JP2018529745A5 - - Google Patents
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- Publication number
- JP2018529745A5 JP2018529745A5 JP2018517532A JP2018517532A JP2018529745A5 JP 2018529745 A5 JP2018529745 A5 JP 2018529745A5 JP 2018517532 A JP2018517532 A JP 2018517532A JP 2018517532 A JP2018517532 A JP 2018517532A JP 2018529745 A5 JP2018529745 A5 JP 2018529745A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cycloalkyl
- heterocycloalkyl
- substituted
- unsubstituted
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 158
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 67
- 125000001424 substituent group Chemical group 0.000 claims 48
- 229910052739 hydrogen Inorganic materials 0.000 claims 41
- 239000001257 hydrogen Substances 0.000 claims 40
- 125000002619 bicyclic group Chemical group 0.000 claims 32
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 26
- 125000001425 triazolyl group Chemical group 0.000 claims 23
- 125000005843 halogen group Chemical group 0.000 claims 22
- 125000004076 pyridyl group Chemical group 0.000 claims 22
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 21
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 19
- 229910052757 nitrogen Inorganic materials 0.000 claims 18
- 125000002098 pyridazinyl group Chemical group 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 13
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 12
- YXDVRIQBOMUBEQ-UHFFFAOYSA-N 2-oxa-8-azaspiro[5.5]undecane Chemical compound C1CCNCC21COCCC2 YXDVRIQBOMUBEQ-UHFFFAOYSA-N 0.000 claims 11
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 10
- 125000003226 pyrazolyl group Chemical group 0.000 claims 10
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 8
- 229910052799 carbon Inorganic materials 0.000 claims 8
- 125000006413 ring segment Chemical group 0.000 claims 8
- 125000004432 carbon atom Chemical group C* 0.000 claims 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- LGKNCSVHCNCJQG-UHFFFAOYSA-N 1-azaspiro[4.5]decane Chemical compound C1CCNC21CCCCC2 LGKNCSVHCNCJQG-UHFFFAOYSA-N 0.000 claims 6
- SIQBPWRTJNBBER-UHFFFAOYSA-N 2,3,4,5-tetrahydro-1h-2-benzazepine Chemical compound C1CCNCC2=CC=CC=C21 SIQBPWRTJNBBER-UHFFFAOYSA-N 0.000 claims 6
- FTGUMOQCPJEKOR-UHFFFAOYSA-N 6-oxa-9-azaspiro[4.5]decane Chemical compound C1CCCC21OCCNC2 FTGUMOQCPJEKOR-UHFFFAOYSA-N 0.000 claims 6
- JFNPSSKPSOKMJH-UHFFFAOYSA-N 7-azaspiro[4.5]decane Chemical compound C1CCCC21CNCCC2 JFNPSSKPSOKMJH-UHFFFAOYSA-N 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 239000001301 oxygen Substances 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 125000003373 pyrazinyl group Chemical group 0.000 claims 6
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 6
- HVFHYYCWZWCTMW-UHFFFAOYSA-N 4-azaspiro[2.5]octane Chemical compound C1CC11NCCCC1 HVFHYYCWZWCTMW-UHFFFAOYSA-N 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 125000005605 benzo group Chemical group 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000002883 imidazolyl group Chemical group 0.000 claims 4
- 208000009304 Acute Kidney Injury Diseases 0.000 claims 3
- 208000033626 Renal failure acute Diseases 0.000 claims 3
- 201000011040 acute kidney failure Diseases 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 3
- AQNQGBUEVCAVML-UHFFFAOYSA-N oxazepane Chemical compound C1CCNOCC1 AQNQGBUEVCAVML-UHFFFAOYSA-N 0.000 claims 3
- WXLCDTBTIVJDCE-UHFFFAOYSA-N 1,4-oxazepine Chemical compound O1C=CC=NC=C1 WXLCDTBTIVJDCE-UHFFFAOYSA-N 0.000 claims 2
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 206010016654 Fibrosis Diseases 0.000 claims 2
- 208000024412 Friedreich ataxia Diseases 0.000 claims 2
- 208000032376 Lung infection Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- -1 Piridajini Chemical group 0.000 claims 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 208000019423 liver disease Diseases 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims 2
- RSJKGSCJYJTIGS-UHFFFAOYSA-N undecane Chemical compound CCCCCCCCCCC RSJKGSCJYJTIGS-UHFFFAOYSA-N 0.000 claims 2
- HDVHFHONOKCUHQ-UHFFFAOYSA-N 2,3,4,5-tetrahydro-1,4-benzoxazepine Chemical compound C1NCCOC2=CC=CC=C21 HDVHFHONOKCUHQ-UHFFFAOYSA-N 0.000 claims 1
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 206010072082 Environmental exposure Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 206010019799 Hepatitis viral Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010062016 Immunosuppression Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010064911 Pulmonary arterial hypertension Diseases 0.000 claims 1
- 206010062237 Renal impairment Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 208000024716 acute asthma Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 102000015395 alpha 1-Antitrypsin Human genes 0.000 claims 1
- 108010050122 alpha 1-Antitrypsin Proteins 0.000 claims 1
- 229940024142 alpha 1-antitrypsin Drugs 0.000 claims 1
- 206010003119 arrhythmia Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 230000000747 cardiac effect Effects 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 208000023819 chronic asthma Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000020832 chronic kidney disease Diseases 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 230000007850 degeneration Effects 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- HSUGRBWQSSZJOP-RTWAWAEBSA-N diltiazem Chemical group C1=CC(OC)=CC=C1[C@H]1[C@@H](OC(C)=O)C(=O)N(CCN(C)C)C2=CC=CC=C2S1 HSUGRBWQSSZJOP-RTWAWAEBSA-N 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000003511 endothelial effect Effects 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 230000001506 immunosuppresive effect Effects 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 230000002107 myocardial effect Effects 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 230000008518 non respiratory effect Effects 0.000 claims 1
- TVMXDCGIABBOFY-UHFFFAOYSA-N octane Chemical compound CCCCCCCC TVMXDCGIABBOFY-UHFFFAOYSA-N 0.000 claims 1
- 229960005489 paracetamol Drugs 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 201000011461 pre-eclampsia Diseases 0.000 claims 1
- 230000005855 radiation Effects 0.000 claims 1
- 238000007634 remodeling Methods 0.000 claims 1
- 230000000241 respiratory effect Effects 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 239000003053 toxin Substances 0.000 claims 1
- 231100000765 toxin Toxicity 0.000 claims 1
- 108700012359 toxins Proteins 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
- 230000008733 trauma Effects 0.000 claims 1
- 201000001862 viral hepatitis Diseases 0.000 claims 1
- 0 Cc1cccc(*)c1 Chemical compound Cc1cccc(*)c1 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562237655P | 2015-10-06 | 2015-10-06 | |
| US62/237,655 | 2015-10-06 | ||
| PCT/IB2016/055996 WO2017060854A1 (en) | 2015-10-06 | 2016-10-06 | Biaryl pyrazoles as nrf2 regulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018529745A JP2018529745A (ja) | 2018-10-11 |
| JP2018529745A5 true JP2018529745A5 (enExample) | 2019-11-21 |
Family
ID=57184570
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018517532A Pending JP2018529745A (ja) | 2015-10-06 | 2016-10-06 | Ｎｒｆ２レギュレーターとしてのビアリールピラゾール |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US10364256B2 (enExample) |
| EP (1) | EP3359532A1 (enExample) |
| JP (1) | JP2018529745A (enExample) |
| WO (1) | WO2017060854A1 (enExample) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2988338C (en) | 2015-06-15 | 2024-05-14 | Glaxosmithkline Intellectual Property Development Limited | Nrf2 regulators |
| CN108137557B (zh) | 2015-06-15 | 2021-09-07 | 葛兰素史密斯克莱知识产权发展有限公司 | Nrf2调节剂 |
| WO2017060855A1 (en) * | 2015-10-06 | 2017-04-13 | Glaxosmithkline Intellectual Property Development Limited | Arylcyclohexyl pyrazoles as nrf2 regulators |
| WO2018109642A1 (en) * | 2016-12-12 | 2018-06-21 | Glaxosmithkline Intellectual Property Development Limited | N-aryl pyrazoles as nrf2 regulators |
| ES2901617T3 (es) | 2016-12-14 | 2022-03-23 | Glaxosmithkline Ip Dev Ltd | Bisarilamidas como reguladores de NRF2 |
| US11117905B2 (en) | 2016-12-14 | 2021-09-14 | Glaxosmithkline Intellectual Property Development Limited | Bisaryl heterocycles as NRF2 activators |
| US11059816B2 (en) | 2016-12-15 | 2021-07-13 | Glaxosmithkline Intellectual Property Development Limited | Ether linked triazoles as NRF2 activators |
| WO2018165520A1 (en) | 2017-03-10 | 2018-09-13 | Vps-3, Inc. | Metalloenzyme inhibitor compounds |
| US11643407B2 (en) | 2018-05-23 | 2023-05-09 | Glaxosmithkline Intellectual Property Development Limited | Indanes as NRF2 activators |
| EP3813797A4 (en) * | 2018-06-27 | 2022-03-30 | Kindeva Drug Delivery L.P. | TIOTROPIUM FORMULATION AND INHALER |
| MX2021002060A (es) | 2018-08-20 | 2021-07-21 | Janssen Pharmaceutica Nv | Inhibidores de la interacción proteína-proteína keap1-nrf2. |
| CA3121952C (en) | 2018-12-05 | 2025-05-13 | Scohia Pharma, Inc. | MACROCYCLICAL COMPOUND AND ITS USES |
| CN113474349B (zh) * | 2019-02-15 | 2024-03-01 | 葛兰素史密斯克莱知识产权发展有限公司 | 作为nrf2活化剂的羟基吡啶并氧氮杂环庚三烯 |
| BR112021023927A2 (pt) | 2019-05-31 | 2022-02-08 | Ube Industries | Composto, e, composição farmacêutica |
| CN114727974A (zh) | 2019-07-30 | 2022-07-08 | 艾科尼佐治疗股份有限公司 | Hdac6抑制剂及其用途 |
| WO2023210741A1 (ja) | 2022-04-28 | 2023-11-02 | 第一三共株式会社 | ベンゾトリアゾール化合物 |
| EP4619399A1 (en) | 2022-11-16 | 2025-09-24 | Basf Se | New substituted tetrahydrobenzoxazepine |
| CN116120252B (zh) * | 2022-12-22 | 2024-10-29 | 浙江工业大学 | 一种雷米普利关键中间体衍生物的制备方法 |
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| US4778054A (en) | 1982-10-08 | 1988-10-18 | Glaxo Group Limited | Pack for administering medicaments to patients |
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| WO2013067036A1 (en) | 2011-10-31 | 2013-05-10 | Rutgers, The State University Of New Jersey | Direct inhibitors of keap1-nrf2 interaction as antioxidant inflammation modulators |
| EP2816023A4 (en) | 2012-02-13 | 2015-09-09 | Takeda Pharmaceutical | AROMATIC RING CONNECTION |
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| US20160046616A1 (en) | 2013-03-15 | 2016-02-18 | The Johns Hopkins University | Nrf2 small molecule inhibitors for cancer therapy |
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| TW201625601A (zh) | 2014-07-02 | 2016-07-16 | 諾華公司 | 噻吩－２－基－吡啶－２－基－１ｈ－吡唑－４－羧酸衍生物及其作為可溶性鳥苷酸環化酶活化劑之用途 |
| TW201625586A (zh) | 2014-07-02 | 2016-07-16 | 諾華公司 | 環己烯－１－基－吡啶－２－基－１ｈ－吡唑－４－羧酸衍生物及其作為可溶性鳥苷酸環化酶活化劑之用途 |
| TW201625584A (zh) | 2014-07-02 | 2016-07-16 | 諾華公司 | 茚滿及吲哚啉衍生物及其作為可溶性鳥苷酸環化酶活化劑之用途 |
| CN108137557B (zh) | 2015-06-15 | 2021-09-07 | 葛兰素史密斯克莱知识产权发展有限公司 | Nrf2调节剂 |
| JP2018517732A (ja) | 2015-06-15 | 2018-07-05 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ | Ｎｒｆ２レギュレーター |
| CA2988338C (en) | 2015-06-15 | 2024-05-14 | Glaxosmithkline Intellectual Property Development Limited | Nrf2 regulators |
| WO2017060855A1 (en) | 2015-10-06 | 2017-04-13 | Glaxosmithkline Intellectual Property Development Limited | Arylcyclohexyl pyrazoles as nrf2 regulators |
-
2016
- 2016-10-06 WO PCT/IB2016/055996 patent/WO2017060854A1/en not_active Ceased
- 2016-10-06 EP EP16784966.0A patent/EP3359532A1/en not_active Withdrawn
- 2016-10-06 US US15/765,354 patent/US10364256B2/en not_active Expired - Fee Related
- 2016-10-06 JP JP2018517532A patent/JP2018529745A/ja active Pending
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