Novel functionalized lactams as serotonin receptor 7 modulators and methods of use thereof

Abstract

The pharmaceutical composition of the present invention comprises a functionalized lactam derivative having a disease ameliorating effect in the treatment of diseases associated with dysregulation of serotonin receptor 7 activity. # imgabs 0 # A selected from the group consisting of (groups): # imgabs 1 #

Description

[0001] Cross - Reference to Related Applications

[0002] This patent application is a divisional application of a Chinese patent application with application number 201980046137.1, filing date May 10, 2019, and invention title "Novel Functionalized Lactams as Serotonin Receptor 7 Modulators and Methods of Use Thereof". The original application is the Chinese national phase application of a PCT patent application with international application number PCT / US2019 / 031824, which claims the priority of a US provisional patent application No. 62 / 670,116 filed on May 11, 2018. The entire text of each of these patent applications is hereby incorporated by reference into this application.

[0003] Statement of Federally Sponsored Research

[0004] The United States Government has a paid - up license in this invention and in limited circumstances has the right to require the patent owner to license others on reasonable terms as provided by authorization numbers 143DK115254 - 01 granted by the National Institute of Diabetes and Digestive and Kidney Diseases and HHSN - 271 - 2008 - 00025 - C granted by the National Institute of Mental Health. Technical Field

[0005] Embodiments of the present invention relate to novel compounds useful as serotonin receptor 7 (5 - HT7) activity modulators and methods of use thereof. Embodiments also relate to entirely new chemical types that can be used to treat diseases associated with dysregulation of serotonin receptor 7 activity. Background Art

[0006] Serotonin was discovered in the late 1940s and is present in the peripheral and central nervous systems [Physiol. Res, 60(2011)15 - 25; Psychopharmacology 213(2011)167 - 169]. Serotonin or 5 - hydroxytryptamine (5 - HT) is a monoamine neurotransmitter of the indolealkylamine group that acts on the synapses of nerve cells. Seven different serotonin receptor families have been identified, and at least 20 subtypes have been cloned based on sequence similarity, signal transduction coupling, and pharmacological characteristics. The seven 5 - HT receptor families are named 5 - HT1, 5 - HT2, 5 - HT3, 5 - HT4, 5 - HT5, 5 - HT6, and 5 - HT7, and each of these receptors in turn has subfamilies or subtypes. The signal transduction mechanisms of all seven families have been studied, and activation of the 5 - HT1 and 5 - HT5 receptors is known to result in a decrease in intracellular cAMP, while activation of 5 - HT2, 5 - HT3, 5 - HT4, 5 - HT6, and 5 - HT7 results in an increase in intracellular IP3 and DAG. The 5 - HT pathway in the brain is an important target for drug development in the field of CNS diseases. The neurotransmitter binds to its G - protein - coupled receptors and is involved in a variety of effects, including cognition, mood, anxiety, attention, appetite, cardiovascular function, vasoconstriction, sleep (ACS Medicinal Chemistry Letters, 2011, 2, 929 - 932; Physiological Research, 2011, 60, 15 - 25), inflammatory bowel disease (IBD) and enteritis (WO2012058769, Khan, W.I. et al., Journal of Immunology, 2013, 190, 4795 - 4804), epilepsy, epileptic disorders (Epilepsy Research(2007)75, 39), drug addiction and alcohol addiction (Hauser, S.R. et al., Frontiers in Neuroscience, 2015, 8, 1 - 9), etc. SUMMARY OF THE INVENTION

[0007] The present invention relates to novel serotonin receptor 7 (5 - HT7) activity regulators, namely compounds of formula (I),

[0008]

[0009] including their enantiomers, diastereomers, hydrates, solvates, pharmaceutically acceptable salts, prodrugs, and complexes, wherein:

[0010] A is selected from the group consisting of consisting of;

[0011] R 1 is selected from hydrogen, C 1-6A linear alkyl group, C 3-7 A group consisting of branched alkyl groups;

[0012] R 2 Is selected from the group consisting of hydrogen, C 1-6 A linear alkyl group, C 3-7 A group consisting of branched alkyl groups;

[0013] Or R 1 And R 2 Together with the atoms to which they are bonded form a ring having 5 to 7 ring atoms, which ring optionally contains a double bond;

[0014] Or R 1 And R 2 Together with the atoms to which they are bonded form a ring having 6 to 8 ring atoms, which ring atoms contain a moiety selected from the group consisting of O, S, SO, SO2 and NR 7 Consisting of the group;

[0015] R 3 Is selected from the group consisting of an optionally substituted phenyl group, an optionally substituted naphthalen-1-yl group, an optionally substituted naphthalen-2-yl group, an optionally substituted 2-pyridyl group, an optionally substituted 3-pyridyl group, an optionally substituted 4-pyridyl group and Consisting of the group;

[0016] R 4 Is selected from the group consisting of an optionally substituted phenyl group, an optionally substituted naphthalen-1-yl group, an optionally substituted naphthalen-2-yl group, an optionally substituted 2-pyridyl group, an optionally substituted 3-pyridyl group, an optionally substituted 4-pyridyl group and Consisting of the group;

[0017] R 5 Is selected from the group consisting of an optionally substituted phenyl group, an optionally substituted naphthalen-1-yl group, an optionally substituted naphthalen-2-yl group, an optionally substituted 2-pyridyl group, an optionally substituted 3-pyridyl group, an optionally substituted 4-pyridyl group and Consisting of the group;

[0018] R 6 Is selected from the group consisting of an optionally substituted phenyl group, an optionally substituted naphthalen-1-yl group, an optionally substituted naphthalen-2-yl group, an optionally substituted 2-pyridyl group, an optionally substituted 3-pyridyl group and an optionally substituted 4-pyridyl group;

[0019] R 7 Is selected from the group consisting of H, C 1-6 A linear alkyl group, C 3-7 A branched alkyl group, C 3-7 A cycloalkyl group, an optionally substituted phenyl group, an optionally substituted benzyl group, COR 8 、CO2R 9 、CONR 10a R 10b, SO2NR 10a R 10b and SO2R 10c group;

[0020] R 8 is selected from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0021] R 9 is selected from the group consisting of C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0022] R 10a is selected from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0023] R 10b is selected from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0024] R 10c is selected from the group consisting of C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, -(CH2) q CN, -(CH2) q SO2R 11 , -(CH2) q OR 12 , group;

[0025] R 11 is selected from the group consisting of C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0026] R 12 is selected from the group consisting of C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0027] R1a , R 1b , R 1c , R 1d and R 1e is independently selected from the group consisting of H, OH, NO2, halogen, CN, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, -S(C 1-6 linear alkyl), S(C 3-7 branched alkyl), -S(C 3-7 cycloalkyl), COR 13 , CO2R 14 , CONR 15a R 15b , SO2NR 15a R 15b , NR 16a R 16b , NR 16a COR 17 , NR 16a SO2R 18 and NR 16a SO2NR 19a R 19b ;

[0028] R 13 is independently selected from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0029] R 14 is independently selected from the group consisting of C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0030] R 15a is independently selected from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0031] R 15b is independently selected from the group consisting of H, C 1-6Straight-chain alkyl, C 3-7 branched-chain alkyl, and C 3-7 cycloalkyl;

[0032] R 16a is independently selected, each time it appears, from the group consisting of H, C 1-6 straight-chain alkyl, C 3-7 branched-chain alkyl, and C 3-7 cycloalkyl;

[0033] R 16b is independently selected, each time it appears, from the group consisting of H, C 1-6 straight-chain alkyl, C 3-7 branched-chain alkyl, and C 3-7 cycloalkyl;

[0034] R 17 is independently selected, each time it appears, from the group consisting of H, C 1-6 straight-chain alkyl, C 3-7 branched-chain alkyl, and C 3-7 cycloalkyl;

[0035] R 18 is independently selected, each time it appears, from the group consisting of C 1-6 straight-chain alkyl, C 3-7 branched-chain alkyl, and C 3-7 cycloalkyl;

[0036] R 19a is independently selected, each time it appears, from the group consisting of C 1-6 straight-chain alkyl, C 3-7 branched-chain alkyl, and C 3-7 cycloalkyl;

[0037] R 19b is independently selected, each time it appears, from the group consisting of C 1-6 straight-chain alkyl, C 3-7 branched-chain alkyl, and C 3-7 cycloalkyl;

[0038] n is 1, 2, 3, or 4;

[0039] m is 1, 2, or 3.

[0040] In an embodiment, A is In an embodiment, n is 1, 2, or 3. In an embodiment, n is 1 or 2. In an embodiment, n is 1. In an embodiment, n is 2. In an embodiment, R 1 and R 2 each is unsubstituted C 1-6 alkyl (for example, R 1 and R 2 each is methyl, or R1 and R 2 each in (is ethyl). In an embodiment, R 1 and R 2 together with the atoms to which they are bonded form a 5- to 8-membered ring (e.g., C3-C8 cycloalkyl, C5-C8 cycloalkenyl, or a 5- to 8-membered ring containing the ring atom NR 7 . In an embodiment, R 1 and R 2 together with the atoms to which they are bonded form cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, cyclooctenyl, pyrrolidinyl, or piperidinyl, wherein the nitrogen atom in the pyrrolidinyl or piperidinyl is NR 7 . In an embodiment, R 7 is alkylsulfonyl -SO2R 10c (e.g., -SO2Me) or acyl -COR 8 (e.g., acetyl). In an embodiment, R 3 is phenyl or pyridinyl. In an embodiment, R 3 is unsubstituted. In an embodiment, R 3 is substituted (e.g., phenyl substituted with 1, 2, 3, 4, or 5 substituents or pyridinyl substituted with 1, 2, 3, or 4 substituents). In an embodiment, the substituents are selected from the group consisting of -OH, -F, -Cl, -Br, -I, -CN, -OMe, -OEt, -O n Pr, -O i Pr, -OCF3, -Me, -Et, - n Pr, - i Pr, -CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

[0041] In an embodiment, A is In an embodiment, n is 1, 2, or 3. In an embodiment, n is 1 or 2. In an embodiment, n is 1. In an embodiment, n is 2. In an embodiment, each of R 1 and R 2 is unsubstituted C 1-6 alkyl (e.g., each of R 1 and R 2 is methyl, or each of R 1 and R 2 is ethyl). In an embodiment, R 1 and R 2 together with the atoms to which they are bonded form a 5- to 8-membered ring (e.g., C3-C8 cycloalkyl, C5-C8 cycloalkenyl, or a 5- to 8-membered ring containing the ring atom NR 7with 5 to 8-membered rings). In an embodiment, R 1 and R 2 together with the atoms to which they are bonded form cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, cyclooctenyl, pyrrolidinyl or piperidinyl, wherein the nitrogen atom in the pyrrolidinyl or piperidinyl is NR 7 . In an embodiment, R 7 is alkylsulfonyl -SO2R 10c (e.g., -SO2Me) or acyl -COR 8 (e.g., acetyl). In an embodiment, R 4 is phenyl or pyridinyl. In an embodiment, R 4 is unsubstituted. In an embodiment, R 4 is substituted (e.g., phenyl substituted with 1, 2, 3, 4 or 5 substituents or pyridinyl substituted with 1, 2, 3 or 4 substituents). In an embodiment, the substituents are selected from the group consisting of -OH, -F, -Cl, -Br, -I, -CN, -OMe, -OEt, -O n Pr, -O i Pr, -OCF3, -Me, -Et, - n Pr, - i Pr, -CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl and morpholino.

[0042] In an embodiment, A is In an embodiment, n is 1, 2 or 3. In an embodiment, n is 1 or 2. In an embodiment, n is 1. In an embodiment, n is 2. In an embodiment, R 1 and R 2 each is unsubstituted C 1-6 alkyl (e.g., each of R 1 and R 2 is methyl, or each of R 1 and R 2 is ethyl). In an embodiment, R 1 and R 2 together with the atoms to which they are bonded form a 5 to 8-membered ring (e.g., C3 - C8 cycloalkyl, C5 - C8 cycloalkenyl or a 5 to 8-membered ring containing the ring atom NR 7 ). In an embodiment, R 1 and R 2 together with the atoms to which they are bonded form cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, cyclooctenyl, pyrrolidinyl or piperidinyl, wherein the nitrogen atom in the pyrrolidinyl or piperidinyl is NR 7。In an embodiment, R 7 is alkylsulfonyl - SO2R 10c (e.g., -SO2Me) or acyl - COR 8 (e.g., acetyl). In an embodiment, R 5 is phenyl or pyridyl. In an embodiment, R 5 is unsubstituted. In an embodiment, R 5 is substituted (e.g., phenyl substituted with 1, 2, 3, 4, or 5 substituents or pyridyl substituted with 1, 2, 3, or 4 substituents). In an embodiment, the substituents are selected from the group consisting of -OH, -F, -Cl, -Br, -I, -CN, -OMe, -OEt, -O n Pr, -O i Pr, -OCF3, -Me, -Et, - n Pr, - i Pr, -CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

[0043] In an embodiment, the compound is any of the formulas described herein or a pharmaceutically acceptable salt thereof. In an embodiment, the compound is any of the compounds described herein or a pharmaceutically acceptable salt thereof (e.g., the compounds described in any one of Tables 1 to 39 described herein or a pharmaceutically acceptable salt thereof). In an embodiment, the compound is any of the compounds described in any one of Tables 34 to 39 or a pharmaceutically acceptable salt thereof.

[0044] In an embodiment, the compound has the S configuration at the carbon substituted by the nitrogen of the lactam. In an embodiment, the compound has the R configuration at the carbon substituted by the nitrogen of the lactam.

[0045] The present invention also relates to a composition comprising:

[0046] an effective amount of one or more compounds according to the present invention and an excipient.

[0047] The present invention also relates to a method for treating or preventing a disease involving a disorder in the activity of serotonin receptor 7, said diseases including, for example, circadian rhythm disorders, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral vascular diseases, migraine, neuropathic pain, peripheral pain, allodynia, thermoregulatory disorders, learning disorders, memory disorders, hippocampal signal transduction disorders, sleep disorders, attention deficit / hyperactivity disorder, anxiety disorders, avoidant personality disorder, premature ejaculation, eating disorders, premenstrual syndrome, premenstrual dysphoric disorder, seasonal affective disorder, bipolar disorder, inflammatory bowel disease (IBD), enteritis, epilepsy, epileptic diseases, drug addiction, alcohol addiction, breast cancer, liver fibrosis, chronic liver injury, hepatocellular carcinoma, small intestinal neuroendocrine tumors, and lung injury, said method comprising administering to a subject an effective amount of a compound or composition according to the present invention.

[0048] The present invention also relates to a method for treating or preventing a disease involving a disorder in the activity of serotonin receptor 7, said diseases including, for example, circadian rhythm disorders, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral vascular diseases, migraine, neuropathic pain, peripheral pain, allodynia, thermoregulatory disorders, learning disorders, memory disorders, hippocampal signal transduction disorders, sleep disorders, attention deficit / hyperactivity disorder, anxiety disorders, avoidant personality disorder, premature ejaculation, eating disorders, premenstrual syndrome, premenstrual dysphoric disorder, seasonal affective disorder, bipolar disorder, inflammatory bowel disease (IBD), enteritis, epilepsy, epileptic diseases, drug addiction, alcohol addiction, breast cancer, liver fibrosis, chronic liver injury, hepatocellular carcinoma, small intestinal neuroendocrine tumors, and lung injury, wherein said method comprises administering to a subject a composition comprising an effective amount of one or more compounds according to the present invention and an excipient.

[0049] The present invention also relates to a method for treating or preventing a disease or disorder associated with circadian rhythm disorders, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral vascular diseases, migraine, neuropathic pain, peripheral pain, allodynia, thermoregulatory disorders, learning disorders, memory disorders, hippocampal signal transduction disorders, sleep disorders, attention deficit / hyperactivity disorder, anxiety disorders, avoidant personality disorder, premature ejaculation, eating disorders, premenstrual syndrome, premenstrual dysphoric disorder, seasonal affective disorder, bipolar disorder, inflammatory bowel disease (IBD), enteritis, epilepsy, epileptic diseases, drug addiction, alcohol addiction, breast cancer, liver fibrosis, chronic liver injury, hepatocellular carcinoma, small intestinal neuroendocrine tumors, and lung injury and diseases involving a disorder in the activity of serotonin receptor 7. The method comprises administering to a subject an effective amount of a compound or composition according to the present invention.

[0050] The present invention also relates to a method for treating or preventing a disease or disorder associated with circadian rhythm disorders, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral vascular disease, migraine, neuropathic pain, peripheral pain, allodynia, thermoregulatory disorders, learning disorders, memory disorders, hippocampal signal transduction disorders, sleep disorders, attention deficit / hyperactivity disorder, anxiety disorders, avoidant personality disorder, premature ejaculation, eating disorders, premenstrual syndrome, premenstrual dysphoric disorder, seasonal affective disorder, bipolar disorder, inflammatory bowel disease (IBD), enteritis, epilepsy, epileptic diseases, drug addiction, alcohol addiction, breast cancer, liver fibrosis, chronic liver injury, hepatocellular carcinoma, small intestinal neuroendocrine tumors and lung injury, and diseases associated with a dysregulation of 5-hydroxytryptamine receptor 7 activity, wherein the method comprises administering to a subject a composition comprising an effective amount of one or more compounds according to the invention and an excipient.

[0051] The present invention also relates to a method for treating or preventing a disease or disorder associated with a dysregulation of 5-hydroxytryptamine receptor 7 activity. The method comprises administering to a subject an effective amount of a compound or composition according to the invention.

[0052] The present invention also relates to a method for treating or preventing a disease or disorder associated with a dysregulation of 5-hydroxytryptamine receptor 7 activity, wherein the method comprises administering to a subject a composition comprising an effective amount of one or more compounds according to the invention and an excipient.

[0053] The present invention also relates to a method for preparing a 5-hydroxytryptamine receptor 7 activity modulator of the present invention.

[0054] In an embodiment, the disease or disorder is inflammatory bowel disease (IBD).

[0055] By reading the following detailed description and the appended claims, the above and other objects, features and advantages will become apparent to those of ordinary skill in the art. All percentages, ratios and proportions herein are by weight unless otherwise indicated. All temperatures are in degrees Celsius (°C) unless otherwise indicated. The relevant portions of all cited documents are incorporated herein by reference; the citation of any document should not be construed as an admission that it is prior art with respect to the present invention. Detailed Description

[0056] There is evidence of the role of the 5-HT7 receptor in a variety of medical disorders. Modulators of 5-HT7 receptor activity may have beneficial effects on patients suffering from these disorders. Disorders in which 5-HT7 dysregulation plays a role and in which modulation of 5-HT7 receptor activity by a therapeutic agent may be a viable approach to therapeutic relief include, but are not limited to, circadian rhythm disorders, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral vascular disease, migraine (Vanhoenacker, P. et al., Trends in Pharmacological Sciences, 2000, 21, 2, 70-77), neuropathic pain, nociceptive pain, allodynia (EP1875899), thermoregulatory disorders, learning disorders, memory disorders, hippocampal signal transduction disorders, sleep disorders (WO20100197700), attention deficit / hyperactivity disorder (ADHD) (WO20100069390), anxiety disorders, avoidant personality disorder, premature ejaculation, eating disorders, premenstrual syndrome, premenstrual dysphoric disorder, seasonal affective disorder, bipolar disorder (WO20040229874), inflammatory bowel disease (IBD), enteritis (WO 2012058769, Khan, W.I. et al., Journal of Immunology, 2013, 190, 4795-4804), epilepsy, epileptic disorders (Epilepsy Research (2007) 75, 39), drug addiction, alcohol addiction (Hauser, S.R. et al., Frontiers in Neuroscience, 2015, 8, 1-9), breast cancer (Gautam, J. Molecular Cancer, 2016, 15, 75, 1-14, Gautam, J. Breast Cancer Research and Treatment, 2017, 161, 29-40), liver fibrosis, chronic liver injury (Halici, Z. International Immunopharmacology, 2017, 43, 227-235), hepatocellular carcinoma (Bian, Z.X. Molecular Oncology, 2016, 10, 195-212), small intestinal neuroendocrine tumors (Modlin, I.M. Cancer Science, 2013, 104, 7, 844-855) and lung injury (Halici, Z. Immunology, 2013, 1271-1283).

[0057] Accordingly, there is a long-standing need for new 5-HT7 modulators that will provide therapeutic relief to patients suffering from disorders associated with dysregulation of 5-hydroxytryptamine receptor 7 activity. The present invention addresses the need for identifying novel 5-HT7 modulators capable of treating disorders associated with dysregulation of 5-hydroxytryptamine receptor 7 activity. The present invention addresses the need for developing new therapeutic agents for the treatment and prevention of circadian rhythm disorders, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral vascular disease, migraine, neuropathic pain, peripheral pain, allodynia, thermoregulatory disorders, learning disorders, memory disorders, hippocampal signaling disorders, sleep disorders, attention deficit / hyperactivity disorder, anxiety disorders, avoidant personality disorder, premature ejaculation, eating disorders, premenstrual syndrome, premenstrual dysphoric disorder, seasonal affective disorder, bipolar disorder, inflammatory bowel disease (IBD), enteritis, epilepsy, epileptic disorders, drug addiction, alcohol addiction, breast cancer, liver fibrosis, chronic liver injury, hepatocellular carcinoma, small intestinal neuroendocrine tumors, and lung injury.

[0058] The serotonin receptor 7 activity modulators of the present invention can treat and prevent diseases associated with disorders of serotonin receptor 7 activity, such as circadian rhythm disorders, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral vascular diseases, migraine, neuropathic pain, peripheral pain, allodynia, thermoregulatory disorders, learning disorders, memory disorders, hippocampal signal transduction disorders, sleep disorders, attention deficit / hyperactivity disorder, anxiety disorders, avoidant personality disorder, premature ejaculation, eating disorders, premenstrual syndrome, premenstrual dysphoric disorder, seasonal affective disorder, bipolar disorder, inflammatory bowel disease (IBD), enteritis, epilepsy, epileptic diseases, drug addiction, alcohol addiction, breast cancer, liver fibrosis, chronic liver injury, hepatocellular carcinoma, small intestinal neuroendocrine tumors, and lung injury. It has been found that serotonin receptor 7 plays a role in a variety of medical diseases. Therefore, 5-HT7 receptor activity modulators may have beneficial effects on patients suffering from these diseases.Diseases in which 5-HT7 dysregulation plays a role and modulating 5-HT7 receptor activity by a therapeutic agent may be a viable approach for therapeutic relief include, but are not limited to, circadian rhythm disorders, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral vascular disease, migraine (Vanhoenacker, P. et al., Trends in Pharmacological Sciences, 2000, 21, 2, 70-77), neuropathic pain, peripheral pain, allodynia (EP1875899), thermoregulatory disorders, learning disorders, memory disorders, hippocampal signal transduction disorders, sleep disorders (WO20100197700), attention deficit / hyperactivity disorder (ADHD) (WO20100069390), anxiety disorders, avoidant personality disorder, premature ejaculation, eating disorders, premenstrual syndrome, premenstrual dysphoric disorder, seasonal affective disorder, bipolar disorder (WO20040229874), inflammatory bowel disease (IBD), enteritis (WO 2012058769), epilepsy, epileptic disorders (Epilepsy Research (2007) 75, 39), drug addiction, alcohol addiction (Hauser, S.R. et al., Frontiers in Neuroscience, 2015, 8, 1-9), breast cancer (Gautam, J. Molecular Cancer, 2016, 15, 75, 1-14, Gautam, J. Breast Cancer Research and Treatment, 2017, 161, 29-40), liver fibrosis, chronic liver injury (Halici, Z. International Immunopharmacology, 2017, 43, 227-235), hepatocellular carcinoma (Bian, Z.X. Molecular Oncology, 2016, 10, 195-212), small intestinal neuroendocrine tumors (Modlin, I.M. Cancer Science, 2013, 104, 7, 844-855) and lung injury (Halici, Z. Immunology, 2013, 1271-1283).

[0059] Without wishing to be bound by theory, it is believed that the serotonin receptor 7 receptor activity modulators of the present invention can improve, alleviate, or otherwise enable the control of diseases associated with serotonin receptor 7 activity dysregulation. These diseases include, but are not limited to, circadian rhythm disorders, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral vascular disease, migraine, neuropathic pain, peripheral pain, allodynia, thermoregulatory disorders, learning disorders, memory disorders, hippocampal signal transduction disorders, sleep disorders, attention deficit / hyperactivity disorder, anxiety disorders, avoidant personality disorder, premature ejaculation, eating disorders, premenstrual syndrome, premenstrual dysphoric disorder, seasonal affective disorder, bipolar disorder, inflammatory bowel disease (IBD), enteritis, epilepsy, epileptic diseases, drug addiction, alcohol addiction, breast cancer, liver fibrosis, chronic liver injury, hepatocellular carcinoma, small intestinal neuroendocrine tumors, and lung injury.

[0060] In an embodiment, the disease is depression, schizophrenia, an anxiety disorder, or bipolar disorder. In an embodiment, the disease is depression. In an embodiment, the disease is schizophrenia. In an embodiment, the disease is an anxiety disorder. In an embodiment, the disease is bipolar disorder.

[0061] In an embodiment, the disease is attention deficit / hyperactivity disorder.

[0062] In an embodiment, the disease is avoidant personality disorder.

[0063] In an embodiment, the disease is seasonal affective disorder.

[0064] In an embodiment, the disease is a circadian rhythm disorder or a hippocampal signal transduction disorder. In an embodiment, the disease is a circadian rhythm disorder. In an embodiment, the disease is a hippocampal signal transduction disorder.

[0065] In an embodiment, the disease is neurogenic inflammation.

[0066] In an embodiment, the disease is neuropathic pain, peripheral pain, or allodynia. In an embodiment, the disease is neuropathic pain. In an embodiment, the disease is peripheral pain. In an embodiment, the disease is allodynia.

[0067] In an embodiment, the disease is migraine.

[0068] In an embodiment, the disease is epilepsy or epileptic diseases. In an embodiment, the disease is epilepsy. In an embodiment, the disease is epileptic diseases.

[0069] In an embodiment, the disease is a learning disorder or a memory disorder. In an embodiment, the disease is a learning disorder. In an embodiment, the disease is a memory disorder.

[0070] In an embodiment, the disease is an eating disorder.

[0071] In an embodiment, the disease is drug addiction or alcohol addiction.

[0072] In an embodiment, the disease is a sleep disorder.

[0073] In an embodiment, the disease is hypertension or peripheral vascular disease. In an embodiment, the disease is hypertension. In an embodiment, the disease is peripheral vascular disease.

[0074] In an embodiment, the disease is a thermoregulatory disorder.

[0075] In an embodiment, the disease is premature ejaculation.

[0076] In an embodiment, the disease is premenstrual syndrome or premenstrual dysphoric disorder. In an embodiment, the disease is premenstrual syndrome. In an embodiment, the disease is premenstrual dysphoric disorder.

[0077] In an embodiment, the disease is inflammatory bowel disease (IBD) or enteritis. In an embodiment, the disease is inflammatory bowel disease (IBD). In an embodiment, the disease is enteritis.

[0078] In an embodiment, the disease is breast cancer.

[0079] In an embodiment, the disease is liver fibrosis, chronic liver injury or hepatocellular carcinoma. In an embodiment, the disease is liver fibrosis. In an embodiment, the disease is chronic liver injury. In an embodiment, the disease is hepatocellular carcinoma.

[0080] In an embodiment, the disease is small intestinal neuroendocrine tumor.

[0081] In an embodiment, the disease is lung injury.

[0082] In an embodiment, the disease is inflammatory bowel disease (IBD).

[0083] In an embodiment, the compounds described herein are selective modulators of the serotonin 5HT7 receptor. In an embodiment, the compounds described herein can bind to the serotonin 5HT7 receptor more effectively compared to other targets (e.g., other serotonin receptors). In an embodiment, the compound can selectively bind to the serotonin 5HT7 receptor in a specific tissue or organ.

[0084] In embodiments, the compounds described herein can have particularly advantageous properties for effective treatment (e.g., treatment of any disease or disorder described herein). For example, in the treatment of CNS or mental disorders, the compounds described herein can exhibit favorable effective blood-brain barrier permeability. Alternatively, in the treatment of non-CNS or non-mental disorders, the compounds described herein will not have high blood-brain barrier permeability (e.g., off-target effects will be reduced). Without being bound by theory, the molecular elements of the compounds can be an effective strategy for obtaining the desired biological targeting.

[0085] For example, the compounds described herein can selectively bind to the serotonin 5HT7 receptor in the intestine of a subject. Accordingly, the compounds can be used to treat or prevent inflammatory bowel disease (IBD) or enteritis.

[0086] Throughout the specification, when a composition is described as having, including, or comprising a particular component, or when a method is described as having, including, or comprising a particular method step, it is contemplated that the compositions of the present teachings also consist essentially of or consist of the recited components, and the methods of the present teachings also consist essentially of or consist of the recited method steps.

[0087] In applications where an element or component is said to be included among the recited elements or components and / or selected from the recited elements or components, it should be understood that the element or component can be any one of the recited elements or components and can be selected from two or more of the recited elements or components.

[0088] Unless otherwise expressly stated, the use of the singular herein includes the plural (and vice versa). Additionally, when the term "about" is used before a quantitative value, unless otherwise expressly stated, the present teachings also include the specific quantitative value itself.

[0089] It should be understood that the order of steps or the order of performing certain acts is not important so long as the present teachings remain operable. Additionally, two or more steps or acts can be performed simultaneously.

[0090] As used herein, the term "halogen" shall mean chlorine, bromine, fluorine, and iodine.

[0091] As used herein, unless otherwise specified, "alkyl" and / or "aliphatic," whether used alone or as part of a substituent group, refer to straight-chain and branched-chain carbon chains having from 1 to 20 carbon atoms or any number within that range (e.g., from 1 to 6 carbon atoms or from 1 to 4 carbon atoms). The specified number of carbon atoms (e.g., C 1-6) shall independently refer to the number of carbon atoms in the alkyl moiety or to the number of carbon atoms in the alkyl moiety of a larger alkyl-containing substituent. Non-limiting examples of alkyl groups include methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, etc. The alkyl groups may be optionally substituted. Non-limiting examples of substituted alkyl groups include hydroxymethyl, chloromethyl, trifluoromethyl, aminomethyl, 1-chloroethyl, 2-hydroxyethyl, 1,2-difluoroethyl, 3-carboxypropyl, etc. In a substituent having multiple alkyl groups such as (C 1-6 alkyl)2amino, the alkyl groups may be the same or different.

[0092] As used herein, the terms "alkenyl" and "alkynyl" groups, whether used alone or as part of a substituent group, refer to straight-chain and branched-chain carbon chains having 2 or more, preferably 2 to 20 carbon atoms, wherein the alkenyl chain has at least one double bond in the chain and the alkynyl chain has at least one triple bond in the chain. The alkenyl and alkynyl groups may be optionally substituted. Non-limiting examples of alkenyl groups include vinyl, 3-propenyl, 1-propenyl (also 2-methylvinyl), isopropenyl (also 2-methylvinyl-2-yl), buten-4-yl, etc. Non-limiting examples of substituted alkenyl groups include 2-chloroethenyl (also 2-chloro vinyl), 4-hydroxybuten-1-yl, 7-hydroxy-7-methyloct-4-en-2-yl, 7-hydroxy-7-methyloct-3,5-dien-2-yl, etc. Non-limiting examples of alkynyl groups include ethynyl, prop-2-ynyl (also propargyl), propyn-1-yl, and 2-methyl-hex-4-yn-1-yl. Non-limiting examples of substituted alkynyl groups include 5-hydroxy-5-methylhex-3-ynyl, 6-hydroxy-6-methylhept-3-yn-2-yl, 5-hydroxy-5-ethylhept-3-ynyl, etc.

[0093] As used herein, "cycloalkyl", whether used alone or as part of another group, refers to a non-aromatic carbon-containing ring that includes, for example, cyclized alkyl, alkenyl, and alkynyl groups having 3 to 14 ring carbon atoms, preferably 3 to 7 or 3 to 6 ring carbon atoms, or even 3 to 4 ring carbon atoms, and optionally contains one or more (e.g., 1, 2, or 3) double bonds or triple bonds. The cycloalkyl group can be monocyclic (e.g., cyclohexyl) or polycyclic (e.g., containing fused, bridged, and / or spiro ring systems), where the carbon atoms are located inside or outside the ring system. Any suitable ring position of the cycloalkyl group can be covalently linked to the defined chemical structure. The cycloalkyl ring can be optionally substituted. Non-limiting examples of cycloalkyl groups include: cyclopropyl, 2-methyl-cyclopropyl, cyclopropenyl, cyclobutyl, 2,3-dihydroxycyclobutyl, cyclobutenyl, cyclopentyl, cyclopentenyl, cyclopentadienyl, cyclohexyl, cyclohexenyl, cycloheptyl, cyclooctyl, decahydronaphthyl, 2,5-dimethylcyclopentyl, 3,5-dichlorocyclohexyl, 4-hydroxycyclohexyl, 3,3,5-trimethylcyclohex-1-yl, octahydroazulenyl, octahydro-1H-indenyl, 3a,4,5,6,7,7a-hexahydro-3H-inden-4-yl, decahydroazulenyl; bicyclo[6.2.0]decyl, decahydronaphthyl, and dodecahydro-1H-fluorenyl. The term "cycloalkyl" also includes carbocyclic rings that are bicyclic hydrocarbons, non-limiting examples of which include bicyclo-[2.1.1]hexyl, bicyclo[2.2.1]heptyl, bicyclo[3.1.1]heptyl, 1,3-dimethyl[2.2.1]hept-2-yl, bicyclo[2.2.2]octyl, and bicyclo[3.3.3]undecyl.

[0094] "Haloalkyl" is intended to include branched and straight-chain saturated aliphatic hydrocarbon groups having a specified number of carbon atoms that are substituted with one or more halogens. Haloalkyl groups include perhaloalkyl groups in which all hydrogens of the alkyl group have been replaced by halogens (e.g., -CF3, -CF2CF3). In addition to halogens, haloalkyl can also be optionally substituted with one or more substituents. Examples of haloalkyl groups include, but are not limited to, fluoromethyl, dichloroethyl, trifluoromethyl, trichloromethyl, pentafluoroethyl, and pentachloroethyl groups.

[0095] The term "alkoxy" refers to the group -O-alkyl, where the alkyl group is as defined above. The alkoxy group can be optionally substituted. The term C3-C6 cycloalkoxy refers to a ring containing 3 to 6 carbon atoms and at least one oxygen atom (e.g., tetrahydrofuran, tetrahydro-2H-pyran). C3-C6 cycloalkoxy can be optionally substituted.

[0096] The term "haloalkoxy" refers to the group -O-haloalkyl, where the haloalkyl group is as defined above. Examples of haloalkoxy groups include, but are not limited to, fluoromethoxy, difluoromethoxy, trifluoromethoxy, and pentafluoroethoxy.

[0097] The term "aryl", used alone or as part of another group, is defined herein as an unsaturated aromatic monocyclic ring of 6 carbon members or an unsaturated aromatic polycyclic ring of 10 to 14 carbon members. The aryl ring can be, for example, a benzene ring or a naphthalene ring each optionally substituted with one or more moieties capable of substituting one or more hydrogen atoms. Non-limiting examples of aryl groups include: phenyl, naphthalen-1-yl, naphthalen-2-yl, 4-fluorophenyl, 2-hydroxyphenyl, 3-methylphenyl, 2-amino-4-fluorophenyl, 2-(N,N-diethylamino)phenyl, 2-cyanophenyl, 2,6-di-tert-butylphenyl, 3-methoxyphenyl, 8-hydroxynaphthalen-2-yl-4,5-dimethoxynaphthalen-1-yl, and 6-cyano-naphthalen-1-yl. The aryl group also includes, for example, a benzene ring or a naphthalene ring fused to one or more saturated or partially saturated carbocyclic rings (e.g., bicyclo[4.2.0]octa-1,3,5-trienyl, indanyl), which may be substituted at one or more carbon atoms of the aromatic ring and / or the saturated or partially saturated ring.

[0098] The term "arylalkyl" or "aralkyl" refers to the group -alkyl-aryl, where the alkyl and aryl groups are as defined herein. The aralkyl groups of the present invention are optionally substituted. Examples of aralkyl groups include, for example, benzyl, 1-phenylethyl, 2-phenylethyl, 3-phenylpropyl, 2-phenylpropyl, fluorenylmethyl, and the like.

[0099] The terms "heterocycle" and / or "heterocyclic group", whether used alone or as part of another group, are defined herein as one or more rings having 3 to 20 atoms, where at least one atom in at least one of the rings is a heteroatom selected from nitrogen (N), oxygen (O), or sulfur (S), and where the ring containing the heteroatom is non-aromatic. In a heterocyclic group containing 2 or more fused rings, the ring bearing no heteroatoms may be aryl (e.g., dihydroindolyl, tetrahydroquinolyl, chromanyl). Exemplary heterocyclic groups have 3 to 14 ring atoms, where 1 to 5 are independently selected from the heteroatoms nitrogen (N), oxygen (O), or sulfur (S). One or more N or S atoms in the heterocyclic group may be oxidized. The heterocyclic group may be optionally substituted.

[0100] Non-limiting examples of heterocyclic units having a single ring include: diaziridinyl, aziridinyl, urazolyl, azetidinyl, pyrazolidinyl, imidazolidinyl, oxazolidinyl, isoxazolinyl, isoxazolyl, thiazolidinyl, isothiazolyl, isothiazolinyl, oxathiazolidinone, oxazolidinone, hydantoin, tetrahydrofuryl, pyrrolidinyl, morpholinyl, piperazinyl, piperidinyl, dihydropyranyl, tetrahydropyranyl, piperidin-2-one (valerolactam), 2,3,4,5-tetrahydro-1H-azepinyl, 2,3-dihydro-1H-indole, and 1,2,3,4-tetrahydroquinoline. Non-limiting examples of heterocyclic units having two or more rings include: hexahydro-1H-pyrrolizinyl, 3a,4,5,6,7,7a-hexahydro-1H-benzo[d]imidazolyl, 3a,4,5,6,7,7a-hexahydro-1H-indolyl, 1,2,3,4-tetrahydroquinolinyl, chromanyl, isochromanyl, dihydroindolyl, isoindolinyl, and decahydro-1H-cycloocta[b]pyrrolyl.

[0101] The term "heteroaryl", whether used alone or as part of another group, is defined herein as one or more rings having from 5 to 20 atoms, wherein at least one atom in at least one of the rings is a heteroatom selected from nitrogen (N), oxygen (O), or sulfur (S), and wherein at least one of the rings containing a heteroatom is aromatic. In heteroaryl groups containing 2 or more fused rings, the ring bearing non-heteroatoms can be a carbocyclic ring (e.g., 6,7-dihydro-5H-cyclopenta[4,5]pyrimidine) or an aryl group (e.g., benzofuranyl, benzothienyl, indolyl). Exemplary heteroaryl groups have from 5 to 14 ring atoms and contain from 1 to 5 ring heteroatoms independently selected from nitrogen (N), oxygen (O), or sulfur (S). One or more N or S atoms in the heteroaryl group can be oxidized. The heteroaryl group can be substituted. Non-limiting examples of heteroaryl rings containing a single ring include: 1,2,3,4-tetrazolyl, [1,2,3]triazolyl, [1,2,4]triazolyl, triazinyl, thiazolyl, 1H-imidazolyl, oxazolyl, furanyl, thienyl, pyrimidinyl, 2-phenylpyrimidinyl, pyridyl, 3-methylpyridyl, and 4-dimethylaminopyridyl. Non-limiting examples of heteroaryl rings containing 2 or more fused rings include: benzofuranyl, benzothienyl, benzoxazolyl, benzothiazolyl, benzotriazolyl, cinnolinyl, naphthyridinyl, phenanthridinyl, 7H-purinyl, 9H-purinyl, 6-amino-9H-purinyl, 5H-pyrrolo[3,2-d]pyrimidinyl, 7H-pyrrolo[2,3-d]pyrimidinyl, pyrido[2,3-d]pyrimidinyl, 2-phenylbenzo[d]thiazolyl, 1H-indolyl, 4,5,6,7-tetrahydro-1-H-indolyl, quinoxalinyl, 5-methylquinoxalinyl, quinazolinyl, quinolinyl, 8-hydroxy-quinolinyl, 1H-benzo[d]imidazol-2(3H)-one, 1H-benzo[d]imidazolyl, and isoquinolinyl.

[0102] A non-limiting example of a heteroaryl group as described above is C1-C5 heteroaryl, which has from 1 to 5 carbocyclic ring atoms and at least one other ring atom that is a heteroatom independently selected from nitrogen (N), oxygen (O), or sulfur (S) (preferably from 1 to 4 other ring atoms as heteroatoms). Examples of C1-C5 heteroaryl include, but are not limited to, triazinyl, thiazol-2-yl, thiazol-4-yl, imidazol-1-yl, 1H-imidazol-2-yl, 1H-imidazol-4-yl, isoxazolin-5-yl, furan-2-yl, furan-3-yl, thiophene-2-yl, thiophene-4-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyridin-2-yl, pyridin-3-yl, and pyridin-4-yl.

[0103] Unless otherwise indicated, when two substituents together form a ring having a specified number of ring atoms (e.g., R 2 and R 3When taken together with the nitrogen (N) to which they are attached to form a ring having 3 to 7 ring members, the ring may have carbon atoms and optionally one or more (e.g., 1 to 3) additional heteroatoms independently selected from nitrogen (N), oxygen (O), or sulfur (S). The ring may be saturated or partially saturated and may optionally be substituted.

[0104] For the purposes of the present invention, fused ring units containing a single heteroatom, as well as spiro rings, bicyclics, etc. will be considered to belong to the cyclic family corresponding to the heteroatom-containing ring. For example, for the purposes of the present invention, 1,2,3,4-tetrahydroquinoline having the following formula:

[0105]

[0106] is considered a heterocyclic unit. For the purposes of the present invention, 6,7-dihydro-5H-cyclopenta[c]pyrimidine having the following formula:

[0107]

[0108] is considered a heteroaryl unit. When a fused ring unit contains heteroatoms in both a saturated ring and an aryl ring, the aryl ring will be dominant and determine the class type designated for the ring. For example, for the purposes of the present invention, 1,2,3,4-tetrahydro-[1,8]naphthyridine having the following formula:

[0109]

[0110] is considered a heteroaryl unit.

[0111] Whenever the term or any of its prefix roots appears in the name of a substituent, the name shall be interpreted to include those limitations provided herein. For example, whenever the term "alkyl" or "aryl" or any of their prefix roots appears in the name of a substituent (e.g., arylalkyl, alkylamino), the name shall be interpreted to include those limitations given above for "alkyl" and "aryl".

[0112] The term "substituted" is used throughout the specification. The term "substituted" as used herein is defined as a moiety, whether acyclic or cyclic, having one or more (e.g., 1 to 10) hydrogen atoms replaced by one or more substituents as defined hereinafter. A substituent can replace one or two hydrogen atoms of a single moiety at a time. Additionally, these substituents can replace two hydrogen atoms on two adjacent carbons to form the substituent, a new moiety or unit. For example, substituent units requiring replacement of a single hydrogen atom include halogen, hydroxy, etc. Replacement of two hydrogen atoms includes carbonyl, oxime, etc. Replacement of two hydrogen atoms from adjacent carbon atoms includes epoxy resin, etc. The term "substituted" is used throughout the specification to indicate that a moiety can have one or more hydrogen atoms replaced by substituents. When a moiety is described as "substituted", any number of hydrogen atoms can be replaced. For example, difluoromethyl is a substituted C1 alkyl; trifluoromethyl is a substituted C1 alkyl; 4-hydroxyphenyl is a substituted aromatic ring; (N,N-dimethyl-5-amino)octyl is a substituted C8 alkyl; 3-guanidinopropyl is a substituted C3 alkyl; and 2-carboxypyridyl is a substituted heteroaryl.

[0113] Variable groups as defined herein (e.g., alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, aryloxy, aryl, heterocycle and heteroaryl groups as defined herein), whether used alone or as part of another group, can optionally be substituted. Optionally substituted groups will be so indicated.

[0114] The following are non-limiting examples of substituents for hydrogen atoms on a substitutable moiety: halogen (chlorine (Cl), bromine (Br), fluorine (F) and iodine (I)), -CN, -NO2, oxygen (=O), -OR 26 , -SR 26 , -N(R 26 )2, -NR 26 C(O)R 26 , -SO2R 26 , -SO2OR 26 , -SO2N(R 26 )2, -C(O)R 26 , -C(O)OR 26 , -C(O)N(R 26 )2, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 alkoxy, C 2-8 alkenyl, C 2-8 alkynyl, C 3-14A cycloalkyl, aryl, heterocyclic or heteroaryl group, wherein each of the alkyl, haloalkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, aryl, heterocyclic and heteroaryl groups is optionally substituted with 1 to 10 (e.g., 1 to 6 or 1 to 4) groups independently selected from halogen, -CN, -NO2, oxygen and R 26 ; wherein R 26 is independently, each time it appears, hydrogen, -OR 27 , -SR 27 , -C(O)R 27 , -C(O)OR 27 , -C(O)N(R 27 )2, -SO2R 27 , -S(O)2OR 27 , -N(R 27 )2, -NR 27 C(O)R 27 , C 1-6 alkyl, C 1-6 haloalkyl, C 2-8 alkenyl, C 2-8 alkynyl, cycloalkyl (e.g., C 3-6 cycloalkyl), aryl, heterocyclic or heteroaryl, or two R 26 units together with the atoms to which they are attached form an optionally substituted carbocyclic or heterocyclic ring, wherein the carbocyclic or heterocyclic ring has 3 to 7 ring atoms; wherein R 27 is independently, each time it appears, hydrogen, C 1-6 alkyl, C 1-6 cycloalkyl, C 2-8 alkenyl, C 2-8 alkynyl, cycloalkyl (e.g., C 3-6 cycloalkyl), aryl, heterocyclic or heteroaryl, or two R 27 units together with the atoms to which they are attached form an optionally substituted carbocyclic or heterocyclic ring, wherein the carbocyclic or heterocyclic ring preferably has 3 to 7 ring atoms.

[0115] In some embodiments, the substituents are selected from

[0116] i) -OR 28 ; for example, -OH, -OCH3, -OCH2CH3, -OCH2CH2CH3;

[0117] ii) -C(O)R 28 ; for example, -COCH3, -COCH2CH3, -COCH2CH2CH3;

[0118] iii) -C(O)OR 28 ; for example, -CO2CH3, -CO2CH2CH3, -CO2CH2CH2CH3;

[0119] iv) - C(O)N(R 28 )2; for example, - CONH2, - CONHCH3, - CON(CH3)2;

[0120] v) - N(R 28 )2; for example, - NH2, - NHCH3, - N(CH3)2, - NH(CH2CH3);

[0121] vi) halogen: - F, - Cl, - Br and - I;

[0122] vii) - CH e X g ; where X is halogen, m is from 0 to 2, and e + g = 3; for example, - CH2F, - CHF2, - CF3, - CCl3 or - CBr3;

[0123] viii) - SO2R 28 ; for example, - SO2H, - SO2CH3, - SO2C6H5;

[0124] ix) C1 - C6 straight-chain, branched-chain or cyclic alkyl;

[0125] x) cyano;

[0126] xi) nitro;

[0127] xii) N(R 28 )C(O)R 28 ;

[0128] xiii) oxygen (=O);

[0129] xiv) heterocycle; and

[0130] xv) heteroaryl.

[0131] Where each R 28 is independently hydrogen, optionally substituted C1 - C6 straight-chain or branched-chain alkyl (for example, optionally substituted C1 - C4 straight-chain or branched-chain alkyl) or optionally substituted C3 - C6 cycloalkyl (for example, optionally substituted C3 - C4 cycloalkyl); or two R 28 units can combine together to form a ring containing 3 - 7 ring atoms. In certain aspects, each R 28 is independently hydrogen, C1 - C6 straight-chain or branched-chain alkyl optionally substituted by halogen or C3 - C6 cycloalkyl, or C3 - C6 cycloalkyl.

[0132] Throughout this specification, substituents of compounds are disclosed in groups or ranges. Specifically, the description includes every individual sub-combination of the members of these groups and ranges. For example, the term "C 1-6 alkyl" specifically intends to individually disclose C1, C2, C3, C4, C5, C6, C1-C6, C1-C5, C1-C4, C1-C3, C1-C2, C2-C6, C2-C5, C2-C4, C2-C3, C3-C6, C3-C5, C3-C4, C4-C6, C4-C5 and C5-C6 alkyls.

[0133] For the purposes of this invention, the terms "compound", "analogue" and "substance composition" also represent the serotonin receptor 7 activity modulators described herein, including all enantiomeric forms, diastereomeric forms, salts, etc., and the terms "compound", "analogue" and "substance composition" are used interchangeably in this specification.

[0134] The compounds described herein may contain asymmetric atoms (also known as chiral centers), and some compounds may contain one or more asymmetric atoms or centers, and thus may give rise to optical isomers (enantiomers) and diastereomers. The teachings and compounds disclosed herein include such enantiomers and diastereomers, as well as racemic and resolved enantiomerically pure R and S stereoisomers, and other mixtures of R and S stereoisomers and their pharmaceutically acceptable salts. Optical isomers can be obtained in pure form by standard procedures known to those skilled in the art, including but not limited to diastereomeric salt formation, kinetic resolution, and asymmetric synthesis. The teachings also cover cis and trans isomers of compounds containing alkenyl moieties (e.g., olefins and imines). It should also be understood that the teachings cover all possible regioisomers and their mixtures, which can be obtained in pure form by standard separation procedures known to those skilled in the art, including but not limited to column chromatography, thin layer chromatography, and high performance liquid chromatography.

[0135] Pharmaceutically acceptable salts of the compounds of the present teachings can be formed using organic and inorganic bases, which may have acidic moieties. Monoanionic and polyanionic salts are contemplated, depending on the number of acidic hydrogens available for deprotonation. Suitable salts formed with bases include metal salts such as alkali metal salts or alkaline earth metal salts, e.g., sodium, potassium or magnesium salts; ammonium salts and organic amine salts such as those with morpholine, thiomorpholine, piperidine, pyrrolidine, mono-, di- or tri-lower alkyl amines (e.g., ethyl-tert-butylamine, diethylamine, diisopropylamine, triethylamine, tributylamine or dimethylpropylamine), or mono-, di- or tri-hydroxy lower alkyl amines (e.g., monoethanolamine, diethanolamine or triethanolamine). Specific non-limiting examples of inorganic bases include NaHCO3, Na2CO3, KHCO3, K2CO3, Cs2CO3, LiOH, NaOH, KOH, NaH2PO4, Na2HPO4 and Na3PO4. Inner salts can also be formed. Similarly, when the compounds disclosed herein contain basic moieties, salts can be formed using organic and inorganic acids. For example, salts can be formed from the following acids: acetic acid, propionic acid, lactic acid, benzenesulfonic acid, benzoic acid, camphorsulfonic acid, citric acid, tartaric acid, succinic acid, dichloroacetic acid, vinylsulfonic acid, formic acid, fumaric acid, gluconic acid, glutamic acid, hippuric acid, hydrobromic acid, hydrochloric acid, isethionic acid, lactic acid, maleic acid, malic acid, malonic acid, mandelic acid, methanesulfonic acid, mucic acid, naphthalenesulfonic acid, nitric acid, oxalic acid, pamoic acid, pantothenic acid, phosphoric acid, phthalic acid, propionic acid, succinic acid, sulfuric acid, tartaric acid, toluenesulfonic acid and camphorsulfonic acid, and other known pharmaceutically acceptable acids.

[0136] When any variable occurs more than once in any component or any formula, its definition at each occurrence is independent of its definition at all other times (e.g., in N(R9)2, each R9 can be the same as or different from each other). Combinations of substituents and / or variables are permitted only if such combinations result in stable compounds.

[0137] As used herein, the term "treat" refers to partially or completely alleviating, inhibiting, ameliorating and / or relieving a condition suspected to be present in a patient.

[0138] As used herein, "therapeutically effective" and "effective dose" refer to a substance or amount that elicits a desired biological activity or effect.

[0139] Unless otherwise indicated, the terms "subject" or "patient" are used interchangeably and refer to mammals such as human patients and non-human primates, as well as laboratory animals such as rabbits, rats, and mice, and other animals. Thus, the term "subject" or "patient" as used herein means any mammalian patient or subject to whom the compounds of the invention can be administered. In one exemplary embodiment of the invention, to identify a subject patient to be treated according to the methods of the invention, accepted screening methods are employed to determine risk factors associated with a targeted or suspected disease or disorder or to determine the status of an existing disease or disorder in a subject. These screening methods include, for example, routine examinations to determine risk factors that may be associated with a targeted or suspected disease or disorder. These and other routine methods enable a clinician to select patients in need of treatment using the methods and compounds of the invention.

[0140] 5 - Hydroxytryptamine receptor 7 activity modulator

[0141] The present invention relates to novel 5 - hydroxytryptamine receptor 7 (5 - HT7) activity modulators, namely compounds of formula (I),

[0142]

[0143] including their enantiomers, diastereomers, hydrates, solvates, pharmaceutically acceptable salts, prodrugs, and complexes, wherein:

[0144] A is selected from the group consisting of ;

[0145] R 1 is selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl;

[0146] R 2 is selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl;

[0147] or R 1 and R 2 together with the atoms to which they are attached form a ring having 5 to 7 ring atoms, which ring optionally contains a double bond;

[0148] or R 1 and R 2 together with the atoms to which they are attached form a ring having 6 to 8 ring atoms, which ring atoms contain a moiety selected from the group consisting of O, S, SO, SO2, and NR 7 ;

[0149] R 3selected from the group consisting of optionally substituted phenyl, optionally substituted naphthalen-1-yl, optionally substituted naphthalen-2-yl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, optionally substituted 4-pyridyl, and the like;

[0150] R 4 selected from the group consisting of optionally substituted phenyl, optionally substituted naphthalen-1-yl, optionally substituted naphthalen-2-yl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, optionally substituted 4-pyridyl, and the like;

[0151] R 5 selected from the group consisting of optionally substituted phenyl, optionally substituted naphthalen-1-yl, optionally substituted naphthalen-2-yl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, optionally substituted 4-pyridyl, and the like;

[0152] R 6 selected from the group consisting of optionally substituted phenyl, optionally substituted naphthalen-1-yl, optionally substituted naphthalen-2-yl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, and optionally substituted 4-pyridyl;

[0153] R 7 selected from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, optionally substituted phenyl, optionally substituted benzyl, COR 8 、CO2R 9 、CONR 10a R 10b 、SO2NR 10a R 10b and SO2R 10c the like;

[0154] R 8 selected from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0155] R 9 selected from the group consisting of C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0156] R 10a selected from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0157] R 10b is selected from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0158] R 10c is selected from the group consisting of C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, -(CH2) q CN, -(CH2) q SO2R 11 、-(CH2) q OR 12 、 ;

[0159] R 11 is selected from the group consisting of C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0160] R 12 is selected from the group consisting of C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0161] R 1a 、R 1b 、R 1c 、R 1d 、and R 1e are each independently selected from the group consisting of H, OH, NO2, halogen, CN, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, -S(C 1-6 linear alkyl), S(C 3-7 branched alkyl), -S(C 3-7 cycloalkyl), COR 13 、CO2R14 , CONR 15a R 15b , SO2NR 15a R 15b , NR 16a R 16b , NR 16a , COR 17 , NR 16a , SO2R 18 and NR 16a , SO2NR 19a R 19b -constituted group;

[0162] R 13 is independently selected, each time it appears, from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0163] R 14 is independently selected, each time it appears, from the group consisting of C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0164] R 15a is independently selected, each time it appears, from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0165] R 15b is independently selected, each time it appears, from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0166] R 16a is independently selected, each time it appears, from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0167] R 16b is independently selected, each time it appears, from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0168] R 17 is independently selected, each time it appears, from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl, and C3-7 A group consisting of cycloalkyl;

[0169] R 18 independently at each occurrence selected from the group consisting of C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0170] R 19a independently at each occurrence selected from the group consisting of C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0171] R 19b independently at each occurrence selected from the group consisting of C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0172] n is 1, 2, 3, or 4;

[0173] m is 1, 2, or 3.

[0174] In an embodiment,

[0175] A is

[0176] each R 1 and R 2 independently is C 1-6 linear alkyl or C 3-7 branched alkyl; or R 1 and R 2 together with the atoms to which they are bonded form a 5- to 8-membered ring,

[0177] wherein the 5- to 8-membered ring is saturated or contains a carbon-carbon double bond and / or a ring atom O, S, SO, SO2, or NR 7 ;

[0178] each R 3 , R 4 and R 5 independently is an optionally substituted phenyl, an optionally substituted 2-pyridyl, an optionally substituted 3-pyridyl, or an optionally substituted 4-pyridyl;

[0179] R 6 independently is an optionally substituted phenyl, an optionally substituted 2-pyridyl, an optionally substituted 3-pyridyl, or an optionally substituted 4-pyridyl;

[0180] R 7 independently is H, C 1-6 linear alkyl, C3-7 branched alkyl, COR 8 or SO2R 10c ;

[0181] R 8 is selected from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0182] R 10c is C 1-6 linear alkyl or C 3-7 branched alkyl;

[0183] n is 1, 2, 3, or 4; and

[0184] m is 1, 2, or 3.

[0185] In an embodiment, n is 1, 2, or 3. In an embodiment, n is 1. In an embodiment, n is 2. In an embodiment, n is 3.

[0186] Embodiments of the invention include compounds having the formula (II):

[0187]

[0188] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes.

[0189] In an embodiment, the compound has the formula (XLII):

[0190] or a pharmaceutically acceptable salt thereof.

[0191] In an embodiment, the compound has the formula (XLIII):

[0192] or a pharmaceutically acceptable salt thereof.

[0193] In an embodiment, n is 1, 2, or 3. In an embodiment, n is 1. In an embodiment, n is 2. In an embodiment, n is 3. In an embodiment, n is 1 or 2.

[0194] In an embodiment, each of R 1 and R 2 is an unsubstituted C 1-6 alkyl. In an embodiment, each of R 1 and R 2 is ethyl. In an embodiment, each of R 1 and R 2 is methyl.

[0195] In an embodiment, R 1 and R 2 together with the atoms to which they are bonded form a 5- to 8-membered ring, which ring optionally contains a carbon-carbon double bond and / or ring atoms selected from the group consisting of O, S, SO, SO2, and NR 7 .

[0196] In an embodiment, R 1 and R 2 together with the atoms to which they are bonded form a C3-C8 cycloalkyl or a C5-C8 cycloalkenyl.

[0197] In an embodiment, R 1 and R 2 together with the atoms to which they are bonded form a C3-C8 cycloalkyl or a C5-C8 cycloalkenyl selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, and cyclooctenyl. In an embodiment, the C3-C8 cycloalkyl or C5-C8 cycloalkenyl is unsubstituted. In an embodiment, the C3-C8 cycloalkyl or C5-C8 cycloalkenyl is substituted with 1, 2, 3, or 4 substituents (e.g., 1 or 2 substituents as described herein). In an embodiment, the substituents are selected from oxygen (=O), hydroxy, halo, cyano, C 1-6 alkoxy, C 1-6 linear alkyl, C 3-7 branched alkyl, C 1-6 haloalkyl, C 3-8 cycloalkyl, and 3- to 8-membered heterocyclic groups. In an embodiment, the substituents are selected from the group consisting of -OH, -F, -Cl, -Br, -I, -CN, -OMe, -OEt, -O n Pr, -O i Pr, -OCF3, -Me, -Et, - n Pr, - i Pr, -CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

[0198] In an embodiment, the compound has a structure according to formula (XXXXIIIa):

[0199] or

[0200] a pharmaceutically acceptable salt thereof, wherein represents a single bond or a double bond.

[0201] In an embodiment, represents a single bond.

[0202] In an embodiment, represents a double bond.

[0203] In an embodiment, the lactam stereocenter substituted with nitrogen has an R-configuration.

[0204] In an embodiment, the lactam stereocenter substituted with nitrogen has an S-configuration.

[0205] In an embodiment, R 1 and R 2 together with the atoms to which they are bonded form a 5- to 8-membered ring containing the ring atom NR 7 . In an embodiment, the 5- to 8-membered ring is not further substituted. In an embodiment, the 5- to 8-membered ring further comprises 1, 2, 3, or 4 substituents (e.g., 1 or 2 substituents as described herein). In an embodiment, the substituents are selected from oxygen (=O), hydroxy, halo, cyano, C 1-6 alkoxy, C 1-6 straight-chain alkyl, C 3-7 branched-chain alkyl, C 1-6 haloalkyl, C 3-8 cycloalkyl, and 3- to 8-membered heterocycloalkyl. In an embodiment, the substituents are selected from the group consisting of -OH, -F, -Cl, -Br, -I, -CN, -OMe, -OEt, -O n Pr, -O i Pr, -OCF3, -Me, -Et, - n Pr, - i Pr, -CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

[0206] In an embodiment, R 1 and R 2 together form a pyrrolidinyl or piperidinyl group, wherein the nitrogen atom is NR 7 . In an embodiment, the pyrrolidinyl or piperidinyl group is not further substituted. In an embodiment, the pyrrolidinyl or piperidinyl group further comprises 1, 2, 3, or 4 substituents as described herein.

[0207] In an embodiment, the compound has formula (XLIIIb)

[0208] or a pharmaceutically acceptable salt thereof.

[0209] In an embodiment, the compound has formula (XLIV)

[0210] or a pharmaceutically acceptable salt thereof.

[0211] In an embodiment, the compound has formula (XLV)

[0212] or a pharmaceutically acceptable salt thereof.

[0213] In an embodiment, n is 1, 2, or 3. In an embodiment, n is 1. In an embodiment, n is 2. In an embodiment, n is 3. In an embodiment, n is 1 or 2.

[0214] In an embodiment, R 7 is COR 8 and R 8 is C 1-6 linear alkyl.

[0215] In an embodiment, R 7 is acetyl.

[0216] In an embodiment, R 7 is SO2R 10c and R 10c is C 1-6 linear alkyl.

[0217] In an embodiment, R 10c is methyl (i.e., R 7 is SO2Me).

[0218] In an embodiment, R 3 is unsubstituted phenyl.

[0219] In an embodiment, R 3 is substituted phenyl. In an embodiment, R 3 is phenyl substituted with 1, 2, 3, 4, or 5 substituents (e.g., phenyl substituted with 1 or 2 substituents as described herein). In an embodiment, the substituents are selected from the group consisting of hydroxyl, halogen, cyano, C 1-6 alkoxy, C 1-6 linear alkyl, C 3-7 branched alkyl, C 1-6 haloalkyl, C 3-8 cycloalkyl, and 3- to 8-membered heterocyclic group. In an embodiment, the substituents are selected from the group consisting of -OH, -F, -Cl, -Br, -I, -CN, -OMe, -OEt, -O n Pr, -O i Pr, -OCF3, -Me, -Et, - n Pr, - i Pr, -CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

[0220] In an embodiment, R 3 is selected from the group consisting of hydroxyphenyl, fluorophenyl, chlorophenyl, bromophenyl, cyanophenyl, tolyl, methoxyphenyl, difluorophenyl, dichlorophenyl, chlorofluorophenyl, dimethylphenyl, trifluoromethylphenyl, di(trifluoromethyl)phenyl.

[0221] In an embodiment, R 3 is selected from the group consisting of 4-hydroxyphenyl, 3-fluorophenyl, 4-fluorophenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 4-fluoro-3-chlorophenyl, 4-cyanophenyl, 2-methoxyphenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2-isopropylphenyl, 4-trifluoromethylphenyl, 2-morpholinophenyl, and 4-methyl-2-morpholinophenyl.

[0222] In an embodiment, R 3 is 2-pyridyl. In an embodiment, R 3 is 3-pyridyl. In an embodiment, R 3 is 4-pyridyl. In an embodiment, the pyridyl is unsubstituted. In an embodiment, the pyridyl is substituted with 1, 2, 3, or 4 substituents (e.g., the pyridyl is substituted with 1 or 2 substituents as described herein). In an embodiment, the substituents are selected from the group consisting of hydroxyl, halo, cyano, C 1-6 alkoxy, C 1-6 straight-chain alkyl, C 3-7 branched-chain alkyl, C 1-6 haloalkyl, C 3-8 cycloalkyl, and 3- to 8-membered heterocyclic group. In an embodiment, the substituents are selected from the group consisting of -OH, -F, -Cl, -Br, -I, -CN, -OMe, -OEt, -O n Pr, -O i Pr, -OCF3, -Me, -Et, - n Pr, - i Pr, -CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholinyl.

[0223] Embodiments of the present invention include compounds having formula (IIa):

[0224]

[0225] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[0226] R 20a 、R 20b 、R 20c 、R 20d and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 straight-chain alkyl, C 3-7 branched-chain alkyl, C 3-7 cycloalkyl, C 1-6 straight-chain alkoxy, C 3-7Branched alkoxy, C 3-7 Cycloalkoxy, C 1-6 Straight-chain haloalkyl, C 3-7 Branched haloalkyl, C 1-6 Straight-chain haloalkoxy, C 3-7 Branched haloalkoxy, SH, SC 1-6 Straight-chain alkyl, SC 3-7 Branched alkyl, SC 3-7 Cycloalkyl, SO2C 1-6 Straight-chain alkyl, SO2C 3-7 Branched alkyl, SO2C 3-7 Cycloalkyl, SO2NH2, SO2NHR 21 , NHSO2R 22 , -NR 23a R 23b , NHC(O)R 24 , C(O)NHR 24 , C(O)N(R 24 )2, morpholino and the group consisting of;

[0227] R 21 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0228] R 22 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0229] R 23a is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0230] R 23b is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0231] R 24 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0232] R25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence;

[0233] and at least three of R 20a , R 20b , R 20c , R 20d , and R 20e are hydrogen.

[0234] Embodiments of the invention include compounds having the formula (IIb):

[0235]

[0236] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[0237] Q 1 is 1 or 2;

[0238] and Q 2 is 1 or 2.

[0239] Embodiments of the invention include compounds having the formula (IIc):

[0240]

[0241] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[0242] Q 1 is 1 or 2;

[0243] and Q 2 is 1 or 2.

[0244] Embodiments of the invention include compounds having the formula (IId):

[0245]

[0246] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[0247] X 1 is selected from the group consisting of O, S, SO, SO2, and NR 7 ;

[0248] Q 1 is 1 or 2;

[0249] and Q 2 is 1 or 2.

[0250] Embodiments of the present invention include compounds having the formula (IId-1):

[0251]

[0252] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0253] Q 1 is 1 or 2;

[0254] and Q 2 is 1 or 2.

[0255] Embodiments of the present invention include compounds having the formula (IId-2):

[0256]

[0257] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0258] Q 1 is 1 or 2;

[0259] and Q 2 is 1 or 2.

[0260] Embodiments of the present invention include compounds having the formula (IId-3):

[0261]

[0262] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0263] Q 1 is 1 or 2;

[0264] and Q 2 is 1 or 2.

[0265] Embodiments of the present invention include compounds having the formula (IId-4):

[0266]

[0267] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0268] Q 1 is 1 or 2;

[0269] and Q 2 is 1 or 2.

[0270] Embodiments of the present invention include compounds having the formula (IId-5):

[0271]

[0272] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0273] Q 1 is 1 or 2;

[0274] and Q 2 is 1 or 2.

[0275] Embodiments of the present invention include compounds having the formula (IIe):

[0276]

[0277] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0278] R 20a R 20b R 20c and R 20d are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 NHSO2R 22 -NR 23a R 23b NHC(O)R 24 C(O)NHR 24 C(O)N(R 24 )2, morpholino and the group consisting thereof;

[0279] R 21 is independently selected from the group consisting of hydrogen, C 1-6Linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0280] R 22 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears;

[0281] R 23a is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears;

[0282] R 23b is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears;

[0283] R 24 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears;

[0284] R 25 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears;

[0285] and at least three of R 20a , R 20b , R 20c , and R 20d are hydrogen.

[0286] Embodiments of the invention include compounds having formula (IIf):

[0287]

[0288] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[0289] Q 1 is 1 or 2;

[0290] and Q 2 is 1 or 2.

[0291] Embodiments of the invention include compounds having formula (IIg):

[0292]

[0293] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0294] Q 1 is 1 or 2;

[0295] and Q 2 is 1 or 2.

[0296] Embodiments of the present invention include compounds having formula (IIh):

[0297]

[0298] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0299] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[0300] Q 1 is 1 or 2;

[0301] and Q 2 is 1 or 2.

[0302] Embodiments of the present invention include compounds having formula (IIh-1):

[0303]

[0304] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0305] Q 1 is 1 or 2;

[0306] and Q 2 is 1 or 2.

[0307] Embodiments of the present invention include compounds having formula (IIh-2):

[0308]

[0309] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0310] Q 1 is 1 or 2;

[0311] and Q 2 is 1 or 2.

[0312] Embodiments of the present invention include compounds having the formula (IIh-3):

[0313]

[0314] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0315] Q 1 is 1 or 2;

[0316] and Q 2 is 1 or 2.

[0317] Embodiments of the present invention include compounds having the formula (IIh-4):

[0318]

[0319] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0320] Q 1 is 1 or 2;

[0321] and Q 2 is 1 or 2.

[0322] Embodiments of the present invention include compounds having the formula (IIh-5):

[0323]

[0324] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0325] Q 1 is 1 or 2;

[0326] and Q 2 is 1 or 2.

[0327] Embodiments of the present invention include compounds having the formula (IIi):

[0328]

[0329] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0330] R 20a 、R 20b 、R 20c and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 , NHSO2R 22 , -NR 23a R 23b , NHC(O)R 24 , C(O)NHR 24 , C(O)N(R 24 )2, morpholino and the group consisting of;

[0331] R 21 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0332] R 22 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0333] R 23a is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0334] R 23b is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0335] R 24 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C3-7 A group consisting of cycloalkyl;

[0336] R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears;

[0337] and at least two of R 20a , R 20b , R 20c and R 20e are hydrogen.

[0338] Embodiments of the present invention include compounds having the formula (IIj):

[0339]

[0340] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0341] Q 1 is 1 or 2;

[0342] and Q 2 is 1 or 2.

[0343] Embodiments of the present invention include compounds having the formula (IIk):

[0344]

[0345] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0346] Q 1 is 1 or 2;

[0347] and Q 2 is 1 or 2.

[0348] Embodiments of the present invention include compounds having the formula (IIL):

[0349]

[0350] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0351] X 1 is selected from the group consisting of O, S, SO, SO2, and NR 7 ;

[0352] Q 1 is 1 or 2;

[0353] and Q2 is 1 or 2.

[0354] Embodiments of the present invention include compounds having the formula (IIL-1):

[0355]

[0356] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0357] Q 1 is 1 or 2;

[0358] and Q 2 is 1 or 2.

[0359] Embodiments of the present invention include compounds having the formula (IIL-2):

[0360]

[0361] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0362] Q 1 is 1 or 2;

[0363] and Q 2 is 1 or 2.

[0364] Embodiments of the present invention include compounds having the formula (IIL-3):

[0365]

[0366] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0367] Q 1 is 1 or 2;

[0368] and Q 2 is 1 or 2.

[0369] Embodiments of the present invention include compounds having the formula (IIL-4):

[0370]

[0371] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0372] Q 1 is 1 or 2;

[0373] and Q 2 is 1 or 2.

[0374] Embodiments of the present invention include compounds having the formula (IIL-5):

[0375]

[0376] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0377] Q 1 is 1 or 2;

[0378] and Q 2 is 1 or 2.

[0379] Embodiments of the present invention include compounds having the formula (IIm):

[0380]

[0381] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0382] R 20a 、R 20b 、R 20cd and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of;

[0383] R 21independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears;

[0384] R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears;

[0385] R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears;

[0386] R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears;

[0387] R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears;

[0388] R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears;

[0389] and at least three of R 20a , R 20b , R 20c and R 20d are hydrogen.

[0390] Embodiments of the present invention include compounds having the formula (IIn):

[0391]

[0392] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0393] Q 1 is 1 or 2;

[0394] and Q 2 is 1 or 2.

[0395] Embodiments of the present invention include compounds having the formula (IIo):

[0396]

[0397] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0398] Q 1 is 1 or 2;

[0399] and Q 2 is 1 or 2.

[0400] Embodiments of the present invention include compounds having the formula (IIp):

[0401]

[0402] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0403] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[0404] Q 1 is 1 or 2;

[0405] and Q 2 is 1 or 2.

[0406] Embodiments of the present invention include compounds having the formula (IIp-1):

[0407]

[0408] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0409] Q 1 is 1 or 2;

[0410] and Q 2 is 1 or 2.

[0411] Embodiments of the present invention include compounds having the formula (IIp-2):

[0412]

[0413] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0414] Q 1 is 1 or 2;

[0415] and Q2 is 1 or 2.

[0416] Embodiments of the invention include compounds having the formula (IIp-3):

[0417]

[0418] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[0419] Q 1 is 1 or 2;

[0420] and Q 2 is 1 or 2.

[0421] Embodiments of the invention include compounds having the formula (IIp-4):

[0422]

[0423] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[0424] Q 1 is 1 or 2;

[0425] and Q 2 is 1 or 2.

[0426] Embodiments of the invention include compounds having the formula (IIp-5):

[0427]

[0428] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[0429] Q 1 is 1 or 2;

[0430] and Q 2 is 1 or 2.

[0431] Embodiments of the invention include compounds having the formula (IIq):

[0432]

[0433] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[0434] R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R20g Independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 , NHSO2R 22 , -NR 23a R 23b , NHC(O)R 24 , C(O)NHR 24 , C(O)N(R 24 )2, morpholino and the group consisting of;

[0435] R 21 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0436] R 22 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0437] R 23a is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0438] R 23b is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0439] R 24 is independently selected, at each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0440] R 25 is independently selected, at each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0441] and at least five of R 20a , R 20b , R 20c , R 20d , R 20e , R 20f , and R 20g are hydrogen.

[0442] Embodiments of the invention include compounds having the formula (IIr):

[0443]

[0444] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[0445] Q 1 is 1 or 2;

[0446] and Q 2 is 1 or 2.

[0447] Embodiments of the invention include compounds having the formula (IIs):

[0448]

[0449] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[0450] Q 1 is 1 or 2;

[0451] and Q 2 is 1 or 2.

[0452] Embodiments of the invention include compounds having the formula (IIt):

[0453]

[0454] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[0455] X 1 is selected from the group consisting of O, S, SO, SO2, and NR 7 ;

[0456] Q 1 is 1 or 2;

[0457] and Q 2 is 1 or 2.

[0458] Embodiments of the invention include compounds having the formula (IIt-1):

[0459]

[0460] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[0461] Q 1 is 1 or 2;

[0462] and Q 2 is 1 or 2.

[0463] Embodiments of the invention include compounds having the formula (IIt-2):

[0464]

[0465] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[0466] Q 1 is 1 or 2;

[0467] and Q 2 is 1 or 2.

[0468] Embodiments of the invention include compounds having the formula (IIt-3):

[0469]

[0470] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[0471] Q 1 is 1 or 2;

[0472] and Q 2 is 1 or 2.

[0473] Embodiments of the invention include compounds having the formula (IIt-4):

[0474]

[0475] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0476] Q 1 is 1 or 2;

[0477] and Q 2 is 1 or 2.

[0478] Embodiments of the present invention include compounds having the formula (IIt-5):

[0479]

[0480] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0481] Q 1 is 1 or 2;

[0482] and Q 2 is 1 or 2.

[0483] Embodiments of the present invention include compounds having the formula (IIu):

[0484]

[0485] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0486] R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7Naphthenyl, SO2NH2, SO2NHR 21 , NHSO2R 22 , -NR 23a R 23b , NHC(O)R 24 , C(O)NHR 24 , C(O)N(R 24 )2, morpholino and the group consisting of;

[0487] R 21 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 naphthenyl each time it appears;

[0488] R 22 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 naphthenyl each time it appears;

[0489] R 23a is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 naphthenyl each time it appears;

[0490] R 23b is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 naphthenyl each time it appears;

[0491] R 24 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 naphthenyl each time it appears;

[0492] R 25 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 naphthenyl each time it appears;

[0493] and at least 5 of R 20a , R 20b , R 20c , R 20d , R 20e , R 20f and R 20g are hydrogen.

[0494] Embodiments of the present invention include compounds having formula (IIv):

[0495]

[0496] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0497] Q 1 is 1 or 2;

[0498] and Q 2 is 1 or 2.

[0499] Embodiments of the present invention include compounds having formula (IIw):

[0500]

[0501] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0502] Q 1 is 1 or 2;

[0503] and Q 2 is 1 or 2.

[0504] Embodiments of the present invention include compounds having formula (IIx):

[0505]

[0506] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0507] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[0508] Q 1 is 1 or 2;

[0509] and Q 2 is 1 or 2.

[0510] Embodiments of the present invention include compounds having formula (IIx-1):

[0511]

[0512] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0513] Q 1 is 1 or 2;

[0514] and Q 2 is 1 or 2.

[0515] Embodiments of the present invention include compounds having the formula (IIx-2):

[0516]

[0517] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0518] Q 1 is 1 or 2;

[0519] and Q 2 is 1 or 2.

[0520] Embodiments of the present invention include compounds having the formula (IIx-3):

[0521]

[0522] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0523] Q 1 is 1 or 2;

[0524] and Q 2 is 1 or 2.

[0525] Embodiments of the present invention include compounds having the formula (IIx-4):

[0526]

[0527] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0528] Q 1 is 1 or 2;

[0529] and Q 2 is 1 or 2.

[0530] Embodiments of the present invention include compounds having the formula (IIx-5):

[0531]

[0532] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0533] Q 1 is 1 or 2;

[0534] and Q 2 is 1 or 2.

[0535] Embodiments of the present invention include compounds having the formula (III):

[0536]

[0537] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes.

[0538] Embodiments of the present invention include compounds having the formula (IIIa):

[0539]

[0540] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[0541] R 20a 、R 20b 、R 20c 、R 20d and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino, and the group consisting of;

[0542] R 21 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C3-7 A group consisting of cycloalkyl;

[0543] R 22 independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0544] R 23a independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0545] R 23b independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0546] R 24 independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0547] R 25 independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0548] and at least three of R 20a , R 20b , R 20c , R 20d and R 20e are hydrogen.

[0549] Embodiments of the present invention include compounds having the formula (IIIb):

[0550]

[0551] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[0552] Q 1 is 1 or 2;

[0553] and Q 2 is 1 or 2.

[0554] Embodiments of the present invention include compounds having the formula (IIIc):

[0555]

[0556] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0557] Q 1 is 1 or 2;

[0558] and Q 2 is 1 or 2.

[0559] Embodiments of the present invention include compounds having formula (IIId):

[0560]

[0561] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0562] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[0563] Q 1 is 1 or 2;

[0564] and Q 2 is 1 or 2.

[0565] Embodiments of the present invention include compounds having formula (IIId-1):

[0566]

[0567] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0568] Q 1 is 1 or 2;

[0569] and Q 2 is 1 or 2.

[0570] Embodiments of the present invention include compounds having formula (IIId-2):

[0571]

[0572] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0573] Q 1 is 1 or 2;

[0574] and Q 2 is 1 or 2.

[0575] Embodiments of the present invention include compounds having the formula (IIId-3):

[0576]

[0577] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0578] Q 1 is 1 or 2;

[0579] and Q 2 is 1 or 2.

[0580] Embodiments of the present invention include compounds having the formula (IIId-4):

[0581]

[0582] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0583] Q 1 is 1 or 2;

[0584] and Q 2 is 1 or 2.

[0585] Embodiments of the present invention include compounds having the formula (IIId-5):

[0586]

[0587] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0588] Q 1 is 1 or 2;

[0589] and Q 2 is 1 or 2.

[0590] Embodiments of the present invention include compounds having the formula (IIIe):

[0591]

[0592] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0593] R 20a 、R 20b 、R 20c and R 20d are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C3-7 Cycloalkyl, C 1-6 Linear alkoxy, C 3-7 Branched alkoxy, C 3-7 Cycloalkoxy, C 1-6 Linear haloalkyl, C 3-7 Branched haloalkyl, C 1-6 Linear haloalkoxy, C 3-7 Branched haloalkoxy, SH, SC 1-6 Linear alkyl, SC 3-7 Branched alkyl, SC 3-7 Cycloalkyl, SO2C 1-6 Linear alkyl, SO2C 3-7 Branched alkyl, SO2C 3-7 Cycloalkyl, SO2NH2, SO2NHR 21 , NHSO2R 22 , -NR 23a R 23b , NHC(O)R 24 , C(O)NHR 24 , C(O)N(R 24 )2, morpholino and the group consisting of;

[0594] R 21 independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0595] R 22 independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0596] R 23a independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0597] R 23b independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0598] R 24 independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C3-7 A group consisting of cycloalkyl;

[0599] R 25 which is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0600] and at least two of R 20a , R 20b , R 20c and R 20d are hydrogen.

[0601] Embodiments of the present invention include compounds having formula (IIIf):

[0602]

[0603] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[0604] Q 1 is 1 or 2;

[0605] and Q 2 is 1 or 2.

[0606] Embodiments of the present invention include compounds having formula (IIIg):

[0607]

[0608] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[0609] Q 1 is 1 or 2;

[0610] and Q 2 is 1 or 2.

[0611] Embodiments of the present invention include compounds having formula (IIIh):

[0612]

[0613] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[0614] X 1 is selected from the group consisting of O, S, SO, SO2, and NR 7 ;

[0615] Q 1 is 1 or 2;

[0616] And Q 2 is 1 or 2.

[0617] Embodiments of the present invention include compounds having the formula (IIIh-1):

[0618]

[0619] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0620] Q 1 is 1 or 2;

[0621] And Q 2 is 1 or 2.

[0622] Embodiments of the present invention include compounds having the formula (IIIh-2):

[0623]

[0624] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0625] Q 1 is 1 or 2;

[0626] And Q 2 is 1 or 2.

[0627] Embodiments of the present invention include compounds having the formula (IIIh-3):

[0628]

[0629] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0630] Q 1 is 1 or 2;

[0631] And Q 2 is 1 or 2.

[0632] Embodiments of the present invention include compounds having the formula (IIIh-4):

[0633]

[0634] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0635] Q 1 is 1 or 2;

[0636] And Q 2 is 1 or 2.

[0637] Embodiments of the present invention include compounds having the formula (IIIh-5):

[0638]

[0639] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes thereof, wherein

[0640] Q 1 is 1 or 2;

[0641] and Q 2 is 1 or 2.

[0642] Embodiments of the present invention include compounds having the formula (IIIi):

[0643]

[0644] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes thereof, wherein

[0645] R 20a 、R 20b 、R 20c and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of;

[0646] R 21 is independently selected, at each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0647] R 22 is independently selected, at each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0648] R 23a is independently selected, at each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0649] R 23b is independently selected, at each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0650] R 24 is independently selected, at each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0651] R 25 is independently selected, at each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0652] and at least two of R 20a , R 20b , R 20c and R 20e are hydrogen.

[0653] Embodiments of the present invention include compounds having the formula (IIIj):

[0654]

[0655] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0656] Q 1 is 1 or 2;

[0657] and Q 2 is 1 or 2.

[0658] Embodiments of the present invention include compounds having the formula (IIIk):

[0659]

[0660] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0661] Q 1 is 1 or 2;

[0662] and Q 2 is 1 or 2.

[0663] Embodiments of the present invention include compounds having the formula (IIIL):

[0664]

[0665] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0666] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[0667] Q 1 is 1 or 2;

[0668] and Q 2 is 1 or 2.

[0669] Embodiments of the present invention include compounds having the formula (IIIL-1):

[0670]

[0671] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0672] Q 1 is 1 or 2;

[0673] and Q 2 is 1 or 2.

[0674] Embodiments of the present invention include compounds having the formula (IIIL-2):

[0675]

[0676] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0677] Q 1 is 1 or 2;

[0678] and Q 2 is 1 or 2.

[0679] Embodiments of the present invention include compounds having the formula (IIIL-3):

[0680]

[0681] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0682] Q 1 is 1 or 2;

[0683] and Q 2 is 1 or 2.

[0684] Embodiments of the present invention include compounds having the formula (IIIL-4):

[0685]

[0686] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0687] Q 1 is 1 or 2;

[0688] and Q 2 is 1 or 2.

[0689] Embodiments of the present invention include compounds having the formula (IIIL-5):

[0690]

[0691] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0692] Q 1 is 1 or 2;

[0693] and Q 2 is 1 or 2.

[0694] Embodiments of the present invention include compounds having the formula (IIIm):

[0695]

[0696] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0697] R 20a 、R 20b 、R 20d and R 20eIndependently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 , NHSO2R 22 , -NR 23a R 23b , NHC(O)R 24 , C(O)NHR 24 , C(O)N(R 24 )2, morpholino and a group consisting of;

[0698] R 21 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence;

[0699] R 22 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence;

[0700] R 23a is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence;

[0701] R 23b is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence;

[0702] R24 is independently selected, at each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0703] R 25 is independently selected, at each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0704] and R 20a , R 20b , R 20c , and R 20d and at least two of R

[0705] Embodiments of the present invention include compounds having the formula (IIIn):

[0706]

[0707] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[0708] Q 1 is 1 or 2;

[0709] and Q 2 is 1 or 2.

[0710] Embodiments of the present invention include compounds having the formula (IIIo):

[0711]

[0712] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[0713] Q 1 is 1 or 2;

[0714] and Q 2 is 1 or 2.

[0715] Embodiments of the present invention include compounds having the formula (IIIp):

[0716]

[0717] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[0718] X 1 is selected from the group consisting of O, S, SO, SO2, and NR 7 ;

[0719] Q 1 is 1 or 2;

[0720] and Q 2 is 1 or 2.

[0721] Embodiments of the invention include compounds having the formula (IIIp-1):

[0722]

[0723] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0724] Q 1 is 1 or 2;

[0725] and Q 2 is 1 or 2.

[0726] Embodiments of the invention include compounds having the formula (IIIp-2):

[0727]

[0728] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0729] Q 1 is 1 or 2;

[0730] and Q 2 is 1 or 2.

[0731] Embodiments of the invention include compounds having the formula (IIIp-3):

[0732]

[0733] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0734] Q 1 is 1 or 2;

[0735] and Q 2 is 1 or 2.

[0736] Embodiments of the invention include compounds having the formula (IIIp-4):

[0737]

[0738] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0739] Q 1is 1 or 2;

[0740] and Q 2 is 1 or 2.

[0741] Embodiments of the invention include compounds having the formula (IIIp-5):

[0742]

[0743] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0744] Q 1 is 1 or 2;

[0745] and Q 2 is 1 or 2.

[0746] Embodiments of the invention include compounds having the formula (IIIq):

[0747]

[0748] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0749] R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b, NHC(O)R 24 , C(O)NHR 24 , C(O)N(R 24 )2, morpholino and the group consisting of;

[0750] R 21 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears;

[0751] R 22 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears;

[0752] R 23a is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears;

[0753] R 23b is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears;

[0754] R 24 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears;

[0755] R 25 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears;

[0756] and at least 5 of R 20a , R 20b , R 20c , R 20d , R 20e , R 20f and R 20g are hydrogen.

[0757] Embodiments of the present invention include compounds having formula (IIIr):

[0758]

[0759] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0760] Q 1 is 1 or 2;

[0761] and Q 2 is 1 or 2.

[0762] Embodiments of the present invention include compounds having the formula (IIIs):

[0763]

[0764] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0765] Q 1 is 1 or 2;

[0766] and Q 2 is 1 or 2.

[0767] Embodiments of the present invention include compounds having the formula (IIIt):

[0768]

[0769] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0770] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[0771] Q 1 is 1 or 2;

[0772] and Q 2 is 1 or 2.

[0773] Embodiments of the present invention include compounds having the formula (IIIt-1):

[0774]

[0775] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0776] Q 1 is 1 or 2;

[0777] and Q 2 is 1 or 2.

[0778] Embodiments of the present invention include compounds having the formula (IIIt-2):

[0779]

[0780] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0781] Q 1 is 1 or 2;

[0782] and Q 2 is 1 or 2.

[0783] Embodiments of the present invention include compounds having formula (IIIt-3):

[0784]

[0785] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0786] Q 1 is 1 or 2;

[0787] and Q 2 is 1 or 2.

[0788] Embodiments of the present invention include compounds having formula (IIIt-4):

[0789]

[0790] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0791] Q 1 is 1 or 2;

[0792] and Q 2 is 1 or 2.

[0793] Embodiments of the present invention include compounds having formula (IIIt-5):

[0794]

[0795] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0796] Q 1 is 1 or 2;

[0797] and Q 2 is 1 or 2.

[0798] Embodiments of the present invention include compounds having formula (IIIu):

[0799]

[0800] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0801] R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of;

[0802] R 21 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears;

[0803] R 22 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears;

[0804] R 23a is independently selected from the group consisting of hydrogen, C 1-6Straight-chain alkyl, C 3-7 branched-chain alkyl, and C 3-7 cycloalkyl;

[0805] R 23b is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched-chain alkyl, and C 3-7 cycloalkyl;

[0806] R 24 is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched-chain alkyl, and C 3-7 cycloalkyl;

[0807] R 25 is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched-chain alkyl, and C 3-7 cycloalkyl;

[0808] and R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g at least five of which are hydrogen.

[0809] Embodiments of the present invention include compounds having the formula (IIIv):

[0810]

[0811] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0812] Q 1 is 1 or 2;

[0813] and Q 2 is 1 or 2.

[0814] Embodiments of the present invention include compounds having the formula (IIIw):

[0815]

[0816] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0817] Q 1 is 1 or 2;

[0818] and Q 2is 1 or 2.

[0819] Embodiments of the invention include compounds having the formula (IIIx):

[0820]

[0821] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0822] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[0823] Q 1 is 1 or 2;

[0824] and Q 2 is 1 or 2.

[0825] Embodiments of the invention include compounds having the formula (IIIx-1):

[0826]

[0827] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0828] Q 1 is 1 or 2;

[0829] and Q 2 is 1 or 2.

[0830] Embodiments of the invention include compounds having the formula (IIIx-2):

[0831]

[0832] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0833] Q 1 is 1 or 2;

[0834] and Q 2 is 1 or 2.

[0835] Embodiments of the invention include compounds having the formula (IIIx-3):

[0836]

[0837] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0838] Q 1 is 1 or 2;

[0839] and Q 2 is 1 or 2.

[0840] Embodiments of the invention include compounds having the formula (IIIx-4):

[0841]

[0842] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0843] Q 1 is 1 or 2;

[0844] and Q 2 is 1 or 2.

[0845] Embodiments of the invention include compounds having the formula (IIIx-5):

[0846]

[0847] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0848] Q 1 is 1 or 2;

[0849] and Q 2 is 1 or 2.

[0850] Embodiments of the invention include compounds having the formula (IV):

[0851]

[0852] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes.

[0853] In an embodiment, the compound has a structure according to formula (XLVII),

[0854] or a pharmaceutically acceptable salt thereof.

[0855] In an embodiment, the compound has a structure according to formula (XLVII),

[0856] or a pharmaceutically acceptable salt thereof.

[0857] In an embodiment, n is 1, 2 or 3. In an embodiment, n is 1. In an embodiment, n is 2. In an embodiment, n is 1 or 2.

[0858] In an embodiment, R 1 and R2 Each of which is an unsubstituted C 1-6 alkyl group. In an embodiment, R 1 and R 2 each is an ethyl group. In an embodiment, R 1 and R 2 each is a methyl group.

[0859] In an embodiment, R 1 and R 2 together with the atoms to which they are attached form a 5- to 8-membered ring, which ring optionally contains a carbon-carbon double bond and / or ring atoms selected from the group consisting of O, S, SO, SO2, and NR 7 .

[0860] In an embodiment, R 1 and R 2 together with the atoms to which they are attached form a C3-C8 cycloalkyl or C5-C8 cycloalkenyl group.

[0861] In an embodiment, R 1 and R 2 together with the atoms to which they are attached form a C3-C8 cycloalkyl or C5-C8 cycloalkenyl group selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, and cyclooctenyl. In an embodiment, the C3-C8 cycloalkyl or C5-C8 cycloalkenyl group is unsubstituted. In an embodiment, the C3-C8 cycloalkyl or C5-C8 cycloalkenyl group is substituted with 1, 2, 3, or 4 substituents (e.g., 1 or 2 substituents as described herein). In an embodiment, the substituents are selected from oxygen (=O), hydroxy, halo, cyano, C 1-6 alkoxy, C 1-6 linear alkyl, C 3-7 branched alkyl, C 1-6 haloalkyl, C 3-8 cycloalkyl, and 3- to 8-membered heterocyclic groups. In an embodiment, the substituents are selected from the group consisting of -OH, -F, -Cl, -Br, -I, -CN, -OMe, -OEt, -O n Pr, -O i Pr, -OCF3, -Me, -Et, - n Pr, - i Pr, -CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

[0862] In an embodiment, R 1 and R 2 together with the atoms to which they are attached form a ring containing the ring atom NR 75- to 8-membered rings. In embodiments, the 5- to 8-membered rings are not further substituted. In embodiments, the 5- to 8-membered rings further comprise 1, 2, 3, or 4 substituents (e.g., 1 or 2 substituents as described herein). In embodiments, the substituents are selected from oxygen (═O), hydroxy, halo, cyano, C 1-6 alkoxy, C 1-6 linear alkyl, C 3-7 branched alkyl, C 1-6 haloalkyl, C 3-8 cycloalkyl, and 3- to 8-membered heterocycloalkyl. In embodiments, the substituents are selected from the group consisting of -OH, -F, -Cl, -Br, -I, -CN, -OMe, -OEt, -O n Pr, -O i Pr, -OCF3, -Me, -Et, - n Pr, - i Pr, -CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

[0863] In embodiments, R 1 and R 2 together form pyrrolidinyl or piperidinyl, wherein the nitrogen atom is NR 7 . In embodiments, the pyrrolidinyl or piperidinyl is not further substituted. In embodiments, the pyrrolidinyl or piperidinyl further comprises 1, 2, 3, or 4 substituents as described herein.

[0864] In embodiments, R 7 is COR 8 , and R 8 is C 1-6 linear alkyl.

[0865] In embodiments, R 7 is acetyl.

[0866] In embodiments, R 7 is SO2R 10c , and R 10c is C 1-6 linear alkyl.

[0867] In embodiments, R 10c is methyl (i.e., R 7 is SO2Me).

[0868] In embodiments, R 4 is phenyl.

[0869] In embodiments, R 4 is substituted phenyl. In embodiments, R 4is phenyl substituted with 1, 2, 3, 4 or 5 substituents (e.g., phenyl substituted with 1 or 2 substituents as described herein). In an embodiment, the substituents are selected from the group consisting of hydroxyl, halogen, cyano, C 1-6 alkoxy, C 1-6 straight-chain alkyl, C 3-7 branched-chain alkyl, C 1-6 haloalkyl, C 3-8 cycloalkyl, and 3- to 8-membered heterocyclic group. In an embodiment, the substituents are selected from the group consisting of -OH, -F, -Cl, -Br, -I, -CN, -OMe, -OEt, -O n Pr, -O i Pr, -OCF3, -Me, -Et, - n Pr, - i Pr, -CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

[0870] In an embodiment, R 4 is selected from the group consisting of hydroxyphenyl, fluorophenyl, chlorophenyl, bromophenyl, cyanophenyl, tolyl, methoxyphenyl, difluorophenyl, dichlorophenyl, chlorofluorophenyl, dimethylphenyl, trifluoromethylphenyl, bis(trifluoromethyl)phenyl.

[0871] In an embodiment, R 4 is selected from the group consisting of 4-hydroxyphenyl, 3-fluorophenyl, 4-fluorophenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 4-fluoro-3-chlorophenyl, 4-cyanophenyl, 2-methoxyphenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2-isopropylphenyl, 4-trifluoromethylphenyl, 2-morpholinophenyl, and 4-methyl-2-morpholinophenyl.

[0872] In an embodiment, R 4 is pyridyl. In an embodiment, R 4 is 2-pyridyl. In an embodiment, R 4 is 3-pyridyl. In an embodiment, R 4 is 4-pyridyl. In an embodiment, the pyridyl is unsubstituted. In an embodiment, the pyridyl is substituted with 1, 2, 3 or 4 substituents (e.g., pyridyl is substituted with 1 or 2 substituents as described herein). In an embodiment, the substituents are selected from the group consisting of hydroxyl, halogen, cyano, C 1-6 alkoxy, C 1-6 straight-chain alkyl, C 3-7 branched-chain alkyl, C 1-6 haloalkyl, C 3-8The group consisting of cycloalkyl and 3- to 8-membered heterocyclic group. In an embodiment, the substituent is selected from the group consisting of -OH, -F, -Cl, -Br, -I, -CN, -OMe, -OEt, -O n Pr, -O i Pr, -OCF3, -Me, -Et, - n Pr, - i Pr, -CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

[0873] Embodiments of the present invention include compounds having the formula (IVa):

[0874]

[0875] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[0876] R 20a 、R 20b 、R 20c 、R 20d and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino, and ;

[0877] R 21 is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0878] R 22 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0879] R 23a is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0880] R 23b is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0881] R 24 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0882] R 25 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0883] and R 20a 、R 20b 、R 20c 、R 20d and R 20e at least three of which are hydrogen.

[0884] Embodiments of the present invention include compounds having formula (IVb):

[0885]

[0886] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[0887] Q 1 is 1 or 2;

[0888] and Q 2 is 1 or 2.

[0889] Embodiments of the present invention include compounds having formula (IVc):

[0890]

[0891] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0892] Q 1 is 1 or 2;

[0893] and Q 2 is 1 or 2.

[0894] Embodiments of the present invention include compounds having formula (IVd):

[0895]

[0896] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0897] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[0898] Q 1 is 1 or 2;

[0899] and Q 2 is 1 or 2.

[0900] Embodiments of the present invention include compounds having formula (IVd-1):

[0901]

[0902] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0903] Q 1 is 1 or 2;

[0904] and Q 2 is 1 or 2.

[0905] Embodiments of the present invention include compounds having formula (IVd-2):

[0906]

[0907] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0908] Q 1 is 1 or 2;

[0909] and Q 2is 1 or 2.

[0910] Embodiments of the present invention include compounds having the formula (IVd-3):

[0911]

[0912] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0913] Q 1 is 1 or 2;

[0914] and Q 2 is 1 or 2.

[0915] Embodiments of the present invention include compounds having the formula (IVd-4):

[0916]

[0917] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0918] Q 1 is 1 or 2;

[0919] and Q 2 is 1 or 2.

[0920] Embodiments of the present invention include compounds having the formula (IVd-5):

[0921]

[0922] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0923] Q 1 is 1 or 2;

[0924] and Q 2 is 1 or 2.

[0925] Embodiments of the present invention include compounds having the formula (IVe):

[0926]

[0927] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0928] R 20a 、R 20b 、R 20c and R 20d are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 , NHSO2R 22 , -NR 23a R 23b , NHC(O)R 24 , C(O)NHR 24 , C(O)N(R 24 )2, morpholino and the group consisting of;

[0929] R 21 is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0930] R 22 is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0931] R 23a is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0932] R 23b is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[0933] R 24 is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 linear alkyl, C3-7 A group consisting of branched alkyl and C 3-7 cycloalkyl;

[0934] R 25 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears;

[0935] and at least two of R 20a , R 20b , R 20c and R 20d are hydrogen.

[0936] Embodiments of the present invention include compounds having the formula (IVf):

[0937]

[0938] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes thereof, wherein

[0939] Q 1 is 1 or 2;

[0940] and Q 2 is 1 or 2.

[0941] Embodiments of the present invention include compounds having the formula (IVg):

[0942]

[0943] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes thereof, wherein

[0944] Q 1 is 1 or 2;

[0945] and Q 2 is 1 or 2.

[0946] Embodiments of the present invention include compounds having the formula (IVh):

[0947]

[0948] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes thereof, wherein

[0949] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[0950] Q 1 is 1 or 2;

[0951] and Q 2 is 1 or 2.

[0952] Embodiments of the present invention include compounds having the formula (IVh-1):

[0953]

[0954] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0955] Q 1 is 1 or 2;

[0956] and Q 2 is 1 or 2.

[0957] Embodiments of the present invention include compounds having the formula (IVh-2):

[0958]

[0959] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0960] Q 1 is 1 or 2;

[0961] and Q 2 is 1 or 2.

[0962] Embodiments of the present invention include compounds having the formula (IVh-3):

[0963]

[0964] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0965] Q 1 is 1 or 2;

[0966] and Q 2 is 1 or 2.

[0967] Embodiments of the present invention include compounds having the formula (IVh-4):

[0968]

[0969] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0970] Q 1 is 1 or 2;

[0971] and Q 2 is 1 or 2.

[0972] Embodiments of the present invention include compounds having the formula (IVh-5):

[0973]

[0974] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0975] Q 1 is 1 or 2;

[0976] and Q 2 is 1 or 2.

[0977] Embodiments of the present invention include compounds having the formula (IVi):

[0978]

[0979] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0980] R 20a 、R 20b 、R 20c and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of;

[0981] R 21 is independently selected, at each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0982] R 22 is independently selected, at each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0983] R 23a is independently selected, at each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0984] R 23b is independently selected, at each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0985] R 24 is independently selected, at each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0986] R 25 is independently selected, at each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[0987] and at least two of R 20a , R 20b , R 20c , and R 20e are hydrogen.

[0988] Embodiments of the invention include compounds having formula (IVj):

[0989]

[0990] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[0991] Q 1 is 1 or 2;

[0992] and Q 2is 1 or 2.

[0993] Embodiments of the present invention include compounds having the formula (IVk):

[0994]

[0995] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[0996] Q 1 is 1 or 2;

[0997] and Q 2 is 1 or 2.

[0998] Embodiments of the present invention include compounds having the formula (IVL):

[0999]

[1000] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1001] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[1002] Q 1 is 1 or 2;

[1003] and Q 2 is 1 or 2.

[1004] Embodiments of the present invention include compounds having the formula (IVL-1):

[1005]

[1006] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1007] Q 1 is 1 or 2;

[1008] and Q 2 is 1 or 2.

[1009] Embodiments of the present invention include compounds having the formula (IVL-2):

[1010]

[1011] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1012] Q 1 is 1 or 2;

[1013] and Q 2 is 1 or 2.

[1014] Embodiments of the present invention include compounds having the formula (IVL-3):

[1015]

[1016] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1017] Q 1 is 1 or 2;

[1018] and Q 2 is 1 or 2.

[1019] Embodiments of the present invention include compounds having the formula (IVL-4):

[1020]

[1021] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1022] Q 1 is 1 or 2;

[1023] and Q 2 is 1 or 2.

[1024] Embodiments of the present invention include compounds having the formula (IVL-5):

[1025]

[1026] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1027] Q 1 is 1 or 2;

[1028] and Q 2 is 1 or 2.

[1029] Embodiments of the present invention include compounds having the formula (IVm):

[1030]

[1031] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1032] R 20a 、R 20b 、R 20d and R 20eIndependently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 , NHSO2R 22 , -NR 23a R 23b , NHC(O)R 24 , C(O)NHR 24 , C(O)N(R 24 )2, morpholino and a group consisting of;

[1033] R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence;

[1034] R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence;

[1035] R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence;

[1036] R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence;

[1037] R24 is independently selected, at each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1038] R 25 is independently selected, at each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1039] and R 20a , R 20b , R 20c and R 20d and at least two of R

[1040] Embodiments of the present invention include compounds having formula (IVn):

[1041]

[1042] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[1043] Q 1 is 1 or 2;

[1044] and Q 2 is 1 or 2.

[1045] Embodiments of the present invention include compounds having formula (IVo):

[1046]

[1047] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[1048] Q 1 is 1 or 2;

[1049] and Q 2 is 1 or 2.

[1050] Embodiments of the present invention include compounds having formula (IVp):

[1051]

[1052] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[1053] X 1 is selected from the group consisting of O, S, SO, SO2, and NR 7 ;

[1054] Q 1 is 1 or 2;

[1055] and Q 2 is 1 or 2.

[1056] Embodiments of the present invention include compounds having the formula (IVp-1):

[1057]

[1058] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1059] Q 1 is 1 or 2;

[1060] and Q 2 is 1 or 2.

[1061] Embodiments of the present invention include compounds having the formula (IVp-2):

[1062]

[1063] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1064] Q 1 is 1 or 2;

[1065] and Q 2 is 1 or 2.

[1066] Embodiments of the present invention include compounds having the formula (IVp-3):

[1067]

[1068] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1069] Q 1 is 1 or 2;

[1070] and Q 2 is 1 or 2.

[1071] Embodiments of the present invention include compounds having the formula (IVp-4):

[1072]

[1073] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1074] Q 1is 1 or 2;

[1075] and Q 2 is 1 or 2.

[1076] Embodiments of the invention include compounds having the formula (IVp-5):

[1077]

[1078] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1079] Q 1 is 1 or 2;

[1080] and Q 2 is 1 or 2.

[1081] Embodiments of the invention include compounds having the formula (IVq):

[1082]

[1083] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1084] R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b, NHC(O)R 24 , C(O)NHR 24 , C(O)N(R 24 )2, morpholino, and the group consisting of;

[1085] R 21 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1086] R 22 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1087] R 23a is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1088] R 23b is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1089] R 24 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1090] R 25 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1091] and at least 5 of R 20a , R 20b , R 20c , R 20d , R 20e , R 20f and R 20g are hydrogen.

[1092] Embodiments of the invention include compounds having the formula (IVr):

[1093]

[1094] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1095] Q 1 is 1 or 2;

[1096] and Q 2 is 1 or 2.

[1097] Embodiments of the present invention include compounds having formula (IVs):

[1098]

[1099] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1100] Q 1 is 1 or 2;

[1101] and Q 2 is 1 or 2.

[1102] Embodiments of the present invention include compounds having formula (IVt):

[1103]

[1104] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1105] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[1106] Q 1 is 1 or 2;

[1107] and Q 2 is 1 or 2.

[1108] Embodiments of the present invention include compounds having formula (IVt-1):

[1109]

[1110] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1111] Q 1 is 1 or 2;

[1112] and Q 2 is 1 or 2.

[1113] Embodiments of the present invention include compounds having formula (IVt-2):

[1114]

[1115] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1116] Q 1 is 1 or 2;

[1117] and Q 2 is 1 or 2.

[1118] Embodiments of the present invention include compounds having the formula (IVt-3):

[1119]

[1120] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1121] Q 1 is 1 or 2;

[1122] and Q 2 is 1 or 2.

[1123] Embodiments of the present invention include compounds having the formula (IVt-4):

[1124]

[1125] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1126] Q 1 is 1 or 2;

[1127] and Q 2 is 1 or 2.

[1128] Embodiments of the present invention include compounds having the formula (IVt-5):

[1129]

[1130] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1131] Q 1 is 1 or 2;

[1132] and Q 2 is 1 or 2.

[1133] Embodiments of the present invention include compounds having the formula (IVu):

[1134]

[1135] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1136] R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of;

[1137] R 21 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears;

[1138] R 22 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears;

[1139] R 23a is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C3-7 The group consisting of branched alkyl and C 3-7 cycloalkyl;

[1140] R 23b is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1141] R 24 is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1142] R 25 is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1143] and R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g at least 5 of which are hydrogen.

[1144] Embodiments of the present invention include compounds having formula (IVv):

[1145]

[1146] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1147] Q 1 is 1 or 2;

[1148] and Q 2 is 1 or 2.

[1149] Embodiments of the present invention include compounds having formula (IVw):

[1150]

[1151] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1152] Q 1 is 1 or 2;

[1153] and Q 2 is 1 or 2.

[1154] Embodiments of the present invention include compounds having formula (IVx):

[1155]

[1156] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1157] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[1158] Q 1 is 1 or 2;

[1159] and Q 2 is 1 or 2.

[1160] Embodiments of the present invention include compounds having formula (IVx-1):

[1161]

[1162] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1163] Q 1 is 1 or 2;

[1164] and Q 2 is 1 or 2.

[1165] Embodiments of the present invention include compounds having formula (IVx-2):

[1166]

[1167] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1168] Q 1 is 1 or 2;

[1169] and Q 2 is 1 or 2.

[1170] Embodiments of the present invention include compounds having formula (IVx-3):

[1171]

[1172] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1173] Q 1 is 1 or 2;

[1174] And Q 2 Is 1 or 2.

[1175] Embodiments of the present invention include compounds having formula (IVx-4):

[1176]

[1177] Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes thereof, wherein

[1178] Q 1 is 1 or 2;

[1179] And Q 2 Is 1 or 2.

[1180] Embodiments of the present invention include compounds having formula (IVx-5):

[1181]

[1182] Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes thereof, wherein

[1183] Q 1 is 1 or 2;

[1184] And Q 2 Is 1 or 2.

[1185] Embodiments of the present invention include compounds having formula (V):

[1186]

[1187] This includes hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes thereof.

[1188] Embodiments of the present invention include compounds having formula (Va):

[1189]

[1190] Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes thereof, wherein

[1191] R 20a , R 20b , R 20c , R 20d and R 20e independently selected from hydrogen, -CN, -NO2, -OH, halogen, C 1-6 Straight chain alkyl, C 3-7 Branched alkyl, C 3-7 Cycloalkyl, C 1-6 Straight chain alkoxy, C3-7 Branched alkoxy, C 3-7 Cycloalkoxy, C 1-6 Straight-chain haloalkyl, C 3-7 Branched haloalkyl, C 1-6 Straight-chain haloalkoxy, C 3-7 Branched haloalkoxy, SH, SC 1-6 Straight-chain alkyl, SC 3-7 Branched alkyl, SC 3-7 Cycloalkyl, SO2C 1-6 Straight-chain alkyl, SO2C 3-7 Branched alkyl, SO2C 3-7 Cycloalkyl, SO2NH2, SO2NHR 21 , NHSO2R 22 , -NR 23a R 23b , NHC(O)R 24 , C(O)NHR 24 , C(O)N(R 24 )2, morpholino and the group consisting of;

[1192] R 21 independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1193] R 22 independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1194] R 23a independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1195] R 23b independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1196] R 24 independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1197] R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears;

[1198] and at least three of R 20a , R 20b , R 20c , R 20d and R 20e are hydrogen.

[1199] Embodiments of the present invention include compounds having the formula (Vb):

[1200]

[1201] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[1202] Q 1 is 1 or 2;

[1203] and Q 2 is 1 or 2.

[1204] Embodiments of the present invention include compounds having the formula (Vc):

[1205]

[1206] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[1207] Q 1 is 1 or 2;

[1208] and Q 2 is 1 or 2.

[1209] Embodiments of the present invention include compounds having the formula (Vd):

[1210]

[1211] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[1212] X 1 is selected from the group consisting of O, S, SO, SO2, and NR 7 ;

[1213] Q 1 is 1 or 2;

[1214] and Q 2 is 1 or 2.

[1215] Embodiments of the present invention include compounds having the formula (Vd-1):

[1216]

[1217] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1218] Q 1 is 1 or 2;

[1219] and Q 2 is 1 or 2.

[1220] Embodiments of the present invention include compounds having the formula (Vd-2):

[1221]

[1222] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1223] Q 1 is 1 or 2;

[1224] and Q 2 is 1 or 2.

[1225] Embodiments of the present invention include compounds having the formula (Vd-3):

[1226]

[1227] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1228] Q 1 is 1 or 2;

[1229] and Q 2 is 1 or 2.

[1230] Embodiments of the present invention include compounds having the formula (Vd-4):

[1231]

[1232] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1233] Q 1 is 1 or 2;

[1234] and Q 2 is 1 or 2.

[1235] Embodiments of the present invention include compounds having the formula (Vd-5):

[1236]

[1237] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1238] Q 1 is 1 or 2;

[1239] and Q 2 is 1 or 2.

[1240] Embodiments of the present invention include compounds having the formula (Ve):

[1241]

[1242] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1243] R 20a 、R 20b 、R 20c and R 20d are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of;

[1244] R 21independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence;

[1245] R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence;

[1246] R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence;

[1247] R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence;

[1248] R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence;

[1249] R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence;

[1250] and at least two of R 20a , R 20b , R 20c and R 20d are hydrogen.

[1251] Embodiments of the present invention include compounds having the formula (Vf):

[1252]

[1253] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1254] Q 1 is 1 or 2;

[1255] and Q 2 is 1 or 2.

[1256] Embodiments of the present invention include compounds having the formula (Vg):

[1257]

[1258] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1259] Q 1 is 1 or 2;

[1260] and Q 2 is 1 or 2.

[1261] Embodiments of the present invention include compounds having the formula (Vh):

[1262]

[1263] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1264] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[1265] Q 1 is 1 or 2;

[1266] and Q 2 is 1 or 2.

[1267] Embodiments of the present invention include compounds having the formula (Vh-1):

[1268]

[1269] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1270] Q 1 is 1 or 2;

[1271] and Q 2 is 1 or 2.

[1272] Embodiments of the present invention include compounds having the formula (Vh-2):

[1273]

[1274] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1275] Q 1 is 1 or 2;

[1276] and Q 2 is 1 or 2.

[1277] Embodiments of the present invention include compounds having the formula (Vh-3):

[1278]

[1279] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1280] Q 1 is 1 or 2;

[1281] and Q 2 is 1 or 2.

[1282] Embodiments of the present invention include compounds having the formula (Vh-4):

[1283]

[1284] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1285] Q 1 is 1 or 2;

[1286] and Q 2 is 1 or 2.

[1287] Embodiments of the present invention include compounds having the formula (Vh-5):

[1288]

[1289] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1290] Q 1 is 1 or 2;

[1291] and Q 2 is 1 or 2.

[1292] Embodiments of the present invention include compounds having the formula (Vi):

[1293]

[1294] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1295] R 20a 、R 20b 、R 20c and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7Branched alkyl, C 3-7 Cycloalkyl, C 1-6 Straight-chain alkoxy, C 3-7 Branched alkoxy, C 3-7 Cycloalkoxy, C 1-6 Straight-chain haloalkyl, C 3-7 Branched haloalkyl, C 1-6 Straight-chain haloalkoxy, C 3-7 Branched haloalkoxy, SH, SC 1-6 Straight-chain alkyl, SC 3-7 Branched alkyl, SC 3-7 Cycloalkyl, SO2C 1-6 Straight-chain alkyl, SO2C 3-7 Branched alkyl, SO2C 3-7 Cycloalkyl, SO2NH2, SO2NHR 21 , NHSO2R 22 , -NR 23a R 23b , NHC(O)R 24 , C(O)NHR 24 , C(O)N(R 24 )2, morpholino and the group consisting of;

[1296] R 21 independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1297] R 22 independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1298] R 23a independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1299] R 23b independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1300] R 24 independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7The group consisting of branched alkyl and C 3-7 cycloalkyl;

[1301] R 25 is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1302] and at least two of R 20a , R 20b , R 20c and R 20e are hydrogen.

[1303] Embodiments of the present invention include compounds having the formula (Vj):

[1304]

[1305] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1306] Q 1 is 1 or 2;

[1307] and Q 2 is 1 or 2.

[1308] Embodiments of the present invention include compounds having the formula (Vk):

[1309]

[1310] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1311] Q 1 is 1 or 2;

[1312] and Q 2 is 1 or 2.

[1313] Embodiments of the present invention include compounds having the formula (VL):

[1314]

[1315] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1316] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[1317] Q 1 is 1 or 2;

[1318] And Q 2 is 1 or 2.

[1319] Embodiments of the present invention include compounds having the formula (VL-1):

[1320]

[1321] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1322] Q 1 is 1 or 2;

[1323] And Q 2 is 1 or 2.

[1324] Embodiments of the present invention include compounds having the formula (VL-2):

[1325]

[1326] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1327] Q 1 is 1 or 2;

[1328] And Q 2 is 1 or 2.

[1329] Embodiments of the present invention include compounds having the formula (VL-3):

[1330]

[1331] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1332] Q 1 is 1 or 2;

[1333] And Q 2 is 1 or 2.

[1334] Embodiments of the present invention include compounds having the formula (VL-4):

[1335]

[1336] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1337] Q 1 is 1 or 2;

[1338] And Q 2 is 1 or 2.

[1339] Embodiments of the present invention include compounds having the formula (VL-5):

[1340]

[1341] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1342] Q 1 is 1 or 2;

[1343] and Q 2 is 1 or 2.

[1344] Embodiments of the present invention include compounds having the formula (Vm):

[1345]

[1346] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1347] R 20a 、R 20b 、R 20d and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of;

[1348] R 21Independently at each occurrence, selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1349] R 22 Independently at each occurrence, selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1350] R 23a Independently at each occurrence, selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1351] R 23b Independently at each occurrence, selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1352] R 24 Independently at each occurrence, selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1353] R 25 Independently at each occurrence, selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1354] And at least two of R 20a , R 20b , R 20c and R 20d are hydrogen.

[1355] Embodiments of the present invention include compounds having the formula (Vn):

[1356]

[1357] Including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1358] Q 1 is 1 or 2;

[1359] And Q 2 is 1 or 2.

[1360] Embodiments of the present invention include compounds having the formula (Vo):

[1361]

[1362] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1363] Q 1 is 1 or 2;

[1364] and Q 2 is 1 or 2.

[1365] Embodiments of the present invention include compounds having the formula (Vp):

[1366]

[1367] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1368] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[1369] Q 1 is 1 or 2;

[1370] and Q 2 is 1 or 2.

[1371] Embodiments of the present invention include compounds having the formula (Vp-1):

[1372]

[1373] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1374] Q 1 is 1 or 2;

[1375] and Q 2 is 1 or 2.

[1376] Embodiments of the present invention include compounds having the formula (Vp-2):

[1377]

[1378] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1379] Q 1 is 1 or 2;

[1380] and Q 2 is 1 or 2.

[1381] Embodiments of the present invention include compounds having formula (Vp-3):

[1382]

[1383] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1384] Q 1 is 1 or 2;

[1385] and Q 2 is 1 or 2.

[1386] Embodiments of the present invention include compounds having formula (Vp-4):

[1387]

[1388] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1389] Q 1 is 1 or 2;

[1390] and Q 2 is 1 or 2.

[1391] Embodiments of the present invention include compounds having formula (Vp-5):

[1392]

[1393] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1394] Q 1 is 1 or 2;

[1395] and Q 2 is 1 or 2.

[1396] Embodiments of the present invention include compounds having formula (Vq):

[1397]

[1398] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1399] R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20gIndependently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 , NHSO2R 22 , -NR 23a R 23b , NHC(O)R 24 , C(O)NHR 24 , C(O)N(R 24 )2, morpholino and the group consisting of;

[1400] R 21 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1401] R 22 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1402] R 23a is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1403] R 23b is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1404] R24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence;

[1405] R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence;

[1406] and R 20a , R 20b , R 20c , R 20d , R 20e , R 20f and R 20g at least 5 of which are hydrogen.

[1407] Embodiments of the present invention include compounds having the formula (Vr):

[1408]

[1409] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1410] Q 1 is 1 or 2;

[1411] and Q 2 is 1 or 2.

[1412] Embodiments of the present invention include compounds having the formula (Vs):

[1413]

[1414] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1415] Q 1 is 1 or 2;

[1416] and Q 2 is 1 or 2.

[1417] Embodiments of the present invention include compounds having the formula (Vt):

[1418]

[1419] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1420] X 1Selected from the group consisting of O, S, SO, SO2, and NR 7 ;

[1421] Q 1 is 1 or 2;

[1422] and Q 2 is 1 or 2.

[1423] Embodiments of the present invention include compounds having the formula (Vt-1):

[1424]

[1425] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[1426] Q 1 is 1 or 2;

[1427] and Q 2 is 1 or 2.

[1428] Embodiments of the present invention include compounds having the formula (Vt-2):

[1429]

[1430] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[1431] Q 1 is 1 or 2;

[1432] and Q 2 is 1 or 2.

[1433] Embodiments of the present invention include compounds having the formula (Vt-3):

[1434]

[1435] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[1436] Q 1 is 1 or 2;

[1437] and Q 2 is 1 or 2.

[1438] Embodiments of the present invention include compounds having the formula (Vt-4):

[1439]

[1440] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[1441] Q 1 is 1 or 2;

[1442] and Q 2 is 1 or 2.

[1443] Embodiments of the invention include compounds having the formula (Vt-5):

[1444]

[1445] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes thereof, wherein

[1446] Q 1 is 1 or 2;

[1447] and Q 2 is 1 or 2.

[1448] Embodiments of the invention include compounds having the formula (Vu):

[1449]

[1450] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes thereof, wherein

[1451] R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR23a R 23b 、 NHC(O)R 24 、 C(O)NHR 24 、 C(O)N(R 24 )2, morpholino, and the group consisting of;

[1452] R 21 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1453] R 22 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1454] R 23a is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1455] R 23b is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1456] R 24 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1457] R 25 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1458] and at least five of R 20a , R 20b , R 20c , R 20d , R 20e , R 20f , and R 20g are hydrogen.

[1459] Embodiments of the invention include compounds having the formula (Vv):

[1460]

[1461] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1462] Q 1 is 1 or 2;

[1463] and Q 2 is 1 or 2.

[1464] Embodiments of the invention include compounds having formula (Vw):

[1465]

[1466] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1467] Q 1 is 1 or 2;

[1468] and Q 2 is 1 or 2.

[1469] Embodiments of the invention include compounds having formula (Vx):

[1470]

[1471] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1472] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[1473] Q 1 is 1 or 2;

[1474] and Q 2 is 1 or 2.

[1475] Embodiments of the invention include compounds having formula (Vx-1):

[1476]

[1477] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1478] Q 1 is 1 or 2;

[1479] and Q 2 is 1 or 2.

[1480] Embodiments of the present invention include compounds having the formula (Vx-2):

[1481]

[1482] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1483] Q 1 is 1 or 2;

[1484] and Q 2 is 1 or 2.

[1485] Embodiments of the present invention include compounds having the formula (Vx-3):

[1486]

[1487] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1488] Q 1 is 1 or 2;

[1489] and Q 2 is 1 or 2.

[1490] Embodiments of the present invention include compounds having the formula (Vx-4):

[1491]

[1492] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1493] Q 1 is 1 or 2;

[1494] and Q 2 is 1 or 2.

[1495] Embodiments of the present invention include compounds having the formula (Vx-5):

[1496]

[1497] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1498] Q 1 is 1 or 2;

[1499] and Q 2 is 1 or 2.

[1500] Embodiments of the present invention include compounds having the formula (VI):

[1501]

[1502] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes.

[1503] In an embodiment, the compound has a structure according to formula (XLVI)

[1504] or a pharmaceutically acceptable salt thereof.

[1505] In an embodiment, the compound has a structure according to formula (XLVIa)

[1506] or a pharmaceutically acceptable salt thereof.

[1507] In an embodiment, n is 1, 2 or 3. In an embodiment, n is 1. In an embodiment, n is 2. In an embodiment, n is 1 or 2.

[1508] In an embodiment, R 1 and R 2 each is an unsubstituted C 1-6 alkyl. In an embodiment, R 1 and R 2 each is ethyl. In an embodiment, R 1 and R 2 each is methyl.

[1509] In an embodiment, R 1 and R 2 together with the atoms to which they are attached form a 5- to 8-membered ring which optionally contains a carbon-carbon double bond and / or ring atoms selected from the group consisting of O, S, SO, SO2 and NR 7 group.

[1510] In an embodiment, R 1 and R 2 together with the atoms to which they are attached form a C3-C8 cycloalkyl or a C5-C8 cycloalkenyl.

[1511] In an embodiment, R 1 and R 2Together with the atoms to which they are bonded, form a C3-C8 cycloalkyl or C5-C8 cycloalkenyl selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl and cyclooctenyl. In an embodiment, the C3-C8 cycloalkyl or C5-C8 cycloalkenyl is unsubstituted. In an embodiment, the C3-C8 cycloalkyl or C5-C8 cycloalkenyl is substituted with 1, 2, 3 or 4 substituents (e.g., 1 or 2 substituents as described herein). In an embodiment, the substituents are selected from oxygen (=O), hydroxy, halo, cyano, C 1-6 alkoxy, C 1-6 linear alkyl, C 3-7 branched alkyl, C 1-6 haloalkyl, C 3-8 cycloalkyl and 3- to 8-membered heterocyclic groups. In an embodiment, the substituents are selected from the group consisting of -OH, -F, -Cl, -Br, -I, -CN, -OMe, -OEt, -O n Pr, -O i Pr, -OCF3, -Me, -Et, - n Pr, - i Pr, -CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl and morpholino.

[1512] In an embodiment, R 1 and R 2 together with the atoms to which they are bonded, form a 5- to 8-membered ring containing the ring atom NR 7 . In an embodiment, the 5- to 8-membered ring is not further substituted. In an embodiment, the 5- to 8-membered ring further contains 1, 2, 3 or 4 substituents (e.g., 1 or 2 substituents as described herein). In an embodiment, the substituents are selected from oxygen (=O), hydroxy, halo, cyano, C 1-6 alkoxy, C 1-6 linear alkyl, C 3-7 branched alkyl, C 1-6 haloalkyl, C 3-8 cycloalkyl and 3- to 8-membered heterocyclic groups. In an embodiment, the substituents are selected from the group consisting of -OH, -F, -Cl, -Br, -I, -CN, -OMe, -OEt, -O n Pr, -O i Pr, -OCF3, -Me, -Et, - n Pr, - i Pr, -CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl and morpholino.

[1513] In an embodiment, R 1 and R 2Combine to form a pyrrolidinyl or piperidinyl group, where the nitrogen atom is NR 7 . In embodiments, the pyrrolidinyl or piperidinyl group is not further substituted. In embodiments, the pyrrolidinyl or piperidinyl group further comprises 1, 2, 3, or 4 substituents as described herein.

[1514] In embodiments, R 7 is COR 8 , and R 8 is C 1-6 linear alkyl.

[1515] In embodiments, R 7 is acetyl.

[1516] In embodiments, R 7 is SO2R 10c , and R 10c is C 1-6 linear alkyl.

[1517] In embodiments, R 10c is methyl (i.e., R 7 is SO2Me).

[1518] In embodiments, R 5 is phenyl.

[1519] In embodiments, R 5 is substituted phenyl. In embodiments, R 5 is phenyl substituted with 1, 2, 3, 4, or 5 substituents (e.g., phenyl substituted with 1 or 2 substituents as described herein). In embodiments, the substituents are selected from the group consisting of hydroxyl, halogen, cyano, C 1-6 alkoxy, C 1-6 linear alkyl, C 3-7 branched alkyl, C 1-6 haloalkyl, C 3-8 cycloalkyl, and 3- to 8-membered heterocyclic groups. In embodiments, the substituents are selected from the group consisting of -OH, -F, -Cl, -Br, -I, -CN, -OMe, -OEt, -O n Pr, -O i Pr, -OCF3, -Me, -Et, - n Pr, - i Pr, -CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.

[1520] In embodiments, R 5Selected from the group consisting of hydroxyphenyl, fluorophenyl, chlorophenyl, bromophenyl, cyanophenyl, tolyl, methoxyphenyl, difluorophenyl, dichlorophenyl, chlorofluorophenyl, dimethylphenyl, trifluoromethylphenyl, bis(trifluoromethyl)phenyl.

[1521] In an embodiment, R 5 Selected from the group consisting of 4-hydroxyphenyl, 3-fluorophenyl, 4-fluorophenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 4-fluoro-3-chlorophenyl, 4-cyanophenyl, 2-methoxyphenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2-isopropylphenyl, 4-trifluoromethylphenyl, 2-morpholinophenyl, and 4-methyl-2-morpholinophenyl.

[1522] In an embodiment, R 5 Is pyridyl. In an embodiment, R 5 Is 2-pyridyl. In an embodiment, R 5 Is 3-pyridyl. In an embodiment, R 5 Is 4-pyridyl. In an embodiment, the pyridyl is unsubstituted. In an embodiment, the pyridyl is substituted with 1, 2, 3, or 4 substituents (e.g., the pyridyl is substituted with 1 or 2 substituents as described herein). In an embodiment, the substituents are selected from the group consisting of hydroxy, halo, cyano, C 1-6 Alkoxy, C 1-6 Straight-chain alkyl, C 3-7 Branched-chain alkyl, C 1-6 Haloalkyl, C 3-8 Cycloalkyl, and 3- to 8-membered heterocyclic group. In an embodiment, the substituents are selected from the group consisting of -OH, -F, -Cl, -Br, -I, -CN, -OMe, -OEt, -O n Pr, -O i Pr, -OCF3, -Me, -Et, - n Pr, - i Pr, -CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholinyl.

[1523] Embodiments of the present invention include compounds having the formula (VIa):

[1524]

[1525] Including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[1526] R 20a 、R 20b 、R 20c 、R 20d And R 20eIndependently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 , NHSO2R 22 , -NR 23a R 23b , NHC(O)R 24 , C(O)NHR 24 , C(O)N(R 24 )2, morpholino and the group consisting of;

[1527] R 21 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1528] R 22 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1529] R 23a is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1530] R 23b is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1531] R24 is independently selected, at each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1532] R 25 is independently selected, at each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1533] and R 20a , R 20b , R 20c , R 20d , and R 20e are each hydrogen.

[1534] Embodiments of the invention include compounds having formula (VIb):

[1535]

[1536] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[1537] Q 1 is 1 or 2;

[1538] and Q 2 is 1 or 2.

[1539] Embodiments of the invention include compounds having formula (VIc):

[1540]

[1541] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[1542] Q 1 is 1 or 2;

[1543] and Q 2 is 1 or 2.

[1544] Embodiments of the invention include compounds having formula (VId):

[1545]

[1546] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[1547] X 1 is selected from the group consisting of O, S, SO, SO2, and NR 7a group consisting of;

[1548] Q 1 is 1 or 2;

[1549] and Q 2 is 1 or 2.

[1550] Embodiments of the present invention include compounds having the formula (Vid-1):

[1551]

[1552] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1553] Q 1 is 1 or 2;

[1554] and Q 2 is 1 or 2.

[1555] Embodiments of the present invention include compounds having the formula (Vid-2):

[1556]

[1557] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1558] Q 1 is 1 or 2;

[1559] and Q 2 is 1 or 2.

[1560] Embodiments of the present invention include compounds having the formula (Vid-3):

[1561]

[1562] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1563] Q 1 is 1 or 2;

[1564] and Q 2 is 1 or 2.

[1565] Embodiments of the present invention include compounds having the formula (Vid-4):

[1566]

[1567] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1568] Q1 is 1 or 2;

[1569] and Q 2 is 1 or 2.

[1570] Embodiments of the invention include compounds having the formula (Vid-5):

[1571]

[1572] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes thereof, wherein

[1573] Q 1 is 1 or 2;

[1574] and Q 2 is 1 or 2.

[1575] Embodiments of the invention include compounds having the formula (VIe):

[1576]

[1577] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes thereof, wherein

[1578] R 20a , R 20b , R 20c and R 20d are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 , NHSO2R 22 , -NR 23a R 23b , NHC(O)R 24 , C(O)NHR24 , C(O)N(R 24 )2, morpholino, and the group consisting of;

[1579] R 21 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1580] R 22 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1581] R 23a is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1582] R 23b is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1583] R 24 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1584] R 25 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1585] and at least two of R 20a , R 20b , R 20c , and R 20d are hydrogen.

[1586] Embodiments of the invention include compounds having formula (VIf):

[1587]

[1588] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[1589] Q 1 is 1 or 2;

[1590] and Q 2 is 1 or 2.

[1591] Embodiments of the invention include compounds having the formula (VIg):

[1592]

[1593] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1594] Q 1 is 1 or 2;

[1595] and Q 2 is 1 or 2.

[1596] Embodiments of the invention include compounds having the formula (VIh):

[1597]

[1598] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1599] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[1600] Q 1 is 1 or 2;

[1601] and Q 2 is 1 or 2.

[1602] Embodiments of the invention include compounds having the formula (VIh-1):

[1603]

[1604] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1605] Q 1 is 1 or 2;

[1606] and Q 2 is 1 or 2.

[1607] Embodiments of the invention include compounds having the formula (VIh-2):

[1608]

[1609] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1610] Q 1 is 1 or 2;

[1611] and Q 2 is 1 or 2.

[1612] Embodiments of the present invention include compounds having formula (VIh-3):

[1613]

[1614] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1615] Q 1 is 1 or 2;

[1616] and Q 2 is 1 or 2.

[1617] Embodiments of the present invention include compounds having formula (VIh-):

[1618]

[1619] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1620] Q 1 is 1 or 2;

[1621] and Q 2 is 1 or 2.

[1622] Embodiments of the present invention include compounds having formula (VIh-5):

[1623]

[1624] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1625] Q 1 is 1 or 2;

[1626] and Q 2 is 1 or 2.

[1627] Embodiments of the present invention include compounds having formula (VIi):

[1628]

[1629] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1630] R 20a , R 20b , R 20c and R 20e independently selected from hydrogen, -CN, -NO2, -OH, halogen, C 1-6 Straight chain alkyl, C 3-7 Branched alkyl, C 3-7 Cycloalkyl, C 1-6 Straight chain alkoxy, C 3-7 Branched alkoxy, C 3-7 Cycloalkoxy, C 1-6 Straight chain halogenated alkyl, C 3-7 Branched chain halogenated alkyl, C 1-6 Straight chain halogenated alkoxy, C 3-7 Branched chain haloalkoxy, SH, SC 1-6 Straight chain alkyl, SC 3-7 Branched chain alkyl, SC 3-7 Cycloalkyl, SO2C 1-6 Straight chain alkyl, SO2C 3-7 Branched alkyl, SO2C 3-7 Cycloalkyl, SO2NH2, SO2NHR 21 NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2. Morpholino and The group composed of;

[1631] R 21 independently at each occurrence selected from hydrogen, C 1-6 Straight chain alkyl, C 3-7 Branched alkyl and C 3-7 A group consisting of cycloalkyl groups;

[1632] R 22 independently at each occurrence selected from hydrogen, C 1-6 Straight chain alkyl, C 3-7 Branched alkyl and C 3-7 A group consisting of cycloalkyl groups;

[1633] R 23a independently at each occurrence selected from hydrogen, C 1-6 Straight chain alkyl, C 3-7 Branched alkyl and C 3-7 A group consisting of cycloalkyl groups;

[1634] R 23b independently at each occurrence selected from hydrogen, C 1-6Straight-chain alkyl, C 3-7 branched-chain alkyl, and C 3-7 cycloalkyl;

[1635] R 24 is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched-chain alkyl, and C 3-7 cycloalkyl;

[1636] R 25 is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched-chain alkyl, and C 3-7 cycloalkyl;

[1637] and R 20a 、R 20b 、R 20c and R 20e at least two of are hydrogen.

[1638] Embodiments of the present invention include compounds having the formula (VIj):

[1639]

[1640] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[1641] Q 1 is 1 or 2;

[1642] and Q 2 is 1 or 2.

[1643] Embodiments of the present invention include compounds having the formula (VIk):

[1644]

[1645] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[1646] Q 1 is 1 or 2;

[1647] and Q 2 is 1 or 2.

[1648] Embodiments of the present invention include compounds having the formula (VIL):

[1649]

[1650] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[1651] X 1 is selected from the group consisting of O, S, SO, SO2, and NR 7 ;

[1652] Q 1 is 1 or 2;

[1653] and Q 2 is 1 or 2.

[1654] Embodiments of the invention include compounds having the formula (VIL-1):

[1655]

[1656] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[1657] Q 1 is 1 or 2;

[1658] and Q 2 is 1 or 2.

[1659] Embodiments of the invention include compounds having the formula (VIL-2):

[1660]

[1661] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[1662] Q 1 is 1 or 2;

[1663] and Q 2 is 1 or 2.

[1664] Embodiments of the invention include compounds having the formula (VIL-3):

[1665]

[1666] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes, wherein

[1667] Q 1 is 1 or 2;

[1668] and Q 2 is 1 or 2.

[1669] Embodiments of the invention include compounds having the formula (VIL-4):

[1670]

[1671] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1672] Q 1 is 1 or 2;

[1673] and Q 2 is 1 or 2.

[1674] Embodiments of the present invention include compounds having formula (VIL-5):

[1675]

[1676] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1677] Q 1 is 1 or 2;

[1678] and Q 2 is 1 or 2.

[1679] Embodiments of the present invention include compounds having formula (VIm):

[1680]

[1681] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1682] R 20a 、R 20b 、R 20d and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR23a R 23b 、 NHC(O)R 24 、 C(O)NHR 24 、 C(O)N(R 24 )2, morpholino, and the group consisting of;

[1683] R 21 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1684] R 22 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1685] R 23a is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1686] R 23b is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1687] R 24 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1688] R 25 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1689] and at least two of R 20a , R 20b , R 20c , and R 20d are hydrogen.

[1690] Embodiments of the invention include compounds having the formula (VIn):

[1691]

[1692] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1693] Q 1 is 1 or 2;

[1694] and Q 2 is 1 or 2.

[1695] Embodiments of the present invention include compounds having formula (VIo):

[1696]

[1697] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1698] Q 1 is 1 or 2;

[1699] and Q 2 is 1 or 2.

[1700] Embodiments of the present invention include compounds having formula (VIp):

[1701]

[1702] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1703] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[1704] Q 1 is 1 or 2;

[1705] and Q 2 is 1 or 2.

[1706] Embodiments of the present invention include compounds having formula (VIp-1):

[1707]

[1708] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1709] Q 1 is 1 or 2;

[1710] and Q 2 is 1 or 2.

[1711] Embodiments of the present invention include compounds having formula (VIp-2):

[1712]

[1713] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1714] Q 1 is 1 or 2;

[1715] and Q 2 is 1 or 2.

[1716] Embodiments of the present invention include compounds having formula (VIp-3):

[1717]

[1718] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1719] Q 1 is 1 or 2;

[1720] and Q 2 is 1 or 2.

[1721] Embodiments of the present invention include compounds having formula (VIp-4):

[1722]

[1723] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1724] Q 1 is 1 or 2;

[1725] and Q 2 is 1 or 2.

[1726] Embodiments of the present invention include compounds having formula (VIp-5):

[1727]

[1728] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1729] Q 1 is 1 or 2;

[1730] and Q 2 is 1 or 2.

[1731] Embodiments of the present invention include compounds having formula (VIq):

[1732]

[1733] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1734] R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of;

[1735] R 21 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears;

[1736] R 22 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears;

[1737] R 23a is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C3-7 The group consisting of cycloalkyl;

[1738] R 23b independently at each occurrence selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1739] R 24 independently at each occurrence selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1740] R 25 independently at each occurrence selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1741] and R 20a , R 20b , R 20c , R 20d , R 20e , R 20f and R 20g at least 5 of which are hydrogen.

[1742] Embodiments of the invention include compounds having formula (VIr):

[1743]

[1744] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes thereof, wherein

[1745] Q 1 is 1 or 2;

[1746] and Q 2 is 1 or 2.

[1747] Embodiments of the invention include compounds having formula (VIs):

[1748]

[1749] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes thereof, wherein

[1750] Q 1 is 1 or 2;

[1751] and Q 2 is 1 or 2.

[1752] Embodiments of the present invention include compounds having the formula (VIt):

[1753]

[1754] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1755] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[1756] Q 1 is 1 or 2;

[1757] and Q 2 is 1 or 2.

[1758] Embodiments of the present invention include compounds having the formula (VIt-1):

[1759]

[1760] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1761] Q 1 is 1 or 2;

[1762] and Q 2 is 1 or 2.

[1763] Embodiments of the present invention include compounds having the formula (VIt-2):

[1764]

[1765] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1766] Q 1 is 1 or 2;

[1767] and Q 2 is 1 or 2.

[1768] Embodiments of the present invention include compounds having the formula (VIt-3):

[1769]

[1770] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1771] Q 1 is 1 or 2;

[1772] and Q2 is 1 or 2.

[1773] Embodiments of the present invention include compounds having the formula (VIt-4):

[1774]

[1775] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1776] Q 1 is 1 or 2;

[1777] and Q 2 is 1 or 2.

[1778] Embodiments of the present invention include compounds having the formula (VIt-5):

[1779]

[1780] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1781] Q 1 is 1 or 2;

[1782] and Q 2 is 1 or 2.

[1783] Embodiments of the present invention include compounds having the formula (VIu):

[1784]

[1785] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1786] R 20a , R 20b , R 20c , R 20d , R 20e , R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7Branched haloalkoxy, SH, SC 1-6 Straight-chain alkyl, SC 3-7 Branched alkyl, SC 3-7 Cycloalkyl, SO2C 1-6 Straight-chain alkyl, SO2C 3-7 Branched alkyl, SO2C 3-7 Cycloalkyl, SO2NH2, SO2NHR 21 , NHSO2R 22 , -NR 23a R 23b , NHC(O)R 24 , C(O)NHR 24 , C(O)N(R 24 )2, morpholino and the group consisting of;

[1787] R 21 is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1788] R 22 is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1789] R 23a is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1790] R 23b is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1791] R 24 is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1792] R 25 is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1793] and R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g and at least 5 of R

[1794] Embodiments of the present invention include compounds having formula (VIv):

[1795]

[1796] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1797] Q 1 is 1 or 2;

[1798] and Q 2 is 1 or 2.

[1799] Embodiments of the present invention include compounds having formula (VIw):

[1800]

[1801] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1802] Q 1 is 1 or 2;

[1803] and Q 2 is 1 or 2.

[1804] Embodiments of the present invention include compounds having formula (VIx):

[1805]

[1806] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1807] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[1808] Q 1 is 1 or 2;

[1809] and Q 2 is 1 or 2.

[1810] Embodiments of the present invention include compounds having formula (VIx-1):

[1811]

[1812] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1813] Q 1 is 1 or 2;

[1814] and Q 2 is 1 or 2.

[1815] Embodiments of the present invention include compounds having the formula (VIx-2):

[1816]

[1817] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1818] Q 1 is 1 or 2;

[1819] and Q 2 is 1 or 2.

[1820] Embodiments of the present invention include compounds having the formula (VIx-3):

[1821]

[1822] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1823] Q 1 is 1 or 2;

[1824] and Q 2 is 1 or 2.

[1825] Embodiments of the present invention include compounds having the formula (VIx-4):

[1826]

[1827] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1828] Q 1 is 1 or 2;

[1829] and Q 2 is 1 or 2.

[1830] Embodiments of the present invention include compounds having the formula (VIx-5):

[1831]

[1832] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1833] Q 1 is 1 or 2;

[1834] and Q 2 is 1 or 2.

[1835] Embodiments of the invention include compounds having formula (VII):

[1836]

[1837] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes.

[1838] Embodiments of the invention include compounds having formula (VIIa):

[1839]

[1840] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1841] R 20a 、R 20b 、R 20c 、R 20d and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R24 ) 2, morpholino and the group consisting of;

[1842] R 21 independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1843] R 22 independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1844] R 23a independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1845] R 23b independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1846] R 24 independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1847] R 25 independently at each occurrence is selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[1848] and at least three of R 20a , R 20b , R 20c , R 20d and R 20e are hydrogen.

[1849] Embodiments of the present invention include compounds having the formula (VIIb):

[1850]

[1851] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1852] Q 1 is 1 or 2;

[1853] and Q 2 is 1 or 2.

[1854] Embodiments of the invention include compounds having the formula (VIIc):

[1855]

[1856] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1857] Q 1 is 1 or 2;

[1858] and Q 2 is 1 or 2.

[1859] Embodiments of the invention include compounds having the formula (VIId):

[1860]

[1861] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1862] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[1863] Q 1 is 1 or 2;

[1864] and Q 2 is 1 or 2.

[1865] Embodiments of the invention include compounds having the formula (VIId-1):

[1866]

[1867] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1868] Q 1 is 1 or 2;

[1869] and Q 2 is 1 or 2.

[1870] Embodiments of the invention include compounds having the formula (VIId-2):

[1871]

[1872] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1873] Q 1 is 1 or 2;

[1874] and Q 2 is 1 or 2.

[1875] Embodiments of the present invention include compounds having formula (VIId-3):

[1876]

[1877] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1878] Q 1 is 1 or 2;

[1879] and Q 2 is 1 or 2.

[1880] Embodiments of the present invention include compounds having formula (VIId-4):

[1881]

[1882] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1883] Q 1 is 1 or 2;

[1884] and Q 2 is 1 or 2.

[1885] Embodiments of the present invention include compounds having formula (VIId-5):

[1886]

[1887] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1888] Q 1 is 1 or 2;

[1889] and Q 2 is 1 or 2.

[1890] Embodiments of the present invention include compounds having formula (VIIe):

[1891]

[1892] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1893] R 20a , R 20b , R 20c and R 20d independently selected from hydrogen, -CN, -NO2, -OH, halogen, C 1-6 Straight chain alkyl, C 3-7 Branched alkyl, C 3-7 Cycloalkyl, C 1-6 Straight chain alkoxy, C 3-7 Branched alkoxy, C 3-7 Cycloalkoxy, C 1-6 Straight chain halogenated alkyl, C 3-7 Branched chain halogenated alkyl, C 1-6 Straight chain halogenated alkoxy, C 3-7 Branched chain haloalkoxy, SH, SC 1-6 Straight chain alkyl, SC 3-7 Branched chain alkyl, SC 3-7 Cycloalkyl, SO2C 1-6 Straight chain alkyl, SO2C 3-7 Branched alkyl, SO2C 3-7 Cycloalkyl, SO2NH2, SO2NHR 21 NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2. Morpholino and The group composed of;

[1894] R 21 independently at each occurrence selected from hydrogen, C 1-6 Straight chain alkyl, C 3-7 Branched alkyl and C 3-7 A group consisting of cycloalkyl groups;

[1895] R 22 independently at each occurrence selected from hydrogen, C 1-6 Straight chain alkyl, C 3-7 Branched alkyl and C 3-7 A group consisting of cycloalkyl groups;

[1896] R 23a independently at each occurrence selected from hydrogen, C 1-6 Straight chain alkyl, C 3-7 Branched alkyl and C 3-7 A group consisting of cycloalkyl groups;

[1897] R 23b independently at each occurrence selected from hydrogen, C1-6 a linear alkyl group, C 3-7 a branched alkyl group, and C 3-7 a cycloalkyl group;

[1898] R 24 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 a linear alkyl group, C 3-7 a branched alkyl group, and C 3-7 a cycloalkyl group;

[1899] R 25 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 a linear alkyl group, C 3-7 a branched alkyl group, and C 3-7 a cycloalkyl group;

[1900] and R 20a , R 20b , R 20c and R 20d are hydrogen.

[1901] Embodiments of the invention include compounds having the formula (VIIf):

[1902]

[1903] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[1904] Q 1 is 1 or 2;

[1905] and Q 2 is 1 or 2.

[1906] Embodiments of the invention include compounds having the formula (VIIg):

[1907]

[1908] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[1909] Q 1 is 1 or 2;

[1910] and Q 2 is 1 or 2.

[1911] Embodiments of the invention include compounds having the formula (VIIh):

[1912]

[1913] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1914] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[1915] Q 1 is 1 or 2;

[1916] and Q 2 is 1 or 2.

[1917] Embodiments of the present invention include compounds having the formula (VIIh-1):

[1918]

[1919] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1920] Q 1 is 1 or 2;

[1921] and Q 2 is 1 or 2.

[1922] Embodiments of the present invention include compounds having the formula (VIIh-2):

[1923]

[1924] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1925] Q 1 is 1 or 2;

[1926] and Q 2 is 1 or 2.

[1927] Embodiments of the present invention include compounds having the formula (VIIh-3):

[1928]

[1929] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1930] Q 1 is 1 or 2;

[1931] and Q 2 is 1 or 2.

[1932] Embodiments of the present invention include compounds having the formula (VIIh-4):

[1933]

[1934] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1935] Q 1 is 1 or 2;

[1936] and Q 2 is 1 or 2.

[1937] Embodiments of the present invention include compounds having the formula (VIIh-5):

[1938]

[1939] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1940] Q 1 is 1 or 2;

[1941] and Q 2 is 1 or 2.

[1942] Embodiments of the present invention include compounds having the formula (VIIi):

[1943]

[1944] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1945] R 20a R 20b R 20c and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR21 、 NHSO2R 22 、 -NR 23a R 23b 、 NHC(O)R 24 、 C(O)NHR 24 、 C(O)N(R 24 )2, morpholino, and the group consisting of;

[1946] R 21 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1947] R 22 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1948] R 23a is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1949] R 23b is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1950] R 24 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1951] R 25 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl;

[1952] and at least two of R 20a 、 R 20b 、 R 20c and R 20e are hydrogen.

[1953] Embodiments of the invention include compounds having the formula (VIIj):

[1954]

[1955] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1956] Q 1 is 1 or 2;

[1957] and Q 2 is 1 or 2.

[1958] Embodiments of the present invention include compounds having formula (VIIk):

[1959]

[1960] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1961] Q 1 is 1 or 2;

[1962] and Q 2 is 1 or 2.

[1963] Embodiments of the present invention include compounds having formula (VIIL):

[1964]

[1965] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1966] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[1967] Q 1 is 1 or 2;

[1968] and Q 2 is 1 or 2.

[1969] Embodiments of the present invention include compounds having formula (VIIL-1):

[1970]

[1971] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1972] Q 1 is 1 or 2;

[1973] and Q 2 is 1 or 2.

[1974] Embodiments of the present invention include compounds having the formula (VIIL-2):

[1975]

[1976] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1977] Q 1 is 1 or 2;

[1978] and Q 2 is 1 or 2.

[1979] Embodiments of the present invention include compounds having the formula (VIIL-3):

[1980]

[1981] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1982] Q 1 is 1 or 2;

[1983] and Q 2 is 1 or 2.

[1984] Embodiments of the present invention include compounds having the formula (VIIL-4):

[1985]

[1986] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1987] Q 1 is 1 or 2;

[1988] and Q 2 is 1 or 2.

[1989] Embodiments of the present invention include compounds having the formula (VIIL-5):

[1990]

[1991] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1992] Q 1 is 1 or 2;

[1993] and Q 2 is 1 or 2.

[1994] Embodiments of the present invention include compounds having the formula (VIIm):

[1995]

[1996] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[1997] R 20a 、R 20b 、R 20d and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of;

[1998] R 21 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence;

[1999] R 22 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence;

[2000] R 23a is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7The group consisting of branched alkyl and C 3-7 cycloalkyl;

[2001] R 23b is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[2002] R 24 is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[2003] R 25 is independently selected, each time it appears, from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[2004] and at least two of R 20a , R 20b , R 20c and R 20d are hydrogen.

[2005] Embodiments of the present invention include compounds having the formula (VIIn):

[2006]

[2007] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2008] Q 1 is 1 or 2;

[2009] and Q 2 is 1 or 2.

[2010] Embodiments of the present invention include compounds having the formula (VIIo):

[2011]

[2012] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2013] Q 1 is 1 or 2;

[2014] and Q 2 is 1 or 2.

[2015] Embodiments of the present invention include compounds having the formula (VIIp):

[2016]

[2017] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2018] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[2019] Q 1 is 1 or 2;

[2020] and Q 2 is 1 or 2.

[2021] Embodiments of the present invention include compounds having the formula (VIIp-1):

[2022]

[2023] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2024] Q 1 is 1 or 2;

[2025] and Q 2 is 1 or 2.

[2026] Embodiments of the present invention include compounds having the formula (VIIp-2):

[2027]

[2028] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2029] Q 1 is 1 or 2;

[2030] and Q 2 is 1 or 2.

[2031] Embodiments of the present invention include compounds having the formula (VIIp-3):

[2032]

[2033] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2034] Q 1 is 1 or 2;

[2035] and Q 2 is 1 or 2.

[2036] Embodiments of the present invention include compounds having the formula (VIIp-4):

[2037]

[2038] Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes thereof, wherein

[2039] Q 1 is 1 or 2;

[2040] And Q 2 Is 1 or 2.

[2041] Embodiments of the present invention include compounds having formula (VIIp-5):

[2042]

[2043] Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes thereof, wherein

[2044] Q 1 is 1 or 2;

[2045] And Q 2 Is 1 or 2.

[2046] Embodiments of the present invention include compounds having formula (VIIq):

[2047]

[2048] Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes thereof, wherein

[2049] R 20a , R 20b , R 20c , R 20d , R 20e , R 20f and R 20g independently selected from hydrogen, -CN, -NO2, -OH, halogen, C 1-6 Straight chain alkyl, C 3-7 Branched alkyl, C 3-7 Cycloalkyl, C 1-6 Straight chain alkoxy, C 3-7 Branched alkoxy, C 3-7 Cycloalkoxy, C 1-6 Straight chain halogenated alkyl, C 3-7 Branched chain halogenated alkyl, C 1-6 Straight chain halogenated alkoxy, C 3-7 Branched chain haloalkoxy, SH, SC 1-6 Straight chain alkyl, SC3-7 Branched alkyl, SC 3-7 Cycloalkyl, SO2C 1-6 Straight-chain alkyl, SO2C 3-7 Branched alkyl, SO2C 3-7 Cycloalkyl, SO2NH2, SO2NHR 21 , NHSO2R 22 , -NR 23a R 23b , NHC(O)R 24 , C(O)NHR 24 , C(O)N(R 24 )2, morpholino and the group consisting of;

[2050] R 21 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[2051] R 22 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[2052] R 23a is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[2053] R 23b is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[2054] R 24 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[2055] R 25 is independently selected, each occurrence, from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl;

[2056] and R 20a , R20b , R 20c , R 20d , R 20e , R 20f and R 20g at least 5 of which are hydrogen.

[2057] Embodiments of the present invention include compounds having the formula (VIIr):

[2058]

[2059] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2060] Q 1 is 1 or 2;

[2061] and Q 2 is 1 or 2.

[2062] Embodiments of the present invention include compounds having the formula (VIIs):

[2063]

[2064] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2065] Q 1 is 1 or 2;

[2066] and Q 2 is 1 or 2.

[2067] Embodiments of the present invention include compounds having the formula (VIIt):

[2068]

[2069] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2070] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[2071] Q 1 is 1 or 2;

[2072] and Q 2 is 1 or 2.

[2073] Embodiments of the present invention include compounds having the formula (VIIt-1):

[2074]

[2075] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2076] Q 1 is 1 or 2;

[2077] and Q 2 is 1 or 2.

[2078] Embodiments of the present invention include compounds having formula (VIIt-2):

[2079]

[2080] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2081] Q 1 is 1 or 2;

[2082] and Q 2 is 1 or 2.

[2083] Embodiments of the present invention include compounds having formula (VIIt-3):

[2084]

[2085] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2086] Q 1 is 1 or 2;

[2087] and Q 2 is 1 or 2.

[2088] Embodiments of the present invention include compounds having formula (VIIt-4):

[2089]

[2090] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2091] Q 1 is 1 or 2;

[2092] and Q 2 is 1 or 2.

[2093] Embodiments of the present invention include compounds having formula (VIIt-5):

[2094]

[2095] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2096] Q 1 is 1 or 2;

[2097] and Q 2 is 1 or 2.

[2098] Embodiments of the invention include compounds having the formula (VIIu):

[2099]

[2100] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2101] R 20a , R 20b , R 20c , R 20d , R 20e , R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 , NHSO2R 22 , -NR 23a R 23b , NHC(O)R 24 , C(O)NHR 24 , C(O)N(R 24 )2, morpholino and the group consisting of;

[2102] R 21 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears;

[2103] R 22 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears;

[2104] R 23a is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears;

[2105] R 23b is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears;

[2106] R 24 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears;

[2107] R 25 is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears;

[2108] and at least five of R 20a , R 20b , R 20c , R 20d , R 20e , R 20f and R 20g are hydrogen.

[2109] Embodiments of the invention include compounds having the formula (VIIv):

[2110]

[2111] including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof, wherein

[2112] Q 1 is 1 or 2;

[2113] and Q 2 is 1 or 2.

[2114] Embodiments of the invention include compounds having the formula (VIIw):

[2115]

[2116] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2117] Q 1 is 1 or 2;

[2118] and Q 2 is 1 or 2.

[2119] Embodiments of the invention include compounds having the formula (VIIx):

[2120]

[2121] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2122] X 1 is selected from the group consisting of O, S, SO, SO2 and NR 7 ;

[2123] Q 1 is 1 or 2;

[2124] and Q 2 is 1 or 2.

[2125] Embodiments of the invention include compounds having the formula (VIIx-1):

[2126]

[2127] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2128] Q 1 is 1 or 2;

[2129] and Q 2 is 1 or 2.

[2130] Embodiments of the invention include compounds having the formula (VIIx-2):

[2131]

[2132] including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2133] Q 1 is 1 or 2;

[2134] and Q 2 is 1 or 2.

[2135] Embodiments of the present invention include compounds having the formula (VIIx-3):

[2136]

[2137] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2138] Q 1 is 1 or 2;

[2139] and Q 2 is 1 or 2.

[2140] Embodiments of the present invention include compounds having the formula (VIIx-4):

[2141]

[2142] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2143] Q 1 is 1 or 2;

[2144] and Q 2 is 1 or 2.

[2145] Embodiments of the present invention include compounds having the formula (VIIx-5):

[2146]

[2147] including their hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein

[2148] Q 1 is 1 or 2;

[2149] and Q 2 is 1 or 2.

[2150] In some embodiments, A is

[2151] In some embodiments, A is

[2152] In some embodiments, A is

[2153] In some embodiments, R 1 is hydrogen.

[2154] In some embodiments, R 1 is C 1-6 linear alkyl.

[2155] In some embodiments, R 1 is a C 3-7 branched alkyl group.

[2156] In some embodiments, R 2 is hydrogen.

[2157] In some embodiments, R 2 is a C 1-6 linear alkyl group.

[2158] In some embodiments, R 2 is a C 3-7 branched alkyl group.

[2159] In some embodiments, R 1 and R 2 together with the atoms to which they are attached form a ring having 5 ring atoms.

[2160] In some embodiments, R 1 and R 2 together with the atoms to which they are attached form a ring having 5 ring atoms and containing a double bond.

[2161] In some embodiments, R 1 and R 2 together with the atoms to which they are attached form a ring having 6 ring atoms.

[2162] In some embodiments, R 1 and R 2 together with the atoms to which they are attached form a ring having 6 ring atoms and containing a double bond.

[2163] In some embodiments, R 1 and R 2 together with the atoms to which they are attached form a ring having 7 ring atoms.

[2164] In some embodiments, R 1 and R 2 together with the atoms to which they are attached form a ring having 7 ring atoms and containing a double bond.

[2165] In some embodiments, R 1 and R 2 together with the atoms to which they are attached form a ring having 6 ring atoms, wherein one of the 6 ring atoms is O.

[2166] In some embodiments, R 1 and R 2Together with the atoms to which they are bonded, form a ring having 7 ring atoms, one of the 7 ring atoms being O.

[2167] In some embodiments, R 1 and R 2 Together with the atoms to which they are bonded, form a ring having 8 ring atoms, one of the 8 ring atoms being O.

[2168] In some embodiments, R 1 and R 2 Together with the atoms to which they are bonded, form a ring having 6 ring atoms, one of the 6 ring atoms being S.

[2169] In some embodiments, R 1 and R 2 Together with the atoms to which they are bonded, form a ring having 7 ring atoms, one of the 7 ring atoms being S.

[2170] In some embodiments, R 1 and R 2 Together with the atoms to which they are bonded, form a ring having 8 ring atoms, one of the 8 ring atoms being S.

[2171] In some embodiments, R 1 and R 2 Together with the atoms to which they are bonded, form a ring having 6 ring atoms, one of the 6 ring atoms being SO.

[2172] In some embodiments, R 1 and R 2 Together with the atoms to which they are bonded, form a ring having 7 ring atoms, one of the 7 ring atoms being SO.

[2173] In some embodiments, R 1 and R 2 Together with the atoms to which they are bonded, form a ring having 8 ring atoms, one of the 8 ring atoms being SO.

[2174] In some embodiments, R 1 and R 2 Together with the atoms to which they are bonded, form a ring having 6 ring atoms, one of the 6 ring atoms being SO2.

[2175] In some embodiments, R 1 and R 2 Together with the atoms to which they are bonded, form a ring having 7 ring atoms, one of the 7 ring atoms being SO2.

[2176] In some embodiments, R 1 and R 2 together with the atoms to which they are bonded form a ring having 8 ring atoms, one of the 8 ring atoms being SO2.

[2177] In some embodiments, R 1 and R 2 together with the atoms to which they are bonded form a ring having 6 ring atoms, one of the 6 ring atoms being NR 7 .

[2178] In some embodiments, R 1 and R 2 together with the atoms to which they are bonded form a ring having 7 ring atoms, one of the 7 ring atoms being NR 7 .

[2179] In some embodiments, R 1 and R 2 together with the atoms to which they are bonded form a ring having 8 ring atoms, one of the 8 ring atoms being NR 7 .

[2180] In some embodiments, R 3 is an optionally substituted phenyl.

[2181] In some embodiments, R 3 is an optionally substituted naphthalen-1-yl.

[2182] In some embodiments, R 3 is an optionally substituted naphthalen-2-yl.

[2183] In some embodiments, R 3 is an optionally substituted 2-pyridyl.

[2184] In some embodiments, R 3 is an optionally substituted 3-pyridyl.

[2185] In some embodiments, R 3 is an optionally substituted 4-pyridyl.

[2186] In some embodiments, R 3 is

[2187] In some embodiments, R 4 is an optionally substituted phenyl.

[2188] In some embodiments, R 4is an optionally substituted naphthalen-1-yl.

[2189] In some embodiments, R 4 is an optionally substituted naphthalen-2-yl.

[2190] In some embodiments, R 4 is an optionally substituted 2-pyridyl.

[2191] In some embodiments, R 4 is an optionally substituted 3-pyridyl.

[2192] In some embodiments, R 4 is an optionally substituted 4-pyridyl.

[2193] In some embodiments, R 4 is

[2194] In some embodiments, R 5 is an optionally substituted phenyl.

[2195] In some embodiments, R 5 is an optionally substituted naphthalen-1-yl.

[2196] In some embodiments, R 5 is an optionally substituted naphthalen-2-yl.

[2197] In some embodiments, R 5 is an optionally substituted 2-pyridyl.

[2198] In some embodiments, R 5 is an optionally substituted 3-pyridyl.

[2199] In some embodiments, R 5 is an optionally substituted 4-pyridyl.

[2200] In some embodiments, R 5 is

[2201] In some embodiments, R6 is an optionally substituted phenyl.

[2202] In some embodiments, R 6 is an optionally substituted naphthalen-1-yl.

[2203] In some embodiments, R 6 is an optionally substituted naphthalen-2-yl.

[2204] In some embodiments, R 6 is an optionally substituted 2-pyridyl.

[2205] In some embodiments, R 6 is an optionally substituted 3-pyridyl group.

[2206] In some embodiments, R 6 is an optionally substituted 4-pyridyl group.

[2207] In some embodiments, R 7 is H.

[2208] In some embodiments, R 7 is C 1-6 a straight-chain alkyl group.

[2209] In some embodiments, R 7 is C 3-7 a branched-chain alkyl group.

[2210] In some embodiments, R 7 is C 3-7 a cycloalkyl group.

[2211] In some embodiments, R 7 is an optionally substituted phenyl group.

[2212] In some embodiments, R 7 is an optionally substituted benzyl group.

[2213] In some embodiments, R 7 is COR 8 .

[2214] In some embodiments, R 7 is CO2R 9 .

[2215] In some embodiments, R 7 is CONR 10a R 10b .

[2216] In some embodiments, R 7 is SO2NR 10a R 10b .

[2217] In some embodiments, R 7 is SO2R 10c .

[2218] In some embodiments, R 8 is selected to be H.

[2219] In some embodiments, R 8 is C 1-6 a straight-chain alkyl group.

[2220] In some embodiments, R8 is C 3-7 branched alkyl

[2221] In some embodiments, R 8 is C 3-7 cycloalkyl

[2222] In some embodiments, R 9 is C 1-6 linear alkyl

[2223] In some embodiments, R 9 is C 3-7 branched alkyl

[2224] In some embodiments, R 9 is C 3-7 cycloalkyl

[2225] In some embodiments, R 10a is H

[2226] In some embodiments, R 10a is C 1-6 linear alkyl

[2227] In some embodiments, R 10a is C 3-7 branched alkyl

[2228] In some embodiments, R 10a is C 3-7 cycloalkyl

[2229] In some embodiments, R 10b is H

[2230] In some embodiments, R 10b is C 1-6 linear alkyl

[2231] In some embodiments, R 10b is C 3-7 branched alkyl

[2232] In some embodiments, R 10b is C 3-7 cycloalkyl

[2233] In some embodiments, R 10c is C 1-6 linear alkyl

[2234] In some embodiments, R 10c is C 3-7 branched alkyl

[2235] In some embodiments, R10c is C 3-7 cycloalkyl

[2236] In some embodiments, R 10c is C 1-6 linear haloalkyl

[2237] In some embodiments, R 10c is C 3-7 branched haloalkyl

[2238] In some embodiments, R 10c is -(CH2) q CN

[2239] In some embodiments, R 10c is -(CH2) q SO2R 11 .

[2240] In some embodiments, R 10c is -(CH2) q OR 12 .

[2241] In some embodiments, R 10c is

[2242] In some embodiments, R 10c is

[2243] In some embodiments, R 10c is

[2244] In some embodiments, R 10c is

[2245] In some embodiments, R 10c is

[2246] In some embodiments, R 10c is

[2247] In some embodiments, R 10c is

[2248] In some embodiments, R 10c is

[2249] In some embodiments, R 10c is

[2250] In some embodiments, R 10c is

[2251] In some embodiments, R 10c is

[2252] In some embodiments, R 10c is

[2253] In some embodiments, R 11 is C 1-6 a straight-chain alkyl group.

[2254] In some embodiments, R 11 is C 3-7 a branched-chain alkyl group.

[2255] In some embodiments, R 11 is C 3-7 a cycloalkyl group.

[2256] In some embodiments, R 12 is C 1-6 a straight-chain alkyl group.

[2257] In some embodiments, R 12 is C 3-7 a branched-chain alkyl group.

[2258] In some embodiments, R 12 is C 3-7 a cycloalkyl group.

[2259] In some embodiments, R 1a is H.

[2260] In some embodiments, R 1a is OH.

[2261] In some embodiments, R 1a is NO2.

[2262] In some embodiments, R 1a is a halogen.

[2263] In some embodiments, R 1a is CN.

[2264] In some embodiments, R 1a is C 1-6 a straight-chain alkyl group.

[2265] In some embodiments, R 1a is C 3-7 a branched-chain alkyl group.

[2266] In some embodiments, R 1a is a C 3-7 cycloalkyl group.

[2267] In some embodiments, R 1a is a C 1-6 linear alkoxy group.

[2268] In some embodiments, R 1a is a C 3-7 branched alkoxy group.

[2269] In some embodiments, R 1a is a C 3-7 cycloalkoxy group.

[2270] In some embodiments, R 1a is a C 1-6 linear haloalkyl group.

[2271] In some embodiments, R 1a is a C 3-7 branched haloalkyl group.

[2272] In some embodiments, R 1a is a C 1-6 linear haloalkoxy group.

[2273] In some embodiments, R 1a is -S(C 1-6 linear alkyl).

[2274] In some embodiments, R 1a is S(C 3-7 branched alkyl).

[2275] In some embodiments, R 1a is -S(C 3-7 cycloalkyl).

[2276] In some embodiments, R 1a is COR 13 .

[2277] In some embodiments, R 1a is CO2R 14 .

[2278] In some embodiments, R 1a is CONR 15a R 15b .

[2279] In some embodiments, R 1a is SO2NR 15a R 15b .

[2280] In some embodiments, R 1a is NR 16a R 16b .

[2281] In some embodiments, R 1a is NR 16a COR 17 .

[2282] In some embodiments, R 1a is NR 16a SO2R 18 .

[2283] In some embodiments, R 1a is NR 16a SO2NR 19a R 19b .

[2284] In some embodiments, R 1b is H.

[2285] In some embodiments, R 1b is OH.

[2286] In some embodiments, R 1b is NO2.

[2287] In some embodiments, R 1b is a halogen.

[2288] In some embodiments, R 1b is CN.

[2289] In some embodiments, R 1b is C 1-6 a straight-chain alkyl.

[2290] In some embodiments, R 1b is C 3-7 a branched-chain alkyl.

[2291] In some embodiments, R 1b is C 3-7 a cycloalkyl.

[2292] In some embodiments, R 1b is C 1-6 a straight-chain alkoxy.

[2293] In some embodiments, R 1b is C 3-7 a branched-chain alkoxy.

[2294] In some embodiments, R 1bis C 3-7 cycloalkyloxy group.

[2295] In some embodiments, R 1b is C 1-6 linear haloalkyl.

[2296] In some embodiments, R 1b is C 3-7 branched haloalkyl.

[2297] In some embodiments, R 1b is C 1-6 linear haloalkyloxy group.

[2298] In some embodiments, R 1b is -S(C 1-6 linear alkyl).

[2299] In some embodiments, R 1b is S(C 3-7 branched alkyl).

[2300] In some embodiments, R 1b is -S(C 3-7 cycloalkyl).

[2301] In some embodiments, R 1b is COR 13 .

[2302] In some embodiments, R 1b is CO2R 14 .

[2303] In some embodiments, R 1b is CONR 15a R 15b .

[2304] In some embodiments, R 1b is SO2NR 15a R 15b .

[2305] In some embodiments, R 1b is NR 16a R 16b .

[2306] In some embodiments, R 1b is NR 16a COR 17 .

[2307] In some embodiments, R 1b is NR 16a SO2R 18 .

[2308] In some embodiments, R 1b is NR 16a SO2NR 19a R 19b .

[2309] In some embodiments, R 1c is H.

[2310] In some embodiments, R 1c is OH.

[2311] In some embodiments, R 1c is NO2.

[2312] In some embodiments, R 1c is a halogen.

[2313] In some embodiments, R 1c is CN.

[2314] In some embodiments, R 1c is C 1-6 a straight-chain alkyl.

[2315] In some embodiments, R 1c is C 3-7 a branched-chain alkyl.

[2316] In some embodiments, R 1c is C 3-7 a cycloalkyl.

[2317] In some embodiments, R 1c is C 1-6 a straight-chain alkoxy.

[2318] In some embodiments, R 1c is C 3-7 a branched-chain alkoxy.

[2319] In some embodiments, R 1c is C 3-7 a cycloalkoxy.

[2320] In some embodiments, R 1c is C 1-6 a straight-chain haloalkyl.

[2321] In some embodiments, R 1c is C 3-7 a branched-chain haloalkyl.

[2322] In some embodiments, R 1c is C 1-6 a straight-chain haloalkoxy.

[2323] In some embodiments, R 1c is - S(C 1-6 linear alkyl).

[2324] In some embodiments, R 1c is S(C 3-7 branched alkyl).

[2325] In some embodiments, R 1c is - S(C 3-7 cycloalkyl).

[2326] In some embodiments, R 1c is COR 13 .

[2327] In some embodiments, R 1c is CO2R 14 .

[2328] In some embodiments, R 1c is CONR 15a R 15b .

[2329] In some embodiments, R 1c is SO2NR 15a R 15b .

[2330] In some embodiments, R 1c is NR 16a R 16b .

[2331] In some embodiments, R 1c is NR 16a COR 17 .

[2332] In some embodiments, R 1c is NR 16a SO2R 18 .

[2333] In some embodiments, R 1c is NR 16a SO2NR 19a R 19b .

[2334] In some embodiments, R 1d is H.

[2335] In some embodiments, R 1d is OH.

[2336] In some embodiments, R 1dis NO2.

[2337] In some embodiments, R 1d is a halogen.

[2338] In some embodiments, R 1d is CN.

[2339] In some embodiments, R 1d is C 1-6 a straight-chain alkyl group.

[2340] In some embodiments, R 1d is C 3-7 a branched-chain alkyl group.

[2341] In some embodiments, R 1d is C 3-7 a cycloalkyl group.

[2342] In some embodiments, R 1d is C 1-6 a straight-chain alkoxy group.

[2343] In some embodiments, R 1d is C 3-7 a branched-chain alkoxy group.

[2344] In some embodiments, R 1d is C 3-7 a cycloalkoxy group.

[2345] In some embodiments, R 1d is C 1-6 a straight-chain haloalkyl group.

[2346] In some embodiments, R 1d is C 3-7 a branched-chain haloalkyl group.

[2347] In some embodiments, R 1d is C 1-6 a straight-chain haloalkoxy group.

[2348] In some embodiments, R 1d is -S(C 1-6 a straight-chain alkyl group).

[2349] In some embodiments, R 1d is S(C 3-7 a branched-chain alkyl group).

[2350] In some embodiments, R 1d is -S(C 3-7 a cycloalkyl group).

[2351] In some embodiments, R1d is COR 13 。

[2352] In some embodiments, R 1d is CO2R 14 。

[2353] In some embodiments, R 1d is CONR 15a R 15b 。

[2354] In some embodiments, R 1d is SO2NR 15a R 15b 。

[2355] In some embodiments, R 1d is NR 16a R 16b 。

[2356] In some embodiments, R 1d is NR 16a COR 17 。

[2357] In some embodiments, R 1d is NR 16a SO2R 18 。

[2358] In some embodiments, R 1d is NR 16a SO2NR 19a R 19b 。

[2359] In some embodiments, R 1e is H.

[2360] In some embodiments, R 1e is OH.

[2361] In some embodiments, R 1e is NO2.

[2362] In some embodiments, R 1e is halogen.

[2363] In some embodiments, R 1e is CN.

[2364] In some embodiments, R 1e is C 1-6 linear alkyl.

[2365] In some embodiments, R 1e is C 3-7Branched alkyl group.

[2366] In some embodiments, R 1e is C 3-7 Cycloalkyl group.

[2367] In some embodiments, R 1e is C 1-6 Straight-chain alkoxy group.

[2368] In some embodiments, R 1e is C 3-7 Branched alkoxy group.

[2369] In some embodiments, R 1e is C 3-7 Cycloalkoxy group.

[2370] In some embodiments, R 1e is C 1-6 Straight-chain haloalkyl group.

[2371] In some embodiments, R 1e is C 3-7 Branched haloalkyl group.

[2372] In some embodiments, R 1e is C 1-6 Straight-chain haloalkoxy group.

[2373] In some embodiments, R 1e is -S(C 1-6 Straight-chain alkyl group).

[2374] In some embodiments, R 1e is S(C 3-7 Branched alkyl group).

[2375] In some embodiments, R 1e is -S(C 3-7 Cycloalkyl group).

[2376] In some embodiments, R 1e is COR 13 .

[2377] In some embodiments, R 1e is CO2R 14 .

[2378] In some embodiments, R 1e is CONR 15a R 15b .

[2379] In some embodiments, R 1e is SO2NR 15a R15b 。

[2380] In some embodiments, R 1e is NR 16a R 16b 。

[2381] In some embodiments, R 1e is NR 16a COR 17 。

[2382] In some embodiments, R 1e is NR 16a SO2R 18 。

[2383] In some embodiments, R 1e is NR 16a SO2NR 19a R 19b 。

[2384] In some embodiments, R 13 is H.

[2385] In some embodiments, R 13 is C 1-6 linear alkyl.

[2386] In some embodiments, R 13 is C 3-7 branched alkyl.

[2387] In some embodiments, R 13 is C 3-7 cycloalkyl.

[2388] In some embodiments, R 14 is C 1-6 linear alkyl.

[2389] In some embodiments, R 14 is C 3-7 branched alkyl.

[2390] In some embodiments, R 14 is C 3-7 cycloalkyl.

[2391] In some embodiments, R 15a is H.

[2392] In some embodiments, R 15a is C 1-6 linear alkyl.

[2393] In some embodiments, R 15a is C3-7 Branched alkyl group.

[2394] In some embodiments, R 15a is C 3-7 Cycloalkyl group.

[2395] In some embodiments, R 15b is H.

[2396] In some embodiments, R 15b is C 1-6 Straight-chain alkyl group.

[2397] In some embodiments, R 15b is C 3-7 Branched alkyl group.

[2398] In some embodiments, R 15b is C 3-7 Cycloalkyl group.

[2399] In some embodiments, R 16a is H.

[2400] In some embodiments, R 16a is C 1-6 Straight-chain alkyl group.

[2401] In some embodiments, R 16a is C 3-7 Branched alkyl group.

[2402] In some embodiments, R 16a is C 3-7 Cycloalkyl group.

[2403] In some embodiments, R 16b is H.

[2404] In some embodiments, R 16b is C 1-6 Straight-chain alkyl group.

[2405] In some embodiments, R 16b is C 3-7 Branched alkyl group.

[2406] In some embodiments, R 16b is C 3-7 Cycloalkyl group.

[2407] In some embodiments, R 17 is H.

[2408] In some embodiments, R 17 is C 1-6 Straight-chain alkyl group.

[2409] In some embodiments, R 17 is a C 3-7 branched alkyl group.

[2410] In some embodiments, R 17 is a C 3-7 cycloalkyl group.

[2411] In some embodiments, R 18 is a C 1-6 linear alkyl group.

[2412] In some embodiments, R 18 is a C 3-7 branched alkyl group.

[2413] In some embodiments, R 18 is a C 3-7 cycloalkyl group.

[2414] In some embodiments, R 19a is a C 1-6 linear alkyl group.

[2415] In some embodiments, R 19a is a C 3-7 branched alkyl group.

[2416] In some embodiments, R 19a is a C 3-7 cycloalkyl group.

[2417] In some embodiments, R 19b is a C 1-6 linear alkyl group.

[2418] In some embodiments, R 19b is a C 3-7 branched alkyl group.

[2419] In some embodiments, R 19b is a C 3-7 cycloalkyl group.

[2420] In some embodiments, n is 1.

[2421] In some embodiments, n is 2.

[2422] In some embodiments, n is 3.

[2423] In some embodiments, n is 4.

[2424] In some embodiments, m is 1.

[2425] In some embodiments, m is 2.

[2426] In some embodiments, m is 3.

[2427] In some embodiments, R 20a is hydrogen.

[2428] In some embodiments, R 20a is -CN.

[2429] In some embodiments, R 20a is -NO2.

[2430] In some embodiments, R 20a is OH.

[2431] In some embodiments, R 20a is a halogen.

[2432] In some embodiments, R 20a is C 1-6 a straight-chain alkyl.

[2433] In some embodiments, R 20a is C 3-7 a branched-chain alkyl.

[2434] In some embodiments, R 20a is C 3-7 a cycloalkyl.

[2435] In some embodiments, R 20a is C 1-6 a straight-chain alkoxy.

[2436] In some embodiments, R 20a is C 3-7 a branched-chain alkoxy.

[2437] In some embodiments, R 20a is C 3-7 a cycloalkoxy.

[2438] In some embodiments, R 20a is C 1-6 a straight-chain haloalkyl.

[2439] In some embodiments, R 20a is C 3-7 a branched-chain haloalkyl.

[2440] In some embodiments, R 20a is C 1-6 a straight-chain haloalkoxy.

[2441] In some embodiments, R 20a is C 3-7 a branched-chain haloalkoxy.

[2442] In some embodiments, R 20a is SH.

[2443] In some embodiments, R 20a is SC 1-6 a straight-chain alkyl group.

[2444] In some embodiments, R 20a is SC 3-7 a branched-chain alkyl group.

[2445] In some embodiments, R 20a is SC 3-7 a cycloalkyl group.

[2446] In some embodiments, R 20a is SO2C 1-6 a straight-chain alkyl group.

[2447] In some embodiments, R 20a is SO2C 3-7 a branched-chain alkyl group.

[2448] In some embodiments, R 20a is SO2C 3-7 a cycloalkyl group.

[2449] In some embodiments, R 20a is SO2NH2.

[2450] In some embodiments, R 20a is SO2NHR 21 .

[2451] In some embodiments, R 20a is NHSO2R 22 .

[2452] In some embodiments, R 20a is -NR 23a R 23b .

[2453] In some embodiments, R 20a is NHC(O)R 24 .

[2454] In some embodiments, R 20a is C(O)NHR 24 .

[2455] In some embodiments, R 20a is C(O)N(R 24 )2.

[2456] In some embodiments, R20a is morpholino.

[2457] In some embodiments, R 20a is

[2458] In some embodiments, R 20b is hydrogen.

[2459] In some embodiments, R 20b is -CN.

[2460] In some embodiments, R 20b is -NO2.

[2461] In some embodiments, R 20b is -OH.

[2462] In some embodiments, R 20b is halogen.

[2463] In some embodiments, R 20b is C 1-6 linear alkyl.

[2464] In some embodiments, R 20b is C 3-7 branched alkyl.

[2465] In some embodiments, R 20b is C 3-7 cycloalkyl.

[2466] In some embodiments, R 20b is C 1-6 linear alkoxy.

[2467] In some embodiments, R 20b is C 3-7 branched alkoxy.

[2468] In some embodiments, R 20b is C 3-7 cycloalkoxy.

[2469] In some embodiments, R 20b is C 1-6 linear haloalkyl.

[2470] In some embodiments, R 20b is C 3-7 branched haloalkyl.

[2471] In some embodiments, R 20b is C 1-6 linear haloalkoxy.

[2472] In some embodiments, R 20b is a C 3-7 branched haloalkyloxy group.

[2473] In some embodiments, R 20b is SH.

[2474] In some embodiments, R 20b is SC 1-6 a straight-chain alkyl group.

[2475] In some embodiments, R 20b is SC 3-7 a branched alkyl group.

[2476] In some embodiments, R 20b is SC 3-7 a cycloalkyl group.

[2477] In some embodiments, R 20b is SO2C 1-6 a straight-chain alkyl group.

[2478] In some embodiments, R 20b is SO2C 3-7 a branched alkyl group.

[2479] In some embodiments, R 20b is SO2C 3-7 a cycloalkyl group.

[2480] In some embodiments, R 20b is SO2NH2.

[2481] In some embodiments, R 20b is SO2NHR 21 .

[2482] In some embodiments, R 20b is NHSO2R 22 .

[2483] In some embodiments, R 20b is -NR 23a R 23b .

[2484] In some embodiments, R 20b is NHC(O)R 24 .

[2485] In some embodiments, R 20b is C(O)NHR 24 .

[2486] In some embodiments, R 20b is C(O)N(R24 ) 2。

[2487] In some embodiments, R 20b is morpholino.

[2488] In some embodiments, R 20b is

[2489] In some embodiments, R 20c is hydrogen.

[2490] In some embodiments, R 20c is -CN.

[2491] In some embodiments, R 20c is -NO2.

[2492] In some embodiments, R 20c is -OH.

[2493] In some embodiments, R 20c is halogen.

[2494] In some embodiments, R 20c is C 1-6 linear alkyl.

[2495] In some embodiments, R 20c is C 3-7 branched alkyl.

[2496] In some embodiments, R 20c is C 3-7 cycloalkyl.

[2497] In some embodiments, R 20c is C 1-6 linear alkoxy.

[2498] In some embodiments, R 20c is C 3-7 branched alkoxy.

[2499] In some embodiments, R 20c is C 3-7 cycloalkoxy.

[2500] In some embodiments, R 20c is C 1-6 linear haloalkyl.

[2501] In some embodiments, R 20c is C 3-7 branched haloalkyl.

[2502] In some embodiments, R20c is C 1-6 a straight-chain haloalkyloxy group.

[2503] In some embodiments, R 20c is C 3-7 a branched-chain haloalkyloxy group.

[2504] In some embodiments, R 20c is SH.

[2505] In some embodiments, R 20c is SC 1-6 a straight-chain alkyl group.

[2506] In some embodiments, R 20c is SC 3-7 a branched-chain alkyl group.

[2507] In some embodiments, R 20c is SC 3-7 a cycloalkyl group.

[2508] In some embodiments, R 20c is SO2C 1-6 a straight-chain alkyl group.

[2509] In some embodiments, R 20c is SO2C 3-7 a branched-chain alkyl group.

[2510] In some embodiments, R 20c is SO2C 3-7 a cycloalkyl group.

[2511] In some embodiments, R 20c is SO2NH2.

[2512] In some embodiments, R 20c is SO2NHR 21 .

[2513] In some embodiments, R 20c is NHSO2R 22 .

[2514] In some embodiments, R 20c is -NR 23a R 23b .

[2515] In some embodiments, R 20c is NHC(O)R 24 .

[2516] In some embodiments, R 20c is C(O)NHR 24。

[2517] In some embodiments, R 20c is C(O)N(R 24 )2.

[2518] In some embodiments, R 20c is morpholino.

[2519] In some embodiments, R 20c is

[2520] In some embodiments, R 20d is hydrogen.

[2521] In some embodiments, R 20d is -CN.

[2522] In some embodiments, R 20d is -NO2.

[2523] In some embodiments, R 20d is -OH.

[2524] In some embodiments, R 20d is halogen.

[2525] In some embodiments, R 20d is C 1-6 a straight-chain alkyl.

[2526] In some embodiments, R 20d is C 3-7 a branched-chain alkyl.

[2527] In some embodiments, R 20d is C 3-7 a cycloalkyl.

[2528] In some embodiments, R 20d is C 1-6 a straight-chain alkoxy.

[2529] In some embodiments, R 20d is C 3-7 a branched-chain alkoxy.

[2530] In some embodiments, R 20d is C 3-7 a cycloalkoxy.

[2531] In some embodiments, R 20d is C 1-6 a straight-chain haloalkyl.

[2532] In some embodiments, R 20d is C3-7 Branched haloalkyl

[2533] In some embodiments, R 20d is a straight-chain haloalkoxy 1-6

[2534] In some embodiments, R 20d is a branched haloalkoxy 3-7

[2535] In some embodiments, R 20d is SH

[2536] In some embodiments, R 20d is SC 1-6 a straight-chain alkyl

[2537] In some embodiments, R 20d is SC 3-7 a branched alkyl

[2538] In some embodiments, R 20d is SC 3-7 a cycloalkyl

[2539] In some embodiments, R 20d is SO2C 1-6 a straight-chain alkyl

[2540] In some embodiments, R 20d is SO2C 3-7 a branched alkyl

[2541] In some embodiments, R 20d is SO2C 3-7 a cycloalkyl

[2542] In some embodiments, R 20d is SO2NH2

[2543] In some embodiments, R 20d is SO2NHR 21

[2544] In some embodiments, R 20d is NHSO2R 22

[2545] In some embodiments, R 20d is -NR 23a R 23b

[2546] In some embodiments, R 20d is NHC(O)R 24 ​​

[2547] In some embodiments, R 20d is C(O)NHR 24 .

[2548] In some embodiments, R 20d is C(O)N(R 24 )2.

[2549] In some embodiments, R 20d is morpholino.

[2550] In some embodiments, R 20d is

[2551] In some embodiments, R 20e is hydrogen.

[2552] In some embodiments, R 20e is -CN.

[2553] In some embodiments, R 20e is -NO2.

[2554] In some embodiments, R 20e is -OH.

[2555] In some embodiments, R 20e is halogen.

[2556] In some embodiments, R 20e is C 1-6 linear alkyl.

[2557] In some embodiments, R 20e is C 3-7 branched alkyl.

[2558] In some embodiments, R 20e is C 3-7 cycloalkyl.

[2559] In some embodiments, R 20e is C 1-6 linear alkoxy.

[2560] In some embodiments, R 20e is C 3-7 branched alkoxy.

[2561] In some embodiments, R 20e is C 3-7 cycloalkoxy.

[2562] In some embodiments, R 20e is C 1-6 linear haloalkyl.

[2563] In some embodiments, R 20e is a C 3-7 branched haloalkyl group.

[2564] In some embodiments, R 20e is a C 1-6 linear haloalkoxy group.

[2565] In some embodiments, R 20e is a C 3-7 branched haloalkoxy group.

[2566] In some embodiments, R 20e is SH.

[2567] In some embodiments, R 20e is SC 1-6 linear alkyl group.

[2568] In some embodiments, R 20e is SC 3-7 branched alkyl group.

[2569] In some embodiments, R 20e is SC 3-7 cycloalkyl group.

[2570] In some embodiments, R 20e is SO2C 1-6 linear alkyl group.

[2571] In some embodiments, R 20e is SO2C 3-7 branched alkyl group.

[2572] In some embodiments, R 20e is SO2C 3-7 cycloalkyl group.

[2573] In some embodiments, R 20e is SO2NH2.

[2574] In some embodiments, R 20e is SO2NHR 21 .

[2575] In some embodiments, R 20e is NHSO2R 22 .

[2576] In some embodiments, R 20e is -NR 23a R 23b .

[2577] In some embodiments, R 20e is NHC(O)R 24 .

[2578] In some embodiments, R 20e is C(O)NHR 24 .

[2579] In some embodiments, R 20e is C(O)N(R 24 )2.

[2580] In some embodiments, R 20e is morpholino.

[2581] In some embodiments, R 20e is

[2582] In some embodiments, R 20f is hydrogen.

[2583] In some embodiments, R 20f is -CN.

[2584] In some embodiments, R 20f is -NO2.

[2585] In some embodiments, R 20f is -OH.

[2586] In some embodiments, R 20f is halogen.

[2587] In some embodiments, R 20f is C 1-6 linear alkyl.

[2588] In some embodiments, R 20f is C 3-7 branched alkyl.

[2589] In some embodiments, R 20f is C 3-7 cycloalkyl.

[2590] In some embodiments, R 20f is C 1-6 linear alkoxy.

[2591] In some embodiments, R 20f is C 3-7 branched alkoxy.

[2592] In some embodiments, R 20f is C 3-7 cycloalkoxy.

[2593] In some embodiments, R 20f is a C 1-6 linear haloalkyl group.

[2594] In some embodiments, R 20f is a C 3-7 branched haloalkyl group.

[2595] In some embodiments, R 20f is a C 1-6 linear haloalkoxy group.

[2596] In some embodiments, R 20f is a C 3-7 branched haloalkoxy group.

[2597] In some embodiments, R 20f is SH.

[2598] In some embodiments, R 20f is SC 1-6 linear alkyl group.

[2599] In some embodiments, R 20f is SC 3-7 branched alkyl group.

[2600] In some embodiments, R 20f is SC 3-7 cycloalkyl group.

[2601] In some embodiments, R 20f is SO2C 1-6 linear alkyl group.

[2602] In some embodiments, R 20f is SO2C 3-7 branched alkyl group.

[2603] In some embodiments, R 20f is SO2C 3-7 cycloalkyl group.

[2604] In some embodiments, R 20f is SO2NH2.

[2605] In some embodiments, R 20f is SO2NHR 21 .

[2606] In some embodiments, R 20f is NHSO2R 22 .

[2607] In some embodiments, R 20f is -NR23a R 23b 。

[2608] In some embodiments, R 20f is NHC(O)R 24 。

[2609] In some embodiments, R 20f is C(O)NHR 24 。

[2610] In some embodiments, R 20f is C(O)N(R 24 )2.

[2611] In some embodiments, R 20f is morpholino.

[2612] In some embodiments, R 20f is

[2613] In some embodiments, R 20g is hydrogen.

[2614] In some embodiments, R 20g is -CN.

[2615] In some embodiments, R 20g is -NO2.

[2616] In some embodiments, R 20g is -OH.

[2617] In some embodiments, R 20g is halogen.

[2618] In some embodiments, R 20g is C 1-6 a straight-chain alkyl.

[2619] In some embodiments, R 20g is C 3-7 a branched-chain alkyl.

[2620] In some embodiments, R 20g is C 3-7 a cycloalkyl.

[2621] In some embodiments, R 20g is C 1-6 a straight-chain alkoxy.

[2622] In some embodiments, R 20g is C 3-7 a branched-chain alkoxy.

[2623] In some embodiments, R 20g is C 3-7 cycloalkyloxy.

[2624] In some embodiments, R 20g is C 1-6 linear haloalkyl.

[2625] In some embodiments, R 20g is C 3-7 branched haloalkyl.

[2626] In some embodiments, R 20g is C 1-6 linear haloalkyloxy.

[2627] In some embodiments, R 20g is C 3-7 branched haloalkyloxy.

[2628] In some embodiments, R 20g is SH.

[2629] In some embodiments, R 20g is SC 1-6 linear alkyl.

[2630] In some embodiments, R 20g is SC 3-7 branched alkyl.

[2631] In some embodiments, R 20g is SC 3-7 cycloalkyl.

[2632] In some embodiments, R 20g is SO2C 1-6 linear alkyl.

[2633] In some embodiments, R 20g is SO2C 3-7 branched alkyl.

[2634] In some embodiments, R 20g is SO2C 3-7 cycloalkyl.

[2635] In some embodiments, R 20g is SO2NH2.

[2636] In some embodiments, R 20g is SO2NHR 21 .

[2637] In some embodiments, R 20g is NHSO2R 22。

[2638] In some embodiments, R 20g is -NR 23a R 23b 。

[2639] In some embodiments, R 20g is NHC(O)R 24 。

[2640] In some embodiments, R 20g is C(O)NHR 24 。

[2641] In some embodiments, R 20g is C(O)N(R 24 )2.

[2642] In some embodiments, R 20g is morpholino.

[2643] In some embodiments, R 20g is

[2644] In some embodiments, R 21 is hydrogen.

[2645] In some embodiments, R 21 is C 1-6 linear alkyl.

[2646] In some embodiments, R 21 is C 3-7 branched alkyl.

[2647] In some embodiments, R 21 is C 3-7 cycloalkyl.

[2648] In some embodiments, R 22 is hydrogen.

[2649] In some embodiments, R 22 is C 1-6 linear alkyl.

[2650] In some embodiments, R 22 is C 3-7 branched alkyl.

[2651] In some embodiments, R 22 is C 3-7 cycloalkyl.

[2652] In some embodiments, R 23a is hydrogen.

[2653] In some embodiments, R 23a is a C 1-6 linear alkyl group.

[2654] In some embodiments, R 23a is a C 3-7 branched alkyl group.

[2655] In some embodiments, R 23a is a C 3-7 cycloalkyl group.

[2656] In some embodiments, R 23b is hydrogen.

[2657] In some embodiments, R 23b is a C 1-6 linear alkyl group.

[2658] In some embodiments, R 23b is a C 3-7 branched alkyl group.

[2659] In some embodiments, R 23b is a C 3-7 cycloalkyl group.

[2660] In some embodiments, R 24 is hydrogen.

[2661] In some embodiments, R 24 is a C 1-6 linear alkyl group.

[2662] In some embodiments, R 24 is a C 3-7 branched alkyl group.

[2663] In some embodiments, R 24 is a C 3-7 cycloalkyl group.

[2664] In some embodiments, R 25 is hydrogen.

[2665] In some embodiments, R 25 is a C 1-6 linear alkyl group.

[2666] In some embodiments, R 25 is a C 3-7 branched alkyl group.

[2667] In some embodiments, R 25 is a C 3-7 cycloalkyl group.

[2668] In some embodiments, Q1 is 1.

[2669] In some embodiments, Q 1 is 2.

[2670] In some embodiments, Q 2 is 1.

[2671] In some embodiments, Q 2 is 2.

[2672] In some embodiments, X 1 is O.

[2673] In some embodiments, X 1 is S.

[2674] In some embodiments, X 1 is SO.

[2675] In some embodiments, X 1 is SO2.

[2676] In some embodiments, X 1 is NR 7 .

[2677] Exemplary compounds

[2678] Exemplary compounds include any of the compounds described herein. In embodiments where the configuration of the lactam stereocenter (i.e., the carbon substituted by the nitrogen of the lactam) is not specified in the compounds or formulas described herein, the lactam stereocenter can have the R-configuration. In other embodiments, the lactam stereocenter can have the S-configuration.

[2679] In embodiments, the compound is any of the compounds described herein or a pharmaceutically acceptable salt thereof. In embodiments, the compound or its pharmaceutically acceptable salt is described in any of Tables 1 to 39. In embodiments, the compound is the compound described in any of Tables 34 to 39 or a pharmaceutically acceptable salt thereof.

[2680] Exemplary embodiments include compounds having the formula (II)

[2681]

[2682] or in the form of a pharmaceutically acceptable salt thereof, as defined in Table 1 below.

[2683] Table 1:

[2684]

[2685]

[2686]

[2687]

[2688]

[2689]

[2690]

[2691] Exemplary embodiments include compounds having the formula (VIII)

[2692]

[2693] or a pharmaceutically acceptable salt form thereof, as defined in Table 2 below.

[2694] Table 2

[2695]

[2696]

[2697]

[2698]

[2699] Exemplary embodiments include compounds having the formula (IX)

[2700]

[2701] or a pharmaceutically acceptable salt form thereof, as defined in Table 3 below.

[2702] Table 3

[2703]

[2704]

[2705]

[2706]

[2707] Exemplary embodiments include compounds having the formula (X)

[2708]

[2709] or a pharmaceutically acceptable salt form thereof, as defined in Table 4 below.

[2710] Table 4

[2711]

[2712]

[2713]

[2714]

[2715] Exemplary embodiments include compounds having the formula (XI)

[2716]

[2717] or a pharmaceutically acceptable salt form thereof, as defined in Table 5 below.

[2718] Table 5

[2719]

[2720]

[2721]

[2722]

[2723] Exemplary embodiments include compounds having the formula (XII)

[2724]

[2725] or a pharmaceutically acceptable salt form thereof, as defined in Table 6 below.

[2726] Table 6:

[2727]

[2728]

[2729]

[2730]

[2731]

[2732]

[2733]

[2734] Exemplary embodiments include compounds having the formula (XIII)

[2735]

[2736] or a pharmaceutically acceptable salt thereof, as defined in Table 7 below

[2737] Table 7:

[2738]

[2739]

[2740]

[2741]

[2742]

[2743] Exemplary embodiments include compounds having formula (XIV)

[2744]

[2745] or a pharmaceutically acceptable salt thereof, as defined in Table 8 below.

[2746] Table 8:

[2747]

[2748]

[2749]

[2750]

[2751] Exemplary embodiments include compounds having formula (XV)

[2752]

[2753] or a pharmaceutically acceptable salt thereof, as defined in Table 9 below.

[2754] Table 9:

[2755]

[2756]

[2757]

[2758]

[2759]

[2760] Exemplary embodiments include compounds having formula (XVI)

[2761]

[2762] or a pharmaceutically acceptable salt form thereof, as defined in Table 10 below.

[2763] Table 10:

[2764]

[2765]

[2766]

[2767]

[2768] Exemplary embodiments include compounds having formula (XVII)

[2769]

[2770] or a pharmaceutically acceptable salt form thereof, as defined in Table 11 below.

[2771] Table 11:

[2772]

[2773]

[2774]

[2775]

[2776]

[2777]

[2778]

[2779]

[2780] Exemplary embodiments include compounds having formula (XVIII)

[2781]

[2782] or a pharmaceutically acceptable salt form thereof, as defined in Table 12 below

[2783] Table 12:

[2784]

[2785]

[2786]

[2787]

[2788] Exemplary embodiments include compounds having formula (XIX)

[2789]

[2790] or a pharmaceutically acceptable salt thereof, as defined in Table 13 below.

[2791] Table 13:

[2792]

[2793]

[2794]

[2795]

[2796] Exemplary embodiments include compounds having formula (XX)

[2797]

[2798] or a pharmaceutically acceptable salt thereof, as defined in Table 14 below.

[2799] Table 14:

[2800]

[2801]

[2802]

[2803]

[2804] Exemplary embodiments include compounds having formula (XXI)

[2805]

[2806] or a pharmaceutically acceptable salt thereof, as defined in Table 15 below.

[2807] Table 15:

[2808]

[2809]

[2810]

[2811]

[2812] Exemplary embodiments include compounds having the formula (XXII)

[2813]

[2814] or a pharmaceutically acceptable salt thereof, as defined in Table 16 below.

[2815] Table 16:

[2816]

[2817]

[2818]

[2819]

[2820]

[2821]

[2822]

[2823]

[2824]

[2825]

[2826]

[2827]

[2828]

[2829]

[2830]

[2831]

[2832]

[2833]

[2834]

[2835]

[2836]

[2837]

[2838]

[2839]

[2840]

[2841]

[2842]

[2843]

[2844]

[2845]

[2846] Exemplary embodiments include compounds having formula (XXIII)

[2847]

[2848] or a pharmaceutically acceptable salt form thereof, as defined in Table 17 below.

[2849] Table 17:

[2850]

[2851]

[2852]

[2853]

[2854]

[2855]

[2856]

[2857]

[2858]

[2859]

[2860]

[2861]

[2862]

[2863]

[2864]

[2865]

[2866]

[2867]

[2868]

[2869]

[2870]

[2871]

[2872]

[2873]

[2874]

[2875]

[2876]

[2877]

[2878]

[2879]

[2880] Exemplary embodiments include compounds having the formula (XXIV)

[2881]

[2882] or a pharmaceutically acceptable salt form thereof, as defined in Table 18 below.

[2883] Table 18:

[2884]

[2885]

[2886]

[2887]

[2888]

[2889]

[2890]

[2891]

[2892]

[2893]

[2894]

[2895]

[2896]

[2897]

[2898]

[2899]

[2900]

[2901]

[2902]

[2903]

[2904]

[2905]

[2906]

[2907]

[2908]

[2909]

[2910]

[2911]

[2912]

[2913]

[2914] Exemplary embodiments include compounds having formula (XXV)

[2915]

[2916] or a pharmaceutically acceptable salt form thereof, as defined in Table 19 below.

[2917] Table 19:

[2918]

[2919]

[2920]

[2921]

[2922]

[2923]

[2924]

[2925]

[2926]

[2927]

[2928]

[2929]

[2930]

[2931]

[2932]

[2933]

[2934]

[2935]

[2936]

[2937]

[2938]

[2939]

[2940]

[2941]

[2942]

[2943]

[2944]

[2945]

[2946]

[2947]

[2948]

[2949]

[2950]

[2951]

[2952]

[2953]

[2954] Exemplary embodiments include compounds having the formula (XXVI)

[2955]

[2956] or a pharmaceutically acceptable salt form thereof, as defined in Table 20 below.

[2957] Table 20:

[2958]

[2959]

[2960]

[2961]

[2962]

[2963]

[2964]

[2965]

[2966]

[2967]

[2968]

[2969]

[2970]

[2971]

[2972]

[2973]

[2974]

[2975]

[2976]

[2977]

[2978]

[2979]

[2980]

[2981]

[2982]

[2983]

[2984]

[2985]

[2986]

[2987]

[2988]

[2989]

[2990]

[2991]

[2992]

[2993]

[2994] Exemplary embodiments include compounds having formula (XXVII)

[2995]

[2996] or a pharmaceutically acceptable salt form thereof, as defined in Table 21 below.

[2997] Table 21:

[2998]

[2999]

[3000]

[3001]

[3002]

[3003]

[3004]

[3005]

[3006]

[3007]

[3008]

[3009]

[3010]

[3011]

[3012]

[3013]

[3014]

[3015]

[3016]

[3017]

[3018]

[3019]

[3020]

[3021]

[3022]

[3023]

[3024]

[3025]

[3026]

[3027]

[3028]

[3029]

[3030]

[3031]

[3032]

[3033]

[3034] Exemplary embodiments include compounds having the formula (XXVIII)

[3035]

[3036] or a pharmaceutically acceptable salt form thereof, as defined in Table 22 below.

[3037] Table 22:

[3038]

[3039]

[3040]

[3041]

[3042]

[3043]

[3044]

[3045]

[3046]

[3047]

[3048]

[3049]

[3050]

[3051]

[3052]

[3053]

[3054]

[3055]

[3056]

[3057]

[3058]

[3059]

[3060]

[3061]

[3062]

[3063]

[3064]

[3065]

[3066]

[3067]

[3068]

[3069]

[3070]

[3071]

[3072]

[3073]

[3074] Exemplary embodiments include compounds having formula (XXIX)

[3075]

[3076] or a pharmaceutically acceptable salt form thereof, as defined in Table 23 below.

[3077] Table 23:

[3078]

[3079]

[3080]

[3081]

[3082]

[3083]

[3084]

[3085]

[3086]

[3087]

[3088]

[3089]

[3090]

[3091]

[3092]

[3093]

[3094]

[3095]

[3096]

[3097]

[3098]

[3099]

[3100]

[3101]

[3102]

[3103]

[3104]

[3105]

[3106]

[3107]

[3108]

[3109]

[3110]

[3111]

[3112]

[3113]

[3114] Exemplary embodiments include a compound having the formula (XXX)

[3115]

[3116] or a pharmaceutically acceptable salt form thereof, as defined in Table 24 below.

[3117] Table 24:

[3118]

[3119]

[3120]

[3121]

[3122]

[3123]

[3124]

[3125]

[3126]

[3127]

[3128]

[3129]

[3130]

[3131]

[3132]

[3133]

[3134]

[3135]

[3136]

[3137]

[3138]

[3139]

[3140]

[3141]

[3142]

[3143]

[3144]

[3145]

[3146]

[3147]

[3148]

[3149]

[3150]

[3151]

[3152]

[3153]

[3154] Exemplary embodiments include compounds having formula (XXXI)

[3155]

[3156] or a pharmaceutically acceptable salt form thereof, as defined in Table 25 below.

[3157] Table 25:

[3158]

[3159]

[3160]

[3161]

[3162]

[3163]

[3164]

[3165]

[3166]

[3167]

[3168]

[3169]

[3170]

[3171]

[3172]

[3173]

[3174]

[3175]

[3176]

[3177] Exemplary embodiments include compounds having the formula (XXXII)

[3178]

[3179] or a pharmaceutically acceptable salt form thereof, as defined in Table 26 below.

[3180] Table 26:

[3181]

[3182]

[3183]

[3184]

[3185]

[3186]

[3187]

[3188]

[3189]

[3190]

[3191]

[3192]

[3193]

[3194]

[3195]

[3196]

[3197]

[3198]

[3199]

[3200] Exemplary embodiments include compounds having formula (XXXIV)

[3201]

[3202] or a pharmaceutically acceptable salt form thereof, as defined in Table 27 below.

[3203] Table 27:

[3204]

[3205]

[3206]

[3207]

[3208]

[3209]

[3210]

[3211]

[3212]

[3213]

[3214]

[3215]

[3216]

[3217]

[3218]

[3219]

[3220]

[3221]

[3222]

[3223] Exemplary embodiments include compounds having the formula (XXXV)

[3224]

[3225] or a pharmaceutically acceptable salt form thereof, as defined in Table 28 below.

[3226] Table 28:

[3227]

[3228]

[3229]

[3230]

[3231]

[3232]

[3233]

[3234]

[3235]

[3236]

[3237]

[3238]

[3239]

[3240]

[3241] Exemplary embodiments include compounds having the formula (XXXVI)

[3242]

[3243] or a pharmaceutically acceptable salt form thereof, as defined in Table 29 below.

[3244] Table 29:

[3245]

[3246]

[3247]

[3248]

[3249]

[3250]

[3251]

[3252]

[3253]

[3254]

[3255]

[3256]

[3257]

[3258]

[3259] Exemplary embodiments include compounds having the formula (XXXVII)

[3260]

[3261] or a pharmaceutically acceptable salt form thereof, as defined in Table 30 below.

[3262] Table 30:

[3263]

[3264]

[3265]

[3266]

[3267]

[3268]

[3269]

[3270]

[3271]

[3272]

[3273]

[3274]

[3275]

[3276]

[3277] Exemplary embodiments include compounds having the formula (XXXVIII)

[3278]

[3279] or a pharmaceutically acceptable salt form thereof, as defined in Table 31 below

[3280] Table 31:

[3281]

[3282]

[3283]

[3284]

[3285]

[3286]

[3287]

[3288]

[3289]

[3290]

[3291]

[3292]

[3293]

[3294]

[3295]

[3296]

[3297]

[3298]

[3299]

[3300]

[3301]

[3302]

[3303]

[3304]

[3305]

[3306]

[3307]

[3308]

[3309]

[3310]

[3311]

[3312]

[3313]

[3314]

[3315]

[3316]

[3317]

[3318]

[3319]

[3320]

[3321]

[3322]

[3323]

[3324]

[3325]

[3326]

[3327]

[3328]

[3329]

[3330]

[3331]

[3332]

[3333]

[3334]

[3335]

[3336]

[3337]

[3338]

[3339]

[3340]

[3341]

[3342]

[3343]

[3344]

[3345]

[3346]

[3347]

[3348]

[3349]

[3350]

[3351]

[3352]

[3353]

[3354]

[3355]

[3356]

[3357]

[3358]

[3359]

[3360] Exemplary embodiments include a compound having the formula (XXXIX)

[3361]

[3362] or a pharmaceutically acceptable salt form thereof, as defined in Table 32 below.

[3363] Table 32:

[3364]

[3365]

[3366]

[3367]

[3368]

[3369]

[3370]

[3371]

[3372]

[3373]

[3374]

[3375]

[3376]

[3377]

[3378]

[3379]

[3380]

[3381]

[3382]

[3383]

[3384]

[3385]

[3386]

[3387]

[3388]

[3389]

[3390]

[3391]

[3392]

[3393]

[3394]

[3395]

[3396]

[3397]

[3398]

[3399]

[3400]

[3401]

[3402]

[3403]

[3404]

[3405]

[3406]

[3407]

[3408]

[3409]

[3410]

[3411]

[3412]

[3413]

[3414]

[3415]

[3416]

[3417] Exemplary embodiments include compounds having the formula (XXXX)

[3418]

[3419] or a pharmaceutically acceptable salt form thereof, as defined in Table 33 below.

[3420] Table 33:

[3421]

[3422]

[3423]

[3424]

[3425]

[3426]

[3427]

[3428]

[3429]

[3430]

[3431]

[3432]

[3433]

[3434]

[3435]

[3436]

[3437]

[3438]

[3439]

[3440]

[3441]

[3442]

[3443]

[3444]

[3445]

[3446]

[3447]

[3448]

[3449]

[3450]

[3451]

[3452]

[3453]

[3454]

[3455]

[3456]

[3457]

[3458]

[3459]

[3460]

[3461]

[3462]

[3463]

[3464]

[3465]

[3466]

[3467]

[3468]

[3469]

[3470]

[3471]

[3472]

[3473]

[3474]

[3475] For purposes of showing the manner in which the compounds of the present invention are named and referred to herein, a compound having the formula:

[3476]

[3477] The chemical name is 8-(methylsulfonyl)-3-(2-(4-phenylpiperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one.

[3478] For purposes of showing the manner in which the compounds of the present invention are named and referred to herein, a compound having the formula:

[3479]

[3480] The chemical name is 8-(methylsulfonyl)-3-(2-(5-phenylhexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one.

[3481] For purposes of showing the manner in which the compounds of the present invention are named and referred to herein, a compound having the formula:

[3482]

[3483] The chemical name is 8-(methylsulfonyl)-3-(2-(4-phenylpiperidin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one.

[3484] For purposes of the present invention, compounds depicted as racemates, e.g.:

[3485]

[3486] will likewise represent either of the two enantiomers having the formula:

[3487]

[3488] or the formula:

[3489]

[3490] or a mixture thereof, or, in the presence of a second chiral center, all diastereomers.

[3491] In all embodiments provided herein, examples of suitable optional substituents are not intended to limit the scope of the claimed invention. The compounds of the present invention may contain any substituent or combination of substituents provided herein.

[3492] Method for preparing the 5 - hydroxytryptamine receptor 7 activity modulator of the present invention

[3493] The present invention also relates to a method for preparing the 5 - hydroxytryptamine receptor 7 activity modulator of the present invention.

[3494] The compounds of the present teachings can be prepared from commercially available starting materials, compounds known in the literature, or readily prepared intermediates by standard synthetic methods and procedures known to those skilled in the art, in accordance with the procedures outlined herein. Standard synthetic methods and procedures for the preparation of organic molecules and for the transformation and manipulation of functional groups can be readily obtained from relevant scientific literature or standard textbooks in the art. It should be understood that, given typical or preferred process conditions (i.e., reaction temperature, time, molar ratio of reactants, solvent, pressure, etc.), other process conditions can also be used unless otherwise stated. The optimal reaction conditions can vary depending on the specific reactants or solvents used, but such conditions can be determined by those skilled in the art through routine optimization procedures. Those skilled in the art of organic synthesis will recognize that the nature and order of the proposed synthetic steps can be varied in order to optimize the formation of the compounds described herein.

[3495] The methods described herein can be monitored according to any suitable method known in the art. For example, product formation can be monitored by spectroscopic means such as nuclear magnetic resonance spectroscopy (e.g., 1 H or 13 C), infrared spectroscopy, spectrophotometry (e.g., UV - visible light), mass spectrometry, or by chromatography such as high - performance liquid chromatography (HPLC), gas chromatography (GC), gel permeation chromatography (GPC), or thin - layer chromatography (TLC).

[3496] The preparation of compounds can involve the protection and de - protection of various chemical groups. Those skilled in the art can readily determine the need for protection and de - protection and the selection of appropriate protecting groups. The chemistry of protecting groups can be found, for example, in Greene et al., Protective Groups in Organic Synthesis, 2nd Edition (Wiley & Sons, 1991), the entire disclosure of which is incorporated herein by reference for all purposes.

[3497] The reactions or methods described herein can be carried out in a suitable solvent, which can be readily selected by those skilled in the art of organic synthesis. Suitable solvents are generally substantially non - reactive with the reactants, intermediates, and / or products at the temperature at which the reaction is carried out, which temperature can be within the range from the freezing temperature to the boiling temperature of the solvent. A given reaction can be carried out in one solvent or a mixture of more than one solvent. The solvent suitable for a particular reaction step can be selected according to the specific reaction step.

[3498] The compounds of these teachings can be prepared by methods known in the field of organic chemistry. The reagents for preparing the compounds of these teachings can be obtained commercially or can be prepared by standard procedures described in the literature. For example, the compounds of the present invention can be prepared according to the methods shown in the general synthetic scheme:

[3499] General synthetic scheme for preparing compounds

[3500] The reagents for preparing the compounds of the present invention can be obtained commercially or can be prepared by standard procedures described in the literature. According to the present invention, the compounds in the genus can be prepared by one of the following reaction schemes. Accordingly, the present invention is also characterized by any synthetic intermediate or method as described herein.

[3501] The compounds of the present disclosure can be prepared according to the method outlined in Scheme 1.

[3502]

[3503] In the presence of BnNEt3Cl, in the presence of a base such as potassium carbonate, sodium carbonate, cesium carbonate, lithium carbonate, sodium hydroxide, potassium hydroxide, cesium hydroxide, lithium hydroxide, etc., in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, acetonitrile, methanol, ethanol, isopropanol, N,N-dimethylformamide, N,N-dimethylacetamide, dimethyl sulfoxide, etc., optionally by heating, optionally by microwave irradiation, reacting a suitably substituted compound of formula (1) (a known compound or a compound prepared by a known method, wherein PG is a protecting group selected from the group consisting of benzyl, tert-butyl carbonate, benzyl carbonate, and tert-butyldimethylsilyl) with a compound of formula (2) (a known compound or a compound prepared by a known method) to obtain a compound of formula (3). In the presence of a base such as pyridine, 2,6-dimethylpyridine, 2,6-di-tert-butylpyridine, triethylamine, diisopropylethylamine, etc., in a solvent such as dichloromethane, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethyl sulfoxide, etc., optionally by heating, optionally by microwave irradiation, reacting the compound of formula (3) with a compound of formula (4) (a known compound or a compound prepared by a known method, wherein Z 1React with a group selected from methyl, trifluoromethyl, p-tolyl and p-NO2-phenyl) to obtain a compound of formula (5). In a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethyl sulfoxide, etc., optionally by heating, optionally by microwave irradiation, react the compound of formula (5) with a base such as potassium carbonate, sodium carbonate, cesium carbonate, lithium carbonate, etc. to obtain a compound of formula (6).

[3504]

[3505] In the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, etc., in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, etc., optionally by heating, optionally by microwave irradiation, react the compound of formula (6) with a compound of formula (7) (a known compound or a compound prepared by a known method) to obtain a compound of formula (8). In a solvent such as benzene, toluene, p-xylene, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethyl sulfoxide, etc., optionally by heating, optionally by microwave irradiation, react the compound of formula (8) with an acid such as hydrochloric acid, hydrobromic acid, sulfuric acid, p-toluenesulfonic acid, acetic acid, trifluoroacetic acid, etc. to obtain a compound of formula (9). In the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, etc., in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, etc., optionally by heating, optionally by microwave irradiation, react the compound of formula (9) with a compound of formula (10) (a known compound or a compound prepared by a known method, where LG is selected from the group consisting of bromine, chlorine, methanesulfonate, p-toluenesulfonate) to obtain a compound of formula (11).

[3506] Scheme 3

[3507]

[3508] In the presence of naphthalene, in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, etc., optionally by heating, optionally by microwave irradiation, the compound of formula (11) is reacted with sodium to obtain the compound of formula (12). In the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium(II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis(triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)palladium(II) dichloride, etc., in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, etc., optionally by heating, the compound of formula (12) is reacted with hydrogen to obtain the compound of formula (13). Alternatively, in a solvent such as tetrahydrofuran, 1,4-dioxane, dichloromethane, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, etc., optionally by heating, optionally by microwave irradiation, the compound of formula (12) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, etc. to obtain the compound of formula (13). Alternatively, in a solvent such as tetrahydrofuran, 1,4-dioxane, dichloromethane, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, etc., optionally by heating, optionally by microwave irradiation, the compound of formula (12) is reacted with tetrabutylammonium fluoride to obtain the compound of formula (13). In the presence of triphenylphosphine, in a solvent such as dichloromethane, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, etc., optionally by heating, optionally by microwave irradiation, the compound of formula (13) is reacted with carbon tetrabromide to obtain the compound of formula (14). In the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, etc., in a solvent such as dichloromethane, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, etc., optionally by heating, optionally by microwave irradiation, the compound of formula (14) is reacted with the compound of formula (15) (a known compound or a compound prepared by a known method) to obtain the compound of formula (16).

[3509]

[3510] In the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, etc., in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, etc., optionally by heating, optionally by microwave irradiation, the compound of formula (6) is reacted with the compound of formula (17) (a known compound or a compound prepared by a known method) to obtain the compound of formula (18). In a solvent such as benzene, toluene, p-xylene, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethyl sulfoxide, etc., optionally by heating, optionally by microwave irradiation, the compound of formula (18) is reacted with an acid such as hydrochloric acid, hydrobromic acid, sulfuric acid, p-toluenesulfonic acid, acetic acid, trifluoroacetic acid, etc. to obtain the compound of formula (19). In the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, etc., in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, etc., optionally by heating, optionally by microwave irradiation, the compound of formula (19) is reacted with the compound of formula (20) (a known compound or a compound prepared by a known method, wherein LG is selected from the group consisting of bromine, chlorine, methanesulfonate, p-toluenesulfonate) to obtain the compound of formula (21). In the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, etc., in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, etc., optionally by heating, optionally by microwave irradiation, the compound of formula (21) is reacted with the compound of formula (22) (a known compound or a compound prepared by a known method, wherein LG is selected from the group consisting of bromine, chlorine, methanesulfonate, p-toluenesulfonate) to obtain the compound of formula (11).

[3511] Scheme 5

[3512]

[3513] In the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, etc., in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, etc., optionally by heating, optionally by microwave irradiation, a compound of formula (19) is reacted with a compound of formula (23) (a known compound or a compound prepared by a known method, where LG is selected from the group consisting of bromine, chlorine, mesylate, p-toluenesulfonate, and where Q 1 is selected from the group consisting of 1 and 2) to obtain a compound of formula (24). In the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, etc., in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, etc., optionally by heating, optionally by microwave irradiation, a compound of formula (24) is reacted with a compound of formula (25) (a known compound or a compound prepared by a known method, where LG is selected from the group consisting of bromine, chlorine, mesylate, p-toluenesulfonate, and where Q 2React with a group selected from 1 and 2) to obtain the compound of formula (26). In the presence of a solvent such ...

Claims

1. A compound having the formula (I): including its enantiomers, diastereomers, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes, wherein: A is selected from the group consisting of ; R 1 selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl; R 2 selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl; or R 1 and R 2 together with the atoms to which they are bonded form a ring having 5 to 7 ring atoms, said ring optionally containing double bonds; or R 1 and R 2 together with the atoms to which they are bonded form a ring having 6 to 8 ring atoms, said ring atoms comprising moieties selected from the group consisting of O, S, SO, SO2, and NR 7 constituting the group; R 3 selected from the group consisting of optionally substituted phenyl, optionally substituted naphthalen-1-yl, optionally substituted naphthalen-2-yl, optionally substituted pyridin-2-yl, optionally substituted pyridin-3-yl, optionally substituted pyridin-4-yl, and the like; R 4 selected from the group consisting of optionally substituted phenyl, optionally substituted naphthalen-1-yl, optionally substituted naphthalen-2-yl, optionally substituted pyridin-2-yl, optionally substituted pyridin-3-yl, optionally substituted pyridin-4-yl, and the like; R 5 selected from the group consisting of optionally substituted phenyl, optionally substituted naphthalen-1-yl, optionally substituted naphthalen-2-yl, optionally substituted pyridin-2-yl, optionally substituted pyridin-3-yl, optionally substituted pyridin-4-yl, and the like; R 6 selected from the group consisting of an optionally substituted phenyl, an optionally substituted naphthalen-1-yl, an optionally substituted naphthalen-2-yl, an optionally substituted 2-pyridyl, an optionally substituted 3-pyridyl, and an optionally substituted 4-pyridyl; R 7 selected from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, optionally substituted phenyl, optionally substituted benzyl, COR 8 , CO2R 9 , CONR 10a R 10b , SO2NR 10a R 10b and SO2R 10c ; R 8 selected from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl; R 9 selected from the group consisting of C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 10a selected from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 10b selected from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 10c selected from C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, -(CH2) q CN, -(CH2) q SO2R 11 、-(CH2) q OR 12 、 group consisting of; R 11 selected from the group consisting of C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 12 selected from the group consisting of C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 1a 、R 1b 、R 1c 、R 1d and R 1e are each independently selected from the group consisting of H, OH, NO2, halogen, CN, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, -S(C 1-6 linear alkyl), S(C 3-7 branched alkyl), -S(C 3-7 cycloalkyl), COR 13 、CO2R 14 、CONR 15a R 15b 、SO2NR 15a R 15b 、NR 16a R 16b 、NR 16a COR 17 、NR 16a SO2R 18 and NR 16a SO2NR 19a R 19b ; R 13 each occurrence independently selected from the group consisting of H, C 1-6 a straight-chain alkyl group, C 3-7 a branched-chain alkyl group, and a C3-7 cycloalkyl group; R 14 independently selected from the group consisting of C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 15a independently selected from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 15b independently selected from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl; each time it appears R 16a independently selected from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 16b each occurrence independently selected from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 17 independently selected from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl and C3-7 cycloalkyl each time it appears; R 18 independently selected from the group consisting of C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 19a independently selected from the group consisting of C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 19b independently selected from the group consisting of C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; n is 1, 2, 3 or 4; m is 1, 2 or 3.

2. The compound according to claim 1, wherein: A is Each R 1 and R 2 is independently C 1-6 a straight-chain alkyl or C 3-7 a branched-chain alkyl; or R 1 and R 2 together with the atoms to which they are bonded form a 5- to 8-membered ring, wherein said 5- to 8-membered ring is saturated or contains a carbon-carbon double bond and / or a ring atom O, S, SO, SO2 or NR 7 ; Each R 3 , R 4 and R 5 is independently an optionally substituted phenyl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl or optionally substituted 4-pyridyl; R 6 independently optionally substituted phenyl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl or optionally substituted 4-pyridyl; R 7 independently H, C 1-6 linear alkyl, C 3-7 branched alkyl, COR 8 or SO2R 10c ; R 8 selected from the group consisting of H, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 10c is C 1-6 a straight-chain alkyl or C 3-7 a branched-chain alkyl; n is 1, 2, 3 or 4; and m is 1, 2 or 3.

3. The compound according to claim 1 or 2, wherein n is 1, 2 or 3.

4. The compound according to any one of claims 1 to 3, having the formula (II): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes.

5. The compound according to claim 4, having the formula (XXXXII): or a pharmaceutically acceptable salt thereof.

6. The compound according to claim 4, having the formula (XXXXIII): or a pharmaceutically acceptable salt thereof.

7. The compound according to claim 1, having the formula (IIa): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、 R 20b 、 R 20c 、 R 20d and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、 NHSO2R 22 、 -NR 23a R 23b 、 NHC(O)R 24 、 C(O)NHR 24 、 R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 22 independently selected from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched-chain alkyl and C 3-7 cycloalkyl at each occurrence; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 24 Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; And R 20a 、R 20b 、R 20c 、R 20d and R 20e At least three of them are hydrogen.

8. The compound according to claim 1, having the formula (IIe): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、 R 20b 、 R 20c and R 20d are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、 NHSO2R 22 、 -NR 23a R 23b 、 NHC(O)R 24 、 C(O)NHR 24 、 C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; and R 20a 、R 20b 、R 20c and R 20d at least three of which are hydrogen.

9. The compound according to claim 1, having the formula (IIi): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、 R 20b 、 R 20c and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、 NHSO2R 22 、 -NR 23a R 23b 、 NHC(O)R 24 、 C(O)NHR 24 、 C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 23b Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; And R 20a 、R 20b 、R 20c and R 20e At least two of them are hydrogen.

10. The compound according to claim 1, having the formula (IIm): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、 R 20b 、 R 20cd and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、 NHSO2R 22 、 -NR 23a R 23b 、 NHC(O)R 24 、 C(O)NHR 24 、 C(O)N(R 24 )2, morpholino and the group consisting of; R 21 Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched-chain alkyl, and C 3-7 cycloalkyl; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23a Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 25 Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; And R 20a 、R 20b 、R 20c and R 20d at least three of which are hydrogen.

11. The compound according to claim 1, having the formula (IIq): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 23a Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; And R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g at least five of which are hydrogen.

12. The compound according to claim 1, having the formula (IIu): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; And R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g at least five of which are hydrogen.

13. The compound according to claim 1, having the formula (III): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes.

14. The compound according to claim 1, having the formula (IIIa): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、R 20b 、R 20c 、R 20d and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of; R 21 Independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 23a Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; And R 20a 、R 20b 、R 20c 、R 20d and R 20e At least three of them are hydrogen.

15. The compound according to claim 1, having the formula (IIIe): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a , R 20b , R 20c and R 20d independently selected from hydrogen, -CN, -NO2, -OH, halogen, C 1-6 Straight chain alkyl, C 3-7 Branched alkyl, C 3-7 Cycloalkyl, C 1-6 Straight chain alkoxy, C 3-7 Branched alkoxy, C 3-7 Cycloalkoxy, C 1-6 Straight chain halogenated alkyl, C 3-7 Branched chain halogenated alkyl, C 1-6 Straight chain halogenated alkoxy, C 3-7 Branched chain haloalkoxy, SH, SC 1-6 Straight chain alkyl, SC 3-7 Branched chain alkyl, SC 3-7 Cycloalkyl, SO2C 1-6 Straight chain alkyl, SO2C 3-7 Branched alkyl, SO2C 3-7 Cycloalkyl, SO2NH2, SO2NHR 21 NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2. Morpholino and The group composed of; R 21 Independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 25 Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; And R 20a 、R 20b 、R 20c and R 20d At least two of them are hydrogen.

16. The compound according to claim 1, having the formula (IIIi): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a , R 20b , R 20c and R 20e independently selected from hydrogen, -CN, -NO2, -OH, halogen, C 1-6 Straight chain alkyl, C 3-7 Branched alkyl, C 3-7 Cycloalkyl, C 1-6 Straight chain alkoxy, C 3-7 Branched alkoxy, C 3-7 Cycloalkoxy, C 1-6 Straight chain halogenated alkyl, C 3-7 Branched chain halogenated alkyl, C 1-6 Straight chain halogenated alkoxy, C 3-7 Branched chain haloalkoxy, SH, SC 1-6 Straight chain alkyl, SC 3-7 Branched chain alkyl, SC 3-7 Cycloalkyl, SO2C 1-6 Straight chain alkyl, SO2C 3-7 Branched alkyl, SO2C 3-7 Cycloalkyl, SO2NH2, SO2NHR 21 NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2. Morpholino and The group composed of; R 21 Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 25 Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; And R 20a 、R 20b 、R 20c and R 20e At least two of them are hydrogen.

17. The compound according to claim 1, having the formula (IIIm): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a , R 20b , R 20d and R 20e independently selected from hydrogen, -CN, -NO2, -OH, halogen, C 1-6 Straight chain alkyl, C 3-7 Branched alkyl, C 3-7 Cycloalkyl, C 1-6 Straight chain alkoxy, C 3-7 Branched alkoxy, C 3-7 Cycloalkoxy, C 1-6 Straight chain halogenated alkyl, C 3-7 Branched chain halogenated alkyl, C 1-6 Straight chain halogenated alkoxy, C 3-7 Branched chain haloalkoxy, SH, SC 1-6 Straight chain alkyl, SC 3-7 Branched chain alkyl, SC 3-7 Cycloalkyl, SO2C 1-6 Straight chain alkyl, SO2C 3-7 Branched alkyl, SO2C 3-7 Cycloalkyl, SO2NH2, SO2NHR 21 NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2. Morpholino and The group composed of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 22 Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; And R 20a 、R 20b 、R 20c and R 20d At least two of them are hydrogen.

18. The compound according to claim 1, having the formula (IIIq): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; And R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g At least five of them are hydrogen.

19. The compound according to claim 1, having the formula (IIIu): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; And R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g at least five of which are hydrogen.

20. The compound according to claim 1 has the formula (IV): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes.

21. The compound according to claim 20 has the following formula or a pharmaceutically acceptable salt thereof.

22. The compound according to claim 20 has the following formula or a pharmaceutically acceptable salt thereof.

23. The compound according to claim 1 has the formula (IVa): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、 R 20b 、 R 20c 、 R 20d and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、 NHSO2R 22 、 -NR 23a R 23b 、 NHC(O)R 24 、 C(O)NHR 24 、 C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 24 Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; And R 20a 、R 20b 、R 20c 、R 20d and R 20e At least three of them are hydrogen.

24. The compound according to claim 1 has the formula (IVe): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、 R 20b 、 R 20c and R 20d are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、 NHSO2R 22 、 -NR 23a R 23b 、 NHC(O)R 24 、 C(O)NHR 24 、 C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 23a Independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; And R 20a 、R 20b 、R 20c and R 20d At least two of them are hydrogen.

25. The compound according to claim 1 has the formula (IVi): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、 R 20b 、 R 20c and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、 NHSO2R 22 、 -NR 23a R 23b 、 NHC(O)R 24 、 C(O)NHR 24 、 C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 24 Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; And R 20a 、R 20b 、R 20c and R 20e At least two of them are hydrogen.

26. The compound according to claim 1 has the formula (IVm): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、R 20b 、R 20d and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 25 Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; And R 20a , R 20b , R 20c and R 20d At least two of them are hydrogen.

27. The compound according to claim 1 has the formula (IVq): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; And R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g At least five of them are hydrogen.

28. The compound according to claim 1 has the formula (IVu): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; And R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g At least five of them are hydrogen.

29. The compound according to claim 1 has the formula (V): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes.

30. The compound according to claim 1 has the formula (Va): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、R 20b 、R 20c 、R 20d and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; And R 20a 、R 20b 、R 20c 、R 20d and R 20e At least three of them are hydrogen.

31. The compound according to claim 1 has the formula (Vb): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein Q 1 is 1 or 2; And Q 2 is 1 or 2.

32. The compound according to claim 1 has the formula (Ve): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、 R 20b 、 R 20c and R 20d are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、 NHSO2R 22 、 -NR 23a R 23b 、 NHC(O)R 24 、 C(O)NHR 24 、 C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23b Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; And R 20a 、R 20b 、R 20c and R 20d At least two of them are hydrogen.

33. The compound according to claim 1 has the formula (Vi): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、 R 20b 、 R 20c and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、 NHSO2R 22 、 -NR 23a R 23b 、 NHC(O)R 24 、 C(O)NHR 24 、 C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; And R 20a 、R 20b 、R 20c and R 20e At least two of them are hydrogen.

34. The compound according to claim 1 has the formula (Vm): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、 R 20b 、 R 20d and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、 NHSO2R 22 、 -NR 23a R 23b 、 NHC(O)R 24 、 C(O)NHR 24 、 C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; And R 20a 、R 20b 、R 20c and R 20d At least two of them are hydrogen.

35. The compound according to claim 1 has the formula (Vq): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 24 independently selected from the group consisting of hydrogen, C 1-6 straight-chain alkyl, C 3-7 branched-chain alkyl, and C 3-7 cycloalkyl each time it appears; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; And R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g at least five of which are hydrogen.

36. The compound according to claim 1 has the formula (Vu): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 22 Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; And R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g at least 5 of which are hydrogen.

37. The compound according to claim 1 has the formula (VI): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes.

38. The compound according to claim 37 has the formula (XXXXVI): or a pharmaceutically acceptable salt thereof.

39. The compound according to claim 37 has the formula: or a pharmaceutically acceptable salt thereof.

40. The compound according to claim 1 has the formula (VIa): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、R 20b 、R 20c 、R 20d and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; And R 20a 、R 20b 、R 20c 、R 20d and R 20e At least three of them are hydrogen.

41. The compound according to claim 1 has the formula (VIe): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、R 20b 、R 20c and R 20d are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of; R 21 Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; And R 20a 、R 20b 、R 20c and R 20d At least two of them are hydrogen.

42. The compound according to claim 1 has the formula (VIi): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、R 20b 、R 20c and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 22 Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; And R 20a 、R 20b 、R 20c and R 20e At least two of them are hydrogen.

43. The compound according to claim 1 has the formula (VIm): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a , R 20b , R 20d and R 20e independently selected from hydrogen, -CN, -NO2, -OH, halogen, C 1-6 Straight chain alkyl, C 3-7 Branched alkyl, C 3-7 Cycloalkyl, C 1-6 Straight chain alkoxy, C 3-7 Branched alkoxy, C 3-7 Cycloalkoxy, C 1-6 Straight chain halogenated alkyl, C 3-7 Branched chain halogenated alkyl, C 1-6 Straight chain halogenated alkoxy, C 3-7 Branched chain haloalkoxy, SH, SC 1-6 Straight chain alkyl, SC 3-7 Branched chain alkyl, SC 3-7 Cycloalkyl, SO2C 1-6 Straight chain alkyl, SO2C 3-7 Branched alkyl, SO2C 3-7 Cycloalkyl, SO2NH2, SO2NHR 21 NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2. Morpholino and The group composed of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; And R 20a 、R 20b 、R 20c and R 20d At least two of them are hydrogen.

44. The compound according to claim 1 has the formula (VIq): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl, each time it appears; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; And R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g At least five of them are hydrogen.

45. The compound according to claim 1 has the formula (VIu): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、 R 20b 、 R 20c 、 R 20d 、 R 20e 、 R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、 NHSO2R 22 、 -NR 23a R 23b 、 NHC(O)R 24 、 C(O)NHR 24 、 C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; And R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g at least five of which are hydrogen.

46. The compound according to claim 1 has the formula (VII): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes.

47. The compound according to claim 1 has the formula (VIIa): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、 R 20b 、 R 20c 、 R 20d and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、 NHSO2R 22 、 -NR 23a R 23b 、 NHC(O)R 24 、 C(O)NHR 24 、 C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 23b Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; And R 20a 、R 20b 、R 20c 、R 20d and R 20e At least three of them are hydrogen.

48. The compound according to claim 1 has the formula (VIIe): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、 R 20b 、 R 20c and R 20d are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、 NHSO2R 22 、 -NR 23a R 23b 、 NHC(O)R 24 、 C(O)NHR 24 、 C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; And R 20a , R 20b , R 20c and R 20d At least two of them are hydrogen.

49. The compound according to claim 1 has the formula (VIIi): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、 R 20b 、 R 20c and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、 NHSO2R 22 、 -NR 23a R 23b 、 NHC(O)R 24 、 C(O)NHR 24 、 C(O)N(R 24 )2, morpholino and the group consisting of; R 21 Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; And R 20a 、R 20b 、R 20c and R 20e At least two of them are hydrogen.

50. The compound according to claim 1 has the formula (VIIm): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、 R 20b 、 R 20d and R 20e are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、 NHSO2R 22 、 -NR 23a R 23b 、 NHC(O)R 24 、 C(O)NHR 24 、 C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 22 Independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 23a Independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; And R 20a 、R 20b 、R 20c and R 20d At least two of them are hydrogen.

51. The compound according to claim 1 has the formula (VIIq): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 23a Each occurrence is independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; and R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g at least five of which are hydrogen.

52. The compound according to claim 1 has the formula (VIIu): including its hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts and complexes, wherein R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g are independently selected from the group consisting of hydrogen, -CN, -NO2, -OH, halogen, C 1-6 linear alkyl, C 3-7 branched alkyl, C 3-7 cycloalkyl, C 1-6 linear alkoxy, C 3-7 branched alkoxy, C 3-7 cycloalkoxy, C 1-6 linear haloalkyl, C 3-7 branched haloalkyl, C 1-6 linear haloalkoxy, C 3-7 branched haloalkoxy, SH, SC 1-6 linear alkyl, SC 3-7 branched alkyl, SC 3-7 cycloalkyl, SO2C 1-6 linear alkyl, SO2C 3-7 branched alkyl, SO2C 3-7 cycloalkyl, SO2NH2, SO2NHR 21 、NHSO2R 22 、-NR 23a R 23b 、NHC(O)R 24 、C(O)NHR 24 、C(O)N(R 24 )2, morpholino and the group consisting of; R 21 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl at each occurrence; R 22 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl, and C 3-7 cycloalkyl each time it appears; R 23a independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 23b independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl at each occurrence; R 24 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; R 25 independently selected from the group consisting of hydrogen, C 1-6 linear alkyl, C 3-7 branched alkyl and C 3-7 cycloalkyl each time it appears; And R 20a 、R 20b 、R 20c 、R 20d 、R 20e 、R 20f and R 20g At least 5 of them are hydrogen.

53. A compound according to any one of claims 1 to 52, wherein R 1 and R 2 are each independently a C 1-6 linear alkyl or a C 3-7 branched alkyl.

54. The compound according to claim 53, wherein each of R 1 and R 2 is ethyl.

55. A compound according to any one of claims 1 to 52, wherein R 1 and R 2 together with the atoms to which they are attached form a 5- to 8-membered ring, which ring optionally contains a carbon-carbon double bond and / or ring atoms selected from the group consisting of O, S, SO, SO2 and NR 7 .

56. The compound according to claim 55, wherein R 1 and R 2 together with the atoms to which they are attached form a C3-C8 cycloalkyl or a C5-C8 cycloalkenyl.

57. The compound according to claim 56, wherein R 1 and R 2 together with the atoms to which they are attached form cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl or cyclooctenyl.

58. The compound according to any one of claims 55 to 57 has the formula (XLIIIa): or Its pharmaceutically acceptable salts, wherein represents a single bond or a double bond.

59. The compound according to claim 58, wherein represents a single bond.

60. The compound according to claim 58, wherein represents a double bond.

61. The compound according to claim 55, wherein R 1 and R 2 together with the atoms to which they are attached form a 5- to 8-membered ring containing the ring atom NR 7 ​ 62. The compound according to claim 61, wherein R 1 and R 2 together form a pyrrolidinyl or piperidinyl group, wherein the nitrogen atom is NR 7 .

63. The compound according to claim 61 or 62, wherein R 7 is COR 8 , and R 8 is C 1-6 a straight-chain alkyl group.

64. The compound according to claim 63, wherein R 7 is an acetyl group.

65. The compound according to claim 61 or 62, wherein R 7 is SO2R 10c , and R 10c is C 1-6 linear alkyl group.

66. The compound according to claim 65, wherein R 10c is methyl.

67. The compound according to any one of claims 61 to 66 has the formula (XLIIIb): or a pharmaceutically acceptable salt thereof.

68. The compound according to claim 67 has the formula (XLIV): or a pharmaceutically acceptable salt thereof.

69. The compound according to claim 67 has the formula (XLV): or a pharmaceutically acceptable salt thereof.

70. A compound according to any one of claims 53 to 69, wherein R 3 is an unsubstituted phenyl group.

71. The compound according to any one of claims 53 to 69, wherein R 3 is a substituted phenyl, wherein the substituent is selected from the group consisting of a hydroxyl group, a halogen group, a cyano group, C 1-6 alkoxy, C 1-6 linear alkyl, C 3-7 branched alkyl, C 1-6 haloalkyl, and heterocycle.

72. The compound according to claim 71, wherein R 3 is selected from the group consisting of 4-hydroxyphenyl, 3-fluorophenyl, 4-fluorophenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 4-fluoro-3-chlorophenyl, 4-cyanophenyl, 2-methoxyphenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2-isopropylphenyl, 4-trifluoromethylphenyl, 2-morpholinophenyl, and 4-methyl-2-morpholinophenyl.

73. A compound according to any one of claims 53 to 69, wherein R 3 is 2-pyridyl.

74. A compound according to any one of claims 53 to 56 and 61 to 62, wherein A is and R 5 is an optionally substituted phenyl group.

75. The compound according to claim 74 has the formula (XLVI), or a pharmaceutically acceptable salt thereof.

76. The compound according to claim 74 has the formula (XLVIa), or a pharmaceutically acceptable salt thereof.

77. The compound according to claim 74, wherein R 5 is an unsubstituted phenyl group.

78. The compound according to claim 74, wherein R 5 is selected from the group consisting of 4-hydroxyphenyl, 3-fluorophenyl, 4-fluorophenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 4-fluoro-3-chlorophenyl, 4-cyanophenyl, 2-methoxyphenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2-isopropylphenyl, 4-trifluoromethylphenyl, 2-morpholinophenyl, and 4-methyl-2-morpholinophenyl.

79. The compound according to any one of claims 1 to 78, or a pharmaceutically acceptable salt thereof.

80. The compound according to claim 79, wherein the compound is a compound described in any one of Tables 1 to 39 or a pharmaceutically acceptable salt thereof.

81. The compound according to claim 80, wherein the compound is a compound described in any one of Tables 34 to 39 or a pharmaceutically acceptable salt thereof.

82. A composition comprising an effective amount of at least one compound according to any one of claims 1 to 81 or a pharmaceutically acceptable salt thereof.

83. The composition according to claim 82, further comprising at least one excipient.

84. A method of treating a disease associated with a dysregulation of 5 - hydroxytryptamine receptor 7 activity, the method comprising administering to a subject an effective amount of at least one compound according to any one of claims 1 to 81 or a pharmaceutically acceptable salt thereof.

85. The method according to claim 84, wherein the at least one compound or a pharmaceutically acceptable salt thereof is administered in the form of a composition further comprising at least one excipient.

86. The method according to claim 84 or 85, wherein the disease associated with a dysregulation of 5 - hydroxytryptamine receptor 7 activity is selected from the group consisting of circadian rhythm disorders, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral vascular disease, migraine, neuropathic pain, peripheral pain, allodynia, thermoregulatory disorders, learning disorders, memory disorders, hippocampal signal transduction disorders, sleep disorders, attention deficit / hyperactivity disorder, anxiety disorders, avoidant personality disorder, premature ejaculation, eating disorders, premenstrual syndrome, premenstrual dysphoric disorder, seasonal affective disorder, bipolar disorder, inflammatory bowel disease (IBD), enteritis, epilepsy, epileptic disorders, drug addiction, alcohol addiction, breast cancer, liver fibrosis, chronic liver injury, hepatocellular carcinoma, small intestinal neuroendocrine tumors, and lung injury.

87. The method according to claim 84 or 85, wherein the disease associated with a dysregulation of 5 - hydroxytryptamine receptor 7 activity is inflammatory bowel disease (IBD) or enteritis.

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