ES2526671T3 - Compuestos de benzotriazoldiazepina inhibidores de bromodominios - Google Patents
Compuestos de benzotriazoldiazepina inhibidores de bromodominios Download PDFInfo
- Publication number
- ES2526671T3 ES2526671T3 ES11725769.1T ES11725769T ES2526671T3 ES 2526671 T3 ES2526671 T3 ES 2526671T3 ES 11725769 T ES11725769 T ES 11725769T ES 2526671 T3 ES2526671 T3 ES 2526671T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- ring
- carbocyclyl
- groups
- elements
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 102000001805 Bromodomains Human genes 0.000 title 1
- 108050009021 Bromodomains Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- -1 -CO-carbocyclyl Chemical group 0.000 abstract description 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 10
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000004452 carbocyclyl group Chemical group 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 229910052717 sulfur Inorganic materials 0.000 abstract 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000006528 (C2-C6) alkyl group Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 125000005884 carbocyclylalkyl group Chemical group 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 9
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 6
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
- BDAGIHXWWSANSR-UHFFFAOYSA-M Formate Chemical compound [O-]C=O BDAGIHXWWSANSR-UHFFFAOYSA-M 0.000 description 3
- 239000012074 organic phase Substances 0.000 description 3
- 239000011541 reaction mixture Substances 0.000 description 3
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 description 2
- YNHIGQDRGKUECZ-UHFFFAOYSA-L bis(triphenylphosphine)palladium(ii) dichloride Chemical compound [Cl-].[Cl-].[Pd+2].C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 YNHIGQDRGKUECZ-UHFFFAOYSA-L 0.000 description 2
- 238000004895 liquid chromatography mass spectrometry Methods 0.000 description 2
- 229910000029 sodium carbonate Inorganic materials 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- ITMCEJHCFYSIIV-UHFFFAOYSA-M triflate Chemical compound [O-]S(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-M 0.000 description 2
- VOAAEKKFGLPLLU-UHFFFAOYSA-N (4-methoxyphenyl)boronic acid Chemical compound COC1=CC=C(B(O)O)C=C1 VOAAEKKFGLPLLU-UHFFFAOYSA-N 0.000 description 1
- NEUWPDLMDVINSN-UHFFFAOYSA-N 1h-pyrazol-5-ylboronic acid Chemical compound OB(O)C=1C=CNN=1 NEUWPDLMDVINSN-UHFFFAOYSA-N 0.000 description 1
- PJPRMRNFJZOFLA-FQEVSTJZSA-N 2-[(4s)-6-(4-chlorophenyl)-1-methyl-8-(1h-pyrazol-4-yl)-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-n-ethylacetamide Chemical compound N([C@H](C1=NN=C(C)N1C1=CC=C(C=C11)C2=CNN=C2)CC(=O)NCC)=C1C1=CC=C(Cl)C=C1 PJPRMRNFJZOFLA-FQEVSTJZSA-N 0.000 description 1
- WMKQEPQCESYBNS-FQEVSTJZSA-N 2-[(4s)-6-(4-chlorophenyl)-1-methyl-8-(1h-pyrazol-5-yl)-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-n-ethylacetamide Chemical compound N([C@H](C1=NN=C(C)N1C1=CC=C(C=C11)C=2NN=CC=2)CC(=O)NCC)=C1C1=CC=C(Cl)C=C1 WMKQEPQCESYBNS-FQEVSTJZSA-N 0.000 description 1
- DBNRUVQIPZTZFK-DEOSSOPVSA-N 2-[(4s)-6-(4-chlorophenyl)-8-(4-methoxyphenyl)-1-methyl-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-n-ethylacetamide Chemical compound N([C@H](C1=NN=C(C)N1C1=CC=C(C=C11)C=2C=CC(OC)=CC=2)CC(=O)NCC)=C1C1=CC=C(Cl)C=C1 DBNRUVQIPZTZFK-DEOSSOPVSA-N 0.000 description 1
- UXRDAJMOOGEIAQ-CKOZHMEPSA-N [(8r,9s,10r,13s,14s,17r)-17-acetyl-10,13-dimethyl-16-methylidene-3-oxo-1,2,8,9,11,12,14,15-octahydrocyclopenta[a]phenanthren-17-yl] acetate Chemical compound C1=CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC(=C)[C@](OC(=O)C)(C(C)=O)[C@@]1(C)CC2 UXRDAJMOOGEIAQ-CKOZHMEPSA-N 0.000 description 1
- 229910021529 ammonia Inorganic materials 0.000 description 1
- 239000008346 aqueous phase Substances 0.000 description 1
- 239000012267 brine Substances 0.000 description 1
- 239000003607 modifier Substances 0.000 description 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 description 1
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
- 239000007787 solid Substances 0.000 description 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
-
- 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
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB201010514 | 2010-06-22 | ||
| GBGB1010514.6A GB201010514D0 (en) | 2010-06-22 | 2010-06-22 | Novel compounds |
| GB201106801 | 2011-04-21 | ||
| GBGB1106801.2A GB201106801D0 (en) | 2011-04-21 | 2011-04-21 | Novel compounds |
| PCT/EP2011/060179 WO2011161031A1 (en) | 2010-06-22 | 2011-06-20 | Benzotriazolodiazepine compounds inhibitors of bromodomains |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2526671T3 true ES2526671T3 (es) | 2015-01-14 |
Family
ID=44310320
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES11725769.1T Active ES2526671T3 (es) | 2010-06-22 | 2011-06-20 | Compuestos de benzotriazoldiazepina inhibidores de bromodominios |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US9085582B2 (enExample) |
| EP (1) | EP2585465B1 (enExample) |
| JP (1) | JP5844358B2 (enExample) |
| ES (1) | ES2526671T3 (enExample) |
| WO (1) | WO2011161031A1 (enExample) |
Families Citing this family (81)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8440693B2 (en) | 2009-12-22 | 2013-05-14 | Novartis Ag | Substituted isoquinolinones and quinazolinones |
| MX373121B (es) | 2010-05-14 | 2020-04-30 | Dana Farber Cancer Inst Inc | Composiciones y metodos para el tratamiento de leucemia. |
| MX384074B (es) | 2010-05-14 | 2025-03-12 | Dana Farber Cancer Inst Inc | Composiciones y métodos para tratar neoplasias, enfermedades inflamatorias y otros trastornos. |
| US9301962B2 (en) | 2010-05-14 | 2016-04-05 | Baylor College Of Medicine | Male contraceptive compositions and methods of use |
| 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 |
| EP2705039B1 (en) | 2011-05-04 | 2017-07-26 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| US9328117B2 (en) | 2011-06-17 | 2016-05-03 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| WO2013027168A1 (en) | 2011-08-22 | 2013-02-28 | Pfizer Inc. | Novel heterocyclic compounds as bromodomain inhibitors |
| WO2013033270A2 (en) * | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bromodomain ligands capable of dimerizing in an aqueous solution, and methods of using same |
| WO2013033269A1 (en) * | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same |
| US8969341B2 (en) | 2011-11-29 | 2015-03-03 | Novartis Ag | Pyrazolopyrrolidine compounds |
| WO2013097052A1 (en) * | 2011-12-30 | 2013-07-04 | Abbott Laboratories | Bromodomain inhibitors |
| JP6171003B2 (ja) | 2012-05-24 | 2017-07-26 | ノバルティス アーゲー | ピロロピロリジノン化合物 |
| US9624244B2 (en) | 2012-06-06 | 2017-04-18 | Constellation Pharmaceuticals, Inc. | Benzo [B] isoxazoloazepine bromodomain inhibitors and uses thereof |
| TWI602820B (zh) * | 2012-06-06 | 2017-10-21 | 星宿藥物公司 | 溴域抑制劑及其用途 |
| HK1208448A1 (en) * | 2012-09-28 | 2016-03-04 | Bayer Pharma Aktiengesellschaft | Bet protein-inhibiting 5-aryl triazole azepines |
| US9422290B2 (en) | 2012-11-13 | 2016-08-23 | Boehringer Ingelheim International Gmbh | Triazolopyridazine |
| US9266891B2 (en) | 2012-11-16 | 2016-02-23 | Boehringer Ingelheim International Gmbh | Substituted [1,2,4]triazolo[4,3-A]pyrazines that are BRD4 inhibitors |
| US9403827B2 (en) | 2013-01-22 | 2016-08-02 | Novartis Ag | Substituted purinone compounds |
| US9556180B2 (en) | 2013-01-22 | 2017-01-31 | Novartis Ag | Pyrazolo[3,4-d]pyrimidinone compounds as inhibitors of the P53/MDM2 interaction |
| JP2016513117A (ja) * | 2013-02-22 | 2016-05-12 | バイエル ファーマ アクチエンゲゼルシャフト | 過剰増殖性疾患を治療するためのｂｅｔタンパク質阻害剤としてのピロロ−およびピラゾロ−トリアゾロジアゼピン類 |
| EP2970285B1 (en) | 2013-03-11 | 2019-04-17 | AbbVie Inc. | Fused tetracyclic bromodomain inhibitors |
| JP6401773B2 (ja) | 2013-03-11 | 2018-10-10 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | Ｂｅｔブロモドメイン阻害剤およびこれを用いる治療方法 |
| JP2016512524A (ja) | 2013-03-11 | 2016-04-28 | アッヴィ・インコーポレイテッド | ブロモドメイン阻害剤 |
| CN105026403B (zh) * | 2013-03-12 | 2018-05-18 | 艾伯维公司 | 四环布罗莫结构域抑制剂 |
| US9714946B2 (en) | 2013-03-14 | 2017-07-25 | Dana-Farber Cancer Institute, Inc. | Bromodomain binding reagents and uses thereof |
| US9227985B2 (en) | 2013-03-15 | 2016-01-05 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| WO2014173241A1 (en) | 2013-04-26 | 2014-10-30 | Beigene, Ltd. | Substituted5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones |
| CA2913697A1 (en) | 2013-05-27 | 2014-12-04 | Novartis Ag | Imidazopyrrolidinone derivatives and their use in the treatment of disease |
| US8975417B2 (en) | 2013-05-27 | 2015-03-10 | Novartis Ag | Pyrazolopyrrolidine derivatives and their use in the treatment of disease |
| CA2912986A1 (en) | 2013-05-28 | 2014-12-04 | Novartis Ag | Pyrazolo-pyrrolidin-4-one derivatives as bet inhibitors and their use in the treatment of disease |
| CA2912991A1 (en) | 2013-05-28 | 2014-12-04 | Novartis Ag | Pyrazolo-pyrrolidin-4-one derivatives and their use in the treatment of disease |
| EP3019502B1 (en) | 2013-07-08 | 2017-05-17 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors |
| WO2015013635A2 (en) | 2013-07-25 | 2015-01-29 | Dana-Farber Cancer Institute, Inc. | Inhibitors of transcription factors and uses thereof |
| EP3066101B1 (en) | 2013-11-08 | 2020-07-29 | Dana-Farber Cancer Institute, Inc. | Combination therapy for cancer using bromodomain and extra-terminal (bet) protein inhibitors |
| MX2016006667A (es) | 2013-11-21 | 2016-07-26 | Novartis Ag | Derivados de pirrolo-pirrolona y su uso como inhibidores. |
| US9399640B2 (en) | 2013-11-26 | 2016-07-26 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| GB201320994D0 (en) * | 2013-11-28 | 2014-01-15 | Univ Dundee | Enzyme function probes |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| WO2015117087A1 (en) | 2014-01-31 | 2015-08-06 | Dana-Farber Cancer Institute, Inc. | Uses of diazepane derivatives |
| JP2017504650A (ja) | 2014-01-31 | 2017-02-09 | 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 | ジアゼパン誘導体およびその使用 |
| EP3099677A4 (en) | 2014-01-31 | 2017-07-26 | Dana-Farber Cancer Institute, Inc. | Diaminopyrimidine benzenesulfone derivatives and uses thereof |
| JP2017511801A (ja) | 2014-02-28 | 2017-04-27 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | ＢＥＴブロモドメイン阻害剤としての９Ｈ−ピリミド［４，５−ｂ］インドールおよび関連類似体 |
| KR20160130778A (ko) | 2014-02-28 | 2016-11-14 | 텐샤 세러퓨틱스 인코포레이티드 | 고인슐린혈증과 관련된 질환의 치료 |
| MY180775A (en) | 2014-04-23 | 2020-12-09 | Incyte Corp | 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins |
| PL3157928T3 (pl) | 2014-06-20 | 2019-07-31 | Constellation Pharmaceuticals, Inc. | Krystaliczne postacie 2-((4S)-6-(4-chlorofenylo)-1-metylo-4H-benzo[ c]izoksazolo-[4,5-e]azepin-4-ylo)acetamidu |
| MX2017001757A (es) | 2014-08-08 | 2017-05-30 | Dana Farber Cancer Inst Inc | Derivados de dihidropteridinona y sus usos. |
| EP3177626A4 (en) | 2014-08-08 | 2017-12-27 | Dana Farber Cancer Institute, Inc. | Diazepane derivatives and uses thereof |
| US9527864B2 (en) | 2014-09-15 | 2016-12-27 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| AU2015339511B2 (en) | 2014-10-27 | 2020-05-14 | Tensha Therapeutics, Inc. | Bromodomain inhibitors |
| US10307407B2 (en) | 2015-02-27 | 2019-06-04 | The Regents Of The University Of Michigan | 9H-pyrimido [4,5-B] indoles as BET bromodomain inhibitors |
| GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
| DK3277683T3 (en) | 2015-03-30 | 2022-05-02 | Jubilant Biosys Ltd | Tricyklisk sammensmeltet afledt af 1-(cyklo)alkyl pyridin-2-one nyttig til behandling af kræft |
| WO2016196065A1 (en) | 2015-05-29 | 2016-12-08 | Genentech, Inc. | Methods and compositions for assessing responsiveness of cancers to bet inhibitors |
| EP3307728A4 (en) | 2015-06-12 | 2019-07-17 | Dana Farber Cancer Institute, Inc. | COMBINATION THERAPY OF TRANSCRIPTION INHIBITORS AND CHINESE INHIBITORS |
| WO2016203335A1 (en) | 2015-06-18 | 2016-12-22 | Pfizer Inc. | Novel pyrido[2,3-b]pyrazinones as bet-family bromodomain inhibitors |
| BR112017028178A2 (en) | 2015-06-26 | 2018-08-28 | Tensha Therapeutics, Inc. | nut midline carcinoma treatment |
| UA123946C2 (uk) | 2015-09-11 | 2021-06-30 | Дана-Фарбер Кенсер Інстітьют, Інк. | Ацетамідтієнотриазолодіазепіни й шляхи їх застосування |
| PE20181287A1 (es) | 2015-09-11 | 2018-08-07 | Dana Farber Cancer Inst Inc | Ciano tienotriazolpirazinas y usos de las mismas |
| WO2017075377A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| CA3003288A1 (en) | 2015-11-25 | 2017-06-01 | Dana-Farber Cancer Institute, Inc. | Bivalent bromodomain inhibitors and uses thereof |
| JP6967522B2 (ja) | 2016-02-15 | 2021-11-17 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | Ｂｅｔブロモドメイン阻害剤としての融合１，４−オキサゼピンおよび関連類似体 |
| AU2017246453A1 (en) | 2016-04-06 | 2018-11-08 | The Regents Of The University Of Michigan | Monofunctional intermediates for ligand-dependent target protein degradation |
| JP7037500B2 (ja) | 2016-04-06 | 2022-03-16 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | Ｍｄｍ２タンパク質分解剤 |
| AU2017250076B2 (en) | 2016-04-12 | 2021-07-22 | The Regents Of The University Of Michigan | Bet protein degraders |
| ES2793239T3 (es) | 2016-04-15 | 2020-11-13 | Abbvie Inc | Inhibidores del bromodominio |
| KR102643344B1 (ko) | 2016-06-20 | 2024-03-07 | 인사이트 코포레이션 | Bet 저해제의 결정질 고체 형태 |
| WO2018022802A1 (en) | 2016-07-26 | 2018-02-01 | University Of Southern California | Selective bromodomain inhibition of fungal bdf1 |
| ES2857743T3 (es) | 2016-09-13 | 2021-09-29 | Univ Michigan Regents | 1,4-diazepinas fusionadas como degradadores de proteína BET |
| CN110062759B (zh) | 2016-09-13 | 2022-05-24 | 密执安大学评议会 | 作为bet蛋白降解剂的稠合的1,4-氧氮杂䓬 |
| US11046709B2 (en) | 2017-02-03 | 2021-06-29 | The Regents Of The University Of Michigan | Fused 1,4-diazepines as BET bromodomain inhibitors |
| US11267822B2 (en) | 2017-09-13 | 2022-03-08 | The Regents Of The University Of Michigan | BET bromodomain protein degraders with cleavable linkers |
| CN107759607B (zh) * | 2017-11-29 | 2019-08-23 | 上海万巷制药有限公司 | 具有抗肿瘤活性的三氮唑并二氮卓化合物及其制备方法 |
| KR102954013B1 (ko) | 2018-07-25 | 2026-04-16 | 치아타이 티안큉 파마수티컬 그룹 주식회사 | 브로모도메인 단백질 억제제로서의 설폭시민 화합물과 약학적 조성물 및 이의 의학적 용도 |
| WO2021175432A1 (en) | 2020-03-04 | 2021-09-10 | Boehringer Ingelheim International Gmbh | Method for administration of an anti cancer agent |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| AR122707A1 (es) | 2020-06-23 | 2022-09-28 | Genentech Inc | Compuestos macrocíclicos y métodos de uso de los mismos |
| AR124681A1 (es) | 2021-01-20 | 2023-04-26 | Abbvie Inc | Conjugados anticuerpo-fármaco anti-egfr |
| JP2025514712A (ja) | 2022-04-19 | 2025-05-09 | ヌエヴォリューション・アクティーゼルスカブ | ブロモドメインに対して活性な化合物 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3610848A1 (de) | 1986-04-01 | 1987-10-15 | Boehringer Ingelheim Kg | Neue 1,4-diazepine |
| MC1999A1 (fr) * | 1987-12-18 | 1990-01-26 | Hoffmann La Roche | Composes tricycliques |
| GB9004781D0 (en) | 1990-03-02 | 1990-04-25 | Glaxo Group Ltd | Device |
| WO1993007129A1 (fr) | 1991-10-11 | 1993-04-15 | Yoshitomi Pharmaceutical Industries, Ltd. | Medicament utilise pour traiter l'osteoporose et compose de diazepine |
| JPH06128257A (ja) | 1992-10-13 | 1994-05-10 | Yoshitomi Pharmaceut Ind Ltd | ピリドジアゼピン化合物 |
| JP2840454B2 (ja) | 1993-11-22 | 1998-12-24 | メルク エンド カンパニー インコーポレーテッド | ベンゾジアゼピン類 |
| CA2205173A1 (en) | 1994-11-18 | 1996-05-30 | Takeshi Nakamura | Therapeutic agent for osteoporosis and triazepine compound |
| IL127516A0 (en) | 1996-06-12 | 1999-10-28 | Japan Tobacco Inc | A cytokine production inhibitor |
| DE69717160T2 (de) | 1996-09-13 | 2003-05-08 | Mitsubishi Pharma Corp., Osaka | Thienotriazolodiazepinverbindungen und ihre medizinischen anwendungen |
| CN1901958B (zh) | 2003-11-03 | 2011-03-09 | 葛兰素集团有限公司 | 流体分配装置 |
| SG115845A1 (en) | 2004-03-31 | 2005-10-28 | Univ Singapore | Modulation of trip-br function and method of treating proliferative disorders |
| GB0420970D0 (en) | 2004-09-21 | 2004-10-20 | Smithkline Beecham Corp | Novel triazoloquinoline compounds |
| EP1888594A2 (en) * | 2005-05-16 | 2008-02-20 | Wisys Technology Foundation, Inc. | Gabaergic agents to treat memory deficits |
| 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 |
| CL2007003244A1 (es) * | 2006-11-16 | 2008-04-04 | Millennium Pharm Inc | Compuestos derivados de pirimido[5,4-d][2]benzazepina; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento del cancer. |
| JP2008156311A (ja) | 2006-12-26 | 2008-07-10 | Institute Of Physical & Chemical Research | Ｂｒｄ２ブロモドメイン結合剤 |
| US8476260B2 (en) | 2007-12-28 | 2013-07-02 | Mitsubishi Tanabe Pharma Corporation | Antitumor agent |
| GB0919431D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
-
2011
- 2011-06-20 ES ES11725769.1T patent/ES2526671T3/es active Active
- 2011-06-20 JP JP2013515827A patent/JP5844358B2/ja not_active Expired - Fee Related
- 2011-06-20 WO PCT/EP2011/060179 patent/WO2011161031A1/en not_active Ceased
- 2011-06-20 EP EP11725769.1A patent/EP2585465B1/en not_active Not-in-force
- 2011-06-20 US US13/702,177 patent/US9085582B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| US9085582B2 (en) | 2015-07-21 |
| JP2013529611A (ja) | 2013-07-22 |
| US20130079335A1 (en) | 2013-03-28 |
| EP2585465A1 (en) | 2013-05-01 |
| WO2011161031A1 (en) | 2011-12-29 |
| JP5844358B2 (ja) | 2016-01-13 |
| EP2585465B1 (en) | 2014-11-12 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ES2586908T3 (es) | Derivados de azetidina N-sustituidos | |
| ES2592515T3 (es) | Inhibidores de CDK | |
| RU2510397C2 (ru) | Алкилциклогексиловые эфиры дигидротетраазабензоазуленов | |
| ES2641465T3 (es) | Triazolopirazinas como inhibidores de BRD4 para su uso en el tratamiento del cáncer | |
| ES2552311T3 (es) | Derivados heterocíclicos | |
| ES2640049T3 (es) | Derivados de 3,6-dihidropirimidina 2,4,5,6-sustituidos como inhibidores de la polimerasa del virus de la hepatitis B (VHB) para el tratamiento de, por ejemplo, la hepatitis crónica | |
| ES2688600T3 (es) | Procesos para preparar derivados de dihidropirimidina e intermedios de los mismos | |
| ES2564204T3 (es) | Derivados de pirrolopiridinil-pirimidin-2-il-amina | |
| UY25204A1 (es) | Agonistas de prostaglandinas útiles en el tratamiento de desórdenes óseos | |
| ES2445715T3 (es) | Procedimiento de fabricación de derivados de ácido neuramínico | |
| AR047678A1 (es) | Derivados de benzamidas y su uso como activadores de glucoquinasa | |
| AR067105A1 (es) | Moleculas pequenas que contienen boro | |
| CO6160296A2 (es) | Derivados de acido benzoazepin-oxi-acetico como agonistas de receptores activados por proliferador de peroxisona delta usados para incrementar la lipoproteina de alta densidad-colesterol-colesterol reducir la lipoproteina de baja densidad-colesterol | |
| TW201609079A (zh) | 新穎之異羥肟酸（ｈｙｄｒｏｘａｍｉｃ ａｃｉｄ）衍生物 | |
| AR062159A1 (es) | Compuestos que inhiben el enlace de la proteina smac al inhibidor de proteinas de apoptosis (iap) | |
| RU2009105669A (ru) | Способ получения 3-замещенных 2-амино-5-галогенбензамидов | |
| BRPI0717092B1 (pt) | Processo para preparar azoxistrobina e seu derivado dimetóxi acetal | |
| CY1115643T1 (el) | Διεγερτης νευρογενεσης ή θεραπευτικος παραγων νευροπαθειας που περιλαμβανει παραγωγα αλκυλ αιθερα ή αλας αυτου | |
| BR0313078A (pt) | Composto ou um sal deste farmaceuticamente aceitável, composição farmacêutica, e, uso do composto ou de um sal deste farmaceuticamente aceitável | |
| ES2656110T3 (es) | Procedimiento sintético para la preparación de 1,2-Bencisotiazolin-3-ona | |
| RU2015140387A (ru) | Пиридопиримидиновое или пиримидопиримидиновое соединение, способ получения, фармацевтическая композиция и применение указанных соединений | |
| AR042067A1 (es) | Derivados de anilinopirazol utiles en el tratamiento de la diabetes | |
| BR112019017667A2 (pt) | Fotoiniciador, e, método de síntese dos fotoiniciadores. | |
| ES2595508T3 (es) | Ésteres de glicol de apixabán como intermedios clave e impurezas de la síntesis de apixabán | |
| TW201729B (enExample) |