JP2009513563A - ヒトのステアロイル−CoAデサチュラーゼ阻害剤としてのアミノチアゾール誘導体 - Google Patents
ヒトのステアロイル−CoAデサチュラーゼ阻害剤としてのアミノチアゾール誘導体 Download PDFInfo
- Publication number
- JP2009513563A JP2009513563A JP2008525998A JP2008525998A JP2009513563A JP 2009513563 A JP2009513563 A JP 2009513563A JP 2008525998 A JP2008525998 A JP 2008525998A JP 2008525998 A JP2008525998 A JP 2008525998A JP 2009513563 A JP2009513563 A JP 2009513563A
- Authority
- JP
- Japan
- Prior art keywords
- carboxylic acid
- methyl
- methylthiazole
- amide
- thiazole
- 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
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- 0 Cc1c(C(NCc2ccccc2)=O)[s]c(NC(C(C2)C2c2ccccc2)=*)n1 Chemical compound Cc1c(C(NCc2ccccc2)=O)[s]c(NC(C(C2)C2c2ccccc2)=*)n1 0.000 description 2
- ODETUOQNLWOPHL-UHFFFAOYSA-N CCOC(c1c(C)nc(NC(c2ccncc2)=O)[s]1)=O Chemical compound CCOC(c1c(C)nc(NC(c2ccncc2)=O)[s]1)=O ODETUOQNLWOPHL-UHFFFAOYSA-N 0.000 description 1
- RMOZDIBMQMEMPB-UHFFFAOYSA-N Cc1c(C(NCCc2ccccc2)=O)[s]c(NC(c2ccncc2)=O)n1 Chemical compound Cc1c(C(NCCc2ccccc2)=O)[s]c(NC(c2ccncc2)=O)n1 RMOZDIBMQMEMPB-UHFFFAOYSA-N 0.000 description 1
- PFYVVYXJNXUVQZ-UHFFFAOYSA-N Cc1c(C(NCc2ccccc2)=O)[s]c(N(C)C(c2ccccc2)=O)n1 Chemical compound Cc1c(C(NCc2ccccc2)=O)[s]c(N(C)C(c2ccccc2)=O)n1 PFYVVYXJNXUVQZ-UHFFFAOYSA-N 0.000 description 1
- GNXKFBIOKRDWRR-UHFFFAOYSA-N Cc1c(C(NCc2ccccc2)=O)[s]c(NC(C2CCC2)=O)n1 Chemical compound Cc1c(C(NCc2ccccc2)=O)[s]c(NC(C2CCC2)=O)n1 GNXKFBIOKRDWRR-UHFFFAOYSA-N 0.000 description 1
- DYDBVXKCAUNBFQ-UHFFFAOYSA-N Cc1c(C(NCc2ccccc2)=O)[s]c(NC(c(cc2)ccc2C#N)=O)n1 Chemical compound Cc1c(C(NCc2ccccc2)=O)[s]c(NC(c(cc2)ccc2C#N)=O)n1 DYDBVXKCAUNBFQ-UHFFFAOYSA-N 0.000 description 1
- KLJXPGPPZGRRQJ-UHFFFAOYSA-N Cc1c(C(NCc2ccccc2)=O)[s]c(NC(c2cc(OC(F)(F)F)ccc2)=O)n1 Chemical compound Cc1c(C(NCc2ccccc2)=O)[s]c(NC(c2cc(OC(F)(F)F)ccc2)=O)n1 KLJXPGPPZGRRQJ-UHFFFAOYSA-N 0.000 description 1
- BMEUFKNLLGITPA-UHFFFAOYSA-N Cc1c(C(NCc2ccccc2)=O)[s]c(NC(c2ccc(C[n]3nccc3)cc2)=O)n1 Chemical compound Cc1c(C(NCc2ccccc2)=O)[s]c(NC(c2ccc(C[n]3nccc3)cc2)=O)n1 BMEUFKNLLGITPA-UHFFFAOYSA-N 0.000 description 1
- GHVHTMHPONITMN-UHFFFAOYSA-N Cc1c(C(NCc2ccccc2)=O)[s]c(NC(c2cccc(C#N)c2)=O)n1 Chemical compound Cc1c(C(NCc2ccccc2)=O)[s]c(NC(c2cccc(C#N)c2)=O)n1 GHVHTMHPONITMN-UHFFFAOYSA-N 0.000 description 1
- ACXLGEFHEPHVPV-UHFFFAOYSA-N O=C(c1c(Cc2ccccc2)nc(NC(c2ccccc2)=O)[s]1)NCc1ccccc1 Chemical compound O=C(c1c(Cc2ccccc2)nc(NC(c2ccccc2)=O)[s]1)NCc1ccccc1 ACXLGEFHEPHVPV-UHFFFAOYSA-N 0.000 description 1
- MZEDARPIUXMJLY-UHFFFAOYSA-N O=C(c1cnc(NC(c2ccccc2)=O)[s]1)NCc1ccccc1 Chemical compound O=C(c1cnc(NC(c2ccccc2)=O)[s]1)NCc1ccccc1 MZEDARPIUXMJLY-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/587—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with aliphatic hydrocarbon radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms, said aliphatic radicals being substituted in the alpha-position to the ring by a hetero atom, e.g. with m >= 0, Z being a singly or a doubly bound hetero atom
-
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- 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
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
-
- A—HUMAN NECESSITIES
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- 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
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
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- A61K31/60—Salicylic acid; Derivatives thereof
- A61K31/612—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid
- A61K31/616—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/26—Glucagons
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- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/28—Insulins
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- 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
- C07D417/02—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 two hetero rings
- C07D417/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D417/02—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 two hetero rings
- C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Gastroenterology & Hepatology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Immunology (AREA)
- Zoology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US68713305P | 2005-06-03 | 2005-06-03 | |
| PCT/US2006/021660 WO2007130075A1 (en) | 2005-06-03 | 2006-06-05 | Aminothiazole derivatives as human stearoyl-coa desaturase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013042546A Division JP2013100376A (ja) | 2005-06-03 | 2013-03-05 | ヒトのステアロイル−CoAデサチュラーゼ阻害剤としてのアミノチアゾール誘導体 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009513563A true JP2009513563A (ja) | 2009-04-02 |
| JP2009513563A5 JP2009513563A5 (https=) | 2009-07-02 |
Family
ID=37067442
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008525998A Pending JP2009513563A (ja) | 2005-06-03 | 2006-06-05 | ヒトのステアロイル−CoAデサチュラーゼ阻害剤としてのアミノチアゾール誘導体 |
| JP2013042546A Pending JP2013100376A (ja) | 2005-06-03 | 2013-03-05 | ヒトのステアロイル−CoAデサチュラーゼ阻害剤としてのアミノチアゾール誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013042546A Pending JP2013100376A (ja) | 2005-06-03 | 2013-03-05 | ヒトのステアロイル−CoAデサチュラーゼ阻害剤としてのアミノチアゾール誘導体 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US8541457B2 (https=) |
| EP (2) | EP2029138A1 (https=) |
| JP (2) | JP2009513563A (https=) |
| CN (1) | CN101208089A (https=) |
| AU (1) | AU2006343359A1 (https=) |
| BR (1) | BRPI0611187A2 (https=) |
| CA (1) | CA2618646A1 (https=) |
| MX (1) | MX2007015216A (https=) |
| WO (1) | WO2007130075A1 (https=) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009541367A (ja) * | 2006-06-27 | 2009-11-26 | インスティテュート オブ ファーマコロジー アンド トキシコロジー アカデミー オブ ミリタリー メディカル サイエンシス ピーエルエイ | 2,4,5−三置換チアゾール化合物、それを含有する医薬組成物、並びにその調製及び医学的使用 |
| WO2017099237A1 (ja) * | 2015-12-11 | 2017-06-15 | 帝人ファーマ株式会社 | アミノアゾール誘導体 |
| JP2019513762A (ja) * | 2016-04-11 | 2019-05-30 | ジェンフィGenfit | 胆汁うっ滞及び線維症の処置方法 |
| JP2021519263A (ja) * | 2018-03-23 | 2021-08-10 | ユマニティ セラピューティクス,インコーポレーテッド | 化合物及びその使用 |
Families Citing this family (47)
| 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 |
| JP5080256B2 (ja) * | 2004-09-20 | 2012-11-21 | 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 | 二環式複素環誘導体およびステアロイル−CoAデサチュラーゼ(SCD)のインヒビターとしてのそれらの使用 |
| CA2580857A1 (en) * | 2004-09-20 | 2006-09-28 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors |
| US7829712B2 (en) | 2004-09-20 | 2010-11-09 | Xenon Pharmaceuticals Inc. | Pyridazine derivatives for inhibiting human stearoyl-CoA-desaturase |
| AR051091A1 (es) * | 2004-09-20 | 2006-12-20 | Xenon Pharmaceuticals Inc | Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa |
| CA2580762A1 (en) | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as therapeutic agents |
| AU2005286648A1 (en) * | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors |
| EP1807085B1 (en) | 2004-09-20 | 2013-08-21 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors |
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| JP2009541367A (ja) * | 2006-06-27 | 2009-11-26 | インスティテュート オブ ファーマコロジー アンド トキシコロジー アカデミー オブ ミリタリー メディカル サイエンシス ピーエルエイ | 2,4,5−三置換チアゾール化合物、それを含有する医薬組成物、並びにその調製及び医学的使用 |
| WO2017099237A1 (ja) * | 2015-12-11 | 2017-06-15 | 帝人ファーマ株式会社 | アミノアゾール誘導体 |
| JPWO2017099237A1 (ja) * | 2015-12-11 | 2018-04-12 | 帝人ファーマ株式会社 | アミノアゾール誘導体 |
| US10689354B2 (en) | 2015-12-11 | 2020-06-23 | Teijin Pharma Limited | Aminoazole derivative |
| JP2019513762A (ja) * | 2016-04-11 | 2019-05-30 | ジェンフィGenfit | 胆汁うっ滞及び線維症の処置方法 |
| JP2021519263A (ja) * | 2018-03-23 | 2021-08-10 | ユマニティ セラピューティクス,インコーポレーテッド | 化合物及びその使用 |
| JP2024037913A (ja) * | 2018-03-23 | 2024-03-19 | ユマニティ セラピューティクス,インコーポレーテッド | 化合物及びその使用 |
| JP7517992B2 (ja) | 2018-03-23 | 2024-07-17 | ヤンセン ファーマシューティカ エヌ.ベー. | 化合物及びその使用 |
Also Published As
| Publication number | Publication date |
|---|---|
| CA2618646A1 (en) | 2007-11-15 |
| AU2006343359A8 (en) | 2008-04-03 |
| WO2007130075A8 (en) | 2008-01-24 |
| EP2029138A1 (en) | 2009-03-04 |
| EP2540296A1 (en) | 2013-01-02 |
| JP2013100376A (ja) | 2013-05-23 |
| US8541457B2 (en) | 2013-09-24 |
| CN101208089A (zh) | 2008-06-25 |
| US20100152187A1 (en) | 2010-06-17 |
| MX2007015216A (es) | 2008-02-22 |
| AU2006343359A1 (en) | 2007-11-15 |
| WO2007130075A1 (en) | 2007-11-15 |
| US20130096056A1 (en) | 2013-04-18 |
| BRPI0611187A2 (pt) | 2010-08-24 |
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