CL2019000090A1 - 3-metil pirazinas 2,5-disustituidas y 3-metil pirazinas 2,5,6-trisustituidas como inhibidores alostéricos de shp2. - Google Patents
3-metil pirazinas 2,5-disustituidas y 3-metil pirazinas 2,5,6-trisustituidas como inhibidores alostéricos de shp2.Info
- Publication number
- CL2019000090A1 CL2019000090A1 CL2019000090A CL2019000090A CL2019000090A1 CL 2019000090 A1 CL2019000090 A1 CL 2019000090A1 CL 2019000090 A CL2019000090 A CL 2019000090A CL 2019000090 A CL2019000090 A CL 2019000090A CL 2019000090 A1 CL2019000090 A1 CL 2019000090A1
- Authority
- CL
- Chile
- Prior art keywords
- methyl pyrazines
- pyrazines
- methyl
- trisubstituted
- disubstituted
- Prior art date
Links
Classifications
-
- 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
-
- 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
-
- 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
- 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
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
-
- 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
- C07D471/04—Ortho-condensed systems
-
- 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
- C07D471/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D477/00—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring
- C07D477/26—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hetero atoms or carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-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
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- 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
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662361249P | 2016-07-12 | 2016-07-12 | |
| US201762449523P | 2017-01-23 | 2017-01-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CL2019000090A1 true CL2019000090A1 (es) | 2019-06-21 |
Family
ID=59383648
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CL2019000090A CL2019000090A1 (es) | 2016-07-12 | 2019-01-11 | 3-metil pirazinas 2,5-disustituidas y 3-metil pirazinas 2,5,6-trisustituidas como inhibidores alostéricos de shp2. |
Country Status (22)
| Country | Link |
|---|---|
| US (3) | US10590090B2 (enExample) |
| EP (2) | EP3484856B1 (enExample) |
| JP (3) | JP6916279B2 (enExample) |
| KR (2) | KR20230156174A (enExample) |
| CN (3) | CN109983001B (enExample) |
| AU (3) | AU2017296289A1 (enExample) |
| CA (1) | CA3030167A1 (enExample) |
| CL (1) | CL2019000090A1 (enExample) |
| CO (1) | CO2019000613A2 (enExample) |
| CR (1) | CR20190063A (enExample) |
| DO (1) | DOP2019000005A (enExample) |
| EC (1) | ECSP19010079A (enExample) |
| IL (3) | IL264186B2 (enExample) |
| MA (1) | MA45660A (enExample) |
| MX (2) | MX395351B (enExample) |
| MY (1) | MY199046A (enExample) |
| PE (1) | PE20190624A1 (enExample) |
| PH (1) | PH12019500056B1 (enExample) |
| SG (1) | SG11201900157RA (enExample) |
| TN (1) | TN2019000010A1 (enExample) |
| TW (2) | TWI806832B (enExample) |
| WO (1) | WO2018013597A1 (enExample) |
Families Citing this family (138)
| 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 |
| 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 |
| EP3571189B1 (en) | 2017-01-23 | 2023-03-29 | Revolution Medicines, Inc. | Pyridine compounds as allosteric shp2 inhibitors |
| 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 |
| 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 |
| 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 |
| EP3724189B1 (en) | 2017-12-15 | 2023-10-04 | Revolution Medicines, Inc. | Polycyclic compounds as allosteric shp2 inhibitors |
| MY196582A (en) | 2018-02-13 | 2023-04-19 | Gilead Sciences Inc | PD-1/PD-L1 Inhibitors |
| 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 |
| CN110655520A (zh) * | 2018-06-29 | 2020-01-07 | 上海青煜医药科技有限公司 | 嘧啶并环化合物及其制备方法和应用 |
| 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 |
| 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 |
| 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 |
| AU2019263294B2 (en) | 2018-05-02 | 2024-03-21 | Navire Pharma, Inc. | Substituted heterocyclic inhibitors of PTPN11 |
| PT3820572T (pt) | 2018-07-13 | 2023-11-10 | Gilead Sciences Inc | Inibidores pd-1/pd-l1 |
| 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 |
| 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 |
| 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 |
| ES2947464T3 (es) | 2018-10-17 | 2023-08-09 | Array Biopharma Inc | Inhibidores de la proteína tirosina fosfatasa |
| CN109265352B (zh) * | 2018-10-31 | 2021-06-04 | 杭州迈世腾药物科技有限公司 | 芳基环丙基醚及其衍生物的制备方法 |
| TW202039498A (zh) | 2018-11-30 | 2020-11-01 | 大陸商上海拓界生物醫藥科技有限公司 | 嘧啶並五員氮雜環類衍生物、其製備方法及其在醫藥上的應用 |
| 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 |
| 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 |
| MX2021014855A (es) * | 2019-06-07 | 2022-01-18 | Revolution Medicines Inc | {6-[(2-amino-3-cloropiridin-4-il)sulfanil]-3-[(3s,4s)-4-amino-3-m etil-2 oxa-8-azaspiro[4.5]decan-8-il]-5-metilpirazin-2-il}metanol, un inhibidor de shp2. |
| AU2020306124A1 (en) | 2019-06-28 | 2022-02-03 | Tuojie Biotech (Shanghai) Co., Ltd. | Pyrimidine five-membered nitrogen heterocyclic derivative, preparation method thereof and pharmaceutical use thereof |
| CN111704611B (zh) * | 2019-07-25 | 2022-01-14 | 上海凌达生物医药有限公司 | 一类芳基螺环类shp2抑制剂化合物、制备方法和用途 |
| CN112300160A (zh) * | 2019-08-01 | 2021-02-02 | 上海奕拓医药科技有限责任公司 | 一种螺芳环化合物、其制备及应用 |
| EP3772513A1 (en) | 2019-08-09 | 2021-02-10 | C.N.C.C.S. S.c.a.r.l. Collezione Nazionale Dei Composti Chimici e Centro Screening | Shp2 inhibitors |
| GB201911928D0 (en) | 2019-08-20 | 2019-10-02 | Otsuka Pharma Co Ltd | Pharmaceutical compounds |
| WO2021043077A1 (zh) * | 2019-09-06 | 2021-03-11 | 四川科伦博泰生物医药股份有限公司 | 一种取代吡嗪化合物、其制备方法和用途 |
| WO2021061515A1 (en) * | 2019-09-23 | 2021-04-01 | Synblia Therapeutics, Inc. | Shp2 inhibitors and uses thereof |
| MX2022003454A (es) | 2019-09-24 | 2022-04-19 | Relay Therapeutics Inc | Inhibidores de fosfatasa shp2 y metodos para su fabricacion y uso. |
| CN112724145A (zh) * | 2019-10-14 | 2021-04-30 | 杭州雷索药业有限公司 | 用于抑制shp2活性的吡嗪衍生物 |
| US20240139193A1 (en) | 2019-10-15 | 2024-05-02 | Amgen Inc. | Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers |
| US11739074B2 (en) | 2019-11-04 | 2023-08-29 | Revolution Medicines, Inc. | Ras inhibitors |
| 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 |
| 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 |
| EP4069301A1 (en) | 2019-12-04 | 2022-10-12 | Bayer Aktiengesellschaft | Inhibitors of shp2 |
| IL294484A (en) * | 2020-01-07 | 2022-09-01 | Revolution Medicines Inc | Shp2 inhibitor dosing and methods of treating cancer |
| WO2021143680A1 (zh) | 2020-01-16 | 2021-07-22 | 浙江海正药业股份有限公司 | 杂芳基类衍生物及其制备方法和用途 |
| CN113135910A (zh) * | 2020-01-19 | 2021-07-20 | 北京诺诚健华医药科技有限公司 | 嘧啶-4(3h)-酮类杂环化合物、其制备方法及其在医药学上的应用 |
| WO2021147879A1 (zh) * | 2020-01-21 | 2021-07-29 | 贝达药业股份有限公司 | Shp2抑制剂及其应用 |
| EP4110338A1 (en) | 2020-02-28 | 2023-01-04 | Novartis AG | A triple pharmaceutical combination comprising dabrafenib, an erk inhibitor and a shp2 inhibitor |
| CN113493440B (zh) * | 2020-04-03 | 2024-08-23 | 上海翰森生物医药科技有限公司 | 含氮杂芳类衍生物的盐及其晶型 |
| TW202144334A (zh) * | 2020-04-03 | 2021-12-01 | 大陸商上海翰森生物醫藥科技有限公司 | 含氮雜芳類衍生物游離鹼的晶型 |
| CN115362149B (zh) * | 2020-04-26 | 2024-05-14 | 贝达药业股份有限公司 | Shp2抑制剂及其组合物和应用 |
| IL298917A (en) * | 2020-06-11 | 2023-02-01 | Betta Pharmaceuticals Co Ltd | Shp2 inhibitors, compositions and uses thereof |
| 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 |
| WO2022042331A1 (zh) * | 2020-08-25 | 2022-03-03 | 四川科伦博泰生物医药股份有限公司 | 杂环化合物及其制备方法和用途 |
| 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 |
| CA3198809A1 (en) | 2020-10-20 | 2022-04-28 | Amgen Inc. | Heterocyclic spiro compounds and methods of use |
| CA3199082A1 (en) | 2020-10-27 | 2022-05-05 | Amgen Inc. | Heterocyclic spiro compounds and methods of use |
| CN116848121A (zh) * | 2020-12-18 | 2023-10-03 | 建新公司 | 制备shp2抑制剂的方法 |
| KR20230171917A (ko) * | 2020-12-18 | 2023-12-21 | 젠자임 코포레이션 | Shp2 억제제를 제조하는 방법 |
| CA3203111A1 (en) | 2020-12-22 | 2022-06-30 | Kailiang Wang | Sos1 inhibitors and uses thereof |
| WO2022161222A1 (zh) * | 2021-01-29 | 2022-08-04 | 四川科伦博泰生物医药股份有限公司 | 一类杂环类shp2抑制剂、其制备方法及用途 |
| EP4039685A1 (en) | 2021-02-08 | 2022-08-10 | Irbm S.P.A. | Azabicyclic shp2 inhibitors |
| 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 |
| EP4067358A1 (en) | 2021-04-02 | 2022-10-05 | C.N.C.C.S. S.c.a.r.l. Collezione Nazionale Dei Composti Chimici e Centro Screening | (s)-1-(5-((pyridin-3-yl)thio)pyrazin-2-yl)-4'h,6'h-spiro[piperidine-4,5'-pyrrolo[1,2-b]pyrazol]-4'-amine derivatives and similar compounds as shp2 inhibitors for the treatment of e.g. cancer |
| MX2023012725A (es) | 2021-04-29 | 2024-09-23 | Amgen Inc | Compuestos de 2-aminobenzotiazol y metodos de uso de los mismos. |
| EP4334324A1 (en) | 2021-05-05 | 2024-03-13 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| US12390469B2 (en) | 2021-05-05 | 2025-08-19 | Huyabio International, Llc | SHP2 inhibitor monotherapy and uses thereof |
| WO2022234409A1 (en) | 2021-05-05 | 2022-11-10 | Novartis Ag | Compounds and compositions for the treatment of mpnst |
| 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 |
| IL308193A (en) | 2021-05-05 | 2024-01-01 | Revolution Medicines Inc | RAS inhibitors |
| KR20240007279A (ko) * | 2021-05-13 | 2024-01-16 | 상하이 인스티튜트 오브 마테리아 메디카 차이니즈 아카데미 오브 싸이언시즈 | Shp2활성을 억제하는 헤테로고리 화합물, 이의 제조 방법 및 용도 |
| WO2022242767A1 (zh) | 2021-05-21 | 2022-11-24 | 石药集团中奇制药技术(石家庄)有限公司 | 螺环类化合物及其用途 |
| 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 |
| 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 |
| KR102682323B1 (ko) * | 2021-07-09 | 2024-07-09 | 주식회사 카나프테라퓨틱스 | Shp2 억제제 및 이의 용도 |
| CN113636952B (zh) * | 2021-07-19 | 2023-07-21 | 河南农业大学 | 一种制备4-溴苯甲酰胺的方法 |
| KR20240050360A (ko) * | 2021-08-09 | 2024-04-18 | 주식회사 유빅스테라퓨틱스 | Shp2 단백질 분해활성을 갖는 화합물 및 이들의 의약 용도 |
| 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 |
| CN116323566B (zh) * | 2021-09-27 | 2024-05-17 | 中国医药研究开发中心有限公司 | 磺胺酮类化合物及其制备方法和医药用途 |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| US20250109118A1 (en) * | 2021-12-28 | 2025-04-03 | Js Innomed Holdings Ltd. | Heterocyclic compounds as shp2 inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof |
| CN118715215A (zh) | 2022-02-16 | 2024-09-27 | 美国安进公司 | 作为突变kras蛋白抑制剂的喹唑啉化合物及其用途 |
| JP2025508702A (ja) | 2022-02-16 | 2025-04-10 | アムジエン・インコーポレーテツド | キナゾリン化合物、及び変異krasタンパク質の阻害剤としてのその使用 |
| EP4486345A1 (en) | 2022-03-04 | 2025-01-08 | Eli Lilly and Company | Method of treatment including kras g12c inhibitors and shp2 inhibitors |
| 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 |
| WO2023169170A1 (zh) * | 2022-03-10 | 2023-09-14 | 捷思英达控股有限公司 | 作为shp2抑制剂的杂环化合物、包括该杂环化合物的组合物、及其使用方法 |
| US20250134885A1 (en) | 2022-03-21 | 2025-05-01 | Institut National de la Santé et de la Recherche Médicale | Use of shp2 inhibitors for inhibiting senescence |
| EP4499648A1 (en) * | 2022-03-28 | 2025-02-05 | Genzyme Corporation | Process for preparing shp2 inhibitors |
| TW202404581A (zh) | 2022-05-25 | 2024-02-01 | 美商醫肯納腫瘤學公司 | Mek抑制劑及其用途 |
| EP4536364A1 (en) | 2022-06-10 | 2025-04-16 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2024015360A1 (en) | 2022-07-11 | 2024-01-18 | Amgen Inc. | Methods of treating cancer |
| WO2024040131A1 (en) | 2022-08-17 | 2024-02-22 | Treeline Biosciences, Inc. | Pyridopyrimidine kras inhibitors |
| EP4345101A1 (en) | 2022-09-29 | 2024-04-03 | Irbm S.P.A. | Azole derivatives as shp2 inhibitors |
| WO2024085699A1 (ko) * | 2022-10-19 | 2024-04-25 | 주식회사 유빅스테라퓨틱스 | Shp2 단백질 분해용 화합물 및 이들의 의약 용도 |
| WO2024113194A1 (en) * | 2022-11-30 | 2024-06-06 | Canwell Biotech Limited | Shp2 inhibitors, compositions and methods thereof |
| 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 |
| 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 |
| TW202528315A (zh) | 2023-09-21 | 2025-07-16 | 美商樹線生物科學公司 | 螺環二氫哌喃并吡啶KRas抑制劑 |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025081291A1 (en) * | 2023-10-16 | 2025-04-24 | Canwell Biotech Limited | Benzo [c] [1, 2] oxaborol-1 (3h) -ol derivatives as shp2 inhibitors, compositions and methods thereof |
| 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 |
| WO2025194057A1 (en) | 2024-03-14 | 2025-09-18 | Amgen Inc. | Macrocyclic compounds as modulators of kras and uses thereof |
| WO2025194054A1 (en) | 2024-03-14 | 2025-09-18 | Amgen Inc. | Spirocyclic compounds as modulators of kras and uses thereof |
| WO2025217247A1 (en) | 2024-04-10 | 2025-10-16 | Amgen Inc. | Tethered spiro-heterocyclic inhibitors of kras g12c mutant proteins and uses thereof |
| WO2025230878A1 (en) | 2024-04-29 | 2025-11-06 | Amgen Inc. | Macrocyclic compounds as modulators of kras and uses thereof |
| WO2025240582A1 (en) | 2024-05-14 | 2025-11-20 | Amgen Inc. | Macrocyclic compounds as modulators of kras and uses thereof |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025245127A1 (en) | 2024-05-21 | 2025-11-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| CN119661551B (zh) * | 2024-12-16 | 2025-11-25 | 重庆大学 | 一种(3r,4s)-3-甲基-2-氧杂-8-氮杂螺[4.5]癸烷-4-胺盐酸盐的制备方法 |
Family Cites Families (125)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2572728A (en) * | 1949-01-07 | 1951-10-23 | American Cyanamid Co | Hydroxybenzenesulfonamidopyra-zines and preparation of same |
| US2636882A (en) | 1950-08-11 | 1953-04-28 | Quaker Oats Co | Preparation of 3-pyridols from 2-acylfurans |
| BE758503A (fr) | 1969-11-07 | 1971-05-05 | Shell Int Research | Compositions pesticides |
| GB1459571A (en) | 1974-09-12 | 1976-12-22 | Pfizer Ltd | Thiophene-2-sulphonamide derivatives and their use as therapeutic agents sheet orienting apparatus |
| JPS5762269A (en) * | 1980-10-03 | 1982-04-15 | Ogawa Koryo Kk | 2,3,5-trisubstituted pyrazine derivative |
| US4513135A (en) * | 1982-03-05 | 1985-04-23 | Eli Lilly And Company | Diaryl-pyrazine derivatives affecting GABA binding |
| JPH0249775A (ja) | 1988-05-19 | 1990-02-20 | Nippon Soda Co Ltd | 6員環又は7員環を有する複素環化合物及びその製造方法 |
| JPH04112877A (ja) | 1990-09-04 | 1992-04-14 | Nippon Soda Co Ltd | 新規シアノピラジン誘導体及びその製造方法 |
| EP0579835A4 (en) | 1991-11-12 | 1994-06-01 | Nippon Soda Co | Wavelength conversion material for agriculture |
| US5262564A (en) | 1992-10-30 | 1993-11-16 | Octamer, Inc. | Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents |
| GB9504854D0 (en) * | 1994-03-31 | 1995-04-26 | Zeneca Ltd | Nitrogen derivatives |
| ATE336495T1 (de) | 1996-02-07 | 2006-09-15 | Neurocrine Biosciences Inc | Pyrazolopyrimidine als crf rezeptor-antagonisten |
| AU8071698A (en) * | 1997-06-13 | 1998-12-30 | Sugen, Inc. | Novel heteroaryl compounds for the modulation of protein tyrosine enzyme relatedcellular signal transduction |
| US6596772B1 (en) | 1999-08-27 | 2003-07-22 | Sugen, Inc. | Phosphate mimics and methods of treatment using phosphatase inhibitors |
| JP2004500383A (ja) | 2000-02-16 | 2004-01-08 | ニューロゲン コーポレイション | 置換アリールピラジン |
| TWI316055B (enExample) * | 2001-04-26 | 2009-10-21 | Nippon Shinyaku Co Ltd | |
| EP1448587B1 (en) | 2001-10-01 | 2009-09-02 | Mount Sinai School of Medicine | Noonan syndrome gene |
| US6921762B2 (en) | 2001-11-16 | 2005-07-26 | Amgen Inc. | Substituted indolizine-like compounds and methods of use |
| WO2003045924A1 (en) | 2001-11-21 | 2003-06-05 | Pharmacia & Upjohn Company | Substituted aryl 1,4-pyrazine derivatives |
| JP2005531520A (ja) | 2002-03-28 | 2005-10-20 | メルク エンド カムパニー インコーポレーテッド | 置換2,3−ジフェニルピリジン類 |
| EP1499599A1 (en) * | 2002-04-26 | 2005-01-26 | Pharmacia & Upjohn Company LLC | Substituted pyrazine derivatives |
| WO2004024719A1 (en) * | 2002-09-12 | 2004-03-25 | Pharmacia & Upjohn Company Llc | Substituted 1,4-pyrazine derivatives |
| BR0316880A (pt) | 2002-12-23 | 2005-10-25 | Wyeth Corp | Anticorpos contra pd-1 e usos dos mesmos |
| US7157460B2 (en) | 2003-02-20 | 2007-01-02 | Sugen Inc. | Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors |
| EP1625125A1 (en) | 2003-05-09 | 2006-02-15 | Pharmacia & Upjohn Company LLC | Compounds as crf1 receptor antagonists |
| GB0314057D0 (en) * | 2003-06-18 | 2003-07-23 | Astrazeneca Ab | Therapeutic agents |
| FR2856684B1 (fr) | 2003-06-26 | 2008-04-11 | Sanofi Synthelabo | Derives de diphenylpyridine, leur preparation et leur application en therapeutique |
| US7326706B2 (en) * | 2003-08-15 | 2008-02-05 | Bristol-Myers Squibb Company | Pyrazine modulators of cannabinoid receptors |
| EP1675858A2 (en) | 2003-09-03 | 2006-07-05 | Neurogen Corporation | 5-aryl-pyrazolo [4,3-d] pyrimidines, pyridines, and pyrazines and related compounds |
| ATE369370T1 (de) | 2003-10-10 | 2007-08-15 | Pfizer Prod Inc | Substituierte 2h-(1,2,4)triazolo(4,3-a)pyrazine als gsk-3-inhibitoren |
| CA2543644A1 (en) * | 2003-10-27 | 2005-05-06 | Astellas Pharma Inc. | Pyrazine derivatives and pharmaceutical use thereof |
| DE102004015954A1 (de) * | 2004-04-01 | 2005-11-10 | Ina-Schaeffler Kg | Umschlingungstrieb |
| 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 |
| US20050282818A1 (en) | 2004-06-22 | 2005-12-22 | Rigel Pharmaceuticals, Inc. | Ubiquitin ligase inhibitors |
| JP2008525487A (ja) | 2004-12-23 | 2008-07-17 | マリンクロッド・インコーポレイテッド | 蛍光ピラジン誘導体および腎機能評価におけるその使用方法 |
| JP2008536950A (ja) * | 2005-04-18 | 2008-09-11 | ニューロジェン・コーポレーション | 置換ヘテロアリールのcb1拮抗薬 |
| PL1893612T3 (pl) | 2005-06-22 | 2012-01-31 | Plexxikon Inc | Pochodne pirolo-[2,3-b]pirydyny jako inhibitory kinazy białkowej |
| AU2006304876B2 (en) | 2005-10-21 | 2013-04-18 | Regents Of The University Of California | c-KIT oncogene mutations in melanoma |
| CA2616147A1 (en) | 2006-02-24 | 2007-09-20 | Mallinckrodt Inc. | Process for using optical agents |
| WO2007117699A2 (en) | 2006-04-07 | 2007-10-18 | University Of South Florida | Inhibition of shp2/ptpn11 protein tyrosine phosphatase by nsc-87877, nsc-117199 and their analogs |
| AU2007243280A1 (en) | 2006-04-28 | 2007-11-08 | Northwestern University | Formulations containing pyridazine compounds for treating neuroinflammatory diseases |
| US7893058B2 (en) | 2006-05-15 | 2011-02-22 | Janssen Pharmaceutica Nv | Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases |
| WO2007138072A2 (en) | 2006-05-31 | 2007-12-06 | Galapagos N.V. | Triazolopyrazine compounds useful for the treatment of degenerative & inflammatory diseases |
| TW200808802A (en) | 2006-06-06 | 2008-02-16 | Schering Corp | Imidazopyrazines as protein kinase inhibitors |
| JP2010520238A (ja) | 2007-03-01 | 2010-06-10 | マリンクロット インコーポレイテッド | 統合された光活性低分子および統合された光活性低分子使用 |
| ATE502940T1 (de) | 2007-04-06 | 2011-04-15 | Novartis Ag | Ä2,6-ünaphthyridine als proteinkinasehemmer |
| US8133895B2 (en) | 2007-05-10 | 2012-03-13 | Janssen Pharmaceutica N.V. | Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases |
| US8148369B2 (en) | 2007-05-10 | 2012-04-03 | Janssen Pharmaceutica Nv | Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases |
| WO2008156174A1 (ja) | 2007-06-21 | 2008-12-24 | Taisho Pharmaceutical Co., Ltd. | ピラジンアミド化合物 |
| WO2009020642A1 (en) | 2007-08-09 | 2009-02-12 | Merck & Co., Inc. | Pyridine carboxamide orexin receptor antagonists |
| WO2009025823A1 (en) | 2007-08-21 | 2009-02-26 | Amgen Inc. | Phosphodiesterase 10 inhibitors |
| JP2010031249A (ja) * | 2008-06-23 | 2010-02-12 | Sumitomo Chemical Co Ltd | 組成物及び該組成物を用いてなる発光素子 |
| WO2010011666A2 (en) | 2008-07-21 | 2010-01-28 | University Of South Florida | Indoline scaffold shp-2 inhibitors and cancer treatment method |
| WO2010051238A1 (en) | 2008-10-30 | 2010-05-06 | Merck Sharp & Dohme Corp. | Pyridazine carboxamide orexin receptor antagonists |
| AU2009314631B2 (en) * | 2008-11-12 | 2014-07-31 | Takeda Pharmaceutical Company Limited | Pyrazinopyrazines and derivatives as kinase inhibitors |
| CN102356075B (zh) | 2009-01-23 | 2015-06-10 | 里格尔药品股份有限公司 | 抑制jak途径的组合物和方法 |
| 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 |
| WO2010141275A1 (en) | 2009-06-01 | 2010-12-09 | Merck Sharp & Dohme Corp. | Pyrazine carboxamide orexin receptor antagonists |
| 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 |
| CA2780713A1 (en) | 2009-09-03 | 2011-03-10 | Vancouver Biotech Ltd. | Monoclonal antibodies against gonadotropin-releasing hormone receptor |
| US8673913B2 (en) | 2009-11-13 | 2014-03-18 | Case Western Reserve University | SHP-2 phosphatase inhibitor |
| JP5989547B2 (ja) | 2010-03-05 | 2016-09-07 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | ヒトcsf−1rに対する抗体及びその使用 |
| TW201202251A (en) | 2010-05-11 | 2012-01-16 | Sanofi Aventis | Substituted N-heteroaryl spirolactam bipyrrolidines, preparation and therapeutic use thereof |
| US8703768B2 (en) | 2010-06-09 | 2014-04-22 | Hoffmann-La Roche Inc. | Nitrogen containing heteroaryl compounds |
| PL2593452T3 (pl) | 2010-07-14 | 2017-07-31 | Novartis Ag | Związki heterocykliczne będące agonistami receptora IP |
| GB201106829D0 (en) * | 2011-04-21 | 2011-06-01 | Proximagen Ltd | Heterocyclic compounds |
| US9127000B2 (en) | 2011-02-23 | 2015-09-08 | Intellikine, LLC. | Heterocyclic compounds and uses thereof |
| WO2012149280A2 (en) | 2011-04-29 | 2012-11-01 | Abbott Laboratories | Novel tricyclic compounds |
| CN103181918B (zh) | 2011-05-04 | 2014-10-29 | 厦门大学 | 脂肪酸类化合物在制备预防和治疗肝癌药物中的应用 |
| US20150005311A1 (en) * | 2012-01-13 | 2015-01-01 | Novartis Ag | IP receptor agonist heterocyclic compounds |
| ME02648B (me) * | 2012-01-17 | 2017-06-20 | Astellas Pharma Inc | Jedinjenje pirazin karboksamida |
| EP2882746B1 (en) | 2012-08-07 | 2016-12-07 | Merck Patent GmbH | Pyridopyrimidine derivatives as protein kinase inhibitors |
| AU2013343104A1 (en) | 2012-11-08 | 2015-04-23 | Pfizer Inc. | Heteroaromatic compounds and their use as dopamine D1 ligands |
| BR112015012366A8 (pt) | 2012-11-29 | 2019-10-01 | Chemocentryx Inc | antagonistas de cxcr7, uso dos mesmos, composição farmacêutica, bem como métodos para detectar níveis elevados de cxcr7 em uma amostra e para imagear um tumor, órgão, ou tecido |
| WO2014113584A1 (en) | 2013-01-16 | 2014-07-24 | Rhode Island Hospital | Compositions and methods for the prevention and treatment of osteolysis and osteoporosis |
| WO2014121885A1 (en) * | 2013-02-07 | 2014-08-14 | Merck Patent Gmbh | Substituted quinoxaline derivatives and their use as positive allosteric modulators of mglur4 |
| EP2958943B1 (en) | 2013-02-20 | 2019-09-11 | The Trustees Of The University Of Pennsylvania | Treatment of cancer using humanized anti-egfrviii chimeric antigen receptor |
| EP3689904A1 (en) | 2013-03-13 | 2020-08-05 | Prothena Biosciences Limited | Tau immunotherapy |
| CN103554038B (zh) | 2013-06-19 | 2015-10-14 | 云南大学 | 多卤代苯腈喹唑啉酮化合物及其制备方法和用途 |
| 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 |
| EP3094629B1 (en) * | 2014-01-17 | 2018-08-22 | Novartis AG | 1-(triazin-3-yl/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 |
| TWI687419B (zh) | 2014-07-10 | 2020-03-11 | 美商英塞特公司 | 作為lsd1抑制劑之咪唑并吡啶及咪唑并吡嗪 |
| CN106573915B (zh) | 2014-08-01 | 2020-12-25 | 纽韦卢森公司 | 针对布罗莫结构域有活性的化合物 |
| CN112125901A (zh) * | 2014-09-05 | 2020-12-25 | 赛尔基因昆蒂赛尔研究公司 | 赖氨酸特异性脱甲基酶-1的抑制剂 |
| MX381180B (es) | 2014-11-18 | 2025-03-12 | Merck Sharp & Dohme | Compuestos aminopirazina con propiedades antagonistas a2a. |
| ES2881305T3 (es) | 2014-12-17 | 2021-11-29 | Siemens Healthcare Diagnostics Inc | Diseño de ensayo sandwich para pequeñas moléculas |
| HRP20190805T1 (hr) | 2014-12-23 | 2019-06-28 | Novartis Ag | Spojevi triazolopirimidina i njihova uporaba |
| US10533016B2 (en) | 2015-01-09 | 2020-01-14 | Revolution Medicines, Inc. | Compounds that participate in cooperative binding and uses thereof |
| US10112929B2 (en) * | 2015-03-09 | 2018-10-30 | Bristol-Myers Squibb Company | Lactams as inhibitors of rock |
| MX373154B (es) | 2015-04-03 | 2020-04-22 | Incyte Holdings Corp | Compuestos heterocíclicos como inhibidores de demetilasa 1 específica de lisina (lsd1). |
| US10308660B2 (en) | 2015-06-19 | 2019-06-04 | 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 |
| WO2016203404A1 (en) | 2015-06-19 | 2016-12-22 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| US10426842B2 (en) | 2015-07-15 | 2019-10-01 | The Curators Of The University Of Missouri | Targeted nanoparticle conjugate and method for co-delivery of siRNA and drug |
| US9989535B2 (en) | 2015-10-01 | 2018-06-05 | Warp Drive Bio, Inc. | Methods and reagents for analyzing protein-protein interfaces |
| WO2017079723A1 (en) | 2015-11-07 | 2017-05-11 | Board Of Regents, The University Of Texas System | Targeting proteins for degradation |
| WO2017156397A1 (en) | 2016-03-11 | 2017-09-14 | Board Of Regents, The University Of Texas Sysytem | Heterocyclic inhibitors of ptpn11 |
| 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 |
| EP3571189B1 (en) | 2017-01-23 | 2023-03-29 | Revolution Medicines, Inc. | Pyridine compounds as allosteric shp2 inhibitors |
| 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 |
| 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 |
| KR20200003802A (ko) | 2017-04-05 | 2020-01-10 | 레볼루션 메디슨즈, 인크. | 단백질-단백질 계면을 분석하기 위한 방법 및 시약 |
| CN110831632A (zh) | 2017-04-05 | 2020-02-21 | 锐新医药公司 | 参与协同结合的化合物及其用途 |
| US11591336B2 (en) | 2017-05-26 | 2023-02-28 | D. E. Shaw Research, Llc | Substituted pyrazolo[3,4-b]pyrazines as SHP2 phosphatase inhibitors |
| KR20200051684A (ko) | 2017-09-07 | 2020-05-13 | 레볼루션 메디슨즈, 인크. | 암 치료를 위한 shp2 억제제 조성물 및 방법 |
| AU2018347516A1 (en) | 2017-10-12 | 2020-05-07 | Revolution Medicines, Inc. | Pyridine, pyrazine, and triazine compounds as allosteric SHP2 inhibitors |
| 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 |
| 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 |
| 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 |
| 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 |
| MX2020011564A (es) | 2018-05-01 | 2021-01-29 | Revolution Medicines Inc | Analogos de rapamicina unidos a c26 como inhibidores de mtor. |
| JP2022500384A (ja) | 2018-09-10 | 2022-01-04 | 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 |
| CA3113234A1 (en) | 2018-09-18 | 2020-03-26 | Nikang Therapeutics, Inc. | Tri-substituted heteroaryl derivatives as src homology-2 phosphatase inhibitors |
| WO2020076723A1 (en) | 2018-10-08 | 2020-04-16 | Revolution Medicines, Inc. | Shp2 inhibitor compositions for use in treating cancer |
| JP7377679B2 (ja) | 2018-11-19 | 2023-11-10 | アムジエン・インコーポレーテツド | がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法 |
| EP3897644A4 (en) | 2018-12-21 | 2022-09-07 | Revolution Medicines, Inc. | CONNECTIONS INVOLVING IN A COOPERATIVE BINDING AND USES THEREOF |
| US11739074B2 (en) | 2019-11-04 | 2023-08-29 | Revolution Medicines, Inc. | Ras inhibitors |
-
2017
- 2017-07-11 PE PE2019000035A patent/PE20190624A1/es unknown
- 2017-07-11 CR CR20190063A patent/CR20190063A/es unknown
- 2017-07-11 CN CN201780050842.XA patent/CN109983001B/zh active Active
- 2017-07-11 PH PH1/2019/500056A patent/PH12019500056B1/en unknown
- 2017-07-11 TN TNP/2019/000010A patent/TN2019000010A1/en unknown
- 2017-07-11 MX MX2019000548A patent/MX395351B/es unknown
- 2017-07-11 TW TW106123173A patent/TWI806832B/zh active
- 2017-07-11 EP EP17742609.5A patent/EP3484856B1/en active Active
- 2017-07-11 KR KR1020237037794A patent/KR20230156174A/ko active Pending
- 2017-07-11 TW TW112121134A patent/TW202413340A/zh unknown
- 2017-07-11 JP JP2019522611A patent/JP6916279B2/ja active Active
- 2017-07-11 CN CN202310268752.5A patent/CN116478131A/zh active Pending
- 2017-07-11 CA CA3030167A patent/CA3030167A1/en active Pending
- 2017-07-11 IL IL264186A patent/IL264186B2/en unknown
- 2017-07-11 MY MYPI2018003070A patent/MY199046A/en unknown
- 2017-07-11 EP EP23209237.9A patent/EP4302834A3/en active Pending
- 2017-07-11 KR KR1020197004088A patent/KR102598895B1/ko active Active
- 2017-07-11 WO PCT/US2017/041577 patent/WO2018013597A1/en not_active Ceased
- 2017-07-11 SG SG11201900157RA patent/SG11201900157RA/en unknown
- 2017-07-11 CN CN202310285469.3A patent/CN116478132A/zh active Pending
- 2017-07-11 AU AU2017296289A patent/AU2017296289A1/en not_active Abandoned
- 2017-07-11 MA MA045660A patent/MA45660A/fr unknown
-
2018
- 2018-12-20 US US16/228,324 patent/US10590090B2/en active Active
-
2019
- 2019-01-08 DO DO2019000005A patent/DOP2019000005A/es unknown
- 2019-01-11 CL CL2019000090A patent/CL2019000090A1/es unknown
- 2019-01-11 MX MX2022007607A patent/MX2022007607A/es unknown
- 2019-01-22 CO CONC2019/0000613A patent/CO2019000613A2/es unknown
- 2019-02-12 EC ECSENADI201910079A patent/ECSP19010079A/es unknown
-
2020
- 2020-06-18 US US16/905,884 patent/US11661401B2/en active Active
-
2021
- 2021-07-15 JP JP2021116788A patent/JP7416740B2/ja active Active
- 2021-11-30 AU AU2021277664A patent/AU2021277664B2/en active Active
-
2023
- 2023-03-21 US US18/124,352 patent/US20240116878A1/en active Pending
- 2023-10-13 JP JP2023177195A patent/JP2024009957A/ja active Pending
- 2023-11-16 AU AU2023266357A patent/AU2023266357A1/en not_active Abandoned
-
2024
- 2024-03-21 IL IL311645A patent/IL311645B2/en unknown
-
2025
- 2025-06-26 IL IL321811A patent/IL321811A/en unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CL2019000090A1 (es) | 3-metil pirazinas 2,5-disustituidas y 3-metil pirazinas 2,5,6-trisustituidas como inhibidores alostéricos de shp2. | |
| SV2017005426A (es) | Derivados de feniltriazol sustituido con hidroxialquilo y sus usos | |
| CL2019001292A1 (es) | Nuevos derivados de quinolina. | |
| CL2019000230A1 (es) | Composiciones y métodos de inhibición del masp-3 para el tratamiento de diversas enfermedades y trastornos. | |
| CO2017001994A2 (es) | Compuestos activos hacia bromodominios | |
| CY1125205T1 (el) | Φαρμακευτικες συνθεσεις δραστικων απο θεραπευτικη αποψη ενωσεων | |
| CO2019000386A2 (es) | Compuestos heterocíclicos como inmunomoduladores | |
| CL2018001685A1 (es) | Compuestos heterociclicos como inmuno moduladores. | |
| CL2020000301A1 (es) | Nuevos derivados de quinolina. | |
| MX2018015252A (es) | Inhibidores de la interaccion de menina-leucemia de linaje mixto. | |
| CL2018002697A1 (es) | Moduladores alostéricos de receptores de acetilcolina nicotínicos. | |
| MX373045B (es) | Inhibidores de mdm2 y metodos terapeuticos que utilizan el mismo. | |
| SV2018005687A (es) | Derivados de dihidroimidazopirazinona usados en el tratamiento del cancer | |
| EA201791454A1 (ru) | Лекарственные формы для трансдермального введения | |
| MX2018004664A (es) | Antagonistas de ep4. | |
| CL2018001493A1 (es) | Nuevos derivados de fenilo | |
| CL2019002480A1 (es) | Derivados de pirazol como inhibidores de bromodominio. | |
| CL2020001062A1 (es) | Sulfonas y sulfóxidos bicíclicos y métodos de uso de los mismos. | |
| CO2017001601A2 (es) | Derivados de 1-acetil-4-((pirazin-2-il) amino)-1,2,3,4-tetrahydroquinolina-6 carboxamida como inhibidores de bromodominio | |
| MX2017013137A (es) | Derivados de cromeno como inhibidores de las fosfoinositido-3-cina sas. | |
| MX2018005987A (es) | Compuestos heterociclicos para el tratamiento de enfermedades. | |
| CO2017002813A2 (es) | Derivados estabilizados de adrenomedulina y uso de los mismos | |
| MX2018014790A (es) | Formulacion combinada de tres compuestos antivirales. | |
| MX380547B (es) | Composición que comprende un inhibidor de fgfr1/kdr micronizado y el uso del mismo en el tratamiento de tumores neuroendocrinos. | |
| UY36732A (es) | Piridin pirazinonas novedosas como inhibidores de bromodominios de la familia bet |