CA3220099A1 - (r)-n-ethyl-5-fluoro-n-isopropyl-2-((5-(2-(6-((2-methoxyethyl)(methyl)amino)-2-methylhexan-3-yl)-2,6-diazaspiro[3.4]octan-6-yl)-1,2,4-triazin-6-yl)oxy)benzamide besylate salt for the treatment of diseases such as cance - Google Patents

(r)-n-ethyl-5-fluoro-n-isopropyl-2-((5-(2-(6-((2-methoxyethyl)(methyl)amino)-2-methylhexan-3-yl)-2,6-diazaspiro[3.4]octan-6-yl)-1,2,4-triazin-6-yl)oxy)benzamide besylate salt for the treatment of diseases such as cance Download PDF

Info

Publication number
CA3220099A1
CA3220099A1 CA3220099A CA3220099A CA3220099A1 CA 3220099 A1 CA3220099 A1 CA 3220099A1 CA 3220099 A CA3220099 A CA 3220099A CA 3220099 A CA3220099 A CA 3220099A CA 3220099 A1 CA3220099 A1 CA 3220099A1
Authority
CA
Canada
Prior art keywords
compound
leukemias
mixture
triazin
fluoro
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.)
Pending
Application number
CA3220099A
Other languages
English (en)
French (fr)
Inventor
Wei Cai
Xuedong Dai
Olivier Alexis Georges Querolle
Johannes Wilhelmus J. Thuring
Alicia Tee Fuay Ng
Nicolas Freddy Jacques Bruno DARVILLE
Robert Michael Geertman
Dipali AHUJA
Yingtao LIU
Vineet PANDE
Cyril BEN HAIM
Simon Jan C SMOLDERS
Edward Cleator
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Janssen Pharmaceutica NV
Original Assignee
Janssen Pharmaceutica NV
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 Janssen Pharmaceutica NV filed Critical Janssen Pharmaceutica NV
Publication of CA3220099A1 publication Critical patent/CA3220099A1/en
Pending legal-status Critical Current

Links

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
    • C07D487/10—Spiro-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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/02—Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/46—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/58—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/60—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CA3220099A 2021-06-17 2022-06-16 (r)-n-ethyl-5-fluoro-n-isopropyl-2-((5-(2-(6-((2-methoxyethyl)(methyl)amino)-2-methylhexan-3-yl)-2,6-diazaspiro[3.4]octan-6-yl)-1,2,4-triazin-6-yl)oxy)benzamide besylate salt for the treatment of diseases such as cance Pending CA3220099A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CNPCT/CN2021/100466 2021-06-17
CN2021100466 2021-06-17
CNPCT/CN2022/091677 2022-05-09
CN2022091677 2022-05-09
PCT/CN2022/099089 WO2022262796A1 (en) 2021-06-17 2022-06-16 (r)-n-ethyl-5-fluoro-n-isopropyl-2-((5-(2-(6-((2-methoxyethyl)(methyl)amino)-2-m ethylhexan-3-yl)-2,6-diazaspiro[3.4]octan-6-yl)-1,2,4-triazin-6-yl)oxy)benzamide besylate salt for the treatment of diseases such as cancer

Publications (1)

Publication Number Publication Date
CA3220099A1 true CA3220099A1 (en) 2022-12-22

Family

ID=82196389

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3220099A Pending CA3220099A1 (en) 2021-06-17 2022-06-16 (r)-n-ethyl-5-fluoro-n-isopropyl-2-((5-(2-(6-((2-methoxyethyl)(methyl)amino)-2-methylhexan-3-yl)-2,6-diazaspiro[3.4]octan-6-yl)-1,2,4-triazin-6-yl)oxy)benzamide besylate salt for the treatment of diseases such as cance

Country Status (16)

Country Link
EP (1) EP4355747A1 (https=)
JP (1) JP2024525145A (https=)
KR (1) KR20240021808A (https=)
CN (2) CN117597348A (https=)
AU (1) AU2022292697A1 (https=)
CA (1) CA3220099A1 (https=)
CL (1) CL2023003731A1 (https=)
CO (1) CO2023018577A2 (https=)
DO (1) DOP2023000260A (https=)
IL (1) IL309359A (https=)
MX (1) MX2023014890A (https=)
PE (1) PE20240923A1 (https=)
PH (1) PH12023553300A1 (https=)
TW (1) TW202315636A (https=)
UY (1) UY39823A (https=)
WO (1) WO2022262796A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202525813A (zh) 2019-12-19 2025-07-01 比利時商健生藥品公司 經取代之直鏈螺環接衍生物
EP4698182A1 (en) 2023-04-17 2026-02-25 Janssen Pharmaceutica NV Combination of a menin-ll1 inhibitor, a dna intercalating agent and a pyrimidine analogue to treat a hematopoietic disorder
WO2025082444A2 (en) 2023-10-20 2025-04-24 Janssen Pharmaceutica Nv (r) -n-ethyl-5-fluoro-n-isopropyl-2- ( (5- (2- (6- ( (2-methoxyethyl) (methyl) amino) -2-methylhexan-3-yl) -2, 6-diazaspiro [3.4] octan-6-yl) -1, 2, 4-triazin-6-yl) oxy) benzamide, formulations and dosage regimens thereof, for use in treating cancer

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102984941B (zh) 2009-09-04 2016-08-17 密执安大学评议会 用于治疗白血病的组合物和方法
WO2014164543A1 (en) 2013-03-13 2014-10-09 The Regents Of The University Of Michigan Compositions comprising thienopyrimidine and thienopyridine compounds and methods of use thereof
USRE49687E1 (en) 2014-09-09 2023-10-10 The Regents Of The University Of Michigan Thienopyrimidine and thienopyridine compounds and methods of use thereof
TWI703150B (zh) 2015-06-04 2020-09-01 美商庫拉腫瘤技術股份有限公司 用於抑制ｍｅｎｉｎ及ｍｌｌ蛋白之交互作用的方法及組合物
HK1246593A1 (zh) 2015-06-04 2018-09-14 Kura Oncology, Inc. 用於抑制menin蛋白与mll蛋白的相互作用的方法及组合物
AU2016378579A1 (en) 2015-12-22 2018-06-14 Vitae Pharmaceuticals, Inc. Inhibitors of the menin-MLL interaction
US10869868B2 (en) 2016-01-26 2020-12-22 Memorial Sloan Kettering Cancer Center Targeting chromatin regulators inhibits leukemogenic gene expression in NPM1 mutant leukemia
PH12018501955B1 (en) 2016-03-16 2024-01-24 Kura Oncology Inc Bridged bicyclic inhibitors of menin-mll and methods of use
PL3429591T3 (pl) 2016-03-16 2023-07-17 Kura Oncology, Inc. Podstawione pochodne tieno[2,3-d]pirymidyny jako inhibitory meniny-mll i metody ich zastosowania
JP6991585B2 (ja) 2016-05-02 2022-01-12 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン メニン阻害剤としてのピペリジン
WO2017207387A1 (en) 2016-05-31 2017-12-07 Bayer Pharma Aktiengesellschaft Spiro condensed azetidine derivatives as inhibitors of the menin-mml1 interaction
WO2017214367A1 (en) * 2016-06-10 2017-12-14 Vitae Pharmaceuticals, Inc. Inhibitors of the menin-mll interaction
WO2018024602A1 (en) 2016-08-04 2018-02-08 Bayer Aktiengesellschaft 2,7-diazaspiro[4.4]nonanes
CA3033239A1 (en) 2016-09-14 2018-03-22 Janssen Pharmaceutica Nv Spiro bicyclic inhibitors of menin-mll interaction
CA3033020A1 (en) 2016-09-14 2018-03-22 Janssen Pharmaceutica Nv Fused bicyclic inhibitors of menin-mll interaction
AU2017326006B2 (en) 2016-09-16 2021-10-28 Vitae Pharmaceuticals, LLC. Inhibitors of the menin-MLL interaction
WO2018106818A1 (en) 2016-12-07 2018-06-14 Kura Oncology, Inc. Methods of promoting beta cell proliferation
WO2018106820A1 (en) 2016-12-07 2018-06-14 Kura Oncology, Inc. Methods of promoting beta cell proliferation
WO2018109088A1 (en) 2016-12-15 2018-06-21 Janssen Pharmaceutica Nv Azepane inhibitors of menin-mll interaction
CN108456208B (zh) 2017-02-22 2021-04-16 广州市恒诺康医药科技有限公司 氮杂螺环类化合物及其制备方法和应用
WO2018175746A1 (en) 2017-03-24 2018-09-27 Kura Oncology, Inc. Methods for treating hematological malignancies and ewing's sarcoma
WO2018226976A1 (en) 2017-06-08 2018-12-13 Kura Oncology, Inc. Methods and compositions for inhibiting the interaction of menin with mll proteins
EP3684361A4 (en) 2017-09-20 2021-09-08 Kura Oncology, Inc. SUBSTITUTED INHIBITORS OF MENIN-MLL AND METHOD OF USING
JP2022503792A (ja) 2018-09-26 2022-01-12 クラ オンコロジー，インク． メニン阻害剤を用いた血液悪性腫瘍の処置
TW202525813A (zh) * 2019-12-19 2025-07-01 比利時商健生藥品公司 經取代之直鏈螺環接衍生物

Also Published As

Publication number Publication date
TW202315636A (zh) 2023-04-16
DOP2023000260A (es) 2024-05-15
WO2022262796A1 (en) 2022-12-22
CN118852178A (zh) 2024-10-29
AU2022292697A1 (en) 2024-02-01
PH12023553300A1 (en) 2024-04-08
WO2022262796A8 (en) 2023-03-23
IL309359A (en) 2024-02-01
EP4355747A1 (en) 2024-04-24
CN117597348A (zh) 2024-02-23
PE20240923A1 (es) 2024-04-30
CL2023003731A1 (es) 2024-07-05
UY39823A (es) 2023-01-31
MX2023014890A (es) 2024-04-29
KR20240021808A (ko) 2024-02-19
JP2024525145A (ja) 2024-07-10
CO2023018577A2 (es) 2024-01-15

Similar Documents

Publication Publication Date Title
JP7781961B2 (ja) 置換直鎖スピロ誘導体
AU2023264608A1 (en) Heterocyclic compounds and uses thereof
TWI393566B (zh) 作為週期素依賴性激酶之新穎吡唑并嘧啶
WO2023215802A1 (en) Heterocyclic compounds and uses thereof
EP2170827B1 (en) Indolin-2-ones and aza-indolin-2-ones
CA3220099A1 (en) (r)-n-ethyl-5-fluoro-n-isopropyl-2-((5-(2-(6-((2-methoxyethyl)(methyl)amino)-2-methylhexan-3-yl)-2,6-diazaspiro[3.4]octan-6-yl)-1,2,4-triazin-6-yl)oxy)benzamide besylate salt for the treatment of diseases such as cance
US11192890B2 (en) FGFR kinase inhibitors and pharmaceutical uses
EP4076664B1 (en) Egfr inhibitors
WO2022237720A1 (en) Combination therapies
CA3214861A1 (en) Combination therapies
TW202448429A (zh) 組合治療
US20260125387A1 (en) (r)-n-ethyl-5-fluoro-n-isopropyl-2-((5-(2-(6-((2-methoxyethyl)(methyl)amino)-2-methylhexan-3-yl)-2,6-diazaspiro[3.4]octan-6-yl)-1,2,4-triazin-6-yl)oxy)benzamide besylate salt
IL322876A (en) A disintegrant containing an aryl substituent for CDK12/13, a method for its preparation, as well as a pharmaceutical composition and medical use thereof
CN117425659A (zh) 哒嗪或被螺环胺取代的1,2,4-三嗪
EA050953B1 (ru) Безилатная соль (r)-n-этил-5-фтор-n-изопропил-2-((5-(2-(6-((2-метоксиэтил)(метил)амино)-2-метилгексан-3-ил)-2,6-диазаспиро[3,4]октан-6-ил)-1,2,4-триазин-6-ил)окси)бензамида для лечения заболеваний, таких как рак
HK40117713A (zh) 用於治疗诸如癌症的疾病的化合物
HK40101887A (zh) 用於治疗诸如癌症的疾病的(r)-n-乙基-5-氟-n-异丙基-2-((5-(2-(6-((2-甲氧基乙基)(甲基)氨基)-2-甲基己-3-基)-2，6-二氮杂螺[3.4]辛-6-基)-1，2，4-三嗪-6-基)氧基)苯甲酰胺苯磺酸盐
HK40113255A (zh) 取代的直链螺环衍生物
HK40071760A (en) Substituted straight chain spiro derivatives
HK40113268A (zh) Kif18a抑制剂及其用途

Legal Events

Date Code Title Description
D00 Search and/or examination requested or commenced

Free format text: ST27 STATUS EVENT CODE: A-1-1-D10-D00-D120 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: VOLUNTARY SUBMISSION OF PRIOR ART RECEIVED

Effective date: 20240717

D00 Search and/or examination requested or commenced

Free format text: ST27 STATUS EVENT CODE: A-1-1-D10-D00-D120 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: VOLUNTARY SUBMISSION OF PRIOR ART RECEIVED

Effective date: 20240924

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-1-1-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT

Effective date: 20241003

MFA Maintenance fee for application paid

Free format text: FEE DESCRIPTION TEXT: MF (APPLICATION, 2ND ANNIV.) - STANDARD

Year of fee payment: 2

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-1-1-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20241022

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-1-1-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT DETERMINED COMPLIANT

Effective date: 20241022

MFA Maintenance fee for application paid

Free format text: FEE DESCRIPTION TEXT: MF (APPLICATION, 3RD ANNIV.) - STANDARD

Year of fee payment: 3

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-1-1-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20241227

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-1-1-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT DETERMINED COMPLIANT

Effective date: 20241227

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-1-1-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT

Effective date: 20250129

D00 Search and/or examination requested or commenced

Free format text: ST27 STATUS EVENT CODE: A-1-1-D10-D00-D123 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: PRIOR ART DISCLOSURE DETERMINED COMPLIANT

Effective date: 20250211

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-1-1-W10-W00-W100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: LETTER SENT

Effective date: 20250211