CO2018005370A2 - Inhibidores de bromodominio bivalentes y usos de los mismos - Google Patents
Inhibidores de bromodominio bivalentes y usos de los mismosInfo
- Publication number
- CO2018005370A2 CO2018005370A2 CONC2018/0005370A CO2018005370A CO2018005370A2 CO 2018005370 A2 CO2018005370 A2 CO 2018005370A2 CO 2018005370 A CO2018005370 A CO 2018005370A CO 2018005370 A2 CO2018005370 A2 CO 2018005370A2
- Authority
- CO
- Colombia
- Prior art keywords
- bivalent
- bromodominiums
- bromodomain
- compounds
- inhibitors
- Prior art date
Links
- 102000001805 Bromodomains Human genes 0.000 title abstract 4
- 108050009021 Bromodomains Proteins 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 108091005625 BRD4 Proteins 0.000 abstract 2
- 102100029895 Bromodomain-containing protein 4 Human genes 0.000 abstract 2
- 108091005575 Bromodomain-containing proteins Proteins 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000003993 interaction Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
Classifications
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- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- 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
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
- A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/16—Masculine contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
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- 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
- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
- A61P39/02—Antidotes
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- 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
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- 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)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Reproductive Health (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Biomedical Technology (AREA)
- Communicable Diseases (AREA)
- Pulmonology (AREA)
- Transplantation (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Physical Education & Sports Medicine (AREA)
- Toxicology (AREA)
- Dermatology (AREA)
- Emergency Medicine (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562259797P | 2015-11-25 | 2015-11-25 | |
| US201562261703P | 2015-12-01 | 2015-12-01 | |
| US201662338968P | 2016-05-19 | 2016-05-19 | |
| PCT/US2016/063502 WO2017091673A2 (en) | 2015-11-25 | 2016-11-23 | Bivalent bromodomain inhibtors and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO2018005370A2 true CO2018005370A2 (es) | 2018-05-31 |
Family
ID=58763670
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CONC2018/0005370A CO2018005370A2 (es) | 2015-11-25 | 2018-05-23 | Inhibidores de bromodominio bivalentes y usos de los mismos |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US10913752B2 (OSRAM) |
| EP (1) | EP3380100A4 (OSRAM) |
| JP (2) | JP7385356B2 (OSRAM) |
| KR (1) | KR20180081809A (OSRAM) |
| CN (2) | CN114957291A (OSRAM) |
| AU (2) | AU2016361478B2 (OSRAM) |
| BR (1) | BR112018009798A8 (OSRAM) |
| CA (1) | CA3003288A1 (OSRAM) |
| CL (1) | CL2018001404A1 (OSRAM) |
| CO (1) | CO2018005370A2 (OSRAM) |
| CR (1) | CR20180336A (OSRAM) |
| IL (1) | IL258970A (OSRAM) |
| MX (1) | MX2018006499A (OSRAM) |
| PE (1) | PE20181298A1 (OSRAM) |
| PH (1) | PH12018550070A1 (OSRAM) |
| RU (1) | RU2742035C2 (OSRAM) |
| SG (2) | SG10201913450PA (OSRAM) |
| WO (1) | WO2017091673A2 (OSRAM) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IN2014DN09346A (OSRAM) | 2012-06-13 | 2015-07-17 | Hoffmann La Roche | |
| MA37940B1 (fr) | 2012-09-25 | 2018-09-28 | Hoffmann La Roche | Derives d'octahydro-cyclopenta(c)pyrrole substitues inhibiteurs de l'autotaxine, utiles pour traiter les affections renales, hepatiques et inflammatoires, les affections du systeme nerveux, les maladies fibreuses. |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| UA118201C2 (uk) | 2013-11-26 | 2018-12-10 | Ф. Хоффманн-Ля Рош Аг | НОВИЙ ОКТАГІДРОЦИКЛОБУТА[1,2-c;3,4-c']ДИПІРОЛ-2-ІЛ |
| RU2016134947A (ru) | 2014-01-31 | 2018-03-01 | Дана-Фарбер Кансер Институт, Инк. | Производные диаминопиримидин бензолсульфона и их применение |
| US10793571B2 (en) | 2014-01-31 | 2020-10-06 | Dana-Farber Cancer Institute, Inc. | Uses of diazepane derivatives |
| EP3590939A1 (en) | 2014-03-26 | 2020-01-08 | F. Hoffmann-La Roche AG | Bicyclic compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors |
| WO2015144609A1 (en) | 2014-03-26 | 2015-10-01 | F. Hoffmann-La Roche Ag | Condensed [1,4]diazepine compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors |
| MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
| PE20180479A1 (es) | 2015-09-04 | 2018-03-07 | Hoffmann La Roche | Nuevos derivados de fenoximetilo |
| BR112018004618A2 (pt) | 2015-09-11 | 2018-09-25 | Dana-Farber Cancer Institute, Inc. | ciano tienotriazoldiazepinas e usos das mesmas |
| CA2996977A1 (en) | 2015-09-11 | 2017-03-16 | Dana-Farber Cancer Institute, Inc. | Acetamide thienotriazolodiazepines and uses thereof |
| MX2018002217A (es) | 2015-09-24 | 2018-03-23 | Hoffmann La Roche | Nuevos compuestos biciclicos como inhibidores de autotaxina (atx). |
| CA2984585A1 (en) | 2015-09-24 | 2017-03-30 | F. Hoffmann-La Roche Ag | New bicyclic compounds as dual atx/ca inhibitors |
| PE20180451A1 (es) | 2015-09-24 | 2018-03-05 | Hoffmann La Roche | Nuevos compuestos biciclicos como inhibidores de atx |
| CR20180057A (es) | 2015-09-24 | 2018-04-02 | Hoffmann La Roche | Nuevos compuestos biciclicos como inhibidores duales de atx/ca. |
| AU2016361428A1 (en) | 2015-11-25 | 2018-05-24 | Gilead Apollo, Llc | Triazole ACC inhibitors and uses thereof |
| US20170166582A1 (en) | 2015-11-25 | 2017-06-15 | Gilead Apollo, Llc | Pyrazole acc inhibitors and uses thereof |
| SI3379933T1 (sl) | 2015-11-25 | 2023-07-31 | Gilead Apollo, Llc | Fungicidni sestavki, ki vsebujejo derivate 2,4-diokso-1,4-dihidrotieno (2,3-d)pirimidina |
| MX2018006288A (es) | 2015-11-25 | 2018-09-07 | Gilead Apollo Llc | Inhibidores de acc tipo ester y usos de los mismos. |
| US10913752B2 (en) | 2015-11-25 | 2021-02-09 | Dana-Farber Cancer Institute, Inc. | Bivalent bromodomain inhibitors and uses thereof |
| RU2019132254A (ru) | 2017-03-16 | 2021-04-16 | Ф. Хоффманн-Ля Рош Аг | Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca |
| EP3596060B1 (en) | 2017-03-16 | 2023-09-20 | F. Hoffmann-La Roche AG | New bicyclic compounds as atx inhibitors |
| FI3778573T3 (fi) * | 2018-03-30 | 2024-06-27 | Kyowa Kirin Co Ltd | Yhdiste, jolla on syöpää ehkäisevä vaikutus |
| US12161648B2 (en) | 2018-10-09 | 2024-12-10 | The Regents Of The University Of California | Covalent targeting of E3 ligases |
| CN110101705B (zh) * | 2019-05-07 | 2022-01-14 | 河南农业大学 | Bet家族蛋白抑制剂的抗病毒用途 |
| JP7642552B2 (ja) * | 2019-09-30 | 2025-03-10 | 協和キリン株式会社 | Ｂｅｔ分解剤 |
| PT116050B (pt) * | 2020-01-09 | 2022-06-15 | Hovione Farm S A | Conjugados fármaco-ligando e inibidores das proteínas da família bromodomínio e domínio extraterminal -(bet) modificados |
| CN113679724B (zh) * | 2020-05-18 | 2023-04-07 | 中国科学院微生物研究所 | 一种流感病毒小分子抑制剂 |
| CN114276333B (zh) * | 2020-09-28 | 2023-05-09 | 中国科学院上海药物研究所 | 二氢喹喔啉类溴结构域二价抑制剂 |
| AU2022246090A1 (en) * | 2021-03-25 | 2023-09-28 | Dana-Farber Cancer Institute, Inc. | Enamine n-oxides: synthesis and application to hypoxia-responsive prodrugs and imaging agents |
| IT202100015467A1 (it) * | 2021-06-14 | 2022-12-14 | Univ Degli Studi Roma Tre | Inibitori delle proteine BET per l’uso nel trattamento della malattia di Niemann–Pick. |
| CN115626949A (zh) * | 2021-07-14 | 2023-01-20 | 南京澳健生物制药有限公司 | 一种bet蛋白靶向降解化合物及其制备方法和用途 |
| CN119318655B (zh) * | 2024-12-02 | 2025-09-23 | 合肥综合性国家科学中心大健康研究院 | Mps1-IN-1在作为铁死亡抑制剂及制备用于防治铁死亡相关疾病药物中的应用 |
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| ATE203026T1 (de) | 1995-01-06 | 2001-07-15 | Hoffmann La Roche | Hydroxymethyl-imidazodiazepine und deren ester |
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| 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 |
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2016
- 2016-11-23 US US15/778,831 patent/US10913752B2/en active Active
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- 2016-11-23 CN CN202210306276.7A patent/CN114957291A/zh active Pending
- 2016-11-23 CA CA3003288A patent/CA3003288A1/en not_active Abandoned
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