BR112018009798A8 - inibidores de bromodomínio bivalentes e usos dos mesmos - Google Patents
inibidores de bromodomínio bivalentes e usos dos mesmosInfo
- Publication number
- BR112018009798A8 BR112018009798A8 BR112018009798A BR112018009798A BR112018009798A8 BR 112018009798 A8 BR112018009798 A8 BR 112018009798A8 BR 112018009798 A BR112018009798 A BR 112018009798A BR 112018009798 A BR112018009798 A BR 112018009798A BR 112018009798 A8 BR112018009798 A8 BR 112018009798A8
- Authority
- BR
- Brazil
- Prior art keywords
- bromodomain
- bivalent
- bromodomains
- brd4
- inhibitors
- Prior art date
Links
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
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- 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
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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
- 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
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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
- A61P15/16—Masculine contraceptives
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- 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
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- 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
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- 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]
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- 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
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- 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
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- 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
Abstract
a presente invenção refere-se a inibidores bivalentes de bromodomínios de bet, tal como os compostos de fórmulas (i), (ii), (iii), (iv), (v) e (vi). algumas proteínas contendo bromodomínio (por exemplo, brd4) têm uma estrutura primária de bromodomínio tandem compreendendo mais do que um sítio de ligação de bromodomínio (por exemplo, brd4 compreende bd1 e bd2). os inibidores bivalentes de bromodomínios de bet fornecidos aqui podem alvejar bromodomínios através de interações multivalentes vantajosas, e podem, portanto, ser usados para tratar doenças ou condições associadas com proteínas contendo bromodomínio. a presente invenção também refere-se a composições farmacêuticas e kits compreendendo os compostos inventivos, bem como métodos de uso dos compostos inventivos.
Applications Claiming Priority (7)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562259797P | 2015-11-25 | 2015-11-25 | |
US62/259,797 | 2015-11-25 | ||
US201562261703P | 2015-12-01 | 2015-12-01 | |
US62/261,703 | 2015-12-01 | ||
US201662338968P | 2016-05-19 | 2016-05-19 | |
US62/338,968 | 2016-05-19 | ||
PCT/US2016/063502 WO2017091673A2 (en) | 2015-11-25 | 2016-11-23 | Bivalent bromodomain inhibtors and uses thereof |
Publications (2)
Publication Number | Publication Date |
---|---|
BR112018009798A2 BR112018009798A2 (pt) | 2018-11-06 |
BR112018009798A8 true BR112018009798A8 (pt) | 2019-02-26 |
Family
ID=58763670
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112018009798A BR112018009798A8 (pt) | 2015-11-25 | 2016-11-23 | inibidores de bromodomínio bivalentes e usos dos mesmos |
Country Status (19)
Country | Link |
---|---|
US (2) | US10913752B2 (pt) |
EP (1) | EP3380100A4 (pt) |
JP (2) | JP7385356B2 (pt) |
KR (1) | KR20180081809A (pt) |
CN (2) | CN108472295B (pt) |
AU (2) | AU2016361478B2 (pt) |
BR (1) | BR112018009798A8 (pt) |
CA (1) | CA3003288A1 (pt) |
CL (1) | CL2018001404A1 (pt) |
CO (1) | CO2018005370A2 (pt) |
CR (1) | CR20180336A (pt) |
HK (1) | HK1256796A1 (pt) |
IL (1) | IL258970A (pt) |
MX (1) | MX2018006499A (pt) |
PE (1) | PE20181298A1 (pt) |
PH (1) | PH12018550070A1 (pt) |
RU (1) | RU2742035C2 (pt) |
SG (2) | SG11201803210YA (pt) |
WO (1) | WO2017091673A2 (pt) |
Families Citing this family (32)
Publication number | Priority date | Publication date | Assignee | Title |
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AU2013276617B9 (en) | 2012-06-13 | 2018-03-29 | F. Hoffmann-La Roche Ag | New diazaspirocycloalkane and azaspirocycloalkane |
LT2900669T (lt) | 2012-09-25 | 2019-11-11 | Hoffmann La Roche | Heksahidropirol[3,4-c]pirolo dariniai ir susiję junginai kaip autotaksino (atx) inhibitoriai ir kaip lizofosfatidinės rūgšties (lpa) gamybos inhibitoriai, skirti gydyti pvz., inkstų ligas |
AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
MX2016005186A (es) | 2013-11-26 | 2016-07-08 | Hoffmann La Roche | Nuevo octahidro-ciclobuta[1,2-c;3,4-c']dipirrol-2-ilo. |
US10793571B2 (en) | 2014-01-31 | 2020-10-06 | Dana-Farber Cancer Institute, Inc. | Uses of diazepane derivatives |
CA2936865A1 (en) | 2014-01-31 | 2015-08-06 | Dana-Farber Cancer Institute, Inc. | Diaminopyrimidine benzenesulfone derivatives and uses thereof |
RS59477B1 (sr) | 2014-03-26 | 2019-12-31 | Hoffmann La Roche | Biciklička jedinjenja kao inhibitori proizvodnje autotaksina (atx) i lizofosfatidne kiseline (lpa) |
EA032357B1 (ru) | 2014-03-26 | 2019-05-31 | Ф. Хоффманн-Ля Рош Аг | Конденсированные [1,4]диазепиновые соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa) |
MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
EP3344619B1 (en) | 2015-09-04 | 2020-10-28 | H. Hoffnabb-La Roche Ag | Phenoxymethyl derivatives |
BR112018004618A2 (pt) | 2015-09-11 | 2018-09-25 | Dana-Farber Cancer Institute, Inc. | ciano tienotriazoldiazepinas e usos das mesmas |
PE20181086A1 (es) | 2015-09-11 | 2018-07-05 | Dana Farber Cancer Inst Inc | Acetamida tienotrizolodiazepinas y usos de las mismas |
JP6846414B2 (ja) | 2015-09-24 | 2021-03-24 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Atx阻害剤としての二環式化合物 |
JP6876685B2 (ja) | 2015-09-24 | 2021-05-26 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Atx阻害剤としての二環式化合物 |
KR20180053408A (ko) | 2015-09-24 | 2018-05-21 | 에프. 호프만-라 로슈 아게 | 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서의 신규한 이환형 화합물 |
CR20180057A (es) | 2015-09-24 | 2018-04-02 | Hoffmann La Roche | Nuevos compuestos biciclicos como inhibidores duales de atx/ca. |
SI3380479T1 (sl) | 2015-11-25 | 2023-04-28 | Gilead Apollo, Llc | Triazolni inhibitorji ACC in uporabe le-teh |
BR112018009798A8 (pt) | 2015-11-25 | 2019-02-26 | Dana Farber Cancer Inst Inc | inibidores de bromodomínio bivalentes e usos dos mesmos |
EA201890913A1 (ru) | 2015-11-25 | 2018-11-30 | Джилид Аполло, Ллс | Пиразоловые соединения в качестве ингибиторов акк и их применение |
EA201890949A1 (ru) | 2015-11-25 | 2018-12-28 | Джилид Аполло, Ллс | СЛОЖНОЭФИРНЫЕ ИНГИБИТОРЫ АЦЕТИЛ-КоА-КАРБОКСИЛАЗЫ И ВАРИАНТЫ 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 |
KR20190129924A (ko) | 2017-03-16 | 2019-11-20 | 에프. 호프만-라 로슈 아게 | 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서 유용한 헤테로환형 화합물 |
EP3596060B1 (en) | 2017-03-16 | 2023-09-20 | F. Hoffmann-La Roche AG | New bicyclic compounds as atx inhibitors |
KR20200138778A (ko) * | 2018-03-30 | 2020-12-10 | 쿄와 기린 가부시키가이샤 | 항암 활성을 갖는 화합물 |
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 |
CN114502534A (zh) * | 2019-09-30 | 2022-05-13 | 协和麒麟株式会社 | Bet降解剂 |
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 |
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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. |
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2016
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- 2016-11-23 AU AU2016361478A patent/AU2016361478B2/en not_active Ceased
- 2016-11-23 CN CN202210306276.7A patent/CN114957291A/zh active Pending
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2018
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2020
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2021
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