CA2776294A1 - Pyrazole derivatives which modulate stearoyl-coa desaturase - Google Patents
Pyrazole derivatives which modulate stearoyl-coa desaturase Download PDFInfo
- Publication number
- CA2776294A1 CA2776294A1 CA2776294A CA2776294A CA2776294A1 CA 2776294 A1 CA2776294 A1 CA 2776294A1 CA 2776294 A CA2776294 A CA 2776294A CA 2776294 A CA2776294 A CA 2776294A CA 2776294 A1 CA2776294 A1 CA 2776294A1
- Authority
- CA
- Canada
- Prior art keywords
- c4alkyl
- optionally substituted
- compound
- c10aryl
- pyrazole
- 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.)
- Abandoned
Links
- 108010087894 Fatty acid desaturases Proteins 0.000 title claims abstract description 91
- 102000016553 Stearoyl-CoA Desaturase Human genes 0.000 title claims abstract 7
- 150000003217 pyrazoles Chemical class 0.000 title 1
- 238000000034 method Methods 0.000 claims abstract description 59
- 230000000694 effects Effects 0.000 claims abstract description 42
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract description 41
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 29
- 150000001875 compounds Chemical class 0.000 claims description 250
- -1 C1-C7alkoxy Chemical group 0.000 claims description 138
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 114
- 239000001257 hydrogen Substances 0.000 claims description 94
- 229910052739 hydrogen Inorganic materials 0.000 claims description 94
- 201000010099 disease Diseases 0.000 claims description 79
- 125000003118 aryl group Chemical group 0.000 claims description 58
- 125000000217 alkyl group Chemical group 0.000 claims description 52
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 51
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 50
- 150000003839 salts Chemical class 0.000 claims description 47
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 44
- 125000001072 heteroaryl group Chemical group 0.000 claims description 43
- 208000035475 disorder Diseases 0.000 claims description 35
- 125000006690 (C2-C6) heterocyclyl group Chemical group 0.000 claims description 32
- 230000001404 mediated effect Effects 0.000 claims description 28
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 26
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 21
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- 238000002360 preparation method Methods 0.000 claims description 21
- 125000001424 substituent group Chemical group 0.000 claims description 21
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 20
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 20
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 20
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- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 16
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims description 16
- 125000006694 (C2-C10) heterocyclyl group Chemical group 0.000 claims description 16
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 16
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- PEDOHBLQSDEKAX-UHFFFAOYSA-N 3-[3-[(4-fluorophenyl)methyl]-2-oxoimidazolidin-1-yl]-n-(1,3-thiazol-2-ylmethyl)-1h-pyrazole-5-carboxamide Chemical compound C1=CC(F)=CC=C1CN1C(=O)N(C2=NNC(=C2)C(=O)NCC=2SC=CN=2)CC1 PEDOHBLQSDEKAX-UHFFFAOYSA-N 0.000 claims description 3
- JZCLAEDJPSTYEQ-UHFFFAOYSA-N 3-[3-[(4-fluorophenyl)methyl]-2-oxoimidazolidin-1-yl]-n-(pyridin-2-ylmethyl)-1h-pyrazole-5-carboxamide Chemical compound C1=CC(F)=CC=C1CN1C(=O)N(C2=NNC(=C2)C(=O)NCC=2N=CC=CC=2)CC1 JZCLAEDJPSTYEQ-UHFFFAOYSA-N 0.000 claims description 3
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- 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
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- 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
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| US61/247,634 | 2009-10-01 | ||
| PCT/EP2010/064672 WO2011039358A1 (en) | 2009-10-01 | 2010-10-01 | Pyrazole derivatives which modulate stearoyl-coa desaturase |
Publications (1)
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| CA2776294A1 true CA2776294A1 (en) | 2011-04-07 |
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| CA2850836A1 (en) | 2011-10-15 | 2013-04-18 | Genentech, Inc. | Methods of using scd1 antagonists |
| CN110099898B (zh) | 2016-10-24 | 2023-07-25 | 优曼尼蒂治疗公司 | 化合物及其用途 |
| CN110392833A (zh) | 2017-01-06 | 2019-10-29 | 优曼尼蒂治疗公司 | 治疗神经病症的方法 |
| WO2019084157A1 (en) | 2017-10-24 | 2019-05-02 | Yumanity Therapeutics, Inc. | COMPOUNDS AND USES THEREOF |
| CN112312913B (zh) | 2018-03-23 | 2024-03-08 | 詹森药业有限公司 | 化合物和其用途 |
| CN113906019A (zh) | 2019-01-24 | 2022-01-07 | 优曼尼蒂治疗公司 | 化合物及其用途 |
| EA202192047A1 (ru) | 2019-11-13 | 2021-12-08 | Юманити Терапьютикс, Инк. | Соединения и их применение |
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| CZ296858B6 (cs) | 1999-09-28 | 2006-07-12 | Bayer Corporation | Agonisté receptoru 3 (R3) hypofyzárního peptidu aktivujícího adenylátcyklázu (PACAP) a jejich farmaceutické pouzití |
| ATE475718T1 (de) | 2000-02-24 | 2010-08-15 | Xenon Pharmaceuticals Inc | Stearoyl-coa-desaturase zur identifizierung von triglyceridreduktionstherapeutika |
| US7232662B2 (en) | 2000-09-26 | 2007-06-19 | Xenon Pharmaceuticals Inc. | Methods and compositions employing a novel stearoyl-CoA desaturase-hSCD5 |
| CA2580855A1 (en) * | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors |
| JP4958784B2 (ja) * | 2004-09-20 | 2012-06-20 | ゼノン・ファーマシューティカルズ・インコーポレイテッド | ステアロイル−ＣｏＡデサチュラーゼ酵素によって媒介される疾患の処置のための複素環誘導体 |
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| US8068738B2 (en) * | 2007-02-21 | 2011-11-29 | Tte Technology, Inc. | System and method for decoding infra-red (IR) signals |
| MX2010009158A (es) * | 2008-02-20 | 2010-09-24 | Novartis Ag | Inhibidores heterociclicos de estearoil-coa-desaturasa. |
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| TN2012000085A1 (en) | 2013-09-19 |
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| MX2012003938A (es) | 2012-08-03 |
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| AU2010302577A1 (en) | 2012-03-15 |
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