DE14760712T1 - Pyridopyrimidin- oder Pyrimidopyrimidlnverbindung, Herstellungsverfahren, PharmazeutischeZusammensetzung und Verwendung davon - Google Patents
Pyridopyrimidin- oder Pyrimidopyrimidlnverbindung, Herstellungsverfahren, PharmazeutischeZusammensetzung und Verwendung davon Download PDFInfo
- Publication number
- DE14760712T1 DE14760712T1 DE14760712.1T DE14760712T DE14760712T1 DE 14760712 T1 DE14760712 T1 DE 14760712T1 DE 14760712 T DE14760712 T DE 14760712T DE 14760712 T1 DE14760712 T1 DE 14760712T1
- Authority
- DE
- Germany
- Prior art keywords
- octanyl
- azabicyclo
- oxa
- alkyl
- pharmaceutically acceptable
- 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.)
- Pending
Links
- -1 pyrimidopyrimidine compound Chemical class 0.000 title claims abstract 48
- BWESROVQGZSBRX-UHFFFAOYSA-N pyrido[3,2-d]pyrimidine Chemical compound C1=NC=NC2=CC=CN=C21 BWESROVQGZSBRX-UHFFFAOYSA-N 0.000 title claims abstract 22
- 239000008194 pharmaceutical composition Substances 0.000 title claims 3
- 229910052736 halogen Inorganic materials 0.000 claims abstract 23
- 150000002367 halogens Chemical class 0.000 claims abstract 23
- 150000002148 esters Chemical class 0.000 claims abstract 21
- 239000000651 prodrug Substances 0.000 claims abstract 21
- 229940002612 prodrug Drugs 0.000 claims abstract 21
- 150000003839 salts Chemical class 0.000 claims abstract 21
- 239000012453 solvate Substances 0.000 claims abstract 21
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 8
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims abstract 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 6
- 125000001424 substituent group Chemical group 0.000 claims abstract 6
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical group C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims abstract 5
- 125000006413 ring segment Chemical group 0.000 claims abstract 5
- FQUYSHZXSKYCSY-UHFFFAOYSA-N 1,4-diazepane Chemical group C1CNCCNC1 FQUYSHZXSKYCSY-UHFFFAOYSA-N 0.000 claims abstract 3
- ZNGWEEUXTBNKFR-UHFFFAOYSA-N 1,4-oxazepane Chemical group C1CNCCOC1 ZNGWEEUXTBNKFR-UHFFFAOYSA-N 0.000 claims abstract 3
- PVOAHINGSUIXLS-UHFFFAOYSA-N 1-Methylpiperazine Chemical group CN1CCNCC1 PVOAHINGSUIXLS-UHFFFAOYSA-N 0.000 claims abstract 3
- 125000000217 alkyl group Chemical group 0.000 claims abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 3
- 125000004193 piperazinyl group Chemical group 0.000 claims abstract 3
- 125000003386 piperidinyl group Chemical group 0.000 claims abstract 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims abstract 3
- 125000004076 pyridyl group Chemical group 0.000 claims abstract 2
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 4
- 230000004064 dysfunction Effects 0.000 claims 4
- 229940124302 mTOR inhibitor Drugs 0.000 claims 4
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- JOZPEVMCAKXSEY-UHFFFAOYSA-N pyrimido[5,4-d]pyrimidine Chemical class N1=CN=CC2=NC=NC=C21 JOZPEVMCAKXSEY-UHFFFAOYSA-N 0.000 claims 2
- 230000019491 signal transduction Effects 0.000 claims 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 claims 1
- 108091007960 PI3Ks Proteins 0.000 claims 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- WKDMSBTWYDKICI-UHFFFAOYSA-N CNC(c1cc(-c(cc2)nc3c2c(N2CCOCC2)nc(N2CC(CC4)OC4C2)n3)ccc1)=O Chemical compound CNC(c1cc(-c(cc2)nc3c2c(N2CCOCC2)nc(N2CC(CC4)OC4C2)n3)ccc1)=O WKDMSBTWYDKICI-UHFFFAOYSA-N 0.000 description 1
- YUEDLIZBQYCXAU-UHFFFAOYSA-N CNC(c1cc(-c2nc3nc(N4C5COCC4CC5)nc(N4CCOCC4)c3cc2)ccc1)=O Chemical compound CNC(c1cc(-c2nc3nc(N4C5COCC4CC5)nc(N4CCOCC4)c3cc2)ccc1)=O YUEDLIZBQYCXAU-UHFFFAOYSA-N 0.000 description 1
- WAGGOCMPCZLOTQ-UHFFFAOYSA-N COc(c(CO)c1)ccc1-c1nc2nc(N3C4COCC3CC4)nc(N3CC(CC4)OC4C3)c2cc1 Chemical compound COc(c(CO)c1)ccc1-c1nc2nc(N3C4COCC3CC4)nc(N3CC(CC4)OC4C3)c2cc1 WAGGOCMPCZLOTQ-UHFFFAOYSA-N 0.000 description 1
- JQGXBMXWVCTLPO-DZIBYMRMSA-N C[C@@H](COCC1)N1c1c(ccc(-c(cc2)cc(CO)c2OC)n2)c2nc(N2C3COCC2CC3)n1 Chemical compound C[C@@H](COCC1)N1c1c(ccc(-c(cc2)cc(CO)c2OC)n2)c2nc(N2C3COCC2CC3)n1 JQGXBMXWVCTLPO-DZIBYMRMSA-N 0.000 description 1
- HBQHRASIFZAJJQ-AGXSTUJCSA-N C[C@H](C1)O[C@@H](C)CN1c1c(ccc(-c2cccc(C(NC)=O)c2)n2)c2nc(N2C3COCC2CC3)n1 Chemical compound C[C@H](C1)O[C@@H](C)CN1c1c(ccc(-c2cccc(C(NC)=O)c2)n2)c2nc(N2C3COCC2CC3)n1 HBQHRASIFZAJJQ-AGXSTUJCSA-N 0.000 description 1
- KVMLDDLEDRJZCM-AGXSTUJCSA-N C[C@H](C1)O[C@@H](C)CN1c1nc(N2C3COCC2CC3)c(ccc(-c(cc2CO)ccc2OC)n2)c2n1 Chemical compound C[C@H](C1)O[C@@H](C)CN1c1nc(N2C3COCC2CC3)c(ccc(-c(cc2CO)ccc2OC)n2)c2n1 KVMLDDLEDRJZCM-AGXSTUJCSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- 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
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)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310068888 | 2013-03-04 | ||
| CN201310068888.8A CN103588792B (zh) | 2013-03-04 | 2013-03-04 | 吡啶并嘧啶或嘧啶并嘧啶类化合物、其制备方法、药物组合物及其用途 |
| EP14760712.1A EP2966079B1 (en) | 2013-03-04 | 2014-02-28 | Pyridopyrimidine or pyrimidopyrimidine compound, preparation method, pharmaceutical composition and use thereof |
| PCT/CN2014/072678 WO2014135028A1 (zh) | 2013-03-04 | 2014-02-28 | 吡啶并嘧啶或嘧啶并嘧啶类化合物、其制备方法、药物组合物及其用途 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DE14760712T1 true DE14760712T1 (de) | 2017-12-14 |
Family
ID=50079144
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE14760712.1T Pending DE14760712T1 (de) | 2013-03-04 | 2014-02-28 | Pyridopyrimidin- oder Pyrimidopyrimidlnverbindung, Herstellungsverfahren, PharmazeutischeZusammensetzung und Verwendung davon |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9796732B2 (OSRAM) |
| EP (1) | EP2966079B1 (OSRAM) |
| JP (1) | JP2016510042A (OSRAM) |
| CN (1) | CN103588792B (OSRAM) |
| AU (1) | AU2014225155B2 (OSRAM) |
| CA (1) | CA2903072C (OSRAM) |
| DE (1) | DE14760712T1 (OSRAM) |
| DK (1) | DK2966079T3 (OSRAM) |
| ES (1) | ES2572105T3 (OSRAM) |
| RU (1) | RU2662713C2 (OSRAM) |
| WO (1) | WO2014135028A1 (OSRAM) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103588792B (zh) * | 2013-03-04 | 2016-03-23 | 中国科学院上海药物研究所 | 吡啶并嘧啶或嘧啶并嘧啶类化合物、其制备方法、药物组合物及其用途 |
| CN106008559B (zh) | 2015-03-25 | 2020-10-16 | 中国科学院上海药物研究所 | 取代吡啶并嘧啶类化合物的合成工艺 |
| US10722484B2 (en) | 2016-03-09 | 2020-07-28 | K-Gen, Inc. | Methods of cancer treatment |
| CN111148747B (zh) * | 2017-11-07 | 2023-04-04 | 中国科学院上海药物研究所 | 吡啶并嘧啶类化合物的盐型和晶型及其制备方法 |
| CN109867667B (zh) * | 2017-12-05 | 2021-06-11 | 中国药科大学 | 含有吡啶并嘧啶结构的parp和pi3k双靶点抑制剂 |
| CN113825760B (zh) * | 2019-05-06 | 2022-08-19 | 南京明德新药研发有限公司 | 一种mTORC1/2双激酶活性抑制剂的盐型、晶型及其制备方法 |
| EP4161926A4 (en) * | 2020-06-03 | 2024-06-19 | Yumanity Therapeutics, Inc. | PYRIDOPYRIMIDINES AND THEIR METHODS OF USE |
| US20230081426A1 (en) * | 2020-09-18 | 2023-03-16 | Plexxikon Inc. | Compounds and methods for kras modulation and indications therefor |
| WO2022228576A1 (zh) * | 2021-04-30 | 2022-11-03 | 上海医药集团股份有限公司 | 一种靶向蛋白调节剂的化合物及其应用 |
| JP2024532735A (ja) * | 2021-08-10 | 2024-09-10 | アムジエン・インコーポレーテツド | 複素環式化合物及び使用方法 |
| EP4384160A4 (en) * | 2021-08-10 | 2025-10-29 | Amgen Inc | HETEROCYCLIC COMPOUNDS AND METHODS OF USE |
| US20250376483A1 (en) * | 2022-06-15 | 2025-12-11 | Mirati Therapeutics, Inc. | Prodrugs of pan-kras inhibitors |
| WO2024057013A1 (en) * | 2022-09-12 | 2024-03-21 | Exscientia Ai Limited | Nlrp3 modulators |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20070113252A (ko) * | 2005-02-25 | 2007-11-28 | 쿠도스 파마슈티칼스 리미티드 | 2,4-디아미노-피리도피리미딘 유도체 및 이의 ｍＴＯＲ억제제로서의 용도 |
| CN101360746B (zh) * | 2005-11-22 | 2013-12-11 | 库多斯药物有限公司 | 作为mTOR抑制剂的吡啶并-、吡唑并-和嘧啶并-嘧啶衍生物 |
| PT2050749T (pt) * | 2006-08-08 | 2018-01-02 | Chugai Pharmaceutical Co Ltd | Derivado de pirimidina como inibidador de pi3k e sua utilização |
| CN101558067B (zh) * | 2006-08-23 | 2014-05-28 | 库多斯药物有限公司 | 作为mtor抑制剂的2-甲基吗啉吡啶并、吡唑并和嘧啶并-嘧啶衍生物 |
| US20080233127A1 (en) * | 2007-03-21 | 2008-09-25 | Wyeth | Imidazolopyrimidine analogs and their use as pi3 kinase and mtor inhibitors |
| WO2010120987A1 (en) * | 2009-04-17 | 2010-10-21 | Wyeth Llc | Ring fused, ureidoaryl- and carbamoylaryl-bridged morpholino-pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses |
| CN102887895B (zh) * | 2011-07-22 | 2016-08-24 | 山东轩竹医药科技有限公司 | 吡啶并嘧啶类mTOR抑制剂 |
| CN102911172A (zh) * | 2011-08-04 | 2013-02-06 | 上海恒瑞医药有限公司 | 杂芳基并嘧啶类衍生物、其制备方法和用途 |
| CN103588792B (zh) * | 2013-03-04 | 2016-03-23 | 中国科学院上海药物研究所 | 吡啶并嘧啶或嘧啶并嘧啶类化合物、其制备方法、药物组合物及其用途 |
-
2013
- 2013-03-04 CN CN201310068888.8A patent/CN103588792B/zh active Active
-
2014
- 2014-02-28 AU AU2014225155A patent/AU2014225155B2/en not_active Ceased
- 2014-02-28 RU RU2015140387A patent/RU2662713C2/ru active
- 2014-02-28 JP JP2015560533A patent/JP2016510042A/ja active Pending
- 2014-02-28 DE DE14760712.1T patent/DE14760712T1/de active Pending
- 2014-02-28 CA CA2903072A patent/CA2903072C/en active Active
- 2014-02-28 DK DK14760712.1T patent/DK2966079T3/da active
- 2014-02-28 EP EP14760712.1A patent/EP2966079B1/en active Active
- 2014-02-28 ES ES14760712T patent/ES2572105T3/es active Active
- 2014-02-28 WO PCT/CN2014/072678 patent/WO2014135028A1/zh not_active Ceased
-
2015
- 2015-09-01 US US14/842,682 patent/US9796732B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| AU2014225155B2 (en) | 2017-11-23 |
| WO2014135028A1 (zh) | 2014-09-12 |
| CN103588792A (zh) | 2014-02-19 |
| ES2572105T3 (es) | 2022-04-13 |
| EP2966079B1 (en) | 2021-11-24 |
| EP2966079A1 (en) | 2016-01-13 |
| DK2966079T1 (da) | 2016-05-17 |
| US9796732B2 (en) | 2017-10-24 |
| JP2016510042A (ja) | 2016-04-04 |
| AU2014225155A1 (en) | 2015-10-15 |
| US20150368274A1 (en) | 2015-12-24 |
| DK2966079T3 (da) | 2022-02-14 |
| HK1217197A1 (en) | 2016-12-30 |
| RU2015140387A (ru) | 2017-03-30 |
| EP2966079A4 (en) | 2016-11-09 |
| CA2903072C (en) | 2019-05-07 |
| ES2572105T1 (es) | 2016-05-30 |
| RU2662713C2 (ru) | 2018-07-27 |
| CN103588792B (zh) | 2016-03-23 |
| CA2903072A1 (en) | 2014-09-12 |
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