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
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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
- 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 heteroatoms 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
- 125000004435 hydrogen atoms Chemical class [H]* 0.000 claims 9
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 8
- 125000005418 aryl aryl group Chemical group 0.000 claims 8
- 125000003118 aryl 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
- 239000011780 sodium chloride Substances 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
- 201000011510 cancer Diseases 0.000 claims 6
- 125000004432 carbon atoms Chemical group C* 0.000 claims 6
- 102100017818 PTPN11 Human genes 0.000 claims 5
- 101710018405 PTPN11 Proteins 0.000 claims 5
- 125000003368 amide group Chemical group 0.000 claims 5
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 3
- 208000005101 LEOPARD Syndrome Diseases 0.000 claims 3
- 206010024324 Leukaemias Diseases 0.000 claims 3
- 206010025650 Malignant melanoma Diseases 0.000 claims 3
- 206010062901 Multiple lentigines syndrome Diseases 0.000 claims 3
- 206010029748 Noonan syndrome Diseases 0.000 claims 3
- 125000000392 cycloalkenyl group Chemical group 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
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 230000001404 mediated Effects 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- 230000001668 ameliorated Effects 0.000 claims 1
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 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
- 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 (US07794700-20100914-C00125.png) | 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 (7)
Families Citing this family (57)
| 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 |
| MX2021001091A (es) | 2015-12-10 | 2022-04-26 | Ptc Therapeutics Inc | Compuestos para usarse en el tratamiento o mejoramiento de la enfermedad de huntington. |
| JP7044375B2 (ja) | 2016-05-31 | 2022-03-30 | ボード オブ リージェンツ，ザ ユニバーシティ オブ テキサス システム | Ｐｔｐｎ１１の複素環式阻害剤 |
| EA201990001A1 (ru) | 2016-06-07 | 2019-05-31 | Джакобио Фармасьютикалс Ко., Лтд. | Новые гетероциклические производные, применимые в качестве ингибиторов shp2 |
| US10934285B2 (en) | 2016-06-14 | 2021-03-02 | Novartis Ag | Compounds and compositions for inhibiting the activity of 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 |
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| WO2018218133A1 (en) | 2017-05-26 | 2018-11-29 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors |
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| CN112351780B (zh) * | 2018-05-02 | 2023-12-01 | 纳维尔制药有限公司 | Ptpn11的取代的杂环抑制剂 |
| EP3814360A1 (en) | 2018-06-27 | 2021-05-05 | PTC Therapeutics, Inc. | Heteroaryl compounds for treating huntington's disease |
| EP3814357B1 (en) * | 2018-06-27 | 2024-05-01 | PTC Therapeutics, Inc. | Heterocyclic and heteroaryl compounds for treating huntington's disease |
| IL280331B2 (en) * | 2018-07-24 | 2023-12-01 | Otsuka Pharma Co Ltd | Tricyclic compounds to inhibit the activity of SHP2 |
| IL307361A (en) | 2018-08-10 | 2023-11-01 | Navire Pharma Inc | History of 6-(4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-3-(3,2-dichlorophenyl)-2-methylpyrimidin-4(H3)-one and compounds associated as PTPN11 (SHP2) inhibitors for cancer treatment |
| MX2021003158A (es) | 2018-09-18 | 2021-07-16 | Nikang Therapeutics Inc | Derivados de anillo tricíclico condensado como inhibidores de la fosfatasa de homología a src 2. |
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| KR20210146287A (ko) | 2019-03-01 | 2021-12-03 | 레볼루션 메디슨즈, 인크. | 이환식 헤테로아릴 화합물 및 이의 용도 |
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| 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 |
| TW202126660A (zh) | 2019-09-24 | 2021-07-16 | 美商傳達治療有限公司 | Ｓｈｐ２磷酸酶抑制劑及其製備與使用方法 |
| BR112022008565A2 (pt) | 2019-11-04 | 2022-08-09 | Revolution Medicines Inc | Composto, composição farmacêutica, conjugado, métodos para tratar câncer e um distúrbio relativo à proteína ras |
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| TW202132314A (zh) | 2019-11-04 | 2021-09-01 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| KR20220100903A (ko) | 2019-11-08 | 2022-07-18 | 레볼루션 메디슨즈, 인크. | 이환식 헤테로아릴 화합물 및 이의 용도 |
| 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 |
| JP2023530351A (ja) | 2020-06-18 | 2023-07-14 | 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 | Ｒａｓ阻害剤への獲得耐性を遅延させる、防止する、及び、治療する方法 |
| IL301062A (en) | 2020-09-03 | 2023-05-01 | Revolution Medicines Inc | Use of SOS1 inhibitors to treat malignancies with SHP2 mutations |
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| CN117396472A (zh) | 2020-12-22 | 2024-01-12 | 上海齐鲁锐格医药研发有限公司 | Sos1抑制剂及其用途 |
| 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 |
| CA3217393A1 (en) | 2021-05-05 | 2022-11-10 | Elena S. Koltun | Ras inhibitors |
| US20220370458A1 (en) * | 2021-05-05 | 2022-11-24 | Huyabio International, Llc | Shp2 inhibitor monotherapy and uses thereof |
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