JP6900406B2 - Ａｋｔ阻害剤としてのジヒドロピラゾロアゼピン系化合物 - Google Patents
Ａｋｔ阻害剤としてのジヒドロピラゾロアゼピン系化合物 Download PDFInfo
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- JP6900406B2 JP6900406B2 JP2018565750A JP2018565750A JP6900406B2 JP 6900406 B2 JP6900406 B2 JP 6900406B2 JP 2018565750 A JP2018565750 A JP 2018565750A JP 2018565750 A JP2018565750 A JP 2018565750A JP 6900406 B2 JP6900406 B2 JP 6900406B2
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- 0 O=C(c1ccccc11)N2C1=*[C@@](Cc(c(F)c1)ccc1F)C2 Chemical compound O=C(c1ccccc11)N2C1=*[C@@](Cc(c(F)c1)ccc1F)C2 0.000 description 9
- IBPPPQFKQRPIBK-UHFFFAOYSA-N Cc1c(-c2c(OCC3)[s]c(C)c2)[n]3nc1 Chemical compound Cc1c(-c2c(OCC3)[s]c(C)c2)[n]3nc1 IBPPPQFKQRPIBK-UHFFFAOYSA-N 0.000 description 2
- OBDSBCMKJMLIQF-NSHDSACASA-N NC[C@H](Cc(ccc(F)c1F)c1F)NC(c1cc(-c([n](CCC2)nc3)c3Br)c2[s]1)=O Chemical compound NC[C@H](Cc(ccc(F)c1F)c1F)NC(c1cc(-c([n](CCC2)nc3)c3Br)c2[s]1)=O OBDSBCMKJMLIQF-NSHDSACASA-N 0.000 description 2
- ADVGOHATHNLNRT-UHFFFAOYSA-N OC(c1cc(-c([n](CCC2)nc3)c3Br)c2[s]1)=O Chemical compound OC(c1cc(-c([n](CCC2)nc3)c3Br)c2[s]1)=O ADVGOHATHNLNRT-UHFFFAOYSA-N 0.000 description 2
- QGSVAPKORFFOLR-UHFFFAOYSA-N OC(c1cc(-c([n](CCC2)nc3)c3Cl)c2[s]1)=O Chemical compound OC(c1cc(-c([n](CCC2)nc3)c3Cl)c2[s]1)=O QGSVAPKORFFOLR-UHFFFAOYSA-N 0.000 description 2
- GUZOHNPVOLMVJA-ZDUSSCGKSA-N Bc1c(-c2c(CCC3)[s]c(C(N[C@@H](Cc4ccccn4)CN)=O)c2)[n]3nc1 Chemical compound Bc1c(-c2c(CCC3)[s]c(C(N[C@@H](Cc4ccccn4)CN)=O)c2)[n]3nc1 GUZOHNPVOLMVJA-ZDUSSCGKSA-N 0.000 description 1
- BVNTXRLOTOGZGB-UHFFFAOYSA-N Cc1c(-c2c(C(CC3)(F)F)[s]c(C)c2)[n]3nc1 Chemical compound Cc1c(-c2c(C(CC3)(F)F)[s]c(C)c2)[n]3nc1 BVNTXRLOTOGZGB-UHFFFAOYSA-N 0.000 description 1
- VRNPNSWBJNYSMM-UHFFFAOYSA-N Cc1c(-c2c(C(CC3)OC)[s]c(C)c2)[n]3nc1 Chemical compound Cc1c(-c2c(C(CC3)OC)[s]c(C)c2)[n]3nc1 VRNPNSWBJNYSMM-UHFFFAOYSA-N 0.000 description 1
- SKSVOPLRIKOUII-UHFFFAOYSA-N Cc1c(-c2c(CCC3)[o]c(C)c2)[n]3nc1 Chemical compound Cc1c(-c2c(CCC3)[o]c(C)c2)[n]3nc1 SKSVOPLRIKOUII-UHFFFAOYSA-N 0.000 description 1
- IISRRSCRROCKQD-UHFFFAOYSA-N Cc1c(-c2c(CCC3)[s]c(C)c2)[n]3nc1 Chemical compound Cc1c(-c2c(CCC3)[s]c(C)c2)[n]3nc1 IISRRSCRROCKQD-UHFFFAOYSA-N 0.000 description 1
- FCVDAJZACBWLCJ-UHFFFAOYSA-N Cc1c(-c2cc(C)n[n]2CCC2)[n]2nc1 Chemical compound Cc1c(-c2cc(C)n[n]2CCC2)[n]2nc1 FCVDAJZACBWLCJ-UHFFFAOYSA-N 0.000 description 1
- AZPPODUWSAHYRC-ZDUSSCGKSA-N NC[C@H](Cc(ccc(F)c1)c1F)NC(c1cc(-c([n](CCC2)nc3)c3Cl)c2[s]1)=O Chemical compound NC[C@H](Cc(ccc(F)c1)c1F)NC(c1cc(-c([n](CCC2)nc3)c3Cl)c2[s]1)=O AZPPODUWSAHYRC-ZDUSSCGKSA-N 0.000 description 1
- UBZODNUPELGYFS-ZDUSSCGKSA-N NC[C@H](Cc(cccc1)c1F)NC(c1cc(-c([n](CCC2)nc3)c3Cl)c2[s]1)=O Chemical compound NC[C@H](Cc(cccc1)c1F)NC(c1cc(-c([n](CCC2)nc3)c3Cl)c2[s]1)=O UBZODNUPELGYFS-ZDUSSCGKSA-N 0.000 description 1
- LZPOEVTYJFKFKK-HNNXBMFYSA-N O=C(c1cc(-c([n](CCC2)nc3)c3Br)c2[s]1)N[C@@H](Cc(c(F)c1F)ccc1F)CN(C(c1ccccc11)=O)C1=O Chemical compound O=C(c1cc(-c([n](CCC2)nc3)c3Br)c2[s]1)N[C@@H](Cc(c(F)c1F)ccc1F)CN(C(c1ccccc11)=O)C1=O LZPOEVTYJFKFKK-HNNXBMFYSA-N 0.000 description 1
- SPEOWTCABZWIGN-KRWDZBQOSA-N O=C(c1cc(-c([n](CCC2)nc3)c3Br)c2[s]1)N[C@@H](Cc1ccccn1)CN(C(c1ccccc11)=O)C1=O Chemical compound O=C(c1cc(-c([n](CCC2)nc3)c3Br)c2[s]1)N[C@@H](Cc1ccccn1)CN(C(c1ccccc11)=O)C1=O SPEOWTCABZWIGN-KRWDZBQOSA-N 0.000 description 1
- HCPFZYFWJBKBFH-KRWDZBQOSA-N O=C(c1cc(-c([n](CCC2)nc3)c3Cl)c2[s]1)N[C@@H](Cc(c(F)c1)ccc1F)CN(C(c1c2cccc1)=O)C2=O Chemical compound O=C(c1cc(-c([n](CCC2)nc3)c3Cl)c2[s]1)N[C@@H](Cc(c(F)c1)ccc1F)CN(C(c1c2cccc1)=O)C2=O HCPFZYFWJBKBFH-KRWDZBQOSA-N 0.000 description 1
- IJYOYBCYVAXHHR-KRWDZBQOSA-N O=C(c1cc(-c([n](CCC2)nc3)c3Cl)c2[s]1)N[C@@H](Cc1ccccc1F)CN(C(c1ccccc11)=O)C1=O Chemical compound O=C(c1cc(-c([n](CCC2)nc3)c3Cl)c2[s]1)N[C@@H](Cc1ccccc1F)CN(C(c1ccccc11)=O)C1=O IJYOYBCYVAXHHR-KRWDZBQOSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/14—Ortho-condensed systems
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D487/12—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 three hetero rings
- C07D487/14—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
- C07D491/12—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 three hetero rings
- C07D491/14—Ortho-condensed systems
- C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Obesity (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610428049 | 2016-06-16 | ||
| CN201610428049.6 | 2016-06-16 | ||
| CN201610674021.0 | 2016-08-15 | ||
| CN201610674021 | 2016-08-15 | ||
| PCT/CN2017/088030 WO2017215588A1 (zh) | 2016-06-16 | 2017-06-13 | 作为Akt抑制剂的二氢吡唑氮杂卓类化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019518052A JP2019518052A (ja) | 2019-06-27 |
| JP2019518052A5 JP2019518052A5 (enExample) | 2020-05-14 |
| JP6900406B2 true JP6900406B2 (ja) | 2021-07-07 |
Family
ID=60663995
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018565750A Active JP6900406B2 (ja) | 2016-06-16 | 2017-06-13 | Ａｋｔ阻害剤としてのジヒドロピラゾロアゼピン系化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US10654868B2 (enExample) |
| EP (1) | EP3473628B1 (enExample) |
| JP (1) | JP6900406B2 (enExample) |
| KR (1) | KR102351270B1 (enExample) |
| CN (1) | CN109311908B (enExample) |
| WO (1) | WO2017215588A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2021508319A (ja) * | 2017-12-13 | 2021-03-04 | ハルビン チェンバオ ファーマシューティカル カンパニー リミテッド | Ａｋｔ阻害剤としての塩形態及びその結晶形態 |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2022121788A1 (zh) * | 2020-12-07 | 2022-06-16 | 南京正大天晴制药有限公司 | 一种吡唑并氮杂卓类akt抑制剂 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6887864B2 (en) | 2002-03-12 | 2005-05-03 | Hoffmann-La Roche Inc. | Azepane derivatives |
| CN101094833A (zh) * | 2004-07-12 | 2007-12-26 | 伊邓药品公司 | 四肽类似物 |
| WO2008065054A1 (en) * | 2006-11-28 | 2008-06-05 | Nerviano Medical Sciences S.R.L. | Tricyclic indoles and (4,5-dihydro) indoles |
| UY30892A1 (es) | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
| DE602008003055D1 (de) * | 2007-05-31 | 2010-12-02 | Nerviano Medical Sciences Srl | Zyklokondensierte Azaindole, die als Kinase-Hemmer wirken |
| JP2011509261A (ja) * | 2008-01-07 | 2011-03-24 | シンタ ファーマシューティカルズ コーポレーション | 炎症および免疫関連用途向けの化合物 |
| WO2009158371A1 (en) | 2008-06-26 | 2009-12-30 | Smithklike Beecham Corporation | Inhibitors of akt activity |
| EP2640369A1 (en) | 2010-11-17 | 2013-09-25 | F.Hoffmann-La Roche Ag | Methods of treating tumors |
-
2017
- 2017-06-13 CN CN201780037686.3A patent/CN109311908B/zh active Active
- 2017-06-13 JP JP2018565750A patent/JP6900406B2/ja active Active
- 2017-06-13 US US16/309,648 patent/US10654868B2/en active Active
- 2017-06-13 WO PCT/CN2017/088030 patent/WO2017215588A1/zh not_active Ceased
- 2017-06-13 EP EP17812699.1A patent/EP3473628B1/en active Active
- 2017-06-13 KR KR1020197001396A patent/KR102351270B1/ko active Active
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2021508319A (ja) * | 2017-12-13 | 2021-03-04 | ハルビン チェンバオ ファーマシューティカル カンパニー リミテッド | Ａｋｔ阻害剤としての塩形態及びその結晶形態 |
| US11261196B2 (en) | 2017-12-13 | 2022-03-01 | Harbin Zhenbao Pharmaceutical Co., Ltd. | Salt serving as AKT inhibitor and crystal thereof |
| JP7101781B2 (ja) | 2017-12-13 | 2022-07-15 | ハルビン チェンバオ ファーマシューティカル カンパニー リミテッド | Ａｋｔ阻害剤としての塩形態及びその結晶形態 |
Also Published As
| Publication number | Publication date |
|---|---|
| CN109311908B (zh) | 2021-05-07 |
| US10654868B2 (en) | 2020-05-19 |
| CN109311908A (zh) | 2019-02-05 |
| KR20190017996A (ko) | 2019-02-20 |
| JP2019518052A (ja) | 2019-06-27 |
| KR102351270B1 (ko) | 2022-01-14 |
| WO2017215588A1 (zh) | 2017-12-21 |
| EP3473628A4 (en) | 2019-05-01 |
| US20190233434A1 (en) | 2019-08-01 |
| EP3473628B1 (en) | 2019-12-11 |
| EP3473628A1 (en) | 2019-04-24 |
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