JP2009507758A5 - - Google Patents
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- Publication number
- JP2009507758A5 JP2009507758A5 JP2008511498A JP2008511498A JP2009507758A5 JP 2009507758 A5 JP2009507758 A5 JP 2009507758A5 JP 2008511498 A JP2008511498 A JP 2008511498A JP 2008511498 A JP2008511498 A JP 2008511498A JP 2009507758 A5 JP2009507758 A5 JP 2009507758A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- hydrogen
- unsubstituted
- alkyl
- unsubstituted lower
- 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
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- 125000000217 alkyl group Chemical group 0.000 claims 40
- 229910052739 hydrogen Inorganic materials 0.000 claims 39
- 239000001257 hydrogen Substances 0.000 claims 39
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 21
- 150000002431 hydrogen Chemical class 0.000 claims 17
- 125000003118 aryl group Chemical group 0.000 claims 16
- -1 hydroxy, formyl Chemical group 0.000 claims 16
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 15
- 229910052736 halogen Inorganic materials 0.000 claims 11
- 150000002367 halogens Chemical class 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 10
- 125000002947 alkylene group Chemical group 0.000 claims 8
- 125000001589 carboacyl group Chemical group 0.000 claims 8
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 7
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 5
- 125000004423 acyloxy group Chemical group 0.000 claims 4
- 125000001118 alkylidene group Chemical group 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 3
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 3
- 208000011231 Crohn disease Diseases 0.000 claims 3
- 206010061218 Inflammation Diseases 0.000 claims 3
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 3
- 201000004681 Psoriasis Diseases 0.000 claims 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 230000004054 inflammatory process Effects 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 239000001301 oxygen Substances 0.000 claims 3
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 3
- 125000004750 (C1-C6) alkylaminosulfonyl group Chemical group 0.000 claims 2
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 2
- 125000005278 alkyl sulfonyloxy group Chemical group 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- VBXYJTRDAAYDCJ-SFHVURJKSA-N chembl2170284 Chemical compound CC1=CC=CC=C1N1C(=O)C=CC(C=2C(=NN3CC[C@@H](CO)NC3=2)C=2C=CC(F)=CC=2)=N1 VBXYJTRDAAYDCJ-SFHVURJKSA-N 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 238000006467 substitution reaction Methods 0.000 claims 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 1
- AAILEWXSEQLMNI-UHFFFAOYSA-N 1h-pyridazin-6-one Chemical compound OC1=CC=CN=N1 AAILEWXSEQLMNI-UHFFFAOYSA-N 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- RPPJHJYVSWATLF-UHFFFAOYSA-N 6-[2'-(4-fluorophenyl)spiro[1,3-dioxolane-2,6'-5,7-dihydro-4H-pyrazolo[1,5-a]pyrimidine]-3'-yl]-2-(2-methylphenyl)pyridazin-3-one Chemical compound CC1=CC=CC=C1N1C(=O)C=CC(C=2C(=NN3CC4(CNC3=2)OCCO4)C=2C=CC(F)=CC=2)=N1 RPPJHJYVSWATLF-UHFFFAOYSA-N 0.000 claims 1
- KTPOXQVGTABKFF-UHFFFAOYSA-N 6-[2-(2,4-difluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3-one Chemical compound CC1=CC=CC=C1N1C(=O)C=CC(C=2C(=NN3CC(CO)CNC3=2)C=2C(=CC(F)=CC=2)F)=N1 KTPOXQVGTABKFF-UHFFFAOYSA-N 0.000 claims 1
- KDWXNVQYEFVHPZ-UHFFFAOYSA-N 6-[2-(2,4-difluorophenyl)-6-[(dimethylamino)methyl]-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3-one Chemical compound N=1N2CC(CN(C)C)CNC2=C(C2=NN(C(=O)C=C2)C=2C(=CC=CC=2)C)C=1C1=CC=C(F)C=C1F KDWXNVQYEFVHPZ-UHFFFAOYSA-N 0.000 claims 1
- SUDIDDCAFMIBIF-UHFFFAOYSA-N 6-[2-(4-fluorophenyl)-6,6-dimethyl-5,7-dihydro-4H-pyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3-one Chemical compound CC1=C(C=CC=C1)N1N=C(C=CC1=O)C1=C2NCC(C)(C)CN2N=C1C1=CC=C(F)C=C1 SUDIDDCAFMIBIF-UHFFFAOYSA-N 0.000 claims 1
- LYHNSWOZRDSWLX-UHFFFAOYSA-N 6-[2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3-one Chemical compound CC1=CC=CC=C1N1C(=O)C=CC(C=2C(=NN3CC(CO)CNC3=2)C=2C=CC(F)=CC=2)=N1 LYHNSWOZRDSWLX-UHFFFAOYSA-N 0.000 claims 1
- QXYRMVUWXFWUKP-UHFFFAOYSA-N 6-[2-(4-fluorophenyl)-6-hydroxy-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3-one Chemical compound CC1=CC=CC=C1N1C(=O)C=CC(C=2C(=NN3CC(O)CNC3=2)C=2C=CC(F)=CC=2)=N1 QXYRMVUWXFWUKP-UHFFFAOYSA-N 0.000 claims 1
- SXKMPLDBLZUHKW-UHFFFAOYSA-N 6-[2-(4-fluorophenyl)spiro[5,7-dihydro-4H-pyrazolo[1,5-a]pyrimidine-6,4'-oxane]-3-yl]-2-(2-methylphenyl)pyridazin-3-one Chemical compound CC1=CC=CC=C1N1C(=O)C=CC(C=2C(=NN3CC4(CCOCC4)CNC3=2)C=2C=CC(F)=CC=2)=N1 SXKMPLDBLZUHKW-UHFFFAOYSA-N 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 125000005194 alkoxycarbonyloxy group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000005281 alkyl ureido group Chemical group 0.000 claims 1
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 239000008177 pharmaceutical agent Substances 0.000 claims 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000003944 tolyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US71282505P | 2005-09-01 | 2005-09-01 | |
| US60/712,825 | 2005-09-01 | ||
| PCT/JP2006/317691 WO2007026950A1 (en) | 2005-09-01 | 2006-08-31 | Pyridazinone derivatives used for the treatment of pain |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009507758A JP2009507758A (ja) | 2009-02-26 |
| JP2009507758A5 true JP2009507758A5 (https=) | 2012-08-30 |
| JP5066516B2 JP5066516B2 (ja) | 2012-11-07 |
Family
ID=37607561
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008511498A Expired - Fee Related JP5066516B2 (ja) | 2005-09-01 | 2006-08-31 | 疼痛の治療に用いられるピリダジノン誘導体 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20090042856A1 (https=) |
| EP (1) | EP1919919A1 (https=) |
| JP (1) | JP5066516B2 (https=) |
| KR (1) | KR20080049758A (https=) |
| CN (1) | CN101268079B (https=) |
| AU (1) | AU2006285599A1 (https=) |
| BR (1) | BRPI0617100A2 (https=) |
| CA (1) | CA2620740A1 (https=) |
| IL (1) | IL189697A0 (https=) |
| NO (1) | NO20081572L (https=) |
| RU (1) | RU2008112290A (https=) |
| TW (1) | TW200745034A (https=) |
| WO (1) | WO2007026950A1 (https=) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200904421A (en) | 2007-05-03 | 2009-02-01 | Astellas Pharma Inc | New compounds |
| WO2009005675A1 (en) | 2007-06-28 | 2009-01-08 | Abbott Laboratories | Novel triazolopyridazines |
| CN102099036B (zh) | 2008-06-03 | 2015-05-27 | 英特芒尼公司 | 用于治疗炎性疾患和纤维化疾患的化合物和方法 |
| KR101851518B1 (ko) * | 2010-09-08 | 2018-04-23 | 스미또모 가가꾸 가부시끼가이샤 | 피리다지논 화합물 및 그 중간체의 제조 방법 |
| MX355016B (es) | 2011-10-06 | 2018-04-02 | Bayer Ip Gmbh | Heterociclilpiri(mi)dinilpirazoles como fungicidas. |
| JO3407B1 (ar) | 2012-05-31 | 2019-10-20 | Eisai R&D Man Co Ltd | مركبات رباعي هيدرو بيرازولو بيريميدين |
| AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
| CA2902686C (en) | 2013-04-25 | 2017-01-24 | Beigene, Ltd. | Fused heterocyclic compounds as protein kinase inhibitors |
| CN112552401B (zh) | 2013-09-13 | 2023-08-25 | 广州百济神州生物制药有限公司 | 抗pd1抗体及其作为治疗剂与诊断剂的用途 |
| MX382781B (es) | 2014-04-02 | 2025-03-13 | Intermune Inc | Piridinonas anti-fibroticas. |
| CN106604742B (zh) | 2014-07-03 | 2019-01-11 | 百济神州有限公司 | 抗pd-l1抗体及其作为治疗剂及诊断剂的用途 |
| CN111153859B (zh) * | 2015-04-15 | 2021-09-03 | 江苏恩华药业股份有限公司 | 哒嗪酮类衍生物及其应用 |
| US10864203B2 (en) | 2016-07-05 | 2020-12-15 | Beigene, Ltd. | Combination of a PD-1 antagonist and a RAF inhibitor for treating cancer |
| WO2018033853A2 (en) | 2016-08-16 | 2018-02-22 | Beigene, Ltd. | Crystalline form of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof |
| WO2018033135A1 (en) | 2016-08-19 | 2018-02-22 | Beigene, Ltd. | Use of a combination comprising a btk inhibitor for treating cancers |
| JP6832430B2 (ja) | 2016-08-31 | 2021-02-24 | アジオス ファーマシューティカルズ， インコーポレイテッド | 細胞代謝過程の阻害剤 |
| WO2018119142A1 (en) | 2016-12-21 | 2018-06-28 | Amgen Inc. | Anti-tnf alpha antibody formulations |
| US11555038B2 (en) | 2017-01-25 | 2023-01-17 | Beigene, Ltd. | Crystalline forms of (S)-7-(1-(but-2-ynoyl)piperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof |
| WO2018195155A1 (en) | 2017-04-18 | 2018-10-25 | Celgene Quanticel Research, Inc. | Therapeutic compounds |
| EP3645569A4 (en) | 2017-06-26 | 2021-03-24 | BeiGene, Ltd. | IMMUNOTHERAPY FOR LIVER CELL CARCINOMA |
| US11377449B2 (en) | 2017-08-12 | 2022-07-05 | Beigene, Ltd. | BTK inhibitors with improved dual selectivity |
| US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
| BR112020006677A2 (pt) | 2017-10-05 | 2020-10-06 | Fulcrum Therapeutics, Inc. | uso de inibidores p38 para reduzir a expressão de dux4 |
| WO2019108795A1 (en) | 2017-11-29 | 2019-06-06 | Beigene Switzerland Gmbh | Treatment of indolent or aggressive b-cell lymphomas using a combination comprising btk inhibitors |
| US20220249491A1 (en) | 2019-06-10 | 2022-08-11 | Beigene Switzerland Gmbh | Oral solid tablet comprising bruton's tyrosine kinase inhibitor and preparation method therefor |
| TW202112368A (zh) | 2019-06-13 | 2021-04-01 | 荷蘭商法西歐知識產權股份有限公司 | 用於治療有關dux4表現之疾病的抑制劑組合 |
| US11786531B1 (en) | 2022-06-08 | 2023-10-17 | Beigene Switzerland Gmbh | Methods of treating B-cell proliferative disorder |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5356897A (en) * | 1991-09-09 | 1994-10-18 | Fujisawa Pharmaceutical Co., Ltd. | 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines |
| AU4431000A (en) * | 1999-05-12 | 2000-12-05 | Fujisawa Pharmaceutical Co., Ltd. | Novel use |
| US20040152659A1 (en) * | 1999-05-12 | 2004-08-05 | Fujisawa Pharmaceutical Co. Ltd. | Method for the treatment of parkinson's disease comprising administering an A1A2a receptor dual antagonist |
| AUPQ441499A0 (en) * | 1999-12-02 | 2000-01-06 | Fujisawa Pharmaceutical Co., Ltd. | Novel compound |
| WO2006038734A1 (en) * | 2004-10-08 | 2006-04-13 | Astellas Pharma Inc. | Pyridazinone derivatives cytokines inhibitors |
-
2006
- 2006-08-31 WO PCT/JP2006/317691 patent/WO2007026950A1/en not_active Ceased
- 2006-08-31 CA CA002620740A patent/CA2620740A1/en not_active Abandoned
- 2006-08-31 CN CN2006800322174A patent/CN101268079B/zh not_active Expired - Fee Related
- 2006-08-31 BR BRPI0617100-1A patent/BRPI0617100A2/pt not_active IP Right Cessation
- 2006-08-31 TW TW095132103A patent/TW200745034A/zh unknown
- 2006-08-31 KR KR1020087007056A patent/KR20080049758A/ko not_active Ceased
- 2006-08-31 AU AU2006285599A patent/AU2006285599A1/en not_active Abandoned
- 2006-08-31 RU RU2008112290/04A patent/RU2008112290A/ru not_active Application Discontinuation
- 2006-08-31 EP EP06797567A patent/EP1919919A1/en not_active Withdrawn
- 2006-08-31 US US12/063,766 patent/US20090042856A1/en not_active Abandoned
- 2006-08-31 JP JP2008511498A patent/JP5066516B2/ja not_active Expired - Fee Related
-
2008
- 2008-02-24 IL IL189697A patent/IL189697A0/en unknown
- 2008-03-31 NO NO20081572A patent/NO20081572L/no not_active Application Discontinuation
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