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 PDFInfo
- Publication number
- 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
- Authority
- JP
- Japan
- Prior art keywords
- amino
- mmol
- alkyl
- halo
- hydrogen
- 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
- C07D401/02—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic 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
- C07D241/14—Heterocyclic 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
- C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
- C07D249/10—1,2,4-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
- C07D249/14—Nitrogen atoms
-
- 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017502994A JP2017502994A (ja) | 2017-01-26 |
| JP2017502994A5 JP2017502994A5 (OSRAM) | 2018-02-22 |
| JP6473457B2 true JP6473457B2 (ja) | 2019-02-20 |
Family
ID=52462362
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016546924A Active JP6473457B2 (ja) | 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 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US9815813B2 (OSRAM) |
| EP (1) | EP3094629B1 (OSRAM) |
| JP (1) | JP6473457B2 (OSRAM) |
| CN (1) | CN105899493B (OSRAM) |
| ES (1) | ES2699354T3 (OSRAM) |
| WO (1) | WO2015107494A1 (OSRAM) |
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 (118)
| 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 |
| EP3094627B1 (en) | 2014-01-17 | 2018-08-22 | Novartis AG | 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2 |
| GB201416351D0 (en) * | 2014-09-16 | 2014-10-29 | Shire Internat Gmbh | Heterocyclic derivatives |
| WO2016203404A1 (en) | 2015-06-19 | 2016-12-22 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| EP3310774B1 (en) * | 2015-06-19 | 2020-04-29 | Novartis AG | Compounds and compositions for inhibiting the activity of shp2 |
| MX382671B (es) | 2015-12-10 | 2025-03-13 | Ptc Therapeutics Inc | Compuestos para usarse en el tratamiento o mejoramiento de la enfermedad de huntington |
| JP7044375B2 (ja) | 2016-05-31 | 2022-03-30 | ボード オブ リージェンツ，ザ ユニバーシティ オブ テキサス システム | Ｐｔｐｎ１１の複素環式阻害剤 |
| HUE057838T2 (hu) * | 2016-06-07 | 2022-06-28 | Jacobio Pharmaceuticals Co Ltd | SHP2 inhibitorokként hasznos új heterociklusos származékok |
| RU2744988C2 (ru) * | 2016-06-14 | 2021-03-17 | Новартис Аг | Соединения и композиции для подавления активности shp2 |
| PE20190624A1 (es) * | 2016-07-12 | 2019-04-26 | Revolution Medicines Inc | 3-metil pirazinas 2,5-disustituidas y 3-metil pirazinas 2,5,6-trisustituidas como inhibidores alostericos de shp2 |
| WO2018057884A1 (en) | 2016-09-22 | 2018-03-29 | Relay Therapeutics, Inc. | Shp2 phosphatase inhibitors and methods of use thereof |
| TWI848901B (zh) | 2016-10-24 | 2024-07-21 | 美商傳達治療有限公司 | Shp2磷酸酶抑制劑及其使用方法 |
| ES2964956T3 (es) | 2017-01-10 | 2024-04-10 | Novartis Ag | Combinación farmacéutica que comprende un inhibidor de ALK y un inhibidor de SHP2 |
| CN117327075A (zh) | 2017-01-23 | 2024-01-02 | 锐新医药公司 | 作为变构shp2抑制剂的二环化合物 |
| EP3571189B1 (en) * | 2017-01-23 | 2023-03-29 | Revolution Medicines, Inc. | Pyridine compounds as allosteric shp2 inhibitors |
| TWI664175B (zh) * | 2017-03-23 | 2019-07-01 | 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 |
| US11591336B2 (en) | 2017-05-26 | 2023-02-28 | D. E. Shaw Research, Llc | Substituted pyrazolo[3,4-b]pyrazines as SHP2 phosphatase inhibitors |
| JP7376471B2 (ja) | 2017-06-05 | 2023-11-08 | 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 |
| MX2019015580A (es) | 2017-06-28 | 2020-07-28 | Ptc Therapeutics Inc | Metodos para tratar la enfermedad de huntington. |
| MX2019015578A (es) | 2017-06-28 | 2020-07-28 | Ptc Therapeutics Inc | Metodos para tratar la enfermedad de huntington. |
| JPWO2019039390A1 (ja) * | 2017-08-25 | 2020-07-30 | 国立大学法人東海国立大学機構 | 若年性骨髄単球性白血病治療薬 |
| KR20200051684A (ko) | 2017-09-07 | 2020-05-13 | 레볼루션 메디슨즈, 인크. | 암 치료를 위한 shp2 억제제 조성물 및 방법 |
| WO2019051469A1 (en) | 2017-09-11 | 2019-03-14 | Krouzon Pharmaceuticals, Inc. | Octahydrocyclopenta[c]pyrrole allosteric inhibitors of shp2 |
| US11701354B2 (en) | 2017-09-29 | 2023-07-18 | D. E. Shaw Research, Llc | Pyrazolo[3,4-b]pyrazine derivatives as SHP2 phosphatase inhibitors |
| AU2018347516A1 (en) * | 2017-10-12 | 2020-05-07 | Revolution Medicines, Inc. | Pyridine, pyrazine, and triazine compounds as allosteric SHP2 inhibitors |
| 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 |
| EP3724189B1 (en) | 2017-12-15 | 2023-10-04 | Revolution Medicines, Inc. | Polycyclic compounds as allosteric shp2 inhibitors |
| KR102614939B1 (ko) | 2018-02-13 | 2023-12-19 | 블루레이 테라퓨틱스 (상하이) 컴퍼니 리미티드 | 피리미딘-융합고리 화합물 및 그의 제조방법과 용도 |
| AU2019226480B2 (en) | 2018-03-02 | 2022-12-15 | Otsuka Pharmaceutical Co., Ltd. | Pharmaceutical compounds |
| CN112368272B (zh) | 2018-03-21 | 2023-04-21 | 苏州浦合医药科技有限公司 | Shp2抑制剂及其用途 |
| EP4506035A3 (en) | 2018-03-21 | 2025-04-16 | Relay Therapeutics, Inc. | Shp2 phosphatase inhibitors and methods of use thereof |
| EP3768680A1 (en) | 2018-03-21 | 2021-01-27 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use thereof |
| JP7399870B2 (ja) | 2018-03-27 | 2023-12-18 | 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 |
| IL277783B2 (en) | 2018-04-10 | 2024-07-01 | Revolution Medicines Inc | Shp2 inhibitor compositions, methods for treating cancer and methods for identifying a subject with shp2 mutations |
| FI3788049T3 (fi) | 2018-05-01 | 2023-05-30 | Revolution Medicines Inc | C40-, c28- ja c-32-liittyneitä rapamysiinianalogeja mtor-estäjinä |
| AU2019263294B2 (en) | 2018-05-02 | 2024-03-21 | Navire Pharma, Inc. | Substituted heterocyclic inhibitors of PTPN11 |
| LT3814357T (lt) | 2018-06-27 | 2024-06-25 | Ptc Therapeutics, Inc. | Heterocikliniai ir heteroarilų junginiai, skirti hantingtono ligos gydymui |
| EA202092899A1 (ru) | 2018-06-27 | 2021-05-14 | ПиТиСи ТЕРАПЬЮТИКС, ИНК. | Гетероарильные соединения для лечения болезни гентингтона |
| EP3827009A4 (en) | 2018-07-24 | 2022-04-27 | Taiho Pharmaceutical Co., Ltd. | HETEROBICYCLIC COMPOUNDS TO INHIBIT SHP2 ACTIVITY |
| PE20211050A1 (es) | 2018-08-10 | 2021-06-04 | Navire Pharma Inc | Inhibidores de ptpn11 |
| CA3113234A1 (en) | 2018-09-18 | 2020-03-26 | Nikang Therapeutics, Inc. | Tri-substituted heteroaryl derivatives as src homology-2 phosphatase inhibitors |
| 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 |
| IL281726B2 (en) | 2018-09-29 | 2024-03-01 | Novartis Ag | Manufacture of compounds and compositions for inhibiting the activity of shp2 |
| BR112021005606A2 (pt) * | 2018-09-29 | 2021-06-22 | Novartis Ag | processo de produção de um composto para inibir a atividade de shp2 |
| EP3860717A1 (en) | 2018-10-03 | 2021-08-11 | Gilead Sciences, Inc. | Imidozopyrimidine derivatives |
| WO2020076723A1 (en) | 2018-10-08 | 2020-04-16 | Revolution Medicines, Inc. | Shp2 inhibitor compositions for use in treating cancer |
| ES2947464T3 (es) | 2018-10-17 | 2023-08-09 | Array Biopharma Inc | Inhibidores de la proteína tirosina fosfatasa |
| 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 |
| JP2022509724A (ja) | 2018-12-05 | 2022-01-24 | ミラティ セラピューティクス， インコーポレイテッド | 組み合わせ療法 |
| KR20210146288A (ko) | 2019-03-01 | 2021-12-03 | 레볼루션 메디슨즈, 인크. | 이환식 헤테로사이클릴 화합물 및 이의 용도 |
| US20230148450A9 (en) | 2019-03-01 | 2023-05-11 | 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 |
| JP7284830B2 (ja) | 2019-04-02 | 2023-05-31 | アレイ バイオファーマ インコーポレイテッド | タンパク質チロシンホスファターゼ阻害剤 |
| EP3952998A1 (en) | 2019-04-08 | 2022-02-16 | Merck Patent GmbH | Pyrimidinone derivatives as shp2 antagonists |
| 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 |
| 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 |
| 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 |
| CR20220241A (es) | 2019-11-04 | 2022-08-03 | Revolution Medicines Inc | Inhibidores de ras |
| BR112022008535A2 (pt) | 2019-11-04 | 2022-08-09 | Revolution Medicines Inc | Composto, composição farmacêutica, métodos para tratar câncer e um distúrbio relativo à proteína ras |
| US11739074B2 (en) | 2019-11-04 | 2023-08-29 | Revolution Medicines, Inc. | Ras inhibitors |
| BR112022008858A2 (pt) | 2019-11-08 | 2022-09-06 | Revolution Medicines Inc | Composto, composição farmacêutica e métodos para inibir sos1 em um sujeito, para inibir a interação de sos1 e uma proteína, para tratar ou prevenir uma doença e para tratar ou prevenir câncer |
| CN114980976A (zh) | 2019-11-27 | 2022-08-30 | 锐新医药公司 | 共价ras抑制剂及其用途 |
| IL294484A (en) | 2020-01-07 | 2022-09-01 | 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 |
| WO2021247836A1 (en) | 2020-06-03 | 2021-12-09 | Board Of Regents, The University Of Texas System | Methods for targeting shp-2 to overcome resistance |
| EP4168002A1 (en) | 2020-06-18 | 2023-04-26 | Revolution Medicines, Inc. | Methods for delaying, preventing, and treating acquired resistance to ras inhibitors |
| US20230212180A1 (en) * | 2020-06-22 | 2023-07-06 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | Substituted pyrazine compound, pharmaceutical composition comprising same, and use thereof |
| KR20230038197A (ko) | 2020-07-08 | 2023-03-17 | 노파르티스 아게 | Shp2의 활성 억제를 위한 화합물 및 조성물의 제조 |
| WO2022006780A1 (en) * | 2020-07-08 | 2022-01-13 | Novartis Ag | Manufacture of compounds and compositions for inhibiting activity of shp2 |
| IL301062A (en) | 2020-09-03 | 2023-05-01 | Revolution Medicines Inc | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| US11690915B2 (en) | 2020-09-15 | 2023-07-04 | Revolution Medicines, Inc. | Ras inhibitors |
| CA3203111A1 (en) | 2020-12-22 | 2022-06-30 | Kailiang Wang | 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 |
| US12390469B2 (en) | 2021-05-05 | 2025-08-19 | Huyabio International, Llc | SHP2 inhibitor monotherapy and uses thereof |
| IL308193A (en) | 2021-05-05 | 2024-01-01 | Revolution Medicines Inc | RAS inhibitors |
| EP4334324A1 (en) | 2021-05-05 | 2024-03-13 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| EP4334318A4 (en) | 2021-05-05 | 2025-03-05 | Huyabio International, LLC | COMBINATION THERAPIES WITH SHP2 INHIBITORS AND PD-1 INHIBITORS |
| EP4334325A1 (en) | 2021-05-05 | 2024-03-13 | Revolution Medicines, Inc. | Ras inhibitors for the treatment of cancer |
| 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 |
| 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 |
| TW202313041A (zh) | 2021-06-09 | 2023-04-01 | 瑞士商諾華公司 | 包含達拉菲尼、曲美替尼和shp2抑制劑之三重藥物組合 |
| CA3216220A1 (en) | 2021-06-09 | 2022-12-15 | 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 |
| MX2023014565A (es) | 2021-06-09 | 2024-02-08 | Chugai Pharmaceutical Co Ltd | Tratamiento conjunto para tratamiento contra el cancer. |
| 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 |
| TW202327569A (zh) | 2021-09-01 | 2023-07-16 | 瑞士商諾華公司 | 包含ｔｅａｄ抑制劑的藥物組合及其用於癌症治療之用途 |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| CA3230652A1 (en) | 2021-11-04 | 2023-05-11 | 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 |
| CN116903581A (zh) * | 2022-04-14 | 2023-10-20 | 山东大学 | Shp2/hdac双靶点抑制剂及其制备方法和应用 |
| EP4536364A1 (en) | 2022-06-10 | 2025-04-16 | 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 |
| TW202504611A (zh) | 2023-03-30 | 2025-02-01 | 美商銳新醫藥公司 | 用於誘導ｒａｓ ｇｔｐ水解之組合物及其用途 |
| AU2024243852A1 (en) | 2023-04-07 | 2025-11-06 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| AR132338A1 (es) | 2023-04-07 | 2025-06-18 | Revolution Medicines Inc | Inhibidores de ras |
| TW202448897A (zh) | 2023-04-14 | 2024-12-16 | 美商銳新醫藥公司 | Ｒａｓ抑制劑之結晶形式、含有其之組合物及其使用方法 |
| CN121100123A (zh) | 2023-04-14 | 2025-12-09 | 锐新医药公司 | Ras抑制剂的结晶形式 |
| WO2024218632A1 (en) | 2023-04-17 | 2024-10-24 | Array Biopharma Inc. | Erk protein kinase inhibitors |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| 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 |
| WO2025137507A1 (en) | 2023-12-22 | 2025-06-26 | Regor Pharmaceuticals, Inc. | Sos1 inhibitors and uses thereof |
| 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 |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| 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)
| 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 |
| US4959368A (en) * | 1986-02-24 | 1990-09-25 | Mitsui Petrochemical Industries Ltd. | Therapeutic agent for neurological diseases |
| 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 |
| WO2000059893A1 (en) | 1999-04-06 | 2000-10-12 | 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 |
| PT1438053E (pt) | 2001-10-17 | 2008-09-25 | Boehringer Ingelheim Int | Derivados de pirimidina, medicamento contendo estes compostos, sua utilização e processo para a sua preparação |
| CN101717410B (zh) | 2002-02-01 | 2015-04-29 | 阿里亚德医药股份有限公司 | 含磷化合物及其应用 |
| ATE395911T1 (de) | 2002-03-05 | 2008-06-15 | Merck Frosst Canada Ltd | Cathepsin-cystein-protease-hemmer |
| 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 |
| JP4978192B2 (ja) | 2004-04-01 | 2012-07-18 | アステラス製薬株式会社 | ピラジン誘導体およびその医薬的使用 |
| US8076338B2 (en) * | 2004-04-23 | 2011-12-13 | Exelixis, Inc. | Kinase modulators and methods of use |
| EP1789390B1 (en) | 2004-09-02 | 2011-11-09 | Genentech, Inc. | Pyridyl inhibitors of hedgehog signalling |
| BRPI0516319A (pt) | 2004-09-30 | 2008-09-02 | Lg Eletroctronics Inc | método de suporte da operação em modo de descanso em um sistema de acesso de rádio de banda larga |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| AU2006290715A1 (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 |
| EP2066645A2 (en) * | 2006-09-12 | 2009-06-10 | UCB Pharma S.A. | 2 amino-pyrimidine derivatives as h4 receptor antagonists, processes for preparing them and their use in pharmaceutical compositions |
| WO2008055959A1 (en) | 2006-11-09 | 2008-05-15 | Galapagos N.V. | Novel compounds useful for the treatment of degenerative & inflammatory diseases |
| JP2010518014A (ja) * | 2007-01-31 | 2010-05-27 | バーテックス ファーマシューティカルズ インコーポレイテッド | キナーゼ阻害剤として有用な２−アミノピリジン誘導体 |
| JP2010518083A (ja) | 2007-02-12 | 2010-05-27 | メルク・シャープ・エンド・ドーム・コーポレイション | ピペリジン誘導体 |
| AU2008225766B2 (en) * | 2007-03-15 | 2012-06-07 | Novartis Ag | Organic compounds and their uses |
| JP5658565B2 (ja) | 2007-09-12 | 2015-01-28 | ジェネンテック， インコーポレイテッド | ホスホイノシチド３−キナーゼ阻害剤化合物と化学療法剤との組合せ、および使用方法 |
| 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 |
| WO2009131687A2 (en) | 2008-04-22 | 2009-10-29 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| KR20110031318A (ko) | 2008-06-13 | 2011-03-25 | 노파르티스 아게 | Ｉａ 심부전 및 암 치료에 유용한 단백질 키나제 ｄ 억제제로서의 2,4'-비피리디닐 화합물 |
| US20110294836A1 (en) | 2008-06-20 | 2011-12-01 | Metabolex, Inc. | Aryl gpr119 agonists and uses thereof |
| US8168784B2 (en) | 2008-06-20 | 2012-05-01 | Abbott Laboratories | Processes to make apoptosis promoters |
| US8450335B2 (en) | 2008-06-27 | 2013-05-28 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| WO2010048149A2 (en) | 2008-10-20 | 2010-04-29 | Kalypsys, Inc. | Heterocyclic modulators of gpr119 for treatment of disease |
| MX2011004953A (es) * | 2008-11-10 | 2011-12-14 | Vertex Pharma | Compuestos utiles como inhibidores de cinasa atr. |
| JP2012511567A (ja) | 2008-12-10 | 2012-05-24 | ドン ファ ファーム カンパニー リミテッド | 新規の２，６−置換−３−ニトロピリジン誘導体、その製造方法及びこれを含む薬学組成物 |
| 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 |
| EP3205647B1 (en) | 2009-08-17 | 2020-05-13 | Memorial Sloan-Kettering Cancer Center | 2-(pyrimidin-5-yl)-thiopyrimidine derivatives as hsp70 and hsc70 modulators for the treatment of proliferative disorders |
| 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 |
| AU2011272198B2 (en) | 2010-06-30 | 2016-09-22 | Fujifilm Corporation | Novel nicotinamide derivatives or salts thereof |
| AU2011279509A1 (en) | 2010-07-13 | 2013-01-10 | Merck Sharp & Dohme Corp. | Spirocyclic compounds |
| ES2823350T3 (es) | 2010-07-29 | 2021-05-06 | Rigel Pharmaceuticals Inc | Compuestos heterocíclicos que activan AMPK y métodos de uso de los mismos |
| WO2012027495A1 (en) | 2010-08-27 | 2012-03-01 | University Of The Pacific | Piperazinylpyrimidine analogues as protein kinase inhibitors |
| EP2630134B9 (en) | 2010-10-20 | 2018-04-18 | Pfizer Inc | Pyridine-2- derivatives as smoothened receptor modulators |
| SI2755958T1 (sl) | 2011-09-12 | 2017-12-29 | Merck Patent Gmbh | Aminopirimidinski derivati za uporabo kot modulatorji kinazne aktivnosti |
| WO2013096093A1 (en) | 2011-12-21 | 2013-06-27 | Merck Sharp & Dohme Corp. | Compounds as dgat-1 inhibitors |
| EP2858994A1 (en) | 2012-06-07 | 2015-04-15 | F. Hoffmann-La Roche AG | Pyrazolopyrimidone and pyrazolopyridone inhibitors of tankyrase |
| WO2014054053A1 (en) | 2012-10-03 | 2014-04-10 | Advinus Therapeutics Limited | Spirocyclic compounds, compositions and medicinal applications thereof |
| US9499522B2 (en) | 2013-03-15 | 2016-11-22 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| EP3094627B1 (en) | 2014-01-17 | 2018-08-22 | Novartis AG | 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2 |
| 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 |
| US10308660B2 (en) | 2015-06-19 | 2019-06-04 | Novartis Ag | Compounds and compositions for inhibiting the activity of SHP2 |
| WO2016203404A1 (en) | 2015-06-19 | 2016-12-22 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| EP3310774B1 (en) | 2015-06-19 | 2020-04-29 | Novartis AG | Compounds and compositions for inhibiting the activity of shp2 |
-
2015
- 2015-01-16 EP EP15703106.3A patent/EP3094629B1/en active Active
- 2015-01-16 WO PCT/IB2015/050344 patent/WO2015107494A1/en not_active Ceased
- 2015-01-16 US US15/110,504 patent/US9815813B2/en active Active
- 2015-01-16 CN CN201580004207.9A patent/CN105899493B/zh active Active
- 2015-01-16 JP JP2016546924A patent/JP6473457B2/ja active Active
- 2015-01-16 ES ES15703106T patent/ES2699354T3/es active Active
-
2017
- 2017-10-05 US US15/726,189 patent/US10301278B2/en 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 |
|---|---|
| US20180065949A1 (en) | 2018-03-08 |
| CN105899493B (zh) | 2019-03-29 |
| JP2017502994A (ja) | 2017-01-26 |
| EP3094629B1 (en) | 2018-08-22 |
| US10301278B2 (en) | 2019-05-28 |
| CN105899493A (zh) | 2016-08-24 |
| US20170001975A1 (en) | 2017-01-05 |
| WO2015107494A1 (en) | 2015-07-23 |
| US9815813B2 (en) | 2017-11-14 |
| EP3094629A1 (en) | 2016-11-23 |
| ES2699354T3 (es) | 2019-02-08 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| 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 | |
| US11401259B2 (en) | 1-Pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and compositions thereof for inhibiting the activity of SHP2 | |
| US11952386B2 (en) | N-azaspirocycloalkane substituted N-heteroaryl compounds and compositions for inhibiting the activity of SHP2 | |
| JP6718889B2 (ja) | Ｓｈｐ２の活性を阻害するための化合物および組成物 | |
| US10308660B2 (en) | Compounds and compositions for inhibiting the activity of SHP2 | |
| HK1228375A1 (en) | N-azaspirocycloalkane substituted n-heteroaryl compounds and compositions for inhibiting the activity of shp2 | |
| HK1228375B (en) | N-azaspirocycloalkane substituted n-heteroaryl compounds and compositions for inhibiting the activity of shp2 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20180115 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20180115 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20181026 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20181106 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20181221 |
|
| 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: 20190115 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20190125 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 6473457 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 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |