SG11201803210YA - Bivalent bromodomain inhibitors and uses thereof - Google Patents

Bivalent bromodomain inhibitors and uses thereof

Info

Publication number
SG11201803210YA
SG11201803210YA SG11201803210YA SG11201803210YA SG11201803210YA SG 11201803210Y A SG11201803210Y A SG 11201803210YA SG 11201803210Y A SG11201803210Y A SG 11201803210YA SG 11201803210Y A SG11201803210Y A SG 11201803210YA SG 11201803210Y A SG11201803210Y A SG 11201803210YA
Authority
SG
Singapore
Prior art keywords
bivalent
bromodomain inhibitors
bromodomain
inhibitors
bivalent bromodomain
Prior art date
Application number
SG11201803210YA
Other languages
English (en)
Inventor
Jun Qi
Minoru Tanaka
Justin Roberts
James E Bradner
Original Assignee
Dana Farber Cancer Inst Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Dana Farber Cancer Inst Inc filed Critical Dana Farber Cancer Inst Inc
Publication of SG11201803210YA publication Critical patent/SG11201803210YA/en

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Classifications

    • 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
    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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
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    • 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
    • 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
    • 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
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Toxicology (AREA)
  • Emergency Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
SG11201803210YA 2015-11-25 2016-11-23 Bivalent bromodomain inhibitors and uses thereof SG11201803210YA (en)

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 (fr) 2015-11-25 2016-11-23 Inhibiteurs de bromodomaines bivalents et leurs utilisations

Publications (1)

Publication Number Publication Date
SG11201803210YA true SG11201803210YA (en) 2018-05-30

Family

ID=58763670

Family Applications (2)

Application Number Title Priority Date Filing Date
SG11201803210YA SG11201803210YA (en) 2015-11-25 2016-11-23 Bivalent bromodomain inhibitors and uses thereof
SG10201913450PA SG10201913450PA (en) 2015-11-25 2016-11-23 Bivalent bromodomain inhibitors and uses thereof

Family Applications After (1)

Application Number Title Priority Date Filing Date
SG10201913450PA SG10201913450PA (en) 2015-11-25 2016-11-23 Bivalent bromodomain inhibitors and uses thereof

Country Status (19)

Country Link
US (2) US10913752B2 (fr)
EP (1) EP3380100A4 (fr)
JP (2) JP7385356B2 (fr)
KR (1) KR20180081809A (fr)
CN (2) CN108472295B (fr)
AU (2) AU2016361478B2 (fr)
BR (1) BR112018009798A8 (fr)
CA (1) CA3003288A1 (fr)
CL (1) CL2018001404A1 (fr)
CO (1) CO2018005370A2 (fr)
CR (1) CR20180336A (fr)
HK (1) HK1256796A1 (fr)
IL (1) IL258970A (fr)
MX (1) MX2018006499A (fr)
PE (1) PE20181298A1 (fr)
PH (1) PH12018550070A1 (fr)
RU (1) RU2742035C2 (fr)
SG (2) SG11201803210YA (fr)
WO (1) WO2017091673A2 (fr)

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BR112018010113B1 (pt) 2015-11-25 2022-06-14 Gilead Apollo, Llc Composto de pirazol útil como inibidor da acetil-coa carboxilase (acc)
KR20180082557A (ko) 2015-11-25 2018-07-18 길리어드 아폴로, 엘엘씨 트리아졸 acc 억제제 및 그의 용도
KR20180086191A (ko) 2015-11-25 2018-07-30 길리어드 아폴로, 엘엘씨 2,4-디옥소-1,4-디히드로티에노[2,3-d]피리미딘 유도체를 함유하는 살진균 조성물
SG11201803210YA (en) 2015-11-25 2018-05-30 Dana Farber Cancer Inst Inc Bivalent bromodomain inhibitors and uses thereof
CA3004798C (fr) 2015-11-25 2023-10-31 Gilead Apollo, Llc Inhibiteurs de l'acc a base d'esters et utilisations associees
JP7090099B2 (ja) 2017-03-16 2022-06-23 エフ．ホフマン－ラ ロシュ アーゲー Ａｔｘインヒビターとしての新規二環式化合物
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BR112020019963A2 (pt) 2018-03-30 2021-01-05 Kyowa Kirin Co., Ltd. Composto com atividade anticâncer
CN113164495A (zh) * 2018-10-09 2021-07-23 加利福尼亚大学董事会 E3连接酶的共价靶向
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
JPWO2021065980A1 (fr) * 2019-09-30 2021-04-08
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
JP2024512568A (ja) * 2021-03-25 2024-03-19 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 エナミンｎ－オキシド：低酸素応答性プロドラッグおよび造影剤の合成およびそれらへの適用
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BR112018009798A8 (pt) 2019-02-26
CN108472295B (zh) 2022-04-15
RU2742035C2 (ru) 2021-02-01
KR20180081809A (ko) 2018-07-17
EP3380100A2 (fr) 2018-10-03
CN108472295A (zh) 2018-08-31
AU2016361478B2 (en) 2020-09-10
IL258970A (en) 2018-06-28
AU2016361478A8 (en) 2019-01-03
CO2018005370A2 (es) 2018-05-31
JP2018538281A (ja) 2018-12-27
PH12018550070A1 (en) 2019-01-21
JP7385356B2 (ja) 2023-11-22
US20180354973A1 (en) 2018-12-13
CR20180336A (es) 2018-08-06
WO2017091673A2 (fr) 2017-06-01
US20220119416A9 (en) 2022-04-21
AU2020286224A1 (en) 2021-01-07
RU2018122641A3 (fr) 2020-03-02
US20210221826A1 (en) 2021-07-22
RU2018122641A (ru) 2019-12-26
WO2017091673A3 (fr) 2017-07-06
AU2016361478A1 (en) 2018-05-17
MX2018006499A (es) 2018-08-01
CA3003288A1 (fr) 2017-06-01
US10913752B2 (en) 2021-02-09
SG10201913450PA (en) 2020-03-30
HK1256796A1 (zh) 2019-10-04
CL2018001404A1 (es) 2018-07-20
PE20181298A1 (es) 2018-08-07
WO2017091673A8 (fr) 2018-05-17
BR112018009798A2 (pt) 2018-11-06
EP3380100A4 (fr) 2019-10-02
CN114957291A (zh) 2022-08-30
JP2022043073A (ja) 2022-03-15
US20200172553A9 (en) 2020-06-04

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