MX2021003460A - Fabricacion de compuestos y composiciones para inhibir la actividad de shp2. - Google Patents

Fabricacion de compuestos y composiciones para inhibir la actividad de shp2.

Info

Publication number
MX2021003460A
MX2021003460A MX2021003460A MX2021003460A MX2021003460A MX 2021003460 A MX2021003460 A MX 2021003460A MX 2021003460 A MX2021003460 A MX 2021003460A MX 2021003460 A MX2021003460 A MX 2021003460A MX 2021003460 A MX2021003460 A MX 2021003460A
Authority
MX
Mexico
Prior art keywords
manufacture
shp2
inhibiting
compositions
activity
Prior art date
Application number
MX2021003460A
Other languages
English (en)
Inventor
Wei Li
Hui Wang
Jianhua Wang
Hao Zhang
Zhongcheng Min
Zhongbo Fei
Huanqing Jia
Xiaohui Lin
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 MX2021003460A publication Critical patent/MX2021003460A/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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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 invención se refiere a un método para la fabricación de un compuesto de Fórmula I o una sal, co-cristal ácido, hidrato u otro solvato del mismo farmacéuticamente aceptable, comprendiendo dicho método hacer reaccionar un compuesto de la fórmula II con un compuesto de la fórmula III de acuerdo con el siguiente esquema de reacción: (ver Fórmulas) en donde LG, A, n, m y p son como se definen en la Breve Descripción de la Invención.
MX2021003460A 2018-09-29 2019-09-18 Fabricacion de compuestos y composiciones para inhibir la actividad de shp2. MX2021003460A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2018108738 2018-09-29
PCT/IB2019/057863 WO2020065452A1 (en) 2018-09-29 2019-09-18 Manufacture of compounds and compositions for inhibiting the activity of shp2

Publications (1)

Publication Number Publication Date
MX2021003460A true MX2021003460A (es) 2021-06-18

Family

ID=68051872

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2021003460A MX2021003460A (es) 2018-09-29 2019-09-18 Fabricacion 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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WO2018057884A1 (en) 2016-09-22 2018-03-29 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
CN111902415A (zh) 2018-03-02 2020-11-06 大冢制药株式会社 药学化合物
TW202003471A (zh) 2018-03-21 2020-01-16 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其使用方法
AU2019344897B2 (en) 2018-09-18 2024-01-18 Nikang Therapeutics, Inc. Tri-substituted heteroaryl derivatives AS SRC homology-2 phosphatase inhibitors
AU2019346118B2 (en) 2018-09-29 2024-05-16 Novartis Ag Manufacture of compounds and compositions for inhibiting the activity of SHP2
US20210346375A1 (en) * 2018-09-29 2021-11-11 Novartis Ag Process of manufacture of a compound for inhibiting the activity of shp2, as well as products resulting from acid addition
EP3860717A1 (en) 2018-10-03 2021-08-11 Gilead Sciences, Inc. Imidozopyrimidine derivatives
TW202126660A (zh) 2019-09-24 2021-07-16 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其製備與使用方法
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
EP4178962A1 (en) * 2020-07-08 2023-05-17 Novartis AG Manufacture of compounds and compositions for inhibiting the activity of shp2
IL301062A (en) 2020-09-03 2023-05-01 Revolution Medicines Inc Use of SOS1 inhibitors to treat malignancies with SHP2 mutations
EP4214209A1 (en) 2020-09-15 2023-07-26 Revolution Medicines, Inc. Indole derivatives as ras inhibitors in the treatment of cancer
CR20230558A (es) 2021-05-05 2024-01-24 Revolution Medicines Inc Inhibidores de ras para el tratamiento del cáncer
WO2022235866A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
BR112023022819A2 (pt) 2021-05-05 2024-01-16 Revolution Medicines Inc Compostos, composição farmacêutica, conjugados e métodos para tratar câncer em um sujeito, para tratar um distúrbio e para inibir uma proteína ras em uma célula
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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CN105899493B (zh) * 2014-01-17 2019-03-29 诺华股份有限公司 用于抑制shp2活性的1-(三嗪-3-基/哒嗪-3-基)-哌(-嗪)啶衍生物及其组合物
JP6523303B2 (ja) 2014-01-17 2019-05-29 ノバルティス アーゲー Shp2の活性を阻害するための1−ピリダジン/トリアジン−3−イル−ピペラジン/ピペリジン/ピロリジン誘導体およびその組成物
JO3517B1 (ar) * 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
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US20210346375A1 (en) 2018-09-29 2021-11-11 Novartis Ag Process of manufacture of a compound for inhibiting the activity of shp2, as well as products resulting from acid addition
AU2019346118B2 (en) 2018-09-29 2024-05-16 Novartis Ag Manufacture of compounds and compositions for inhibiting the activity of SHP2
MX2021009563A (es) 2019-02-12 2021-09-08 Novartis Ag Combinacion farmaceutica que comprende tno155 y ribociclib.
WO2020165733A1 (en) 2019-02-12 2020-08-20 Novartis Ag Pharmaceutical combination comprising tno155 and a pd-1 inhibitor
US20220152026A1 (en) 2019-02-12 2022-05-19 Novartis Ag Pharmaceutical combination comprising tno155 and a krasg12c inhibitor
CN111647000B (zh) 2019-03-04 2021-10-12 勤浩医药(苏州)有限公司 吡嗪类衍生物及其在抑制shp2中的应用
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
KR20220148847A (ko) 2020-02-28 2022-11-07 노파르티스 아게 다브라페닙, erk 억제제, 및 shp2 억제제를 포함하는 삼중 약학적 조합물
US20230172928A1 (en) 2020-05-08 2023-06-08 Novartis Ag Pharmaceutical combination comprising tno155 and nazartinib
EP4178962A1 (en) 2020-07-08 2023-05-17 Novartis AG Manufacture of compounds and compositions for inhibiting the activity of shp2

Also Published As

Publication number Publication date
CN112867718A (zh) 2021-05-28
JP7386855B2 (ja) 2023-11-27
KR20210068472A (ko) 2021-06-09
US20210355134A1 (en) 2021-11-18
AU2019346118B2 (en) 2024-05-16
AR116522A1 (es) 2021-05-19
AU2019346118A1 (en) 2021-04-01
IL281726A (en) 2021-05-31
TWI829771B (zh) 2024-01-21
WO2020065452A1 (en) 2020-04-02
IL304526A (en) 2023-09-01
TW202035417A (zh) 2020-10-01
IL281726B2 (en) 2024-03-01
BR112021005593A2 (pt) 2021-06-29
CL2021000737A1 (es) 2021-10-22
JP2022502388A (ja) 2022-01-11
JP2024009810A (ja) 2024-01-23
AU2024202897A1 (en) 2024-05-23
IL281726B1 (en) 2023-11-01
EP3856744A1 (en) 2021-08-04
US11873307B2 (en) 2024-01-16
CA3112322A1 (en) 2020-04-02

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