AR116522A1 - Elaboración de compuestos y composiciones para inhibir la actividad de shp2 - Google Patents

Elaboración de compuestos y composiciones para inhibir la actividad de shp2

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Publication number
AR116522A1
AR116522A1 ARP190102733A ARP190102733A AR116522A1 AR 116522 A1 AR116522 A1 AR 116522A1 AR P190102733 A ARP190102733 A AR P190102733A AR P190102733 A ARP190102733 A AR P190102733A AR 116522 A1 AR116522 A1 AR 116522A1
Authority
AR
Argentina
Prior art keywords
formula
compound
shp2
elaboration
inhibit
Prior art date
Application number
ARP190102733A
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English (en)
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.)
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Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR116522A1 publication Critical patent/AR116522A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/22Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente se relaciona con un método para la elaboración de un compuesto de la fórmula (1) o una sal, cocristal ácido, hidrato farmacéuticamente aceptable u otro solvato del mismo, que comprende: la reacción de un compuesto de la formula (2) con un compuesto de la fórmula (3) de acuerdo con el esquema de reacción [1], donde LG es un grupo saliente, A es el anión de un ácido prótico, y n, m y p son números enteros, por lo que la sal de la fórmula (2) es eléctricamente neutra, y diversos pasos adicionales, individuales o continuos, como así también intermediarios del proceso.
ARP190102733A 2018-09-29 2019-09-26 Elaboración de compuestos y composiciones para inhibir la actividad de shp2 AR116522A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2018108738 2018-09-29

Publications (1)

Publication Number Publication Date
AR116522A1 true AR116522A1 (es) 2021-05-19

Family

ID=68051872

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP190102733A AR116522A1 (es) 2018-09-29 2019-09-26 Elaboración de compuestos y composiciones para inhibir la actividad de shp2

Country Status (14)

Country Link
US (1) US11873307B2 (es)
EP (1) EP3856744A1 (es)
JP (2) JP7386855B2 (es)
KR (1) KR20210068472A (es)
CN (1) CN112867718A (es)
AR (1) AR116522A1 (es)
AU (2) AU2019346118B2 (es)
BR (1) BR112021005593A2 (es)
CA (1) CA3112322A1 (es)
CL (1) CL2021000737A1 (es)
IL (2) IL281726B2 (es)
MX (1) MX2021003460A (es)
TW (1) TWI829771B (es)
WO (1) WO2020065452A1 (es)

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US11529347B2 (en) 2016-09-22 2022-12-20 Relay Therapeutics, Inc. SHP2 phosphatase inhibitors and methods of use thereof
TW201819386A (zh) 2016-10-24 2018-06-01 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其使用方法
US11591336B2 (en) 2017-05-26 2023-02-28 D. E. Shaw Research, Llc Substituted pyrazolo[3,4-b]pyrazines as SHP2 phosphatase inhibitors
EP3687997A1 (en) 2017-09-29 2020-08-05 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
NZ766835A (en) 2018-03-02 2023-09-29 Otsuka Pharma Co Ltd Pharmaceutical compounds
CN112166110B (zh) 2018-03-21 2023-08-11 传达治疗有限公司 Shp2磷酸酶抑制剂及其使用方法
CA3113233A1 (en) 2018-09-18 2020-03-26 Nikang Therapeutics, Inc. Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors
CA3112322A1 (en) 2018-09-29 2020-04-02 Novartis Ag Manufacture of compounds and compositions for inhibiting the activity of shp2
EP3856345A1 (en) * 2018-09-29 2021-08-04 Novartis AG Process of manufacture of a compound for inhibiting the activity of shp2
WO2020072656A1 (en) 2018-10-03 2020-04-09 Gilead Sciences, Inc. Imidozopyrimidine derivatives
AU2020354475A1 (en) 2019-09-24 2022-05-05 Relay Therapeutics, Inc. SHP2 phosphatase inhibitors and methods of making and using the same
IL299131A (en) 2020-06-18 2023-02-01 Revolution Medicines Inc Methods for delaying, preventing and treating acquired resistance to RAS inhibitors
WO2022006780A1 (en) * 2020-07-08 2022-01-13 Novartis Ag Manufacture of compounds and compositions for inhibiting activity of shp2
CA3183946A1 (en) 2020-07-08 2022-01-13 Novartis Ag Manufacture of compounds and compositions for inhibiting the activity of shp2
WO2022060583A1 (en) 2020-09-03 2022-03-24 Revolution Medicines, Inc. Use of sos1 inhibitors to treat malignancies with shp2 mutations
US11690915B2 (en) 2020-09-15 2023-07-04 Revolution Medicines, Inc. Ras inhibitors
JP2024516450A (ja) 2021-05-05 2024-04-15 レボリューション メディシンズ インコーポレイテッド 共有結合性ras阻害剤及びその使用
AR125782A1 (es) 2021-05-05 2023-08-16 Revolution Medicines Inc Inhibidores de ras
WO2022235870A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
TW202342040A (zh) 2022-02-21 2023-11-01 瑞士商諾華公司 藥物配製物
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
CN115490697B (zh) * 2022-11-07 2023-09-29 西华大学 一种手性氮杂螺[4,5]-癸胺的不对称合成方法

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EP3094629B1 (en) 2014-01-17 2018-08-22 Novartis AG 1-(triazin-3-yl/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions thereof for inhibiting the activity of shp2
CN105899491B (zh) 2014-01-17 2019-04-02 诺华股份有限公司 用于抑制shp2活性的1-哒嗪-/三嗪-3-基-哌(-嗪)/啶/吡咯烷衍生物及其组合物
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
JP6878316B2 (ja) 2015-06-19 2021-05-26 ノバルティス アーゲー Shp2の活性を阻害するための化合物および組成物
US10287266B2 (en) 2015-06-19 2019-05-14 Novartis Ag Compounds and compositions for inhibiting the activity of SHP2
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EP3856345A1 (en) 2018-09-29 2021-08-04 Novartis AG Process of manufacture of a compound for inhibiting the activity of shp2
CA3112322A1 (en) 2018-09-29 2020-04-02 Novartis Ag Manufacture of compounds and compositions for inhibiting the activity of shp2
CN113382774A (zh) 2019-02-12 2021-09-10 诺华股份有限公司 包含tno155和krasg12c抑制剂的药物组合
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KR20210126653A (ko) 2019-02-12 2021-10-20 노파르티스 아게 Tno155 및 리보시클립을 포함하는 약제학적 조합물
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CN110713447B (zh) 2019-11-15 2021-07-23 山东国邦药业有限公司 一种对甲硫基苯甲醛的制备方法
CN115297862A (zh) 2020-02-28 2022-11-04 诺华股份有限公司 包含达拉菲尼、erk抑制剂和shp2抑制剂的三重药物组合
WO2021224867A1 (en) 2020-05-08 2021-11-11 Novartis Ag Pharmaceutical combination comprising tno155 and nazartinib
CA3183946A1 (en) 2020-07-08 2022-01-13 Novartis Ag Manufacture of compounds and compositions for inhibiting the activity of shp2

Also Published As

Publication number Publication date
JP7386855B2 (ja) 2023-11-27
IL304526A (en) 2023-09-01
AU2019346118B2 (en) 2024-05-16
CN112867718A (zh) 2021-05-28
JP2024009810A (ja) 2024-01-23
CL2021000737A1 (es) 2021-10-22
BR112021005593A2 (pt) 2021-06-29
IL281726B1 (en) 2023-11-01
IL281726B2 (en) 2024-03-01
TWI829771B (zh) 2024-01-21
TW202035417A (zh) 2020-10-01
AU2019346118A1 (en) 2021-04-01
AU2024202897A1 (en) 2024-05-23
EP3856744A1 (en) 2021-08-04
IL281726A (en) 2021-05-31
MX2021003460A (es) 2021-06-18
US11873307B2 (en) 2024-01-16
KR20210068472A (ko) 2021-06-09
US20210355134A1 (en) 2021-11-18
CA3112322A1 (en) 2020-04-02
WO2020065452A1 (en) 2020-04-02
JP2022502388A (ja) 2022-01-11

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