JP2013532652A5 - - Google Patents
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- Publication number
- JP2013532652A5 JP2013532652A5 JP2013520164A JP2013520164A JP2013532652A5 JP 2013532652 A5 JP2013532652 A5 JP 2013532652A5 JP 2013520164 A JP2013520164 A JP 2013520164A JP 2013520164 A JP2013520164 A JP 2013520164A JP 2013532652 A5 JP2013532652 A5 JP 2013532652A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- independently
- compound according
- cycloalkyl
- optionally substituted
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 35
- 150000003839 salts Chemical class 0.000 claims description 14
- 206010028980 Neoplasm Diseases 0.000 claims description 5
- 201000011510 cancer Diseases 0.000 claims description 5
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 4
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 4
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 4
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 4
- 239000013543 active substance Substances 0.000 claims description 3
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- 208000035473 Communicable disease Diseases 0.000 claims description 2
- 206010061218 Inflammation Diseases 0.000 claims description 2
- 231100000433 cytotoxic Toxicity 0.000 claims description 2
- 230000001472 cytotoxic effect Effects 0.000 claims description 2
- 230000004054 inflammatory process Effects 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 claims 47
- 229910052739 hydrogen Inorganic materials 0.000 claims 15
- 239000001257 hydrogen Substances 0.000 claims 15
- 125000003118 aryl group Chemical group 0.000 claims 14
- 229910052736 halogen Inorganic materials 0.000 claims 14
- 150000002367 halogens Chemical class 0.000 claims 14
- 125000000623 heterocyclic group Chemical group 0.000 claims 14
- 125000001072 heteroaryl group Chemical group 0.000 claims 11
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 125000001424 substituent group Chemical group 0.000 claims 9
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims 7
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 6
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000006574 non-aromatic ring group Chemical group 0.000 claims 3
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 125000004618 benzofuryl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000005946 imidazo[1,2-a]pyridyl group Chemical group 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000036456 mitotic arrest Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 229910052760 oxygen Chemical group 0.000 claims 1
- 239000001301 oxygen Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 239000011593 sulfur Chemical group 0.000 claims 1
- 238000011282 treatment Methods 0.000 description 4
- 230000002265 prevention Effects 0.000 description 3
- 238000000034 method Methods 0.000 description 2
- 239000000825 pharmaceutical preparation Substances 0.000 description 2
- 239000000969 carrier Substances 0.000 description 1
- 239000000824 cytostatic agent Substances 0.000 description 1
- 230000001085 cytostatic effect Effects 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 150000004677 hydrates Chemical class 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10170683.6 | 2010-07-23 | ||
| EP10170683 | 2010-07-23 | ||
| PCT/EP2011/062683 WO2012010704A1 (en) | 2010-07-23 | 2011-07-22 | New aminopyrazoloquinazolines |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013532652A JP2013532652A (ja) | 2013-08-19 |
| JP2013532652A5 true JP2013532652A5 (https=) | 2015-09-03 |
| JP5991974B2 JP5991974B2 (ja) | 2016-09-14 |
Family
ID=43037625
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013520164A Active JP5991974B2 (ja) | 2010-07-23 | 2011-07-22 | 新規アミノピラゾロキナゾリン |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US8735386B2 (https=) |
| EP (1) | EP2595987B1 (https=) |
| JP (1) | JP5991974B2 (https=) |
| KR (1) | KR20130132394A (https=) |
| CN (1) | CN103097388A (https=) |
| AP (1) | AP2012006640A0 (https=) |
| AR (1) | AR082850A1 (https=) |
| AU (1) | AU2011281504A1 (https=) |
| BR (1) | BR112013000107A2 (https=) |
| CA (1) | CA2803467A1 (https=) |
| CL (1) | CL2012003745A1 (https=) |
| CO (1) | CO6670575A2 (https=) |
| EA (1) | EA201201661A1 (https=) |
| EC (1) | ECSP13012448A (https=) |
| GE (1) | GEP20156289B (https=) |
| MA (1) | MA34389B1 (https=) |
| MX (1) | MX2013000821A (https=) |
| PE (1) | PE20131143A1 (https=) |
| PH (1) | PH12013500152A1 (https=) |
| SG (1) | SG187548A1 (https=) |
| TW (1) | TW201217380A (https=) |
| UY (1) | UY33526A (https=) |
| WO (1) | WO2012010704A1 (https=) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013110585A1 (en) | 2012-01-23 | 2013-08-01 | Boehringer Ingelheim International Gmbh | 5, 8 -dihydro- 6h- pyrazolo [3, 4 -h] quinazolines as igf-lr/lr inhibitors |
| US9376437B2 (en) | 2013-03-13 | 2016-06-28 | Oncoceutics, Inc | 7-benzyl-4-(2-methylbenzyl)-2,4,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1H)-one, salts thereof and methods of using the same in combination therapy |
| KR102318238B1 (ko) * | 2013-11-15 | 2021-10-26 | 온코슈틱스 인코포레이티드 | 7-벤질-4-(2-메틸벤질)-2,4,6,7,8,9-헥사하이드로이미다조[1,2-a]피리도[3,4-e]피리미딘-5(1H)-온, 이의 염 및 이의 용도 |
| HUE052821T2 (hu) | 2015-01-30 | 2021-05-28 | Oncoceutics Inc | 7-benzil-4-(4-trifluormetil)benzil-1,2,6,7,8,9-hexahidroimidazo[1,2-a]pirido[3,4-e]pirimidin-5(4H)-on és sói és azok terápiában történõ alkalmazása |
| JP6664414B2 (ja) * | 2015-05-13 | 2020-03-13 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ＩＧＦ−１Ｒ／ＩＲ阻害薬としての新規５，８−ジメチル−９−フェニル−５，８−ジヒドロ−６Ｈ−ピラゾロ［３，４−ｈ］キナゾリン−２−イル）−（１Ｈ−ピラゾール−３−イル）−アミン及び誘導体 |
| EP3505519B1 (en) * | 2016-11-11 | 2022-01-05 | Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | Pyridinamine-substituted heterotricyclo compounds, preparation thereof, and use in medicines |
| EP3632904B1 (en) * | 2017-05-26 | 2022-04-20 | Jiangsu Atom Bioscience and Pharmaceutical Co., Ltd. | Urat1 inhibitors for promoting uric acid excretion |
| CN107383019B (zh) * | 2017-07-28 | 2019-10-15 | 江苏艾凡生物医药有限公司 | 吡唑并[4,3-h]喹唑啉类化合物及其用途 |
| WO2019206154A1 (zh) | 2018-04-24 | 2019-10-31 | 上海海雁医药科技有限公司 | Cdk4/6抑制剂及其药学上可接受的盐和多晶型物及其应用 |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| SG11202109443QA (en) | 2018-11-02 | 2021-09-29 | Fount Bio Inc | Crosslinked materials |
| US12570670B2 (en) | 2019-01-30 | 2026-03-10 | Yale University | Compounds, compositions, and methods for treating fibrosis |
| US11384083B2 (en) | 2019-02-15 | 2022-07-12 | Incyte Corporation | Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors |
| TW202100520A (zh) | 2019-03-05 | 2021-01-01 | 美商英塞特公司 | 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物 |
| BR112021016960A2 (pt) * | 2019-03-07 | 2021-11-23 | BioNTech SE | Processo para a preparação de uma imidazoquinolina substituída |
| WO2020205560A1 (en) | 2019-03-29 | 2020-10-08 | Incyte Corporation | Sulfonylamide compounds as cdk2 inhibitors |
| US20220175819A1 (en) * | 2019-04-19 | 2022-06-09 | Fount Bio, Inc. | Delivery and retention of active agents within the skin |
| WO2020223469A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer |
| US11447494B2 (en) | 2019-05-01 | 2022-09-20 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| CA3150681A1 (en) | 2019-08-14 | 2021-02-18 | Incyte Corporation | Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors |
| US11851426B2 (en) | 2019-10-11 | 2023-12-26 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| US11345681B1 (en) | 2020-06-05 | 2022-05-31 | Kinnate Biopharma Inc. | Inhibitors of fibroblast growth factor receptor kinases |
| CN111960974A (zh) * | 2020-08-28 | 2020-11-20 | 山东潍坊润丰化工股份有限公司 | 一种烯草酮中间体的合成方法 |
| CN121537408A (zh) | 2021-02-08 | 2026-02-17 | 上海复星医药产业发展有限公司 | 5，6-二氢噻吩并[3，4-h]喹唑啉类化合物 |
| US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
| US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3071830B2 (ja) * | 1995-10-02 | 2000-07-31 | エフ・ホフマン−ラ ロシュ アーゲー | ５ｈｔ２ｃ受容体アンタゴニストとしてのピリミジン誘導体 |
| BR122019010200B8 (pt) | 2003-05-22 | 2021-07-27 | Nerviano Medical Science S R L | compostos de pirazol-quinazolina, seus sais, produtos ou kits e composições farmacêuticas |
| CN1897950A (zh) | 2003-10-14 | 2007-01-17 | 惠氏公司 | 稠合芳基和杂芳基衍生物及其使用方法 |
-
2011
- 2011-07-20 US US13/187,100 patent/US8735386B2/en active Active
- 2011-07-21 UY UY0001033526A patent/UY33526A/es not_active Application Discontinuation
- 2011-07-22 PE PE2013000125A patent/PE20131143A1/es not_active Application Discontinuation
- 2011-07-22 EA EA201201661A patent/EA201201661A1/ru unknown
- 2011-07-22 WO PCT/EP2011/062683 patent/WO2012010704A1/en not_active Ceased
- 2011-07-22 AU AU2011281504A patent/AU2011281504A1/en not_active Abandoned
- 2011-07-22 AR ARP110102670A patent/AR082850A1/es unknown
- 2011-07-22 MA MA35577A patent/MA34389B1/fr unknown
- 2011-07-22 SG SG2013003645A patent/SG187548A1/en unknown
- 2011-07-22 GE GEAP201113008A patent/GEP20156289B/en unknown
- 2011-07-22 BR BR112013000107A patent/BR112013000107A2/pt not_active IP Right Cessation
- 2011-07-22 KR KR1020137003430A patent/KR20130132394A/ko not_active Withdrawn
- 2011-07-22 AP AP2012006640A patent/AP2012006640A0/xx unknown
- 2011-07-22 EP EP11734158.6A patent/EP2595987B1/en active Active
- 2011-07-22 PH PH1/2013/500152A patent/PH12013500152A1/en unknown
- 2011-07-22 TW TW100126062A patent/TW201217380A/zh unknown
- 2011-07-22 MX MX2013000821A patent/MX2013000821A/es active IP Right Grant
- 2011-07-22 CN CN201180043930XA patent/CN103097388A/zh active Pending
- 2011-07-22 JP JP2013520164A patent/JP5991974B2/ja active Active
- 2011-07-22 CA CA2803467A patent/CA2803467A1/en not_active Abandoned
-
2012
- 2012-12-28 CL CL2012003745A patent/CL2012003745A1/es unknown
-
2013
- 2013-01-22 CO CO13011464A patent/CO6670575A2/es active IP Right Grant
- 2013-02-19 EC ECSP13012448 patent/ECSP13012448A/es unknown
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