JP2019517487A5 - - Google Patents
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- JP2019517487A5 JP2019517487A5 JP2018562312A JP2018562312A JP2019517487A5 JP 2019517487 A5 JP2019517487 A5 JP 2019517487A5 JP 2018562312 A JP2018562312 A JP 2018562312A JP 2018562312 A JP2018562312 A JP 2018562312A JP 2019517487 A5 JP2019517487 A5 JP 2019517487A5
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- JP
- Japan
- Prior art keywords
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- compound
- alkyl
- hydroxy
- halo
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 150000001875 compounds Chemical class 0.000 claims 39
- 125000000217 alkyl group Chemical group 0.000 claims 25
- 125000005843 halogen group Chemical group 0.000 claims 22
- 239000008194 pharmaceutical composition Substances 0.000 claims 18
- 125000003118 aryl group Chemical group 0.000 claims 16
- 229910052799 carbon Inorganic materials 0.000 claims 16
- 125000001072 heteroaryl group Chemical group 0.000 claims 16
- 125000003282 alkyl amino group Chemical group 0.000 claims 14
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 14
- 125000003545 alkoxy group Chemical group 0.000 claims 13
- 125000004093 cyano group Chemical group *C#N 0.000 claims 13
- 125000004103 aminoalkyl group Chemical group 0.000 claims 12
- 125000005842 heteroatom Chemical group 0.000 claims 11
- 229910052760 oxygen Inorganic materials 0.000 claims 11
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 11
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- -1 hydroxy, amino Chemical group 0.000 claims 10
- 229910052757 nitrogen Inorganic materials 0.000 claims 10
- 229910052717 sulfur Inorganic materials 0.000 claims 10
- 201000010099 disease Diseases 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 9
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 9
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 8
- 125000004663 dialkyl amino group Chemical group 0.000 claims 8
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 6
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 101001087416 Homo sapiens Tyrosine-protein phosphatase non-receptor type 11 Proteins 0.000 claims 5
- 102100033019 Tyrosine-protein phosphatase non-receptor type 11 Human genes 0.000 claims 5
- 125000003368 amide group Chemical group 0.000 claims 5
- 150000001721 carbon Chemical group 0.000 claims 5
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 208000026310 Breast neoplasm Diseases 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 3
- 208000005101 LEOPARD Syndrome Diseases 0.000 claims 3
- 206010062901 Multiple lentigines syndrome Diseases 0.000 claims 3
- 206010029748 Noonan syndrome Diseases 0.000 claims 3
- 208000010708 Noonan syndrome with multiple lentigines Diseases 0.000 claims 3
- 208000029742 colonic neoplasm Diseases 0.000 claims 3
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 3
- 208000032839 leukemia Diseases 0.000 claims 3
- 201000001441 melanoma Diseases 0.000 claims 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 230000001668 ameliorated effect Effects 0.000 claims 1
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 0 C*#CC(CCC1)C1(CC1)CCN1c1cnc(c(-c(ccnc2)c2Cl)n[n]2)c2n1 Chemical compound C*#CC(CCC1)C1(CC1)CCN1c1cnc(c(-c(ccnc2)c2Cl)n[n]2)c2n1 0.000 description 3
- IEUPVYYCTFCLTF-UHFFFAOYSA-N CC(CC1)(CCN1c1cnc(c(-c(cc2)cc(Cl)c2Cl)n[nH]2)c2n1)N Chemical compound CC(CC1)(CCN1c1cnc(c(-c(cc2)cc(Cl)c2Cl)n[nH]2)c2n1)N IEUPVYYCTFCLTF-UHFFFAOYSA-N 0.000 description 1
- QKNOZCPUZKQEHX-UHFFFAOYSA-N CC(CC1)(CCN1c1cnc(c(-c2cccc(F)c2Cl)n[nH]2)c2n1)N Chemical compound CC(CC1)(CCN1c1cnc(c(-c2cccc(F)c2Cl)n[nH]2)c2n1)N QKNOZCPUZKQEHX-UHFFFAOYSA-N 0.000 description 1
- FIDMRKBBOFQQJM-UHFFFAOYSA-N CC(CC1)(CCN1c1nc(N)c(C(c(cccn2)c2Cl)=N)nc1)N Chemical compound CC(CC1)(CCN1c1nc(N)c(C(c(cccn2)c2Cl)=N)nc1)N FIDMRKBBOFQQJM-UHFFFAOYSA-N 0.000 description 1
- HILFUTGZGNSLCF-UHFFFAOYSA-N CC(CC1)(CCN1c1nc([nH]nc2-c(cc3)cc(Cl)c3F)c2nc1)N Chemical compound CC(CC1)(CCN1c1nc([nH]nc2-c(cc3)cc(Cl)c3F)c2nc1)N HILFUTGZGNSLCF-UHFFFAOYSA-N 0.000 description 1
- MGGGLWKKMYVXPD-UHFFFAOYSA-N CC(CC1)(CCN1c1nc([nH]nc2-c(cc3)ccc3Cl)c2nc1)N Chemical compound CC(CC1)(CCN1c1nc([nH]nc2-c(cc3)ccc3Cl)c2nc1)N MGGGLWKKMYVXPD-UHFFFAOYSA-N 0.000 description 1
- JQWPQEJDTUKOCS-UHFFFAOYSA-N CC(CC1)(CCN1c1nc([nH]nc2-c(cccc3)c3Cl)c2nc1)N Chemical compound CC(CC1)(CCN1c1nc([nH]nc2-c(cccc3)c3Cl)c2nc1)N JQWPQEJDTUKOCS-UHFFFAOYSA-N 0.000 description 1
- HXKDFUSJAFLWKF-UHFFFAOYSA-N CC(CN)(CC1)CCN1c1cnc(c(-c(cc2)cc(Cl)c2F)n[nH]2)c2n1 Chemical compound CC(CN)(CC1)CCN1c1cnc(c(-c(cc2)cc(Cl)c2F)n[nH]2)c2n1 HXKDFUSJAFLWKF-UHFFFAOYSA-N 0.000 description 1
- BHDQDMSKLZFAOP-UHFFFAOYSA-N CC(CN)(CC1)CCN1c1nc([nH]nc2-c(cc3)ccc3Cl)c2nc1 Chemical compound CC(CN)(CC1)CCN1c1nc([nH]nc2-c(cc3)ccc3Cl)c2nc1 BHDQDMSKLZFAOP-UHFFFAOYSA-N 0.000 description 1
- VBWUNPVCLSZAAP-UHFFFAOYSA-N CC(CN)(CC1)CCN1c1nc([nH]nc2-c3cc(C(F)(F)F)ccc3)c2nc1 Chemical compound CC(CN)(CC1)CCN1c1nc([nH]nc2-c3cc(C(F)(F)F)ccc3)c2nc1 VBWUNPVCLSZAAP-UHFFFAOYSA-N 0.000 description 1
- DEVWTTPPKFBRGL-UHFFFAOYSA-N Clc(cccc1)c1-c1n[nH]c2c1ncc(N1CCC3(CCCC3)CC1)n2 Chemical compound Clc(cccc1)c1-c1n[nH]c2c1ncc(N1CCC3(CCCC3)CC1)n2 DEVWTTPPKFBRGL-UHFFFAOYSA-N 0.000 description 1
- KQCBXUUPBHKHKB-UHFFFAOYSA-N FC(CC1)(CC1(CC1)CCN1c1nc([nH]nc2-c3cccc(Cl)c3Cl)c2nc1)F Chemical compound FC(CC1)(CC1(CC1)CCN1c1nc([nH]nc2-c3cccc(Cl)c3Cl)c2nc1)F KQCBXUUPBHKHKB-UHFFFAOYSA-N 0.000 description 1
- AKZKUGUQZMUCJC-UHFFFAOYSA-N NC(CCC1)C1(CC1)CCN1c1nc([nH]nc2-c(cccc3Cl)c3Cl)c2nc1 Chemical compound NC(CCC1)C1(CC1)CCN1c1nc([nH]nc2-c(cccc3Cl)c3Cl)c2nc1 AKZKUGUQZMUCJC-UHFFFAOYSA-N 0.000 description 1
- KCRBJSWWABFQLC-UHFFFAOYSA-N NC(CF)(CC1)CCN1c1nc([nH]nc2-c3cccc(Cl)c3Cl)c2nc1 Chemical compound NC(CF)(CC1)CCN1c1nc([nH]nc2-c3cccc(Cl)c3Cl)c2nc1 KCRBJSWWABFQLC-UHFFFAOYSA-N 0.000 description 1
- DCZHDAUEYSJCLK-UHFFFAOYSA-N NC(CO)(CC1)CCN1c1cnc(c(-c(cccc2)c2Cl)n[nH]2)c2n1 Chemical compound NC(CO)(CC1)CCN1c1cnc(c(-c(cccc2)c2Cl)n[nH]2)c2n1 DCZHDAUEYSJCLK-UHFFFAOYSA-N 0.000 description 1
- YCRNZPYPOFXDCB-UHFFFAOYSA-N NC(CO)(CC1)CCN1c1cnc(c(-c2cccc(Cl)c2Cl)n[nH]2)c2n1 Chemical compound NC(CO)(CC1)CCN1c1cnc(c(-c2cccc(Cl)c2Cl)n[nH]2)c2n1 YCRNZPYPOFXDCB-UHFFFAOYSA-N 0.000 description 1
- FHEXWCNTNTWBTH-UHFFFAOYSA-N NC(CO)(CC1)CCN1c1cnc(c(-c2cccc(F)c2Cl)n[nH]2)c2n1 Chemical compound NC(CO)(CC1)CCN1c1cnc(c(-c2cccc(F)c2Cl)n[nH]2)c2n1 FHEXWCNTNTWBTH-UHFFFAOYSA-N 0.000 description 1
- XVECDRYVLBLJQU-UHFFFAOYSA-N NC(CO)(CC1)CCN1c1nc([nH]nc2-c(cccn3)c3Cl)c2nc1 Chemical compound NC(CO)(CC1)CCN1c1nc([nH]nc2-c(cccn3)c3Cl)c2nc1 XVECDRYVLBLJQU-UHFFFAOYSA-N 0.000 description 1
- OLCQKOFQXXDERP-UHFFFAOYSA-N NCC(CC1)(CCN1c1nc([nH]nc2-c(c(F)ccc3)c3Cl)c2nc1)O Chemical compound NCC(CC1)(CCN1c1nc([nH]nc2-c(c(F)ccc3)c3Cl)c2nc1)O OLCQKOFQXXDERP-UHFFFAOYSA-N 0.000 description 1
- YMDXJDQSJVLAPR-UHFFFAOYSA-N NCC(CC1)(CCN1c1nc([nH]nc2-c(cccc3)c3Cl)c2nc1)O Chemical compound NCC(CC1)(CCN1c1nc([nH]nc2-c(cccc3)c3Cl)c2nc1)O YMDXJDQSJVLAPR-UHFFFAOYSA-N 0.000 description 1
- FKZOMXXYVRQPKU-CYBMUJFWSA-N N[C@H](CCC1)C1(CC1)CCN1c1cnc(c(-c(cccn2)c2Cl)n[nH]2)c2n1 Chemical compound N[C@H](CCC1)C1(CC1)CCN1c1cnc(c(-c(cccn2)c2Cl)n[nH]2)c2n1 FKZOMXXYVRQPKU-CYBMUJFWSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662343455P | 2016-05-31 | 2016-05-31 | |
| US62/343,455 | 2016-05-31 | ||
| US201762451432P | 2017-01-27 | 2017-01-27 | |
| US62/451,432 | 2017-01-27 | ||
| PCT/US2017/034806 WO2017210134A1 (en) | 2016-05-31 | 2017-05-26 | Heterocyclic inhibitors of ptpn11 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019517487A JP2019517487A (ja) | 2019-06-24 |
| JP2019517487A5 true JP2019517487A5 (enExample) | 2020-07-02 |
| JP7044375B2 JP7044375B2 (ja) | 2022-03-30 |
Family
ID=60420381
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018562312A Active JP7044375B2 (ja) | 2016-05-31 | 2017-05-26 | Ｐｔｐｎ１１の複素環式阻害剤 |
Country Status (6)
| Country | Link |
|---|---|
| US (3) | US10280171B2 (enExample) |
| EP (1) | EP3463343B1 (enExample) |
| JP (1) | JP7044375B2 (enExample) |
| CN (1) | CN109475531B (enExample) |
| AU (1) | AU2017274199B2 (enExample) |
| WO (1) | WO2017210134A1 (enExample) |
Families Citing this family (92)
| 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 |
| CA3119019C (en) | 2015-12-10 | 2024-06-11 | Ptc Therapeutics, Inc. | Compounds and methods for treating huntington's disease |
| WO2017210134A1 (en) | 2016-05-31 | 2017-12-07 | Board Of Regents, University Of Texas System | Heterocyclic inhibitors of ptpn11 |
| KR102218333B1 (ko) | 2016-06-07 | 2021-02-22 | 자코바이오 파마슈티칼스 컴퍼니 리미티드 | Shp2 억제제로서 유용한 신규한 헤테로환형 유도체 |
| PT3468972T (pt) | 2016-06-14 | 2020-08-21 | Novartis Ag | Compostos e composições para inibir a atividade da shp2 |
| EP3515916B1 (en) * | 2016-09-22 | 2023-06-07 | Relay Therapeutics, Inc. | Shp2 phosphatase inhibitors and methods of use thereof |
| TW202500565A (zh) | 2016-10-24 | 2025-01-01 | 美商傳達治療有限公司 | Shp2磷酸酶抑制劑及其使用方法 |
| SG11201908820VA (en) | 2017-03-23 | 2019-10-30 | Jacobio Pharmaceuticals Co Ltd | Novel heterocyclic derivatives useful as shp2 inhibitors |
| US11591336B2 (en) | 2017-05-26 | 2023-02-28 | D. E. Shaw Research, Llc | Substituted pyrazolo[3,4-b]pyrazines as SHP2 phosphatase inhibitors |
| EP4151627A1 (en) | 2017-06-05 | 2023-03-22 | PTC Therapeutics, Inc. | Compounds for treating huntington's disease |
| CN111163838B (zh) | 2017-06-28 | 2023-03-28 | Ptc医疗公司 | 用于治疗亨廷顿氏病的方法 |
| CN111182898B (zh) | 2017-06-28 | 2024-04-16 | Ptc医疗公司 | 用于治疗亨廷顿氏病的方法 |
| EP3687997A1 (en) | 2017-09-29 | 2020-08-05 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors |
| US11498930B2 (en) | 2018-02-13 | 2022-11-15 | Blueray Therapeutics (Shanghai) Co., Ltd | Pyrimidine-fused cyclic compound, preparation method therefor and application thereof |
| WO2019165073A1 (en) * | 2018-02-21 | 2019-08-29 | Relay Therapeutics, Inc. | Shp2 phosphatase inhibitors and methods of use thereof |
| MA52421A (fr) * | 2018-03-02 | 2021-01-06 | Otsuka Pharma Co Ltd | Composés pharmaceutiques |
| CN117263942A (zh) | 2018-03-21 | 2023-12-22 | 传达治疗有限公司 | Shp2磷酸酶抑制剂及其使用方法 |
| US12138263B2 (en) | 2018-03-21 | 2024-11-12 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine SHP2 phosphatase inhibitors and methods of use thereof |
| BR112020019373A2 (pt) | 2018-03-27 | 2020-12-29 | Ptc Therapeutics, Inc. | Compostos para o tratamento da doença de hutington |
| KR102611661B1 (ko) * | 2018-05-02 | 2023-12-08 | 나비레 파르마, 인코퍼레이티드 | Ptpn11의 치환된 헤테로사이클릭 억제제 |
| KR20210038845A (ko) | 2018-06-27 | 2021-04-08 | 피티씨 테라퓨틱스, 인크. | 헌팅턴병 치료를 위한 헤테로아릴 화합물 |
| IL279688B2 (en) * | 2018-06-27 | 2025-01-01 | Ptc Therapeutics Inc | Heterocyclic and heteroaryl compounds for the treatment of Huntington's disease |
| WO2020005882A1 (en) | 2018-06-27 | 2020-01-02 | Ptc Therapeutics, Inc. | Heteroaryl compounds for treating huntington's disease |
| MA53395A (fr) * | 2018-07-24 | 2021-06-02 | Otsuka Pharma Co Ltd | Composés hétérobicycliques pour inhiber l'activité de shp2 |
| PL3833670T3 (pl) | 2018-08-10 | 2024-08-19 | Navire Pharma, Inc. | Pochodne 6-(4-amino-3-metylo-2-oksa-8-azaspiro[4.5]dekan-8-ylo)-3-(2,3-dichlorofenylo)-2-metylopirymidyn-4(3h)-onu oraz powiązane związki jako inhibitory ptpn11 (shp2) do leczenia raka |
| JP7337174B2 (ja) | 2018-09-18 | 2023-09-01 | ニカング セラピューティクス， インコーポレイテッド | Ｓｒｃホモロジー－２ホスファターゼ阻害剤としての三置換ヘテロアリール誘導体 |
| 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 |
| EP3860717A1 (en) | 2018-10-03 | 2021-08-11 | Gilead Sciences, Inc. | Imidozopyrimidine derivatives |
| WO2020073945A1 (zh) * | 2018-10-10 | 2020-04-16 | 江苏豪森药业集团有限公司 | 双环类衍生物抑制剂、其制备方法和应用 |
| MA53921A (fr) | 2018-10-17 | 2022-01-26 | Array Biopharma Inc | Inhibiteurs de protéine tyrosine phosphatase |
| US20230096028A1 (en) | 2019-03-01 | 2023-03-30 | Revolution Medicines, Inc. | Bicyclic heterocyclyl compounds and uses thereof |
| WO2020180768A1 (en) | 2019-03-01 | 2020-09-10 | Revolution Medicines, Inc. | Bicyclic heteroaryl compounds and uses thereof |
| AU2020251841B2 (en) | 2019-04-02 | 2025-01-30 | Array Biopharma Inc. | Protein tyrosine phosphatase inhibitors |
| CA3139821A1 (en) | 2019-05-13 | 2020-11-19 | Ptc Therapeutics, Inc. | Compounds for treating huntington's disease |
| 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 |
| EP4034539A1 (en) | 2019-09-24 | 2022-08-03 | Relay Therapeutics, Inc. | Shp2 phosphatase inhibitors and methods of making and using the same |
| WO2021091956A1 (en) | 2019-11-04 | 2021-05-14 | Revolution Medicines, Inc. | Ras inhibitors |
| MX2022005359A (es) | 2019-11-04 | 2022-06-02 | Revolution Medicines Inc | Inhibidores de ras. |
| CN121471132A (zh) | 2019-11-04 | 2026-02-06 | 锐新医药公司 | Ras抑制剂 |
| PH12022551102A1 (en) | 2019-11-08 | 2023-11-20 | Revolution Medicines Inc | Bicyclic heteroaryl compounds and uses thereof |
| CN114980976A (zh) | 2019-11-27 | 2022-08-30 | 锐新医药公司 | 共价ras抑制剂及其用途 |
| WO2021247836A1 (en) * | 2020-06-03 | 2021-12-09 | Board Of Regents, The University Of Texas System | Methods for targeting shp-2 to overcome resistance |
| CN115916194A (zh) | 2020-06-18 | 2023-04-04 | 锐新医药公司 | 用于延迟、预防和治疗针对ras抑制剂的获得性抗性的方法 |
| EP4208261A1 (en) | 2020-09-03 | 2023-07-12 | Revolution Medicines, Inc. | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| IL301298A (en) | 2020-09-15 | 2023-05-01 | Revolution Medicines Inc | Indole derivatives as RAS inhibitors in cancer therapy |
| AU2021409816A1 (en) | 2020-12-22 | 2023-07-06 | Qilu Regor Therapeutics Inc. | Sos1 inhibitors and uses thereof |
| EP4039685A1 (en) | 2021-02-08 | 2022-08-10 | Irbm S.P.A. | Azabicyclic shp2 inhibitors |
| 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 |
| WO2022235866A1 (en) | 2021-05-05 | 2022-11-10 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| PE20240088A1 (es) | 2021-05-05 | 2024-01-16 | Revolution Medicines Inc | Inhibidores de ras |
| IL308195A (en) | 2021-05-05 | 2024-01-01 | Revolution Medicines Inc | RAS inhibitors for cancer treatment |
| CA3217084A1 (en) | 2021-05-05 | 2022-11-10 | Farbod Shojaei | Combination therapies comprising shp2 inhibitors and pd-1 inhibitors |
| CN117642167A (zh) * | 2021-05-05 | 2024-03-01 | 沪亚生物国际有限责任公司 | Shp2抑制剂单一疗法及其用途 |
| WO2022235822A1 (en) * | 2021-05-05 | 2022-11-10 | Huabio International, Llc | Shp2 inhibitor monotherapy and uses thereof |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| CN114213417B (zh) * | 2021-11-16 | 2023-08-22 | 郑州大学 | 吡唑并六元氮杂环类化合物及其合成方法和应用 |
| WO2023172940A1 (en) | 2022-03-08 | 2023-09-14 | Revolution Medicines, Inc. | Methods for treating immune refractory lung cancer |
| CN117088887A (zh) * | 2022-05-20 | 2023-11-21 | 安徽中科拓苒药物科学研究有限公司 | Shp2抑制剂及其用途 |
| EP4536364A1 (en) | 2022-06-10 | 2025-04-16 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| EP4345101A1 (en) | 2022-09-29 | 2024-04-03 | Irbm S.P.A. | Azole derivatives as shp2 inhibitors |
| CN118344343A (zh) * | 2023-01-16 | 2024-07-16 | 上海美悦生物科技发展有限公司 | 一种杂环取代的吡嗪类化合物及其制备方法和用途 |
| CN121487738A (zh) | 2023-03-30 | 2026-02-06 | 锐新医药公司 | 诱导ras gtp水解的组合物和其用途 |
| WO2024211712A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
| CN121487951A (zh) | 2023-04-07 | 2026-02-06 | 锐新医药公司 | 大环ras抑制剂 |
| AU2024251341A1 (en) | 2023-04-14 | 2025-10-16 | Revolution Medicines, Inc. | Crystalline forms of a ras inhibitor |
| EP4695261A1 (en) | 2023-04-14 | 2026-02-18 | Revolution Medicines, Inc. | Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof |
| KR20260019479A (ko) | 2023-05-04 | 2026-02-10 | 레볼루션 메디슨즈, 인크. | Ras 관련 질환 또는 장애를 위한 병용 요법 |
| CN121889155A (zh) | 2023-08-07 | 2026-04-17 | 锐新医药公司 | 用于治疗ras蛋白相关疾病或病症的rmc-6291 |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| AU2024404879A1 (en) | 2023-12-22 | 2026-06-25 | Regor Pharmaceuticals, Inc. | Sos1 inhibitors and uses thereof |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026017098A1 (zh) * | 2024-07-19 | 2026-01-22 | 药捷安康(南京)科技股份有限公司 | Alox抑制剂及其用途 |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
| WO2026090116A2 (en) | 2024-10-21 | 2026-04-30 | Revolution Medicines, Inc. | Ras inhibitors |
| US20260108528A1 (en) | 2024-10-22 | 2026-04-23 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2026090245A1 (en) | 2024-10-22 | 2026-04-30 | Revolution Medicines, Inc. | Use of ras inhibitors for treating cancer |
| WO2026106912A1 (en) | 2024-11-12 | 2026-05-21 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026112260A1 (en) | 2024-11-21 | 2026-05-28 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026122764A2 (en) | 2024-12-06 | 2026-06-11 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026128688A2 (en) | 2024-12-13 | 2026-06-18 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026160446A1 (ja) * | 2025-01-24 | 2026-07-30 | アステラス製薬株式会社 | Ｓｈｐ２タンパク質の分解を誘導するための複素環化合物 |
| WO2026161839A1 (en) | 2025-01-27 | 2026-07-30 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (64)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2004274403A1 (en) | 2003-09-03 | 2005-03-31 | Aventis Pharmaceuticals Inc. | 5-aryl-Pyrazolo(4,3-d)pyrimidines, pyridines, and pyrazines and related compounds |
| KR100844864B1 (ko) | 2004-02-27 | 2008-07-09 | 에프. 호프만-라 로슈 아게 | 헤테로아릴-융합 피라졸로 유도체 |
| JP4790703B2 (ja) | 2004-04-07 | 2011-10-12 | 武田薬品工業株式会社 | 環式化合物 |
| AU2005309566A1 (en) | 2004-11-22 | 2006-06-01 | Vertex Pharmaceuticals Incorporated | Bicyclic inhibitors or Rho kinase |
| GB0427604D0 (en) | 2004-12-16 | 2005-01-19 | Novartis Ag | Organic compounds |
| GB0506147D0 (en) | 2005-03-24 | 2005-05-04 | Merck Sharp & Dohme | Therapeutic agents |
| US20080153810A1 (en) | 2006-11-15 | 2008-06-26 | Forest Laboratories Holdings Limited | Indazole derivatives useful as melanin concentrating receptor ligands |
| US8361959B2 (en) | 2008-10-03 | 2013-01-29 | Merck Sharp & Dohme Corp. | Spiro-imidazolone derivatives as glucagon receptor antagonists |
| JP2010111624A (ja) | 2008-11-06 | 2010-05-20 | Shionogi & Co Ltd | Ｔｔｋ阻害作用を有するインダゾール誘導体 |
| KR20110049217A (ko) | 2009-11-04 | 2011-05-12 | 다우어드밴스드디스플레이머티리얼 유한회사 | 신규한 유기 발광 화합물 및 이를 채용하고 있는 유기 전계 발광 소자 |
| JP2011246389A (ja) | 2010-05-26 | 2011-12-08 | Oncotherapy Science Ltd | Ｔｔｋ阻害作用を有する縮環ピラゾール誘導体 |
| USRE47009E1 (en) | 2011-02-01 | 2018-08-28 | The Children's Hospital Of Philadelphia | HDAC inhibitors and therapeutic methods using the same |
| WO2013052263A2 (en) | 2011-09-16 | 2013-04-11 | Microbiotix, Inc. | Antifungal compounds |
| WO2013040527A1 (en) | 2011-09-16 | 2013-03-21 | Microbiotix, Inc. | Antimicrobial compounds |
| US9738610B2 (en) | 2012-09-24 | 2017-08-22 | Whitehead Institute For Biomedical Research | Indazole derivatives and uses thereof |
| CA2944198C (en) | 2013-04-26 | 2021-11-16 | Indiana University Research & Technology Corporation | Hydroxyindole carboxylic acid based inhibitors for oncogenic src homology-2 domain containing protein tyrosine phosphatase-2 (shp2) |
| WO2014200682A1 (en) | 2013-05-24 | 2014-12-18 | The Scripps Research Institute | Bidentate-binding modulators of lrrk2 and jnk kinases |
| WO2015099481A1 (ko) | 2013-12-27 | 2015-07-02 | 주식회사 두산 | 유기 전계 발광 소자 |
| ES2699351T3 (es) | 2014-01-17 | 2019-02-08 | Novartis Ag | Derivados de 1-piridazin/triazin-3-il-piper(-azina)/idina/pirolidina y composiciones de las mismas para inhibir la actividad de SHP2 |
| WO2015107494A1 (en) | 2014-01-17 | 2015-07-23 | Novartis Ag | 1 -(triazin-3-yi_/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions thereof for inhibiting the activity of shp2 |
| JO3517B1 (ar) * | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| KR101998435B1 (ko) | 2014-06-09 | 2019-07-09 | 주식회사 두산 | 유기 전계 발광 소자 |
| KR101708097B1 (ko) | 2014-10-22 | 2017-02-17 | 주식회사 두산 | 유기 전계 발광 소자 |
| WO2016151501A1 (en) | 2015-03-25 | 2016-09-29 | Novartis Ag | Pharmaceutical combinations |
| WO2016203406A1 (en) | 2015-06-19 | 2016-12-22 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| EP3310779B1 (en) | 2015-06-19 | 2019-05-08 | Novartis AG | Compounds and compositions for inhibiting the activity of shp2 |
| ES2824576T3 (es) | 2015-06-19 | 2021-05-12 | Novartis Ag | Compuestos y composiciones para inhibir la actividad de SHP2 |
| WO2017156397A1 (en) | 2016-03-11 | 2017-09-14 | Board Of Regents, The University Of Texas Sysytem | Heterocyclic inhibitors of ptpn11 |
| CN107286150B (zh) | 2016-04-11 | 2020-07-07 | 中国科学院上海有机化学研究所 | N-杂环类化合物、其中间体、制备方法、药物组合物和应用 |
| WO2017210134A1 (en) | 2016-05-31 | 2017-12-07 | Board Of Regents, University Of Texas System | Heterocyclic inhibitors of ptpn11 |
| KR102218333B1 (ko) | 2016-06-07 | 2021-02-22 | 자코바이오 파마슈티칼스 컴퍼니 리미티드 | Shp2 억제제로서 유용한 신규한 헤테로환형 유도체 |
| PT3468972T (pt) | 2016-06-14 | 2020-08-21 | Novartis Ag | Compostos e composições para inibir a atividade da shp2 |
| IL311645B2 (en) | 2016-07-12 | 2025-11-01 | Revolution Medicines Inc | 2,5- disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines asallosteric shp2 inhibitors |
| EP3515916B1 (en) | 2016-09-22 | 2023-06-07 | Relay Therapeutics, Inc. | Shp2 phosphatase inhibitors and methods of use thereof |
| TW202500565A (zh) | 2016-10-24 | 2025-01-01 | 美商傳達治療有限公司 | Shp2磷酸酶抑制劑及其使用方法 |
| CN110730678B (zh) | 2017-01-10 | 2022-07-15 | 诺华股份有限公司 | 包含alk抑制剂和shp2抑制剂的药物组合 |
| CA3051054A1 (en) | 2017-01-23 | 2018-07-26 | Revolution Medicines, Inc. | Pyridine compounds as allosteric shp2 inhibitors |
| CN110446709B (zh) | 2017-01-23 | 2023-09-12 | 锐新医药公司 | 作为变构shp2抑制剂的二环化合物 |
| SG11201908820VA (en) | 2017-03-23 | 2019-10-30 | Jacobio Pharmaceuticals Co Ltd | Novel heterocyclic derivatives useful as shp2 inhibitors |
| US11591336B2 (en) | 2017-05-26 | 2023-02-28 | D. E. Shaw Research, Llc | Substituted pyrazolo[3,4-b]pyrazines as SHP2 phosphatase inhibitors |
| TWI852912B (zh) | 2017-09-07 | 2024-08-21 | 美商銳新醫藥公司 | Shp2抑制劑組合物以及治療癌症的方法 |
| 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 |
| BR112020007058A2 (pt) | 2017-10-12 | 2020-10-06 | Revolution Medicines, Inc. | compostos de piridina, pirazina, e triazina como inibidores de shp2 alostéricos |
| BR112020009757A2 (pt) | 2017-12-15 | 2020-11-03 | Revolution Medicines, Inc. | compostos policíclicos como inibidores alostéricos de shp2 |
| WO2019152454A1 (en) | 2018-01-30 | 2019-08-08 | Research Development Foundation | Shp2 inhibitors and methods of use thereof |
| US11498930B2 (en) | 2018-02-13 | 2022-11-15 | Blueray Therapeutics (Shanghai) Co., Ltd | Pyrimidine-fused cyclic compound, preparation method therefor and application thereof |
| WO2019165073A1 (en) | 2018-02-21 | 2019-08-29 | Relay Therapeutics, Inc. | Shp2 phosphatase inhibitors and methods of use thereof |
| MA52421A (fr) | 2018-03-02 | 2021-01-06 | Otsuka Pharma Co Ltd | Composés pharmaceutiques |
| US12138263B2 (en) | 2018-03-21 | 2024-11-12 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine SHP2 phosphatase inhibitors and methods of use thereof |
| RU2020133727A (ru) | 2018-03-21 | 2022-04-21 | Сучжоу Пухе Биофарма Ко., Лтд. | Ингибиторы shp2 и их применение |
| CN117263942A (zh) | 2018-03-21 | 2023-12-22 | 传达治疗有限公司 | Shp2磷酸酶抑制剂及其使用方法 |
| KR20200143417A (ko) | 2018-04-10 | 2020-12-23 | 레볼루션 메디슨즈, 인크. | Shp2 억제제 조성물, 암을 치료하는 방법 및 shp2 돌연변이를 갖는 대상체를 확인하는 방법 |
| KR102611661B1 (ko) | 2018-05-02 | 2023-12-08 | 나비레 파르마, 인코퍼레이티드 | Ptpn11의 치환된 헤테로사이클릭 억제제 |
| CN116003321A (zh) | 2018-05-09 | 2023-04-25 | 北京加科思新药研发有限公司 | 可用作shp2抑制剂的新型杂环衍生物 |
| US20210230300A1 (en) | 2018-06-04 | 2021-07-29 | Bayer Aktiengesellschaft | Inhibitors of shp2 |
| MA53395A (fr) | 2018-07-24 | 2021-06-02 | Otsuka Pharma Co Ltd | Composés hétérobicycliques pour inhiber l'activité de shp2 |
| TWI825144B (zh) | 2018-08-10 | 2023-12-11 | 美商思達利醫藥公司 | 第二型轉麩醯胺酸酶(tg2)抑制劑 |
| PL3833670T3 (pl) | 2018-08-10 | 2024-08-19 | Navire Pharma, Inc. | Pochodne 6-(4-amino-3-metylo-2-oksa-8-azaspiro[4.5]dekan-8-ylo)-3-(2,3-dichlorofenylo)-2-metylopirymidyn-4(3h)-onu oraz powiązane związki jako inhibitory ptpn11 (shp2) do leczenia raka |
| AU2019389168A1 (en) | 2018-11-30 | 2021-06-24 | Comet Therapeutics, Inc. | Pantetheine derivatives and uses thereof |
| AR117164A1 (es) | 2018-11-30 | 2021-07-14 | Merck Sharp & Dohme | Derivados de amino-triazoloquinazolina 9-sustituidos como antagonistas del receptor de adenosina, composiciones farmacéuticas y su uso para el tratamiento de diversos tipos de cáncer |
| CN113613724B (zh) | 2018-11-30 | 2024-11-08 | 葛兰素史克知识产权开发有限公司 | 可用于hiv疗法的化合物 |
| AR117200A1 (es) | 2018-11-30 | 2021-07-21 | Syngenta Participations Ag | Derivados de tiazol microbiocidas |
| PY1999867A (es) | 2018-11-30 | 2020-10-19 | Syngenta Crop Protection Ag | Derivados de tiazol microbiocidas |
-
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- 2017-05-26 WO PCT/US2017/034806 patent/WO2017210134A1/en not_active Ceased
- 2017-05-26 AU AU2017274199A patent/AU2017274199B2/en active Active
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- 2017-05-26 EP EP17807297.1A patent/EP3463343B1/en active Active
- 2017-05-26 JP JP2018562312A patent/JP7044375B2/ja active Active
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-
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- 2022-07-29 US US17/876,958 patent/US11840536B2/en active Active
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