CR20190063A - 3-metil pirazinas 2,5-disustituídas y 3-metil pirazinas 2,5,6-trisustituídas como inhibidores alostéricos de shp2 - Google Patents
3-metil pirazinas 2,5-disustituídas y 3-metil pirazinas 2,5,6-trisustituídas como inhibidores alostéricos de shp2Info
- Publication number
- CR20190063A CR20190063A CR20190063A CR20190063A CR20190063A CR 20190063 A CR20190063 A CR 20190063A CR 20190063 A CR20190063 A CR 20190063A CR 20190063 A CR20190063 A CR 20190063A CR 20190063 A CR20190063 A CR 20190063A
- Authority
- CR
- Costa Rica
- Prior art keywords
- methyl pyrazines
- pyrazines
- methyl
- trisubstituted
- disubstituted
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- -1 2,5-disubstituted 3-methyl pyrazines Chemical class 0.000 title 2
- 230000003281 allosteric effect Effects 0.000 title 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
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
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)
- 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)
- 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)
Abstract
La presente divulgación se refiere a inhibidores de SHP2 y su uso en el tratamiento de enfermedades. También se divulgan composiciones farmacéuticas que los comprenden
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201662361249P | 2016-07-12 | 2016-07-12 | |
US201762449523P | 2017-01-23 | 2017-01-23 | |
PCT/US2017/041577 WO2018013597A1 (en) | 2016-07-12 | 2017-07-11 | 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
CR20190063A true CR20190063A (es) | 2019-05-27 |
Family
ID=59383648
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CR20190063A CR20190063A (es) | 2016-07-12 | 2017-07-11 | 3-metil pirazinas 2,5-disustituídas y 3-metil pirazinas 2,5,6-trisustituídas como inhibidores alostéricos de shp2 |
Country Status (22)
Country | Link |
---|---|
US (3) | US10590090B2 (es) |
EP (2) | EP3484856B1 (es) |
JP (3) | JP6916279B2 (es) |
KR (2) | KR102598895B1 (es) |
CN (3) | CN109983001B (es) |
AU (3) | AU2017296289A1 (es) |
BR (1) | BR112019000494A2 (es) |
CA (1) | CA3030167A1 (es) |
CL (1) | CL2019000090A1 (es) |
CO (1) | CO2019000613A2 (es) |
CR (1) | CR20190063A (es) |
DO (1) | DOP2019000005A (es) |
EC (1) | ECSP19010079A (es) |
IL (2) | IL311645A (es) |
MA (1) | MA45660A (es) |
MX (2) | MX2019000548A (es) |
PE (1) | PE20190624A1 (es) |
PH (1) | PH12019500056A1 (es) |
SG (1) | SG11201900157RA (es) |
TN (1) | TN2019000010A1 (es) |
TW (1) | TWI806832B (es) |
WO (1) | WO2018013597A1 (es) |
Families Citing this family (107)
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 |
WO2017210134A1 (en) | 2016-05-31 | 2017-12-07 | Board Of Regents, University Of Texas System | Heterocyclic inhibitors of ptpn11 |
WO2017211303A1 (en) | 2016-06-07 | 2017-12-14 | Jacobio Pharmaceuticals Co., Ltd. | Novel heterocyclic derivatives useful as shp2 inhibitors |
ES2810852T3 (es) | 2016-06-14 | 2021-03-09 | Novartis Ag | Compuestos y composiciones para inhibir la actividad de shp2 |
MX2019000548A (es) | 2016-07-12 | 2019-10-30 | 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 |
TW201819386A (zh) | 2016-10-24 | 2018-06-01 | 美商傳達治療有限公司 | Shp2磷酸酶抑制劑及其使用方法 |
AR110740A1 (es) | 2017-01-23 | 2019-05-02 | Revolution Medicines Inc | Compuestos bicíclicos como inhibidores alostéricos de shp2 |
EP3571189B1 (en) | 2017-01-23 | 2023-03-29 | Revolution Medicines, Inc. | Pyridine compounds as allosteric shp2 inhibitors |
EA202190196A1 (ru) * | 2017-03-23 | 2021-08-31 | Джакобио Фармасьютикалс Ко., Лтд. | Новые гетероциклические производные, применимые в качестве ингибиторов shp2 |
EP3630770A1 (en) | 2017-05-26 | 2020-04-08 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors |
EP3678703A1 (en) | 2017-09-07 | 2020-07-15 | Revolution Medicines, Inc. | Shp2 inhibitor compositions and methods for treating cancer |
JP7447002B2 (ja) | 2017-09-11 | 2024-03-11 | クルーゾン・ファーマシューティカルズ・インコーポレイテッド | SHP2のオクタヒドロシクロペンタ[c]ピロールのアロステリック阻害剤 |
EP3687997A1 (en) | 2017-09-29 | 2020-08-05 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors |
CA3078565A1 (en) | 2017-10-12 | 2019-04-18 | Revolution Medicines, Inc. | Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors |
MX2020006273A (es) | 2017-12-15 | 2020-09-14 | Revolution Medicines Inc | Compuestos policiclicos como inhibidores alostericos de shp2. |
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 |
MA51845A (fr) * | 2018-02-13 | 2020-12-23 | Shanghai Blueray Biopharma Co Ltd | Composé cyclique fusionné à une pyrimidine, son procédé de préparation et son application |
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 |
CA3094690A1 (en) * | 2018-03-21 | 2019-09-26 | Relay Therapeutics, Inc. | Shp2 phosphatase inhibitors and methods of use thereof |
KR20200144102A (ko) * | 2018-03-21 | 2020-12-28 | 신블리아 테라퓨틱스 인코포레이티드 | Shp2 억제제 및 이의 용도 |
CA3096535A1 (en) | 2018-04-10 | 2019-10-17 | Revolution Medicines, Inc. | Shp2 inhibitor compositions, methods for treating cancer and methods for identifying a subject with shp2 mutations |
KR102611661B1 (ko) | 2018-05-02 | 2023-12-08 | 나비레 파르마, 인코퍼레이티드 | Ptpn11의 치환된 헤테로사이클릭 억제제 |
JP2021534124A (ja) | 2018-08-10 | 2021-12-09 | ナビール ファーマ,インコーポレイティド | 癌治療用ptpn11(shp2)阻害剤としての6−(4−アミノ−3−メチル−2−オキサ−8−アザスピロ[4.5]デカン−8−イル)−3−(2,3−ジクロロフェニル)−2−メチルピリミジン−4(3h)−オン誘導体及び関連化合物 |
US20200115389A1 (en) * | 2018-09-18 | 2020-04-16 | Nikang Therapeutics, Inc. | Fused tricyclic ring 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 |
WO2020065452A1 (en) * | 2018-09-29 | 2020-04-02 | Novartis Ag | Manufacture of compounds and compositions for inhibiting the activity of shp2 |
US11179397B2 (en) | 2018-10-03 | 2021-11-23 | Gilead Sciences, Inc. | Imidazopyrimidine derivatives |
JP2022508651A (ja) * | 2018-10-08 | 2022-01-19 | レヴォリューション・メディスンズ,インコーポレイテッド | 癌を処置するためのshp2阻害剤組成物および方法 |
TW202028183A (zh) * | 2018-10-10 | 2020-08-01 | 大陸商江蘇豪森藥業集團有限公司 | 含氮雜芳類衍生物調節劑、其製備方法和應用 |
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 |
EP3889153A4 (en) | 2018-11-30 | 2022-09-07 | Tuojie Biotech (Shanghai) Co., Ltd. | PYRIMIDINE AND PENTAGONAL HETEROCYCLE DERIVATIVE OF NITROGEN, METHOD FOR THE PREPARATION AND MEDICAL APPLICATIONS |
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 |
EP3930845A1 (en) | 2019-03-01 | 2022-01-05 | Revolution Medicines, Inc. | Bicyclic heterocyclyl compounds and uses thereof |
KR20210146287A (ko) | 2019-03-01 | 2021-12-03 | 레볼루션 메디슨즈, 인크. | 이환식 헤테로아릴 화합물 및 이의 용도 |
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 |
CA3135555C (en) | 2019-04-02 | 2023-09-19 | Array Biopharma Inc. | Protein tyrosine phosphatase inhibitors |
US11001561B2 (en) | 2019-04-08 | 2021-05-11 | Merck Patent Gmbh | Pyrimidinone derivatives as SHP2 antagonists |
TW202112785A (zh) | 2019-06-07 | 2021-04-01 | 美商銳新醫藥公司 | Shp2抑制劑的固體形式 |
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 |
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 |
EP4034539A1 (en) | 2019-09-24 | 2022-08-03 | Relay Therapeutics, Inc. | Shp2 phosphatase inhibitors and methods of making and using the same |
CN112724145A (zh) * | 2019-10-14 | 2021-04-30 | 杭州雷索药业有限公司 | 用于抑制shp2活性的吡嗪衍生物 |
EP4045047A1 (en) | 2019-10-15 | 2022-08-24 | Amgen Inc. | Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers |
WO2021091967A1 (en) | 2019-11-04 | 2021-05-14 | Revolution Medicines, Inc. | Ras inhibitors |
TW202132316A (zh) | 2019-11-04 | 2021-09-01 | 美商銳新醫藥公司 | Ras抑制劑 |
KR20220109407A (ko) | 2019-11-04 | 2022-08-04 | 레볼루션 메디슨즈, 인크. | Ras 억제제 |
JP2023500328A (ja) | 2019-11-08 | 2023-01-05 | レボリューション メディシンズ インコーポレイテッド | 二環式ヘテロアリール化合物及びその使用 |
EP4065231A1 (en) | 2019-11-27 | 2022-10-05 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
US20230034584A1 (en) | 2019-12-04 | 2023-02-02 | Bayer Aktiengesellschaft | Inhibitors of shp2 |
IL294484A (en) | 2020-01-07 | 2022-09-01 | Revolution Medicines Inc | Dosage for shp2 inhibitor and methods for treating cancer |
EP4092019A4 (en) | 2020-01-16 | 2024-02-28 | Zhejiang Hisun Pharmaceutical Co., Ltd. | HETEROARYL DERIVATIVE, PROCESS THEREOF AND USE THEREOF |
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 |
CN114846005B (zh) * | 2020-01-21 | 2024-04-02 | 贝达药业股份有限公司 | Shp2抑制剂及其应用 |
CA3173358A1 (en) | 2020-02-28 | 2021-09-02 | Novartis Ag | A triple pharmaceutical combination comprising dabrafenib, an erk inhibitor and a shp2 inhibitor |
CN113493440A (zh) * | 2020-04-03 | 2021-10-12 | 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 |
WO2021218752A1 (en) * | 2020-04-26 | 2021-11-04 | Betta Pharmaceuticals Co., Ltd | Shp2 inhibitors, compositions and uses thereof |
CA3183032A1 (en) | 2020-06-18 | 2021-12-23 | Mallika Singh | Methods for delaying, preventing, and treating acquired resistance to ras inhibitors |
WO2021259077A1 (zh) | 2020-06-22 | 2021-12-30 | 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 |
CN116113418A (zh) * | 2020-08-25 | 2023-05-12 | 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 |
CA3187757A1 (en) | 2020-09-03 | 2022-03-24 | Ethan AHLER | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
CA3194067A1 (en) | 2020-09-15 | 2022-03-24 | Revolution Medicines, Inc. | Ras inhibitors |
EP4237086A1 (en) | 2020-10-27 | 2023-09-06 | Amgen Inc. | Heterocyclic spiro compounds and methods of use |
IL303782A (en) * | 2020-12-18 | 2023-08-01 | Genzyme Corp | Preparation process of SHP2 inhibitors |
EP4267250A1 (en) | 2020-12-22 | 2023-11-01 | Qilu Regor Therapeutics Inc. | Sos1 inhibitors and uses thereof |
CN116568308A (zh) * | 2021-01-29 | 2023-08-08 | 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 |
WO2022206684A1 (zh) * | 2021-03-31 | 2022-10-06 | 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 |
WO2022232332A1 (en) | 2021-04-29 | 2022-11-03 | Amgen Inc. | 2-aminobenzothiazole compounds and methods of use thereof |
CN117616031A (zh) | 2021-05-05 | 2024-02-27 | 锐新医药公司 | 用于治疗癌症的ras抑制剂 |
CN117500811A (zh) | 2021-05-05 | 2024-02-02 | 锐新医药公司 | 共价ras抑制剂及其用途 |
CA3217097A1 (en) * | 2021-05-05 | 2022-11-10 | 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 |
IL308193A (en) | 2021-05-05 | 2024-01-01 | Revolution Medicines Inc | RAS inhibitors |
JP2024517965A (ja) * | 2021-05-13 | 2024-04-23 | 中国科学院上海薬物研究所 | Shp2活性を阻害する複素環化合物、その製造方法および使用 |
JP2024519098A (ja) | 2021-05-21 | 2024-05-08 | 石薬集団中奇制薬技術(石家庄)有限公司 | スピロ系化合物およびその使用 |
TW202313041A (zh) | 2021-06-09 | 2023-04-01 | 瑞士商諾華公司 | 包含達拉菲尼、曲美替尼和shp2抑制劑之三重藥物組合 |
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 |
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 |
EP4385991A1 (en) * | 2021-08-09 | 2024-06-19 | Ubix Therapeutics, Inc. | Compound having shp2 protein degrading activity, and medical uses thereof |
IL309086A (en) | 2021-09-01 | 2024-02-01 | Novartis Ag | Pharmaceutical combinations involving a tonic inhibitor and its uses for the treatment of cancer |
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 |
WO2023122938A1 (en) * | 2021-12-28 | 2023-07-06 | Js Innomed Holdings Ltd. | Heterocyclic compounds as shp2 inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof |
WO2023159087A1 (en) | 2022-02-16 | 2023-08-24 | Amgen Inc. | Quinazoline compounds and use thereof as inhibtors of mutant kras proteins |
WO2023159086A1 (en) | 2022-02-16 | 2023-08-24 | Amgen Inc. | Quinazoline compounds and use thereof as inhibtors of mutant kras proteins |
WO2023168036A1 (en) | 2022-03-04 | 2023-09-07 | Eli Lilly And Company | Method of treatment including kras g12c inhibitors and shp2 inhibitors |
WO2023172940A1 (en) | 2022-03-08 | 2023-09-14 | Revolution Medicines, Inc. | Methods for treating immune refractory lung cancer |
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 |
WO2023180245A1 (en) | 2022-03-21 | 2023-09-28 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of shp2 inhibitors for inhibiting senescence |
WO2023192112A1 (en) * | 2022-03-28 | 2023-10-05 | Genzyme Corporation | Process for preparing shp2 inhibitors |
US11878958B2 (en) | 2022-05-25 | 2024-01-23 | Ikena Oncology, Inc. | MEK inhibitors and uses thereof |
WO2023240263A1 (en) | 2022-06-10 | 2023-12-14 | 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 |
Family Cites Families (118)
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 |
WO1993009664A1 (en) | 1991-11-12 | 1993-05-27 | Nippon Soda Co., Ltd. | 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 |
CA2233285C (en) | 1996-02-07 | 2006-07-04 | Janssen Pharmaceutica N.V. | Pyrazolopyrimidines as crf receptor antagonists |
CA2293400A1 (en) * | 1997-06-13 | 1998-12-17 | Gerald Mcmahon | Novel heteroaryl compounds for the modulation of protein tyrosine enzyme related cellular signal transduction |
AU775625B2 (en) | 1999-08-27 | 2004-08-05 | Sugen, Inc. | Phosphate mimics and methods of treatment using phosphatase inhibitors |
DE60114153T2 (de) | 2000-02-16 | 2006-07-06 | Neurogen Corp., Branford | Substituierte arylpyrazine |
US7335469B2 (en) | 2001-10-01 | 2008-02-26 | Mt. Sinai School Of Medicine Of New York University | Methods for diagnosing Noonan syndrome |
US6921762B2 (en) | 2001-11-16 | 2005-07-26 | Amgen Inc. | Substituted indolizine-like compounds and methods of use |
DE60234269D1 (de) | 2001-11-21 | 2009-12-17 | Pharmacia & Upjohn Co Llc | Substituierte aryl 1,4-pyrazin derivate |
CA2479744A1 (en) | 2002-03-28 | 2003-10-09 | Paul E. Finke | Substituted 2,3-diphenyl pyridines |
US20040116444A1 (en) | 2002-09-12 | 2004-06-17 | Corbett Jeffrey W. | Substituted 1,4-pyrazine derivatives |
EP1576014B1 (en) | 2002-12-23 | 2011-06-29 | Wyeth LLC | Antibodies against pd-1 and uses thereof |
US7157460B2 (en) | 2003-02-20 | 2007-01-02 | Sugen Inc. | Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors |
CA2524519A1 (en) | 2003-05-09 | 2004-11-18 | 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 |
AU2004274403A1 (en) | 2003-09-03 | 2005-03-31 | Aventis Pharmaceuticals Inc. | 5-aryl-Pyrazolo(4,3-d)pyrimidines, pyridines, and pyrazines and related compounds |
JP2007508290A (ja) | 2003-10-10 | 2007-04-05 | ファイザー・プロダクツ・インク | GSK−3阻害剤としての置換2H−[1,2,4]トリアゾロ[4,3−a]ピラジン |
CA2543644A1 (en) * | 2003-10-27 | 2005-05-06 | Astellas Pharma Inc. | Pyrazine derivatives and pharmaceutical use thereof |
WO2005095384A1 (en) * | 2004-04-01 | 2005-10-13 | Astellas Pharma Inc. | Pyrazine derivatives and pharmaceutical use thereof as adenosine antagonists |
DE102004015954A1 (de) * | 2004-04-01 | 2005-11-10 | Ina-Schaeffler Kg | Umschlingungstrieb |
WO2006002284A1 (en) | 2004-06-22 | 2006-01-05 | Rigel Pharmaceuticals, Inc. | Ubiquitin ligase inhibitors |
CA2592021A1 (en) | 2004-12-23 | 2006-07-06 | Raghavan Rajagopalan | Fluorescent pyrazine derivatives and methods of using the same in assessing renal function |
AU2006236387A1 (en) * | 2005-04-18 | 2006-10-26 | Neurogen Corporation | Subtituted heteroaryl CB1 antagonists |
CN102603581B (zh) | 2005-06-22 | 2015-06-24 | 普莱希科公司 | 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物 |
NZ568385A (en) | 2005-10-21 | 2012-07-27 | Univ California | C-kit oncogene mutations in melanoma |
AU2006340061A1 (en) | 2006-02-24 | 2007-09-20 | Mallinckrodt Llc | Process for using optical agents |
US8987474B2 (en) | 2006-04-07 | 2015-03-24 | University Of South Florida | Inhibition of Shp2/PTPN11 protein tyrosine phosphatase by NSC-87877, NSC-117199 and their analogs |
JP2009535344A (ja) | 2006-04-28 | 2009-10-01 | ノースウェスタン ユニバーシティ | 神経炎症性疾患の処置のためのピリダジン化合物を含む処方物 |
US7893058B2 (en) | 2006-05-15 | 2011-02-22 | Janssen Pharmaceutica Nv | Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases |
EA200870592A1 (ru) | 2006-05-31 | 2009-08-28 | Галапагос Н.В. | Триазолопиразиновые соединения, пригодные для лечения дегенеративных и воспалительных заболеваний |
AR061229A1 (es) | 2006-06-06 | 2008-08-13 | Schering Corp | Imidazopirazinas como inhibidores de la proteina quinasa |
CN101687040A (zh) * | 2007-03-01 | 2010-03-31 | 马林克罗特公司 | 整合光活性的小分子及其用途 |
EP2144909B1 (en) | 2007-04-06 | 2011-03-23 | Novartis AG | [2,6]naphthyridines useful as protein kinase inhibitors |
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 |
US20100190980A1 (en) | 2007-06-21 | 2010-07-29 | Taisho Pharmaceutical Co., Ltd | Pyrazinamide compound |
JP2010535769A (ja) | 2007-08-09 | 2010-11-25 | メルク・シャープ・エンド・ドーム・コーポレイション | ピリジンカルボキサミドオレキシン受容体アンタゴニスト |
WO2009025823A1 (en) | 2007-08-21 | 2009-02-26 | Amgen Inc. | Phosphodiesterase 10 inhibitors |
US9174969B2 (en) | 2008-07-21 | 2015-11-03 | University Of South Florida | Indoline scaffold SHP-2 inhibitors and cancer treatment method |
JP2012507540A (ja) | 2008-10-30 | 2012-03-29 | メルク・シャープ・エンド・ドーム・コーポレイション | ピリダジンカルボキサミド・オレキシン受容体アンタゴニスト |
HUE026315T2 (en) | 2009-01-23 | 2016-06-28 | Rigel Pharmaceuticals Inc | Preparations and methods for inhibiting the JAK pathway |
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 |
US20120065205A1 (en) | 2009-06-01 | 2012-03-15 | Mercer Swati P | 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 |
EP2473530B1 (en) | 2009-09-03 | 2015-04-22 | 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 |
BR112012022046A2 (pt) | 2010-03-05 | 2017-02-14 | F Hoffamann-La Roche Ag | ''anticorpo,composição farmacêutica,ácido nucleico ,vetores de expressão,célula hospedeira e método para a produção de um anticorpo recombinante''. |
AR081908A1 (es) | 2010-05-11 | 2012-10-31 | Sanofi Aventis | N-heteroaril-espirolactama-bipirrolidinas sustituidas, preparacion y usos terapeuticos de las mismas |
US8703768B2 (en) * | 2010-06-09 | 2014-04-22 | Hoffmann-La Roche Inc. | Nitrogen containing heteroaryl compounds |
ES2622519T3 (es) * | 2010-07-14 | 2017-07-06 | Novartis Ag | Componentes heterocíclicos agonistas del receptor IP |
GB201106829D0 (en) * | 2011-04-21 | 2011-06-01 | Proximagen Ltd | Heterocyclic compounds |
JP5808826B2 (ja) | 2011-02-23 | 2015-11-10 | インテリカイン, エルエルシー | 複素環化合物およびその使用 |
US20120330012A1 (en) | 2011-04-29 | 2012-12-27 | 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 |
EP2802583A1 (en) * | 2012-01-13 | 2014-11-19 | Novartis AG | Fused piperidines as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders |
ES2613399T3 (es) * | 2012-01-17 | 2017-05-24 | Astellas Pharma Inc. | Compuesto de pirazincarboxamida |
WO2014023385A1 (en) | 2012-08-07 | 2014-02-13 | Merck Patent Gmbh | Pyridopyrimidine derivatives as protein kinase inhibitors |
RU2617842C2 (ru) | 2012-11-08 | 2017-04-28 | Пфайзер Инк. | Гетероароматические соединения и их применение в качестве допаминовых D1 лигандов |
ES2681593T3 (es) | 2012-11-29 | 2018-09-14 | Chemocentryx, Inc. | Antagonistas de CXCR7 |
US20150352131A1 (en) | 2013-01-16 | 2015-12-10 | Rhode Island Hospital | Compositions and Methods for the Prevention and Treatment of Osteolysis and Osteoporosis |
US20150374687A1 (en) * | 2013-02-07 | 2015-12-31 | Merck Patent Gmbh | Substituted quinoxaline derivatives and their use as positive allosteric modulators of mglur4 |
CN105358576B (zh) | 2013-02-20 | 2020-05-05 | 诺华股份有限公司 | 使用人源化抗EGFRvIII嵌合抗原受体治疗癌症 |
AU2014248515B2 (en) | 2013-03-13 | 2019-03-07 | 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 |
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 |
US10093646B2 (en) * | 2014-01-17 | 2018-10-09 | Novartis Ag | 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and compositions thereof for inhibiting the activity of 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 |
AU2015295405B2 (en) | 2014-08-01 | 2020-04-09 | Nuevolution A/S | Compounds active towards bromodomains |
WO2016081290A1 (en) * | 2014-11-18 | 2016-05-26 | Merck Sharp & Dohme Corp. | Aminopyrazine compounds with a2a antagonist properties |
US20170362305A1 (en) | 2014-12-17 | 2017-12-21 | Siemens Healthcare Diagnostics Inc. | Sandwich assay design for small molecules |
MY186837A (en) | 2014-12-23 | 2021-08-25 | Novartis Ag | Triazolopyrimidine compounds and uses thereof |
US10533016B2 (en) | 2015-01-09 | 2020-01-14 | Revolution Medicines, Inc. | Compounds that participate in cooperative binding and uses thereof |
ES2757948T3 (es) | 2015-04-03 | 2020-04-30 | Incyte Corp | Compuestos heterocíclicos como inhibidores LSD1 |
CN112625028A (zh) * | 2015-06-19 | 2021-04-09 | 诺华股份有限公司 | 用于抑制shp2活性的化合物和组合物 |
EP3310779B1 (en) | 2015-06-19 | 2019-05-08 | Novartis AG | Compounds and compositions for inhibiting the activity of shp2 |
US10308660B2 (en) | 2015-06-19 | 2019-06-04 | 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 |
US11008372B2 (en) | 2015-11-07 | 2021-05-18 | 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 |
WO2017211303A1 (en) | 2016-06-07 | 2017-12-14 | Jacobio Pharmaceuticals Co., Ltd. | Novel heterocyclic derivatives useful as shp2 inhibitors |
ES2810852T3 (es) | 2016-06-14 | 2021-03-09 | Novartis Ag | Compuestos y composiciones para inhibir la actividad de shp2 |
MX2019000548A (es) | 2016-07-12 | 2019-10-30 | 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 |
TW201819386A (zh) | 2016-10-24 | 2018-06-01 | 美商傳達治療有限公司 | Shp2磷酸酶抑制劑及其使用方法 |
EP3568204B1 (en) | 2017-01-10 | 2023-08-30 | Novartis AG | Pharmaceutical combination comprising an alk inhibitor and an shp2 inhibitor |
EP3571189B1 (en) | 2017-01-23 | 2023-03-29 | Revolution Medicines, Inc. | Pyridine compounds as allosteric shp2 inhibitors |
AR110740A1 (es) | 2017-01-23 | 2019-05-02 | Revolution Medicines Inc | Compuestos bicíclicos como inhibidores alostéricos de shp2 |
EA202190196A1 (ru) | 2017-03-23 | 2021-08-31 | Джакобио Фармасьютикалс Ко., Лтд. | Новые гетероциклические производные, применимые в качестве ингибиторов shp2 |
US20200199102A1 (en) | 2017-04-05 | 2020-06-25 | Revolution Medicines, Inc. | Compounds that participate in cooperative binding and uses thereof |
BR112019020967A2 (pt) | 2017-04-05 | 2020-05-05 | Revolution Medicines Inc | métodos e reagentes para analisar interfaces de proteína-proteína |
EP3630770A1 (en) | 2017-05-26 | 2020-04-08 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors |
EP3678703A1 (en) | 2017-09-07 | 2020-07-15 | Revolution Medicines, Inc. | Shp2 inhibitor compositions and methods for treating cancer |
CA3078565A1 (en) | 2017-10-12 | 2019-04-18 | Revolution Medicines, Inc. | Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors |
MX2020006273A (es) | 2017-12-15 | 2020-09-14 | Revolution Medicines Inc | Compuestos policiclicos como inhibidores alostericos de shp2. |
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 |
MA51845A (fr) | 2018-02-13 | 2020-12-23 | Shanghai Blueray Biopharma Co Ltd | Composé cyclique fusionné à une pyrimidine, son procédé de préparation et son application |
KR20200144102A (ko) | 2018-03-21 | 2020-12-28 | 신블리아 테라퓨틱스 인코포레이티드 | Shp2 억제제 및 이의 용도 |
CA3096535A1 (en) | 2018-04-10 | 2019-10-17 | Revolution Medicines, Inc. | Shp2 inhibitor compositions, methods for treating cancer and methods for identifying a subject with shp2 mutations |
SG11202010560QA (en) | 2018-05-01 | 2020-11-27 | Revolution Medicines Inc | C26-linked rapamycin analogs as mtor inhibitors |
SG11202010559UA (en) | 2018-05-01 | 2020-11-27 | Revolution Medicines Inc | C40-, c28-, and c-32-linked rapamycin analogs as mtor inhibitors |
CA3111980A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
US20200115389A1 (en) | 2018-09-18 | 2020-04-16 | Nikang Therapeutics, Inc. | Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors |
JP2022508651A (ja) | 2018-10-08 | 2022-01-19 | レヴォリューション・メディスンズ,インコーポレイテッド | 癌を処置するためのshp2阻害剤組成物および方法 |
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 |
CN113498342A (zh) | 2018-12-21 | 2021-10-12 | 锐新医药公司 | 参与协同结合的化合物和其用途 |
WO2021091967A1 (en) | 2019-11-04 | 2021-05-14 | Revolution Medicines, Inc. | Ras inhibitors |
-
2017
- 2017-07-11 MX MX2019000548A patent/MX2019000548A/es unknown
- 2017-07-11 MA MA045660A patent/MA45660A/fr unknown
- 2017-07-11 CA CA3030167A patent/CA3030167A1/en active Pending
- 2017-07-11 CN CN201780050842.XA patent/CN109983001B/zh active Active
- 2017-07-11 WO PCT/US2017/041577 patent/WO2018013597A1/en unknown
- 2017-07-11 AU AU2017296289A patent/AU2017296289A1/en not_active Abandoned
- 2017-07-11 JP JP2019522611A patent/JP6916279B2/ja active Active
- 2017-07-11 IL IL311645A patent/IL311645A/en unknown
- 2017-07-11 CN CN202310268752.5A patent/CN116478131A/zh active Pending
- 2017-07-11 CR CR20190063A patent/CR20190063A/es unknown
- 2017-07-11 KR KR1020197004088A patent/KR102598895B1/ko active IP Right Grant
- 2017-07-11 IL IL264186A patent/IL264186B1/en unknown
- 2017-07-11 BR BR112019000494-7A patent/BR112019000494A2/pt unknown
- 2017-07-11 KR KR1020237037794A patent/KR20230156174A/ko active Application Filing
- 2017-07-11 TN TNP/2019/000010A patent/TN2019000010A1/en unknown
- 2017-07-11 EP EP17742609.5A patent/EP3484856B1/en active Active
- 2017-07-11 TW TW106123173A patent/TWI806832B/zh active
- 2017-07-11 PE PE2019000035A patent/PE20190624A1/es unknown
- 2017-07-11 EP EP23209237.9A patent/EP4302834A2/en active Pending
- 2017-07-11 SG SG11201900157RA patent/SG11201900157RA/en unknown
- 2017-07-11 CN CN202310285469.3A patent/CN116478132A/zh active Pending
-
2018
- 2018-12-20 US US16/228,324 patent/US10590090B2/en active Active
-
2019
- 2019-01-08 DO DO2019000005A patent/DOP2019000005A/es unknown
- 2019-01-09 PH PH12019500056A patent/PH12019500056A1/en 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 active Pending
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
CO2019000613A2 (es) | 3-metil pirazinas 2,5-disustituidas y 3-metil pirazinas 2,5,6-trisustituidas como inhibidores alostéricos de shp2 | |
CO2020003714A2 (es) | Compuestos de piridina, pirazina, y triazina como inhibidores de shp2 alostéricos | |
CO2020005887A2 (es) | Compuestos policíclicos como inhibidores alostéricos de shp2 | |
CY1121413T1 (el) | Διυδροπυρρολοπυριδινης αναστολεις ror-γαμμα | |
CL2018001624A1 (es) | Antagonistas policíclicos del tlr7/8 y uso de los mismos en el tratamiento de trastornos inmunitarios | |
DOP2017000109A (es) | Derivados de feniltriazol sustituido con hidroxialquilo y sus usos | |
CO2017001994A2 (es) | Compuestos activos hacia bromodominios | |
CR20170563A (es) | Compuestos de benzoxacepina oxazolidinona y métodos de uso. | |
SV2018005687A (es) | Derivados de dihidroimidazopirazinona usados en el tratamiento del cancer | |
NI201600018A (es) | Derivados de pirrolamida sustituidos con glioxamida y su uso como medicamentos para el tratamiento de la hepatitis b. | |
NI201500059A (es) | Inhibidores de la tirosina-quinasa de bruton | |
CR20160203A (es) | Inhibidores de tirosina cinasa de bruton | |
BR112015022545A2 (pt) | compostos de pirazolo e os usos disso | |
BR112016028845A2 (pt) | composto, composição farmacêutica e uso de um composto | |
GT201500235A (es) | Estra -1,3,5 (10) , 16- tetraeno -3-carboxamidas para la inhibicion de la 17b-hidroxiesteroide deshidrogenasa (akr1c3) | |
BR112017009012A2 (pt) | derivados de anel benzo de seis membros como inibidor de dpp-4 e seu uso | |
CL2018001493A1 (es) | Nuevos derivados de fenilo | |
CO2017001601A2 (es) | Derivados de 1-acetil-4-((pirazin-2-il) amino)-1,2,3,4-tetrahydroquinolina-6 carboxamida como inhibidores de bromodominio | |
CR20180091A (es) | 5-(n-bencil-tetrahidroisoquinolin-6-il)-piridin-3-il acético como inhibidores de la replicación del vih | |
EA201890075A1 (ru) | Инъецируемые фармацевтические композиции лефамулина | |
CL2019002480A1 (es) | Derivados de pirazol como inhibidores de bromodominio. | |
MX2018014790A (es) | Formulacion combinada de tres compuestos antivirales. | |
CO2019007671A2 (es) | Una composición farmacéutica que comprende un derivado de oxazina y su uso en el tratamiento o la prevención de la enfermedad de alzheimer | |
CL2018002848A1 (es) | Formulaciones liquidas de fosfoplatino | |
BR112019017314A2 (pt) | composições farmacêuticas para terapia de combinação |