RU2016134941A - Производные диазепана и их применения - Google Patents
Производные диазепана и их применения Download PDFInfo
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- RU2016134941A RU2016134941A RU2016134941A RU2016134941A RU2016134941A RU 2016134941 A RU2016134941 A RU 2016134941A RU 2016134941 A RU2016134941 A RU 2016134941A RU 2016134941 A RU2016134941 A RU 2016134941A RU 2016134941 A RU2016134941 A RU 2016134941A
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- Prior art keywords
- substituted
- unsubstituted
- compound
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- compound according
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- 150000000117 diazepanes Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 178
- 238000000034 method Methods 0.000 claims 63
- 125000000623 heterocyclic group Chemical group 0.000 claims 62
- 229910052739 hydrogen Inorganic materials 0.000 claims 62
- 239000001257 hydrogen Substances 0.000 claims 61
- 125000000217 alkyl group Chemical group 0.000 claims 54
- 125000001072 heteroaryl group Chemical group 0.000 claims 53
- 229910052757 nitrogen Inorganic materials 0.000 claims 52
- 125000006239 protecting group Chemical group 0.000 claims 52
- 150000002431 hydrogen Chemical class 0.000 claims 50
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 44
- 125000003342 alkenyl group Chemical group 0.000 claims 38
- 125000000304 alkynyl group Chemical group 0.000 claims 38
- 125000003118 aryl group Chemical group 0.000 claims 38
- 150000003839 salts Chemical class 0.000 claims 33
- 229910052717 sulfur Inorganic materials 0.000 claims 33
- 201000010099 disease Diseases 0.000 claims 30
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 30
- 125000004430 oxygen atom Chemical group O* 0.000 claims 29
- 125000004434 sulfur atom Chemical group 0.000 claims 28
- 229910052736 halogen Inorganic materials 0.000 claims 27
- 150000002367 halogens Chemical class 0.000 claims 27
- 102000001805 Bromodomains Human genes 0.000 claims 22
- 125000002252 acyl group Chemical group 0.000 claims 20
- 239000008194 pharmaceutical composition Substances 0.000 claims 16
- 108091005575 Bromodomain-containing proteins Proteins 0.000 claims 15
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 11
- 125000004429 atom Chemical group 0.000 claims 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 9
- 229910052760 oxygen Inorganic materials 0.000 claims 9
- 239000001301 oxygen Substances 0.000 claims 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 108090000623 proteins and genes Proteins 0.000 claims 9
- 108050009021 Bromodomains Proteins 0.000 claims 7
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 6
- 125000002837 carbocyclic group Chemical group 0.000 claims 6
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 6
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 5
- 230000001594 aberrant effect Effects 0.000 claims 5
- 230000000694 effects Effects 0.000 claims 5
- 102000004169 proteins and genes Human genes 0.000 claims 5
- 239000011593 sulfur Substances 0.000 claims 5
- 201000003176 Severe Acute Respiratory Syndrome Diseases 0.000 claims 4
- 230000002401 inhibitory effect Effects 0.000 claims 4
- 201000001320 Atherosclerosis Diseases 0.000 claims 3
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 3
- 208000030507 AIDS Diseases 0.000 claims 2
- 102100033641 Bromodomain-containing protein 2 Human genes 0.000 claims 2
- 101710126816 Bromodomain-containing protein 2 Proteins 0.000 claims 2
- 102100033642 Bromodomain-containing protein 3 Human genes 0.000 claims 2
- 101710126814 Bromodomain-containing protein 3 Proteins 0.000 claims 2
- 102100029895 Bromodomain-containing protein 4 Human genes 0.000 claims 2
- 101710126815 Bromodomain-containing protein 4 Proteins 0.000 claims 2
- 108010040163 CREB-Binding Protein Proteins 0.000 claims 2
- 102100021975 CREB-binding protein Human genes 0.000 claims 2
- 201000011001 Ebola Hemorrhagic Fever Diseases 0.000 claims 2
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 2
- 102100038885 Histone acetyltransferase p300 Human genes 0.000 claims 2
- 101000882390 Homo sapiens Histone acetyltransferase p300 Proteins 0.000 claims 2
- 241000725303 Human immunodeficiency virus Species 0.000 claims 2
- 241000701806 Human papillomavirus Species 0.000 claims 2
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 208000005374 Poisoning Diseases 0.000 claims 2
- 241000700584 Simplexvirus Species 0.000 claims 2
- 230000036523 atherogenesis Effects 0.000 claims 2
- 125000001246 bromo group Chemical group Br* 0.000 claims 2
- 208000024908 graft versus host disease Diseases 0.000 claims 2
- 208000010710 hepatitis C virus infection Diseases 0.000 claims 2
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 231100000572 poisoning Toxicity 0.000 claims 2
- 230000000607 poisoning effect Effects 0.000 claims 2
- 230000005855 radiation Effects 0.000 claims 2
- 230000001105 regulatory effect Effects 0.000 claims 2
- 238000013518 transcription Methods 0.000 claims 2
- 230000035897 transcription Effects 0.000 claims 2
- 230000009385 viral infection Effects 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010060999 Benign neoplasm Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000017701 Endocrine disease Diseases 0.000 claims 1
- 108010033040 Histones Proteins 0.000 claims 1
- 101000596093 Homo sapiens Transcription initiation factor TFIID subunit 1 Proteins 0.000 claims 1
- 101000596092 Homo sapiens Transcription initiation factor TFIID subunit 1-like Proteins 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 201000004253 NUT midline carcinoma Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 208000034038 Pathologic Neovascularization Diseases 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 102100035222 Transcription initiation factor TFIID subunit 1 Human genes 0.000 claims 1
- 102100035238 Transcription initiation factor TFIID subunit 1-like Human genes 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 102000023732 binding proteins Human genes 0.000 claims 1
- 108091008324 binding proteins Proteins 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 208000016097 disease of metabolism Diseases 0.000 claims 1
- 208000030172 endocrine system disease Diseases 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
- 208000004104 gestational diabetes Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 206010022000 influenza Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 230000001681 protective effect Effects 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
- A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/14—Ortho-condensed systems
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Virology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Molecular Biology (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Biotechnology (AREA)
- Toxicology (AREA)
- Child & Adolescent Psychology (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pain & Pain Management (AREA)
- AIDS & HIV (AREA)
- Vascular Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461934668P | 2014-01-31 | 2014-01-31 | |
| US61/934,668 | 2014-01-31 | ||
| PCT/US2015/014109 WO2015117083A1 (en) | 2014-01-31 | 2015-02-02 | Diazepane derivatives and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2016134941A true RU2016134941A (ru) | 2018-03-01 |
| RU2016134941A3 RU2016134941A3 (https=) | 2018-09-24 |
Family
ID=53757810
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2016134941A RU2016134941A (ru) | 2014-01-31 | 2015-02-02 | Производные диазепана и их применения |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9695172B2 (https=) |
| EP (1) | EP3099696A4 (https=) |
| JP (1) | JP2017504650A (https=) |
| KR (1) | KR20160111036A (https=) |
| CN (1) | CN105940005A (https=) |
| BR (1) | BR112016017045A2 (https=) |
| CA (1) | CA2936256A1 (https=) |
| HK (1) | HK1225383A1 (https=) |
| MX (1) | MX2016009976A (https=) |
| RU (1) | RU2016134941A (https=) |
| WO (1) | WO2015117083A1 (https=) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011090738A2 (en) | 2009-12-29 | 2011-07-28 | Dana-Farber Cancer Institute, Inc. | Type ii raf kinase inhibitors |
| MX354217B (es) | 2010-05-14 | 2018-02-19 | Dana Farber Cancer Inst Inc | Composiciones y metodos para el tratamiento de leucemia. |
| PL2902030T3 (pl) | 2010-05-14 | 2017-07-31 | Dana-Farber Cancer Institute, Inc. | Związki tienotriazolodiazepinowe do leczenia nowotworu |
| EP2571875A4 (en) | 2010-05-14 | 2013-10-30 | Dana Farber Cancer Inst Inc | CONTRACEPTIVE COMPOSITIONS FOR MEN AND METHODS OF USE THEREOF |
| US9382239B2 (en) | 2011-11-17 | 2016-07-05 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-Jun-N-terminal kinase (JNK) |
| EP2909194A1 (en) | 2012-10-18 | 2015-08-26 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| USRE48175E1 (en) | 2012-10-19 | 2020-08-25 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
| WO2014063054A1 (en) | 2012-10-19 | 2014-04-24 | Dana-Farber Cancer Institute, Inc. | Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof |
| US9975896B2 (en) | 2013-07-25 | 2018-05-22 | Dana-Farber Cancer Institute, Inc. | Inhibitors of transcription factors and uses thereof |
| EP3057956B1 (en) | 2013-10-18 | 2021-05-05 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7) |
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