RU2018112953A - Ацетамидтиенотриазолодиазепины и пути их применения - Google Patents
Ацетамидтиенотриазолодиазепины и пути их применения Download PDFInfo
- Publication number
- RU2018112953A RU2018112953A RU2018112953A RU2018112953A RU2018112953A RU 2018112953 A RU2018112953 A RU 2018112953A RU 2018112953 A RU2018112953 A RU 2018112953A RU 2018112953 A RU2018112953 A RU 2018112953A RU 2018112953 A RU2018112953 A RU 2018112953A
- Authority
- RU
- Russia
- Prior art keywords
- optionally substituted
- pharmaceutically acceptable
- acceptable salt
- compound according
- compound
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 claims 70
- 238000000034 method Methods 0.000 claims 57
- 150000003839 salts Chemical class 0.000 claims 57
- 201000010099 disease Diseases 0.000 claims 22
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 22
- 102000001805 Bromodomains Human genes 0.000 claims 21
- 239000008194 pharmaceutical composition Substances 0.000 claims 19
- 108091005575 Bromodomain-containing proteins Proteins 0.000 claims 14
- 125000000623 heterocyclic group Chemical group 0.000 claims 14
- 125000001072 heteroaryl group Chemical group 0.000 claims 13
- 239000012472 biological sample Substances 0.000 claims 12
- 108090000623 proteins and genes Proteins 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 125000004452 carbocyclyl group Chemical group 0.000 claims 9
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 150000002367 halogens Chemical class 0.000 claims 9
- 102000004169 proteins and genes Human genes 0.000 claims 9
- 125000000547 substituted alkyl group Chemical group 0.000 claims 9
- 125000003107 substituted aryl group Chemical group 0.000 claims 9
- 125000002252 acyl group Chemical group 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 8
- 230000002401 inhibitory effect Effects 0.000 claims 8
- 108050009021 Bromodomains Proteins 0.000 claims 7
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 7
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 7
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 230000000694 effects Effects 0.000 claims 5
- VEYYWZRYIYDQJM-ZETCQYMHSA-N N(2)-acetyl-L-lysine Chemical group CC(=O)N[C@H](C([O-])=O)CCCC[NH3+] VEYYWZRYIYDQJM-ZETCQYMHSA-N 0.000 claims 4
- 230000001939 inductive effect Effects 0.000 claims 4
- 208000015181 infectious disease Diseases 0.000 claims 4
- 230000001594 aberrant effect Effects 0.000 claims 3
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 208000030507 AIDS Diseases 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 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
- 241000711549 Hepacivirus C Species 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
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 201000003176 Severe Acute Respiratory Syndrome Diseases 0.000 claims 2
- 241000700584 Simplexvirus Species 0.000 claims 2
- 102000006467 TATA-Box Binding Protein Human genes 0.000 claims 2
- 108010044281 TATA-Box Binding Protein Proteins 0.000 claims 2
- 230000006907 apoptotic process Effects 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 230000000903 blocking effect Effects 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 230000001105 regulatory effect Effects 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 1
- 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
- 201000011001 Ebola Hemorrhagic Fever 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
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000000172 Medulloblastoma Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 201000004253 NUT midline carcinoma Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 208000025966 Neurological disease 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
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms 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
- 125000003118 aryl group Chemical group 0.000 claims 1
- 230000036523 atherogenesis Effects 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 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
- 208000024908 graft versus host disease Diseases 0.000 claims 1
- 125000004404 heteroalkyl group Chemical group 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 206010022000 influenza Diseases 0.000 claims 1
- 208000036971 interstitial lung disease 2 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
- 206010025482 malaise Diseases 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 230000005855 radiation Effects 0.000 claims 1
- 229910052702 rhenium Inorganic materials 0.000 claims 1
- WUAPFZMCVAUBPE-UHFFFAOYSA-N rhenium atom Chemical compound [Re] WUAPFZMCVAUBPE-UHFFFAOYSA-N 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K31/55—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K31/55—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
- A61P31/22—Antivirals for DNA viruses for herpes viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Virology (AREA)
- Diabetes (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Tropical Medicine & Parasitology (AREA)
- Biotechnology (AREA)
- AIDS & HIV (AREA)
- Endocrinology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562217544P | 2015-09-11 | 2015-09-11 | |
| US62/217,544 | 2015-09-11 | ||
| PCT/US2016/051017 WO2017044792A1 (en) | 2015-09-11 | 2016-09-09 | Acetamide thienotriazoldiazepines and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2018112953A true RU2018112953A (ru) | 2019-10-14 |
| RU2018112953A3 RU2018112953A3 (enExample) | 2019-12-26 |
Family
ID=58240133
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2018112953A RU2018112953A (ru) | 2015-09-11 | 2016-09-09 | Ацетамидтиенотриазолодиазепины и пути их применения |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US10881668B2 (enExample) |
| EP (1) | EP3347020A4 (enExample) |
| JP (1) | JP2018526424A (enExample) |
| KR (1) | KR20180051576A (enExample) |
| CN (1) | CN108472299A (enExample) |
| AU (2) | AU2016319785C1 (enExample) |
| BR (1) | BR112018004617A2 (enExample) |
| CA (1) | CA2996977A1 (enExample) |
| CL (1) | CL2018000622A1 (enExample) |
| CO (1) | CO2018002568A2 (enExample) |
| CR (1) | CR20180199A (enExample) |
| HK (1) | HK1256419A1 (enExample) |
| IL (1) | IL257593A (enExample) |
| MX (1) | MX2018003030A (enExample) |
| PE (1) | PE20181086A1 (enExample) |
| PH (1) | PH12018550026A1 (enExample) |
| RU (1) | RU2018112953A (enExample) |
| SG (1) | SG10202007099TA (enExample) |
| UA (1) | UA123946C2 (enExample) |
| WO (1) | WO2017044792A1 (enExample) |
| ZA (1) | ZA201801549B (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10793571B2 (en) | 2014-01-31 | 2020-10-06 | Dana-Farber Cancer Institute, Inc. | Uses of diazepane derivatives |
| CN106029653A (zh) | 2014-01-31 | 2016-10-12 | 达纳-法伯癌症研究所股份有限公司 | 二氨基嘧啶苯砜衍生物及其用途 |
| MX2017001756A (es) | 2014-08-08 | 2017-05-30 | Dana Farber Cancer Inst Inc | Derivados de diazepano y sus usos. |
| US10702527B2 (en) | 2015-06-12 | 2020-07-07 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| HK1256417A1 (zh) | 2015-09-11 | 2019-09-20 | 达纳-法伯癌症研究所股份有限公司 | 氰基噻吩並三唑並二氮雜環庚三烯及其用途 |
| CR20180199A (es) | 2015-09-11 | 2018-05-25 | Dana Farber Cancer Inst Inc | Acetamida tienotriazolodiazepinas y usos de las mismas |
| RU2742035C2 (ru) | 2015-11-25 | 2021-02-01 | Дана-Фарбер Кэнсер Инститьют, Инк. | Бивалентные ингибиторы бромодоменов и пути их применения |
| CN107629057B (zh) * | 2016-07-19 | 2020-03-27 | 上海勋和医药科技有限公司 | Bet蛋白抑制剂及其应用 |
| WO2019056950A1 (zh) * | 2017-09-22 | 2019-03-28 | 南京明德新药研发股份有限公司 | 噻吩并二氮杂卓衍生物及其应用 |
| JP7292400B2 (ja) * | 2019-03-07 | 2023-06-16 | メッドシャイン ディスカバリー インコーポレイテッド | ＢＥＴ Ｂｒｏｍｏｄｏｍａｉｎタンパク質の阻害とＰＤ－Ｌ１遺伝子の調節の両方の効果を持つ化合物 |
| WO2021175432A1 (en) | 2020-03-04 | 2021-09-10 | Boehringer Ingelheim International Gmbh | Method for administration of an anti cancer agent |
| CN112444582B (zh) * | 2021-02-01 | 2021-06-04 | 宁波大学 | 基于液滴萃取的质谱分析方法 |
| CN113816970B (zh) * | 2021-09-18 | 2022-08-09 | 济宁医学院附属医院 | 一种选择性铜离子螯合剂、其制备方法及其在肺纤维化中的应用 |
Family Cites Families (175)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3709898A (en) | 1971-02-09 | 1973-01-09 | Upjohn Co | Process for the production of triazolobenzodiazepines and intermediates |
| US3681343A (en) | 1971-05-11 | 1972-08-01 | Upjohn Co | 6-phenyl-s-triazolo{8 4,3-a{9 {8 1,4{9 {0 benzodiazepines |
| US3812259A (en) | 1971-08-09 | 1974-05-21 | Upjohn Co | Animal feed and process |
| CH622019A5 (en) | 1975-10-23 | 1981-03-13 | Upjohn Co | Process for the preparation of aminotriazolobenzodiazepines |
| FR2329668A1 (fr) | 1975-10-27 | 1977-05-27 | Upjohn Co | Procede de preparation d'aminotriazolobenzodiazepines |
| EP0087850A1 (en) | 1982-01-04 | 1983-09-07 | The Upjohn Company | Benzodiazepines for anti-hypertensive use |
| DE3435973A1 (de) | 1984-10-01 | 1986-04-10 | Boehringer Ingelheim KG, 6507 Ingelheim | Diazepine enthaltende pharmazeutische zusammensetzungen mit paf-antagonistischer wirkung |
| ZA87377B (en) | 1986-01-21 | 1988-09-28 | Boehringer Ingelheim Int | New thieno-1,4-diazepine |
| DE3724164A1 (de) | 1986-07-25 | 1988-01-28 | Boehringer Ingelheim Kg | Neue 1,4-benzodiazepine, ihre herstellung und verwendung |
| ATE86256T1 (de) | 1987-05-28 | 1993-03-15 | Yoshitomi Pharmaceutical | Thieno(triazolo)diazepinverbindungen, und medizinische verwendung derselben. |
| JPH0676326B2 (ja) | 1988-05-24 | 1994-09-28 | 吉富製薬株式会社 | 循環器系疾患治療薬 |
| EP0368175A1 (de) * | 1988-11-06 | 1990-05-16 | Boehringer Ingelheim Kg | 3S,7S-3-(Morpholinocarbonyl)-5-(2-chlorphenyl)-7,10-dimethyl-3,4-dihydro-2H,7H-cyclopenta[4,5]thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin. |
| EP0387613A1 (de) | 1989-03-03 | 1990-09-19 | Boehringer Ingelheim Kg | Neue Thienodiazepine |
| EP0407955A1 (de) | 1989-07-12 | 1991-01-16 | Boehringer Ingelheim Kg | Neue Hetrazepine mit PAF-antagonistischer Wirkung, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| DE4010528A1 (de) | 1990-04-02 | 1991-10-17 | Boehringer Ingelheim Kg | Praeparativ chromatographisches trennverfahren zur herstellung enantiomerenreiner hetrazepine |
| JP2959591B2 (ja) | 1990-05-23 | 1999-10-06 | 吉富製薬株式会社 | チエノトリアゾロジアゼピン化合物 |
| DE4107521A1 (de) | 1991-03-08 | 1992-09-10 | Boehringer Ingelheim Kg | Neue acylaminosubstituierte hetrazepine |
| CA2120939A1 (en) | 1991-10-11 | 1993-04-15 | Tetsuya Tahara | Therapeutic agent for osteoporosis and diazepine compound |
| WO1994006802A1 (fr) * | 1992-09-18 | 1994-03-31 | Yoshitomi Pharmaceutical Industries, Ltd. | Compose de thienodiazepine et son utilisation medicinale |
| CA2159344A1 (en) | 1993-03-30 | 1994-10-13 | Minoru Moriwaki | Cell adhesion inhibitor and thienotriazolodiazepine compound |
| JP3001979U (ja) | 1994-03-14 | 1994-09-06 | 有限会社マルセ木工 | 竿掛け具 |
| WO1995032963A1 (en) * | 1994-06-01 | 1995-12-07 | Yoshitomi Pharmaceutical Industries, Ltd. | Thienylazole compound and thienotriazolodiazepine compound |
| DK0801651T3 (da) | 1995-01-06 | 2001-10-22 | Hoffmann La Roche | Hydroxymethyl-imidazodiazepiner og deres estere |
| KR19990044460A (ko) | 1995-09-09 | 1999-06-25 | 프리돌린 클라우스너, 롤란드 비. 보레르 | 아포리포단백질 에이-아이의 양을 증대시키는 티에노트리아졸로디아제핀의 용도 |
| US5893397A (en) | 1996-01-12 | 1999-04-13 | Bioject Inc. | Medication vial/syringe liquid-transfer apparatus |
| BR9710453A (pt) | 1996-06-12 | 1999-08-17 | Japan Tobacco Inc | Inhibidor de produ-Æo de citocina composto de triazepina e intermedi rio para o mesmo |
| US5693641A (en) | 1996-08-16 | 1997-12-02 | Berlex Laboratories Inc. | Bicyclic pyrimidine derivatives and their use as anti-coagulants |
| EP0989131B1 (en) | 1996-09-13 | 2002-11-13 | Mitsubishi Pharma Corporation | Thienotriazolodiazepine compounds and medicinal uses thereof |
| US6444664B1 (en) | 1997-04-18 | 2002-09-03 | Nederlandse Organisatie Voor Toegepast - Natuurweten Schappelijk Onderzoek (Tno) | Method for controlling the plasma level of lipoproteins to treat alzheimeris disease |
| US5993412A (en) | 1997-05-19 | 1999-11-30 | Bioject, Inc. | Injection apparatus |
| JPH11228576A (ja) | 1997-12-10 | 1999-08-24 | Japan Tobacco Inc | アポトーシス抑制剤 |
| FR2779652B1 (fr) | 1998-06-15 | 2001-06-08 | Sod Conseils Rech Applic | Utilisation de diazepines pour la preparation de medicaments destines a traiter les etats pathologiques ou les maladies dans lesquels un des recepteurs de la somatostatine est implique |
| US7589167B2 (en) | 2000-02-22 | 2009-09-15 | J. David Gladstone Institutes | ZA loops of bromodomains |
| CA2412776C (en) | 2000-06-16 | 2011-03-15 | Mitsubishi Pharma Corporation | Compositions controlling release ph range and/or speed |
| WO2002002557A2 (en) | 2000-06-30 | 2002-01-10 | Neurogen Corporation | 2-phenylimidazo[1,2-a]pyridine derivatives: a new class of gaba brain receptor ligands |
| US20060142257A1 (en) | 2001-01-19 | 2006-06-29 | Eberhard Nieschlag | Male contraceptive formulation comprising norethisterone |
| US6979682B2 (en) | 2001-02-23 | 2005-12-27 | Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College | Platelet-activating factor antagonist inhibition of angiogenesis and tumor growth induced by basic fibroblast |
| HRP20040213A2 (en) | 2001-09-04 | 2005-02-28 | Boehringer Ingelheim Pharma Gmbh & Co.Kg | Novel dihydropteridinones, method for producing the same and the use thereof as medicaments |
| US6806272B2 (en) | 2001-09-04 | 2004-10-19 | Boehringer Ingelheim Pharma Kg | Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions |
| US20030216758A1 (en) | 2001-12-28 | 2003-11-20 | Angiotech Pharmaceuticals, Inc. | Coated surgical patches |
| GB0206215D0 (en) | 2002-03-15 | 2002-05-01 | Novartis Ag | Organic compounds |
| JP3096299U (ja) | 2003-02-20 | 2003-09-12 | 宇輪工業股▲ふん▼有限公司 | 足踏み式健康器 |
| US6861422B2 (en) | 2003-02-26 | 2005-03-01 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions |
| WO2004076454A1 (de) | 2003-02-26 | 2004-09-10 | Boehringer Ingelheim Pharma Gmbh & Co Kg | Dihydropteridinone, verfahren zu deren herstellung und deren verwendung als arzneimittel |
| GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
| WO2005002526A2 (en) | 2003-07-01 | 2005-01-13 | President And Fellows Of Harvard College | Method and compositions for treatment of viral infections |
| JP2007505858A (ja) | 2003-09-18 | 2007-03-15 | ノバルティス アクチエンゲゼルシャフト | 増殖性障害の処置に有用な２，４−ジ（フェニルアミノ）ピリミジン |
| EP1528056A1 (en) | 2003-10-29 | 2005-05-04 | Academisch Ziekenhuis bij de Universiteit van Amsterdam | Deoxynojirimycin analogues and their uses as glucosylceramidase inhibitors |
| US7759485B2 (en) | 2004-08-14 | 2010-07-20 | Boehringer Ingelheim International Gmbh | Process for the manufacture of dihydropteridinones |
| US20060058311A1 (en) | 2004-08-14 | 2006-03-16 | Boehringer Ingelheim International Gmbh | Combinations for the treatment of diseases involving cell proliferation |
| US20060035903A1 (en) | 2004-08-14 | 2006-02-16 | Boehringer Ingelheim International Gmbh | Storage stable perfusion solution for dihydropteridinones |
| US20060074088A1 (en) | 2004-08-14 | 2006-04-06 | Boehringer Ingelheim International Gmbh | Dihydropteridinones for the treatment of cancer diseases |
| US7728134B2 (en) | 2004-08-14 | 2010-06-01 | Boehringer Ingelheim International Gmbh | Hydrates and polymorphs of 4[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, process for their manufacture and their use as medicament |
| GB0419161D0 (en) | 2004-08-27 | 2004-09-29 | Novartis Ag | Organic compounds |
| WO2006021548A1 (de) | 2004-08-27 | 2006-03-02 | Boehringer Ingelheim International Gmbh | Dihydropteridinone, verfahren zu deren herstellung und deren verwendung als arzneimittel |
| CN1759834B (zh) | 2004-09-17 | 2010-06-23 | 中国医学科学院医药生物技术研究所 | 黄连素或其与辛伐他汀联合在制备用于预防或治疗与血脂有关疾病或症状的产品中用途 |
| WO2006129623A1 (ja) | 2005-05-30 | 2006-12-07 | Mitsubishi Tanabe Pharma Corporation | チエノトリアゾロジアゼピン化合物及びその医薬としての用途 |
| US7491732B2 (en) | 2005-06-08 | 2009-02-17 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
| US20070203161A1 (en) | 2006-02-24 | 2007-08-30 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| EP1915155A1 (en) | 2005-08-03 | 2008-04-30 | Boehringer Ingelheim International GmbH | Dihydropteridinones in the treatment of respiratory diseases |
| NZ592990A (en) | 2005-11-01 | 2013-01-25 | Targegen Inc | Bi-aryl meta-pyrimidine inhibitors of kinases |
| US8604042B2 (en) | 2005-11-01 | 2013-12-10 | Targegen, Inc. | Bi-aryl meta-pyrimidine inhibitors of kinases |
| US8133900B2 (en) | 2005-11-01 | 2012-03-13 | Targegen, Inc. | Use of bi-aryl meta-pyrimidine inhibitors of kinases |
| MX2008008320A (es) | 2005-12-23 | 2008-09-03 | Smithkline Beecham Corp | Inhibidores de azaindol de aurora cinasas. |
| BRPI0706560A2 (pt) | 2006-01-17 | 2011-03-29 | Hoffmann La Roche | derivados de aril-isoxazol-4-il-imidazo [1,2-a] piridina úteis para o tratamento de doença de alzheimer por intermédio de receptores gaba |
| ZA200806871B (en) | 2006-02-14 | 2009-10-28 | Vertex Pharma | Dihydrodiazepines useful as inhibitors of protein kinases |
| ATE479434T1 (de) | 2006-02-14 | 2010-09-15 | Vertex Pharma | Als protein-kinase-inhibitoren nutzbare dyhydrodiazepine |
| US20070218135A1 (en) | 2006-03-14 | 2007-09-20 | Glenmark Pharmaceuticals Limited | Sustained release matrix pharmaceutical composition |
| AU2007248112A1 (en) | 2006-05-03 | 2007-11-15 | Novartis Ag | Use of organic compounds |
| EP2029599A1 (en) | 2006-05-19 | 2009-03-04 | Astra Zeneca AB | Dihydropteridine compounds as anti proliferative agents |
| WO2008009909A1 (en) | 2006-07-17 | 2008-01-24 | Astrazeneca Ab | Pteridimones as modulators of polo-like kinase |
| CN105693730A (zh) | 2006-10-19 | 2016-06-22 | 西格诺药品有限公司 | 杂芳基化合物、其组合物以及它们作为蛋白激酶抑制剂的用途 |
| US8338464B2 (en) | 2006-11-30 | 2012-12-25 | Albert Einstein College Of Medicine Of Yeshiva University | Small molecule inhibitors of BCL6 |
| JP2008156311A (ja) | 2006-12-26 | 2008-07-10 | Institute Of Physical & Chemical Research | Ｂｒｄ２ブロモドメイン結合剤 |
| TWI618544B (zh) | 2006-12-26 | 2018-03-21 | 藍瑟斯醫學影像公司 | 使心臟神經分布顯像之配位體 |
| KR101157848B1 (ko) | 2007-03-22 | 2012-07-11 | 다케다 야쿠힌 고교 가부시키가이샤 | Ｐｌｋ１ 저해제로서 유용한 치환된 피리미도디아제핀 |
| WO2008137081A1 (en) | 2007-05-02 | 2008-11-13 | The Trustees Of Columbia University In The City Of New York | Substituted ( 5, 6 ) -dihydronaphraalenyl compounds as reversible male contraceptives |
| KR20080107050A (ko) | 2007-06-05 | 2008-12-10 | 울산대학교 산학협력단 | 항-ｃｄ１３７ 단일클론 항체를 포함하는 만성이식편대숙주 질환의 예방 또는 치료용 약학적 조성물 |
| CA2695753A1 (en) | 2007-08-15 | 2009-02-19 | Vertex Pharmaceuticals Incorporated | Compounds useful as protein kinases inhibitors |
| EA019487B1 (ru) | 2007-09-25 | 2014-04-30 | Такеда Фармасьютикал Компани Лимитед | Соединения в качестве ингибиторов plk, фармацевтические композиции, их содержащие, и их применение |
| EP2610256B1 (en) | 2007-09-28 | 2016-04-27 | Cyclacel Limited | Pyrimidine derivatives as protein kinase inhibitors |
| WO2009067547A1 (en) | 2007-11-19 | 2009-05-28 | Takeda Pharmaceutical Company Limited | Polo-like kinase inhibitors |
| CA2710118A1 (en) | 2007-12-20 | 2009-07-02 | Cellzome Limited | Sulfamides as zap-70 inhibitors |
| JP5478262B2 (ja) | 2007-12-28 | 2014-04-23 | 田辺三菱製薬株式会社 | 抗癌剤 |
| DK2283024T3 (da) | 2008-03-10 | 2013-08-05 | Janssen Pharmaceutica Nv | 4-aryl-2-anilinpyrimidiner som PLK-kinaseinhibitorer |
| EP2276747A1 (en) | 2008-03-11 | 2011-01-26 | Cellzome Limited | Sulfonamides as zap-70 inhibitors |
| FR2928923B1 (fr) | 2008-03-21 | 2010-04-23 | Sanofi Aventis | Derives polysubstitues de 2-heteroaryl-6-phenyl-imidazo °1,2-a!pyridines, leur preparation et leur application en therapeutiques |
| EP2112152A1 (en) | 2008-04-22 | 2009-10-28 | GPC Biotech AG | Dihydropteridinones as Plk Inhibitors |
| JP2011527667A (ja) | 2008-06-18 | 2011-11-04 | 武田薬品工業株式会社 | ハロ置換ピリミドジアゼピン |
| WO2010015340A1 (en) | 2008-08-06 | 2010-02-11 | Bayer Schering Pharma Aktiengesellschaft | Daa-pyridine as peripheral benzodiazepine receptor ligand for diagnostic imaging and pharmaceutical treatment |
| WO2010032195A1 (en) | 2008-09-16 | 2010-03-25 | Csir | Imidazopyridines and imidazopyrimidines as hiv-i reverse transcriptase inhibitors |
| EP2362876B1 (en) | 2008-10-30 | 2013-12-11 | Circomed LLC | Thienotriazolodiazepine derivatives active on apo a |
| EP2379559B1 (en) | 2009-01-06 | 2017-10-25 | Dana-Farber Cancer Institute, Inc. | Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders |
| CA2750106A1 (en) | 2009-01-23 | 2010-07-29 | Takeda Pharmaceutical Company Limited | Poly (adp-ribose) polymerase (parp) inhibitors |
| CN102020643A (zh) | 2009-09-22 | 2011-04-20 | 上海恒瑞医药有限公司 | 二氢喋啶酮类衍生物、其制备方法及其在医药上的应用 |
| JP2013505927A (ja) | 2009-09-25 | 2013-02-21 | バーテックス ファーマシューティカルズ インコーポレイテッド | プロテインキナーゼ阻害剤として有用なピリミジン誘導体の調製方法 |
| GB0919431D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| DK2722334T3 (en) | 2009-11-05 | 2016-03-07 | Glaxosmithkline Llc | benzodiazepine bromdomæneinhibitor |
| GB0919434D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919432D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| HUE026967T2 (en) * | 2009-11-05 | 2016-07-28 | Glaxosmithkline Llc | Benzodiazepine Bromodomain inhibitor |
| GB0919433D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919426D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| JP5841548B2 (ja) | 2010-02-17 | 2016-01-13 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ジヒドロプテリジノン、その製造方法及び使用 |
| US9301962B2 (en) * | 2010-05-14 | 2016-04-05 | Baylor College Of Medicine | Male contraceptive compositions and methods of use |
| CA2799403C (en) * | 2010-05-14 | 2020-01-21 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for treating leukemia |
| JP5913292B2 (ja) | 2010-05-14 | 2016-04-27 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | 代謝を調節する組成物および方法 |
| JP5715241B2 (ja) * | 2010-05-14 | 2015-05-07 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | 新生物、炎症性疾患、およびその他の障害を治療するための組成物および方法 |
| DK2571503T3 (en) | 2010-05-14 | 2015-04-20 | Dana Farber Cancer Inst Inc | COMPOSITIONS AND THEIR USE IN THE TREATMENT OF NEOPLASIA, INFLAMMATORY DISEASE AND OTHER DISORDERS |
| ES2526671T3 (es) | 2010-06-22 | 2015-01-14 | Glaxosmithkline Llc | Compuestos de benzotriazoldiazepina inhibidores de bromodominios |
| US20120014979A1 (en) | 2010-07-16 | 2012-01-19 | Alexander Dent | Use of bcl6 inhibitors for treating autoimmune diseases |
| US9358233B2 (en) | 2010-11-29 | 2016-06-07 | Boehringer Ingelheim International Gmbh | Method for treating acute myeloid leukemia |
| US9249161B2 (en) * | 2010-12-02 | 2016-02-02 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| CA2828212A1 (en) | 2011-02-23 | 2012-08-30 | Shiraz Mujtaba | Inhibitors of bromodomains as modulators of gene expression |
| EP3323820B1 (en) | 2011-02-28 | 2023-05-10 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| JP2014513925A (ja) | 2011-03-07 | 2014-06-19 | フォンダッツィオーネ・テレソン | Ｔｆｅｂ変異体およびその使用 |
| GB201106799D0 (en) | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| WO2013033269A1 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same |
| WO2013033270A2 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bromodomain ligands capable of dimerizing in an aqueous solution, and methods of using same |
| DE102011082013A1 (de) | 2011-09-01 | 2013-03-07 | Bayer Pharma AG | 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine |
| WO2013097052A1 (en) | 2011-12-30 | 2013-07-04 | Abbott Laboratories | Bromodomain inhibitors |
| EP2841092B1 (en) | 2012-02-17 | 2023-12-06 | Ansun Biopharma, Inc. | Compounds and compositions for use in a method of treatment of parainfluenza virus |
| WO2013148197A1 (en) | 2012-03-28 | 2013-10-03 | The J. David Gladstone Institutes | Compositions and methods for reactivating latent immunodeficiency virus |
| SG11201500291TA (en) | 2012-08-08 | 2015-04-29 | Novomatic Ag | Method of and system for tracking gaming activity |
| HK1208448A1 (en) * | 2012-09-28 | 2016-03-04 | Bayer Pharma Aktiengesellschaft | Bet protein-inhibiting 5-aryl triazole azepines |
| KR20150100613A (ko) | 2012-09-28 | 2015-09-02 | 온코에틱스 게엠베하 | 티에노트리아졸로디아제핀 화합물을 함유하는 약제학적 제제 |
| US9567301B2 (en) | 2012-11-02 | 2017-02-14 | Dana-Farber Cancer Institute, Inc. | Pyrrol-1-yl benzoic acid derivatives useful as myc inhibitors |
| EP2935260A1 (de) | 2012-12-20 | 2015-10-28 | Bayer Pharma Aktiengesellschaft | Bet-proteininhibitorische dihydropyridopyrazinone |
| US20140254659A1 (en) | 2013-03-11 | 2014-09-11 | Mediatek Inc. | Video coding method using at least evaluated visual quality and related video coding apparatus |
| US8980879B2 (en) | 2013-03-11 | 2015-03-17 | Abbvie Inc. | Bromodomain inhibitors |
| JP6419735B2 (ja) | 2013-03-12 | 2018-11-07 | アッヴィ・インコーポレイテッド | 四環系ブロモドメイン阻害剤 |
| RU2015139054A (ru) | 2013-03-14 | 2017-04-19 | Дженентек, Инк. | Способы лечения рака и профилактики лекарственной резистентности рака |
| WO2014159392A1 (en) | 2013-03-14 | 2014-10-02 | Dana-Farber Cancer Institute, Inc. | Bromodomain binding reagents and uses thereof |
| CA2918910A1 (en) | 2013-07-25 | 2015-01-29 | Dana-Farber Cancer Institute, Inc. | Inhibitors of transcription factors and uses thereof |
| JP6663852B2 (ja) | 2013-09-19 | 2020-03-13 | デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド | Ｂｈ３プロファイリングの方法 |
| WO2015081284A1 (en) | 2013-11-26 | 2015-06-04 | Coferon, Inc. | Bivalent bromodomain ligands, and methods of using same |
| WO2015081280A1 (en) | 2013-11-26 | 2015-06-04 | Coferon, Inc. | Bromodomain ligands capable of dimerizing in an aqueous solution |
| AU2014361381A1 (en) | 2013-12-10 | 2016-06-16 | Abbvie Inc. | Bromodomain inhibitors |
| CN105940005A (zh) | 2014-01-31 | 2016-09-14 | 达纳-法伯癌症研究所股份有限公司 | 二氮杂环庚烷衍生物及其用途 |
| CA2936871A1 (en) | 2014-01-31 | 2015-08-06 | Dana-Farber Cancer Institute, Inc. | Dihydropteridinone derivatives and uses thereof |
| CN106029653A (zh) | 2014-01-31 | 2016-10-12 | 达纳-法伯癌症研究所股份有限公司 | 二氨基嘧啶苯砜衍生物及其用途 |
| US10793571B2 (en) | 2014-01-31 | 2020-10-06 | Dana-Farber Cancer Institute, Inc. | Uses of diazepane derivatives |
| WO2015129927A1 (en) * | 2014-02-26 | 2015-09-03 | Kyorin Pharmaceutical Co., Ltd. | Heterocyclic compounds |
| MX377534B (es) * | 2014-02-28 | 2025-03-10 | Tensha Therapeutics Inc | Compuestos para usarse en el tratamiento de hiperinsulinemia. |
| US20180228907A1 (en) * | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| MX2017001756A (es) | 2014-08-08 | 2017-05-30 | Dana Farber Cancer Inst Inc | Derivados de diazepano y sus usos. |
| MX2017001757A (es) | 2014-08-08 | 2017-05-30 | Dana Farber Cancer Inst Inc | Derivados de dihidropteridinona y sus usos. |
| WO2016090219A1 (en) * | 2014-12-05 | 2016-06-09 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Bromodomain inhibitor as adjuvant in cancer immunotherapy |
| US9694084B2 (en) * | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| JP6815318B2 (ja) | 2014-12-23 | 2021-01-20 | ダナ−ファーバー キャンサー インスティテュート，インコーポレイテッド | 二官能性分子によって標的化タンパク質分解を誘導する方法 |
| CN108601764A (zh) * | 2015-03-18 | 2018-09-28 | 阿尔维纳斯股份有限公司 | 用于靶蛋白的增强降解的化合物和方法 |
| US10702527B2 (en) * | 2015-06-12 | 2020-07-07 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| WO2017007612A1 (en) * | 2015-07-07 | 2017-01-12 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| EP3331906A1 (en) * | 2015-08-06 | 2018-06-13 | Dana-Farber Cancer Institute, Inc. | Tunable endogenous protein degradation |
| EP3337476A4 (en) * | 2015-08-19 | 2019-09-04 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| MX377277B (es) | 2015-09-04 | 2025-03-07 | Hoffmann La Roche | Derivados de fenoximetilo. |
| PT3347356T (pt) * | 2015-09-09 | 2021-06-28 | Jubilant Biosys Ltd | Derivados tricíclicos de piridinaa-2-ona fundidos e a sua utilização como inibidores brd4 |
| CR20180199A (es) * | 2015-09-11 | 2018-05-25 | Dana Farber Cancer Inst Inc | Acetamida tienotriazolodiazepinas y usos de las mismas |
| HK1256417A1 (zh) * | 2015-09-11 | 2019-09-20 | 达纳-法伯癌症研究所股份有限公司 | 氰基噻吩並三唑並二氮雜環庚三烯及其用途 |
| US9845314B2 (en) | 2015-09-11 | 2017-12-19 | Boehrnger Ingelheim International Gmbh | Pyrazolyl-substituted heteroaryls and their use as medicaments |
| EA201890949A1 (ru) | 2015-11-25 | 2018-12-28 | Джилид Аполло, Ллс | СЛОЖНОЭФИРНЫЕ ИНГИБИТОРЫ АЦЕТИЛ-КоА-КАРБОКСИЛАЗЫ И ВАРИАНТЫ ИХ ПРИМЕНЕНИЯ |
| JP2019502660A (ja) | 2015-11-25 | 2019-01-31 | ギリアド アポロ， エルエルシー | ピラゾールａｃｃ阻害剤およびその使用 |
| EP3888658B1 (en) | 2015-11-25 | 2023-12-27 | Effector Therapeutics, Inc. | Eif4-a-inhibiting compounds and methods related thereto |
| RU2742035C2 (ru) | 2015-11-25 | 2021-02-01 | Дана-Фарбер Кэнсер Инститьют, Инк. | Бивалентные ингибиторы бромодоменов и пути их применения |
| EA201890910A1 (ru) | 2015-11-25 | 2018-11-30 | Джилид Аполло, Ллс | ФУНГИЦИДНЫЕ КОМПОЗИЦИИ, СОДЕРЖАЩИЕ ПРОИЗВОДНЫЕ 2,4-ДИОКСО-1,4-ДИГИДРОТИЕНО[2,3-d]ПИРИМИДИНА |
| CN109089419B (zh) | 2015-11-25 | 2024-03-01 | 威特拉公司 | April的抗体分子及其应用 |
| BR112018010453B1 (pt) | 2015-11-25 | 2022-06-14 | Gilead Apollo, Llc | Compostos triazólicos inibindores de acetil coa carboxilase (acc) |
| AU2016362040B2 (en) | 2015-12-01 | 2019-10-10 | Nihon Nohyaku Co., Ltd. | 3H-pyrrolopyridine compound, N-oxide thereof or salt thereof, agricultural and horticultural insecticide comprising the compound and method for using the same |
| CN109641874A (zh) * | 2016-05-10 | 2019-04-16 | C4医药公司 | 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体 |
| CN109790143A (zh) * | 2016-05-10 | 2019-05-21 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
| WO2017201069A1 (en) * | 2016-05-18 | 2017-11-23 | Biotheryx, Inc. | Oxoindoline derivatives as protein function modulators |
| GB201608797D0 (en) | 2016-05-19 | 2016-07-06 | Ucb Biopharma Sprl | Therapeutic use |
| WO2018064589A1 (en) * | 2016-09-29 | 2018-04-05 | Dana-Farber Cancer Institute, Inc. | Targeted protein degradation using a mutant e3 ubiquitin ligase |
-
2016
- 2016-09-09 CR CR20180199A patent/CR20180199A/es unknown
- 2016-09-09 RU RU2018112953A patent/RU2018112953A/ru unknown
- 2016-09-09 MX MX2018003030A patent/MX2018003030A/es unknown
- 2016-09-09 BR BR112018004617A patent/BR112018004617A2/pt not_active IP Right Cessation
- 2016-09-09 SG SG10202007099TA patent/SG10202007099TA/en unknown
- 2016-09-09 KR KR1020187009781A patent/KR20180051576A/ko not_active Withdrawn
- 2016-09-09 AU AU2016319785A patent/AU2016319785C1/en not_active Ceased
- 2016-09-09 PE PE2018000377A patent/PE20181086A1/es unknown
- 2016-09-09 WO PCT/US2016/051017 patent/WO2017044792A1/en not_active Ceased
- 2016-09-09 US US15/758,787 patent/US10881668B2/en active Active
- 2016-09-09 CN CN201680062105.7A patent/CN108472299A/zh active Pending
- 2016-09-09 JP JP2018513363A patent/JP2018526424A/ja active Pending
- 2016-09-09 HK HK18115551.9A patent/HK1256419A1/zh unknown
- 2016-09-09 UA UAA201803875A patent/UA123946C2/uk unknown
- 2016-09-09 EP EP16845148.2A patent/EP3347020A4/en not_active Withdrawn
- 2016-09-09 CA CA2996977A patent/CA2996977A1/en not_active Abandoned
-
2018
- 2018-02-19 IL IL257593A patent/IL257593A/en unknown
- 2018-03-06 ZA ZA2018/01549A patent/ZA201801549B/en unknown
- 2018-03-07 PH PH12018550026A patent/PH12018550026A1/en unknown
- 2018-03-09 CL CL2018000622A patent/CL2018000622A1/es unknown
- 2018-03-12 CO CONC2018/0002568A patent/CO2018002568A2/es unknown
-
2020
- 2020-09-09 US US17/016,084 patent/US11406645B2/en active Active
- 2020-12-21 AU AU2020294169A patent/AU2020294169B2/en not_active Expired - Fee Related
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2018112953A (ru) | Ацетамидтиенотриазолодиазепины и пути их применения | |
| RU2018112961A (ru) | Цианотиенотриазолодиазепины и пути их применения | |
| JP2018526424A5 (enExample) | ||
| RU2018122641A (ru) | Бивалентные ингибиторы бромодоменов и пути их применения | |
| JP2017504650A5 (enExample) | ||
| RU2017104897A (ru) | Производные диазепана и их применения | |
| JP2018526421A5 (enExample) | ||
| JP2017504651A5 (enExample) | ||
| RU2016134941A (ru) | Производные диазепана и их применения | |
| RU2017104898A (ru) | Дигидроптеридиноновые производные и их применения | |
| EP2909214B1 (en) | Etp derivatives | |
| Zhang et al. | Design, synthesis and biological evaluation of novel 1, 2, 4-triazolo [3, 4-b][1, 3, 4] thiadiazines bearing furan and thiophene nucleus | |
| RU2016134947A (ru) | Производные диаминопиримидин бензолсульфона и их применение | |
| WO2013033270A2 (en) | Bromodomain ligands capable of dimerizing in an aqueous solution, and methods of using same | |
| JP2009519222A5 (enExample) | ||
| Ashok et al. | Design, synthesis of new β-carboline derivatives and their selective anti-HIV-2 activity | |
| JP2018538281A5 (enExample) | ||
| WO2015081280A1 (en) | Bromodomain ligands capable of dimerizing in an aqueous solution | |
| WO2013033269A1 (en) | Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same | |
| AR108223A1 (es) | Derivados de 6-oxo-1,6-dihidro-piridin-3-il | |
| MA38323B1 (fr) | Dérivés pyrimidone et leur utilisation dans le traitement, l'amélioration ou la prévention d'une maladie virale | |
| AU2016229136A1 (en) | DNA alkylating agents | |
| JP2015503622A5 (enExample) | ||
| WO2016040084A1 (en) | Inhibitors of human immunodeficiency virus replication | |
| WO2015187998A2 (en) | Use of inhibitor of apoptosis protein (iap) antagonists in hiv therapy |