JP6718889B2 - Shp2の活性を阻害するための化合物および組成物 - Google Patents
Shp2の活性を阻害するための化合物および組成物 Download PDFInfo
- Publication number
- JP6718889B2 JP6718889B2 JP2017565777A JP2017565777A JP6718889B2 JP 6718889 B2 JP6718889 B2 JP 6718889B2 JP 2017565777 A JP2017565777 A JP 2017565777A JP 2017565777 A JP2017565777 A JP 2017565777A JP 6718889 B2 JP6718889 B2 JP 6718889B2
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- amino
- hydrogen
- mmol
- fluoro
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/14—Heterocyclic 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/02—Heterocyclic 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
- C07D401/04—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic 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
- C07D471/02—Heterocyclic 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
- C07D471/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic 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
- C07D491/02—Heterocyclic 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
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Oncology (AREA)
- Psychiatry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562181893P | 2015-06-19 | 2015-06-19 | |
| US62/181,893 | 2015-06-19 | ||
| PCT/IB2016/053550 WO2016203406A1 (en) | 2015-06-19 | 2016-06-15 | Compounds and compositions for inhibiting the activity of shp2 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018517752A JP2018517752A (ja) | 2018-07-05 |
| JP2018517752A5 JP2018517752A5 (enExample) | 2019-07-18 |
| JP6718889B2 true JP6718889B2 (ja) | 2020-07-08 |
Family
ID=56194530
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017565777A Active JP6718889B2 (ja) | 2015-06-19 | 2016-06-15 | Shp2の活性を阻害するための化合物および組成物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US10287266B2 (enExample) |
| EP (1) | EP3310774B1 (enExample) |
| JP (1) | JP6718889B2 (enExample) |
| CN (2) | CN107922388B (enExample) |
| ES (1) | ES2805232T3 (enExample) |
| WO (1) | WO2016203406A1 (enExample) |
Cited By (1)
| 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 (120)
| 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 |
| 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 |
| 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 |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| US10287266B2 (en) * | 2015-06-19 | 2019-05-14 | 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| IL276232B2 (en) | 2018-03-02 | 2024-04-01 | Otsuka Pharma Co Ltd | Pyrazine derivatives, pharmaceutical compositions comprising them and their use for treating diseases |
| 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. |
| 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. |
| MX2020011528A (es) | 2018-05-02 | 2021-02-09 | Navire Pharma Inc | Inhibidores heterociclicos sustituidos de ptpn11. |
| CN110143949A (zh) * | 2018-05-09 | 2019-08-20 | 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 |
| MX2021000795A (es) | 2018-07-24 | 2021-04-12 | Taiho Pharmaceutical Co Ltd | Compuestos heterociclicos para inhibir la actividad de shp2. |
| 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 |
| IL305106B2 (en) | 2018-09-29 | 2025-08-01 | Novartis Ag | Process of manufacture of a compound for inhibiting the activity of shp2 |
| 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 |
| CN117143079A (zh) | 2018-11-06 | 2023-12-01 | 上海奕拓医药科技有限责任公司 | 一种螺芳环化合物及其应用 |
| 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 |
| MX2021002804A (es) | 2018-12-05 | 2021-07-15 | Mirati Therapeutics Inc | Terapias de combinacion. |
| 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 |
| WO2020156243A1 (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 |
| US20220152026A1 (en) * | 2019-02-12 | 2022-05-19 | Novartis Ag | Pharmaceutical combination comprising tno155 and a krasg12c inhibitor |
| MX2021010319A (es) | 2019-03-01 | 2021-12-10 | Revolution Medicines Inc | Compuestos biciclicos de heteroarilo y usos de estos. |
| MX2021010323A (es) | 2019-03-01 | 2021-12-10 | Revolution Medicines Inc | Compuestos bicíclicos de heterociclilo y usos de este. |
| 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 |
| 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 |
| AU2020328598A1 (en) | 2019-08-15 | 2022-03-03 | Black Diamond Therapeutics, Inc. | Alkynyl quinazoline compounds |
| GB201911928D0 (en) | 2019-08-20 | 2019-10-02 | Otsuka Pharma Co Ltd | Pharmaceutical compounds |
| 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. |
| 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 |
| AU2020377925A1 (en) | 2019-11-04 | 2022-05-05 | 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 |
| 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 |
| WO2021142026A1 (en) | 2020-01-07 | 2021-07-15 | Revolution Medicines, Inc. | Shp2 inhibitor dosing and methods of treating cancer |
| 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 |
| CN113754683A (zh) | 2020-06-05 | 2021-12-07 | 上海奕拓医药科技有限责任公司 | 同位素取代的螺芳环化合物及其应用 |
| 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 |
| CN114195799B (zh) * | 2020-09-02 | 2025-01-28 | 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 |
| 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 |
| CN116348466B (zh) * | 2020-09-23 | 2025-05-30 | 上海齐鲁制药研究中心有限公司 | 吡嗪硫联苯基类化合物及其应用 |
| CN112062699B (zh) * | 2020-11-13 | 2021-02-26 | 苏州开元民生科技股份有限公司 | 一种邻氨基苯硫酚的制备方法 |
| 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 |
| CN113376301B (zh) * | 2020-12-25 | 2022-11-15 | 上海药坦药物研究开发有限公司 | 一种2-氨基-3-氯吡啶-4-硫醇钠的检测方法 |
| US20240190843A1 (en) * | 2021-04-01 | 2024-06-13 | Array Biopharma Inc. | Crystalline form of a shp2 inhibitor |
| IL308222A (en) | 2021-05-05 | 2024-01-01 | Huyabio Int Llc | Combination therapies that include SHP2 inhibitors and PD-1 inhibitors |
| JP2024516450A (ja) | 2021-05-05 | 2024-04-15 | レボリューション メディシンズ インコーポレイテッド | 共有結合性ras阻害剤及びその使用 |
| TW202309052A (zh) | 2021-05-05 | 2023-03-01 | 美商銳新醫藥公司 | Ras抑制劑 |
| 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 |
| KR20240017811A (ko) | 2021-05-05 | 2024-02-08 | 레볼루션 메디슨즈, 인크. | 암의 치료를 위한 ras 억제제 |
| 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 |
| WO2023280237A1 (zh) * | 2021-07-07 | 2023-01-12 | 海创药业股份有限公司 | 一种磷酸酶降解剂的合成和应用 |
| KR20240055778A (ko) | 2021-09-01 | 2024-04-29 | 노파르티스 아게 | Tead 억제제를 포함하는 제약 조합물 및 암의 치료를 위한 이의 용도 |
| CN118019537A (zh) * | 2021-09-28 | 2024-05-10 | 上海翰森生物医药科技有限公司 | Shp2抑制剂联合egfr-tki治疗和预防肿瘤疾病的医药用途 |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| CN116063307B (zh) | 2021-10-29 | 2025-08-19 | 中国药科大学 | Shp2与cdk4/6双靶点抑制化合物合成及其制备方法与应用 |
| 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 |
| WO2023240263A1 (en) | 2022-06-10 | 2023-12-14 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| 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 |
| CR20250420A (es) | 2023-04-07 | 2025-11-20 | Revolution Medicines Inc | Inhibidores macrocíclicos de ras |
| AR132338A1 (es) | 2023-04-07 | 2025-06-18 | Revolution Medicines Inc | Inhibidores de ras |
| CN121100123A (zh) | 2023-04-14 | 2025-12-09 | 锐新医药公司 | Ras抑制剂的结晶形式 |
| 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 |
| 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 |
| AU2024321817A1 (en) | 2023-08-08 | 2026-03-05 | Quanta Therapeutics, Inc. | Combination therapies with kras modulators |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic 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 |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ras抑制劑 |
| WO2025242126A1 (zh) * | 2024-05-22 | 2025-11-27 | 上海正大天晴医药科技开发有限公司 | 一种药物组合及其应用 |
| 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 |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| 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 |
| 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 |
| CN119039223B (zh) * | 2024-10-31 | 2025-02-25 | 江苏豪森药业集团有限公司 | 一种含氮杂芳类衍生物的制备方法及其中间体 |
| 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 (66)
| 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 |
| US3453257A (en) | 1967-02-13 | 1969-07-01 | Corn Products Co | Cyclodextrin with cationic properties |
| US3426011A (en) | 1967-02-13 | 1969-02-04 | Corn Products Co | Cyclodextrins with anionic 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 |
| WO1987004928A1 (fr) | 1986-02-24 | 1987-08-27 | Mitsui Petrochemical Industries, Ltd. | Agents therapeutiques de la neuropathie |
| 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 |
| PT1478648E (pt) | 2002-02-01 | 2014-07-15 | Ariad Pharma Inc | Compostos contendo fósforo e suas utilizações |
| CN100430052C (zh) | 2002-03-05 | 2008-11-05 | 默克弗罗斯特加拿大有限公司 | 组织蛋白酶半胱氨酸蛋白酶抑制剂 |
| TWI275390B (en) | 2002-04-30 | 2007-03-11 | Wyeth Corp | Process for the preparation of 7-substituted-3- quinolinecarbonitriles |
| AU2004218228A1 (en) | 2003-03-07 | 2004-09-16 | Merck Sharp & Dohme Limited | Tetrahydropyran compounds as tachykinin antagonists |
| US7399865B2 (en) | 2003-09-15 | 2008-07-15 | Wyeth | Protein tyrosine kinase enzyme inhibitors |
| WO2005095384A1 (en) | 2004-04-01 | 2005-10-13 | Astellas Pharma Inc. | Pyrazine derivatives and pharmaceutical use thereof as adenosine antagonists |
| WO2005117909A2 (en) | 2004-04-23 | 2005-12-15 | Exelixis, Inc. | Kinase modulators and methods of use |
| ES2377430T3 (es) | 2004-09-02 | 2012-03-27 | Genentech, Inc. | Inhibidores piridílicos de la señalización de hedgehog |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| CA2622372A1 (en) | 2005-09-13 | 2007-03-22 | Palau Pharma, S.A. | 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 |
| US20090137549A1 (en) | 2006-11-09 | 2009-05-28 | Paul John Edward | Novel compounds useful for the treatment of degenerative & inflamatory diseases |
| US8252803B2 (en) | 2007-02-12 | 2012-08-28 | Merck Sharp & Dohme Corp. | Piperidine derivatives |
| CA2681162C (en) | 2007-03-15 | 2015-11-24 | Novartis Ag | Benzyl and pyridine derivatives as modulators of hedgehog pathway |
| EP2205242B1 (en) | 2007-09-12 | 2015-04-15 | Genentech, Inc. | Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use |
| JP5348725B2 (ja) | 2007-10-25 | 2013-11-20 | ジェネンテック, インコーポレイテッド | チエノピリミジン化合物の製造方法 |
| AU2009238590A1 (en) | 2008-04-22 | 2009-10-29 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| JP2011522865A (ja) | 2008-06-13 | 2011-08-04 | ノバルティス アーゲー | Ia心不全および癌の治療に有用なプロテインキナーゼd阻害剤としての2,4’−ビピリジニル化合物 |
| US8168784B2 (en) | 2008-06-20 | 2012-05-01 | Abbott Laboratories | Processes to make apoptosis promoters |
| CA2727174A1 (en) | 2008-06-20 | 2010-01-21 | Jiangao Song | Aryl gpr119 agonists and uses thereof |
| NZ603525A (en) | 2008-06-27 | 2015-02-27 | Celgene Avilomics Res Inc | Pyrimidine based compound and uses thereof |
| WO2010048149A2 (en) | 2008-10-20 | 2010-04-29 | Kalypsys, Inc. | Heterocyclic modulators of gpr119 for treatment of disease |
| CN102356066A (zh) | 2008-12-10 | 2012-02-15 | 同和药品株式会社 | 新型2,6-取代的-3-硝基吡啶衍生物、其制备方法及包含有其的药物组合物 |
| 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 |
| 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 |
| ES2689103T3 (es) | 2010-06-30 | 2018-11-08 | Fujifilm Corporation | Nuevo derivado de nicotinamida o sal del mismo |
| 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 |
| PE20130774A1 (es) | 2010-07-29 | 2013-06-26 | Rigel Pharmaceuticals Inc | Compuestos heterociclicos activadores de ampk y metodos para emplearlos |
| US8609672B2 (en) | 2010-08-27 | 2013-12-17 | University Of The Pacific | Piperazinylpyrimidine analogues as protein kinase inhibitors |
| CA2813162C (en) | 2010-10-20 | 2015-06-16 | Pfizer Inc. | Pyridine-2- derivatives as smoothened receptor modulators |
| US9321760B2 (en) | 2011-09-12 | 2016-04-26 | Merck Patent Gmbh | Aminopyrimidine derivatives for use as modulators of kinase activity |
| 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 |
| JP6099753B2 (ja) | 2012-10-03 | 2017-03-22 | アドビナス セラピューティクス リミテッド | スピロ環化合物、その組成物及びその医薬応用 |
| WO2014160521A1 (en) | 2013-03-15 | 2014-10-02 | Blueprint Medicines Corporation | Piperazine derivatives and their use as kit modulators |
| 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 |
| 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 |
| JO3517B1 (ar) * | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| KR102400920B1 (ko) | 2014-05-01 | 2022-05-20 | 셀젠 콴티셀 리서치, 인크. | 리신 특이적 데메틸라제-1의 억제제 |
| US10174032B2 (en) | 2014-05-05 | 2019-01-08 | Signalrx Pharmaceuticals, Inc. | Heterocyclic compound classes for signaling modulation |
| WO2016203405A1 (en) | 2015-06-19 | 2016-12-22 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| US10287266B2 (en) * | 2015-06-19 | 2019-05-14 | 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 |
-
2016
- 2016-06-15 US US15/736,925 patent/US10287266B2/en active Active
- 2016-06-15 CN CN201680035707.3A patent/CN107922388B/zh active Active
- 2016-06-15 CN CN202011428718.2A patent/CN112625028B/zh active Active
- 2016-06-15 WO PCT/IB2016/053550 patent/WO2016203406A1/en not_active Ceased
- 2016-06-15 EP EP16731666.0A patent/EP3310774B1/en active Active
- 2016-06-15 ES ES16731666T patent/ES2805232T3/es active Active
- 2016-06-15 JP JP2017565777A patent/JP6718889B2/ja active Active
Cited By (2)
| 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 |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2018517752A (ja) | 2018-07-05 |
| US10287266B2 (en) | 2019-05-14 |
| EP3310774A1 (en) | 2018-04-25 |
| CN107922388A (zh) | 2018-04-17 |
| WO2016203406A1 (en) | 2016-12-22 |
| EP3310774B1 (en) | 2020-04-29 |
| US20180186770A1 (en) | 2018-07-05 |
| CN107922388B (zh) | 2020-12-29 |
| CN112625028B (zh) | 2024-10-29 |
| ES2805232T3 (es) | 2021-02-11 |
| CN112625028A (zh) | 2021-04-09 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP7146016B2 (ja) | Shp2の活性を阻害するための化合物および組成物 | |
| JP6718889B2 (ja) | Shp2の活性を阻害するための化合物および組成物 | |
| JP7278359B2 (ja) | Shp2の活性を阻害するための化合物および組成物 | |
| JP6523303B2 (ja) | 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 | |
| JP6473457B2 (ja) | 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 | |
| JP6534389B2 (ja) | Shp2の活性を阻害するためのn−アザスピロシクロアルカン置換n−ヘテロアリール化合物および組成物 | |
| BR112018075663B1 (pt) | Compostos para inibição da atividade de shp2, seu uso, e composição farmacêutica |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20190613 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20190613 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20200423 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20200519 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20200615 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 6718889 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |