DE60039359D1 - Amide als pyruvatdehydrogenaseinhibitoren - Google Patents
Amide als pyruvatdehydrogenaseinhibitorenInfo
- Publication number
- DE60039359D1 DE60039359D1 DE60039359T DE60039359T DE60039359D1 DE 60039359 D1 DE60039359 D1 DE 60039359D1 DE 60039359 T DE60039359 T DE 60039359T DE 60039359 T DE60039359 T DE 60039359T DE 60039359 D1 DE60039359 D1 DE 60039359D1
- Authority
- DE
- Germany
- Prior art keywords
- formula
- ring
- fluoro
- compounds
- optionally substituted
- 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
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
- C07D295/182—Radicals derived from carboxylic acids
- C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
-
- 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
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/30—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
- C07D211/32—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
- C07D211/56—Nitrogen atoms
- C07D211/58—Nitrogen atoms attached in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
- C07D295/182—Radicals derived from carboxylic acids
- C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
- C07D295/26—Sulfur atoms
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9920821.7A GB9920821D0 (en) | 1999-09-04 | 1999-09-04 | Chemical compounds |
| GBGB9929835.8A GB9929835D0 (en) | 1999-12-18 | 1999-12-18 | Chemical compounds |
| PCT/GB2000/003297 WO2001017942A1 (en) | 1999-09-04 | 2000-08-30 | Amides as inhibitors for pyruvate dehydrogenase |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DE60039359D1 true DE60039359D1 (de) | 2008-08-14 |
Family
ID=26315903
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60039359T Expired - Fee Related DE60039359D1 (de) | 1999-09-04 | 2000-08-30 | Amide als pyruvatdehydrogenaseinhibitoren |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US6878712B1 (de) |
| EP (1) | EP1214287B1 (de) |
| JP (1) | JP2003508509A (de) |
| AT (1) | ATE399753T1 (de) |
| AU (1) | AU6715200A (de) |
| DE (1) | DE60039359D1 (de) |
| ES (1) | ES2307528T3 (de) |
| WO (1) | WO2001017942A1 (de) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2307528T3 (es) | 1999-09-04 | 2008-12-01 | Astrazeneca Ab | Amidas como inhibidores para la piruvato deshidrogenasa. |
| AR051026A1 (es) | 2004-09-20 | 2006-12-13 | Xenon Pharmaceuticals Inc | Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa |
| CA2580844A1 (en) | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as mediators of stearoyl-coa desaturase |
| US7829712B2 (en) | 2004-09-20 | 2010-11-09 | Xenon Pharmaceuticals Inc. | Pyridazine derivatives for inhibiting human stearoyl-CoA-desaturase |
| AR051090A1 (es) | 2004-09-20 | 2006-12-20 | Xenon Pharmaceuticals Inc | Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa |
| EP1799664A1 (de) | 2004-09-20 | 2007-06-27 | Xenon Pharmaceuticals Inc. | Heterozyklische derivate und ihre verwendung als stearoyl-coa-desaturase-inhibitoren |
| JP4958786B2 (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 | 複素環誘導体および治療薬としてのそれらの使用 |
| JP4958785B2 (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 | 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 |
| US8541457B2 (en) | 2005-06-03 | 2013-09-24 | Xenon Pharmaceuticals Inc. | Aminothiazole derivatives as human stearoyl-CoA desaturase inhibitors |
| EP2295432A1 (de) * | 2006-02-10 | 2011-03-16 | TransTech Pharma Inc. | Verfahren zur Herstellung von Aminobenzimidazolderivaten |
| ES2812537T3 (es) | 2009-10-21 | 2021-03-17 | Agios Pharmaceuticals Inc | Métodos y composiciones para trastornos relacionados con la proliferación celular |
| EP2491145B1 (de) | 2009-10-21 | 2016-03-09 | Agios Pharmaceuticals, Inc. | Verfahren und zusammensetzungen für zellproliferationsbedingte erkrankungen |
| GB201106817D0 (en) | 2011-04-21 | 2011-06-01 | Astex Therapeutics Ltd | New compound |
| GB201218850D0 (en) | 2012-10-19 | 2012-12-05 | Astex Therapeutics Ltd | Bicyclic heterocycle compounds and their uses in therapy |
| GB201218864D0 (en) | 2012-10-19 | 2012-12-05 | Astex Therapeutics Ltd | Bicyclic heterocycle compounds and their uses in therapy |
| GB201218862D0 (en) | 2012-10-19 | 2012-12-05 | Astex Therapeutics Ltd | Bicyclic heterocycle compounds and their uses in therapy |
| US9980973B2 (en) | 2012-10-19 | 2018-05-29 | Astex Therapeutics Limited | Bicyclic heterocycle compounds and their uses in therapy |
| ES2861180T3 (es) | 2013-03-13 | 2021-10-05 | Forma Therapeutics Inc | Derivados de 2-hidroxi-1-{4-[(4-fenil)fenil]carbonil}piperazin-1-il}etan-1-ona y compuestos relacionados como inhibidores de sintasa de ácido graso (FASN) para el tratamiento del cáncer |
| CA2933939C (en) | 2013-12-20 | 2021-03-16 | Astex Therapeutics Limited | Bicyclic heterocycle compounds and their uses in therapy |
| JP6847942B2 (ja) * | 2015-07-31 | 2021-03-24 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | 二環式複素環式誘導体 |
| JP6923551B2 (ja) * | 2016-03-29 | 2021-08-18 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | ピルバートデヒドロゲナーゼキナーゼのインヒビターとしてのｎ１−（３，３，３−トリフルオロ−２−ヒドロキシ−２−メチルプロピオニル）−ピペリジン誘導体 |
| CA3022231A1 (en) | 2016-04-28 | 2017-11-02 | Merck Patent Gmbh | Piperidinyl derivatives |
| WO2017210545A1 (en) | 2016-06-02 | 2017-12-07 | Cadent Therapeutics, Inc. | Potassium channel modulators |
| TW201825478A (zh) | 2016-12-19 | 2018-07-16 | 德商拜耳製藥公司 | ［４－（苯基磺醯基）哌嗪－１－-基］（１ｈ－１，２，３－三唑－４-基）甲酮 |
| CA3047191A1 (en) | 2016-12-19 | 2018-06-28 | Bayer Pharma Aktiengesellschaft | [4-(phenylsulfonyl)piperazin-1-yl](1h-1,2,3-triazol-4-yl)methanones |
| UA123810C2 (uk) | 2017-01-23 | 2021-06-02 | Цадент Терапеутікс, Інк. | Модулятори калієвих каналів |
| TWI767148B (zh) | 2018-10-10 | 2022-06-11 | 美商弗瑪治療公司 | 抑制脂肪酸合成酶(fasn) |
| CN113382633A (zh) | 2018-10-29 | 2021-09-10 | 福马治疗股份有限公司 | (4-(2-氟-4-(1-甲基-1H-苯并[d]咪唑-5-基)苯甲酰基)哌嗪-1-基)(1-羟基环丙基)甲酮的固体形式 |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2862100D1 (en) | 1977-10-12 | 1983-01-05 | Ici Plc | Acylanilides, process for their manufacture and pharmaceutical and veterinary compositions containing them |
| US4191775A (en) | 1977-12-15 | 1980-03-04 | Imperial Chemical Industries Limited | Amide derivatives |
| NZ197008A (en) | 1980-05-22 | 1984-10-19 | Ici Ltd | Acylanilide derivatives and pharmaceutical compositions |
| AU8961382A (en) | 1981-11-06 | 1983-05-12 | Imperial Chemical Industries Plc | Amide derivatives |
| US4537618A (en) | 1982-05-26 | 1985-08-27 | Ciba Geigy Corporation | N-phenylsulfonyl-N'-pyrimidinylureas |
| LU88769I2 (fr) | 1982-07-23 | 1996-11-05 | Zeneca Ltd | Bicalutamide et ses sels et esters pharmaceutiquement acceptables (Casodex (R)) |
| GB8617653D0 (en) | 1986-07-18 | 1986-08-28 | Ici Plc | Amide derivatives |
| GB8617652D0 (en) | 1986-07-18 | 1986-08-28 | Ici Plc | Acylanilide derivatives |
| GB9214120D0 (en) | 1991-07-25 | 1992-08-12 | Ici Plc | Therapeutic amides |
| EP0539329A1 (de) | 1991-10-25 | 1993-04-28 | Ciba-Geigy Ag | Acetylen-Verbindungen, verwendbar als Leukotrien-Antagonisten |
| SE9103397D0 (sv) | 1991-11-18 | 1991-11-18 | Kabi Pharmacia Ab | Nya substituerade salicylsyror |
| IL105558A (en) | 1992-05-18 | 1998-04-05 | Zeneca Ltd | Tertiary carbinols with channel activity potassium process for their preparation and pharmaceutical preparations containing them |
| GB9305295D0 (en) | 1993-03-15 | 1993-05-05 | Zeneca Ltd | Therapeutic compounds |
| GB9309716D0 (en) | 1993-05-12 | 1993-06-23 | Zeneca Ltd | Heterocyclic derivatives |
| GB9310069D0 (en) | 1993-05-17 | 1993-06-30 | Zeneca Ltd | Heterocyclic compounds |
| GB9310095D0 (en) | 1993-05-17 | 1993-06-30 | Zeneca Ltd | Therapeutic compounds |
| GB2278054A (en) | 1993-05-18 | 1994-11-23 | Zeneca Ltd | Compounds for the treatment of urinary incontinence |
| GB9505082D0 (en) | 1995-03-14 | 1995-05-03 | Zeneca Ltd | Medicament |
| GB9607458D0 (en) | 1996-04-10 | 1996-06-12 | Zeneca Ltd | Enzymatic process for stereoselective preparation of therapeutic amides |
| GB9804648D0 (en) | 1998-03-06 | 1998-04-29 | Zeneca Ltd | Chemical compounds |
| GB9805520D0 (en) | 1998-03-17 | 1998-05-13 | Zeneca Ltd | Chemical compounds |
| GB9811427D0 (en) | 1998-05-29 | 1998-07-22 | Zeneca Ltd | Chemical compounds |
| GB9811932D0 (en) | 1998-06-04 | 1998-07-29 | Zeneca Ltd | Chemical compunds |
| EP1214295B1 (de) | 1999-09-04 | 2006-11-02 | AstraZeneca AB | Hydroxyacetamidobenzolsulfonamidderivate |
| ES2307528T3 (es) | 1999-09-04 | 2008-12-01 | Astrazeneca Ab | Amidas como inhibidores para la piruvato deshidrogenasa. |
| BR0013694A (pt) | 1999-09-04 | 2002-05-21 | Astrazeneca Ab | Composto, processo para a preparação de um composto, composição farmacêutica, e, uso de um composto |
-
2000
- 2000-08-30 ES ES00954797T patent/ES2307528T3/es not_active Expired - Lifetime
- 2000-08-30 US US10/069,995 patent/US6878712B1/en not_active Expired - Fee Related
- 2000-08-30 WO PCT/GB2000/003297 patent/WO2001017942A1/en active IP Right Grant
- 2000-08-30 EP EP00954797A patent/EP1214287B1/de not_active Expired - Lifetime
- 2000-08-30 DE DE60039359T patent/DE60039359D1/de not_active Expired - Fee Related
- 2000-08-30 AU AU67152/00A patent/AU6715200A/en not_active Abandoned
- 2000-08-30 JP JP2001521689A patent/JP2003508509A/ja active Pending
- 2000-08-30 AT AT00954797T patent/ATE399753T1/de not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| EP1214287A1 (de) | 2002-06-19 |
| ATE399753T1 (de) | 2008-07-15 |
| AU6715200A (en) | 2001-04-10 |
| ES2307528T3 (es) | 2008-12-01 |
| US6878712B1 (en) | 2005-04-12 |
| EP1214287B1 (de) | 2008-07-02 |
| WO2001017942A1 (en) | 2001-03-15 |
| JP2003508509A (ja) | 2003-03-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 8364 | No opposition during term of opposition | ||
| 8339 | Ceased/non-payment of the annual fee |