CL2016001790A1 - Compuestos derivados y composiciones de n-azaspirocicloalcano n-heteroaril sustituido para inhibir la actividad de shp2. - Google Patents
Compuestos derivados y composiciones de n-azaspirocicloalcano n-heteroaril sustituido para inhibir la actividad de shp2.Info
- Publication number
- CL2016001790A1 CL2016001790A1 CL2016001790A CL2016001790A CL2016001790A1 CL 2016001790 A1 CL2016001790 A1 CL 2016001790A1 CL 2016001790 A CL2016001790 A CL 2016001790A CL 2016001790 A CL2016001790 A CL 2016001790A CL 2016001790 A1 CL2016001790 A1 CL 2016001790A1
- Authority
- CL
- Chile
- Prior art keywords
- azaspirocycloalkane
- compositions
- heteroaryl substituted
- derivative compounds
- shp2 activity
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 title 1
- 206010006187 Breast cancer Diseases 0.000 abstract 1
- 208000026310 Breast neoplasm Diseases 0.000 abstract 1
- 102100033019 Tyrosine-protein phosphatase non-receptor type 11 Human genes 0.000 abstract 1
- 101710116241 Tyrosine-protein phosphatase non-receptor type 11 Proteins 0.000 abstract 1
- 210000001072 colon Anatomy 0.000 abstract 1
- 208000005017 glioblastoma Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 210000004072 lung Anatomy 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
- C07D241/18—Oxygen or sulfur atoms
-
- 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
- C07D241/20—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
- C07D401/02—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
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
-
- 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
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/10—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)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461928754P | 2014-01-17 | 2014-01-17 | |
| US201461991129P | 2014-05-09 | 2014-05-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CL2016001790A1 true CL2016001790A1 (es) | 2016-12-30 |
Family
ID=52462974
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CL2016001790A CL2016001790A1 (es) | 2014-01-17 | 2016-07-13 | Compuestos derivados y composiciones de n-azaspirocicloalcano n-heteroaril sustituido para inhibir la actividad de shp2. |
Country Status (42)
Families Citing this family (140)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10357184B2 (en) * | 2012-06-21 | 2019-07-23 | Globus Medical, Inc. | Surgical tool systems and method |
| US11466017B2 (en) | 2011-03-10 | 2022-10-11 | Board Of Regents, The University Of Texas System | Heterocyclic inhibitors of PTPN11 |
| MY188450A (en) | 2013-01-29 | 2021-12-09 | Aptinyx Inc | Spiro-lactam nmda receptor modulators and uses thereof |
| CN105899491B (zh) | 2014-01-17 | 2019-04-02 | 诺华股份有限公司 | 用于抑制shp2活性的1-哒嗪-/三嗪-3-基-哌(-嗪)/啶/吡咯烷衍生物及其组合物 |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| WO2015107494A1 (en) | 2014-01-17 | 2015-07-23 | Novartis Ag | 1 -(triazin-3-yi_/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions thereof for inhibiting the activity of shp2 |
| CN107787226A (zh) * | 2015-03-25 | 2018-03-09 | 诺华股份有限公司 | 药物组合 |
| EP3310771B1 (en) * | 2015-06-19 | 2020-07-22 | Novartis AG | Compounds and compositions for inhibiting the activity of shp2 |
| WO2016203406A1 (en) * | 2015-06-19 | 2016-12-22 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| CN105503725B (zh) * | 2015-12-30 | 2018-03-27 | 天津药明康德新药开发有限公司 | 一种叔丁基1‑羟基‑8‑氮杂螺烷[4,5]葵烷‑8‑羧酸酯的制备方法 |
| 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 |
| CA3026784A1 (en) * | 2016-06-07 | 2017-12-14 | Jacobio Pharmaceuticals Co., Ltd. | Heterocyclic pyrazine derivatives useful as shp2 inhibitors |
| KR102457146B1 (ko) | 2016-06-14 | 2022-10-19 | 노파르티스 아게 | Shp2의 활성을 억제하기 위한 화합물 및 조성물 |
| EP3484856B1 (en) * | 2016-07-12 | 2023-11-15 | Revolution Medicines, Inc. | 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors |
| KR102503590B1 (ko) | 2016-08-01 | 2023-02-24 | 앱티닉스 인크. | 스피로-락탐 nmda 수용체 조정제 및 그의 용도 |
| CN109937204B (zh) | 2016-08-01 | 2022-11-25 | 阿普廷伊克斯股份有限公司 | 螺-内酰胺nmda受体调节剂及其用途 |
| EP3490990B1 (en) | 2016-08-01 | 2023-12-06 | Tenacia Biotechnology (Hong Kong) Co., Limited | Spiro-lactam nmda modulators and methods of using same |
| 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 |
| JP7503380B2 (ja) | 2017-01-10 | 2024-06-20 | ノバルティス アーゲー | Alk阻害剤およびshp2阻害剤を含む組合せ医薬 |
| IL296456A (en) | 2017-01-23 | 2022-11-01 | Revolution Medicines Inc | Bicyclics as allosteric shp2 inhibitors |
| RU2019126455A (ru) * | 2017-01-23 | 2021-02-24 | Революшн Медсинз, Инк. | Пиридиновые соединения в качестве аллостерических ингибиторов shp2 |
| MY200227A (en) | 2017-03-23 | 2023-12-15 | Jacobio Pharmaceuticals Co Ltd | Novel heterocyclic derivatives useful as shp2 inhibitors |
| US11591336B2 (en) | 2017-05-26 | 2023-02-28 | D. E. Shaw Research, Llc | Substituted pyrazolo[3,4-b]pyrazines as SHP2 phosphatase inhibitors |
| US10690253B2 (en) * | 2017-06-20 | 2020-06-23 | Control Components, Inc. | Multi-stage, multi-path rotary disc |
| KR20200051684A (ko) | 2017-09-07 | 2020-05-13 | 레볼루션 메디슨즈, 인크. | 암 치료를 위한 shp2 억제제 조성물 및 방법 |
| TW202517628A (zh) * | 2017-09-11 | 2025-05-01 | 美商克魯松藥物公司 | Shp2之八氫環戊烷并[c]吡咯別構抑制劑 |
| US11701354B2 (en) | 2017-09-29 | 2023-07-18 | D. E. Shaw Research, Llc | Pyrazolo[3,4-b]pyrazine derivatives as SHP2 phosphatase inhibitors |
| SG11202002941WA (en) * | 2017-10-12 | 2020-04-29 | 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 |
| RU2020123241A (ru) * | 2017-12-15 | 2022-01-17 | Революшн Медсинз, Инк. | Полициклические соединения в качестве аллостерических ингибиторов shp2 |
| WO2019152454A1 (en) * | 2018-01-30 | 2019-08-08 | Research Development Foundation | Shp2 inhibitors and methods of use thereof |
| US11578072B2 (en) | 2018-01-31 | 2023-02-14 | Aptinyx Inc. | Spiro-lactam NMDA receptor modulators and uses thereof |
| KR102614939B1 (ko) * | 2018-02-13 | 2023-12-19 | 블루레이 테라퓨틱스 (상하이) 컴퍼니 리미티드 | 피리미딘-융합고리 화합물 및 그의 제조방법과 용도 |
| CN115448923B (zh) * | 2018-02-13 | 2024-03-22 | 上海青煜医药科技有限公司 | 嘧啶并环化合物及其制备方法和应用 |
| EP3755699A1 (en) | 2018-02-21 | 2020-12-30 | Relay Therapeutics, Inc. | Shp2 phosphatase inhibitors and methods of use thereof |
| US11466016B2 (en) | 2018-03-02 | 2022-10-11 | Otsuka Pharmaceutical Co., Ltd. | Pharmaceutical compounds |
| US12138263B2 (en) | 2018-03-21 | 2024-11-12 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine SHP2 phosphatase inhibitors and methods of use thereof |
| MX2020009782A (es) * | 2018-03-21 | 2021-01-20 | Relay Therapeutics Inc | Inhibidores de la fosfatasa shp2 y métodos para su uso. |
| KR102724968B1 (ko) | 2018-03-21 | 2024-10-31 | 수조우 푸허 바이오파마 컴퍼니 리미티드 | Shp2 억제제 및 이의 용도 |
| AU2019251207A1 (en) * | 2018-04-10 | 2020-11-19 | 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 |
| KR102611661B1 (ko) | 2018-05-02 | 2023-12-08 | 나비레 파르마, 인코퍼레이티드 | Ptpn11의 치환된 헤테로사이클릭 억제제 |
| CN116003321A (zh) * | 2018-05-09 | 2023-04-25 | 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 |
| EP3827009A4 (en) | 2018-07-24 | 2022-04-27 | Taiho Pharmaceutical Co., Ltd. | HETEROBICYCLIC COMPOUNDS TO INHIBIT SHP2 ACTIVITY |
| PL3833670T3 (pl) | 2018-08-10 | 2024-08-19 | Navire Pharma, Inc. | Pochodne 6-(4-amino-3-metylo-2-oksa-8-azaspiro[4.5]dekan-8-ylo)-3-(2,3-dichlorofenylo)-2-metylopirymidyn-4(3h)-onu oraz powiązane związki jako inhibitory ptpn11 (shp2) do leczenia raka |
| BR112021005082A2 (pt) | 2018-09-18 | 2021-06-08 | Nikang Therapeutics, Inc. | derivados de anel tricíclico fundido como inibidores de src homologia-2 fosfatase |
| US20210393623A1 (en) | 2018-09-26 | 2021-12-23 | Jacobio Pharmaceuticals Co., Ltd. | Novel Heterocyclic Derivatives Useful as SHP2 Inhibitors |
| US11873307B2 (en) * | 2018-09-29 | 2024-01-16 | Novartis Ag | Manufacture of compounds and compositions for inhibiting the activity of SHP2 |
| EP3856345A1 (en) * | 2018-09-29 | 2021-08-04 | Novartis AG | Process of manufacture of a compound for inhibiting the activity of shp2 |
| WO2020072656A1 (en) | 2018-10-03 | 2020-04-09 | Gilead Sciences, Inc. | Imidozopyrimidine derivatives |
| 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 |
| HUE062404T2 (hu) | 2018-10-17 | 2023-10-28 | Array Biopharma Inc | Protein tirozin foszfatáz inhibitorok |
| 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 |
| 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 |
| AU2019386036A1 (en) | 2018-11-30 | 2021-05-27 | Tuojie Biotech (Shanghai) Co., Ltd. | Pyrimidine and five-membered nitrogen heterocycle derivative, preparation method therefor, and medical uses thereof |
| 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 |
| 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 |
| EP3923941B1 (en) * | 2019-02-12 | 2025-12-03 | Novartis AG | Pharmaceutical combination comprising tno155 and ribociclib |
| WO2020165733A1 (en) | 2019-02-12 | 2020-08-20 | Novartis Ag | Pharmaceutical combination comprising tno155 and a pd-1 inhibitor |
| CN113382774A (zh) | 2019-02-12 | 2021-09-10 | 诺华股份有限公司 | 包含tno155和krasg12c抑制剂的药物组合 |
| 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 |
| WO2020181283A1 (en) | 2019-03-07 | 2020-09-10 | Merck Patent Gmbh | Carboxamide-pyrimidine derivatives as shp2 antagonists |
| MA55511A (fr) | 2019-04-02 | 2022-02-09 | Array Biopharma Inc | Inhibiteurs de protéine tyrosine phosphatase |
| 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 |
| CN114126620B (zh) | 2019-05-13 | 2024-12-31 | 传达治疗有限公司 | Fgfr抑制剂和其使用方法 |
| SG11202112461QA (en) * | 2019-06-07 | 2021-12-30 | Revolution Medicines Inc | Solid forms of {6-[(2-amino-3-chloropyridin-4-yl)sulfanyl]-3-[(3s,4s)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-methylpyrazin-2-yl}methanol, an shp2 inhibitor |
| 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 |
| KR20220054285A (ko) | 2019-06-28 | 2022-05-02 | 투오지에 바이오텍 (상하이) 컴퍼니 리미티드 | 피리미딘 5 원 질소 헤테로고리형 유도체, 이의 제조 방법 및 이의 약학적 용도 |
| CN111704611B (zh) * | 2019-07-25 | 2022-01-14 | 上海凌达生物医药有限公司 | 一类芳基螺环类shp2抑制剂化合物、制备方法和用途 |
| CN112300160A (zh) * | 2019-08-01 | 2021-02-02 | 上海奕拓医药科技有限责任公司 | 一种螺芳环化合物、其制备及应用 |
| EP3772513A1 (en) | 2019-08-09 | 2021-02-10 | C.N.C.C.S. S.c.a.r.l. Collezione Nazionale Dei Composti Chimici e Centro Screening | Shp2 inhibitors |
| GB201911928D0 (en) | 2019-08-20 | 2019-10-02 | Otsuka Pharma Co Ltd | Pharmaceutical compounds |
| US12122787B2 (en) | 2019-09-20 | 2024-10-22 | Shanghai Jemincare Pharmaceuticals Co., Ltd | Fused pyridone compound, and preparation method therefor and use thereof |
| TW202126660A (zh) | 2019-09-24 | 2021-07-16 | 美商傳達治療有限公司 | Shp2磷酸酶抑制劑及其製備與使用方法 |
| US20210139517A1 (en) | 2019-11-08 | 2021-05-13 | Revolution Medicines, Inc. | Bicyclic heteroaryl compounds and uses thereof |
| CN114761394B (zh) * | 2020-01-16 | 2024-03-29 | 浙江海正药业股份有限公司 | 吡啶或嘧啶类衍生物及其制备方法和用途 |
| CN113135910A (zh) | 2020-01-19 | 2021-07-20 | 北京诺诚健华医药科技有限公司 | 嘧啶-4(3h)-酮类杂环化合物、其制备方法及其在医药学上的应用 |
| CN115297862A (zh) | 2020-02-28 | 2022-11-04 | 诺华股份有限公司 | 包含达拉菲尼、erk抑制剂和shp2抑制剂的三重药物组合 |
| 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 |
| WO2021218755A1 (zh) * | 2020-04-30 | 2021-11-04 | 贝达药业股份有限公司 | Shp2抑制剂及其组合物和应用 |
| CA3179994A1 (en) | 2020-05-08 | 2021-11-11 | Novartis Ag | Pharmaceutical combination comprising tno155 and nazartinib |
| WO2021236775A1 (en) * | 2020-05-19 | 2021-11-25 | The Regents Of The University Ofmichigan | Small molecule degraders of shp2 protein |
| WO2021247836A1 (en) | 2020-06-03 | 2021-12-09 | Board Of Regents, The University Of Texas System | Methods for targeting shp-2 to overcome resistance |
| WO2021249057A1 (zh) * | 2020-06-12 | 2021-12-16 | 石药集团中奇制药技术(石家庄)有限公司 | 杂环化合物及其用途 |
| TW202214253A (zh) | 2020-06-18 | 2022-04-16 | 美商銳新醫藥公司 | 延遲、預防及治療對ras抑制劑之後天抗性之方法 |
| CN115667239B (zh) | 2020-06-22 | 2025-11-18 | 四川科伦博泰生物医药股份有限公司 | 取代吡嗪类化合物,包含其的药物组合物及其用途 |
| JP7729870B2 (ja) | 2020-07-08 | 2025-08-26 | 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及び組成物の製造 |
| WO2022006780A1 (en) * | 2020-07-08 | 2022-01-13 | Novartis Ag | Manufacture of compounds and compositions for inhibiting activity of shp2 |
| CN115515947B (zh) * | 2020-07-24 | 2024-02-06 | 贝达药业股份有限公司 | Shp2抑制剂及其组合物和应用 |
| CN116209438A (zh) | 2020-09-03 | 2023-06-02 | 锐新医药公司 | 使用sos1抑制剂治疗具有shp2突变的恶性疾病 |
| EP4214209A1 (en) | 2020-09-15 | 2023-07-26 | Revolution Medicines, Inc. | Indole derivatives as ras inhibitors in the treatment of cancer |
| WO2022063190A1 (zh) * | 2020-09-23 | 2022-03-31 | 南京明德新药研发有限公司 | 吡嗪硫联苯基类化合物及其应用 |
| TW202233625A (zh) | 2020-11-18 | 2022-09-01 | 美商傳達治療有限公司 | Fgfr抑制劑及其製造及使用方法 |
| EP4039685A1 (en) | 2021-02-08 | 2022-08-10 | Irbm S.P.A. | Azabicyclic shp2 inhibitors |
| EP4317144A4 (en) * | 2021-03-23 | 2025-07-23 | Shanghai Haiyan Pharmaceutical Tech Co Ltd | HETEROCYCLE-SUBSTITUTED KETONE DERIVATIVE, AND COMPOSITION AND MEDICINAL USE THEREOF |
| CN117083285A (zh) * | 2021-03-31 | 2023-11-17 | 南京明德新药研发有限公司 | 一系列含Se的吡嗪类化合物及其应用 |
| 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 |
| JP2024517788A (ja) | 2021-05-05 | 2024-04-23 | ノバルティス アーゲー | Mpnstの処置のための化合物及び組成物 |
| EP4334324A1 (en) | 2021-05-05 | 2024-03-13 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| EP4334325A1 (en) | 2021-05-05 | 2024-03-13 | Revolution Medicines, Inc. | Ras inhibitors for the treatment of cancer |
| US12390469B2 (en) | 2021-05-05 | 2025-08-19 | Huyabio International, Llc | SHP2 inhibitor monotherapy and uses thereof |
| CN118561952A (zh) | 2021-05-05 | 2024-08-30 | 锐新医药公司 | Ras抑制剂 |
| JP2024516037A (ja) | 2021-05-05 | 2024-04-11 | フヤバイオ インターナショナル,エルエルシー | Shp2阻害剤とpd-1阻害剤とを含む併用療法 |
| WO2022259157A1 (en) | 2021-06-09 | 2022-12-15 | Novartis Ag | A triple pharmaceutical combination comprising dabrafenib, trametinib and a shp2 inhibitor |
| TW202313046A (zh) | 2021-06-09 | 2023-04-01 | 瑞士商赫孚孟拉羅股份公司 | 用於癌症治療之組合療法 |
| 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 |
| 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 |
| CN115594666B (zh) * | 2021-07-07 | 2024-05-31 | 海创药业股份有限公司 | 一种磷酸酶降解剂的合成和应用 |
| AU2022336415A1 (en) | 2021-09-01 | 2024-01-04 | 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 |
| EP4426305A1 (en) | 2021-11-04 | 2024-09-11 | F. Hoffmann-La Roche AG | Novel use of quinazolinone compound for the treatment of cancer |
| TW202342040A (zh) | 2022-02-21 | 2023-11-01 | 瑞士商諾華公司 | 藥物配製物 |
| CN114524772B (zh) * | 2022-02-28 | 2023-07-11 | 中国药科大学 | 一种含杂环串联类化合物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 |
| 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 |
| AU2023285116A1 (en) | 2022-06-10 | 2024-12-19 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| TW202413348A (zh) | 2022-08-11 | 2024-04-01 | 美商傳達治療有限公司 | Cdk抑制劑及其製備及使用方法 |
| EP4345101A1 (en) | 2022-09-29 | 2024-04-03 | Irbm S.P.A. | Azole derivatives as shp2 inhibitors |
| WO2024105610A1 (en) | 2022-11-18 | 2024-05-23 | Novartis Ag | Pharmaceutical combinations and uses thereof |
| WO2024113194A1 (en) * | 2022-11-30 | 2024-06-06 | Canwell Biotech Limited | Shp2 inhibitors, compositions and methods thereof |
| EP4634172A1 (en) | 2022-12-15 | 2025-10-22 | F. Hoffmann-La Roche AG | Combination therapy for cancer treatment |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| WO2024211663A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
| WO2024211712A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
| 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 |
| 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 |
| 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 |
| WO2025034919A1 (en) | 2023-08-08 | 2025-02-13 | Quanta Therapeutics, Inc. | Combination therapies with kras modulators |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | 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 |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025215527A2 (en) | 2024-04-10 | 2025-10-16 | Novartis Ag | Pharmaceutical combinations and uses thereof |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| 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 |
| CN119661551B (zh) * | 2024-12-16 | 2025-11-25 | 重庆大学 | 一种(3r,4s)-3-甲基-2-氧杂-8-氮杂螺[4.5]癸烷-4-胺盐酸盐的制备方法 |
Family Cites Families (135)
| 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 |
| GB2116183B (en) | 1982-03-03 | 1985-06-05 | Genentech Inc | Human antithrombin iii dna sequences therefore expression vehicles and cloning vectors containing such sequences and cell cultures transformed thereby a process for expressing human antithrombin iii and pharmaceutical compositions comprising it |
| US4512991A (en) * | 1982-12-27 | 1985-04-23 | Merck & Co., Inc. | 3-Acyl-2-amino-5-halo-6-(substituted)pyrazine antimicrobial compounds |
| 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 |
| GB9012316D0 (en) | 1990-06-01 | 1990-07-18 | Wellcome Found | Pharmacologically active cns compounds |
| 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 |
| EP1947183B1 (en) | 1996-08-16 | 2013-07-17 | Merck Sharp & Dohme Corp. | Mammalian cell surface antigens; related reagents |
| US6111090A (en) | 1996-08-16 | 2000-08-29 | Schering Corporation | Mammalian cell surface antigens; related reagents |
| MA26473A1 (fr) * | 1997-03-01 | 2004-12-20 | Glaxo Group Ltd | Composes pharmacologiquement actifs. |
| CA2308114A1 (en) | 1997-10-21 | 1999-04-29 | Human Genome Sciences, Inc. | Human tumor necrosis factor receptor-like proteins tr11, tr11sv1, and tr11sv2 |
| WO1999040196A1 (en) | 1998-02-09 | 1999-08-12 | Genentech, Inc. | Novel tumor necrosis factor receptor homolog and nucleic acids encoding the same |
| 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 |
| CA2378179A1 (en) | 1999-07-12 | 2001-01-18 | Genentech, Inc. | Promotion or inhibition of angiogenesis and cardiovascularization by tumor necrosis factor ligand/receptor homologs |
| 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 |
| JP4460292B2 (ja) | 2001-10-17 | 2010-05-12 | ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | ピリミジン誘導体、これらの化合物を含む医薬組成物、その使用及びその調製方法 |
| PT1478648E (pt) | 2002-02-01 | 2014-07-15 | Ariad Pharma Inc | Compostos contendo fósforo e suas utilizações |
| RU2004126671A (ru) * | 2002-02-06 | 2005-04-10 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Гетероарилсоединения, полезные в качестве ингибиторов gsk-3 |
| IL163748A0 (en) | 2002-03-05 | 2005-12-18 | Merck Frosst Canada Inc | Cathepsin cysteine protease inhibitors |
| TWI275390B (en) | 2002-04-30 | 2007-03-11 | Wyeth Corp | Process for the preparation of 7-substituted-3- quinolinecarbonitriles |
| CA2508660C (en) | 2002-12-23 | 2013-08-20 | Wyeth | Antibodies against pd-1 and uses therefor |
| GB0300783D0 (en) | 2003-01-14 | 2003-02-12 | Btg Int Ltd | Treatment of neurodegenerative conditions |
| AU2004218228A1 (en) | 2003-03-07 | 2004-09-16 | Merck Sharp & Dohme Limited | Tetrahydropyran compounds as tachykinin antagonists |
| RU2369636C2 (ru) | 2003-05-23 | 2009-10-10 | Уайт | Лиганд gitr и связанные с лигандом gitr молекулы и антитела и варианты их применения |
| US20050048054A1 (en) | 2003-07-11 | 2005-03-03 | Shino Hanabuchi | Lymphocytes; methods |
| US7399865B2 (en) | 2003-09-15 | 2008-07-15 | Wyeth | Protein tyrosine kinase enzyme inhibitors |
| JP2007518399A (ja) | 2003-12-02 | 2007-07-12 | ジェンザイム コーポレイション | 肺癌を診断および治療する組成物並びに方法 |
| 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 |
| US8076338B2 (en) * | 2004-04-23 | 2011-12-13 | Exelixis, Inc. | Kinase modulators and methods of use |
| GB0409799D0 (en) | 2004-04-30 | 2004-06-09 | Isis Innovation | Method of generating improved immune response |
| US20060002932A1 (en) | 2004-06-04 | 2006-01-05 | Duke University | Methods and compositions for enhancement of immunity by in vivo depletion of immunosuppressive cell activity |
| ES2377430T3 (es) | 2004-09-02 | 2012-03-27 | Genentech, Inc. | Inhibidores piridílicos de la señalización de hedgehog |
| RU2423351C2 (ru) | 2004-12-16 | 2011-07-10 | Вертекс Фармасьютикалз Инкорпорейтед | Пирид-2-оны, применимые как ингибиторы протеинкиназ семейства тес для лечения воспалительных, пролиферативных и иммунологически-опосредованных заболеваний |
| PT1866339E (pt) | 2005-03-25 | 2013-09-03 | Gitr Inc | Moléculas de ligação a gitr e suas utilizações |
| PL2161336T5 (pl) | 2005-05-09 | 2017-10-31 | Ono Pharmaceutical Co | Ludzkie przeciwciała monoklonalne przeciwko białku Programmed Death 1 (PD-1) oraz sposoby leczenia raka z zastosowaniem samych przeciwciał anty-PD-1 lub w połączeniu z innymi środkami immunoterapeutycznymi |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| PL1907424T3 (pl) | 2005-07-01 | 2015-12-31 | Squibb & Sons Llc | Ludzkie monoklonalne przeciwciała wobec liganda zaprogramowanej śmierci 1 (PD-L1) |
| JP2009507896A (ja) | 2005-09-13 | 2009-02-26 | パラウ・フアルマ・ソシエダツド・アノニマ | ヒスタミンh4受容体活性の調節剤としての2−アミノピリミジン誘導体 |
| AR057579A1 (es) * | 2005-11-23 | 2007-12-05 | Merck & Co Inc | Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac) |
| US20110212086A1 (en) | 2006-01-19 | 2011-09-01 | Genzyme Corporation | GITR Antibodies For The Treatment of Cancer |
| JP2009531456A (ja) | 2006-03-28 | 2009-09-03 | 武田薬品工業株式会社 | (r)−3−アミノピペリジン二塩酸塩の調製 |
| DK2041071T3 (da) | 2006-06-29 | 2014-09-01 | Kinex Pharmaceuticals Llc | Biarylsammensætninger og fremgangsmåder til modulering af en kinasekaskade |
| 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 |
| EP2120573A4 (en) | 2007-02-12 | 2011-05-25 | Merck Sharp & Dohme | piperidine |
| KR101473504B1 (ko) * | 2007-03-15 | 2014-12-16 | 노파르티스 아게 | 유기 화합물 및 그의 용도 |
| US8354509B2 (en) | 2007-06-18 | 2013-01-15 | Msd Oss B.V. | Antibodies to human programmed death receptor PD-1 |
| WO2009009116A2 (en) | 2007-07-12 | 2009-01-15 | Tolerx, Inc. | Combination therapies employing gitr binding molecules |
| CL2008002687A1 (es) | 2007-09-12 | 2009-01-16 | Genentech Inc | Uso de una combinacion farmaceutica de un compuesto derivado de tieno[3,2-d]pirimidina con un agente quimioterapeutico en el tratamiento de un trastorno hiperproliferativo; kit farmaceutico. |
| CA2701292C (en) | 2007-10-25 | 2015-03-24 | Genentech, Inc. | Process for making thienopyrimidine compounds |
| CA2715166C (en) | 2008-02-11 | 2017-05-16 | Curetech Ltd. | Monoclonal antibodies for tumor treatment |
| WO2009114335A2 (en) | 2008-03-12 | 2009-09-17 | Merck & Co., Inc. | Pd-1 binding proteins |
| CA2723185A1 (en) | 2008-04-22 | 2009-10-29 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| EA201100136A1 (ru) | 2008-06-13 | 2011-08-30 | Новартис Аг | 2,4'-бипиридинилы в качестве ингибиторов протеинкиназы d, применимые для лечения сердечной недостаточности и рака |
| US8168784B2 (en) | 2008-06-20 | 2012-05-01 | Abbott Laboratories | Processes to make apoptosis promoters |
| KR20110026481A (ko) | 2008-06-20 | 2011-03-15 | 메타볼렉스, 인코포레이티드 | 아릴 gpr119 작동약 및 이의 용도 |
| CA3031835C (en) | 2008-06-27 | 2021-09-07 | Celgene Car Llc | Heteroaryl compounds and uses thereof |
| GB0812031D0 (en) | 2008-07-01 | 2008-08-06 | 7Tm Pharma As | Thiazole derivatives |
| KR20110044992A (ko) | 2008-07-02 | 2011-05-03 | 이머전트 프로덕트 디벨롭먼트 시애틀, 엘엘씨 | TGF-β 길항제 다중-표적 결합 단백질 |
| US9174969B2 (en) | 2008-07-21 | 2015-11-03 | University Of South Florida | Indoline scaffold SHP-2 inhibitors and cancer treatment method |
| AR072999A1 (es) | 2008-08-11 | 2010-10-06 | Medarex Inc | Anticuerpos humanos que se unen al gen 3 de activacion linfocitaria (lag-3) y los usos de estos |
| EA201500417A1 (ru) | 2008-08-25 | 2015-11-30 | Эмплиммьюн, Инк. | Композиции антагонистов pd-1 и способы применения |
| JP2012500652A (ja) | 2008-08-25 | 2012-01-12 | アンプリミューン、インコーポレーテッド | 標的化共刺激ポリペプチドおよび癌を処置するための使用方法 |
| JPWO2010030002A1 (ja) | 2008-09-12 | 2012-02-02 | 国立大学法人三重大学 | 外来性gitrリガンド発現細胞 |
| WO2010048149A2 (en) | 2008-10-20 | 2010-04-29 | Kalypsys, Inc. | Heterocyclic modulators of gpr119 for treatment of disease |
| AU2009313198B2 (en) * | 2008-11-10 | 2016-03-24 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| RU2017132160A (ru) | 2008-12-09 | 2019-02-08 | Дженентек, Инк. | Антитела к pd-l1 и их применение для усиления функции t-клеток |
| 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 |
| JP5844159B2 (ja) | 2009-02-09 | 2016-01-13 | ユニヴェルシテ デクス−マルセイユUniversite D’Aix−Marseille | Pd−1抗体およびpd−l1抗体ならびにその使用 |
| 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 |
| CN102753177A (zh) | 2009-08-17 | 2012-10-24 | 纪念斯隆-凯特琳癌症中心 | 热休克蛋白结合化合物、组合物以及其制备和使用方法 |
| RU2646139C1 (ru) | 2009-09-03 | 2018-03-01 | Мерк Шарп И Доум Корп. | Анти-gitr-антитела |
| GB0919054D0 (en) | 2009-10-30 | 2009-12-16 | Isis Innovation | Treatment of obesity |
| US8673913B2 (en) | 2009-11-13 | 2014-03-18 | Case Western Reserve University | SHP-2 phosphatase inhibitor |
| WO2011066342A2 (en) | 2009-11-24 | 2011-06-03 | Amplimmune, Inc. | Simultaneous inhibition of pd-l1/pd-l2 |
| 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 |
| CN103124743A (zh) | 2009-12-29 | 2013-05-29 | 新兴产品开发西雅图有限公司 | Ron结合构建物及其使用方法 |
| PL2589592T3 (pl) | 2010-06-30 | 2019-03-29 | Fujifilm Corporation | Nowe pochodne nikotynamidu lub ich sole |
| WO2012009217A1 (en) | 2010-07-13 | 2012-01-19 | Merck Sharp & Dohme Corp. | Spirocyclic compounds |
| PE20130774A1 (es) | 2010-07-29 | 2013-06-26 | Rigel Pharmaceuticals Inc | Compuestos heterociclicos activadores de ampk y metodos para emplearlos |
| WO2012027495A1 (en) * | 2010-08-27 | 2012-03-01 | University Of The Pacific | Piperazinylpyrimidine analogues as protein kinase inhibitors |
| ES2543151T3 (es) | 2010-10-20 | 2015-08-17 | Pfizer Inc | Derivados de 2-piridina como moduladores del receptor Smoothened |
| UY33801A (es) | 2010-12-13 | 2013-06-28 | Array Biopharma Inc | COMPUESTOS SUSTITUIDOS DE N-(1H-INDAZOL-4IL)IMIDAZO[1,2-a]PIRIDIN-3-CARBOXAMIDA COMO INHIBIDORES DE LA TIROSINA QUINASA RECEPTORA DE TIPO III |
| JP5727276B2 (ja) | 2011-03-04 | 2015-06-03 | 協同油脂株式会社 | グリース組成物及びグリース封入転がり軸受 |
| JP6082011B2 (ja) | 2011-09-12 | 2017-02-15 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung | キナーゼ活性のモジュレーターとして使用するためのアミノピリミジン誘導体 |
| US20130108641A1 (en) | 2011-09-14 | 2013-05-02 | Sanofi | Anti-gitr antibodies |
| CN103987405B (zh) | 2011-11-28 | 2017-03-29 | 默克专利股份公司 | 抗pd‑l1抗体及其用途 |
| WO2013096093A1 (en) | 2011-12-21 | 2013-06-27 | Merck Sharp & Dohme Corp. | Compounds as dgat-1 inhibitors |
| BR112014030410A2 (pt) | 2012-06-07 | 2017-06-27 | Hoffmann La Roche | inibidores de pirazolopirimidona e pirazolopiridona de tanquirase |
| CN104364239B (zh) | 2012-06-13 | 2017-08-25 | 霍夫曼-拉罗奇有限公司 | 二氮杂螺环烷烃和氮杂螺环烷烃 |
| AR091649A1 (es) | 2012-07-02 | 2015-02-18 | Bristol Myers Squibb Co | Optimizacion de anticuerpos que se fijan al gen de activacion de linfocitos 3 (lag-3) y sus usos |
| 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 |
| EP2970231A1 (en) * | 2013-03-15 | 2016-01-20 | Blueprint Medicines Corporation | Piperazine derivatives and their use as kit modulators |
| US10189859B2 (en) | 2013-12-21 | 2019-01-29 | Nektar Therapeutics | Derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine |
| 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 |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| CN105899491B (zh) | 2014-01-17 | 2019-04-02 | 诺华股份有限公司 | 用于抑制shp2活性的1-哒嗪-/三嗪-3-基-哌(-嗪)/啶/吡咯烷衍生物及其组合物 |
| RS62874B1 (sr) | 2014-05-01 | 2022-02-28 | Celgene Quanticel Research Inc | Inhibitori lizin specifične demetilaze-1 |
| US10174032B2 (en) | 2014-05-05 | 2019-01-08 | Signalrx Pharmaceuticals, Inc. | Heterocyclic compound classes for signaling modulation |
| EP3310771B1 (en) | 2015-06-19 | 2020-07-22 | Novartis AG | Compounds and compositions for inhibiting the activity of shp2 |
| WO2016203406A1 (en) | 2015-06-19 | 2016-12-22 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| EP3310779B1 (en) | 2015-06-19 | 2019-05-08 | Novartis AG | Compounds and compositions for inhibiting the activity of shp2 |
| WO2017156397A1 (en) | 2016-03-11 | 2017-09-14 | Board Of Regents, The University Of Texas Sysytem | Heterocyclic inhibitors of ptpn11 |
| 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 |
| CA3026784A1 (en) | 2016-06-07 | 2017-12-14 | Jacobio Pharmaceuticals Co., Ltd. | Heterocyclic pyrazine derivatives useful as shp2 inhibitors |
| EP3484856B1 (en) | 2016-07-12 | 2023-11-15 | 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 |
| 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 |
| JP7503380B2 (ja) | 2017-01-10 | 2024-06-20 | ノバルティス アーゲー | Alk阻害剤およびshp2阻害剤を含む組合せ医薬 |
| IL296456A (en) | 2017-01-23 | 2022-11-01 | Revolution Medicines Inc | Bicyclics as allosteric shp2 inhibitors |
| RU2019126455A (ru) | 2017-01-23 | 2021-02-24 | Революшн Медсинз, Инк. | Пиридиновые соединения в качестве аллостерических ингибиторов shp2 |
| MY200227A (en) | 2017-03-23 | 2023-12-15 | Jacobio Pharmaceuticals Co Ltd | Novel heterocyclic derivatives useful as shp2 inhibitors |
| KR20200051684A (ko) | 2017-09-07 | 2020-05-13 | 레볼루션 메디슨즈, 인크. | 암 치료를 위한 shp2 억제제 조성물 및 방법 |
| US11701354B2 (en) | 2017-09-29 | 2023-07-18 | D. E. Shaw Research, Llc | Pyrazolo[3,4-b]pyrazine derivatives as SHP2 phosphatase inhibitors |
| SG11202002941WA (en) | 2017-10-12 | 2020-04-29 | Revolution Medicines Inc | Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors |
| RU2020123241A (ru) | 2017-12-15 | 2022-01-17 | Революшн Медсинз, Инк. | Полициклические соединения в качестве аллостерических ингибиторов shp2 |
| EP3755699A1 (en) | 2018-02-21 | 2020-12-30 | Relay Therapeutics, Inc. | Shp2 phosphatase inhibitors and methods of use thereof |
| MX2020009782A (es) | 2018-03-21 | 2021-01-20 | Relay Therapeutics Inc | Inhibidores de la fosfatasa shp2 y métodos para su uso. |
| AU2019251207A1 (en) | 2018-04-10 | 2020-11-19 | Revolution Medicines, Inc. | SHP2 inhibitor compositions, methods for treating cancer and methods for identifying a subject with SHP2 mutations |
-
2015
- 2015-01-15 JO JOP/2015/0004A patent/JO3517B1/ar active
- 2015-01-16 EP EP15703321.8A patent/EP3094628B1/en active Active
- 2015-01-16 AU AU2015207757A patent/AU2015207757B8/en active Active
- 2015-01-16 JP JP2016546839A patent/JP6534389B2/ja active Active
- 2015-01-16 CR CR20160328A patent/CR20160328A/es unknown
- 2015-01-16 PL PL15703321T patent/PL3094628T3/pl unknown
- 2015-01-16 LT LTEP15703321.8T patent/LT3094628T/lt unknown
- 2015-01-16 CN CN201580004708.7A patent/CN105916845B/zh active Active
- 2015-01-16 KR KR1020167021977A patent/KR102501558B1/ko active Active
- 2015-01-16 SI SI201530432T patent/SI3094628T1/sl unknown
- 2015-01-16 DK DK15703321.8T patent/DK3094628T3/en active
- 2015-01-16 US US15/110,511 patent/US10077276B2/en active Active
- 2015-01-16 BR BR112016016432-6A patent/BR112016016432B1/pt active IP Right Grant
- 2015-01-16 SG SG11201605272SA patent/SG11201605272SA/en unknown
- 2015-01-16 MA MA39282A patent/MA39282B1/fr unknown
- 2015-01-16 KR KR1020237005361A patent/KR102688024B1/ko active Active
- 2015-01-16 AR ARP150100117A patent/AR100033A1/es active IP Right Grant
- 2015-01-16 PT PT15703321T patent/PT3094628T/pt unknown
- 2015-01-16 RS RS20181174A patent/RS57757B1/sr unknown
- 2015-01-16 TN TN2016000268A patent/TN2016000268A1/en unknown
- 2015-01-16 HU HUE15703321A patent/HUE039869T2/hu unknown
- 2015-01-16 CR CR20200617A patent/CR20200617A/es unknown
- 2015-01-16 CU CU2016000115A patent/CU24424B1/es unknown
- 2015-01-16 UY UY0001035957A patent/UY35957A/es active IP Right Grant
- 2015-01-16 AP AP2016009299A patent/AP2016009299A0/en unknown
- 2015-01-16 WO PCT/IB2015/050345 patent/WO2015107495A1/en not_active Ceased
- 2015-01-16 MY MYPI2016702327A patent/MY176357A/en unknown
- 2015-01-16 NZ NZ721598A patent/NZ721598A/en unknown
- 2015-01-16 MX MX2016009223A patent/MX356895B/es active IP Right Grant
- 2015-01-16 ES ES15703321T patent/ES2695242T3/es active Active
- 2015-01-16 EA EA201691442A patent/EA031573B1/ru not_active IP Right Cessation
- 2015-01-16 TW TW104101593A patent/TWI657083B/zh active
- 2015-01-16 PE PE2016001228A patent/PE20170011A1/es unknown
- 2015-01-16 HR HRP20181832TT patent/HRP20181832T1/hr unknown
- 2015-01-16 CA CA2935695A patent/CA2935695C/en active Active
-
2016
- 2016-06-23 IL IL24643616A patent/IL246436B/en active IP Right Grant
- 2016-07-05 PH PH12016501336A patent/PH12016501336B1/en unknown
- 2016-07-13 CL CL2016001790A patent/CL2016001790A1/es unknown
- 2016-07-15 GT GT201600147A patent/GT201600147A/es unknown
- 2016-07-15 SV SV2016005245A patent/SV2016005245A/es unknown
- 2016-07-15 DO DO2016000177A patent/DOP2016000177A/es unknown
- 2016-07-15 NI NI201600101A patent/NI201600101A/es unknown
- 2016-08-16 EC ECIEPI201667692A patent/ECSP16067692A/es unknown
-
2018
- 2018-02-20 US US15/899,821 patent/US10336774B2/en active Active
- 2018-11-08 CY CY20181101177T patent/CY1121155T1/el unknown
-
2019
- 2019-05-21 US US16/418,978 patent/US10968235B2/en active Active
-
2021
- 2021-02-23 US US17/182,756 patent/US11952386B2/en active Active
- 2021-02-23 US US17/182,744 patent/US12209098B2/en active Active
- 2021-11-22 US US17/532,367 patent/US20220073537A1/en not_active Abandoned
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CL2016001790A1 (es) | Compuestos derivados y composiciones de n-azaspirocicloalcano n-heteroaril sustituido para inhibir la actividad de shp2. | |
| CL2014001793A1 (es) | Compuestos derivados de 1,3,5-triazinas sustituidas y sus sales, como inhibidores de la idh2 mutante; composicion farmaceutica que los comprende; y su uso para el tratamiento del cancer. | |
| CL2019001711A1 (es) | Composiciones y métodos para inhibir la acción de la arginasa. | |
| DOP2015000270A (es) | Potenciador de inhibidores del homólogo de zeste | |
| CO2018004124A2 (es) | Compuestos heterocíclicos | |
| CL2016003246A1 (es) | Compuestos de dihidroisoquinolinona sustituida | |
| SV2018005794A (es) | Derivados de carbonucleósidos sustituidos útiles como agentes antineoplásicos | |
| GT201700189A (es) | Derivados de nucleósidos sustituidos útiles como agentes antineoplásicos | |
| CU20160162A7 (es) | Derivados de pirrolidina-2,5-diona,para usar como inhibidores ido1 y composiciones farmacéuticas que los contienen | |
| CL2016003398A1 (es) | Compuestos de heteroarilo útiles como inhibidores de enzima activadora de sumo. | |
| CL2016001889A1 (es) | (2s)-n-[(1s)-1-ciano-2-feniletil]-1,4-oxazepan-2-carboxamidas como inhibidores de dipeptidil peptidasa 1. | |
| CU20160149A7 (es) | Compuestos de heteroarilo o arilo bicíclicos fusionados y su uso como inhibidores de irak4 | |
| MX2016014253A (es) | Inhibidores de desmetilasa-1 especifica de lisina. | |
| UY35485A (es) | Compuestos heterocíclicos y usos de los mismos | |
| MX2016015565A (es) | Ciertos inhibidores de la proteina quinasa. | |
| MX2019007243A (es) | Inhibidores de ectonucleotidasa y metodos de uso de los mismos. | |
| CL2016003074A1 (es) | Compuestos derivados de 2-oxi-2-fenil-n-5-pirrolidin-3-ilamino-1,3,4-tiadiazol-2-ilacetamida, inhibidores gls1 composición farmacéutica y su uso para tratar el cáncer. | |
| DOP2018000062A (es) | Piridinona dicaboxamidas para uso como inhibidores de bromodominio | |
| CL2015000976A1 (es) | Compuestos de 2-fenil-5-heterociclil-tetrahidro-2h-piran-3-amina para uso en el tratamiento de diabetes y sus trastornos asociados. | |
| MX373320B (es) | Compuestos inhibidores de pde2. | |
| DOP2016000312A (es) | Compuestos derivados de 1-(ciclopent-2-en-1-il)-3-(2-hidroxi-3-(arilsulfonil)fenil)urea como inhibidores cxcr2 | |
| MX2017001352A (es) | Derivados de pirrolidinona como inhibidores de metionina aminopeptidasa 2 (metap-2). | |
| CL2016000568A1 (es) | Compuestos derivados de 2h-indazol-2-il-n-hidroxi-2-metilsulfonil-2-metil-butanamida sustituidos o sus sales; sus composiciones farmacéuticas que los contiene y su uso para la prevención y/o tratamiento de infecciones bacterianas gram-negativas. | |
| DOP2018000066A (es) | Compuestos útiles para inhibir ror-gamma-t | |
| MX388564B (es) | Compuestos de indolinona y usos de los mismos. |