JP2013506638A - ステアロイル−ＣｏＡデサチュラーゼを調節するピラゾール誘導体 - Google Patents
ステアロイル−ＣｏＡデサチュラーゼを調節するピラゾール誘導体 Download PDFInfo
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- JP2013506638A JP2013506638A JP2012531447A JP2012531447A JP2013506638A JP 2013506638 A JP2013506638 A JP 2013506638A JP 2012531447 A JP2012531447 A JP 2012531447A JP 2012531447 A JP2012531447 A JP 2012531447A JP 2013506638 A JP2013506638 A JP 2013506638A
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- Prior art keywords
- alkyl
- aryl
- cycloalkyl
- heteroaryl
- heterocyclyl
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- 108010087894 Fatty acid desaturases Proteins 0.000 title claims abstract description 90
- 102000016553 Stearoyl-CoA Desaturase Human genes 0.000 title claims abstract 7
- 150000003217 pyrazoles Chemical class 0.000 title 1
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- 230000000694 effects Effects 0.000 claims abstract description 41
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- 125000003118 aryl group Chemical group 0.000 claims description 229
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 194
- 125000001072 heteroaryl group Chemical group 0.000 claims description 175
- 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 description 132
- 125000000217 alkyl group Chemical group 0.000 claims description 107
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- 125000006690 (C2-C6) heterocyclyl group Chemical group 0.000 claims description 78
- 150000002431 hydrogen Chemical class 0.000 claims description 67
- 238000000034 method Methods 0.000 claims description 57
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 49
- 150000003839 salts Chemical class 0.000 claims description 47
- 125000006694 (C2-C10) heterocyclyl group Chemical group 0.000 claims description 46
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- 238000004519 manufacturing process Methods 0.000 claims description 24
- 125000001424 substituent group Chemical group 0.000 claims description 24
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- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 15
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims description 15
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- 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 4
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Classifications
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- 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
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
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- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A61P17/00—Drugs for dermatological disorders
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D403/14—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 three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
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- Chemical Kinetics & Catalysis (AREA)
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- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
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| US24763409P | 2009-10-01 | 2009-10-01 | |
| 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)
| Publication Number | Publication Date |
|---|---|
| JP2013506638A true JP2013506638A (ja) | 2013-02-28 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2023538434A (ja) * | 2020-08-19 | 2023-09-07 | ユニヴァーシティ・オブ・オックスフォード | Ｌｍｏ２タンパク質阻害剤 |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007046867A2 (en) * | 2005-05-19 | 2007-04-26 | Xenon Pharmaceuticals Inc. | Piperidine derivatives and their uses as therapeutic agents |
| WO2008024390A2 (en) * | 2006-08-24 | 2008-02-28 | Novartis Ag | 2- (pyrazin-2-yl) -thiazole and 2- (1h-pyraz0l-3-yl) -thiazole derivatives as well as related compounds as stearoyl-coa desaturase (scd) inhibitors for the treatment of metabolic, cardiovascular and other disorders |
| WO2008036715A1 (en) * | 2006-09-22 | 2008-03-27 | Novartis Ag | Heterocyclic organic compounds |
| WO2008103739A1 (en) * | 2007-02-21 | 2008-08-28 | Tte Technology, Inc. | System and method for decoding infra-red (ir) signals |
| WO2008127349A2 (en) * | 2006-08-15 | 2008-10-23 | Novartis Ag | Heterocyclic compounds suitable for the treatment of diseases related to elevated lipid level |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE272650T1 (de) | 1999-03-29 | 2004-08-15 | Uutech Ltd | Analoge des magensaft inhibierenden peptides und ihre verwendung für die behandlung von diabetes |
| DE60039111D1 (de) | 1999-09-28 | 2008-07-17 | Bayer Corp | Agonisten des rezeptors 3 (r3) von pituitary adenylate cyclase aktivierendem peptid (pacap) und ihre pharmakologische verwendung |
| EP1315831B8 (en) | 2000-02-24 | 2010-09-01 | Xenon Pharmaceuticals Inc. | Stearoyl-coa desaturase to identify triglyceride reducing therapeutic agents |
| EP1322767B1 (en) | 2000-09-26 | 2008-07-23 | Xenon Pharmaceuticals Inc. | Methods and compositions employing a stearoyl-coa desaturase-hscd5 |
| EP2289510A1 (en) * | 2004-09-20 | 2011-03-02 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-coa desaturase enzymes |
| US7767677B2 (en) * | 2004-09-20 | 2010-08-03 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors |
| CA2715947C (en) * | 2008-02-20 | 2016-10-25 | Novartis Ag | Heterocyclic inhibitors of stearoyl-coa desaturase |
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2010
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- 2010-10-01 EP EP10761003A patent/EP2483264A1/en not_active Withdrawn
- 2010-10-01 PE PE2012000427A patent/PE20121439A1/es not_active Application Discontinuation
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- 2012-04-26 MA MA34807A patent/MA33693B1/fr unknown
- 2012-04-27 EC ECSP12011837 patent/ECSP12011837A/es unknown
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007046867A2 (en) * | 2005-05-19 | 2007-04-26 | Xenon Pharmaceuticals Inc. | Piperidine derivatives and their uses as therapeutic agents |
| WO2008127349A2 (en) * | 2006-08-15 | 2008-10-23 | Novartis Ag | Heterocyclic compounds suitable for the treatment of diseases related to elevated lipid level |
| WO2008024390A2 (en) * | 2006-08-24 | 2008-02-28 | Novartis Ag | 2- (pyrazin-2-yl) -thiazole and 2- (1h-pyraz0l-3-yl) -thiazole derivatives as well as related compounds as stearoyl-coa desaturase (scd) inhibitors for the treatment of metabolic, cardiovascular and other disorders |
| WO2008036715A1 (en) * | 2006-09-22 | 2008-03-27 | Novartis Ag | Heterocyclic organic compounds |
| WO2008103739A1 (en) * | 2007-02-21 | 2008-08-28 | Tte Technology, Inc. | System and method for decoding infra-red (ir) signals |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2023538434A (ja) * | 2020-08-19 | 2023-09-07 | ユニヴァーシティ・オブ・オックスフォード | Ｌｍｏ２タンパク質阻害剤 |
| JP7850458B2 (ja) | 2020-08-19 | 2026-04-23 | ユニヴァーシティ・オブ・オックスフォード | Ｌｍｏ２タンパク質阻害剤 |
Also Published As
| Publication number | Publication date |
|---|---|
| MA33693B1 (fr) | 2012-10-01 |
| IL218294A0 (en) | 2012-04-30 |
| CR20120134A (es) | 2012-05-17 |
| PH12012500648A1 (en) | 2012-11-12 |
| ZA201201390B (en) | 2012-10-31 |
| SG178869A1 (en) | 2012-04-27 |
| CL2012000797A1 (es) | 2013-08-09 |
| BR112012007509A2 (pt) | 2016-11-22 |
| TN2012000085A1 (en) | 2013-09-19 |
| IN2012DN01913A (enExample) | 2015-07-24 |
| AU2010302577A1 (en) | 2012-03-15 |
| CO6761294A2 (es) | 2013-09-30 |
| KR20120080226A (ko) | 2012-07-16 |
| MX2012003938A (es) | 2012-08-03 |
| WO2011039358A1 (en) | 2011-04-07 |
| CA2776294A1 (en) | 2011-04-07 |
| EP2483264A1 (en) | 2012-08-08 |
| ECSP12011837A (es) | 2012-06-29 |
| US20130011361A1 (en) | 2013-01-10 |
| EA201200545A1 (ru) | 2012-12-28 |
| CN102574841A (zh) | 2012-07-11 |
| PE20121439A1 (es) | 2012-11-06 |
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