JOP20220069A1 - عوامل محللة لـ brd9 ثنائية الوظيفة وطرق لاستخدامها - Google Patents

عوامل محللة لـ brd9 ثنائية الوظيفة وطرق لاستخدامها

Info

Publication number
JOP20220069A1
JOP20220069A1 JOP/2022/0069A JOP20220069A JOP20220069A1 JO P20220069 A1 JOP20220069 A1 JO P20220069A1 JO P20220069 A JOP20220069 A JO P20220069A JO P20220069 A1 JOP20220069 A1 JO P20220069A1
Authority
JO
Jordan
Prior art keywords
brd9
methods
bifunctional
containing protein
degraders
Prior art date
Application number
JOP/2022/0069A
Other languages
English (en)
Inventor
Marie-Line Goude
Thomas Zoller
Martin Sendzik
Xin Chen
Anna Vulpetti
Julien Lorber
Edmund Martin Harrington
Gregory John Hollingworth
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of JOP20220069A1 publication Critical patent/JOP20220069A1/ar

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K47/54—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 compound
    • A61K47/55—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 compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

يتعلق الاختراع الحايل بمركبات BRD9 ثنائية الوظيفة بالصيغة (A)، (BF-I)، (BF-II)، (BF-III)، (BF-IIIa)، (BF-IIIb)، (BF-IV)، (BF-IVa)، (BF-IVb)، (BF-I’)، (BF-II’)، (BF-III’)، (BF-IV’)، أو (BF-V’)، أو ملح مقبول صيدلانياً، هيدرات، ذوابة، عقار أولي، أيزومر فراغي، أو مركب صنوي منها، بتحضيرها، بتركيبات صيدلانية تشتمل عليها، وباستخدامها في معالجة أمراض واضطرابات ناتجة عن بروتين يحتوي على نطاق برومو، مثل بروتين يحتوي على نطاق برومو 9 (BRD9).
JOP/2022/0069A 2019-09-16 2020-09-14 عوامل محللة لـ brd9 ثنائية الوظيفة وطرق لاستخدامها JOP20220069A1 (ar)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201962900865P 2019-09-16 2019-09-16
US201962900863P 2019-09-16 2019-09-16
US201962900869P 2019-09-16 2019-09-16
US201962900860P 2019-09-16 2019-09-16
PCT/US2020/050768 WO2021055295A1 (en) 2019-09-16 2020-09-14 Brd9 bifunctional degraders and their methods of use

Publications (1)

Publication Number Publication Date
JOP20220069A1 true JOP20220069A1 (ar) 2023-01-30

Family

ID=72915891

Family Applications (1)

Application Number Title Priority Date Filing Date
JOP/2022/0069A JOP20220069A1 (ar) 2019-09-16 2020-09-14 عوامل محللة لـ brd9 ثنائية الوظيفة وطرق لاستخدامها

Country Status (19)

Country Link
US (1) US20220315578A1 (ar)
EP (1) EP4041724A1 (ar)
JP (1) JP2022547952A (ar)
KR (1) KR20220063192A (ar)
CN (1) CN114641473A (ar)
AU (1) AU2020349451B2 (ar)
BR (1) BR112022003514A2 (ar)
CA (1) CA3153529A1 (ar)
CO (1) CO2022002842A2 (ar)
CR (1) CR20220105A (ar)
DO (1) DOP2022000053A (ar)
EC (1) ECSP22018571A (ar)
IL (1) IL290677A (ar)
JO (1) JOP20220069A1 (ar)
MX (1) MX2022003102A (ar)
PE (1) PE20221417A1 (ar)
TW (1) TW202123942A (ar)
UY (1) UY38880A (ar)
WO (1) WO2021055295A1 (ar)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019152440A1 (en) 2018-01-30 2019-08-08 Foghorn Therapeutics Inc. Methods and compounds for treating disorders
US20230066136A1 (en) 2019-01-29 2023-03-02 Foghorn Therapeutics Inc. Compounds and uses thereof
AU2021214767A1 (en) 2020-01-29 2022-07-28 Foghorn Therapeutics Inc. Compounds and uses thereof
CA3165309A1 (en) 2020-03-05 2021-09-10 Christopher G. Nasveschuk Compounds for targeted degradation of brd9
US11787800B2 (en) 2020-07-29 2023-10-17 Foghorn Therapeutics Inc. BRD9 degraders and uses thereof
WO2023283263A1 (en) 2021-07-06 2023-01-12 Foghorn Therapeutics Inc. Citrate salt, pharmaceutical compositions, and methods of making and using the same
WO2023039208A1 (en) * 2021-09-09 2023-03-16 C4 Therapeutics, Inc. Selected compounds for targeted degradation of brd9
WO2023109892A1 (zh) * 2021-12-15 2023-06-22 海思科医药集团股份有限公司 一种抑制或降解brd9的化合物及其组合物和药学上的应用
WO2023200800A1 (en) * 2022-04-11 2023-10-19 Foghorn Therapeutics Inc. Methods of treating androgen receptor-independent prostate cancer
CN117229202B (zh) * 2023-11-15 2024-01-26 苏州美诺医药科技有限公司 一种brd9靶向降解化合物的中间体的制备方法

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9227969B2 (en) 2013-08-14 2016-01-05 Novartis Ag Compounds and compositions as inhibitors of MEK
US9694084B2 (en) * 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
CA3025806C (en) * 2016-06-23 2023-04-04 Dana-Farber Cancer Institute, Inc. Degradation of bromodomain-containing protein 9 (brd9) by conjugation of brd9 inhibitors with e3 ligase ligand and methods of use
WO2018064589A1 (en) * 2016-09-29 2018-04-05 Dana-Farber Cancer Institute, Inc. Targeted protein degradation using a mutant e3 ubiquitin ligase
BR112019015484A2 (pt) * 2017-01-31 2020-04-28 Arvinas Operations Inc ligantes de cereblon e compostos bifuncionais compreendendo os mesmos
CN117186108A (zh) * 2018-03-26 2023-12-08 诺华股份有限公司 布鲁顿酪氨酸激酶降解剂
US11613543B2 (en) * 2018-03-26 2023-03-28 Novartis Ag Substituted pyrrolo[2,3-d]pyrimidines as Bruton's Tyrosine Kinase inhibitors
EP3846800A4 (en) * 2018-09-04 2022-08-24 C4 Therapeutics, Inc. COMPOUNDS FOR THE DEGRADATION OF BRD9 OR MTH1
EP3917517A4 (en) * 2019-01-29 2023-01-25 Foghorn Therapeutics Inc. CONNECTIONS AND USES THEREOF

Also Published As

Publication number Publication date
CN114641473A (zh) 2022-06-17
AU2020349451A1 (en) 2022-04-21
TW202123942A (zh) 2021-07-01
DOP2022000053A (es) 2023-01-31
PE20221417A1 (es) 2022-09-20
CA3153529A1 (en) 2021-03-25
WO2021055295A1 (en) 2021-03-25
ECSP22018571A (es) 2022-04-29
KR20220063192A (ko) 2022-05-17
EP4041724A1 (en) 2022-08-17
CO2022002842A2 (es) 2022-04-19
UY38880A (es) 2021-04-30
CR20220105A (es) 2022-06-13
IL290677A (en) 2022-04-01
AU2020349451B2 (en) 2024-02-01
BR112022003514A2 (pt) 2022-05-17
JP2022547952A (ja) 2022-11-16
US20220315578A1 (en) 2022-10-06
MX2022003102A (es) 2022-04-06

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