia; acute myeloid leukemia; acute promyelocytic leukemia; B-cell prelymphoblastic leukemia; chronic lymphocytic leukemia; chronic myeloid leukemia; hairy cell leukemia; macrogranular lymphocytic leukemia; mast cell leukemia; precursor B-cell lymphoblastic leukemia; T-cell prelymphoblastic leukemia; Lymphoma, e.g.: AIDS-associated lymphoma; anaplastic large cell lymphoma; angioimmunoblastic T-cell lymphoma; Burkitt lymphoma; cutaneous T-cell lymphoma; generalized large B-cell lymphoma; follicular lymphoma; pleomorphic T-cell lymphoma; Hodgkin lymphoma; intravascular large B-cell lymphoma; lymphomatoid granulomatosis; lymphoplasmacytic lymphoma; mantle cell lymphoma; marginal zone B-cell lymphoma; mediastinal large B-cell lymphoma; mucosal connective tissue lymphoma; mycosis fungoides; nodular marginal zone B-cell lymphoma; non-Hodgkin lymphoma; plasmablastic lymphoma; primary central nervous system lymphoma; primary cutaneous follicular lymphoma; primary cutaneous immunocytomas; primary exudative lymphoma; Sézary syndrome; or splenic marginal zone lymphoma; or Myelodysplastic syndrome; Skin cancers, for example: basal cell carcinoma; dermatofibrosarcoma protuberans; fibrosarcoma; keratosacral cell carcinoma; malignant melanoma; melanoma; Merkel cell carcinoma; sebaceous carcinoma; or squamous cell carcinoma; Cancers of the chest and respiratory system, e.g.: adenocarcinoma; bronchial adenoma; bronchial carcinoid; laryngeal cancer; lung cancer; mediastinal cancer; mesothelioma; non-small cell lung cancer; peritoneal cancer; pleuroblastoma; small cell lung cancer; thymic cancer; or thymoma carcinoma; HIV / AIDS-related cancers, such as Kaposi's sarcoma; or other cancers, such as epithelioid hemangioendothelioma; fibrous round cell tumor; or liposarcoma. That is the case.

[0733] One argument is that cancer is: Endometrial cancer, uterine cancer, ovarian cancer, breast cancer, stomach cancer, bladder cancer, pancreatic cancer, mesothelioma, kidney cancer, esophageal cancer, colorectal cancer, glioblastoma, lung cancer, or squamous cell carcinoma of the lung That is the case.

[0734] In one example, the cancer is endometrial cancer.

[0735] In one version, the cancer is uterine cancer.

[0736] In one embodiment, the cancer is ovarian cancer.

[0737] In one way, the cancer is breast cancer.

[0738] In one example, the cancer is stomach cancer.

[0739] In one embodiment, the cancer is bladder cancer.

[0740] In one embodiment, the cancer is pancreatic cancer.

[0741] In one manifestation, the cancer is mesothelioma.

[0742] In one possible explanation, the cancer is kidney cancer.

[0743] In one example, the cancer is stomach cancer.

[0744] In one example, the cancer is esophageal cancer.

[0745] In one embodiment, the cancer is colorectal cancer.

[0746] In one embodiment, the cancer is glioblastoma.

[0747] In one interpretation, the cancer is lung cancer.

[0748] In one embodiment, the cancer is a squamous cell carcinoma of the lung.

[0749] In one embodiment, cancer is characterized or further characterized by inappropriate activity (e.g., overexpression) of PKMYT1. For example, in one embodiment, cancer is: Squamous cell carcinoma of the lung, adenocarcinoma of the lung, endometrioid carcinoma of the uterine body, breast cancer, invasive breast cancer, hepatocellular carcinoma, clear cell carcinoma of the kidney, chromophobic renal cell carcinoma, papillary cell carcinoma of the kidney, squamous cell carcinoma of the head and neck, adenocarcinoma of the colon, adenocarcinoma of the stomach, thyroid cancer, adenocarcinoma of the prostate, adrenal cortical carcinoma, low-grade glioma, mesothelioma, adenocarcinoma of the pancreas, melanoma of the skin, melanoma of the uvea That is the case.

[0750] In one embodiment, cancer is characterized or further characterized by the involvement of PKMYT1 in progression, invasion, and / or metastasis. For example, in one embodiment, cancer: Non-small cell lung cancer, osteosarcoma, clear cell renal carcinoma, oral squamous cell carcinoma, gastric cancer, prostate cancer, esophageal squamous cell carcinoma, colorectal cancer, hepatocellular carcinoma, ovarian cancer, neuroblastoma (especially with MYCN amplification), glioblastoma, acute lymphoblastic leukemia, multiple myeloma, Kaposi's sarcoma, primary exudative lymphoma (PEL), or plasmablastic subtype of multicentric Castleman disease. That is the case.

[0751] In one embodiment, cancer is characterized or further characterized by inappropriate activity (e.g., overexpression) of CCNE1. For example, in one embodiment, cancer is: Uterine carcinosarcoma, uterine cancer, endometrial cancer, breast cancer, ovarian cancer, stomach cancer, colorectal cancer, bladder cancer, esophageal cancer, cervical cancer, sarcoma, lung squamous cell carcinoma, adenoid cystic carcinoma, pancreatic cancer, mesothelioma, lung adenocarcinoma, head and neck cancer, generalized large B-cell lymphoma, or liver cancer That is the case.

[0752] In one embodiment, cancer is characterized or further characterized by inappropriate activity (e.g., overexpression) of CCNE1. For example, in one embodiment, cancer is: Uterine carcinosarcoma, uterine cancer, endometrial cancer, breast cancer, ovarian cancer, stomach cancer, colorectal cancer, bladder cancer, esophageal cancer, cervical cancer, sarcoma, or pulmonary squamous cell carcinoma That is the case.

[0753] In one embodiment, the cancer is uterine carcinosarcoma (UCS) or serous uterine carcinoma (USC).

[0754] In one embodiment, the cancer is high-grade serous ovarian cancer (HGSOC).

[0755] In one embodiment, the cancer is a high-grade serous ovarian cancer with CCNE1 amplification.

[0756] In one embodiment, the cancer is triple-negative breast cancer (TNBC).

[0757] In one embodiment, cancer is characterized or further characterized by inappropriate activity (e.g., inactivation) of FBXW7. For example, in one embodiment, cancer is: Uterine carcinosarcoma, uterine cancer, endometrial cancer, breast cancer, ovarian cancer, stomach cancer, colorectal cancer, bladder cancer, esophageal cancer, cervical cancer, sarcoma, lung squamous cell carcinoma, or head and neck cancer That is the case.

[0758] In one embodiment, cancer is characterized or further characterized by inappropriate activity (e.g., inactivation) of FBXW7. For example, in one embodiment, cancer is: Uterine carcinosarcoma, endometrial cancer, colorectal cancer, cervical cancer, bladder cancer, head and neck cancer, stomach cancer, or lung squamous cell carcinoma That is the case.

[0759] In one embodiment, the cancer is uterine carcinosarcoma (UCS) or serous uterine carcinoma (USC).

[0760] In one embodiment, cancer is characterized or further characterized by inappropriate activity of PPP2R2A (e.g., inactivation, reduced activity, reduced expression). For example, in one embodiment, cancer is: Prostate adenocarcinoma, ovarian serous adenocarcinoma, rectal adenocarcinoma, bladder urothelial carcinoma, colorectal adenocarcinoma, invasive breast cancer, endometrioid carcinoma of the uterine body, carcinosarcoma of the uterus, hepatocellular carcinoma of the liver, squamous cell carcinoma of the lung, or lung adenocarcinoma That is the case.

[0761] In one embodiment, cancer (e.g., as described above) is characterized or further characterized as a treatment-resistant cancer, e.g., chemotherapy-resistant cancer, radiotherapy-resistant cancer, and / or immunotherapy-resistant cancer.

[0762] In one embodiment, treatment-resistant cancer is resistant to standard therapy.

[0763] In one embodiment, treatment-resistant cancer is resistant to one or more PARP inhibitors, cisplatin, WEE1 inhibitors, and Cdk4 / 6 inhibitors.

[0764] In one embodiment, treatment-resistant cancer is ovarian cancer with recombinant ability. In one embodiment, treatment-resistant cancer is HER2-ER+ breast cancer with Cdk4 / 6 resistance.

[0765] In one embodiment, cancer (e.g., as described above) is characterized or further characterized as metastatic cancer.

[0766] Anticancer effects may arise through one or more mechanisms, including, but not limited to, the control of cell proliferation, inhibition of cell cycle progression, inhibition of angiogenesis (neovascularization), inhibition of metastasis (spread of tumor from its origin), inhibition of cell migration (spread of cancer cells to other parts of the body), inhibition of invasion (spread of tumor cells to neighboring normal structures), promotion of apoptosis (programmed cell death), death by necrosis, or induction of death by autophagy. The compounds described herein may be used for the treatment of the cancers described herein, independently of the mechanisms described herein.

[0767] treatment In the context of treating a disorder (e.g., a disease), the term "treatment" as used herein generally refers to a treatment of a human or animal (e.g., a veterinary indication) that achieves a somewhat desired therapeutic effect, such as inhibiting the progression of the disorder (e.g., including reducing or stopping the rate of progression), alleviating the symptoms of the disorder, improving the disorder, or curing the disorder. Treatment as a preventive measure (i.e., prevention) is also included. For example, use on a subject (e.g., a patient) who has not yet developed a disorder but is at risk of developing one is included in the term "treatment."

[0768] For example, cancer treatment includes reducing the progression of cancer, alleviating cancer symptoms, reducing the incidence of cancer, and preventing cancer.

[0769] The term "therapeutic dose" as used herein refers to the amount of a compound, or a substance, composition, or dosage form containing a compound, that is effective in producing a certain degree of desired therapeutic effect that balances a reasonable benefit-to-risk ratio when administered according to the desired treatment regimen.

[0770] Combination therapy The term "treatment" as used herein includes combination treatments and therapies in which two or more treatment agents or therapies are combined, for example, sequentially or simultaneously. For example, the BAA compounds described herein may also be used in combination therapies, for example, in combination with other agents.

[0771] Therefore, what is also described here is, The BAA compounds listed here, in combination with one or more additional therapeutic agents (e.g., one, two, three, four, etc.).

[0772] For example, also described herein are BAA compounds for use in methods of treating human or animal bodies therapeutically, for example, for use in methods of treating the disorders (e.g., diseases) described herein, in which the BAA compound is administered in combination with one or more (e.g., one, two, three, four, etc.) further therapeutic agents.

[0773] Also described herein is the use of the BAA compounds described herein in methods of treating the human or animal body in the treatment of the disorders (e.g., diseases) described herein, in which the BAA compounds are administered in combination with one or more (e.g., one, two, three, four, etc.) further therapeutic agents.

[0774] Also described herein is the use of the BAA compounds described herein in a method of treating the human or animal body in a therapeutic manner, for example, in a method of treating the disorders (e.g., diseases) described herein, in which the BAA compounds are administered in combination with one or more (e.g., one, two, three, four, etc.) further therapeutic agents.

[0775] Also described herein are the uses of the BAA compounds in the manufacture of pharmaceuticals, for example, for use in a method of treatment, for example, for use in a method of treatment of the disorders (e.g., diseases) described herein, in combination with one or more (e.g., one, two, three, four, etc.) further therapeutic agents.

[0776] In one embodiment, the pharmaceutical product contains a BAA compound.

[0777] Also described herein is a method of treatment, for example, a method of treatment for the disorders (e.g., diseases) described herein, comprising administering a therapeutically effective amount of the BAA compound described herein to a subject requiring treatment, preferably in the form of a pharmaceutical composition, wherein the BAA compound is administered in combination with one or more (e.g., one, two, three, four, etc.) further therapeutic agents.

[0778] The choice of specific combinations is at the discretion of the physician selecting the dosage, using general knowledge and well-known drug regimens.

[0779] Drugs (e.g., the BAA compounds described herein plus one or more other drugs) may be administered simultaneously or sequentially, with individually varying administration schedules and via different routes. For example, when administered sequentially, multiple drugs may be administered at close intervals (e.g., over 5-10 minutes) or long intervals (e.g., 1 hour, 2 hours, 3 hours, 4 hours or longer, or longer if necessary), and the precise dosage regimen should be balanced with the properties of the therapeutic agents.

[0780] Multiple drugs (for example, the BAA compound described here + one or more other drugs) can be formulated together as a single dosage form, or the individual drugs can be formulated separately and may be available together in the form of a kit, along with instructions for their use, as desired.

[0781] In one embodiment, the other agent (e.g., further therapeutic agent) is an immunotherapy agent, such as an immune checkpoint inhibitor.

[0782] In one embodiment, other agents (e.g., further therapeutic agents, e.g., further anticancer agents) include immunotherapeutic agents, such as monoclonal antibodies (e.g., trastuzumab, bevacizumab, cetuximab, daratumumab, or naxitamab, necitumumab, obinutuzumab, ofatumumab, panitumumab, pertuzumab, ramucirumab, or rituximab), bispecific antibodies (e.g., blinatumomab), and immune checkpoint inhibitors. These include agents (e.g., ipilimumab, nivolumab, pembrolizumab, semiprimab, atezolizumab, durvalumab, avelumab, dostallimumab, or tremelimumab), immunomodulators (e.g., imiquimod, thalidomide, lenalidomide, or pomalidomide), cytokines (e.g., interleukins, IL-2 aldezleukin), interferons (e.g., IFNa), oncolytic viruses (e.g., tarimodine, rherparepbec), or T-cell therapy.

[0783] In one embodiment, the other drug is an antibody-drug conjugate (i.e., "ADCs," such as brentuximab vedotin, inotuzumab ozogamicin, milbetuximab sorabtansine-gynx, fam-trastuzumab deruxtecan-nxki, ado-trastuzumab emtansine, gemtuzumab ozogamicin, enfortumab vedotin-ejfv, polatuzumab vedotin-piiq, tisotumab vedotin-tftv, sacituzumab govitecan-hziy, loncustuximab tecilin-lpyl, or disitamab vedotin).

[0784] In one embodiment, other agents include DNA damaging agents, such as alkylating agents (e.g., cisplatin, oxaliplatin, carboplatin, cyclophosphamide, melphalan, chlorambucil, bendamustine, temozolomide, trabectedin, mitomycin C, or dacarbazine); antimetabolites (e.g., capecitabine, gemcitabine, 5-fluorouracil, fluoropyrimidine, trifluridine and tipiracil, cytarabine, or methotrexate); and DNA intervening agents (e.g., anthracyclines, e.g., doxorubicin, epil). These include bicin (or daunorubicin), antibiotics (e.g., bleomycin, dactinomycin, or mitramycin); topoisomerase 1 inhibitors (e.g., camptothecin, irinotecan, or topotecan), topoisomerase 2 inhibitors (e.g., etoposide), microtubule targeting agents (e.g., taxanes, e.g., paclitaxel; or vinca alkaloids, e.g., vincristine, vinblastine, vindesine, vinorelbine, or eribulin); or antibiotics (e.g., bleomycin or mitomycin-C).

[0785] In one embodiment, the other agent is a topoisomerase I inhibitor (e.g., irinotecan or topotecan), a topoisomerase II inhibitor (e.g., etoposide), or an antimetabolite (e.g., gemcitabine).

[0786] In one embodiment, the other agent is an alkylating agent (e.g., cisplatin).

[0787] In one embodiment, the other agent is a topoisomerase I inhibitor (e.g., irinotecan or topotecan).

[0788] In one embodiment, the other drug is a topoisomerase II inhibitor (e.g., etoposide).

[0789] In one embodiment, the other drug is an antimetabolite (e.g., gemcitabine).

[0790] In one embodiment, the other agent is a DNA damage repair inhibitor (e.g., PARP inhibitors, e.g., olaparib, rucaparib, niraparib, or talazoparib; or PARG inhibitors; or USP1 inhibitors).

[0791] In one embodiment, the other agent is a double-strand break repair inhibitor (e.g., a Polθ inhibitor or a RAD51 inhibitor).

[0792] In one embodiment, other drugs are signaling pathway inhibitors, such as kinase inhibitors (e.g., abemaciclib, acalabrutinib, afatinib, alectinib, avapritinib, axitinib, baricitinib, belmosdil, binimetinib, bosutinib, brigutinib, cabozantinib, capmatinib, ceritinib, cobimetinib, lyzotinib, dabrafenib, dacomitinib, dasatinib, encorafenib, entrectinib, erdafitinib, erlotinib, everolimus, fedratinib, hostamatinib, gefitinib, gilteritinib, ibrutinib, imatinib, infiglatinib, ra These include patinib, lalotrectinib, lenvatinib, lorlatinib, midostaurinib, mobocertinib, neratinib, netaludil, nilotinib, nintedanib, osimertinib, palbociclib, pazopanib, pemigatinib, pexidartinib, ponatinib, pralcetinib, regorafenib, ribociclib, lipretinib, ruxolitinib, serpercatinib, selumetinib, sirolimus, sorafenib, sunitinib, temsirolimus, tepotinib, tivozanib, tofacitinib, trametinib, trilaciclib, tucatinib, upadacitinib, vandetanib, vemurafenib, or zanubrutinib.

[0793] In one embodiment, the other drug is a cell cycle targeting inhibitor, such as a CDK4 / 6 inhibitor (e.g., palbociclib, abemaciclib, or ribociclib).

[0794] In one embodiment, other agents are agents that target DNA damage checkpoints, such as ATR inhibitors (e.g., celaracertib, galticertive, tubcertib, elimsertib, or camoncertib), ATM inhibitors (e.g., AZD0156), CHK1 inhibitors (e.g., prexasertib), CHK2 inhibitors, WEE1 inhibitors (e.g., adavocertib, or azenocertib), PLK1 inhibitors (e.g., onvancertib), or AUR-A inhibitors (e.g., JAB-2485).

[0795] In one embodiment, the other drug is an ATR inhibitor (e.g., celara certib, galticertive, tub certib, elimsertive, or camon certib), a CHK1 inhibitor (e.g., prexasertive), or a WEE1 inhibitor (e.g., adavo certib or azenocertive).

[0796] In one embodiment, the other drug is an ATR inhibitor (e.g., celara certib, gulticertive, tub certib, or camon certib) or a WEE1 inhibitor (e.g., azenocertive).

[0797] In one embodiment, the other drug is a CHK1 inhibitor (e.g., prexasertib).

[0798] In one embodiment, the other drug is an ATR inhibitor (e.g., celara certib, galticertive, tub certib, elimsertib, or camon certib).

[0799] In one embodiment, the other drug is a WEE1 inhibitor (e.g., adavocertib or azenocertib).

[0800] In one embodiment, the drug is a hormonal therapy agent, such as an anti-estrogen (e.g., tamoxifen, fulvestrant, toremifene, raloxifene, doroxifene, or idoxifene), an anti-androgen (e.g., abiraterone, bicalutamide, enzalutamide, flutamide, nilutamide, or cyproterone acetate), an LHRH antagonist or LHRH agonist (e.g., goserelin, leuprorelin, or buserelin), a progestogen (e.g., megestrol acetate), an aromatase inhibitor (e.g., anastrozole, letrozole, borazole, or exemestane), a 5α-reductase inhibitor (e.g., finasteride), or a somatostatin analog (e.g., lanreotide).

[0801] In one embodiment, the other agent is a proteasome inhibitor (e.g., bortezomib), a histone deacetylase inhibitor (e.g., vorinostat, romidepsin, panobinostat, or belinostat), or a DNA demethylating agent (e.g., azacitidine or decitabine).

[0802] In one embodiment, the other agent is radiotherapy, for example, radiotherapy involving treatment with radiotherapy drugs (e.g., lutetium Lu 177 doatete, lutetium Lu 177 bipivotide tetraxetan, samarium Sm 153 lexidronam, radium Ra 223 dichloride, or Y-90 ibritumomab tiuxetan).

[0803] Other uses The BAA compounds described herein can also be used as cell culture additives to inhibit PKMYT1 (for example, to inhibit, reduce, or block the activity or function of PKMYT1).

[0804] The BAA compounds described herein may also be used as part of an in vitro assay, for example, to determine whether a candidate host may benefit from treatment with the compound.

[0805] The BAA compounds described herein can also be used as reference samples in assays, for example, to identify other active compounds, other PKMYT1 inhibitors, etc.

[0806] kit Also described herein are (a) the BAA compounds described herein, preferably provided as a composition (e.g., a pharmaceutical composition), in a suitable container and / or in suitable packaging; and (b) a kit, including instructions for use, e.g., instructions on how to administer the compound, in a method of treating, for example, a disorder (e.g., a disease) described herein.

[0807] The instruction sheet may also include a list of indications for which BAA compounds are appropriate treatments.

[0808] Route of administration A pharmaceutical composition containing a BAA compound or a BAA compound may be administered to a subject systemically / peripherally or topically (i.e., to the desired site of action) via any conventional route of administration.

[0809] Routes of administration include, for example: oral (e.g., by ingestion); buccal; sublingual; transdermal (e.g., including patches, plasters, etc.); transmucosal (e.g., including patches, plasters, etc.); intranasal (e.g., nasal spray); ocular (e.g., eye drops); lung (e.g., through the throat or nose, e.g., using aerosols, e.g., inhalation or inhalation therapy); rectal (e.g., suppositories or enemas); vaginal (e.g., pessaries); non-enteral injection, including, for example, subcutaneous, intradermal, intramuscular, intravenous, intraarterial, intracardiac, intrathecal, intrathecal, intracapsular, subcapsular, intraorbital, intraperitoneal, intratracheal, subepidermal, intraarticular, subarachnoid, and intrasternal; for example, including subcutaneous or intramuscular depots or reservoir implantations.

[0810] subject The subject (e.g., patient) may be a chordate, vertebrate, mammal, placental mammal, marsupial (e.g., kangaroo, wombat), rodent (e.g., guinea pig, hamster, rat, mouse), murid (e.g., mouse), lagomorph (e.g., rabbit), bird (e.g., bird), canine (e.g., dog), feline (e.g., cat), equid (e.g., horse), pig (e.g., pig), sheep (e.g., sheep), bovine (e.g., cow), primate, ape (e.g., monkey or ape), monkey (e.g., marmoset, baboon), ape (e.g., gorilla, chimpanzee, orangutan, gibbon), or human.

[0811] Furthermore, the subject (for example, a patient) can be at any stage of development, such as a fetus.

[0812] In one preferred embodiment, the subject (e.g., a patient) is a human being.

[0813] formulation While BAA compounds can be administered alone, it is preferable that they be provided as pharmaceutical formulations (e.g., compositions, formulations, pharmaceuticals) comprising at least one of the BAA compounds described herein with one or more other pharmaceutically acceptable components well known to those skilled in the art, such as pharmaceutically acceptable carriers, diluents, additives, adjuvants, fillers, buffers, preservatives, antioxidants, lubricants, stabilizers, solubilizers, surfactants (e.g., wetting agents), masking agents, colorants, flavoring agents, and sweeteners. The formulations may further contain other activators, such as other therapeutic or prophylactic agents.

[0814] Therefore, also described herein are the pharmaceutical compositions as defined above, and methods for producing the pharmaceutical compositions, comprising mixing at least one of the BAA compounds described herein with one or more other pharmaceutically acceptable components well known to those skilled in the art, such as carriers, diluents, additives, etc. If formulated as individual units (e.g., tablets), each unit contains a planned amount (dose) of the compound.

[0815] The term "pharmaceutically acceptable" as used herein refers to a compound, component, substance, composition, dosage form, etc., that is suitable for use in contact with the tissue of the subject (e.g., human) without excessive toxicity, irritation, allergic response, or other problems or complications, and that is balanced by a reasonable benefit / risk ratio, within the bounds of sound medical judgment. Each carrier, diluent, additive, etc., must also be "acceptable" in terms of compatibility with the other components of the formulation.

[0816] Suitable carriers, diluents, additives, etc., can be found in the Standard Medical Textbook, for example, Remington: The Science and Practice of Pharmacy , 21st edition, Lippinott Williams and Wilkins, 2005; Remington: The Science and Practice of Pharmacy , 22nd edition, Pharmaceutical Press, 2012; and Handbook of Pharmaceutical Excipients This can be seen in the 7th edition, Pharmaceutical Press, 2012.

[0817] Pharmaceutical preparations can be prepared by any method well known in the field of pharmacy. Such methods involve the step of binding a compound to a carrier consisting of one or more auxiliary components. Generally, pharmaceutical preparations are prepared by uniformly and tightly binding a compound to a carrier (e.g., a liquid carrier, a micronized solid carrier, etc.), and then, if necessary, molding the product.

[0818] The formulation may be manufactured to provide rapid or delayed release; immediate, delayed, timed, or sustained release; or a combination thereof.

[0819] The formulations may be in the form of liquids, solutions (e.g., aqueous, non-aqueous), suspensions (e.g., aqueous, non-aqueous), emulsions (e.g., oil-in-water, water-in-oil), elixirs, syrups, licks, mouthwashes, droplets, tablets (e.g., including coated tablets), granules, powders, lozenges, aromatic tablets, capsules (e.g., including hard and soft gelatin capsules), cachets, pills, ampoules, boluses, suppositories, pessaries, tinctures, gels, pastes, ointments, creams, lotions, oils, foams, sprays, mists, or aerosols.

[0820] The formulation may preferably be provided as a patch, adhesive plaster, bandage, dressing, etc., impregnated with one or more compounds and optionally one or more other pharmaceutically acceptable components, such as penetrating, penetrating, and absorption enhancers. The formulation may also preferably be provided as a depot or reservoir.

[0821] The compound may be dissolved, suspended, or mixed with one or more other pharmaceutically acceptable components. The compound may be provided in liposomes or other microparticles designed to direct the compound to, for example, blood components or one or more organs.

[0822] Formulations suitable for oral administration (e.g., ingestion) may include liquids, solutions (e.g., aqueous, non-aqueous), suspensions (e.g., aqueous, non-aqueous), emulsions (e.g., oil-in-water, water-in-oil), elixirs, syrups, licks, tablets, granules, powders, capsules, cachets, pills, ampoules, and boluses.

[0823] Formulations suitable for buccal administration include mouthwashes, lozenges, aromatic tablets, as well as patches, adhesive plasters, depots, and reservoirs. Lozenges typically contain the compound in an aromatic base, usually sucrose and acacia or tragacanth. Aromatic tablets typically contain the compound in an inert matrix, e.g., gelatin and glycerin, or sucrose and acacia. Mouthwashes typically contain the compound in a suitable liquid carrier.

[0824] Formulations suitable for sublingual administration include tablets, lozenges, aromatic tablets, capsules, and pills.

[0825] Formulations suitable for oral or mucosal administration include liquids, solutions (e.g., aqueous, non-aqueous), suspensions (e.g., aqueous, non-aqueous), emulsions (e.g., oil-in-water, water-in-oil), mouthwashes, lozenges, aromatic tablets, as well as patches, adhesive plasters, depots, and reservoirs.

[0826] Formulations suitable for parenteral transmucosal administration include liquids, solutions (e.g., aqueous, non-aqueous), suspensions (e.g., aqueous, non-aqueous), emulsions (e.g., oil-in-water, water-in-oil), suppositories, pessaries, gels, pastes, ointments, creams, lotions, oils, as well as patches, adhesive plasters, depots, and reservoirs.

[0827] Formulations suitable for transdermal administration include gels, pastes, ointments, creams, lotions, and oils, as well as patches, adhesive plasters, bandages, dressings, depots, and reservoirs.

[0828] Tablets may be manufactured by conventional means, for example, compression or casting, with one or more auxiliary components as desired. Compressed tablets may be manufactured by compressing a compound in a free-flowing form, such as powder or granules, in a suitable machine, together with one or more binders as desired (e.g., povidone, gelatin, acacia, sorbitol, tragacanth, hydroxypropyl methylcellulose); fillers or diluents (e.g., lactose, microcrystalline cellulose, calcium hydrogen phosphate); lubricants (e.g., magnesium stearate, talc, silica); disintegrants (e.g., sodium starch glycolate, cross-linked povidone, cross-linked sodium carboxymethylcellulose); surface-active, dispersing, or wetting agents (e.g., sodium lauryl sulfate); preservatives (e.g., p-hydroxybenzoate methyl, p-hydroxybenzoate propyl, sorbic acid); flavoring agents, flavor enhancers, and sweeteners as desired. Cast tablets may be manufactured by casting a mixture of powdered compounds moistened with an inert liquid diluent in a suitable machine. The tablets may be coated or scored as desired, and may be formulated to provide a delayed or controlled release of the compound therein, for example, using hydroxypropyl methylcellulose in various ratios, in order to provide a desired release profile. The tablets may optionally be coated, for example, an enteric coating, to act on the release, so that they are released in the part of the intestine other than the stomach.

[0829] Ointments are typically prepared from compounds and paraffinic or water-miscible ointment bases.

[0830] The cream is typically prepared from a compound and an oil-in-water cream base. Optionally, the aqueous phase of the cream base may contain, for example, at least about 30% w / w of polyhydric alcohols, i.e., alcohols having two or more hydroxyl groups, such as propylene glycol, butane-1,3-diol, mannitol, sorbitol, glycerol, polyethylene glycol, and mixtures thereof. Topical formulations preferably contain compounds that enhance the absorption or penetration of the compound through the skin or other affected area. Examples of such skin penetration enhancers include dimethyl sulfoxide and related analogues.

[0831] Emulsions are typically prepared from an oil phase that may contain a compound and, optionally, simply an emulsifier (also known as an emulsifier), or at least one emulsifier and a fat or oil or a mixture of both fat and oil. Preferably, a hydrophilic emulsifier is included together with a lipophilic emulsifier that acts as a stabilizer. It is also preferable to include both oil and fat. In summary, emulsifiers with or without stabilizers form a so-called emulsifying wax, and the wax, together with oil and / or fat, forms a so-called emulsifying ointment base, which forms the oily dispersion phase of a cream formulation.

[0832] Suitable emulsions and emulsion stabilizers include Tween 60, Span 80, cetostearyl alcohol, myristyl alcohol, glyceryl monostearate, and sodium lauryl sulfate. The selection of a suitable oil or fat for the formulation is based on achieving the desired cosmetic properties, as the solubility of compounds in most oils that may be used in pharmaceutical emulsion formulations is extremely low. Therefore, the cream should preferably be a non-greasy, colorless, and washable product with appropriate viscosity to avoid leakage from tubes or other containers. Mixtures of linear or branched, one- or two-basic alkyl esters, such as di-isoadipates, isocetyl stearate, propylene glycol diesters of coconut fatty acids, isopropyl myristate, decyl oleate, isopropyl palmitate, butyl stearate, 2-ethylhexyl palmitate, or branched esters known as Crodamol CAP can be used, with the last three being preferred esters. These can be used alone or in combination, depending on the required properties. Alternatively, high-melting-point lipids such as white soft paraffin and / or liquid paraffin or other mineral oils can be used.

[0833] Formulations suitable for intranasal administration, in which the carrier is liquid, include aqueous or oily solutions of the compound, for example, aerosol administration by nasal spray, nasal drops, or nebulizer.

[0834] Formulations suitable for intranasal administration, in which the carrier is solid, include, for example, those provided as a coarse powder having a particle size in the range of about 20 to about 500 microns, which are administered by inhalation through the nose, i.e., by rapid inhalation through the nasal cavity from a container of powder held near the nose.

[0835] Formulations suitable for pulmonary administration (e.g., inhalation or inhalation therapy) include those supplied as aerosol sprays from a pressurized pack, using a suitable propellant such as dichlorodifluoromethane, trichlorofluoromethane, dichlorotetrafluoroethane, carbon dioxide, or other suitable gases.

[0836] Formulations suitable for ocular administration include eye drops in which the compound is dissolved or suspended in a suitable carrier, particularly an aqueous solvent for the compound.

[0837] Formulations suitable for rectal administration may be provided as suppositories with a suitable base, such as a neutral or hydrogenated oil, wax, fat, semi-liquid or liquid polyol, such as cocoa butter or salicylic acid; or as a solution or suspension for enema administration.

[0838] Formulations suitable for vaginal administration may be provided as pessaries, tampons, creams, gels, pastes, foams, or spray formulations, comprising the compound and a carrier known to be suitable in the art.

[0839] Formulations suitable for non-enteral administration (e.g., injection) include aqueous or non-aqueous, isotonic, pyrogen-free, sterile liquids (e.g., solutions, suspensions) in which the compound is provided by dissolution, suspension, or other means (e.g., in liposomes or other microparticles). Such liquids may further contain other pharmaceutically acceptable components such as antioxidants, buffers, preservatives, stabilizers, bacteriostatic agents, suspending agents, concentrating agents, and solutes that make the formulation isotonic with the blood (or other relevant body fluids) of the recipient to whom the formulation is intended. Examples of additives include, for example, water, alcohol, polyols, glycerol, and vegetable oils. Examples of suitable isotonic carriers for use in such formulations include sodium chloride injection, Ringer's solution, or emulsified Ringer's injection. Typically, the concentration of the compound in the liquid may be about 1 ng / mL to about 10 μg / mL, for example, about 10 ng / mL to about 1 μg / mL. The formulations are supplied in unit-dose or multi-dose sealed containers, such as ampoules and vials, and can be stored under freeze-drying conditions requiring only the addition of a sterile liquid carrier, such as water for injection, immediately before use. Immediate injections can be prepared from sterile powders, granules, and tablets.

[0840] Dosage It is recognized by those skilled in the art that the appropriate dosage of the BAA compound and the composition containing the BAA compound can vary for each subject (e.g., for each patient). The determination of the optimal dosage generally involves balancing the therapeutic benefit against some level of risk or adverse side effects. The selected dosage level depends on various factors such as, for example: the activity of a particular BAA compound; the route of administration; the timing of administration; the excretion rate of the BAA compound; the duration of treatment; other drugs, compounds, and / or substances used in combination; the severity of the disorder; and the species, sex, age, weight, condition, general health, and prior medical history of the subject (e.g., patient). The amount and route of administration of the BAA compound are ultimately at the discretion of the physician, veterinarian, or clinician, but generally the dosage is selected to achieve a local concentration at the site of action that achieves the desired effect without substantially causing harmful or toxic side effects.

[0841] Administration can be carried out once, continuously, or intermittently (e.g., divided doses at appropriate intervals) during the course of treatment. The most effective means of administration and the method for determining the dosage are well known to those skilled in the art and vary depending on the formulation used for treatment, the purpose of the treatment, the target cells being treated, and the subject being treated. Single or multiple administrations can be carried out at dosage levels and patterns selected by the physician, veterinarian, or clinician treating the subject.

[0842] Generally, an appropriate dosage of the BAA compound ranges from about 0.01 mg to about 5000 mg per day (more typically from about 0.1 mg to about 1000 mg, for example, from about 0.1 mg to about 300 mg).

[0843] When the compound is a salt, solvate, ester, amide, prodrug, etc., the amount administered is calculated based on the parent compound, and thus the weight actually used increases proportionally.

Example

[0844] chemical synthesis Abbreviation {1H} proton decoupling aq. aqueous BINAP 2,2'-bis(diphenylphosphin)-1,1'-binaphthyl DCM Dichloromethane (Methylene Chloride) DIAD Diisopropylazodicarboxylate DIPEA N,N-diisopropylethylamine DMSO (Dimethyl Sulfoxide) ES electrospray ionization Et2O ether (diethyl ether) HCl ethyl acetate EtOH Ethanol (ethyl alcohol) HATU 2-(7-aza-1H-benzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate MeCN acetonitrile MeOH (Methanol / Methyl Alcohol) Pd / C Palladium / Carbon Pd2dba3 Tris(dibenzylideneacetone)dipalladium(0) RT room temperature Sat aq. STAB Sodium Triacetoxyborohydride T3P 1-Propanephosphone Anhydrous TFA (Trifluoroacetic Acid) THF (Tetrahydrofuran) UPLC Ultra-High-Speed ​​Liquid Chromatography Xantphos 4,5-bis(diphenylphospheno)-9,9-dimethylxanthentrifluoro

[0845] method General experiment Flash chromatography was performed using pre-packed silica gel cartridges (RediSep Rf, Isco). Thin-layer chromatography was performed on 5 × 10 cm plates coated with Merck Type 60 F254 silica gel to a thickness of 0.25 mm. All reagents obtained from commercial sources were used without further purification. Anhydrous solvents were obtained from Sigma-Aldrich Chemical Company Ltd. or Fisher Chemicals Ltd. and used without further drying. HPLC-grade solvents were obtained from Fisher Chemicals Ltd.

[0846] All compounds were analyzed by LCMS and, unless otherwise specified, by LCMS and 1 The purity was determined by testing both 1H NMR spectra, and was >90%. When Cl or Br was present, a predicted isotope distribution pattern was obtained.

[0847] NMR proton( 1 H) and carbon ( 13 C) and ( 19 F) NMR spectra were recorded using a 300 MHz Bruker or 400 MHz Jeol spectrometer. Solutions were typically prepared with deuterated chloroform (chloroform-d), deuterated methanol (methanol-d4), or deuterated dimethyl sulfoxide (DMSO-d6), and the chemical shifts were referenced to tetramethylsilane (TMS) or the deuterated solvent as an internal standard. 1 H NMR data, chemical shift (δ), integral (for example, 1 Report the H), multiplicity (s, singlet; d, doublet; t, triplet; q, quadruplet; m, multiplet; br, broad; dd, doublet-doublet) and coupling constant (J)(Hz). Deuterated solvents were purchased from Sigma-Aldrich Chemical Company, Goss, or Fluorochem.

[0848] Analytical LCMS BEH C, equipped with a diode array detector, connects LCMS analysis to an SQD mass spectrometer with arbitrary ELS detection (Acquity UPLC ELS Detector). 18 BEH C with a Waters Acquity UPLC using a 1.7 μM column (2.1 × 50 mm) or a diode array detector coupled to a QDa mass spectrometer. 18 The analysis was performed using a Waters Acquity I-Class UPLC with a 1.7 μM column (2.1 × 50 mm). The analysis was carried out using buffered acidic or basic solvents with the gradients detailed below: Low pH: Solvent A - Water + 10 mM ammonium bicarbonate + 0.1% formic acid Solvent B - MeCN + 5% water + 0.1% formic acid High pH: Solvent A - Water + 10 mM ammonium bicarbonate + 0.1% ammonia solution Solvent B - MeCN + 5% water + 0.1% ammonia solution gradient: [Table 36]

[0849] For some compounds, the following gradient was used: Acidity 2 minutes 0.1% v / v formic acid in 10 mM ammonium formate solution [eluent A]; 0.1% v / v formic acid in MeCN solution [eluent B]; flow rate 0.8 mL / min; column oven 50°C; sample manager 20°C; injection volume 2 μL and equilibration time 1.5 minutes between samples, on a Waters Acquity UPLC BEH C18 column (2.1 × 50 mm, 1.7 μm).

[0850] [Table 37]

[0851] Acidity 4 minutes 0.1% v / v formic acid in 10 mM ammonium formate solution [eluent A]; 0.1% v / v formic acid in MeCN solution [eluent B]; flow rate 0.8 mL / min; column oven 50°C; sample manager 20°C; injection volume 2 μL and equilibration time 1.5 minutes between samples on a Waters Acquity UPLC BEH C18 column (2.1 × 50 mm, 1.7 μm). [Table 38]

[0852] Acidic 6 minutes ("Acidic_Preparative_Analysis") 0.1% v / v formic acid in 10 mM ammonium formate solution [eluent A]; 0.1% v / v formic acid in MeCN solution [eluent B]; flow rate 0.8 mL / min; column oven 50°C; sample manager 20°C; injection volume 2 μL and equilibration time 1.5 minutes between samples on a Waters Acquity UPLC BEH C18 column (2.1 × 50 mm, 1.7 μm). [Table 39]

[0853] Basic 2 minutes 0.1% aqueous solution of ammonia [eluent A]; 0.1% ammonia in MeCN solution [eluent B]; flow rate 0.8 mL / min; column oven 50°C; sample manager 20°C; injection volume 2 μL and equilibration time 1.5 minutes between samples on a Waters Acquity UPLC BEH C18 column (2.1 × 50 mm, 1.7 μm). [Table 40]

[0854] Basic 4 minutes 0.1% aqueous solution of ammonia [eluent A]; 0.1% ammonia in MeCN solution [eluent B]; flow rate 0.8 mL / min; column oven 50°C; sample manager 20°C; injection volume 2 μL and equilibration time 1.5 minutes between samples on a Waters Acquity UPLC BEH C18 column (2.1 × 50 mm, 1.7 μm). [Table 41]

[0855] Basicity 6 minutes ("Basicity_Preparative_Analysis") 0.1% aqueous solution of ammonia [eluent A]; 0.1% ammonia in MeCN solution [eluent B]; flow rate 0.8 mL / min; column oven 50°C; sample manager 20°C; injection volume 2 μL and equilibration time 1.5 minutes between samples on a Waters Acquity UPLC BEH C18 column (2.1 × 50 mm, 1.7 μm). [Table 42]

[0856] Preparative HPLC-MS Some compounds were tested using Phenomonex Gemini NX 5μm C 18 , 100mm x 21.2mm inner diameter column (for low pH runs) or Waters XBridge 5μm C 18 The solution was purified by preparative HPLC on a Waters FractionLynx automated MS system using a 100 mm × 19 mm inner diameter column (for high pH runs), and then flushed at a flow rate of 20 mL / min under UV diode array detection (210-400 nm) with mass indicator collection using both positive and negative mass ion detection.

[0857] Alternatively, preparative HPLC purification was performed using a Teledyne ISCO ACCQPrep® HP150 system or a Waters Mass-directed PrepLC system with a C1 XBridge BEH C18 (dimensions: 19 mm × 150 mm, 5 μm) or C2 XBridge BEH C18 (dimensions: 19 mm × 150 mm, 5 μm) column at a flow rate of 20 mL / min. The total mass was detected by electrospray ionization (ESI).

[0858] Purification was carried out using buffered acidic or basic solvent systems as appropriate. The retention time of the compound in the system was routinely evaluated using 30–50 μL test injections and standard gradients, and then, based on the observed retention time, purification was performed using appropriately selected intensive gradients as detailed below.

[0859] Low pH: Solvent A - Water + 10 mM ammonium formate + 0.1% formic acid Solvent B - MeCN + 5% water + 0.1% formic acid High pH: Solvent A - Water + 10 mM ammonium formate + 0.1% ammonia solution Solvent B - MeCN + 5% water + 0.1% ammonia solution or MeCN + 0.1% ammonia solution [Table 43]

[0860] Concentrated gradient: [Table 44]

[0861] Synthesis method Several methods for the chemical synthesis of the compounds of the present invention are described herein. These and / or other well-known methods may be modified and / or adapted in known ways to facilitate the synthesis of further compounds within the scope of the present invention.

[0862] [ka] Amide coupling and deprotection to obtain BAA-001 2-amino-N-(3-hydroxy-2,6-dimethylphenyl)thiazole-5-carboxamide (BAA-001) [ka] Step 1: tert-butyl N-[5-[(3-hydroxy-2,6-dimethylphenyl)carbamoyl]thiazole-2-yl]carbamate To a 10 mL solution of 2-N-boc-amino-thiazole-5-carboxylic acid (350 mg, 1.43 mmol, 1.0 equivalent) and 3-amino-2,4-dimethylphenol (236 mg, 1.72 mmol, 1.2 equivalents) (prepared as described in International Patent Publication WO2015 / 079251A1) in THF (0.50 mL, 2.87 mmol, 2.0 equivalents) while stirring, DIPEA (0.50 mL, 2.87 mmol, 2.0 equivalents) and T3P (50% siRNA solution, 1.3 mL, 2.15 mmol, 1.5 equivalents) were added. The mixture was heated to 65°C and stirred overnight. The mixture was cooled to RT, water and siRNA were added, and the layers were separated. The aqueous layer was further extracted with siRNA, the organic layer was collected, and the solvent was removed under reduced pressure by passing it through a phase separator. The crude material was subjected to chromatography (SiO2) using 0-100% siRNA:PE to obtain tert-butyl N-[5-[(3-hydroxy-2,6-dimethylphenyl)carbamoyl]thiazole-2-yl]carbamate (64 mg, 0.176 mmol, 12%) as a pale orange solid. MS (ES+) m / z 364.2 (M+H). 1 H NMR (300 MHz, DMSO-d6) δ 11.77 (br s, 1H), 9.64 (s, 1H), 9.18 (s, 1H), 8.17 (s, 1H), 6.89 (d, J = 8.2 Hz, 1H), 6.69 (d, J = 8.2 Hz, 1H), 2.06 (s, 3H), 1.98 (s, 3H), 1.51 (s, 9H).

[0863] Step 2: 2-amino-N-(3-hydroxy-2,6-dimethylphenyl)thiazole-5-carboxamide (BAA-001) To a suspension of tert-butyl N-[5-[(3-hydroxy-2,6-dimethylphenyl)carbamoyl]thiazole-2-yl]carbamate (66 mg, 0.182 mmol, 1.0 equivalent) in MeOH (2 mL) while stirring, HCl (4 M in 1,4-dioxane, 0.68 mL, 2.72 mmol, 15 equivalents) was added. The mixture was warmed to 40°C and stirred for 2 days. The solvent was removed under reduced pressure, and chromatography (SiO2) was performed using 0-100% siRNA:PE followed by 0-20% MeOH:DCM. The obtained product was dissolved in a small amount of MeOH and packed into a pre-equilibrated SCX-1 g column (washed with MeOH and eluted with 7N NH3:MeOH) to obtain the title compound (9.1 mg, 0.0346 mmol, 19%) as a pale yellow solid. MS (ES+) m / z 264.1 (M+H). 1 H NMR (300 MHz, DMSO-d6) δ 9.32 (s, 1H), 9.13 (s, 1H), 7.83 (s, 1H), 7.53 (br s, 2H), 6.87 (d, J = 8.2 Hz, 1H), 6.67 (d, J = 8.2 Hz, 1H), 2.05 (s, 3H), 1.97 (s, 3H).

[0864] Nitro derivative synthesis Nitration 3,4-dimethyl-5-nitro-1H-pyrazole [ka] 3,4-dimethyl-1H-pyrazole (0.18 mL, 2.08 mmol, 1.0 equivalent) was added to sulfuric acid (95% aqueous solution, 5.0 mL, 88.6 mmol, 42.6 equivalents) at 0°C, and then fuming nitric acid (0.13 mL, 3.12 mmol, 1.5 equivalents) was added dropwise. The reaction mixture was stirred at RT for 18 hours. The mixture was poured onto ice, aqueous ammonia solution was added to pH 4, and extracted with RINKAN (×3). The combined organic layers were dried over MgSO4, filtered, and concentrated under reduced pressure. The crude material was subjected to chromatography (SiO2) eluting with 0-100% RINKAN:PE to obtain the title compound (60 mg, 0.425 mmol, 20%) as a white solid. MS (ES-) m / z 140.0 (MH). 1 H NMR (300 MHz, DMSO-d6) δ 13.62 - 13.42 (brs, 1H), 2.23 (s, 3H), 2.18 (s, 3H).

[0865] Alkylation of nitropyrazole General method A1. Alkylation of 3-nitro-1H-pyrazole [ka] Alkyl halide (1 equivalent) was added under nitrogen at room temperature with stirring to an anhydrous THF or MeCN suspension of unsubstituted or substituted nitropyrazole (1 equivalent) and potassium carbonate (1.5 equivalents) or cesium carbonate (1-1.5 equivalents), or to a DMF suspension of NaH (1.2 equivalents). The reaction mixture was then stirred in rt or heated to 65-75°C with stirring for 4 hours, then cooled to room temperature and partitioned into ethyl acetate and water. The organic phase was washed with brine, dried over anhydrous magnesium sulfate, filtered, and concentrated to obtain the product.

[0866] 1-Cyclopentylpyrazole-3-amine [ka] To a solution of 3-nitro-1H-pyrazole (1.0 g, 8.84 mmol, 1.0 equivalent) in DMF (25 mL), NaH (60% in mineral oil, 425 mg, 10.6 mmol, 1.2 equivalents) was added at RT, and the mixture was stirred for 10 minutes. Then, bromocyclopentane (0.95 mL, 8.84 mmol, 1.0 equivalent) was added. The mixture was stirred at RT for 12 hours. The mixture was partitioned into toluene and water. The aqueous phase was extracted with toluene (3 × 50 mL). The combined organic phase was washed with water (2 × 50 mL), dried, and concentrated under reduced pressure in (MgSO4). The crude material was subjected to chromatography (SiO2) eluting with 0-100% toluene:PE to obtain the title compound (850 mg, 4.69 mmol, 53%) as a white solid. MS (ES+) m / z 182.2 (M+H).

[0867] Ethyl 2-methyl-5-nitropyrazole-3-carboxylate [ka] Prepared similarly from 5-nitro-1H-pyrazole-3-carboxylate ethyl ester (1.0 g, 5.40 mmol, 1.0 equivalent), NaH (60% in mineral oil, 238 mg, 5.94 mmol), and iodomethane (12 mL, 191 mmol, 3.0 equivalents), and eluted by reverse-phase chromatography (C) with 5-95% MeCN:H2O. 18 After the above steps, the title compound (540 mg, 2.71 mmol, 50%) was obtained as a white solid and used in the next step without further purification. 1 ¹H NMR (300 MHz, chloroform-d): δ 7.37 (s, 1H), 4.39 (q, J = 7.1 Hz, 2H), 4.26 (s, 3H), 1.39 (t, J = 7.1 Hz, 3H).

[0868] 3-Nitro-1-(2,2,2-trifluoroethyl)pyrazole [ka] A mixture of 3-nitro-1H-pyrazole (0.70 g, 6.19 mmol, 1.0 equivalent) and Cs2CO3 (4.0 g, 12.4 mmol, 2.0 equivalent) in DMF (25 mL) was stirred for 5 minutes, then 2,2,2-trifluoroethyltrifluoromethanesulfonic acid (1.72 mg, 7.43 mmol, 1.2 equivalents) was added, and the mixture was stirred at RT for 18 hours. The mixture was poured into water (100 mL) and extracted with RINKAN (3 × 25 mL). The combined organic phase was washed with water, dried, and concentrated under reduced pressure to obtain the title compound (850 mg, 4.36 mmol, 70%) as a white solid. 1 H NMR (300 MHz, DMSO-d6) δ 8.16 (d, J = 2.6 Hz, 1H), 7.16 (d, J = 2.6 Hz, 1H), 5.38 (q, J = 9.0 Hz, 2H). 19 F NMR (282 MHz, DMSO-d6) δ -70.11 (t, J = 9.0 Hz).

[0869] 3-Nitro-1-(oxetan-3-yl)pyrazole [ka] The title compound (534 mg, 3.16 mmol, 55%) was obtained by similar preparation from 3-iodooxetane (1.06 g, 5.75 mmol), 3-nitro-1H-pyrazole (0.65 g, 5.75 mmol), and Cs2CO3 (2.81 g, 8.62 mmol) at 100°C for 16 hours. After normal-phase chromatography (SiO2) elution with 0-100% Â:PE, the title compound was obtained. MS (ES-) m / z 168.0 (MH). 1 ¹H NMR (300 MHz, chloroform-d): δ 7.73 (d, J = 2.6 Hz, 1H), 6.97 (d, J = 2.5 Hz, 1H), 5.62 - 5.46 (m, 1H), 5.15 - 4.95 (m, 4H).

[0870] tert-butyl N-[2-(3-nitropyrazole-1-yl)ethyl]carbamate [ka] The title compound (1.3 g, 5.07 mmol, 57%) was obtained as a beige solid by similar preparation from tert-butyl N-(2-bromoethyl)carbamate (2.18 g, 9.73 mmol), 3-nitro-1H-pyrazole (1.00 g, 8.84 mmol), and Cs2CO3 (3.46 g, 10.6 mmol) at 60°C for 12 hours. After normal-phase chromatography (SiO2) eluting with 0-100% siRNA:PE, the title compound was obtained as a beige solid. MS (ES-) m / z 255.1 (MH).

[0871] 1-(difluoromethyl)-3-nitropyrazole [ka] The following compound was prepared in the same manner from sodium chlorodifluoroacetate (5.39 g, 35.38 mmol, 2.0 equivalents), 3-nitro-1H-pyrazole (2.00 g, 17.7 mmol), and cesium carbonate (5.76 g, 17.7 mmol) at 120°C for 2 hours. After normal-phase chromatography (SiO2) eluting with 0-10% siRNA:PE, the title compound (2.0 g, 12.3 mmol, 69%) was obtained as a white solid. 1 ¹H NMR (300 MHz, chloroform-d): δ 7.98 (d, J = 2.8 Hz, 1H), 7.29 (s, 1H), 7.09 (d, J = 2.5 Hz, 1H). 19 F NMR (282 MHz, chloroform-d) δ -95.11 (d, J = 59.7 Hz).

[0872] 3-(3-nitropyrazole-1-yl)propan-1-ol [ka] To a solution of 3-nitro-1H-pyrazole (2.30 g, 20.3 mmol, 1.0 equivalent) in THF (65 mL), 3-chloro-1-propanol (1.8 mL, 21.4 mmol, 1.05 equivalent) and K2CO3 (5.62 g, 40.7 mmol, 2.0 equivalent) were added. The mixture was heated at 60°C for 72 hours, followed by 75°C for 18 hours. The mixture was partitioned into pharmaceutically acceptable (ELISA) and water. The aqueous phase was extracted with ELISA (3 × 50 mL). The combined organic phase was washed with water (2 × 50 mL), dried, and concentrated under reduced pressure in MgSO4. The residue was subjected to chromatography (SiO2) eluting with 0-100% ELISA:PE to obtain the title compound (2.9 g, 17.2 mmol, 84%) as a colorless oil. MS (ES+) m / z 172.2 (M+H). 1 ¹H NMR (300 MHz, chloroform-d): δ 7.53 (d, J = 2.4 Hz, 1H), 6.91 (d, J = 2.5 Hz, 1H), 4.40 (t, J = 6.8 Hz, 2H), 3.74 - 3.60 (m, 2H), 2.28 - 2.06 (m, 2H).

[0873] Ethyl 4-(3-nitropyrazole-1-yl)butanoate [ka] Similarly, the compound was prepared from ethyl 4-bromobutyrate (2.55 mL, 17.69 mmol), 3-nitro-1H-pyrazole (2.00 g, 17.7 mmol), and K2CO3 (4.89 g, 35.4 mmol). After normal-phase chromatography (SiO2) eluting with 0-100% siRNA:PE, the title compound (3.7 g, 16.3 mmol, 92%) was obtained as a colorless oil. 1 ¹H NMR (300 MHz, chloroform-d): δ 7.49 (d, J = 2.5 Hz, 1H), 6.92 - 6.73 (m, 1H), 4.21 (t, J = 6.8 Hz, 2H), 3.99 (q, J = 7.1 Hz, 2H), 2.33 - 2.03 (m, 4H), 1.12 (t, J = 7.1 Hz, 3H).

[0874] N,N-dimethyl-2-(3-nitropyrazole-1-yl)acetamide [ka] The title compound (400 mg, 2.02 mmol, 65%) was obtained as a white solid by similar preparation from 2-bromo-N,N-dimethylacetamide (0.33 mL, 3.10 mmol, 1 equivalent), 3-nitro-1H-pyrazole (350 mg, 3.10 mmol), and K2CO3 (868 mg, 6.19 mmol) at 70°C for 2 hours. After normal-phase chromatography (SiO2) elution with 0-20% MeOH:DCM, the title compound was obtained as a white solid. MS (ES-) m / z 197.1 (MH). 1 ¹H NMR (300 MHz, chloroform-d): δ 7.64 (d, J = 2.6 Hz, 1H), 6.97 (d, J = 2.5 Hz, 1H), 5.10 (s, 2H), 3.12 (s, 3H), 3.02 (s, 3H).

[0875] Ethyl 2-(5-methyl-3-nitropyrazole-1-yl)acetate [ka] Similarly, 5-methyl-3-nitro-1H-pyrazole (1.0 g, 7.87 mmol) and K2CO3 (2.2 g, 15.7 mmol) were prepared using ethyl bromo (0.87 mL, 7.87 mmol, 1.0 equivalent), added at 0°C, and subsequently heated at 70°C for 2 hours to obtain the title compound (1.62 g, 7.60 mmol, 97%) as a white solid. MS (ES-) m / z 211.9 (MH). 1 H NMR (300 MHz, DMSO-d6) δ 6.92 (d, J = 0.8 Hz, 1H), 5.26 (s, 2H), 4.20 (q, J = 7.1 Hz, 2H), 2.29 (d, J = 0.7 Hz, 3H), 1.23 (t, J = 7.1 Hz, 3H).

[0876] 1,4-dimethyl-3-nitropyrazole [ka] Similarly, 4-methyl-3-nitro-1H-pyrazole (300 mg, 2.36 mmol, 1.0 equivalent) and K2CO3 (662 mg, 4.72 mmol) were prepared using iodomethane (0.18 mL, 2.83 mmol, 1.2 equivalents). The mixture was added at 0°C, followed by heating at 70°C for 2 hours. After normal-phase chromatography (SiO2) eluting with 0-100% siRNA:PE, the title compound (270 mg, 1.91 mmol, 81%) was obtained as a white solid. MS (ES+) m / z 142.1 (M+H). 1 H NMR (300 MHz, DMSO-d6) δ 7.82 (d, J = 1.0 Hz, 1H), 3.91 (s, 3H), 2.24 (d, J = 0.8 Hz, 3H).

[0877] Ethyl 2-(4-methyl-3-nitropyrazole-1-yl)acetate [ka] Similarly, 4-methyl-3-nitro-1H-pyrazole (500 mg, 3.93 mmol) and K2CO3 (1.1 g, 7.87 mmol) were prepared using ethyl bromo (0.44 mL, 3.93 mmol, 1.0 equivalent), added at 0°C, and subsequently heated at 70°C for 2 hours to obtain the title compound (820 mg, 3.85 mmol, 98%) as a bright yellow oily substance. MS (ES-) m / z 212.1 (MH). 1 H NMR (300 MHz, DMSO-d6) δ 7.88 (d, J = 0.9 Hz, 1H), 5.22 (s, 2H), 4.18 (q, J = 7.1 Hz, 2H), 2.27 (d, J = 0.8 Hz, 3H), 1.23 (t, J = 7.1 Hz, 3H).

[0878] 1-methyl-3-nitro-indazole [ka] Similarly, 3-nitro-1H-indazole (255 mg, 1.56 mmol) and K2CO3 (438 mg, 3.13 mmol) were prepared using iodomethane (0.12 mL, 1.88 mmol, 1.2 equivalents), added at 0°C, and subsequently heated at 70°C for 2 hours. After normal-phase chromatography (SiO2) eluting with 0-100% siRNA:PE, the title compound (220 mg, 1.24 mmol, 79%) was obtained as a bright yellow solid. MS (ES+) m / z 178.0 (M+H). 1 ¹H NMR (300 MHz, chloroform-d): δ 8.31 - 8.20 (m, 1H), 7.63 - 7.43 (m, 3H), 4.22 (s, 3H).

[0879] 1,4,5-trimethyl-3-nitropyrazole [ka] Similarly, 3,4-dimethyl-5-nitro-1H-pyrazole (80 mg, 0.567 mmol, 1.0 equivalent) and K2CO3 (159 mg, 1.13 mmol) were prepared using iodomethane (0.042 mL, 0.680 mmol, 1.2 equivalents), added at 0°C, and subsequently heated at 70°C for 2 hours to obtain the title compound (60 mg, 0.387 mmol, 68%) as a white solid after normal-phase chromatography (SiO2) elution with 0-100% siRNA:PE. MS (ES+) m / z 155.9 (M+H). 1 ¹H NMR (300 MHz, chloroform-d): δ 3.83 (s, 3H), 2.23 (s, 3H), 2.22 (s, 3H).

[0880] The following examples were prepared using Method A1 in a similar manner with appropriate nitro-pyrazole and alkyl halide: [Table 45] [Table 46]

[0881] 2-(3-nitro-4-vinyl-1H-pyrazole-1-yl)acetonitrile [ka] The solution of potassium vinyltrifluoroborate (175 mg, 1.31 mmol), palladium(II) chloride (12 mg, 0.0677 mmol), triphenylphosphine (52 mg, 0.198 mmol), cesium carbonate (640 mg, 1.96 mmol), and 2-(4-bromo-3-nitropyrazole-1-yl)acetonitrile (150 mg, 0.649 mmol) in a mixture of 1,4-dioxane (3 mL) and water (0.3 mL) was degassed with N2 and stirred in a sealed tube at 85°C for 6 hours. The reaction mixture was cooled to rt and quenched with water (15 mL). The resulting mixture was extracted with DCM (3 × 15 mL), the combined organic layers were dried over Na2SO4, filtered, and concentrated. The crude material was purified by silica column chromatography (40g cartridge) using a gradient of isohexane solution of ethyl acetate (5%-80% v / v) to obtain the title compound (67mg, 0.342 mmol, 52.63% yield) as a yellow solid. 1 H NMR (400 MHz, CDCl3) δ 7.84 (s, 1H), 7.04 (ddd, J = 17.8, 11.1, 0.7 Hz, 1H), 5.69 (dd, J = 17.8, 0.9 Hz, 1H), 5.47 (dd, J = 11.0, 0.8 Hz, 1H), 5.16 (s, 2H).

[0882] 1-(2,2-difluoroethyl)-3-nitro-4-vinyl-1H-pyrazole [ka] The solutions of potassium vinyltrifluoroborate (50 mg, 0.373 mmol), palladium(II) chloride (3.5 mg, 0.0195 mmol), triphenylphosphine (15 mg, 0.0586 mmol), cesium carbonate (200 mg, 0.614 mmol), and 4-bromo-1-(2,2-difluoroethyl)-3-nitropyrazole (50 mg, 0.195 mmol) in a mixture of 1,4-dioxane (1 mL) and water (0.1 mL) were degassed with N2 and stirred in a sealed tube at 85°C for 6 hours. The reaction mixture was quenched with water (5 mL), extracted with DCM (3 × 5 mL), and the combined organic layers were dried over Na2SO4, filtered, and concentrated. The crude material was purified by silica column chromatography (12 g cartridge) using a gradient of isohexane solution of ethyl acetate (5%~80%; v / v) to obtain the desired product 1-(2,2-difluoroethyl)-3-nitro-4-vinylpyrazole (33 mg, 0.149 mmol, 76.29% yield) as a yellow solid. 1 H NMR (400 MHz, CDCl3) δ 7.71 (s, 1H), 7.03 (ddd, J = 17.8, 11.1, 0.7 Hz, 1H), 6.16 (tt, J = 54.9, 4.1 Hz, 1H), 5.65 (dd, J = 17.8, 1.0 Hz, 1H), 5.42 (dd, J = 11.1, 1.0 Hz, 1H), 4.53 (td, J = 13.4, 4.1 Hz, 2H). 19 F NMR (376 MHz, CDCl3) δ -122.32 (dt, J = 54.8, 13.3 Hz).

[0883] 1-(2-fluoroethyl)-3-nitro-4-vinyl-1H-pyrazole [ka] The solution of potassium vinyltrifluoroborate (170 mg, 1.27 mmol), palladium(II) chloride (11 mg, 0.0620 mmol), triphenylphosphine (50 mg, 0.191 mmol), cesium carbonate (620 mg, 1.90 mmol), and 4-bromo-1-(2-fluoroethyl)-3-nitropyrazole (150 mg, 0.630 mmol) in a mixture of 1,4-dioxane (3 mL) and water (0.3 mL) was degassed with N2 and stirred in a sealed tube at 85°C for 2 days. The reaction mixture was cooled to rt and quenched with water (5 mL). The resulting mixture was extracted with DCM (3 × 5 mL), the combined organic layer was dried over Na2SO4, filtered, and concentrated. The crude material was purified by silica column chromatography (12g cartridge) using a gradient of isohexane solution of ethyl acetate (5%-80% v / v) to obtain the title compound (111 mg, 0.535 mmol, 84.89% yield) as a yellow solid. 1 H NMR (400 MHz, CDCl3) δ 7.71 (s, 1H), 7.06 (dd, J = 17.8, 11.1 Hz, 1H), 5.64 (dd, J = 17.8, 1.0 Hz, 1H), 5.40 (dd, J = 11.1, 1.0 Hz, 1H), 4.91 - 4.71 (m, 2H), 4.47 (dt, J = 26.9, 4.5 Hz, 2H). 19 F NMR (376 MHz, CDCl3) δ -221.93 (tt, J = 46.9, 27.0 Hz).

[0884] 1-(4-methoxybenzyl)-3-nitro-4-vinyl-1H-pyrazole [ka] The solutions of potassium vinyltrifluoroborate (130 mg, 0.971 mmol), palladium(II) chloride (9.0 mg, 0.0508 mmol), triphenylphosphine (40 mg, 0.153 mmol), cesium carbonate (480 mg, 1.47 mmol), and 4-bromo-1-[(4-methoxyphenyl)methyl]-3-nitropyrazole (260 mg, 0.491 mmol) in a mixture of 1,4-dioxane (2.5 mL) and water (0.25 mL) were degassed with N2 and stirred overnight in a sealed tube at 85°C. The reaction mixture was quenched with water (5 mL), extracted with DCM (3 × 5 mL), and the combined organic layers were dried over Na2SO4, filtered, and concentrated. The crude material was purified by silica column chromatography (24g cartridge) using a gradient of isohexane solution of DCM (50%~100%; v / v) to obtain the title compound (143 mg, 0.474 mmol, 96.45% yield) as a yellow solid. 1 H NMR (400 MHz, CDCl3) δ 7.46 (s, 1H), 7.27 (d, J = 9.1 Hz, 2H), 7.03 (dd, J = 17.8, 11.1 Hz, 1H), 6.92 (d, J = 8.7 Hz, 2H), 5.53 (dd, J = 17.8, 1.1 Hz, 1H), 5.32 (dd, J = 11.1, 1.1 Hz, 1H), 5.26 (s, 2H), 3.82 (s, 3H).

[0885] 4-methyl-3-nitro-1-(2,2,2-trifluoroethyl)-1H-pyrazole [ka] Similarly, the compound was prepared from sodium hydride (60% in mineral oil, 0.19 g, 4.72 mmol, 1.20 equivalents), 4-methyl-3-nitro-1H-pyrazole (0.50 g, 3.93 mmol, 1.00 equivalent), DMF (10 mL), and 1-iodo-2,2,2-trifluoroethane (0.42 mL, 4.33 mmol, 1.10 equivalents) at 60°C for 48 hours. After chromatography (PE solution of 0-100% siRNA), the t...

Claims

1. The following formula: 【Chemistry 1】 Compounds of or pharmaceutically acceptable salts or solvates thereof; Here: Ring A is: 【Chemistry 2】 And here: -R Ａ１ Ha-R Ａ１１ And; -R Ａ１１ is -R Ａ１１１ , -F, -Cl, -Br, -I, -CF ３ , -CHF ２ , -OH, -OR Ａ１１１ , -OCF ３ , -NH ２ , -NHR Ａ１１１ , -NR Ａ１１１ ２ , -CN, -C(=O)R Ａ１１１ , -C(=O)OH, -C(=O)OR Ａ１１１ , -C(=O)NH ２ , -C(=O)NHR Ａ１１１ , -C(=O)NR Ａ１１１ ２ , or -S(=O) ２ R Ａ１１１ where; Each -R Ａ１１１ These are independently linear or branched saturated C １－４ It is alkyl; -R Ａ２ Ha-R Ａ２２ And; -R Ａ２２ Ha-R Ａ２２２ , -F, -Cl, -Br, -I, -CF ３ ,-CHF ２ -OH, -OR Ａ２２２ , -OCF ３ , -NH ２ , - NHR Ａ２２２ , -NR Ａ２２２ ２ , -CN, -C(=O)R Ａ２２２ , -C(=O)OH, -C(=O)OR Ａ２２２ -C(=O)NH ２ , -C(=O)NHR Ａ２２２ , -C(=O)NR Ａ２２２ ２ , or -S (=O) ２ R Ａ２２２ And; Each -R Ａ２２２ These are independently linear or branched saturated C １－４ It is alkyl; -R Ａ３ is -H or -R Ａ３３ And; -R Ａ３３ Ha-R Ａ３３３ , -F, -Cl, -Br, -I, -CF ３ -OH, -OR Ａ３３３ , or -OCF ３ And; Each -R Ａ３３３ These are independently linear or branched saturated C １－４ It is alkyl; -R Ａ４ is -H or -R Ａ４４ And; -R Ａ４４ Ha-R Ａ４４４ , -F, -Cl, -Br, -I, -CF ３ -OH, -OR Ａ４４４ , or -OCF ３ And; Each -R Ａ４４４ These are independently linear or branched saturated C １－４ It is alkyl; and: Ring B is: 【Transformation 3】 Selected from, here: Y １ is S, O, NH, or NR Ｙ１ And; Y ２ CH, CR Ｙ２ , or N; Y ３ is N, CH, or CR Ｙ３ And; Y ４ is N, CH, or CR Ｙ４ And; Y ５ is S, O, NH, or NR Ｙ５ And; Y ６ is N, CH, or CR Ｙ６ And; Y ７ is N, CH, or CR Ｙ７ And; Y ８ is N, CH, or CR Ｙ８ And; Y ９ is S, O, NH, or NR Ｙ９ And; Here: Each -R Ｙ２ is, -R Ｙ３ is, -R Ｙ４ is, -R Ｙ６ is, -R Ｙ７ , and -R Ｙ８ is independently -H, -F, -Cl, -Br, -I, -R ＹＹ , -CF ３ , -OH, -OR ＹＹ , -OCF ３ , -NH ２ , -NHR ＹＹ , or -NR ＹＹ ２ is; Each -R ＹＹ These are independently linear or branched saturated C １－４ It is alkyl; Here: each -R Ｙ１ wherein, -R Ｙ５ and -R Ｙ９ are each independently -R ＹＹＮ , -C(=O)R ＹＹＮ , -C(=O)OR ＹＹＮ , -C(=O)NH ２ , -C(=O)NHR ＹＹＮ , -C(=O)NR ＹＹＮ ２ , or -S(=O) ２ R ＹＹＮ ; Each -R ＹＹＮ These are independently linear or branched saturated C １－４ Alkyl, C ３－６ Cycloalkyl, C ３－６ Cycloalkyl-C １－３ Alkyl, phenyl, phenyl-C １－３ Alkyl, C ５－６ Heteroaryl, or C ５－６ Heteroaryl-C １－３ It is alkyl, and here, C １－４ Alkyl groups can be -OH or -OCH as desired. ３ The cycloalkyl, phenyl, and heteroaryl atoms are substituted with -F, -Cl, and -CH as desired. ３ , -CF ３ -OH, -OCH ３ , -NH ２ ,-NH(CH ３ ), and -N(CH ３ ) ２ Substituted with one or more elements selected from; Here: -Q is -Q １ , -L Ｑ１ - Q １ , -Q ２ , -L Ｑ２ - Q ２ , -Q ３ , -L Ｑ３ - Q ３ , -Q ４ , -L Ｑ４ - Q ４ , -Q ５ , or -H; Here: Q １ is C ５－１０ It is a heteroaryl; and: If desired, one or more carbon atoms in a group -R Ｑ１Ｃ It is replaced by; and If desired, and if present, add one or more secondary nitrogen atoms to the -R group. Ｑ１Ｎ It has been replaced with; -L Ｑ１ - indicates a linear or branched saturated C １－４ It is alkylene; Q ２ is C ３－１０ It is a heterocycline; and: If desired, if present, the sulfur is substituted with one or two oxygen groups; If desired, one or more carbon atoms in a group -R Ｑ２Ｃ It is replaced by; and If desired, and if present, add one or more secondary nitrogen atoms to the -R group. Ｑ２Ｎ It has been replaced with; -L Ｑ２ - indicates a linear or branched saturated C １－４ It is alkylene; Q ３ is phenyl or naphthyl; And, if desired, one or more bases-R Ｑ３Ｃ It has been replaced with; -L Ｑ３ - indicates a linear or branched saturated C １－４ It is alkylene; Q ４ is C ３－１０ It is carbocyclyl; And, if desired, one or more bases-R Ｑ４Ｃ It has been replaced with; -L Ｑ４ - indicates a linear or branched saturated C １－４ It is alkylene; Q ５ is a linear or branched saturated C １－６ It is alkyl; And, if desired, one or more bases-R Ｑ５Ｃ It has been replaced with; and: Each -R Ｑ１Ｃ Independently: -F, -Cl, -Br, -I, -R Ｑ１ＣＣ 、 -R Ｑ１ＣＸ 、-OR Ｑ１ＣＸ 、 -OH、-OR Ｑ１ＣＣ 、 -L Ｑ１Ｃ -OH、-L Ｑ１Ｃ -OR Ｑ１ＣＣ 、 -NH ２ , - NHR Ｑ１ＣＣ , -NR Ｑ１ＣＣ ２ And, -R Ｑ１ＣＭ , -L Ｑ１Ｃ -NH ２ 、-L Ｑ１Ｃ -NHR Ｑ１ＣＣ 、-L Ｑ１Ｃ -NR Ｑ１ＣＣ ２ 、-L Ｑ１Ｃ -R Ｑ１ＣＭ 、 -NHC(=O)R Ｑ１ＣＣ 、-N(R Ｑ１ＣＣ )C(=O)R Ｑ１ＣＣ 、-NHC(=O)OR Ｑ１ＣＣ 、 -L Ｑ１Ｃ -NHC(=O)R Ｑ１ＣＣ 、-L Ｑ１Ｃ -NHC(=O)OR Ｑ１ＣＣ 、 -C(=O)NH ２ 、-C(=O)NHR Ｑ１ＣＣ 、-C(=O)NR Ｑ１ＣＣ ２ 、-C(=O)R Ｑ１ＣＭ =O -NHC(=O)NH ２ 、-NHC(=O)NHR Ｑ１ＣＣ 、-NHC(=O)NR Ｑ１ＣＣ ２ 、-NHC(=O)R Ｑ１ＣＭ 、 -L Ｑ１Ｃ -C(=O)NH ２ 、-L Ｑ１Ｃ -C(=O)NHR Ｑ１ＣＣ 、-L Ｑ１Ｃ -C(=O)NR Ｑ１ＣＣ ２ 、-L Ｑ１Ｃ -C(=O)R Ｑ１ＣＭ 、 -C(=O)OH、-C(=O)OR Ｑ１ＣＣ 、 -OC(=O)R Ｑ１ＣＣ 、 -OC(=O)NH ２ 、-OC(=O)NHR Ｑ１ＣＣ 、-OC(=O)NR Ｑ１ＣＣ ２ 、-OC(=O)R Ｑ１ＣＭ 、 -S(=O) ２ R Ｑ１ＣＣ 、-S(=O) ２ R Ｑ１ＣＸ 、 -S(=O) ２ NH ２ 、-S(=O) ２ NHR Ｑ１ＣＣ 、-S(=O) ２ NR Ｑ１ＣＣ ２ 、-S(=O) ２ R Ｑ１ＣＭ 、 -NHS(=O)R Ｑ１ＣＣ 、-NHS(=O) ２ R Ｑ１ＣＣ 、 -CN, -C≡CH, or -NO ２ And; Here, two adjacent -R Ｑ１Ｃ If they exist, then they become one with each other - (CH ２ ) ｎ１ -O-(CH ２ ) ｍ１ - or -O-(CH ２ ) ｐ１ Form -O-, where: n1 is 0, 1, 2, or 3; m1 is 0, 1, 2, or 3; and p1 is 1 or 2; however m1 + n1 is 2 or 3; Here: Each -R Ｑ１ＣＣ These are independently linear or branched saturated C １－６ Alkyl, C ２－６ Alkenil, C ３－６ Cycloalkyl, C ３－６ Cycloalkyl-C １－３ Alkyl, C ３－７ Heterocyclyl, phenyl, phenyl-C １－３ Alkyl, C ５－６ Heteroaryl, or C ５－６ Heteroaryl-C １－３ It is alkyl, and here, C １－６ Alkyl groups can be -OH, -CN, or -OCH as desired. ３ The cycloalkyl, phenyl, and heteroaryl atoms are substituted with -F, -Cl, and -C as desired. １－４ Alkyl, -CHF ２ , -CF ３ -OH, -OCH ３ , -NH ２ ,-NH(CH ３ ), and -N(CH ３ ) ２ Substituted with one or more elements selected from; Each -R Ｑ１ＣＸ These are independently linear or branched saturated C １－４ It is a haloalkyl; Each -L Ｑ１Ｃ - is independently linear or branched saturated C １－４ It is alkylene; Each -R Ｑ１ＣＭ Each independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C ３－１１ It is a heterocycline; and: If desired, one or more carbon atoms in a group -R Ｑ１ＣＭＭ It has been replaced with; If desired, if present, sulfur is substituted with one or two =O groups; and Upon request, if available, secondary nitrogen, -R Ｑ１ＣＭＭ , -C(=O)R Ｑ１ＣＭＭ , -C(=O)OR Ｑ１ＣＭＭ -C(=O)NH ２ , -C(=O)NHR Ｑ１ＣＭＭ , -C(=O)NR Ｑ１ＣＭＭ ２ , and -S(=O) ２ R Ｑ１ＣＭＭ It is substituted with a group selected from; and Each -R Ｑ１ＣＭＭ -F and -NH are independent. ２ , straight-chain or branched saturated C １－４ Alkyl, C １－４ Alkyl OC(=O)NH-, C ３－６ Cycloalkyl, C ３－６ Cycloalkyl-C １－３ Alkyl, phenyl, phenyl-C １－３ Alkyl, C ５－６ Heteroaryl, or C ５－６ Heteroaryl-C １－３ It is alkyl, and here, C １－４ Alkyl groups can be -OH or -OCH as desired. ３ The cycloalkyl, phenyl, and heteroaryl atoms are substituted with -F, -Cl, and -CH as desired. ３ , -CF ３ -OH, -OCH ３ , -NH ２ ,-NH(CH ３ ), and -N(CH ３ ) ２ Substituted with one or more elements selected from; and: Each -R Ｑ１Ｎ Independently: -R Ｑ１ＮＣ 、-L Ｑ１Ｎ -R Ｑ１ＮＣ 、 -R Ｑ１ＮＸ 、 -R Ｑ１Ｎｈｅｔ 、-L Ｑ１Ｎ -R Ｑ１Ｎｈｅｔ 、 -L Ｑ１Ｎ -OH、-L Ｑ１Ｎ -OR Ｑ１ＮＣ 、 -L Ｑ１Ｎ -C(=O)R Ｑ１ＮＣ 、 -S(=O) ２ R Ｑ１ＮＣ 、 -L Ｑ１Ｎ -C(=O)OH、-L Ｑ１Ｎ -C(=O)OR Ｑ１ＮＣ 、 -L Ｑ１Ｎ -C(=O)NH ２ 、-L Ｑ１Ｎ -C(=O)NHR Ｑ１ＮＫ 、-L Ｑ１Ｎ -C(=O)NR Ｑ１ＮＣ ２ 、-L Ｑ１Ｎ -C(=O)R Ｑ１ＮＰ 、 -L Ｑ１Ｎ -NH ２ 、-L Ｑ１Ｎ -NHR Ｑ１ＮＣ 、-L Ｑ１Ｎ -NR Ｑ１ＮＣ ２ 、-L Ｑ１Ｎ -R Ｑ１ＮＭ 、 or -L Ｑ１Ｎ -NHC(=O)OR Ｑ１ＮＣ And; Here: Each -R Ｑ１ＮＣ These are independently linear or branched saturated C １－４ Alkyl, C ３－６ Cycloalkyl, C ３－６ Cycloalkyl-C １－３ Alkyl, phenyl, phenyl-C １－３ Alkyl, C ５－６ Heteroaryl, or C ５－６ Heteroaryl-C １－３ It is alkyl, and here each C １－４ Alkyl groups can be -F, -OH, -C≡N, or -SO as desired. ２ -CH ３ , or -OCH ３ The substituted elements are, where each cycloalkyl, phenyl, and heteroaryl is optionally -F, -Cl, -Br, linear or branched saturated C １－４ Alkyl, -CHF ２ , -CF ３ -OH, -OCH ３ ien-CH ２ -O-CH ３ , -OCH ２ CH ３ -C(=O)-NH-phenyl, -NH ２ ,-NH(CH ３ ), and -N(CH ３ ) ２ It is substituted with one or more elements selected from; where C １－４ Alkyl and phenyl are independently and optionally -CH ３ or substituted with -OH; Each -R Ｑ１ＮＸ These are independently linear or branched saturated C １－４ It is a haloalkyl; Each -L Ｑ１Ｎ - is independently linear or branched saturated C １－４ It is an alkylene; here, C １－４ Alkylenes are substituted with -OH or -OMe as desired. Each -R Ｑ１ＮＭ Each independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C ３－７ It is a heterocycline; and: If desired, one or more carbon atoms in a group -R Ｑ１ＮＭＭ It has been replaced with; If desired, if present, sulfur is substituted with one or two =O groups; and Upon request, if available, secondary nitrogen, -R Ｑ１ＮＭＭ , -C(=O)R Ｑ１ＮＭＭ , -C(=O)OR Ｑ１ＮＭＭ -C(=O)NH ２ , -C(=O)NHR Ｑ１ＮＭＭ , -C(=O)NR Ｑ１ＮＭＭ ２ , and -S(=O) ２ R Ｑ１ＮＭＭ It is substituted with a group selected from; and Each -R Ｑ１ＮＭＭ These are independently linear or branched saturated C １－４ Alkyl, C ３－６ Cycloalkyl, C ３－６ Cycloalkyl-C １－３ Alkyl, phenyl, phenyl-C １－３ Alkyl, C ５－６ Heteroaryl, or C ５－６ Heteroaryl-C １－３ It is alkyl, and here, C １－４ Alkyl groups can be -OH or -OCH as desired. ３ The cycloalkyl, phenyl, and heteroaryl atoms are substituted with -F, -Cl, and -CH as desired. ３ , -CF ３ -OH, -OCH ３ , -NH ２ ,-NH(CH ３ ), and -N(CH ３ ) ２ Substituted with one or more elements selected from; and: Each -R Ｑ１Ｎｈｅｔ These are independently non-aromatic C ３－７ It is a heterocycline; and: If desired, if present, the sulfur is substituted with one or two oxygen groups; If desired, one or more carbon atoms in a group -R Ｑ１ＮＨＨ Or it is replaced by = O; and Upon request, if available, secondary nitrogen, -R Ｑ１ＮＨＨ , -C(=O)R Ｑ１ＮＪＪ , -C(=O)OR Ｑ１ＮＨＨ -C(=O)NH ２ , -C(=O)NHR Ｑ１ＮＨＨ , -C(=O)NR Ｑ１ＮＨＨ ２ , and -S(=O) ２ R Ｑ１ＮＨＨ It is substituted with a group selected from; Here: Each -R Ｑ１ＮＨＨ These are independently linear or branched saturated C １－４ Alkyl, C ３－６ Cycloalkyl, C ３－６ Cycloalkyl-C １－３ Alkyl, C ３－７ Heterocyclyl, phenyl, phenyl-C １－３ Alkyl, C ５－６ Heteroaryl, or C ５－６ Heteroaryl-C １－３ It is alkyl, and here, C １－４ Alkyl groups can be -OH or -OCH as desired. ３ The cycloalkyl, phenyl, and heteroaryl atoms are substituted with -F, -Cl, and -CH as desired. ３ , -CF ３ -OH, -OCH ３ , -NH ２ ,-NH(CH ３ ), and -N(CH ３ ) ２ Substituted with one or more elements selected from; Here: -R Ｑ１ＮＪＪ Ha-R Ｊ１ And, -R Ｊ２ , -L Ｊ -R Ｊ２ And, -R Ｊ３ , -L Ｊ -R Ｊ３ And, -R Ｊ４ , -L Ｊ -R Ｊ４ And, -R Ｊ５ , or -L Ｊ -R Ｊ５ And; -R Ｊ１ is a linear or branched saturated C １－６ Alkyl; and optionally -F, -OH, -OR ＪＪ -O-phenyl, -C(=O)OH, -C(=O)OR ＪＪ , -NH ２ , - NHR ＪＪ , and -NR ＪＪ ２ Substituted with one or more elements selected from; Each -R Ｊ２ C is independent ３－６ It is cycloalkyl; and optionally -F and -R ＪＪ , -CF ３ -OH, -OR ＪＪ , -NH ２ , - NHR ＪＪ , and -NR ＪＪ ２ Substituted with one or more elements selected from; Each -R Ｊ３ These are independently non-aromatic C ３－７ It is a heterocycline; and: If desired, if present, the sulfur is substituted with one or two oxygen groups; If desired, carbon is -F and -R ＪＪ , -CF ３ -OH, -OR ＪＪ , -NH ２ , - NHR ＪＪ , and -NR ＪＪ ２ It is replaced by one or more elements selected from; and Upon request, if available, secondary nitrogen, -R ＪＪ , -C(=O)R ＪＪ , -C(=O)OR ＪＪ , and -S(=O) ２ R ＪＪ It is substituted with a group selected from; Each -R Ｊ４ is phenyl; and optionally -F, -Cl, and -R ＪＪ , -CF ３ -OH, -OR ＪＪ , -NH ２ , - NHR ＪＪ , and -NR ＪＪ ２ Substituted with one or more elements selected from; Each -R Ｊ５ C is independent ５－６ It is a heteroaryl; and: If desired, carbon is -F and -R ＪＪ , -CF ３ -OH, -OR ＪＪ , -NH ２ , - NHR ＪＪ , and -NR ＪＪ ２ It is replaced by one or more elements selected from; and Upon request, if available, secondary nitrogen, -R ＪＪ , -C(=O)R ＪＪ , -C(=O)OR ＪＪ , and -S(=O) ２ R ＪＪ It is substituted with a group selected from; Each -L Ｊ - is independently linear or branched saturated C １－４ It is an alkylene and optionally substituted with one or more -F groups; Each -R ＪＪ is a linear or branched saturated C １－４ It is alkyl; Here: -R Ｑ１ＮＫ Ha-R Ｋ１ And, -R Ｋ２ , -L Ｋ -R Ｋ２ And, -R Ｋ３ , -L Ｋ -R Ｋ３ And, -R Ｋ４ , -L Ｋ -R Ｋ４ And, -R Ｋ５ , or -L Ｋ -R Ｋ５ And; -R Ｋ１ is a linear or branched saturated C １－７ Alkyl; and optionally -F, -OH, -OR ＫＫ , -OCH ２ CH ２ OCH ３ -O-phenyl, -C(=O)OH, -C(=O)OR ＫＫ , -NH ２ , - NHR ＫＫ , and -NR ＫＫ ２ Substituted with one or more elements selected from; Each -R Ｋ２ C is independent ３－６ It is cycloalkyl; and optionally -F and -R ＫＫ , -CF ３ -OH, -OR ＫＫ , -NH ２ , - NHR ＫＫ , and -NR ＫＫ ２ Substituted with one or more elements selected from; Each -R Ｋ３ These are independently non-aromatic C ３－７ It is a heterocycline; and: If desired, carbon is -F and -R ＫＫ , -CF ３ -OH, -OR ＫＫ , -NH ２ , - NHR ＫＫ , and -NR ＫＫ ２ It is replaced by one or more elements selected from; and Upon request, if available, secondary nitrogen, -R ＫＫ , -C(=O)R ＫＫ , -C(=O)OR ＫＫ , and -S(=O) ２ R ＫＫ It is substituted with a group selected from; Each -R Ｋ４ is phenyl; and optionally -F, -Cl, and -R ＫＫ , -CF ３ -OH, -OR ＫＫ , -NH ２ , - NHR ＫＫ , and -NR ＫＫ ２ Substituted with one or more elements selected from; Each -R Ｋ５ C is independent ５－６ It is a heteroaryl; and: If desired, carbon is -F and -R ＫＫ , -CF ３ -OH, -OR ＫＫ , -NH ２ , - NHR ＫＫ , and -NR ＫＫ ２ It is replaced by one or more elements selected from; and Upon request, if available, secondary nitrogen, -R ＫＫ , -C(=O)R ＫＫ , -C(=O)OR ＫＫ , and -S(=O) ２ R ＫＫ It is substituted with a group selected from; Each -L Ｋ - indicates a linear or branched saturated C １－４ It is an alkylene, optionally substituted with one or more -F atoms; Each -R ＫＫ is a linear or branched saturated C １－４ It is alkyl; Here: -R Ｑ１ＮＰ It has at least one N-ring atom, and C is bonded via the N-ring atom. ３－１１ It is a heterocycline; and: If desired, if present, the sulfur is substituted with one or two =O groups; Carbon can be added as desired (-R) Ｑ１ＮＰＰ , -F, -OH, -OR Ｑ１ＮＰＰ Substituted with one or more groups selected from , and = O; and Upon request, if available, secondary nitrogen, -R Ｑ１ＮＰＰ And, -R Ｑ１ＮＰＰＸ , -C(=O)R Ｑ１ＮＰＰ , -C(=O)OR Ｑ１ＮＰＰ -C(=O)NH ２ , -C(=O)NHR Ｑ１ＮＰＰ , -C(=O)NR Ｑ１ＮＰＰ ２ , and -S(=O) ２ R Ｑ１ＮＰＰ It is substituted with a group selected from; Each -R Ｑ１ＮＰＰ These are independently linear or branched saturated C １－４ Alkyl, C ３－６ Cycloalkyl, C ３－６ Cycloalkyl-C １－３ Alkyl, phenyl, phenyl-C １－３ Alkyl, C ５－６ Heteroaryl, or C ５－６ Heteroaryl-C １－３ It is alkyl, and here, C １－４ The alkyl group can be -F, -OH, or -OCH as desired. ３ The cycloalkyl, phenyl, and heteroaryl atoms are substituted with -F, -Cl, and -CH as desired. ３ , -CF ３ -OH, -OCH ３ , -NH ２ ,-NH(CH ３ ), and -N(CH ３ ) ２ Substituted with one or more elements selected from; -R Ｑ１ＮＰＰＸ is a linear or branched saturated C １－４ It is a haloalkyl; and: Each -R Ｑ２Ｃ Independently: -F, -R Ｑ２ＣＣ 、-R Ｑ２ＣＸ 、 -OH、-OR Ｑ２ＣＣ 、-OR Ｑ２ＣＸ 、 -NH ２ , - NHR Ｑ２ＣＣ , -NR Ｑ２ＣＣ ２ And, -R Ｑ２ＣＭ , -NHC(=O)R Ｑ２ＣＣ 、-NHC(=O)OR Ｑ２ＣＣ 、 -C(=O)NH ２ 、-C(=O)NHR Ｑ２ＣＣ 、-C(=O)NR Ｑ２ＣＣ ２ 、-C(=O)R Ｑ２ＣＭ 、 -C(=O)OH、-C(=O)OR Ｑ２ＣＣ 、 -OC(=O)R Ｑ２ＣＣ 、 -OC(=O)NH ２ , -OC(=O)NHR Ｑ２ＣＣ , -OC(=O)NR Ｑ２ＣＣ ２ -OC(=O)R Ｑ２ＣＭ ,or = O And; Here: Each -R Ｑ２ＣＣ These are independently linear or branched saturated C １－４ Alkyl, C ３－６ Cycloalkyl, C ３－６ Cycloalkyl-C １－３ Alkyl, phenyl, C ３－７ Heterocyclyl, phenyl-C １－３ Alkyl, C ５－６ Heteroaryl, or C ５－６ Heteroaryl-C １－３ It is alkyl, and here, C １－４ Alkyl groups can be -OH or -OCH as desired. ３ The cycloalkyl, phenyl, and heteroaryl atoms are substituted with -F, -Cl, and -CH as desired. ３ , -CF ３ -OH, -OCH ３ , -NH ２ ,-NH(CH ３ ), and -N(CH ３ ) ２ Substituted with one or more elements selected from; Each -R Ｑ２ＣＸ These are independently linear or branched saturated C １－４ It is a haloalkyl; Each -R Ｑ２ＣＭ Each independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C ３－１１ It is a heterocycline; and: If desired, one or more carbon atoms in a group -R Ｑ２ＣＭＭ It has been replaced with; If desired, if present, sulfur is substituted with one or two =O groups; and Upon request, if available, secondary nitrogen, -R Ｑ２ＣＭＭ , -C(=O)R Ｑ２ＣＭＭ , -C(=O)OR Ｑ２ＣＭＭ -C(=O)NH ２ , -C(=O)NHR Ｑ２ＣＭＭ , -C(=O)NR Ｑ２ＣＭＭ ２ , and -S(=O) ２ R Ｑ２ＣＭＭ It is substituted with a group selected from; and Each -R Ｑ２ＣＭＭ These are independently linear or branched saturated C １－４ Alkyl, C ３－６ Cycloalkyl, C ３－６ Cycloalkyl-C １－３ Alkyl, phenyl, phenyl-C １－３ Alkyl, C ５－６ Heteroaryl, or C ５－６ Heteroaryl-C １－３ It is alkyl, and here, C １－４ Alkyl groups can be -OH or -OCH as desired. ３ The cycloalkyl, phenyl, and heteroaryl atoms are substituted with -F, -Cl, and -CH as desired. ３ , -CF ３ -OH, -OCH ３ , -NH ２ ,-NH(CH ３ ), and -N(CH ３ ) ２ Substituted with one or more elements selected from; and: Each -R Ｑ２Ｎ Independently: -R Ｑ２ＮＣ 、 =O、-C(=O)R Ｑ２ＮＣ 、 -C(=O)-L Ｑ２Ｎ -OH、-C(=O)-L Ｑ２Ｎ -OR Ｑ２ＮＣ 、 -C(=O)-L Ｑ２Ｎ -NH ２ 、-C(=O)-L Ｑ２Ｎ -NHR Ｑ２ＮＣ 、-C(=O)-L Ｑ２Ｎ -NR Ｑ２ＮＣ ２ 、-C(=O)-L Ｑ２Ｎ -R Ｑ２ＮＭ 、 -C(=O)OR Ｑ２ＮＣ 、 -L Ｑ２Ｎ -NH ２ 、-L Ｑ２Ｎ -NHR Ｑ２ＮＣ 、-L Ｑ２Ｎ -NR Ｑ２ＮＣ ２ 、-L Ｑ２Ｎ -R Ｑ２ＮＭ 、 -C(=O)NH ２ 、-C(=O)NHR Ｑ２ＮＣ 、-C(=O)NR Ｑ２ＮＣ ２ 、-C(=O)R Ｑ２ＮＭ 、 -L Ｑ２Ｎ -C(=O)NH ２ ,-L Ｑ２Ｎ -C(=O)NHR Ｑ２ＮＣ ,-L Ｑ２Ｎ -C(=O)NR Ｑ２ＮＣ ２ ,-L Ｑ２Ｎ -C(=O)R Ｑ２ＮＭ 、or -S(=O) ２ R Ｑ２ＮＣ And; Here: Each -R Ｑ２ＮＣ These are independently linear or branched saturated C １－６ Alkyl, C ３－６ Cycloalkyl, C ３－６ Cycloalkyl-C １－３ Alkyl, phenyl, phenyl-C １－３ Alkyl, C ５－６ Heteroaryl, or C ５－６ Heteroaryl-C １－３ It is alkyl, and here, C １－６ Alkyl groups can be -OH or -OCH as desired. ３ The cycloalkyl, phenyl, and heteroaryl atoms are substituted with -F, -Cl, and -CH as desired. ３ , -CF ３ -OH, -OCH ３ , -NH ２ ,-NH(CH ３ ), and -N(CH ３ ) ２ Substituted with one or more elements selected from; Each -L Ｑ２Ｎ - is independently linear or branched saturated C １－４ It is alkylene; Each -R Ｑ２ＮＭ Each independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C ３－１１ It is a heterocycline; and: If desired, one or more carbon atoms in a group -R Ｑ２ＮＭＭ It has been replaced with; If desired, if present, sulfur is substituted with one or two =O groups; and Upon request, if available, secondary nitrogen, -R Ｑ２ＮＭＭ , -C(=O)R Ｑ２ＮＭＭ , -C(=O)OR Ｑ２ＮＭＭ -C(=O)NH ２ , -C(=O)NHR Ｑ２ＮＭＭ , -C(=O)NR Ｑ２ＮＭＭ ２ , and -S(=O) ２ R Ｑ２ＮＭＭ It is substituted with a group selected from; and Each -R Ｑ２ＮＭＭ These are independently linear or branched saturated C １－４ Alkyl, C ３－６ Cycloalkyl, C ３－６ Cycloalkyl-C １－３ Alkyl, phenyl, phenyl-C １－３ Alkyl, C ５－６ Heteroaryl, or C ５－６ Heteroaryl-C １－３ It is alkyl, and here, C １－４ Alkyl groups can be -OH or -OCH as desired. ３ The cycloalkyl, phenyl, and heteroaryl atoms are substituted with -F, -Cl, and -CH as desired. ３ , -CF ３ -OH, -OCH ３ , -NH ２ ,-NH(CH ３ ), and -N(CH ３ ) ２ Substituted with one or more elements selected from; and: Each -R Ｑ３Ｃ Independently: -F, -Cl, -Br, -I, -R Ｑ３ＣＣ 、 -R Ｑ３ＣＸ 、-OR Ｑ３ＣＸ 、 -OH、-OR Ｑ３ＣＣ 、 -L Ｑ３Ｃ -OH、-L Ｑ３Ｃ -OR Ｑ３ＣＣ 、 -NH ２ , - NHR Ｑ３ＣＣ , -NR Ｑ３ＣＣ ２ And, -R Ｑ３ＣＭ , -L Ｑ３Ｃ -NH ２ 、-L Ｑ３Ｃ -NHR Ｑ３ＣＣ 、-L Ｑ３Ｃ -NR Ｑ３ＣＣ ２ 、-L Ｑ３Ｃ -R Ｑ３ＣＭ 、 -NHC(=O)R Ｑ３ＣＣ 、-NHC(=O)OR Ｑ３ＣＣ 、 -L Ｑ３Ｃ -NHC(=O)R Ｑ３ＣＣ 、-L Ｑ３Ｃ -NHC(=O)OR Ｑ３ＣＣ 、 -C(=O)NH ２ 、-C(=O)NHR Ｑ３ＣＣ 、-C(=O)NR Ｑ３ＣＣ ２ 、-C(=O)R Ｑ３ＣＭ 、 -L Ｑ３Ｃ -C(=O)NH ２ 、-L Ｑ３Ｃ -C(=O)NHR Ｑ３ＣＣ 、-L Ｑ３Ｃ -C(=O)NR Ｑ３ＣＣ ２ 、-L Ｑ３Ｃ -C(=O)R Ｑ３ＣＭ 、 -C(=O)OH、-C(=O)OR Ｑ３ＣＣ 、 -OC(=O)R Ｑ３ＣＣ 、 -OC(=O)NH ２ 、-OC(=O)NHR Ｑ３ＣＣ 、-OC(=O)NR Ｑ３ＣＣ ２ 、-OC(=O)R Ｑ３ＣＭ 、 -S(=O) ２ R Ｑ３ＣＣ 、S(=O) ２ R Ｑ３ＣＭ ; -CN, or -NO ２ And; Here, two adjacent -R Ｑ３Ｃ If they exist, then they become one with each other - (CH ２ ) ｎ３ -O-(CH ２ ) ｍ３ -, -(CH ２ ) ｎ３ -NH-(CH ２ ) ｍ３ -, -(CH ２ ) ｑ３ (C(O))-NH-(CH ２ ) ｖ３ - -NH-(CH ２ ) ｑ３ C(O)(CH ２ ) ｖ３ -O-, -NH-(CH ２ ) ｐ３ -NH- or -O-(CH ２ ) ｐ３ Form -O-, where: n3 is 0, 1, 2, or 3; m3 is 0, 1, 2, or 3; p3 is 1 or 2; q3 is 0, 1, 2, or 3; v3 is 0, 1, 2, or 3, where m3 + n3 is 2 or 3; Here: Each -R Ｑ３ＣＣ These are independently linear or branched saturated C １－４ Alkyl, C ３－６ Cycloalkyl, C ３－６ Cycloalkyl-C １－３ Alkyl, C ３－７ Heterocyclyl, phenyl, phenyl-C １－３ Alkyl, C ５－６ Heteroaryl, or C ５－６ Heteroaryl-C １－３ It is alkyl, and here, C １－４ The alkyl group can be -F, -OH, or -OCH as desired. ３ The cycloalkyl, phenyl, and heteroaryl atoms are substituted with -F, -Cl, and -CH as desired. ３ , -CF ３ -OH, -OCH ３ , -NH ２ ,-NH(CH ３ ), and -N(CH ３ ) ２ Substituted with one or more elements selected from; Each -R Ｑ３ＣＸ These are independently linear or branched saturated C １－４ It is a haloalkyl; Each -L Ｑ３Ｃ - is independently linear or branched saturated C １－４ It is alkylene; Each -R Ｑ３ＣＭ Each independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C ３－１１ It is a heterocycline; and: If desired, one or more carbon atoms in a group -R Ｑ３ＣＭＭ It has been replaced with; If desired, if present, sulfur is substituted with one or two =O groups; and Upon request, if available, secondary nitrogen, -R Ｑ３ＣＭＭ , -C(=O)R Ｑ３ＣＭＭ , -C(=O)OR Ｑ３ＣＭＭ -C(=O)NH ２ , -C(=O)NHR Ｑ３ＣＭＭ , -C(=O)NR Ｑ３ＣＭＭ ２ , and -S(=O) ２ R Ｑ３ＣＭＭ It is substituted with a group selected from; and Each -R Ｑ３ＣＭＭ is independently a straight-chain or branched-chain saturated -F, C １－４ alkyl, C ３－６ cycloalkyl, C ３－６ cycloalkyl-C １－３ alkyl, phenyl, phenyl-C １－３ alkyl, C ５－６ heteroaryl, or C ５－６ heteroaryl-C １－３ alkyl, where C １－４ alkyl is optionally -OH or -OCH ３ substituted, and each cycloalkyl, phenyl, and heteroaryl is optionally -F, -Cl, -CH ３ , -CF ３ , -OH, -OCH ３ , -NH ２ , -NH(CH ３ ), and -N(CH ３ ) ２ substituted with one or more groups selected from; and: Each -R Ｑ４Ｃ Independently: -F, -R Ｑ４ＣＣ is, -R Ｑ４ＣＸ , -OH、-OR Ｑ４ＣＣ 、-OR Ｑ４ＣＸ 、 -NH ２ , - NHR Ｑ４ＣＣ , -NR Ｑ４ＣＣ ２ And, -R Ｑ４ＣＭ , -NHC(=O)R Ｑ４ＣＣ 、-NHC(=O)OR Ｑ４ＣＣ 、 -C(=O)NH ２ 、-C(=O)NHR Ｑ４ＣＣ 、-C(=O)NR Ｑ４ＣＣ ２ 、-C(=O)R Ｑ４ＣＭ 、 -C(=O)OH、-C(=O)OR Ｑ４ＣＣ 、 -OC(=O)R Ｑ４ＣＣ 、 -OC(=O)NH ２ , -OC(=O)NHR Ｑ４ＣＣ , -OC(=O)NR Ｑ４ＣＣ ２ -OC(=O)R Ｑ４ＣＭ ,or = O And; Here: Each -R Ｑ４ＣＣ These are independently linear or branched saturated C １－４ Alkyl, C ３－６ Cycloalkyl, C ３－６ Cycloalkyl-C １－３ Alkyl, C ３－７ Heterocyclyl, phenyl, phenyl-C １－３ Alkyl, C ５－６ Heteroaryl, or C ５－６ Heteroaryl-C １－３ It is alkyl, and here, C １－４ Alkyl groups can be -OH or -OCH as desired. ３ The cycloalkyl, phenyl, and heteroaryl atoms are substituted with -F, -Cl, and -CH as desired. ３ , -CF ３ -OH, -OCH ３ , -NH ２ ,-NH(CH ３ ), and -N(CH ３ ) ２ Substituted with one or more elements selected from; Each -R Ｑ４ＣＸ These are independently linear or branched saturated C １－４ It is a haloalkyl; Each -R Ｑ４ＣＭ Each independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C ３－１１ It is a heterocycline; and: If desired, one or more carbon atoms in a group -R Ｑ４ＣＭＭ It has been replaced with; If desired, if present, sulfur is substituted with one or two =O groups; and Upon request, if available, secondary nitrogen, -R Ｑ４ＣＭＭ , -C(=O)R Ｑ４ＣＭＭ , -C(=O)OR Ｑ４ＣＭＭ -C(=O)NH ２ , -C(=O)NHR Ｑ４ＣＭＭ , -C(=O)NR Ｑ４ＣＭＭ ２ , and -S(=O) ２ R Ｑ４ＣＭＭ It is substituted with a group selected from; Each -R Ｑ４ＣＭＭ is independently a straight-chain or branched-chain saturated C １－４ alkyl, C ３－６ cycloalkyl, C ３－６ cycloalkyl-C １－３ alkyl, phenyl, phenyl-C １－３ alkyl, C ５－６ heteroaryl, or C ５－６ heteroaryl-C １－３ alkyl, where C １－４ alkyl is optionally substituted with -OH or -OCH ３ and each cycloalkyl, phenyl and heteroaryl is optionally substituted with one or more groups selected from -F, -Cl, -CH ３ , -CF ３ , -OH, -OCH ３ , -NH ２ , -NH(CH ３ ), and -N(CH ３ ) ２ ; and is substituted with one or more groups selected from and: Each -R Ｑ５Ｃ Independently: -F、-OH、-OR Ｑ５ＣＣ 、-OCF ３ 、 -NH ２ , - NHR Ｑ５ＣＣ , -NR Ｑ５ＣＣ ２ And, -R Ｑ５ＣＭ , -NHC(=O)R Ｑ５ＣＣ 、-NHC(=O)OR Ｑ５ＣＣ 、 -C(=O)NH ２ 、-C(=O)NHR Ｑ５ＣＣ 、-C(=O)NR Ｑ５ＣＣ ２ 、-C(=O)R Ｑ５ＣＭ 、 -C(=O)OH、-C(=O)OR Ｑ５ＣＣ 、 -OC(=O)R Ｑ５ＣＣ 、 -OC(=O)NH ２ , -OC(=O)NHR Ｑ５ＣＣ , -OC(=O)NR Ｑ５ＣＣ ２ , or -OC(=O)R Ｑ５ＣＭ And; Here: Each -R Ｑ５ＣＣ These are independently linear or branched saturated C １－４ Alkyl, C ３－６ Cycloalkyl, C ３－６ Cycloalkyl-C １－３ Alkyl, C ３－７ Heterocyclyl, phenyl, phenyl-C １－３ Alkyl, C ５－６ Heteroaryl, or C ５－６ Heteroaryl-C １－３ It is alkyl, and here, C １－４ Alkyl groups can be -OH or -OCH as desired. ３ The cycloalkyl, phenyl, and heteroaryl atoms are substituted with -F, -Cl, and -CH as desired. ３ , -CF ３ -OH, -OCH ３ , -NH ２ ,-NH(CH ３ ), and -N(CH ３ ) ２ Substituted with one or more elements selected from; Each -R Ｑ５ＣＭ Each independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C ３－１１ It is a heterocycline; and: If desired, one or more carbon atoms in a group -R Ｑ５ＣＭＭ It has been replaced with; If desired, if present, sulfur is substituted with one or two =O groups; and Upon request, if available, secondary nitrogen, -R Ｑ５ＣＭＭ , -C(=O)R Ｑ５ＣＭＭ , -C(=O)OR Ｑ５ＣＭＭ -C(=O)NH ２ , -C(=O)NHR Ｑ５ＣＭＭ , -C(=O)NR Ｑ５ＣＭＭ ２ , and -S(=O) ２ R Ｑ５ＣＭＭ It is substituted with a group selected from; Each -R Ｑ５ＣＭＭ These are independently linear or branched saturated C １－４ Alkyl, C ３－６ Cycloalkyl, C ３－６ Cycloalkyl-C １－３ Alkyl, phenyl, phenyl-C １－３ Alkyl, C ５－６ Heteroaryl, or C ５－６ Heteroaryl-C １－３ It is alkyl, and here, C １－４ Alkyl groups can be -OH or -OCH as desired. ３ The cycloalkyl, phenyl, and heteroaryl atoms are substituted with -F, -Cl, and -CH as desired. ３ , -CF ３ -OH, -OCH ３ , -NH ２ ,-NH(CH ３ ), and -N(CH ３ ) ２ Substituted with one or more elements selected from, A compound or its pharmaceutically acceptable salt or solvate.

2. -R Ａ１ ga-R Ａ１１ and -R Ａ１１ ga-R Ａ１１１ , -F, -Cl, or -Br; and Each -R Ａ１１１ These independently form linear or branched saturated C １－４ It is alkyl. The compound of claim 1 or a pharmaceutically acceptable salt or solvate thereof.

3. -R Ａ２ ga-R Ａ２２ And; -R Ａ２２ ga-R Ａ２２２ , -F, -Cl, or -Br; and Each -R Ａ２２２ These independently form linear or branched saturated C １－４ It is alkyl. A compound according to claim 1 or 2, or a pharmaceutically acceptable salt or solvate thereof.

4. -R Ａ３ is -H or -R Ａ３３ and -R Ａ３３ is -Br, Any compound according to claims 1 to 3 or a pharmaceutically acceptable salt or solvate thereof.

5. -R Ａ４ is -H or -R Ａ４４ And; -R Ａ４４ ga-R Ａ４４４ , -Cl, or -Br; and Each -R Ａ４４４ These independently form linear or branched saturated C １－４ It is alkyl. Any compound according to claims 1 to 4 or a pharmaceutically acceptable salt or solvate thereof.

6. Ring B is: 【Chemistry 4】 Selected from, here: Y １ is S or O; Y ２ CH, CR Ｙ２ , or N; Y ３ N is; and Each -R Ｙ２ NH became independent ２ That is, Any compound according to claims 1 to 5 or a pharmaceutically acceptable salt or solvate thereof.

7. -Q is -Q １ , or -L Ｑ１ - Q １ And; here: Q １ C ５－１０ It is a heteroaryl; and: If desired, one or more carbon atoms in a group -R Ｑ１Ｃ It is replaced by; and If desired, and if present, add one or more secondary nitrogen atoms to the -R group. Ｑ１Ｎ It is replaced by; and -L Ｑ１ - indicates a linear or branched saturated C １－４ It is alkylene; wherein Each -R Ｑ１Ｃ Independently: -F, -Cl, -Br, -R Ｑ１ＣＣ 、 -R Ｑ１ＣＸ 、-OR Ｑ１ＣＸ 、 -OH、-OR Ｑ１ＣＣ 、 -NH ２ , - NHR Ｑ１ＣＣ , -NR Ｑ１ＣＣ ２ And, -R Ｑ１ＣＭ , -L Ｑ１Ｃ -R Ｑ１ＣＭ 、 -NHC(=O)R Ｑ１ＣＣ 、-N(R Ｑ１ＣＣ )C(=O)R Ｑ１ＣＣ 、-NHC(=O)OR Ｑ１ＣＣ 、 -C(=O)NH ２ 、-C(=O)NHR Ｑ１ＣＣ 、-C(=O)NR Ｑ１ＣＣ ２ 、-C(=O)R Ｑ１ＣＭ ,=0, -NHC(=O)NHR Ｑ１ＣＣ 、 -L Ｑ１Ｃ -C(=O)NR Ｑ１ＣＣ ２ 、 -C(=O)OH、-C(=O)OR Ｑ１ＣＣ 、 -OC(=O)NH ２ 、 -S(=O) ２ R Ｑ１ＣＸ 、 -S(=O) ２ R Ｑ１ＣＭ 、 -NHS(=O)R Ｑ１ＣＣ 、-NHS(=O) ２ R Ｑ１ＣＣ 、 -CN, or -C≡CH And; Here: Each -R Ｑ１ＣＣ These independently form linear or branched saturated C １－６ Alkyl, C ２－６ Alkenil, C ３－６ Cycloalkyl, C ３－７ Heterocyclyl, phenyl, or C ５－６ A heteroaryl compound, where C １－６ The alkyl group can be -OH, -CN, or -OCH as desired. ３ The phenyl and heteroaryl compounds are substituted with -F, -Cl, and -CH as desired. ３ ,-CHF ２ , -CF ３ , -OCH ３ Substituted with one or more elements selected from; Each -R Ｑ１ＣＸ These independently form linear or branched saturated C １－４ It is a haloalkyl; Each -L Ｑ１Ｃ - is independently linear or branched saturated C １－４ It is alkylene; Each -R Ｑ１ＣＭ Each element independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C ３－１１ It is a heterocycline; and: If desired, one or more carbon atoms in a group -R Ｑ１ＣＭＭ It has been replaced with; Upon request, if available, secondary nitrogen, -R Ｑ１ＣＭＭ It is substituted with a group selected from; and Each -R Ｑ１ＣＭＭ -F, -NH are independent ２ , straight-chain or branched saturated C １－４ Alkyl, C １－４ Alkyl OC(=O)NH-, C ３－６ It is a cycloalkyl, where C １－４ The alkyl group is optionally substituted with -OH; and: Each -R Ｑ１Ｎ Independently: -R Ｑ１ＮＣ 、-L Ｑ１Ｎ -R Ｑ１ＮＣ 、 -R Ｑ１ＮＸ 、 -R Ｑ１Ｎｈｅｔ 、-L Ｑ１Ｎ -R Ｑ１Ｎｈｅｔ 、 -L Ｑ１Ｎ -OH、-L Ｑ１Ｎ -OR Ｑ１ＮＣ 、 -S(=O) ２ R Ｑ１ＮＣ 、 -L Ｑ１Ｎ -C(=O)OH、-L Ｑ１Ｎ -C(=O)OR Ｑ１ＮＣ 、 -L Ｑ１Ｎ -C(=O)NH ２ 、-L Ｑ１Ｎ -C(=O)NHR Ｑ１ＮＫ 、-L Ｑ１Ｎ -C(=O)NR Ｑ１ＮＣ ２ 、-L Ｑ１Ｎ -C(=O)R Ｑ１ＮＰ 、 -L Ｑ１Ｎ -NH ２ 、-L Ｑ１Ｎ -NR Ｑ１ＮＣ ２ 、 or -L Ｑ１Ｎ -NHC(=O)OR Ｑ１ＮＣ And; Here: Each -R Ｑ１ＮＣ These independently form linear or branched saturated C １－４ Alkyl, C ３－６ Cycloalkyl, phenyl, or C ５－６ It is a heteroaryl, where each C １－４ Alkyl groups can be -F, -OH, -C≡N, or -SO as desired. ２ -CH ３ , or -OCH ３ The substituted elements are, where each cycloalkyl, phenyl, and heteroaryl is optionally -F, -Cl, -Br, linear or branched saturated C １－４ Alkyl, -CHF ２ , -CF ３ ien-CH ２ -O-CH ３ , -OCH ２ CH ３ , -C(=O)-NH-phenyl, where C １－４ by-CH, which is optionally substituted with alkyl and phenyl groups. ３ or substituted with one or more groups selected from -OH; Each -R Ｑ１ＮＸ These independently form linear or branched saturated C １－４ It is a haloalkyl; Each -L Ｑ１Ｎ - is independently linear or branched saturated C １－４ Alkylene and wherein C １－４ The alkylene is substituted with -OH or -OMe as desired; and: Each -R Ｑ１Ｎｈｅｔ These are independently non-aromatic C ３－７ It is a heterocycline; and: The carbon atoms are optionally substituted with one or more or =O atoms; and Upon request, if available, secondary nitrogen, -R Ｑ１ＮＨＨ , -C(=O)R Ｑ１ＮＪＪ , -C(=O)OR Ｑ１ＮＨＨ , -C(=O)NHR Ｑ１ＮＨＨ , -C(=O)NR Ｑ１ＮＨＨ ２ It is substituted with a group selected from; Here: Each -R Ｑ１ＮＨＨ These independently form linear or branched saturated C １－４ Alkyl, C ３－６ Cycloalkyl, phenyl-C １－３ Alkyl; And here: -R Ｑ１ＮＪＪ ga-R Ｊ１ , -L Ｊ -R Ｊ２ And, -R Ｊ３ , -L Ｊ -R Ｊ３ And, -R Ｊ４ , -L Ｊ -R Ｊ４ , or -L Ｊ -R Ｊ５ And; -R Ｊ１ is a linear or branched saturated C １－６ Alkyl; and optionally -F, -OH, -OR ＪＪ -O-phenyl, -C(=O)OR ＪＪ Substituted with one or more elements selected from; Each -R Ｊ２ C ３－６ It is cycloalkyl; Each -R Ｊ３ These are independently non-aromatic C ３－７ It is a heterocycline; Each -R Ｊ４ is phenyl; and optionally -F, -OR ＪＪ , -NH ２ , and -NR ＪＪ ２ Substituted with one or more elements selected from; Each -R Ｊ５ C ５－６ It is a heteroaryl; Each -L Ｊ - is independently linear or branched saturated C １－４ It is an alkylene and optionally substituted with one or more -F groups; Each -R ＪＪ is a linear or branched saturated C １－４ It is alkyl; Here: -R Ｑ１ＮＫ ga-R Ｋ１ And, -R Ｋ２ And, -R Ｋ３ , -L Ｋ -R Ｋ３ And; -R Ｋ１ is a linear or branched saturated C １－７ Alkyl; and optionally -F, -OH, -OR ＫＫ , -OCH ２ CH ２ OCH ３ , and -NR ＫＫ ２ Substituted with one or more elements selected from; Each -R Ｋ２ C ３－６ It is cycloalkyl; Each -R Ｋ３ These are independently non-aromatic C ３－７ It is a heterocycline; and: Upon request, if available, secondary nitrogen, -R ＫＫ , and -C(=O)OR ＫＫ It is substituted with a group selected from; Each -L Ｋ - indicates a linear or branched saturated C １－４ It is alkylene Each -R ＫＫ is a linear or branched saturated C １－４ It is alkyl; Here: -R Ｑ１ＮＰ It has at least one N-ring atom, and C is bonded via the N-ring atom. ３－１１ It is a heterocycline; and: Carbon can be added as desired (-R) Ｑ１ＮＰＰ , -F, -OH, -OR Ｑ１ＮＰＰ Substituted with one or more groups selected from , and = O; and Upon request, if available, secondary nitrogen, -R Ｑ１ＮＰＰ And, -R Ｑ１ＮＰＰＸ , -C(=O)R Ｑ１ＮＰＰ , -C(=O)OR Ｑ１ＮＰＰ , -C(=O)NR Ｑ１ＮＰＰ ２ , and -S(=O) ２ R Ｑ１ＮＰＰ It is substituted with a group selected from; Each -R Ｑ１ＮＰＰ These independently form linear or branched saturated C １－４ Alkyl, C ３－６ Cycloalkyl, C ３－６ Cycloalkyl-C １－３ Alkyl, phenyl, where C １－４ The alkyl group can be -F, -OH, or -OCH as desired. ３ It has been replaced with; -R Ｑ１ＮＰＰＸ is a linear or branched saturated C １－４ It is a haloalkyl, Any compound according to claims 1 to 6 or a pharmaceutically acceptable salt or solvate thereof.

8. -Q is -Q ２ , or -L Ｑ２ - Q ２ And here Q ２ C ３－１０ It is a heterocycline; and: If desired, if present, the sulfur is substituted with one or two oxygen groups; If desired, and if present, add one or more secondary nitrogen atoms to the -R group. Ｑ２Ｎ It is replaced by; and -L Ｑ２ - indicates a linear or branched saturated C １－４ It is alkylene; Here Each -R Ｑ２Ｎ Independently: -R Ｑ２ＮＣ 、 =O、-C(=O)R Ｑ２ＮＣ 、 -C(=O)-L Ｑ２Ｎ -R Ｑ２ＮＭ 、 -C(=O)OR Ｑ２ＮＣ 、 -L Ｑ２Ｎ -C(=O)NR Ｑ２ＮＣ ２ ,or -S(=O) ２ R Ｑ２ＮＣ And; Here: Each -R Ｑ２ＮＣ These independently form linear or branched saturated C １－６ Alkyl, phenyl-C １－３ Alkyl, or C ５－６ Heteroaryl-C １－３ A compound that is alkyl, where C １－６ The alkyl group is optionally substituted with -OH, and each phenyl and heteroaryl group is optionally substituted with -Cl and -OCH ３ Substituted with one or more elements selected from; Each -L Ｑ２Ｎ - is independently linear or branched saturated C １－４ It is alkylene; Each -R Ｑ２ＮＭ Each element independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C ３－１１ It is a heterocycline. Any of claims 1 to 6, or a pharmaceutically acceptable salt or solvate thereof.

9. -Q is -Q ３ , or -L Ｑ３ - Q ３ And; Q ３ is phenyl; And, if desired, one or more bases-R Ｑ３Ｃ It is replaced by; and -L Ｑ３ - indicates a linear or branched saturated C １－４ It is alkylene, and: Each -R Ｑ３Ｃ Independently: -F, -R Ｑ３ＣＣ 、 -R Ｑ３ＣＸ 、 -OH、-OR Ｑ３ＣＣ 、 -NHC(=O)R Ｑ３ＣＣ 、 -C(=O)NHR Ｑ３ＣＣ 、-C(=O)R Ｑ３ＣＭ 、 -S(=O) ２ R Ｑ３ＣＣ 、S(=O) ２ R Ｑ３ＣＭ ; And; And the two adjacent -R Ｑ３Ｃ If it exists, then it will be united as -NH-(CH ２ ) ｑ３ C(O)(CH ２ ) ｖ３ -O- can be formed, where q3 is 0 and v3 is 1, Here: Each -R Ｑ３ＣＣ These independently form linear or branched saturated C １－４ Alkyl, C ３－６ Cycloalkyl, C ３－７ It is a heterocycline, and here, C １－４ The alkyl group is optionally substituted with -F; Each -R Ｑ３ＣＸ These independently form linear or branched saturated C １－４ It is a haloalkyl; Each -R Ｑ３ＣＭ Each element independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C ３－１１ It is a heterocycline; and: If desired, one or more carbon atoms in a group -R Ｑ３ＣＭＭ It has been replaced with; Each -R Ｑ３ＣＭＭ These are independently -F. Any compound according to claims 1 to 6 or a pharmaceutically acceptable salt or solvate thereof.

10. -Q is -Q ４ , or -L Ｑ４ - Q ４ And, Q ４ C ３－１０ It is a carbocycline; and -L Ｑ４ - indicates a linear or branched saturated C １－４ It is alkylene. Any compound according to claims 1 to 6 or a pharmaceutically acceptable salt or solvate thereof.

11. -Q is -Q ５ , or -H; Q ５ is a linear or branched saturated C １－６ It is alkyl; And, if desired, one or more bases-R Ｑ５Ｃ It has been replaced with; Here Each -R Ｑ５Ｃ Independently: -OH、-OR Ｑ５ＣＣ 、 -NHC(=O)R Ｑ５ＣＣ 、-NHC(=O)OR Ｑ５ＣＣ 、 -C(=O)NH ２ 、-C(=O)NHR Ｑ５ＣＣ 、-C(=O)R Ｑ５ＣＭ And here: Each -R Ｑ５ＣＣ These independently form linear or branched saturated C １－４ It is alkyl; Each -R Ｑ５ＣＭ Each element independently has at least one N-ring atom, and is bonded via the N-ring atom to a non-aromatic C ３－１１ It is a heterocycline. Any compound according to claims 1 to 6 or a pharmaceutically acceptable salt or solvate thereof.

12. A pharmaceutical composition comprising any compound according to claims 1 to 11, or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier or diluent.

13. A compound according to any of claims 1 to 11, or a pharmaceutically acceptable salt or solvate thereof, for use in a method of treating a human or animal body by therapeutic means.

14. Use of any compound according to claims 1 to 11, or a pharmaceutically acceptable salt or solvate thereof, in the manufacture of a pharmaceutical for treating proliferative disorders.

15. A method for treating a proliferative disorder of a human or animal body, comprising administering a therapeutically effective amount of any compound according to claims 1 to 11, or a pharmaceutically acceptable salt or solvate thereof, to a subject requiring treatment.

16. A compound, salt, or solvate for use in claim 14, or the method of claim 15, wherein the proliferative disorder is cancer.

17. A compound, salt, or solvate for use of claim 14, or the method of claim 15, wherein the proliferative disorder is: endometrial cancer, uterine cancer, ovarian cancer, breast cancer, gastric cancer, bladder cancer, pancreatic cancer, mesothelioma, kidney cancer, stomach cancer, esophageal cancer, colorectal cancer, glioblastoma, or lung cancer.

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