JP6473457B2 - Shp2の活性を阻害するための1−(トリアジン−3−イル/ピリダジン−3−イル)−ピペリジン/ピペラジン誘導体およびその組成物 - Google Patents

Shp2の活性を阻害するための1−(トリアジン−3−イル/ピリダジン−3−イル)−ピペリジン/ピペラジン誘導体およびその組成物 Download PDF

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JP6473457B2
JP6473457B2 JP2016546924A JP2016546924A JP6473457B2 JP 6473457 B2 JP6473457 B2 JP 6473457B2 JP 2016546924 A JP2016546924 A JP 2016546924A JP 2016546924 A JP2016546924 A JP 2016546924A JP 6473457 B2 JP6473457 B2 JP 6473457B2
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mmol
alkyl
halo
hydrogen
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チェン,ズオリアン
ドレ,マイケル
フォルタネト,ホルヘ,ガルシア
カーキ,ラジェシュ
充典 加藤
充典 加藤
ジェイ. ラマルシュ,マシュー
ジェイ. ラマルシュ,マシュー
ブラ ペレ,ローランス
ブラ ペレ,ローランス
ウィリアムス,サラー
センジック,マーティン
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ノバルティス アーゲー
ノバルティス アーゲー
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    • 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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    • 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
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/101,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
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    • 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
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

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JP2016546924A 2014-01-17 2015-01-16 Shp2の活性を阻害するための1−(トリアジン−3−イル/ピリダジン−3−イル)−ピペリジン/ピペラジン誘導体およびその組成物 Active JP6473457B2 (ja)

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US201461928746P 2014-01-17 2014-01-17
US61/928,746 2014-01-17
US201461991122P 2014-05-09 2014-05-09
US61/991,122 2014-05-09
PCT/IB2015/050344 WO2015107494A1 (en) 2014-01-17 2015-01-16 1 -(triazin-3-yi_/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions thereof for inhibiting the activity of shp2

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JP2017502994A JP2017502994A (ja) 2017-01-26
JP2017502994A5 JP2017502994A5 (https=) 2018-02-22
JP6473457B2 true JP6473457B2 (ja) 2019-02-20

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021130662A (ja) * 2015-06-19 2021-09-09 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

Families Citing this family (128)

* 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
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
GB201416351D0 (en) * 2014-09-16 2014-10-29 Shire Internat Gmbh Heterocyclic derivatives
CN112625028B (zh) * 2015-06-19 2024-10-29 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
ES2741746T3 (es) 2015-06-19 2020-02-12 Novartis Ag Compuestos y composiciones para inhibir la actividad de SHP2
EA201800367A1 (ru) 2015-12-10 2019-02-28 ПиТиСи ТЕРАПЬЮТИКС, ИНК. Способы лечения болезни хантингтона
AU2017274199B2 (en) 2016-05-31 2021-09-23 Board Of Regents, The University Of Texas System Heterocyclic inhibitors of PTPN11
EA202092441A1 (ru) 2016-06-07 2021-05-21 Джакобио Фармасьютикалс Ко., Лтд. Новые гетероциклические производные, применимые в качестве ингибиторов shp2
MX383856B (es) * 2016-06-14 2025-03-14 Novartis Ag Compuestos y composiciones para inhibir la actividad de shp2.
KR102598895B1 (ko) * 2016-07-12 2023-11-07 레볼루션 메디슨즈, 인크. 다른자리 입체성 shp2 억제제로서의 2,5-이치환 3-메틸 피라진 및 2,5,6-3치환 3-메틸 피라진
US11529347B2 (en) 2016-09-22 2022-12-20 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
US20190343836A1 (en) * 2017-01-10 2019-11-14 Novartis Ag Pharmaceutical combination comprising an alk inhibitor and a shp2 inhibitor
MX2019008696A (es) * 2017-01-23 2019-09-13 Revolution Medicines Inc Compuestos de piridina como inhibidores de shp2 alostericos.
MX2019008695A (es) 2017-01-23 2019-09-11 Revolution Medicines Inc Compuestos biciclicos como inhibidores alostericos de shp2.
KR20240026521A (ko) 2017-03-23 2024-02-28 자코바이오 파마슈티칼스 컴퍼니 리미티드 Shp2 억제제로서 유용한 신규한 헤테로환형 유도체
WO2018218133A1 (en) 2017-05-26 2018-11-29 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
EP3634953B1 (en) 2017-06-05 2024-01-03 PTC Therapeutics, Inc. Compounds for treating huntington's disease
CN111182898B (zh) 2017-06-28 2024-04-16 Ptc医疗公司 用于治疗亨廷顿氏病的方法
MX2019015580A (es) 2017-06-28 2020-07-28 Ptc Therapeutics Inc Metodos para tratar la enfermedad de huntington.
WO2019039390A1 (ja) * 2017-08-25 2019-02-28 国立大学法人名古屋大学 若年性骨髄単球性白血病治療薬
CA3074690A1 (en) 2017-09-07 2019-03-14 Revolution Medicines, Inc. Shp2 inhibitor compositions and methods for treating cancer
WO2019051469A1 (en) 2017-09-11 2019-03-14 Krouzon Pharmaceuticals, Inc. Octahydrocyclopenta[c]pyrrole allosteric inhibitors of shp2
EP3687997A1 (en) 2017-09-29 2020-08-05 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
MX2020003579A (es) * 2017-10-12 2020-07-22 Revolution Medicines Inc Compuestos de piridina, pirazina, y triazina como inhibidores de shp2 alostericos.
TWI697490B (zh) * 2017-12-06 2020-07-01 大陸商北京加科思新藥研發有限公司 用於作為shp2抑制劑之新穎雜環衍生物
BR112020009757A2 (pt) 2017-12-15 2020-11-03 Revolution Medicines, Inc. compostos policíclicos como inibidores alostéricos de shp2
KR102614939B1 (ko) 2018-02-13 2023-12-19 블루레이 테라퓨틱스 (상하이) 컴퍼니 리미티드 피리미딘-융합고리 화합물 및 그의 제조방법과 용도
NZ766835A (en) 2018-03-02 2023-09-29 Otsuka Pharma Co Ltd Pharmaceutical compounds
WO2019183364A1 (en) 2018-03-21 2019-09-26 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use thereof
SG11202009245TA (en) 2018-03-21 2020-10-29 Relay Therapeutics Inc 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
EA202092001A1 (ru) 2018-03-27 2021-01-29 ПиТиСи ТЕРАПЬЮТИКС, ИНК. Соединения для лечения болезни гентингтона
SG11202009793TA (en) 2018-04-10 2020-10-29 Revolution Medicines Inc Shp2 inhibitor compositions, methods for treating cancer and methods for identifying a subject with shp2 mutations
IL300091A (en) 2018-05-01 2023-03-01 Revolution Medicines Inc C40-, c28-, and c-32-linked rapamycin analogs as mtor inhibitors
KR102611661B1 (ko) 2018-05-02 2023-12-08 나비레 파르마, 인코퍼레이티드 Ptpn11의 치환된 헤테로사이클릭 억제제
HRP20240935T1 (hr) 2018-06-27 2024-11-22 Ptc Therapeutics, Inc. Heterociklični i heteroaril spojevi za liječenje huntingtonove bolesti
WO2020005877A1 (en) 2018-06-27 2020-01-02 Ptc Therapeutics, Inc. Heteroaryl compounds for treating huntington's disease
JP7174143B2 (ja) 2018-07-24 2022-11-17 大鵬薬品工業株式会社 Shp2活性を阻害するヘテロ二環性化合物
LT3833670T (lt) 2018-08-10 2024-06-25 Navire Pharma, Inc. 6-(4-amino-3-metil-2-oksa-8-azaspiro[4.5]dekan-8-il)-3-(2,3-dichlorfenil)-2-metilpirimidin-4(3h)-ono dariniai ir susiję junginiai kaip ptpn11 (shp2) inhibitoriai, skirti vėžiui gydyti
JP7542538B2 (ja) 2018-09-18 2024-08-30 ニカング セラピューティクス, インコーポレイテッド Srcホモロジー-2ホスファターゼ阻害剤としての縮合三環式環誘導体
CN112839935A (zh) 2018-09-26 2021-05-25 北京加科思新药研发有限公司 可用作shp2抑制剂的新型杂环衍生物
JP2022502385A (ja) 2018-09-29 2022-01-11 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の製造方法
CA3112322A1 (en) * 2018-09-29 2020-04-02 Novartis Ag Manufacture of compounds and compositions for inhibiting the activity of shp2
WO2020072656A1 (en) 2018-10-03 2020-04-09 Gilead Sciences, Inc. Imidozopyrimidine derivatives
CN113473990A (zh) 2018-10-08 2021-10-01 锐新医药公司 用于治疗癌症的shp2抑制剂组合物
US12187721B2 (en) 2018-10-17 2025-01-07 Array Biopharma Inc. Protein tyrosine phosphatase inhibitors
CN111153899B (zh) * 2018-11-08 2023-12-01 四川科伦博泰生物医药股份有限公司 一种取代吡啶化合物、其制备方法和用途
CN113164418A (zh) 2018-12-05 2021-07-23 米拉蒂治疗股份有限公司 组合疗法
CN113727758A (zh) 2019-03-01 2021-11-30 锐新医药公司 双环杂环基化合物及其用途
WO2020180768A1 (en) 2019-03-01 2020-09-10 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
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
CA3127361A1 (en) 2019-03-07 2020-09-10 Merck Patent Gmbh Carboxamide-pyrimidine derivatives as shp2 antagonists
WO2020201991A1 (en) * 2019-04-02 2020-10-08 Array Biopharma Inc. Protein tyrosine phosphatase inhibitors
CA3127475A1 (en) 2019-04-08 2020-10-15 Merck Patent Gmbh Pyrimidinone derivatives as shp2 antagonists
JP7649257B2 (ja) 2019-05-13 2025-03-19 ピーティーシー セラピューティクス, インコーポレイテッド ハンチントン病を処置するための化合物
TWI817018B (zh) 2019-06-28 2023-10-01 美商艾瑞生藥股份有限公司 用於治療braf相關的疾病和失調症之化合物
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
CN114127053B (zh) * 2019-09-06 2023-06-13 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
AU2020354475A1 (en) * 2019-09-24 2022-05-05 Relay Therapeutics, Inc. SHP2 phosphatase inhibitors and methods of making and using the same
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
MX2022005359A (es) 2019-11-04 2022-06-02 Revolution Medicines Inc Inhibidores de ras.
CN120699039A (zh) 2019-11-04 2025-09-26 锐新医药公司 Ras抑制剂
WO2021091956A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
TW202128688A (zh) 2019-11-08 2021-08-01 美商銳新醫藥公司 雙環雜芳基化合物及其用途
EP4065231A1 (en) 2019-11-27 2022-10-05 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
CN114929279A (zh) 2020-01-07 2022-08-19 锐新医药公司 Shp2抑制剂给药和治疗癌症的方法
WO2021171261A1 (en) 2020-02-28 2021-09-02 Novartis Ag A triple pharmaceutical combination comprising dabrafenib, an erk inhibitor and a shp2 inhibitor
WO2021247836A1 (en) 2020-06-03 2021-12-09 Board Of Regents, The University Of Texas System Methods for targeting shp-2 to overcome resistance
IL299131A (en) 2020-06-18 2023-02-01 Revolution Medicines Inc Methods for delaying, preventing and treating acquired resistance to RAS inhibitors
EP4169913A4 (en) * 2020-06-22 2024-10-30 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. SUBSTITUTED PYRAZINE COMPOUND, PHARMACEUTICAL COMPOSITION THEREOF AND USE THEREOF
CN115916786B (zh) 2020-07-08 2025-10-17 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
WO2022006780A1 (en) * 2020-07-08 2022-01-13 Novartis Ag Manufacture of compounds and compositions for inhibiting activity of shp2
MX2023002248A (es) 2020-09-03 2023-05-16 Revolution Medicines Inc Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2.
MX2023003060A (es) 2020-09-15 2023-04-05 Revolution Medicines Inc Derivados indolicos como inhibidores de ras en el tratamiento del cancer.
US20240051956A1 (en) 2020-12-22 2024-02-15 Qilu Regor Therapeutics Inc. Sos1 inhibitors and uses thereof
EP4039685A1 (en) 2021-02-08 2022-08-10 Irbm S.P.A. Azabicyclic shp2 inhibitors
TWI825637B (zh) 2021-03-31 2023-12-11 美商輝瑞股份有限公司 啶-1,6(2h,7h)-二酮
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
AU2022268962A1 (en) 2021-05-05 2023-12-14 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
CA3217084A1 (en) 2021-05-05 2022-11-10 Farbod Shojaei Combination therapies comprising shp2 inhibitors and pd-1 inhibitors
WO2022235866A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
CA3217393A1 (en) 2021-05-05 2022-11-10 Elena S. Koltun Ras inhibitors
IL308234A (en) 2021-05-05 2024-01-01 Huyabio Int Llc Monotherapy with an SHP2 inhibitor and its uses
TW202244049A (zh) * 2021-05-12 2022-11-16 大陸商藥雅科技(上海)有限公司 Shp2磷酸酶抑制劑的製備及其應用
CN115960109B (zh) * 2021-05-31 2024-06-25 药雅科技(上海)有限公司 稠环类shp2磷酸酶抑制剂的制备及其应用
AU2022289684A1 (en) 2021-06-09 2023-10-05 F. Hoffmann-La Roche Ag Combination of a particular braf inhibitor (paradox breaker) and a pd-1 axis binding antagonist for use in the treatment of cancer
WO2022259157A1 (en) 2021-06-09 2022-12-15 Novartis Ag A triple pharmaceutical combination comprising dabrafenib, trametinib and a shp2 inhibitor
BR112023025916A2 (pt) 2021-06-09 2024-02-27 Chugai Pharmaceutical Co Ltd Combinação de um inibidor de braf e um inibidor de mek, uso de uma combinação, método para o tratamento ou profilaxia de câncer, composições farmacêuticas e invenção
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
CA3224341A1 (en) 2021-09-01 2023-03-09 Novartis Ag Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
AU2022383040A1 (en) 2021-11-04 2024-03-07 F. Hoffmann-La Roche Ag Novel use of quinazolinone compound for the treatment of cancer
CN119136806A (zh) 2022-03-08 2024-12-13 锐新医药公司 用于治疗免疫难治性肺癌的方法
CN116903581B (zh) * 2022-04-14 2026-04-14 山东大学 Shp2/hdac双靶点抑制剂及其制备方法和应用
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
EP4345101A1 (en) 2022-09-29 2024-04-03 Irbm S.P.A. Azole derivatives as shp2 inhibitors
CN120359214A (zh) 2022-12-15 2025-07-22 豪夫迈·罗氏有限公司 用于癌症治疗的组合疗法
CN116332908B (zh) * 2023-03-21 2024-07-02 杭州医学院 一种shp2变构抑制剂及其制备方法和应用
EP4687905A1 (en) 2023-03-30 2026-02-11 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
KR20260005904A (ko) 2023-04-07 2026-01-12 레볼루션 메디슨즈, 인크. 매크로사이클릭 ras 억제제
CN121263418A (zh) 2023-04-07 2026-01-02 锐新医药公司 大环ras抑制剂
KR20250172857A (ko) 2023-04-14 2025-12-09 레볼루션 메디슨즈, 인크. Ras 억제제의 결정형
AU2024252105A1 (en) 2023-04-14 2025-10-16 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
WO2024218632A1 (en) 2023-04-17 2024-10-24 Array Biopharma Inc. Erk protein kinase inhibitors
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
IL326136A (en) 2023-08-07 2026-03-01 Revolution Medicines Inc RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein
WO2025034919A1 (en) 2023-08-08 2025-02-13 Quanta Therapeutics, Inc. Combination therapies with kras modulators
WO2025036475A1 (en) * 2023-08-17 2025-02-20 Jacobio Pharmaceuticals Co., Ltd. A pharmaceutical combination and use thereof
WO2025075693A1 (en) * 2023-10-02 2025-04-10 Purdue Research Foundation Shp2 degraders for cancer therapy
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025106901A1 (en) 2023-11-17 2025-05-22 Quanta Therapeutics, Inc. Combination cancer therapies with a kras modulator and an rtk-mapk pathway inhibitor
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
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025261943A1 (en) 2024-06-18 2025-12-26 F. Hoffmann-La Roche Ag Anti-cancer combinations comprising mosperafenib and folfox or folfiri
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
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
WO2026015790A1 (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
WO2026060400A1 (en) 2024-09-16 2026-03-19 Quanta Therapeutics, Inc. Combination therapies with kras modulators
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer
CN119798246B (zh) * 2024-12-20 2025-08-05 山东大学齐鲁医院 靶向shp2的荧光探针、制备方法及其应用

Family Cites Families (69)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH445129A (fr) 1964-04-29 1967-10-15 Nestle Sa Procédé pour la préparation de composés d'inclusion à poids moléculaire élevé
US3459731A (en) 1966-12-16 1969-08-05 Corn Products Co Cyclodextrin polyethers and their production
US3426011A (en) 1967-02-13 1969-02-04 Corn Products Co Cyclodextrins with anionic properties
US3453257A (en) 1967-02-13 1969-07-01 Corn Products Co Cyclodextrin with cationic properties
US3453259A (en) 1967-03-22 1969-07-01 Corn Products Co Cyclodextrin polyol ethers and their oxidation products
JPS6041077B2 (ja) 1976-09-06 1985-09-13 喜徳 喜谷 1,2‐ジアミノシクロヘキサン異性体のシス白金(2)錯体
US4235871A (en) 1978-02-24 1980-11-25 Papahadjopoulos Demetrios P Method of encapsulating biologically active materials in lipid vesicles
US4261989A (en) 1979-02-19 1981-04-14 Kaken Chemical Co. Ltd. Geldanamycin derivatives and antitumor drug
FR2567518B1 (fr) 1984-07-11 1987-11-13 Sanofi Sa Nouveaux composes a noyau heterocyclique azote, leur preparation et les medicaments qui en contiennent
US4737323A (en) 1986-02-13 1988-04-12 Liposome Technology, Inc. Liposome extrusion method
EP0257102B1 (en) * 1986-02-24 1997-11-19 Mitsui Petrochemical Industries, Ltd. Agents for treating neurophathy
US5266573A (en) 1989-08-07 1993-11-30 Elf Sanofi Trifluoromethylphenyltetrahydropyridines for the treatment and/or prophylaxis of intestinal motility disorders
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
DK169008B1 (da) 1990-06-01 1994-07-25 Holec Lk A S Fremgangsmåde og skærm til afskærmning af en strømtransformer samt strømtransformer med en sådan afskærmning
EP0647450A1 (en) 1993-09-09 1995-04-12 BEHRINGWERKE Aktiengesellschaft Improved prodrugs for enzyme mediated activation
IL115849A0 (en) 1994-11-03 1996-01-31 Merz & Co Gmbh & Co Tangential filtration preparation of liposomal drugs and liposome product thereof
AU4198400A (en) 1999-04-06 2000-10-23 Krenitsky Pharmaceuticals Inc. Neurotrophic thio substituted pyrimidines
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
GB0018891D0 (en) 2000-08-01 2000-09-20 Novartis Ag Organic compounds
JP4272338B2 (ja) 2000-09-22 2009-06-03 バイエル アクチェンゲゼルシャフト ピリジン誘導体
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
ATE407678T1 (de) 2001-10-17 2008-09-15 Boehringer Ingelheim Pharma Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung
JP4547911B2 (ja) 2002-02-01 2010-09-22 アリアド・ファーマシューティカルズ・インコーポレイテッド リン含有化合物およびその用途
US7375134B2 (en) 2002-03-05 2008-05-20 Axys Pharmaceuticals, Inc. Cathepsin cysteine protease inhibitors
TWI275390B (en) 2002-04-30 2007-03-11 Wyeth Corp Process for the preparation of 7-substituted-3- quinolinecarbonitriles
US7399865B2 (en) 2003-09-15 2008-07-15 Wyeth Protein tyrosine kinase enzyme inhibitors
CN1938296A (zh) 2004-04-01 2007-03-28 安斯泰来制药有限公司 作为腺苷拮抗剂的吡嗪衍生物及其制药用途
WO2005117909A2 (en) 2004-04-23 2005-12-15 Exelixis, Inc. Kinase modulators and methods of use
DK1789390T3 (da) 2004-09-02 2012-02-27 Genentech Inc Pyridyl-inhibitorer af hedgehog-signalering
US7904122B2 (en) 2004-09-30 2011-03-08 Lg Electronics Inc. Method of supporting operation of sleep mode in a wideband radio access system
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
US20090306038A1 (en) 2005-09-13 2009-12-10 Carceller Gonzalez Elena 2-Aminopyrimidine derivatives as modulators of the histamine H4 receptor activity
US7515405B2 (en) 2006-07-25 2009-04-07 Hewlett-Packard Development Company, L.P. Anti-rotation mechanism for an electronic device
WO2008031556A2 (en) * 2006-09-12 2008-03-20 Ucb Pharma, S.A. 2 amino-pyrimidine derivatives as h4 receptor antagonists, processes for preparing them and their use in pharmaceutical compositions
US20090137549A1 (en) 2006-11-09 2009-05-28 Paul John Edward Novel compounds useful for the treatment of degenerative & inflamatory diseases
AU2008210455A1 (en) * 2007-01-31 2008-08-07 Vertex Pharmaceuticals Incorporated 2-aminopyridine derivatives useful as kinase inhibitors
EP2120573A4 (en) 2007-02-12 2011-05-25 Merck Sharp & Dohme piperidine
PE20090188A1 (es) 2007-03-15 2009-03-20 Novartis Ag Compuestos heterociclicos como moduladores de la senda de hedgehog
AU2008298948B2 (en) 2007-09-12 2014-09-04 F. Hoffmann-La Roche Ag Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use
US8354528B2 (en) 2007-10-25 2013-01-15 Genentech, Inc. Process for making thienopyrimidine compounds
NZ588830A (en) 2008-04-22 2012-11-30 Portola Pharm Inc Inhibitors of protein kinases
AU2009256574A1 (en) 2008-06-13 2009-12-17 Novartis Ag 2,4'-bipyridinyl compounds as protein kinase D inhibitors useful for the treatment of IA heart failure and cancer
MX2010013876A (es) 2008-06-20 2011-03-04 Metabolex Inc Agonistas de arilo grpr119 y sus usos .
US8168784B2 (en) 2008-06-20 2012-05-01 Abbott Laboratories Processes to make apoptosis promoters
TWI546290B (zh) 2008-06-27 2016-08-21 賽基艾維洛米斯研究股份有限公司 雜芳基化合物及其用途
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
KR20170015566A (ko) * 2008-11-10 2017-02-08 버텍스 파마슈티칼스 인코포레이티드 Atr 키나제의 억제제로서 유용한 화합물
WO2010067987A2 (ko) 2008-12-10 2010-06-17 동화약품주식회사 신규한 2, 6-위치에 치환된 3-니트로피리딘 유도체, 그의 제조방법 및 이를 포함하는 약학 조성물
FR2941696B1 (fr) 2009-02-05 2011-04-15 Sanofi Aventis Derives d'azaspiranyl-alkylcarbamates d'heterocycles a 5 chainons, leur preparation et leur application en therapeutique
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
KR101906146B1 (ko) * 2009-08-17 2018-10-10 메모리얼 슬로안-케터링 캔서 센터 열 충격 단백질 결합 화합물, 조성물, 및 이의 제조 방법 및 사용 방법
WO2011078143A1 (ja) 2009-12-22 2011-06-30 塩野義製薬株式会社 ピリミジン誘導体およびそれらを含有する医薬組成物
WO2012002577A1 (ja) 2010-06-30 2012-01-05 富士フイルム株式会社 新規なニコチンアミド誘導体またはその塩
JP2013531037A (ja) 2010-07-13 2013-08-01 メルク・シャープ・エンド・ドーム・コーポレイション スピロ環式化合物
BR112013002112B1 (pt) 2010-07-29 2021-04-06 Rigel Pharmaceuticals, Inc. Composto, composição farmacêutica, e, uso de um composto, ou de um respectivo sal farmaceuticamente aceitável, ou de uma composição
US8609672B2 (en) * 2010-08-27 2013-12-17 University Of The Pacific Piperazinylpyrimidine analogues as protein kinase inhibitors
JP5802756B2 (ja) 2010-10-20 2015-11-04 ファイザー・インク スムーズンド受容体モジュレーターとしてのピリジン−2−誘導体
CN103930407B (zh) 2011-09-12 2019-02-26 默克专利有限公司 用作激酶活性调节剂的氨基嘧啶衍生物
WO2013096093A1 (en) 2011-12-21 2013-06-27 Merck Sharp & Dohme Corp. Compounds as dgat-1 inhibitors
CN104540830A (zh) 2012-06-07 2015-04-22 霍夫曼-拉罗奇有限公司 端锚聚合酶的吡唑并嘧啶酮和吡唑并吡啶酮抑制剂
EP2903985A1 (en) 2012-10-03 2015-08-12 Advinus Therapeutics Limited Spirocyclic compounds, compositions and medicinal applications thereof
WO2014160521A1 (en) * 2013-03-15 2014-10-02 Blueprint Medicines Corporation Piperazine derivatives and their use as kit modulators
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
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
SI3137169T1 (sl) 2014-05-01 2022-04-29 Celgene Quanticel Research, Inc. Inhibitorji lizin specifične demetilaze-1
US10174032B2 (en) 2014-05-05 2019-01-08 Signalrx Pharmaceuticals, Inc. Heterocyclic compound classes for signaling modulation
ES2824576T3 (es) 2015-06-19 2021-05-12 Novartis Ag Compuestos y composiciones para inhibir la actividad de SHP2
CN112625028B (zh) 2015-06-19 2024-10-29 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
ES2741746T3 (es) 2015-06-19 2020-02-12 Novartis Ag Compuestos y composiciones para inhibir la actividad de SHP2

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021130662A (ja) * 2015-06-19 2021-09-09 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
JP7146016B2 (ja) 2015-06-19 2022-10-03 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

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