JP6378182B2 - 過剰増殖性│疾患の処置のためのセリン／スレオニンキナーゼ阻害剤 - Google Patents
過剰増殖性│疾患の処置のためのセリン／スレオニンキナーゼ阻害剤 Download PDFInfo
- Publication number
- JP6378182B2 JP6378182B2 JP2015529957A JP2015529957A JP6378182B2 JP 6378182 B2 JP6378182 B2 JP 6378182B2 JP 2015529957 A JP2015529957 A JP 2015529957A JP 2015529957 A JP2015529957 A JP 2015529957A JP 6378182 B2 JP6378182 B2 JP 6378182B2
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- JP
- Japan
- Prior art keywords
- methyl
- alkyl
- cancer
- phenyl
- pyrazol
- 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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- BKALVWBGYHPZDF-UHFFFAOYSA-N C[n]1ncc(-c2cc(CCNC(c(cc3)nc4c3cnc(NC3CCOCC3)c4)=O)ccc2)c1 Chemical compound C[n]1ncc(-c2cc(CCNC(c(cc3)nc4c3cnc(NC3CCOCC3)c4)=O)ccc2)c1 BKALVWBGYHPZDF-UHFFFAOYSA-N 0.000 description 1
- UNZMOOLJRFBUFO-UHFFFAOYSA-N C[n]1ncc(-c2cccc(CNC(c(cc3)nc4c3cnc(NC3CCOCC3)c4)=O)c2)c1 Chemical compound C[n]1ncc(-c2cccc(CNC(c(cc3)nc4c3cnc(NC3CCOCC3)c4)=O)c2)c1 UNZMOOLJRFBUFO-UHFFFAOYSA-N 0.000 description 1
- LYSFRATYSNJHQU-LUTIACGYSA-N C[n]1ncc([C@H](c(cc2F)ccc2OC)NC(c(cc2)nc3c2cnc(NC2COCC2)c3)=O)c1 Chemical compound C[n]1ncc([C@H](c(cc2F)ccc2OC)NC(c(cc2)nc3c2cnc(NC2COCC2)c3)=O)c1 LYSFRATYSNJHQU-LUTIACGYSA-N 0.000 description 1
- YJLBMYAIWRVOAO-UHFFFAOYSA-N Cc(ccnc1)c1-c1cc(CCNC(c(cc2)nc3c2cnc(NC2CCOCC2)c3)=O)ccc1 Chemical compound Cc(ccnc1)c1-c1cc(CCNC(c(cc2)nc3c2cnc(NC2CCOCC2)c3)=O)ccc1 YJLBMYAIWRVOAO-UHFFFAOYSA-N 0.000 description 1
- ICAWJFUDHQXOBI-UHFFFAOYSA-N O=C(c(cc1)nc2c1cnc(NC1CCOCC1)c2)NCCc(cc1)ccc1-c1ccncc1 Chemical compound O=C(c(cc1)nc2c1cnc(NC1CCOCC1)c2)NCCc(cc1)ccc1-c1ccncc1 ICAWJFUDHQXOBI-UHFFFAOYSA-N 0.000 description 1
- DOXZVVAKDUWHGF-UHFFFAOYSA-N O=C(c(cc1)nc2c1cnc(NC1CCOCC1)c2)NCCc(cc1)ccc1-c1cnccn1 Chemical compound O=C(c(cc1)nc2c1cnc(NC1CCOCC1)c2)NCCc(cc1)ccc1-c1cnccn1 DOXZVVAKDUWHGF-UHFFFAOYSA-N 0.000 description 1
- CHKAAATVGOSVEF-UHFFFAOYSA-N O=C(c(cc1)nc2c1cnc(NC1CCOCC1)c2)NCCc(cc1)ccc1-c1cncnc1 Chemical compound O=C(c(cc1)nc2c1cnc(NC1CCOCC1)c2)NCCc(cc1)ccc1-c1cncnc1 CHKAAATVGOSVEF-UHFFFAOYSA-N 0.000 description 1
- YOXSCBOCKQCKKX-UHFFFAOYSA-N O=C(c(cc1)nc2c1cnc(NC1CCOCC1)c2)NCCc1cccc(-c2ccncc2)c1 Chemical compound O=C(c(cc1)nc2c1cnc(NC1CCOCC1)c2)NCCc1cccc(-c2ccncc2)c1 YOXSCBOCKQCKKX-UHFFFAOYSA-N 0.000 description 1
- MWWYOWSLYNFLSL-UHFFFAOYSA-N O=C(c(cc1)nc2c1cnc(NC1CCOCC1)c2)NCCc1cccc(-c2cnccn2)c1 Chemical compound O=C(c(cc1)nc2c1cnc(NC1CCOCC1)c2)NCCc1cccc(-c2cnccn2)c1 MWWYOWSLYNFLSL-UHFFFAOYSA-N 0.000 description 1
- DBFPAEKSGGBQTR-UHFFFAOYSA-O O=C(c(cc1)nc2c1cnc(NC1CCOCC1)c2)NCCc1ccccc1C1=C[NH2+]N=C1 Chemical compound O=C(c(cc1)nc2c1cnc(NC1CCOCC1)c2)NCCc1ccccc1C1=C[NH2+]N=C1 DBFPAEKSGGBQTR-UHFFFAOYSA-O 0.000 description 1
- FMVZIRSKQWAPQK-UHFFFAOYSA-N O=C(c(cc1)nc2c1cnc(NC1CCOCC1)c2)NCc1cccc(Cc2ccccc2)c1 Chemical compound O=C(c(cc1)nc2c1cnc(NC1CCOCC1)c2)NCc1cccc(Cc2ccccc2)c1 FMVZIRSKQWAPQK-UHFFFAOYSA-N 0.000 description 1
- RJPGVHJFOZTBNI-UHFFFAOYSA-N O=C(c(cc1)nc2c1cnc(NC1CCOCC1)c2)NCc1nccc(Oc2ccccc2)c1 Chemical compound O=C(c(cc1)nc2c1cnc(NC1CCOCC1)c2)NCc1nccc(Oc2ccccc2)c1 RJPGVHJFOZTBNI-UHFFFAOYSA-N 0.000 description 1
Classifications
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- 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
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
-
- 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
- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261693671P | 2012-08-27 | 2012-08-27 | |
| US61/693,671 | 2012-08-27 | ||
| PCT/US2013/056876 WO2014036015A1 (en) | 2012-08-27 | 2013-08-27 | Serine/threonine kinase inhibitors for the treatment of hyperproliferative|diseases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015526519A JP2015526519A (ja) | 2015-09-10 |
| JP2015526519A5 JP2015526519A5 (https=) | 2016-10-13 |
| JP6378182B2 true JP6378182B2 (ja) | 2018-08-22 |
Family
ID=49118823
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015529957A Active JP6378182B2 (ja) | 2012-08-27 | 2013-08-27 | 過剰増殖性│疾患の処置のためのセリン／スレオニンキナーゼ阻害剤 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US9388171B2 (https=) |
| EP (1) | EP2888247B1 (https=) |
| JP (1) | JP6378182B2 (https=) |
| KR (1) | KR20150047597A (https=) |
| CN (1) | CN105143200B (https=) |
| AR (1) | AR092253A1 (https=) |
| BR (1) | BR112015004548A2 (https=) |
| CA (1) | CA2882750A1 (https=) |
| HK (1) | HK1210174A1 (https=) |
| MX (1) | MX369989B (https=) |
| RU (1) | RU2644947C2 (https=) |
| TW (1) | TW201408658A (https=) |
| WO (1) | WO2014036015A1 (https=) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103635472B (zh) | 2011-02-28 | 2018-01-12 | 阵列生物制药公司 | 丝氨酸/苏氨酸激酶抑制剂 |
| JP6097289B2 (ja) | 2011-08-04 | 2017-03-15 | アレイ バイオファーマ、インコーポレイテッド | セリン／スレオニンキナーゼインヒビターとしてのキナゾリン化合物 |
| HUE053994T2 (hu) | 2012-03-01 | 2021-08-30 | Array Biopharma Inc | Szerin/treonin kináz inhibitorok |
| MX363388B (es) | 2012-07-27 | 2019-03-20 | Biogen Ma Inc | Agentes moduladores de autotaxina. |
| JP2015533151A (ja) | 2012-10-16 | 2015-11-19 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | セリン／スレオニンキナーゼ阻害剤 |
| US9532987B2 (en) | 2013-09-05 | 2017-01-03 | Genentech, Inc. | Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases |
| EP3077401B1 (en) | 2013-12-06 | 2018-04-18 | Genentech, Inc. | Serine/threonine kinase inhibitors |
| JP6642942B2 (ja) | 2013-12-30 | 2020-02-12 | アレイ バイオファーマ、インコーポレイテッド | セリン／トレオニンキナーゼ阻害剤 |
| KR102379517B1 (ko) | 2013-12-30 | 2022-03-25 | 제넨테크, 인크. | 세린/트레오닌 키나아제 억제제 |
| WO2016106009A1 (en) * | 2014-12-22 | 2016-06-30 | Eli Lilly And Company | Erk inhibitors |
| WO2017180581A1 (en) | 2016-04-15 | 2017-10-19 | Genentech, Inc. | Diagnostic and therapeutic methods for cancer |
| CN106749117B (zh) * | 2016-11-29 | 2018-10-09 | 北京怡力生物科技有限公司 | 一种3-氨基甲基四氢呋喃的制备方法 |
| RU2019133646A (ru) | 2017-03-30 | 2021-04-30 | Ф. Хоффманн-Ля Рош Аг | Изохинолины в качестве ингибиторов hpk1 |
| JP6906105B2 (ja) * | 2017-06-16 | 2021-07-21 | 成都先導薬物開発股▲ふん▼有限公司Ｈｉｔｇｅｎ Ｌｔｄ． | Ｒｏｃｋを阻害する化合物及びその使用 |
| AU2018329925B2 (en) | 2017-09-08 | 2025-05-29 | F. Hoffmann-La Roche Ag | Diagnostic and therapeutic methods for cancer |
| EP3752200A1 (en) | 2018-02-13 | 2020-12-23 | Vib Vzw | Targeting minimal residual disease in cancer with rxr antagonists |
| CN108558869B (zh) * | 2018-05-10 | 2019-04-09 | 西安培华学院 | 用于治疗肝癌的化合物及其制剂 |
| CN112601584A (zh) | 2018-07-24 | 2021-04-02 | 豪夫迈·罗氏有限公司 | 异喹啉化合物及其用途 |
| TW202024053A (zh) | 2018-10-02 | 2020-07-01 | 美商建南德克公司 | 異喹啉化合物及其用途 |
| US11612606B2 (en) | 2018-10-03 | 2023-03-28 | Genentech, Inc. | 8-aminoisoquinoline compounds and uses thereof |
| WO2020201991A1 (en) | 2019-04-02 | 2020-10-08 | Array Biopharma Inc. | Protein tyrosine phosphatase inhibitors |
| KR20220099958A (ko) * | 2019-10-01 | 2022-07-14 | 골드핀치 바이오 인코포레이티드 | Cdk5의 치환된 1,6-나프티리딘 억제제 |
| US12570640B2 (en) | 2020-09-02 | 2026-03-10 | Merck Sharp & Dohme Llc | 2-aminoquinazolines as LRRK2 inhibitors, pharmaceutical compositions, and uses thereof |
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| KR20070058022A (ko) | 2000-04-26 | 2007-06-07 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 배변을 촉진하는 의약 조성물 |
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| CN103635472B (zh) | 2011-02-28 | 2018-01-12 | 阵列生物制药公司 | 丝氨酸/苏氨酸激酶抑制剂 |
| JP6097289B2 (ja) | 2011-08-04 | 2017-03-15 | アレイ バイオファーマ、インコーポレイテッド | セリン／スレオニンキナーゼインヒビターとしてのキナゾリン化合物 |
| HUE053994T2 (hu) | 2012-03-01 | 2021-08-30 | Array Biopharma Inc | Szerin/treonin kináz inhibitorok |
-
2013
- 2013-08-27 AR ARP130103040A patent/AR092253A1/es unknown
- 2013-08-27 CA CA2882750A patent/CA2882750A1/en not_active Abandoned
- 2013-08-27 BR BR112015004548A patent/BR112015004548A2/pt not_active IP Right Cessation
- 2013-08-27 US US14/011,501 patent/US9388171B2/en active Active
- 2013-08-27 RU RU2015110985A patent/RU2644947C2/ru not_active IP Right Cessation
- 2013-08-27 CN CN201380051518.1A patent/CN105143200B/zh active Active
- 2013-08-27 JP JP2015529957A patent/JP6378182B2/ja active Active
- 2013-08-27 HK HK15111084.7A patent/HK1210174A1/xx unknown
- 2013-08-27 MX MX2015002508A patent/MX369989B/es active IP Right Grant
- 2013-08-27 EP EP13759395.0A patent/EP2888247B1/en active Active
- 2013-08-27 KR KR1020157007729A patent/KR20150047597A/ko not_active Withdrawn
- 2013-08-27 TW TW102130680A patent/TW201408658A/zh unknown
- 2013-08-27 WO PCT/US2013/056876 patent/WO2014036015A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| KR20150047597A (ko) | 2015-05-04 |
| BR112015004548A2 (pt) | 2017-08-08 |
| WO2014036015A1 (en) | 2014-03-06 |
| CA2882750A1 (en) | 2014-03-06 |
| RU2644947C2 (ru) | 2018-02-15 |
| JP2015526519A (ja) | 2015-09-10 |
| CN105143200B (zh) | 2018-10-16 |
| HK1210174A1 (en) | 2016-04-15 |
| US20140066453A1 (en) | 2014-03-06 |
| CN105143200A (zh) | 2015-12-09 |
| RU2015110985A (ru) | 2016-10-20 |
| AR092253A1 (es) | 2015-04-08 |
| MX2015002508A (es) | 2015-10-12 |
| TW201408658A (zh) | 2014-03-01 |
| MX369989B (es) | 2019-11-27 |
| EP2888247B1 (en) | 2020-03-25 |
| EP2888247A1 (en) | 2015-07-01 |
| US9388171B2 (en) | 2016-07-12 |
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