JP2010523653A5 - - Google Patents
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- Publication number
- JP2010523653A5 JP2010523653A5 JP2010502995A JP2010502995A JP2010523653A5 JP 2010523653 A5 JP2010523653 A5 JP 2010523653A5 JP 2010502995 A JP2010502995 A JP 2010502995A JP 2010502995 A JP2010502995 A JP 2010502995A JP 2010523653 A5 JP2010523653 A5 JP 2010523653A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- hydropteridin
- ethyl
- methyl
- oxo
- 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.)
- Withdrawn
Links
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims description 116
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 106
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 100
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 100
- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims description 69
- 150000001875 compounds Chemical class 0.000 claims description 59
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims description 42
- 125000000217 alkyl group Chemical group 0.000 claims description 37
- -1 2-thiazolyl Chemical group 0.000 claims description 23
- 125000003118 aryl group Chemical group 0.000 claims description 23
- 229910052739 hydrogen Inorganic materials 0.000 claims description 23
- 239000001257 hydrogen Substances 0.000 claims description 22
- 125000001072 heteroaryl group Chemical group 0.000 claims description 17
- 150000002431 hydrogen Chemical class 0.000 claims description 17
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims description 16
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims description 12
- 125000002950 monocyclic group Chemical group 0.000 claims description 12
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims description 12
- 125000005843 halogen group Chemical group 0.000 claims description 10
- 125000000623 heterocyclic group Chemical group 0.000 claims description 10
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims description 8
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims description 8
- 125000003342 alkenyl group Chemical group 0.000 claims description 8
- 125000002947 alkylene group Chemical group 0.000 claims description 8
- 150000003857 carboxamides Chemical class 0.000 claims description 8
- 150000002148 esters Chemical class 0.000 claims description 8
- 239000000651 prodrug Substances 0.000 claims description 8
- 229940002612 prodrug Drugs 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 8
- 125000001424 substituent group Chemical group 0.000 claims description 7
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims description 6
- 239000012453 solvate Substances 0.000 claims description 6
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 6
- 108010087894 Fatty acid desaturases Proteins 0.000 claims description 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 5
- 102000016553 Stearoyl-CoA Desaturase Human genes 0.000 claims description 5
- 230000000302 ischemic effect Effects 0.000 claims description 5
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims description 4
- VNDHYTGVCGVETQ-UHFFFAOYSA-N 4-fluorobenzamide Chemical compound NC(=O)C1=CC=C(F)C=C1 VNDHYTGVCGVETQ-UHFFFAOYSA-N 0.000 claims description 4
- 125000003545 alkoxy group Chemical group 0.000 claims description 4
- 125000000304 alkynyl group Chemical group 0.000 claims description 4
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims description 4
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 4
- 201000010099 disease Diseases 0.000 claims description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 4
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims description 3
- 241000124008 Mammalia Species 0.000 claims description 3
- 239000003112 inhibitor Substances 0.000 claims description 3
- NQQRXZOPZBKCNF-NSCUHMNNSA-N (e)-but-2-enamide Chemical compound C\C=C\C(N)=O NQQRXZOPZBKCNF-NSCUHMNNSA-N 0.000 claims description 2
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims description 2
- YPIGHNIIXYSPKF-UHFFFAOYSA-N 3-fluorobenzamide Chemical compound NC(=O)C1=CC=CC(F)=C1 YPIGHNIIXYSPKF-UHFFFAOYSA-N 0.000 claims description 2
- WGRPQCFFBRDZFV-UHFFFAOYSA-N 3-methylbenzamide Chemical compound CC1=CC=CC(C(N)=O)=C1 WGRPQCFFBRDZFV-UHFFFAOYSA-N 0.000 claims description 2
- 201000001320 Atherosclerosis Diseases 0.000 claims description 2
- 101100240528 Caenorhabditis elegans nhr-23 gene Proteins 0.000 claims description 2
- 208000002249 Diabetes Complications Diseases 0.000 claims description 2
- 206010012655 Diabetic complications Diseases 0.000 claims description 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims description 2
- 208000002705 Glucose Intolerance Diseases 0.000 claims description 2
- 206010020772 Hypertension Diseases 0.000 claims description 2
- 206010022489 Insulin Resistance Diseases 0.000 claims description 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 208000008589 Obesity Diseases 0.000 claims description 2
- 208000018262 Peripheral vascular disease Diseases 0.000 claims description 2
- 208000017442 Retinal disease Diseases 0.000 claims description 2
- 206010038923 Retinopathy Diseases 0.000 claims description 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims description 2
- 125000000440 benzylamino group Chemical group [H]N(*)C([H])([H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims description 2
- DNSISZSEWVHGLH-UHFFFAOYSA-N butanamide Chemical compound CCCC(N)=O DNSISZSEWVHGLH-UHFFFAOYSA-N 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 230000002490 cerebral effect Effects 0.000 claims description 2
- 208000026106 cerebrovascular disease Diseases 0.000 claims description 2
- 208000029078 coronary artery disease Diseases 0.000 claims description 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 2
- 206010012601 diabetes mellitus Diseases 0.000 claims description 2
- 229910052736 halogen Inorganic materials 0.000 claims description 2
- 208000019622 heart disease Diseases 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 2
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims description 2
- 235000020824 obesity Nutrition 0.000 claims description 2
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 201000009104 prediabetes syndrome Diseases 0.000 claims description 2
- QLNJFJADRCOGBJ-UHFFFAOYSA-N propionamide Chemical compound CCC(N)=O QLNJFJADRCOGBJ-UHFFFAOYSA-N 0.000 claims description 2
- 230000001052 transient effect Effects 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 4
- 206010010904 Convulsion Diseases 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 0 C*N(c(nc(N*)nc1)c1N=C1*)C1=O Chemical compound C*N(c(nc(N*)nc1)c1N=C1*)C1=O 0.000 description 1
- 208000032382 Ischaemic stroke Diseases 0.000 description 1
- 208000006011 Stroke Diseases 0.000 description 1
- 125000000547 substituted alkyl group Chemical group 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91075007P | 2007-04-09 | 2007-04-09 | |
| PCT/US2007/080629 WO2008123891A1 (en) | 2007-04-09 | 2007-10-05 | PTERIDINONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010523653A JP2010523653A (ja) | 2010-07-15 |
| JP2010523653A5 true JP2010523653A5 (enExample) | 2011-12-08 |
Family
ID=39047496
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010502995A Withdrawn JP2010523653A (ja) | 2007-04-09 | 2007-10-05 | ステアロイルＣｏＡデサチュラーゼのインヒビターとして使用するためのプテリジノン誘導体 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US7662819B2 (enExample) |
| EP (1) | EP2131844A1 (enExample) |
| JP (1) | JP2010523653A (enExample) |
| CA (1) | CA2681560A1 (enExample) |
| WO (1) | WO2008123891A1 (enExample) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050119251A1 (en) * | 2001-12-21 | 2005-06-02 | Jian-Min Fu | Nicotinamide derivatives and their use as therapeutic agents |
| CN101083986A (zh) * | 2004-09-20 | 2007-12-05 | 泽农医药公司 | 双环杂环衍生物及其作为硬脂酰CoA去饱和酶(SCD)抑制剂的用途 |
| CA2580856A1 (en) * | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors |
| US7951805B2 (en) * | 2004-09-20 | 2011-05-31 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as mediators of stearoyl-CoA desaturase |
| EP1804799B1 (en) * | 2004-09-20 | 2013-08-21 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors |
| EP2029138A1 (en) * | 2005-06-03 | 2009-03-04 | Xenon Pharmaceuticals Inc. | Aminothiazole derivatives as human stearoyl-coa desaturase inhibitors |
| RU2009112397A (ru) * | 2006-10-05 | 2010-10-10 | Си Ви ТЕРАПЬЮТИКС, ИНК (US) | Бициклические азотсодержащие гетероциклические соединения для применения в качестве ингибиторов стеароил соа десатуразы |
| US7893066B2 (en) * | 2006-10-05 | 2011-02-22 | Gilead Palo Alto, Inc. | Pyridol[2,3-B]pyrazinones for use as stearoyl CoA desaturase inhibitors |
| US7662819B2 (en) * | 2007-04-09 | 2010-02-16 | Gilead Palo Alto, Inc. | Pteridinone derivatives for use as stearoyl CoA desaturase inhibitors |
| US20090105283A1 (en) * | 2007-04-11 | 2009-04-23 | Dmitry Koltun | 3-HYDROQUINAZOLIN-4-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS |
| US20080255161A1 (en) * | 2007-04-11 | 2008-10-16 | Dmitry Koltun | 3-HYDROQUINAZOLIN-4-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS |
| WO2009097995A1 (de) * | 2008-02-07 | 2009-08-13 | Sanofi-Aventis | Neue phenyl-substituierte imidazolidine, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| CA2719362A1 (en) * | 2008-04-04 | 2009-10-08 | Gilead Sciences, Inc. | Pyrrolotriazinone derivatives for use as stearoyl coa desaturase inhibitors |
| JP2011516498A (ja) * | 2008-04-04 | 2011-05-26 | ギリアード サイエンシーズ， インコーポレイテッド | ステアロイル−ＣｏＡデサチュラーゼの阻害剤として使用するためのトリアゾロピリジノン誘導体 |
| EP2276748A1 (en) * | 2008-04-10 | 2011-01-26 | Gilead Sciences, Inc. | Bicyclic nitrogen containing heterocyclic compounds for use as stearoyl coa desaturase inhibitors |
| WO2010045371A1 (en) * | 2008-10-15 | 2010-04-22 | Gilead Palo Alto, Inc. | Pyrido- and pyrimido (1, 2-a) pyrimidine compounds useful as stearoyl coa desaturase inhibitors |
| WO2010045374A1 (en) * | 2008-10-15 | 2010-04-22 | Gilead Palo Alto, Inc. | 3-hydroquinazolin-4-one derivatives for use as stearoyl coa desaturase inhibitors |
| US9358250B2 (en) | 2011-10-15 | 2016-06-07 | Genentech, Inc. | Methods of using SCD1 antagonists |
| EP3529245A4 (en) | 2016-10-24 | 2020-12-23 | Yumanity Therapeutics, Inc. | COMPOUNDS AND USES OF THE LATEST |
| MA47212A (fr) | 2017-01-06 | 2019-11-13 | Yumanity Therapeutics Inc | Méthodes de traitement de troubles neurologiques |
| WO2019084157A1 (en) | 2017-10-24 | 2019-05-02 | Yumanity Therapeutics, Inc. | COMPOUNDS AND USES THEREOF |
| ES3043183T3 (en) | 2018-03-23 | 2025-11-25 | Janssen Pharmaceutica Nv | Compounds and uses thereof |
| MA54829A (fr) | 2019-01-24 | 2021-12-01 | Yumanity Therapeutics Inc | Composés et leurs utilisations |
| EA202192047A1 (ru) | 2019-11-13 | 2021-12-08 | Юманити Терапьютикс, Инк. | Соединения и их применение |
| PE20231311A1 (es) | 2020-11-18 | 2023-08-24 | Deciphera Pharmaceuticals Llc | Inhibidores de gcn2 y perk quinasas y metodos de uso de los mismos |
| MX2024006627A (es) | 2021-12-03 | 2024-08-22 | Deciphera Pharmaceuticals Llc | Inhibidores de gcn2 y perk quinasa y metodos de uso de los mismos. |
| CN115010711B (zh) * | 2022-07-12 | 2024-12-03 | 江南大学 | 一种蝶啶7（8h）-酮类化合物及其在药学上的应用 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3845770A (en) * | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| US4326525A (en) * | 1980-10-14 | 1982-04-27 | Alza Corporation | Osmotic device that improves delivery properties of agent in situ |
| US5364620A (en) * | 1983-12-22 | 1994-11-15 | Elan Corporation, Plc | Controlled absorption diltiazem formulation for once daily administration |
| US5023252A (en) * | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| US5001139A (en) * | 1987-06-12 | 1991-03-19 | American Cyanamid Company | Enchancers for the transdermal flux of nivadipine |
| US4992445A (en) * | 1987-06-12 | 1991-02-12 | American Cyanamid Co. | Transdermal delivery of pharmaceuticals |
| BR9815785A (pt) | 1998-03-31 | 2000-12-05 | Warner Lambert Co | Quinoxalinonas como inibidores de protease de serina tal como fator xa e trombina |
| JP2003509425A (ja) | 1999-09-15 | 2003-03-11 | ワーナー−ランバート・カンパニー | キナーゼ阻害剤としてのプテリジノン |
| US7196090B2 (en) | 2002-07-25 | 2007-03-27 | Warner-Lambert Company | Kinase inhibitors |
| US7946750B2 (en) * | 2005-08-23 | 2011-05-24 | Innovative Concrete Solutions, Inc. | Composition for and method of pumping concrete |
| US7893066B2 (en) * | 2006-10-05 | 2011-02-22 | Gilead Palo Alto, Inc. | Pyridol[2,3-B]pyrazinones for use as stearoyl CoA desaturase inhibitors |
| RU2009112397A (ru) * | 2006-10-05 | 2010-10-10 | Си Ви ТЕРАПЬЮТИКС, ИНК (US) | Бициклические азотсодержащие гетероциклические соединения для применения в качестве ингибиторов стеароил соа десатуразы |
| US7662819B2 (en) * | 2007-04-09 | 2010-02-16 | Gilead Palo Alto, Inc. | Pteridinone derivatives for use as stearoyl CoA desaturase inhibitors |
| US20090105283A1 (en) * | 2007-04-11 | 2009-04-23 | Dmitry Koltun | 3-HYDROQUINAZOLIN-4-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS |
| US20080255161A1 (en) * | 2007-04-11 | 2008-10-16 | Dmitry Koltun | 3-HYDROQUINAZOLIN-4-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS |
| JP2011516498A (ja) * | 2008-04-04 | 2011-05-26 | ギリアード サイエンシーズ， インコーポレイテッド | ステアロイル−ＣｏＡデサチュラーゼの阻害剤として使用するためのトリアゾロピリジノン誘導体 |
| CA2719362A1 (en) * | 2008-04-04 | 2009-10-08 | Gilead Sciences, Inc. | Pyrrolotriazinone derivatives for use as stearoyl coa desaturase inhibitors |
-
2007
- 2007-10-05 US US11/868,407 patent/US7662819B2/en not_active Expired - Fee Related
- 2007-10-05 WO PCT/US2007/080629 patent/WO2008123891A1/en not_active Ceased
- 2007-10-05 EP EP07853822A patent/EP2131844A1/en not_active Withdrawn
- 2007-10-05 CA CA002681560A patent/CA2681560A1/en not_active Abandoned
- 2007-10-05 JP JP2010502995A patent/JP2010523653A/ja not_active Withdrawn
-
2010
- 2010-01-07 US US12/684,007 patent/US20100113463A1/en not_active Abandoned
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