JP4958785B2 - 複素環誘導体およびステアロイル−CoAデサチュラーゼインヒビターとしてのそれらの使用 - Google Patents
複素環誘導体およびステアロイル−CoAデサチュラーゼインヒビターとしてのそれらの使用 Download PDFInfo
- Publication number
- JP4958785B2 JP4958785B2 JP2007532640A JP2007532640A JP4958785B2 JP 4958785 B2 JP4958785 B2 JP 4958785B2 JP 2007532640 A JP2007532640 A JP 2007532640A JP 2007532640 A JP2007532640 A JP 2007532640A JP 4958785 B2 JP4958785 B2 JP 4958785B2
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- radical
- hydrogen
- aryl
- 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.)
- Expired - Fee Related
Links
- JSQLFBLIHMASQJ-UHFFFAOYSA-N O=C(c1ccc(N(CC2)CCN2c2ncccc2C(F)(F)F)nn1)NCCC1CC1 Chemical compound O=C(c1ccc(N(CC2)CCN2c2ncccc2C(F)(F)F)nn1)NCCC1CC1 JSQLFBLIHMASQJ-UHFFFAOYSA-N 0.000 description 1
Classifications
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having 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
- C07D237/24—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
- 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
- C07D401/02—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 two hetero rings
- C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D403/02—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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Child & Adolescent Psychology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US61164304P | 2004-09-20 | 2004-09-20 | |
| US60/611,643 | 2004-09-20 | ||
| PCT/US2005/033801 WO2006101521A2 (en) | 2004-09-20 | 2005-09-20 | Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008513504A JP2008513504A (ja) | 2008-05-01 |
| JP2008513504A5 JP2008513504A5 (enExample) | 2008-10-16 |
| JP4958785B2 true JP4958785B2 (ja) | 2012-06-20 |
Family
ID=37024256
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007532640A Expired - Fee Related JP4958785B2 (ja) | 2004-09-20 | 2005-09-20 | 複素環誘導体およびステアロイル−CoAデサチュラーゼインヒビターとしてのそれらの使用 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US7592343B2 (enExample) |
| EP (2) | EP1804799B1 (enExample) |
| JP (1) | JP4958785B2 (enExample) |
| CN (1) | CN101083993A (enExample) |
| AR (1) | AR051093A1 (enExample) |
| AU (1) | AU2005329423A1 (enExample) |
| BR (1) | BRPI0515482A (enExample) |
| CA (1) | CA2580857A1 (enExample) |
| TW (1) | TW200626139A (enExample) |
| WO (1) | WO2006101521A2 (enExample) |
Families Citing this family (44)
| 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 |
| EP1804799B1 (en) | 2004-09-20 | 2013-08-21 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors |
| MX2007003321A (es) * | 2004-09-20 | 2007-06-05 | Xenon Pharmaceuticals Inc | Derivados heterociclicos y su uso como agentes terapeuticos. |
| WO2006034312A1 (en) | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Bicyclic heterocyclic derivatives and their use as inhibitors of stearoyl-coa-desaturase (scd) |
| MX2007003327A (es) * | 2004-09-20 | 2007-06-05 | Xenon Pharmaceuticals Inc | Derivados heterociclicos, y su uso como mediadores de estearoil-coa desaturasa. |
| TW200626153A (en) * | 2004-09-20 | 2006-08-01 | Xenon Pharmaceuticals Inc | Heterocyclic derivatives and their use as therapeutic agents |
| AR051094A1 (es) * | 2004-09-20 | 2006-12-20 | Xenon Pharmaceuticals Inc | Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa |
| CN101083982A (zh) | 2004-09-20 | 2007-12-05 | 泽农医药公司 | 用于治疗硬脂酰CoA去饱和酶介导的疾病的杂环衍生物 |
| CN101084207A (zh) | 2004-09-20 | 2007-12-05 | 泽农医药公司 | 杂环衍生物及其作为硬脂酰CoA去饱和酶抑制剂的用途 |
| EP1807085B1 (en) | 2004-09-20 | 2013-08-21 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors |
| BRPI0611187A2 (pt) | 2005-06-03 | 2010-08-24 | Xenon Pharmaceuticals Inc | derivados aminotiazàis como inibidores da estearoil-coa desaturase humana |
| 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 |
| TW200826936A (en) | 2006-12-01 | 2008-07-01 | Merck Frosst Canada Ltd | Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase |
| GB0625654D0 (en) * | 2006-12-21 | 2007-01-31 | Smithkline Beecham Corp | Compounds |
| GB0625594D0 (en) * | 2006-12-21 | 2007-01-31 | Smithkline Beecham Corp | Compounds |
| GB0625604D0 (en) * | 2006-12-21 | 2007-01-31 | Smithkline Beecham Corp | Compounds |
| GB0625605D0 (en) * | 2006-12-21 | 2007-01-31 | Smithkline Beecham Corp | Compounds |
| AR064965A1 (es) | 2007-01-26 | 2009-05-06 | Merck Frosst Canada Inc | Derivados de azacicloalcanos como inhibidores de estearoil - coenzima a delta -9 desaturasa |
| US8575167B2 (en) | 2007-02-06 | 2013-11-05 | Takeda Pharmaceutical Company Limited | Spiro compounds having stearoyl-CoA desaturase action |
| US20080255161A1 (en) * | 2007-04-11 | 2008-10-16 | Dmitry Koltun | 3-HYDROQUINAZOLIN-4-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS |
| JP2010524987A (ja) | 2007-04-27 | 2010-07-22 | サノフィ−アベンティス | 2−ヘテロアリール−ピロロ[3,4−c]ピロール誘導体及びscd阻害剤としてのそれらの使用 |
| CN101932570B (zh) * | 2007-04-27 | 2014-11-26 | 普渡制药公司 | Trpv1拮抗剂以及其用途 |
| WO2008157844A1 (en) | 2007-06-21 | 2008-12-24 | Forest Laboratories Holdings Limited | Novel piperazine derivatives as inhibitors of stearoyl-coa desaturase |
| GB0714129D0 (en) * | 2007-07-19 | 2007-08-29 | Smithkline Beecham Corp | compounds |
| GB0715055D0 (en) * | 2007-08-02 | 2007-09-12 | Smithkline Beecham Corp | Compounds |
| GB0722075D0 (en) | 2007-11-09 | 2007-12-19 | Smithkline Beecham Corp | Compounds |
| JP2012505881A (ja) * | 2008-10-15 | 2012-03-08 | 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3−ヒドロキナゾリン−4−オン誘導体 |
| US9168248B2 (en) | 2009-02-17 | 2015-10-27 | Merck Canada Inc. | Spiro compounds useful as inhibitors of stearoyl-coenzyme A delta-9 desaturase |
| EP2398796A4 (en) * | 2009-02-23 | 2012-10-10 | Merck Canada Inc | HETEROCYCLIC DERIVATIVES AS INHIBITORS OF THE STEAROYL COENZYME A DELTA 9 DESATURASE |
| EP2459568A4 (en) | 2009-07-28 | 2013-02-27 | Merck Frosst Canada Ltd | NEW SPIRO COMPOUNDS AS AN INHIBITORS OF STEAROYL COENZYME A DELTA 9 DESATURASE |
| WO2011030312A1 (en) | 2009-09-10 | 2011-03-17 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | NOVEL INHIBITORS OF STEAROYL-CoA-DESATURASE-1 AND THEIR USES |
| EP3173411B1 (en) | 2011-06-22 | 2018-05-09 | Purdue Pharma L.P. | Trpv1 antagonists including dihydroxy substituent and uses thereof |
| KR20140084164A (ko) | 2011-10-15 | 2014-07-04 | 제넨테크, 인크. | 암의 치료를 위한 scd1 길항제 |
| WO2013134546A1 (en) | 2012-03-07 | 2013-09-12 | Mayo Foundation For Medical Education And Research | Methods and materials for treating cancer |
| WO2013175474A2 (en) | 2012-05-22 | 2013-11-28 | Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. | Selective inhibitors of undifferentiated cells |
| US10301273B2 (en) | 2014-08-07 | 2019-05-28 | Mayo Foundation For Medical Education And Research | Compounds and methods for treating cancer |
| SMT201900517T1 (it) | 2017-03-20 | 2019-11-13 | Forma Therapeutics Inc | Composizioni di pirrolopirrolo come attivatori di piruvato chinasi (pkr) |
| ES2968678T3 (es) * | 2018-04-27 | 2024-05-13 | Univ Osaka | Inhibidores del canal TRPC3 o TRPC6 |
| CN113166060B (zh) | 2018-09-19 | 2024-01-09 | 诺沃挪第克健康护理股份公司 | 用丙酮酸激酶激活化合物治疗镰状细胞病 |
| US11001588B2 (en) | 2018-09-19 | 2021-05-11 | Forma Therapeutics, Inc. | Activating pyruvate kinase R and mutants thereof |
| AU2019387370A1 (en) | 2018-11-30 | 2021-06-10 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| AU2019387367A1 (en) | 2018-11-30 | 2021-06-10 | Nuvation Bio Inc. | Diarylhydantoin compounds and methods of use thereof |
| CA3151612A1 (en) | 2019-09-19 | 2021-03-25 | George P. Luke | Pyruvate kinase r (pkr) activating compositions |
| US12128035B2 (en) | 2021-03-19 | 2024-10-29 | Novo Nordisk Health Care Ag | Activating pyruvate kinase R |
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Also Published As
| Publication number | Publication date |
|---|---|
| EP1804799B1 (en) | 2013-08-21 |
| AU2005329423A1 (en) | 2006-09-28 |
| EP1804799A2 (en) | 2007-07-11 |
| US20080125434A1 (en) | 2008-05-29 |
| AR051093A1 (es) | 2006-12-20 |
| CA2580857A1 (en) | 2006-09-28 |
| US8026360B2 (en) | 2011-09-27 |
| CN101083993A (zh) | 2007-12-05 |
| EP2269610A3 (en) | 2011-03-09 |
| BRPI0515482A (pt) | 2008-07-22 |
| JP2008513504A (ja) | 2008-05-01 |
| EP2269610A2 (en) | 2011-01-05 |
| US7592343B2 (en) | 2009-09-22 |
| US20090306090A1 (en) | 2009-12-10 |
| TW200626139A (en) | 2006-08-01 |
| WO2006101521A3 (en) | 2006-12-28 |
| WO2006101521A2 (en) | 2006-09-28 |
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