RU2017139768A - Нацеленные на белки соединения, их композиции, способы и применения - Google Patents
Нацеленные на белки соединения, их композиции, способы и применения Download PDFInfo
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- 150000001875 compounds Chemical class 0.000 title claims 16
- 102000004169 proteins and genes Human genes 0.000 title claims 3
- 108090000623 proteins and genes Proteins 0.000 title claims 3
- 239000000203 mixture Substances 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- -1 cycloalkynyl Chemical group 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 125000001831 (C6-C10) heteroaryl group Chemical group 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 102000008122 Casein Kinase I Human genes 0.000 claims 2
- 108010049812 Casein Kinase I Proteins 0.000 claims 2
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 2
- 125000005631 S-sulfonamido group Chemical group 0.000 claims 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Natural products NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000004452 carbocyclyl group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 229910052805 deuterium Inorganic materials 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 235000018102 proteins Nutrition 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 102000004127 Cytokines Human genes 0.000 claims 1
- 108090000695 Cytokines Proteins 0.000 claims 1
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- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010027406 Mesothelioma Diseases 0.000 claims 1
- 208000003445 Mouth Neoplasms Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 206010043515 Throat cancer Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 230000001594 aberrant effect Effects 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- UMGDCJDMYOKAJW-UHFFFAOYSA-N aminothiocarboxamide Natural products NC(N)=S UMGDCJDMYOKAJW-UHFFFAOYSA-N 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000005110 aryl thio group Chemical group 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 239000004202 carbamide Substances 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 208000024519 eye neoplasm Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000001261 isocyanato group Chemical group *N=C=O 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 208000012987 lip and oral cavity carcinoma Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 208000037819 metastatic cancer Diseases 0.000 claims 1
- 208000011575 metastatic malignant neoplasm Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000008106 ocular cancer Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
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- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000004646 sulfenyl group Chemical group S(*)* 0.000 claims 1
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims 1
- 125000001273 sulfonato group Chemical class [O-]S(*)(=O)=O 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 claims 1
- 125000003396 thiol group Chemical class [H]S* 0.000 claims 1
- 150000003585 thioureas Chemical class 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 125000005423 trihalomethanesulfonamido group Chemical group 0.000 claims 1
- 125000005152 trihalomethanesulfonyl group Chemical group 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 150000003672 ureas Chemical class 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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Claims (30)
1. Соединение формулы (I):
или его фармацевтически приемлемая соль или сольват, где:
каждый из R1, R2, R3 и R4 независимо выбран из группы, состоящей из Н, дейтерия, гидроксила, галогена, циано, нитро, необязательно замещенного амино, необязательно замещенного С-амидо, необязательно замещенного N-амидо, необязательно замещенного сложного эфира, необязательно замещенного сульфонила, необязательно замещенного S-сульфонамидо, необязательно замещенного N-сульфонамидо, необязательно замещенного сульфоната, необязательно замещенного О-тиокарбамила, необязательно замещенного N-тиокарбамила, необязательно замещенного N-карбамила, необязательно замещенного О-карбамила, необязательно замещенной мочевины, необязательно замещенной тиомочевины, необязательно замещенного C1-С6 алкокси, необязательно замещенного C1-С6 алкила, необязательно замещенного С2-С6 алкенила, необязательно замещенного С2-С6 алкинила, необязательно замещенного С3-C8 карбоциклила, необязательно замещенного С6-С10 арила, необязательно замещенного С3-C8 гетероциклила и необязательно замещенного С6-С10 гетероарила;
R5 выбран из группы, состоящей из Н, дейтерия, оксо, необязательно замещенного C1-С6 алкила, необязательно замещенного С2-С6 алкенила, необязательно замещенного С2-С6 алкинила, необязательно замещенного С3-C8 карбоциклила, необязательно замещенного С6-С10 арила, необязательно замещенного С3-C8 гетероциклила и необязательно замещенного С6-С10 гетероарила;
X выбран из группы, состоящей из C(R5)2, CH(R5), СН2, С=O и C=S;
Q выбран из группы, состоящей из C(R5)2, CH(R5), СН2, С=O, C=S; S=O и SO2; и
n равно 1 или 2; и
где необязательно замещенный заместитель может быть замещен одной или более групп, выбранных из алкила, алкенила, алкинила, циклоалкила, циклоалкенила, циклоалкинила, арила, гетероарила, гетероалициклила, аралкила, гетероаралкила, (гетероалициклил)алкила, гидрокси, защищенного гидроксила, алкокси, арилокси, ацила, меркапто, алкилтио, арилтио, циано, галогена, тиокарбонила, О-карбамила, N-карбамила, О-тиокарбамила, N-тиокарбамила, С-амидо, N-амидо, S-сульфонамидо, N-сульфонамидо, С-карбокси, защищенного С-карбокси, О-карбокси, изоцианато, тиоцианато, изотиоцианато, нитро, силила, сульфенила, сульфинила, сульфонила, галогеналкила, галогеналкокси, тригалогенметансульфонила, тригалогенметансульфонамидо, амино, монозамещенной аминогруппы и дизамещенной аминогруппы.
2. Соединение по п. 1, где Q выбран из группы, состоящей из CH2 и С=O.
3. Соединение по любому из пп. 1-2, где Q представляет собой CH2 или С=O.
4. Соединение по любому из пп. 1-3, где n равно 1.
5. Соединение по любому из пп. 1-4, где R5 выбран из Н, необязательно замещенного C1-С6 алкила и необязательно замещенного С6-С10 арила.
6. Соединение по любому из пп. 1-5, где X представляет собой CH2 или С=O.
7. Соединение по любому из пп. 1-6, где R1 выбран из NH2, NO2, СН3, хлора и метокси.
8. Соединение по любому из пп. 1-7, где R2 выбран из NH2 и NO2.
9. Соединение по любому из п. 1, где соединение формулы (I) выбрано из группы, состоящей из:
10. Фармацевтическая композиция, содержащая соединение по п. 1 или его фармацевтически приемлемую соль или сольват, и по меньшей мере один фармацевтически приемлемый носитель.
11. Применение соединения по любому из пп. 1-9 , или его фармацевтически приемлемой соли, для ингибирования активности цитокина, включающий приведение клетки в контакт с соединением по любому из пп. 1-9, или его фармацевтически приемлемой соли.
12. Применение соединения по любому из пп. 1-9 , или его фармацевтически приемлемой соли, для лечения, облегчения или предотвращения заболевания, расстройства или состояния, связанного с нарушением функции белка, где указанное заболевание, расстройство или состояние представляет собой рак и белок представляет собой казеинкиназу 1.
13. Применение по п. 12, где указанный рак выбран из лейкоза; лимфомы, рака мочевого пузыря, рака кости, рака желудка, колоректального рака, рака мозга, рака молочной железы, рака шейки матки, саркомы, рака глаза, рака полости рта, рака почки, рака печени, рака легкого, немелкоклеточного рака легкого, метастатического рака, меланомы, мезотелиомы, рака яичников, рака поджелудочной железы, рака предстательной железы, рака кожи, рака яичка, рака горла, рака щитовидной железы, рака матки.
14. Применение по п. 13, где известно, что рак имеет р53 дикого типа.
15. Применение по п. 13, где известно, что рак имеет аберрантную казеинкиназу 1.
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