CN105051030A - 二氨基杂芳基取代的吲唑 - Google Patents
二氨基杂芳基取代的吲唑 Download PDFInfo
- Publication number
- CN105051030A CN105051030A CN201480017090.3A CN201480017090A CN105051030A CN 105051030 A CN105051030 A CN 105051030A CN 201480017090 A CN201480017090 A CN 201480017090A CN 105051030 A CN105051030 A CN 105051030A
- Authority
- CN
- China
- Prior art keywords
- alkyl
- group
- hydrogen
- pyrimidine
- base
- 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
- PUHCJOXSFBEREK-DJAIAVIWSA-N C1C2[C@@H](CC3)[S+]3CC12 Chemical compound C1C2[C@@H](CC3)[S+]3CC12 PUHCJOXSFBEREK-DJAIAVIWSA-N 0.000 description 1
- DGRQOCWXUCNTSB-UHFFFAOYSA-N Cc1c(CC(c2c3cccc2)N=C3C(CC2)=CCC(N=C)=CC2NC)c(F)cc(OCC=C)c1 Chemical compound Cc1c(CC(c2c3cccc2)N=C3C(CC2)=CCC(N=C)=CC2NC)c(F)cc(OCC=C)c1 DGRQOCWXUCNTSB-UHFFFAOYSA-N 0.000 description 1
Classifications
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- 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
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring 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
- A61K31/695—Silicon compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- 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
- C07D498/02—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 two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13160350 | 2013-03-21 | ||
| EP13160350.8 | 2013-03-21 | ||
| PCT/EP2014/055540 WO2014147144A1 (en) | 2013-03-21 | 2014-03-19 | Diaminoheteroaryl substituted indazoles |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105051030A true CN105051030A (zh) | 2015-11-11 |
Family
ID=47900948
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201480017090.3A Pending CN105051030A (zh) | 2013-03-21 | 2014-03-19 | 二氨基杂芳基取代的吲唑 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US20160052912A1 (https=) |
| EP (1) | EP2976334A1 (https=) |
| JP (1) | JP2016514717A (https=) |
| CN (1) | CN105051030A (https=) |
| AR (1) | AR095708A1 (https=) |
| CA (1) | CA2907730A1 (https=) |
| HK (1) | HK1217324A1 (https=) |
| TW (1) | TW201514167A (https=) |
| UY (1) | UY35499A (https=) |
| WO (1) | WO2014147144A1 (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA111754C2 (uk) | 2011-10-06 | 2016-06-10 | Байєр Фарма Акцієнгезелльшафт | Заміщені бензиліндазоли для застосування як інгібіторів bub1-кінази для лікування гіперпроліферативних захворювань |
| WO2013092512A1 (en) | 2011-12-21 | 2013-06-27 | Bayer Intellectual Property Gmbh | Substituted benzylpyrazoles |
| EP2976336A1 (en) * | 2013-03-21 | 2016-01-27 | Bayer Pharma Aktiengesellschaft | 3-heteroaryl substituted indazoles |
| EP2976335A1 (en) * | 2013-03-21 | 2016-01-27 | Bayer Pharma Aktiengesellschaft | Heteroaryl substituted indazoles |
| JP2016525076A (ja) | 2013-06-21 | 2016-08-22 | バイエル ファーマ アクチエンゲゼルシャフト | 置換されたベンジルピラゾール類 |
| CN105452237A (zh) | 2013-06-21 | 2016-03-30 | 拜耳制药股份公司 | 杂芳基取代的吡唑 |
| CA2928998A1 (en) | 2013-10-30 | 2015-05-07 | Bayer Pharma Aktiengesellschaft | Heteroaryl substituted pyrazoles |
| AR100886A1 (es) | 2014-06-17 | 2016-11-09 | Bayer Pharma AG | 3-amino-1,5,6,7-tetrahidro-4h-indol-4-onas |
| MA39484A (fr) | 2014-09-19 | 2016-03-24 | Bayer Pharma AG | Indazoles à substituants benzyle utilisés comme inhibiteurs de bub1 |
| WO2018122168A1 (en) | 2016-12-29 | 2018-07-05 | Bayer Pharma Aktiengesellschaft | Combinations of bub1 kinase and parp inhibitors |
| WO2018158175A1 (en) | 2017-02-28 | 2018-09-07 | Bayer Pharma Aktiengesellschaft | Combination of bub1 inhibitors |
| JP7090639B2 (ja) | 2017-04-11 | 2022-06-24 | サンシャイン・レイク・ファーマ・カンパニー・リミテッド | フッ素置換されたインダゾール化合物及びその使用 |
| WO2018206547A1 (en) | 2017-05-12 | 2018-11-15 | Bayer Pharma Aktiengesellschaft | Combination of bub1 and atr inhibitors |
| WO2018215282A1 (en) | 2017-05-26 | 2018-11-29 | Bayer Pharma Aktiengesellschaft | Combination of bub1 and pi3k inhibitors |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999066051A2 (en) * | 1998-06-16 | 1999-12-23 | Sugen, Inc. | Nek-related and bub1-related protein kinases |
| 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 |
| WO2013050438A1 (en) * | 2011-10-06 | 2013-04-11 | Bayer Pharma Aktiengesellschaft | Substituted benzylindazoles for use as bub1 kinase inhibitors in the treatment of hyperproliferative diseases. |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7378532B2 (en) * | 2004-03-26 | 2008-05-27 | Yung Shin Pharmaceutical Ind. Co., Ltd. | Fused pyrazolyl compound |
| SG174527A1 (en) * | 2009-03-27 | 2011-11-28 | Pathway Therapeutics Inc | Pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides and their use in cancer therapy |
| WO2013092512A1 (en) * | 2011-12-21 | 2013-06-27 | Bayer Intellectual Property Gmbh | Substituted benzylpyrazoles |
| WO2013167698A1 (en) * | 2012-05-11 | 2013-11-14 | Bayer Pharma Aktiengesellschaft | Substituted cycloalkenopyrazoles as bub1 inhibitors for the treatment of cancer |
| EP2976335A1 (en) * | 2013-03-21 | 2016-01-27 | Bayer Pharma Aktiengesellschaft | Heteroaryl substituted indazoles |
| EP2976336A1 (en) * | 2013-03-21 | 2016-01-27 | Bayer Pharma Aktiengesellschaft | 3-heteroaryl substituted indazoles |
-
2014
- 2014-03-19 EP EP14710931.8A patent/EP2976334A1/en not_active Withdrawn
- 2014-03-19 CN CN201480017090.3A patent/CN105051030A/zh active Pending
- 2014-03-19 CA CA2907730A patent/CA2907730A1/en not_active Abandoned
- 2014-03-19 JP JP2016503655A patent/JP2016514717A/ja active Pending
- 2014-03-19 HK HK16105232.9A patent/HK1217324A1/zh unknown
- 2014-03-19 WO PCT/EP2014/055540 patent/WO2014147144A1/en not_active Ceased
- 2014-03-19 US US14/778,604 patent/US20160052912A1/en not_active Abandoned
- 2014-03-21 TW TW103110771A patent/TW201514167A/zh unknown
- 2014-03-21 AR ARP140101321A patent/AR095708A1/es unknown
- 2014-03-24 UY UY0001035499A patent/UY35499A/es not_active Application Discontinuation
-
2017
- 2017-03-28 US US15/471,885 patent/US20170283396A1/en not_active Abandoned
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999066051A2 (en) * | 1998-06-16 | 1999-12-23 | Sugen, Inc. | Nek-related and bub1-related protein kinases |
| 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 |
| WO2013050438A1 (en) * | 2011-10-06 | 2013-04-11 | Bayer Pharma Aktiengesellschaft | Substituted benzylindazoles for use as bub1 kinase inhibitors in the treatment of hyperproliferative diseases. |
Non-Patent Citations (1)
| Title |
|---|
| JUNGSEOG KANG ET AL.: "Structure and Substrate Recruitment of the Human Spindle Checkpoint Kinase Bub1", 《MOLECULAR CELL》 * |
Also Published As
| Publication number | Publication date |
|---|---|
| US20160052912A1 (en) | 2016-02-25 |
| EP2976334A1 (en) | 2016-01-27 |
| HK1217324A1 (zh) | 2017-01-06 |
| AR095708A1 (es) | 2015-11-04 |
| JP2016514717A (ja) | 2016-05-23 |
| US20170283396A1 (en) | 2017-10-05 |
| UY35499A (es) | 2014-10-31 |
| WO2014147144A1 (en) | 2014-09-25 |
| TW201514167A (zh) | 2015-04-16 |
| CA2907730A1 (en) | 2014-09-25 |
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