MA45660A - 3-méthylpyrazines 2,5-disubstituées et 3-méthyl pyrazines 2,5,6-trisubstitués en tant qu'inhibiteurs allostériques de shp2 - Google Patents

3-méthylpyrazines 2,5-disubstituées et 3-méthyl pyrazines 2,5,6-trisubstitués en tant qu'inhibiteurs allostériques de shp2

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Publication number
MA45660A
MA45660A MA045660A MA45660A MA45660A MA 45660 A MA45660 A MA 45660A MA 045660 A MA045660 A MA 045660A MA 45660 A MA45660 A MA 45660A MA 45660 A MA45660 A MA 45660A
Authority
MA
Morocco
Prior art keywords
methylpyrazines
shp2
trisubstituted
disubstituted
allosteric inhibitors
Prior art date
Application number
MA045660A
Other languages
English (en)
French (fr)
Inventor
Naing Aay
Andreas Buckl
Adrian Gill
Ashutosh Jogalekar
Gert Kiss
Elena S Koltun
Kevin Mellem
Christopher Semko
Walter Won
Original Assignee
Revolution Medicines Inc
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 Revolution Medicines Inc filed Critical Revolution Medicines Inc
Publication of MA45660A publication Critical patent/MA45660A/fr

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three 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
    • C07D241/20Nitrogen atoms
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
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    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three 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
    • C07D241/18Oxygen or sulfur atoms
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    • 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
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    • 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
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    • 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D477/00Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring
    • C07D477/26Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hetero atoms or carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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    • C07ORGANIC CHEMISTRY
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    • 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
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    • C07D519/00Heterocyclic 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
MA045660A 2016-07-12 2017-07-11 3-méthylpyrazines 2,5-disubstituées et 3-méthyl pyrazines 2,5,6-trisubstitués en tant qu'inhibiteurs allostériques de shp2 MA45660A (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662361249P 2016-07-12 2016-07-12
US201762449523P 2017-01-23 2017-01-23

Publications (1)

Publication Number Publication Date
MA45660A true MA45660A (fr) 2019-05-22

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MA045660A MA45660A (fr) 2016-07-12 2017-07-11 3-méthylpyrazines 2,5-disubstituées et 3-méthyl pyrazines 2,5,6-trisubstitués en tant qu'inhibiteurs allostériques de shp2

Country Status (22)

Country Link
US (3) US10590090B2 (https=)
EP (2) EP4302834A3 (https=)
JP (3) JP6916279B2 (https=)
KR (2) KR102598895B1 (https=)
CN (3) CN109983001B (https=)
AU (3) AU2017296289A1 (https=)
CA (1) CA3030167A1 (https=)
CL (1) CL2019000090A1 (https=)
CO (1) CO2019000613A2 (https=)
CR (1) CR20190063A (https=)
DO (1) DOP2019000005A (https=)
EC (1) ECSP19010079A (https=)
IL (3) IL321811A (https=)
MA (1) MA45660A (https=)
MX (2) MX395351B (https=)
MY (1) MY199046A (https=)
PE (1) PE20190624A1 (https=)
PH (1) PH12019500056B1 (https=)
SG (1) SG11201900157RA (https=)
TN (1) TN2019000010A1 (https=)
TW (2) TWI912604B (https=)
WO (1) WO2018013597A1 (https=)

Families Citing this family (149)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11466017B2 (en) 2011-03-10 2022-10-11 Board Of Regents, The University Of Texas System Heterocyclic inhibitors of PTPN11
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
WO2017210134A1 (en) 2016-05-31 2017-12-07 Board Of Regents, University Of Texas System Heterocyclic inhibitors of ptpn11
MX388576B (es) 2016-06-07 2025-03-20 Jacobio Pharmaceuticals Co Ltd Derivados heterociclicos novedosos utiles como inhibidores de shp2.
WO2017216706A1 (en) 2016-06-14 2017-12-21 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
EP4302834A3 (en) * 2016-07-12 2024-07-17 Revolution Medicines, Inc. 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
WO2018057884A1 (en) 2016-09-22 2018-03-29 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
TW202500565A (zh) 2016-10-24 2025-01-01 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其使用方法
KR20190110588A (ko) 2017-01-23 2019-09-30 레볼루션 메디슨즈, 인크. 알로스테릭 shp2 억제제로서의 피리딘 화합물
JP7240319B2 (ja) 2017-01-23 2023-03-15 レヴォリューション・メディスンズ,インコーポレイテッド アロステリックshp2阻害剤としての二環式化合物
EA202190196A1 (ru) * 2017-03-23 2021-08-31 Джакобио Фармасьютикалс Ко., Лтд. Новые гетероциклические производные, применимые в качестве ингибиторов shp2
BR102018007822A2 (pt) 2017-04-20 2018-11-06 Gilead Sciences, Inc. composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição
EP3630770B1 (en) 2017-05-26 2024-08-28 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
CA3074690A1 (en) * 2017-09-07 2019-03-14 Revolution Medicines, Inc. Shp2 inhibitor compositions and methods for treating cancer
JP7447002B2 (ja) 2017-09-11 2024-03-11 クルーゾン・ファーマシューティカルズ・インコーポレイテッド SHP2のオクタヒドロシクロペンタ[c]ピロールのアロステリック阻害剤
EP3687997A1 (en) 2017-09-29 2020-08-05 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
TW201930292A (zh) 2017-10-12 2019-08-01 美商銳新醫藥公司 作為變構shp2抑制劑的吡啶、吡嗪和三嗪化合物
JP7361693B2 (ja) 2017-12-15 2023-10-16 レヴォリューション・メディスンズ,インコーポレイテッド アロステリックshp2阻害剤としての多環式化合物
CN110156786B (zh) * 2018-02-13 2022-06-03 青煜医药研发(上海)有限公司 嘧啶并环化合物及其制备方法和应用
CR20200347A (es) 2018-02-13 2020-09-23 Gilead Sciences Inc Inhibidores pd-1/pd-l1
CN110655520A (zh) * 2018-06-29 2020-01-07 上海青煜医药科技有限公司 嘧啶并环化合物及其制备方法和应用
JP7335882B2 (ja) * 2018-02-13 2023-08-30 ブルーレイ セラピューティクス (シャンハイ) カンパニー,リミティド ピリミジン縮合環式化合物及びその製造方法、並びに使用
AU2019240299B2 (en) * 2018-03-21 2023-06-22 D.E. Shaw Research, Llc SHP2 phosphatase inhibitors and methods of use thereof
RU2020133727A (ru) * 2018-03-21 2022-04-21 Сучжоу Пухе Биофарма Ко., Лтд. Ингибиторы shp2 и их применение
US12138263B2 (en) 2018-03-21 2024-11-12 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine SHP2 phosphatase inhibitors and methods of use thereof
MX2020010719A (es) * 2018-04-10 2020-11-06 Revolution Medicines Inc Composiciones de inhibidores de shp2, metodos para tratar el cancer y metodos para identificar a un sujeto con mutaciones en shp2.
MX2020011528A (es) * 2018-05-02 2021-02-09 Navire Pharma Inc Inhibidores heterociclicos sustituidos de ptpn11.
SG11202012425QA (en) 2018-07-13 2021-01-28 Gilead Sciences Inc Pd-1/pd-l1 inhibitors
CN112601750B (zh) 2018-08-10 2023-10-31 纳维尔制药有限公司 Ptpn11(shp2)抑制剂
CR20210175A (es) * 2018-09-18 2021-06-01 Nikang Therapeutics Inc Derivados de anillo tricíclico condensado como inhibidores de la fosfatasa de homología a src 2 (shp2)
US20210393623A1 (en) 2018-09-26 2021-12-23 Jacobio Pharmaceuticals Co., Ltd. Novel Heterocyclic Derivatives Useful as SHP2 Inhibitors
CN112867718B (zh) * 2018-09-29 2025-03-04 诺华股份有限公司 用于抑制shp2活性的化合物和组合物的制造
EP3860717A1 (en) 2018-10-03 2021-08-11 Gilead Sciences, Inc. Imidozopyrimidine derivatives
JP2022508651A (ja) * 2018-10-08 2022-01-19 レヴォリューション・メディスンズ,インコーポレイテッド 癌を処置するためのshp2阻害剤組成物および方法
TW202028183A (zh) * 2018-10-10 2020-08-01 大陸商江蘇豪森藥業集團有限公司 含氮雜芳類衍生物調節劑、其製備方法和應用
BR112021005733A2 (pt) 2018-10-17 2021-07-27 Array Biopharma Inc. inibidores de proteína tirosina fosfatase
CN109265352B (zh) * 2018-10-31 2021-06-04 杭州迈世腾药物科技有限公司 芳基环丙基醚及其衍生物的制备方法
EP3889153A4 (en) 2018-11-30 2022-09-07 Tuojie Biotech (Shanghai) Co., Ltd. PYRIMIDINE AND FIVE-MEMBERED HETEROCYCLIC NITROGEN DERIVATIVE, METHOD OF MANUFACTURE THEREOF AND MEDICAL USES THEREOF
WO2020156242A1 (zh) * 2019-01-31 2020-08-06 贝达药业股份有限公司 Shp2抑制剂及其应用
MX2021010323A (es) 2019-03-01 2021-12-10 Revolution Medicines Inc Compuestos bicíclicos de heterociclilo y usos de este.
MX2021010319A (es) 2019-03-01 2021-12-10 Revolution Medicines Inc Compuestos biciclicos de heteroarilo y usos de estos.
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
US11033547B2 (en) 2019-03-07 2021-06-15 Merck Patent Gmbh Carboxamide-pyrimidine derivatives as SHP2 antagonists
CU20210080A7 (es) 2019-04-02 2022-05-11 Array Biopharma Inc Triazinas sustituidas como inhibidores de proteína tirosina fosfatasa
JP7586834B2 (ja) 2019-04-08 2024-11-19 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング Shp2拮抗薬としてのピリミジノン誘導体
CN115141205A (zh) 2019-06-07 2022-10-04 锐新医药公司 Shp2抑制剂的固体形式
KR20220054285A (ko) 2019-06-28 2022-05-02 투오지에 바이오텍 (상하이) 컴퍼니 리미티드 피리미딘 5 원 질소 헤테로고리형 유도체, 이의 제조 방법 및 이의 약학적 용도
CN111704611B (zh) * 2019-07-25 2022-01-14 上海凌达生物医药有限公司 一类芳基螺环类shp2抑制剂化合物、制备方法和用途
CN112300160A (zh) * 2019-08-01 2021-02-02 上海奕拓医药科技有限责任公司 一种螺芳环化合物、其制备及应用
EP3772513A1 (en) 2019-08-09 2021-02-10 C.N.C.C.S. S.c.a.r.l. Collezione Nazionale Dei Composti Chimici e Centro Screening Shp2 inhibitors
GB201911928D0 (en) 2019-08-20 2019-10-02 Otsuka Pharma Co Ltd Pharmaceutical compounds
WO2021043077A1 (zh) * 2019-09-06 2021-03-11 四川科伦博泰生物医药股份有限公司 一种取代吡嗪化合物、其制备方法和用途
CN114502165A (zh) * 2019-09-23 2022-05-13 苏州浦合医药科技有限公司 Shp2抑制剂及其用途
MX2022003454A (es) 2019-09-24 2022-04-19 Relay Therapeutics Inc Inhibidores de fosfatasa shp2 y metodos para su fabricacion y uso.
CN112724145A (zh) * 2019-10-14 2021-04-30 杭州雷索药业有限公司 用于抑制shp2活性的吡嗪衍生物
US20240139193A1 (en) 2019-10-15 2024-05-02 Amgen Inc. Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers
IL322454A (en) 2019-11-04 2025-09-01 Revolution Medicines Inc ras inhibitors
TW202132316A (zh) 2019-11-04 2021-09-01 美商銳新醫藥公司 Ras抑制劑
AU2020377925A1 (en) 2019-11-04 2022-05-05 Revolution Medicines, Inc. Ras inhibitors
CA3156359A1 (en) 2019-11-08 2021-05-14 Adrian Liam Gill Bicyclic heteroaryl compounds and uses thereof
EP4065231A1 (en) 2019-11-27 2022-10-05 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
EP4069301A1 (en) 2019-12-04 2022-10-12 Bayer Aktiengesellschaft Inhibitors of shp2
WO2021142026A1 (en) 2020-01-07 2021-07-15 Revolution Medicines, Inc. Shp2 inhibitor dosing and methods of treating cancer
WO2021143680A1 (zh) 2020-01-16 2021-07-22 浙江海正药业股份有限公司 杂芳基类衍生物及其制备方法和用途
CN113135910A (zh) 2020-01-19 2021-07-20 北京诺诚健华医药科技有限公司 嘧啶-4(3h)-酮类杂环化合物、其制备方法及其在医药学上的应用
CN114846005B (zh) * 2020-01-21 2024-04-02 贝达药业股份有限公司 Shp2抑制剂及其应用
EP4110338A1 (en) 2020-02-28 2023-01-04 Novartis AG A triple pharmaceutical combination comprising dabrafenib, an erk inhibitor and a shp2 inhibitor
CN113493440B (zh) * 2020-04-03 2024-08-23 上海翰森生物医药科技有限公司 含氮杂芳类衍生物的盐及其晶型
TW202144334A (zh) * 2020-04-03 2021-12-01 大陸商上海翰森生物醫藥科技有限公司 含氮雜芳類衍生物游離鹼的晶型
CN115362149B (zh) * 2020-04-26 2024-05-14 贝达药业股份有限公司 Shp2抑制剂及其组合物和应用
CA3181898A1 (en) * 2020-06-11 2021-12-16 Bang Fu Shp2 inhibitors, compositions and uses thereof
IL299131A (en) 2020-06-18 2023-02-01 Revolution Medicines Inc Methods for delaying, preventing and treating acquired resistance to RAS inhibitors
JP2023530838A (ja) 2020-06-22 2023-07-20 スーチュアン・コールン-バイオテック・バイオファーマシューティカル・カンパニー・リミテッド 置換されたピラジン化合物、当該化合物を含む医薬組成物、及びその使用
US12441737B2 (en) 2020-07-08 2025-10-14 Novartis Ag Manufacture of compounds and compositions for inhibiting the activity of SHP2
WO2022042331A1 (zh) * 2020-08-25 2022-03-03 四川科伦博泰生物医药股份有限公司 杂环化合物及其制备方法和用途
US20250195521A1 (en) 2020-09-03 2025-06-19 Revolution Medicines, Inc. Use of sos1 inhibitors to treat malignancies with shp2 mutations
CA3194067A1 (en) 2020-09-15 2022-03-24 Revolution Medicines, Inc. Ras inhibitors
US20240059703A1 (en) 2020-10-20 2024-02-22 Amgen Inc. Heterocyclic spiro compounds and methods of use
WO2022093856A1 (en) 2020-10-27 2022-05-05 Amgen Inc. Heterocyclic spiro compounds and methods of use
CN116848121A (zh) * 2020-12-18 2023-10-03 建新公司 制备shp2抑制剂的方法
TW202241907A (zh) * 2020-12-18 2022-11-01 美商瑞佛路森醫藥公司 製備shp2抑制劑之方法
JP7849366B2 (ja) 2020-12-22 2026-04-21 キル・レガー・セラピューティクス・インコーポレーテッド Sos1阻害剤およびその使用
WO2022161222A1 (zh) * 2021-01-29 2022-08-04 四川科伦博泰生物医药股份有限公司 一类杂环类shp2抑制剂、其制备方法及用途
EP4039685A1 (en) 2021-02-08 2022-08-10 Irbm S.P.A. Azabicyclic shp2 inhibitors
WO2022206684A1 (zh) * 2021-03-31 2022-10-06 南京明德新药研发有限公司 一系列含Se的吡嗪类化合物及其应用
US20240190843A1 (en) * 2021-04-01 2024-06-13 Array Biopharma Inc. Crystalline form of a shp2 inhibitor
EP4067358A1 (en) 2021-04-02 2022-10-05 C.N.C.C.S. S.c.a.r.l. Collezione Nazionale Dei Composti Chimici e Centro Screening (s)-1-(5-((pyridin-3-yl)thio)pyrazin-2-yl)-4'h,6'h-spiro[piperidine-4,5'-pyrrolo[1,2-b]pyrazol]-4'-amine derivatives and similar compounds as shp2 inhibitors for the treatment of e.g. cancer
MX2023012725A (es) 2021-04-29 2024-09-23 Amgen Inc Compuestos de 2-aminobenzotiazol y metodos de uso de los mismos.
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
TW202309052A (zh) 2021-05-05 2023-03-01 美商銳新醫藥公司 Ras抑制劑
KR20240017811A (ko) 2021-05-05 2024-02-08 레볼루션 메디슨즈, 인크. 암의 치료를 위한 ras 억제제
JP2024516997A (ja) 2021-05-05 2024-04-18 フヤバイオ インターナショナル,エルエルシー Shp2阻害剤単独療法およびその使用
CN117177752A (zh) 2021-05-05 2023-12-05 诺华股份有限公司 用于治疗mpnst的化合物和组合物
IL308222A (en) 2021-05-05 2024-01-01 Huyabio Int Llc Combination therapies that include SHP2 inhibitors and PD-1 inhibitors
AU2022274936B2 (en) * 2021-05-13 2025-08-21 Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences Heterocyclic compound for inhibiting shp2 activity, preparation method therefor and use thereof
WO2022242767A1 (zh) 2021-05-21 2022-11-24 石药集团中奇制药技术(石家庄)有限公司 螺环类化合物及其用途
WO2022259157A1 (en) 2021-06-09 2022-12-15 Novartis Ag A triple pharmaceutical combination comprising dabrafenib, trametinib and a shp2 inhibitor
TW202317100A (zh) 2021-06-23 2023-05-01 瑞士商諾華公司 包含kras g12c抑制劑的藥物組合及其用於治療癌症之用途
TW202319056A (zh) * 2021-07-09 2023-05-16 南韓商治納輔醫藥科技有限公司 Shp2抑制劑及其用途
CN113636952B (zh) * 2021-07-19 2023-07-21 河南农业大学 一种制备4-溴苯甲酰胺的方法
EP4385991A4 (en) * 2021-08-09 2025-10-01 Ubix Therapeutics Inc COMPOUND HAVING SHP2 PROTEIN DEGRADING ACTIVITY AND ITS MEDICAL USES
KR20240055778A (ko) 2021-09-01 2024-04-29 노파르티스 아게 Tead 억제제를 포함하는 제약 조합물 및 암의 치료를 위한 이의 용도
WO2023046198A1 (zh) * 2021-09-27 2023-03-30 中国医药研究开发中心有限公司 磺胺酮类化合物及其制备方法和医药用途
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023122938A1 (en) * 2021-12-28 2023-07-06 Js Innomed Holdings Ltd. Heterocyclic compounds as shp2 inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof
EP4479398A1 (en) 2022-02-16 2024-12-25 Amgen Inc. Quinazoline compounds and use thereof as inhibtors of mutant kras proteins
MX2024010045A (es) 2022-02-16 2024-08-26 Amgen Inc Compuestos de quinazolina y uso de los mismos como inhibidores de proteinas mutantes kras.
EP4486345A1 (en) 2022-03-04 2025-01-08 Eli Lilly and Company Method of treatment including kras g12c inhibitors and shp2 inhibitors
JP2025510572A (ja) 2022-03-08 2025-04-15 レボリューション メディシンズ インコーポレイテッド 免疫不応性肺癌を治療するための方法
WO2023169170A1 (zh) * 2022-03-10 2023-09-14 捷思英达控股有限公司 作为shp2抑制剂的杂环化合物、包括该杂环化合物的组合物、及其使用方法
EP4496566A1 (en) 2022-03-21 2025-01-29 Institut National de la Santé et de la Recherche Médicale (INSERM) Use of shp2 inhibitors for inhibiting senescence
CN118871443A (zh) * 2022-03-28 2024-10-29 建新公司 用于制备shp2抑制剂的方法
US11878958B2 (en) 2022-05-25 2024-01-23 Ikena Oncology, Inc. MEK inhibitors and uses thereof
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2024015360A1 (en) 2022-07-11 2024-01-18 Amgen Inc. Methods of treating cancer
EP4573095A1 (en) 2022-08-17 2025-06-25 Treeline Biosciences, Inc. Pyridopyrimidine kras inhibitors
EP4345101A1 (en) 2022-09-29 2024-04-03 Irbm S.P.A. Azole derivatives as shp2 inhibitors
KR20250087568A (ko) * 2022-10-19 2025-06-16 주식회사 유빅스테라퓨틱스 Shp2 단백질 분해용 화합물 및 이들의 의약 용도
AU2023382606A1 (en) 2022-11-14 2025-05-08 Amgen Inc. Macrocyclic kras inhibitors and methods of use
WO2024113194A1 (en) * 2022-11-30 2024-06-06 Canwell Biotech Limited Shp2 inhibitors, compositions and methods thereof
AU2024241633A1 (en) 2023-03-30 2025-11-06 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
AR132338A1 (es) 2023-04-07 2025-06-18 Revolution Medicines Inc Inhibidores de ras
CR20250420A (es) 2023-04-07 2025-11-20 Revolution Medicines Inc Inhibidores macrocíclicos de ras
CN121464140A (zh) 2023-04-14 2026-02-03 锐新医药公司 Ras抑制剂的结晶形式、含有其的组合物及其使用方法
CN121100123A (zh) 2023-04-14 2025-12-09 锐新医药公司 Ras抑制剂的结晶形式
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ras相關疾病或病症之組合療法
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
TW202528315A (zh) 2023-09-21 2025-07-16 美商樹線生物科學公司 螺環二氫哌喃并吡啶KRas抑制劑
AU2024360465A1 (en) 2023-10-12 2026-04-09 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2025081291A1 (en) * 2023-10-16 2025-04-24 Canwell Biotech Limited Benzo [c] [1, 2] oxaborol-1 (3h) -ol derivatives as shp2 inhibitors, compositions and methods thereof
TW202542151A (zh) 2023-12-22 2025-11-01 美商銳格醫藥有限公司 Sos1抑制劑及其用途
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025194054A1 (en) 2024-03-14 2025-09-18 Amgen Inc. Spirocyclic compounds as modulators of kras and uses thereof
TW202602882A (zh) 2024-03-14 2026-01-16 美商安進公司 作為kras調節劑的大環化合物及其用途
WO2025217247A1 (en) 2024-04-10 2025-10-16 Amgen Inc. Tethered spiro-heterocyclic inhibitors of kras g12c mutant proteins and uses thereof
WO2025230878A1 (en) 2024-04-29 2025-11-06 Amgen Inc. Macrocyclic compounds as modulators of kras and uses thereof
WO2025240582A1 (en) 2024-05-14 2025-11-20 Amgen Inc. Macrocyclic compounds as modulators of kras and uses thereof
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ras抑制劑
WO2025245127A1 (en) 2024-05-21 2025-11-27 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026055477A1 (en) 2024-09-06 2026-03-12 Amgen Inc. Macrocyclic compounds as modulators of kras and uses thereof
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer
CN119661551B (zh) * 2024-12-16 2025-11-25 重庆大学 一种(3r,4s)-3-甲基-2-氧杂-8-氮杂螺[4.5]癸烷-4-胺盐酸盐的制备方法

Family Cites Families (125)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2572728A (en) * 1949-01-07 1951-10-23 American Cyanamid Co Hydroxybenzenesulfonamidopyra-zines and preparation of same
US2636882A (en) 1950-08-11 1953-04-28 Quaker Oats Co Preparation of 3-pyridols from 2-acylfurans
BE758503A (fr) 1969-11-07 1971-05-05 Shell Int Research Compositions pesticides
GB1459571A (en) 1974-09-12 1976-12-22 Pfizer Ltd Thiophene-2-sulphonamide derivatives and their use as therapeutic agents sheet orienting apparatus
JPS5762269A (en) * 1980-10-03 1982-04-15 Ogawa Koryo Kk 2,3,5-trisubstituted pyrazine derivative
US4513135A (en) * 1982-03-05 1985-04-23 Eli Lilly And Company Diaryl-pyrazine derivatives affecting GABA binding
JPH0249775A (ja) 1988-05-19 1990-02-20 Nippon Soda Co Ltd 6員環又は7員環を有する複素環化合物及びその製造方法
JPH04112877A (ja) 1990-09-04 1992-04-14 Nippon Soda Co Ltd 新規シアノピラジン誘導体及びその製造方法
EP0579835A4 (en) 1991-11-12 1994-06-01 Nippon Soda Co Wavelength conversion material for agriculture
US5262564A (en) 1992-10-30 1993-11-16 Octamer, Inc. Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents
GB9504854D0 (en) 1994-03-31 1995-04-26 Zeneca Ltd Nitrogen derivatives
AU713673B2 (en) 1996-02-07 1999-12-09 Neurocrine Biosciences Inc. Pyrazolopyrimidines as crf receptor antagonists
CA2293400A1 (en) * 1997-06-13 1998-12-17 Gerald Mcmahon Novel heteroaryl compounds for the modulation of protein tyrosine enzyme related cellular signal transduction
WO2001016097A1 (en) 1999-08-27 2001-03-08 Sugen, Inc. Phosphate mimics and methods of treatment using phosphatase inhibitors
PL365238A1 (en) 2000-02-16 2004-12-27 Neurogen Corporation Substituted arylpyrazines
TWI316055B (https=) 2001-04-26 2009-10-21 Nippon Shinyaku Co Ltd
WO2003029422A2 (en) 2001-10-01 2003-04-10 Mount Sinai School Of Medicine Noonan syndrome gene
US6921762B2 (en) 2001-11-16 2005-07-26 Amgen Inc. Substituted indolizine-like compounds and methods of use
BR0214309A (pt) 2001-11-21 2004-10-13 Upjohn Co Derivados aril-1,4-pirazina substituìdos
EP1492784A4 (en) 2002-03-28 2006-03-29 Merck & Co Inc SUBSTITUTED 2,3-DIPHENYLPYRIDINES
JP2005533014A (ja) 2002-04-26 2005-11-04 ファルマシア・アンド・アップジョン・カンパニー・エルエルシー 置換ピラジン誘導体
US20040116444A1 (en) * 2002-09-12 2004-06-17 Corbett Jeffrey W. Substituted 1,4-pyrazine derivatives
CN101899114A (zh) 2002-12-23 2010-12-01 惠氏公司 抗pd-1抗体及其用途
US7157460B2 (en) 2003-02-20 2007-01-02 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
JP2006525993A (ja) 2003-05-09 2006-11-16 ファルマシア・アンド・アップジョン・カンパニー・エルエルシー Crf1受容体拮抗剤である化合物
GB0314057D0 (en) * 2003-06-18 2003-07-23 Astrazeneca Ab Therapeutic agents
FR2856684B1 (fr) 2003-06-26 2008-04-11 Sanofi Synthelabo Derives de diphenylpyridine, leur preparation et leur application en therapeutique
US7326706B2 (en) * 2003-08-15 2008-02-05 Bristol-Myers Squibb Company Pyrazine modulators of cannabinoid receptors
CA2537916A1 (en) 2003-09-03 2005-03-31 Neurogen Corporation 5-aryl-pyrazolo[4,3-d]pyrimidines, pyridines, and pyrazines and related compounds
BRPI0415185A (pt) 2003-10-10 2006-11-28 Pfizer Prod Inc 2h-[1,2,4]triazol[4,3-a]pirazinas substituìdas como inibidores da gsk-3
CA2543644A1 (en) * 2003-10-27 2005-05-06 Astellas Pharma Inc. Pyrazine derivatives and pharmaceutical use thereof
WO2005095384A1 (en) 2004-04-01 2005-10-13 Astellas Pharma Inc. Pyrazine derivatives and pharmaceutical use thereof as adenosine antagonists
DE102004015954A1 (de) * 2004-04-01 2005-11-10 Ina-Schaeffler Kg Umschlingungstrieb
US20050282818A1 (en) 2004-06-22 2005-12-22 Rigel Pharmaceuticals, Inc. Ubiquitin ligase inhibitors
AU2005322114A1 (en) 2004-12-23 2006-07-06 Mallinckrodt Llc Fluorescent pyrazine derivatives and methods of using the same in assessing renal function
TW200716594A (en) * 2005-04-18 2007-05-01 Neurogen Corp Substituted heteroaryl CB1 antagonists
UA95244C2 (ru) 2005-06-22 2011-07-25 Плексикон, Инк. Соединения и способ модулирования активности киназ, и показания для их применения
EP1948827B1 (en) 2005-10-21 2016-03-23 The Regents of The University of California C-kit oncogene mutations in melanoma
CA2616147A1 (en) * 2006-02-24 2007-09-20 Mallinckrodt Inc. Process for using optical agents
WO2007117699A2 (en) 2006-04-07 2007-10-18 University Of South Florida Inhibition of shp2/ptpn11 protein tyrosine phosphatase by nsc-87877, nsc-117199 and their analogs
AU2007243280A1 (en) 2006-04-28 2007-11-08 Northwestern University Formulations containing pyridazine compounds for treating neuroinflammatory diseases
US7893058B2 (en) 2006-05-15 2011-02-22 Janssen Pharmaceutica Nv Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases
PT2029602E (pt) 2006-05-31 2010-07-08 Galapagos Nv Compostos de triazolopirazina uteis para o tratamento de doenãas degenerativas e inflamatërias
EP2029605A1 (en) 2006-06-06 2009-03-04 Schering Corporation Imidazopyrazines as protein kinase inhibitors
JP2010520238A (ja) * 2007-03-01 2010-06-10 マリンクロット インコーポレイテッド 統合された光活性低分子および統合された光活性低分子使用
CN101679418A (zh) 2007-04-06 2010-03-24 诺瓦提斯公司 用作蛋白质激酶抑制剂的[2,6]萘啶类化合物
WO2008138843A1 (en) 2007-05-10 2008-11-20 Galapagos N.V. Imidazopyridines and triazolopyrimidines useful for the treatment of joint degenerative & inflammatory diseases
US8148369B2 (en) 2007-05-10 2012-04-03 Janssen Pharmaceutica Nv Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases
EP2157090A4 (en) 2007-06-21 2011-09-07 Taisho Pharmaceutical Co Ltd PYRAZINAMIDE COMPOUND
CA2695621A1 (en) 2007-08-09 2009-02-12 Merck Sharp & Dohme Corp. Pyridine carboxamide orexin receptor antagonists
US20090062277A1 (en) 2007-08-21 2009-03-05 Essa Hu Phosphodiesterase 10 inhibitors
JP2010031249A (ja) * 2008-06-23 2010-02-12 Sumitomo Chemical Co Ltd 組成物及び該組成物を用いてなる発光素子
WO2010011666A2 (en) 2008-07-21 2010-01-28 University Of South Florida Indoline scaffold shp-2 inhibitors and cancer treatment method
AU2009308982A1 (en) 2008-10-30 2010-05-06 Merck Sharp & Dohme Corp. Pyridazine carboxamide orexin receptor antagonists
CA2743449C (en) * 2008-11-12 2016-10-18 Ariad Pharmaceuticals, Inc. Pyrazinopyrazines and derivatives as kinase inhibitors
BRPI1006942A2 (pt) 2009-01-23 2016-04-12 Rigel Pharmaceuticals Inc composto, composição farmacêutica, kit, métodos para inibir uma atividade de uma jak quinase, para tratar uma doença, para tratar a rejeição de transplante de aloenxerto em um receptor de transplante, para tratar uma reação de hipersensibilidade, e para inibir uma cascata de transdução de sinal, e, uso do composto
WO2010121212A2 (en) 2009-04-17 2010-10-21 H. Lee Moffit Cancer Center And Research Institute, Inc. Indoline scaffold shp-2 inhibitors and method of treating cancer
EP2438041A4 (en) 2009-06-01 2012-11-21 Merck Sharp & Dohme PYRAZINE-carboxamide-orexin receptor Antagonist
NZ713361A (en) * 2009-08-17 2017-06-30 Memorial Sloan Kettering Cancer Center Heat shock protein binding compounds, compositions, and methods for making and using same
US8163283B2 (en) 2009-09-03 2012-04-24 Vancouver Biotech Ltd. Monoclonal antibodies against gonadotropin-releasing hormone receptor
US8673913B2 (en) 2009-11-13 2014-03-18 Case Western Reserve University SHP-2 phosphatase inhibitor
JP5989547B2 (ja) 2010-03-05 2016-09-07 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト ヒトcsf−1rに対する抗体及びその使用
WO2011143148A1 (en) 2010-05-11 2011-11-17 Sanofi Substituted n-heteroaryl spirolactam bipyrrolidines, preparation and therapeutic use thereof
US8703768B2 (en) 2010-06-09 2014-04-22 Hoffmann-La Roche Inc. Nitrogen containing heteroaryl compounds
PT2593452T (pt) 2010-07-14 2017-04-24 Novartis Ag Compostos heterocíclicos agonistas do receptor ip
GB201106829D0 (en) * 2011-04-21 2011-06-01 Proximagen Ltd Heterocyclic compounds
WO2012116237A2 (en) 2011-02-23 2012-08-30 Intellikine, Llc Heterocyclic compounds and uses thereof
WO2012149280A2 (en) 2011-04-29 2012-11-01 Abbott Laboratories Novel tricyclic compounds
CN103181918B (zh) 2011-05-04 2014-10-29 厦门大学 脂肪酸类化合物在制备预防和治疗肝癌药物中的应用
US20150005311A1 (en) * 2012-01-13 2015-01-01 Novartis Ag IP receptor agonist heterocyclic compounds
EA026353B1 (ru) 2012-01-17 2017-03-31 Астеллас Фарма Инк. Соединение пиразинкарбоксамида
JP6374384B2 (ja) 2012-08-07 2018-08-15 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung プロテインキナーゼ阻害剤としてのピリドピリミジン誘導体
CA2890009C (en) 2012-11-08 2017-11-28 Pfizer Inc. Heteroaromatic compounds and their use as dopamine d1 ligands
MX359651B (es) 2012-11-29 2018-10-05 Chemocentryx Inc Antagonistas de cxcr7.
WO2014113584A1 (en) 2013-01-16 2014-07-24 Rhode Island Hospital Compositions and methods for the prevention and treatment of osteolysis and osteoporosis
WO2014121885A1 (en) * 2013-02-07 2014-08-14 Merck Patent Gmbh Substituted quinoxaline derivatives and their use as positive allosteric modulators of mglur4
JP6647868B2 (ja) 2013-02-20 2020-02-14 ノバルティス アーゲー ヒト化抗EGFRvIIIキメラ抗原受容体を用いたがんの処置
US10501531B2 (en) 2013-03-13 2019-12-10 Prothena Biosciences Limited Tau immunotherapy
CN103554038B (zh) 2013-06-19 2015-10-14 云南大学 多卤代苯腈喹唑啉酮化合物及其制备方法和用途
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
ES2699351T3 (es) 2014-01-17 2019-02-08 Novartis Ag Derivados de 1-piridazin/triazin-3-il-piper(-azina)/idina/pirolidina y composiciones de las mismas para inhibir la actividad de SHP2
WO2015107494A1 (en) * 2014-01-17 2015-07-23 Novartis Ag 1 -(triazin-3-yi_/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions thereof for inhibiting the activity of shp2
WO2016007731A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyridines and imidazopyrazines as lsd1 inhibitors
JP6759514B2 (ja) 2014-08-01 2020-09-23 ヌエヴォリューション・アクティーゼルスカブNuevolution A/S ブロモドメインに対して活性な化合物
AU2015311805B2 (en) * 2014-09-05 2020-04-02 Celgene Quanticel Research, Inc. Inhibitors of lysine specific demethylase-1
US10472347B2 (en) * 2014-11-18 2019-11-12 Merck Sharp & Dohme Corp. Aminopyrazine compounds with A2A antagonist properties
WO2016100116A1 (en) 2014-12-17 2016-06-23 Siemens Healthcare Diagnostics Inc. Sandwich assay design for small molecules
UY36462A (es) 2014-12-23 2016-07-29 Novartis Ag Compuestos de triazolopirimidina y usos de los mismos
EP3247378B8 (en) 2015-01-09 2023-08-23 Revolution Medicines, Inc. Macrocyclic compounds that participate in cooperative binding and medical uses thereof
TW201706265A (zh) * 2015-03-09 2017-02-16 必治妥美雅史谷比公司 做為Rho激酶(ROCK)抑制劑之內醯胺
EP3277689B1 (en) 2015-04-03 2019-09-04 Incyte Corporation Heterocyclic compounds as lsd1 inhibitors
US10287266B2 (en) * 2015-06-19 2019-05-14 Novartis Ag Compounds and compositions for inhibiting the activity of SHP2
WO2016203405A1 (en) 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
EP3310779B1 (en) 2015-06-19 2019-05-08 Novartis AG Compounds and compositions for inhibiting the activity of shp2
US10426842B2 (en) 2015-07-15 2019-10-01 The Curators Of The University Of Missouri Targeted nanoparticle conjugate and method for co-delivery of siRNA and drug
EP4242304A3 (en) 2015-10-01 2024-02-07 Revolution Medicines, Inc. Methods and reagents for analyzing protein-protein interfaces
WO2017079723A1 (en) 2015-11-07 2017-05-11 Board Of Regents, The University Of Texas System Targeting proteins for degradation
WO2017156397A1 (en) 2016-03-11 2017-09-14 Board Of Regents, The University Of Texas Sysytem Heterocyclic inhibitors of ptpn11
MX388576B (es) * 2016-06-07 2025-03-20 Jacobio Pharmaceuticals Co Ltd Derivados heterociclicos novedosos utiles como inhibidores de shp2.
WO2017216706A1 (en) 2016-06-14 2017-12-21 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
EP4302834A3 (en) * 2016-07-12 2024-07-17 Revolution Medicines, Inc. 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
WO2018057884A1 (en) 2016-09-22 2018-03-29 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
TW202500565A (zh) 2016-10-24 2025-01-01 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其使用方法
CA3048340A1 (en) 2017-01-10 2018-07-19 Novartis Ag Pharmaceutical combination comprising an alk inhibitor and a shp2 inhibitor
KR20190110588A (ko) 2017-01-23 2019-09-30 레볼루션 메디슨즈, 인크. 알로스테릭 shp2 억제제로서의 피리딘 화합물
JP7240319B2 (ja) 2017-01-23 2023-03-15 レヴォリューション・メディスンズ,インコーポレイテッド アロステリックshp2阻害剤としての二環式化合物
EA202190196A1 (ru) 2017-03-23 2021-08-31 Джакобио Фармасьютикалс Ко., Лтд. Новые гетероциклические производные, применимые в качестве ингибиторов shp2
IL269779B2 (en) 2017-04-05 2026-04-01 Revolution Medicines Inc Methods and reagents for the analysis of protein-protein interfaces
CA3058953A1 (en) 2017-04-05 2018-10-11 Revolution Medicines, Inc. Compounds that participate in cooperative binding and uses thereof
EP3630770B1 (en) 2017-05-26 2024-08-28 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
CA3074690A1 (en) 2017-09-07 2019-03-14 Revolution Medicines, Inc. Shp2 inhibitor compositions and methods for treating cancer
TW201930292A (zh) 2017-10-12 2019-08-01 美商銳新醫藥公司 作為變構shp2抑制劑的吡啶、吡嗪和三嗪化合物
JP7361693B2 (ja) 2017-12-15 2023-10-16 レヴォリューション・メディスンズ,インコーポレイテッド アロステリックshp2阻害剤としての多環式化合物
JP7335882B2 (ja) 2018-02-13 2023-08-30 ブルーレイ セラピューティクス (シャンハイ) カンパニー,リミティド ピリミジン縮合環式化合物及びその製造方法、並びに使用
CN110156786B (zh) 2018-02-13 2022-06-03 青煜医药研发(上海)有限公司 嘧啶并环化合物及其制备方法和应用
RU2020133727A (ru) 2018-03-21 2022-04-21 Сучжоу Пухе Биофарма Ко., Лтд. Ингибиторы shp2 и их применение
MX2020010719A (es) 2018-04-10 2020-11-06 Revolution Medicines Inc Composiciones de inhibidores de shp2, metodos para tratar el cancer y metodos para identificar a un sujeto con mutaciones en shp2.
MX2020011565A (es) 2018-05-01 2021-01-29 Revolution Medicines Inc Analogos de rapamicina ligados a c40, c28 y c-32 como inhibidores de mtor.
IL312291A (en) 2018-05-01 2024-06-01 Revolution Medicines Inc C-26-linked rapamycin analogs as MTOR inhibitors
EP3849535A4 (en) 2018-09-10 2022-06-29 Mirati Therapeutics, Inc. Combination therapies
CR20210175A (es) 2018-09-18 2021-06-01 Nikang Therapeutics Inc Derivados de anillo tricíclico condensado como inhibidores de la fosfatasa de homología a src 2 (shp2)
JP2022508651A (ja) 2018-10-08 2022-01-19 レヴォリューション・メディスンズ,インコーポレイテッド 癌を処置するためのshp2阻害剤組成物および方法
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法
BR112021012057A2 (pt) 2018-12-21 2021-10-19 Revolution Medicines, Inc. Compostos que participam de ligação cooperativa e usos dos mesmos
IL322454A (en) 2019-11-04 2025-09-01 Revolution Medicines Inc ras inhibitors

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