DK2054397T3 - Småmolekylære hæmmere af kynurenin-3-monooxygenase - Google Patents
Småmolekylære hæmmere af kynurenin-3-monooxygenase Download PDFInfo
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- DK2054397T3 DK2054397T3 DK07814178.5T DK07814178T DK2054397T3 DK 2054397 T3 DK2054397 T3 DK 2054397T3 DK 07814178 T DK07814178 T DK 07814178T DK 2054397 T3 DK2054397 T3 DK 2054397T3
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- substituted
- methyl
- hydrogen
- alkyl
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Classifications
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- C07—ORGANIC CHEMISTRY
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- 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
- C07D277/38—Nitrogen atoms
- C07D277/50—Nitrogen atoms bound to hetero atoms
- C07D277/52—Nitrogen atoms bound to hetero atoms to sulfur atoms, e.g. sulfonamides
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- A—HUMAN NECESSITIES
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Claims (15)
1. Forbindelse med formlen la eller Ib:
hvor: når forbindelsen er af formlen la, er R1 og R2 uafhængigt udvalgt fra gruppen bestående af hydrogen, nitro, trifluormethyl og cyano; når forbindelsen er af formlen Ib, er R1 og R2 uafhængigt udvalgt fra gruppen bestående af hydrogen og nitro; R3 er hydrogen eller substitueret alkyl; R4 og R5 uafhængigt er hydrogen eller alkoxy; og R6 er udvalgt fra gruppen bestående af hydrogen, alkyl, substitueret alkyl, carboxyl, og carboxylester; eller en tautomer og/eller et farmaceutisk acceptabelt salt deraf med det forbehold, at kun én af R3 eller R6 kan være hydrogen, og med det yderligere forbehold, at når R3 er hydrogen, så er R6 ikke alkyl, og hvor alkyl i begreberne alkyl eller alkoxy refererer til monovalente, mættede, alifatiske hydrocarbylgrupper med fra 1 til 10 carbonatomer.
2. Forbindelse ifølge krav 1, hvor R1 og R2 uafhængigt er hydrogen eller nitro.
3. Forbindelse ifølge krav 1, hvor forbindelsen er af formlen la:
fa hvor: R1 og R2 er uafhængigt udvalgt fra gruppen bestående af hydrogen, nitro, trifluormethyl og cyano; R3 er hydrogen, eller substitueret alkyl; R4 og R5 er uafhængigt hydrogen, eller alkoxy; og R6er hydrogen, alkyl, substitueret alkyl, carboxyl, og carboxylester; eller en tautomer og/eller et farmaceutisk acceptabelt salt deraf, med det forbehold, at kun én af R3 eller R6 kan være hydrogen og med det yderligere forbehold, at når R3 er hydrogen, så er R6 ikke alkyl.
4. Forbindelse ifølge krav 1, hvor forbindelsen er af formlen la:
la hvor: R1 og R2 uafhængigt er udvalgt fra gruppen bestående af hydrogen, nitro, trifluormethyl eller cyano; R3 er substitueret a I kyl; R4 og R5 uafhængigt er hydrogen eller alkoxy og R6 er udvalgt fra gruppen bestående af hydrogen, alkyl, substitueret alkyl, carboxyl, og carboxylester; eller en tautomer og/eller et farmaceutisk acceptabelt salt deraf.
5. Forbindelse ifølge et hvilket som helst af de foregående krav, hvor mindst én af R1 og R2 er hydrogen eller nitro.
6. Forbindelse ifølge et hvilket som helst af kravene 3-5, hvor mindst én af R4 og R5er hydrogen eller methoxy;
7. Forbindelse ifølge et hvilket som helst af kravene 3-6, hvor R6 er udvalgt fra gruppen bestående af hydrogen, methyl, (ethylcarboxylat)methyl, ethylcarboxylat og methylcarboxylat.
8. Forbindelse ifølge et hvilket som helst af kravene 3 eller 5-7, hvor R3 er udvalgt fra gruppen bestående af hydrogen, hydroxymethyl, dimethylaminomethyl, pyrrolidin-1 -ylmethyl, piperidin-1 -ylmethyl, morpholinmethyl, (4-methylpiperazin-1 -yl)methyl, (diethylamino)methyl, (methylpropylamino)methyl, thiomorpholinmethyl og bis(hydroxyethyl)amino)methyl.
9. Forbindelse ifølge krav 4, hvor R3 er udvalgt fra gruppen bestående af hydroxymethyl, dimethylaminomethyl, pyrrolidin-1-ylmethyl, piperidin-1-ylmethyl, morpholinmethyl, (4-methylpiperazin-1 -yl)methyl, (diethylamino)methyl, (methylpropylamino)methyl, thiomorpholinmethyl og bis(hydroxyethyl)amino)methyl.
10. Forbindelse ifølge krav 3 eller 4, hvor R1 er hydrogen og R2 er nitro; R3 er udvalgt fra gruppen bestående af hydrogen, hydroxymethyl, dimethylaminomethyl, pyrrolidin-1 -ylmethyl, piperidin-1 -ylmethyl, morpholinmethyl, (4-methylpiperazin-1 -yl)methyl, (diethylamino)methyl, (methylpropylamino)methyl, thiomorpholinmethyl og bis(hydroxyethyl)amino)methyl; R4 og R5 er methoxy; og R6 er udvalgt fra gruppen bestående af hydrogen, methyl, (ethylcarboxylat)methyl, ethylcarboxylat, og methylcarboxylat; eller en tautomer og/eller et farmaceutisk acceptabelt salt deraf.
11. Forbindelse udvalgt fra gruppen bestående af 3.4- dimethoxy-N-[4-(3-nitrophenyl)-5-dimethylaminomethyl-1,3-thiazol-2-yl]benzensulfonamid; 3.4- dimethoxy-N-[4-(3-nitrophenyl)-5-(pyrrolidin-1-ylmethyl)-1,3-thiazol-2-yl]benzensulfonamid; 3.4- dimethoxy-N-[4-(3-nitrophenyl)-5-(piperidin-1-ylmethyl)-1,3-thiazol-2-yl]benzensulfonamid; 3.4- dimethoxy-N-[4-(3-nitrophenyl)-5-morpholinmethyl-1,3-thiazol-2-yl]benzensulfonamid; 3.4- dimethoxy-N-[4-(3-nitrophenyl)-5((4-methylpiperazin-1-yl]methyl)-1,3-thiazol-2-yl]benzensulfonamid; 3.4- dimethoxy-N-[4-(3-nitrophenyl)-5-(diethylamino)methyl-1,3-thiazol-2-yl]benzensulfonamid; 3.4- dimethoxy-N-[4-(3-nitrophenyl)-5-(methylpropylamino)methyl-1,3-thiazol-2- yl]benzensulfonamid; 3.4- dimethoxy-N-[4-(3-nitrophenyl)-5-thiomorpholinmethyl-1,3-thiazol-2-yl]benzensulfonamid; 3.4- dimethoxy-N-[4-(3-nitrophenyl)-5-(bis(hydroxyethyl)amino)methyl)-1,3-thiazol-2-yllbenzensulfonamid; 3.4- dimethoxy-N-[4-(3-nitrophenyl)-5-(hydroxymethyl)-1,3-thiazol-2-yl]benzensulfonamid; 3.4- dimethoxy-N-[4-(3-nitrophenyl)thiazol-2-y1]-N-(methyl)benzensulfonamid; 3.4- dimethoxy-N-[4-(3-nitrophenyl)thiazol-2-4-N-[(ethylcarboxylat)methyl]benzensulfonamid; 3.4- dimethoxy-N-[4-(3-nitrophenyl)thiazol-2-yl]-N--(ethylcarboxylat)benzensulfonamid; og 3.4- dimethoxy-N-[4-(3-nitrophenyl)thiazol-2-yl]-N-(methylcarboxylat)benzensulfonamid; eller tautomere deraf og/eller et farmaceutisk acceptabelt salt deraf.
12. Forbindelse ifølge krav 1, der er
eller en tautomer, eller et farmaceutisk acceptabelt salt deraf.
13. Farmaceutisk sammensætning omfattende en eller flere forbindelser ifølge et hvilket som helst af de foregående krav og en farmaceutisk acceptabel excipiens.
14. Fremgangsmåde in vitro til hæmning af aktivitet af kynurenin-3-monooxygenaseaktivitet, hvilken fremgangsmåde omfatter etablering af kontakt mellem celler med en effektiv mængde af én eller flere forbindelser ifølge et hvilket som helst af kravene 1-12.
15. Forbindelse til anvendelse i en fremgangsmåde til behandling af en sygdom medieret mindst delvist af kynurenin-3-monooxygenase, hvilken forbindelse er en forbindelse ifølge et hvilket som helst af kravene 1-12.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US83844606P | 2006-08-16 | 2006-08-16 | |
| US95109907P | 2007-07-20 | 2007-07-20 | |
| PCT/US2007/076139 WO2008022281A1 (en) | 2006-08-16 | 2007-08-16 | Small molecule inhibitors of kynurenine-3-monooxygenase |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK2054397T3 true DK2054397T3 (da) | 2016-01-18 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK07814178.5T DK2054397T3 (da) | 2006-08-16 | 2007-08-16 | Småmolekylære hæmmere af kynurenin-3-monooxygenase |
Country Status (4)
| Country | Link |
|---|---|
| US (2) | US7994338B2 (da) |
| EP (1) | EP2054397B1 (da) |
| DK (1) | DK2054397T3 (da) |
| WO (1) | WO2008022281A1 (da) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
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| DK2054397T3 (da) | 2006-08-16 | 2016-01-18 | J David Gladstone Inst A Testamentary Trust Established Under The Will Of J David Gladstone | Småmolekylære hæmmere af kynurenin-3-monooxygenase |
| EP2054056A4 (en) | 2006-08-16 | 2010-08-25 | J David Gladstone Inst A Testa | SMALL MOLECULAR INHIBITORS OF KYNURENINE-3-MONOOXYGENASE |
| DE102008019838A1 (de) * | 2008-04-19 | 2009-12-10 | Boehringer Ingelheim International Gmbh | Neue Arylsulfonylglycin-Derivate, deren Herstellung und deren Verwendung als Arzneimittel |
| UA103319C2 (en) | 2008-05-06 | 2013-10-10 | Глаксосмитклайн Ллк | Thiazole- and oxazole-benzene sulfonamide compounds |
| US8691824B2 (en) * | 2008-08-04 | 2014-04-08 | Chdi Foundation, Inc. | Certain kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof |
| CN102811620B (zh) * | 2010-01-25 | 2015-03-25 | Chdi基金会股份有限公司 | 一些犬尿氨酸-3-单加氧酶抑制剂、药物组合物及其使用方法 |
| AU2012300246A1 (en) | 2011-08-30 | 2014-03-06 | Chdi Foundation, Inc. | Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof |
| BR112014004741B1 (pt) | 2011-08-30 | 2021-10-13 | Chdi Foundation, Inc | Entidade química, seu uso e composição farmacêutica compreendendo a mesma |
| NZ702539A (en) | 2012-05-31 | 2016-11-25 | Phenex Pharmaceuticals Ag | Carboxamide or sulfonamide substituted thiazoles and related derivatives as modulators for the orphan nuclear receptor ror[gamma] |
| GB201322538D0 (en) | 2013-06-21 | 2014-02-05 | Immusmol Sas | Method for detecting small molecules in a sample |
| GB201322512D0 (en) | 2013-12-19 | 2014-02-05 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| AU2015289492B2 (en) | 2014-07-17 | 2020-02-20 | Chdi Foundation, Inc. | Methods and compositions for treating HIV-related disorders |
| GB201508864D0 (en) | 2015-05-22 | 2015-07-01 | Glaxosmithkline Ip Dev Ltd | Compounds |
| GB201508857D0 (en) | 2015-05-22 | 2015-07-01 | Glaxosmithkline Ip Dev Ltd | Compounds |
| ES2939646T3 (es) | 2016-10-13 | 2023-04-25 | Juno Therapeutics Inc | Métodos y composiciones de inmunoterapia que comprenden moduladores de la vía metabólica del triptófano |
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| US2921066A (en) | 1957-04-18 | 1960-01-12 | Bayer Ag | Sulfonamides |
| DE1057125B (de) | 1957-12-10 | 1959-05-14 | Bayer Ag | Verfahren zur Herstellung von 5-Arylsulfonamido-1,2,4-thiodiazolen |
| DE1121052B (de) | 1960-02-01 | 1962-01-04 | Nordmark Werke Gmbh | Verfahren zur Herstellung von 4, 5-substituierten 2-Amino-oxazolen |
| GB905369A (en) | 1960-02-01 | 1962-09-05 | Nordmark Werke Gmbh | A process for the production of 2-amino-oxazoles |
| DE1249869B (de) | 1964-06-16 | 1967-09-14 | Heidelberg Dr Takeo Takayanagi | Verfahren zur Herstellung cancerostatisch wirksamer Sulfonamidverbm dun gen |
| US4107288A (en) | 1974-09-18 | 1978-08-15 | Pharmaceutical Society Of Victoria | Injectable compositions, nanoparticles useful therein, and process of manufacturing same |
| AU5175490A (en) | 1989-02-27 | 1990-09-26 | Du Pont Merck Pharmaceutical Company, The | Novel sulfonamides as radiosensitizers |
| US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| DE69116576T2 (de) | 1991-09-05 | 1996-10-10 | Pharno Wedropharm Gmbh | Aromatische sulfonamidderivate, ihre verwendung als enzyminhibitoren und diese verbindungen enthaltende pharmazeutische zusammensetzungen |
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| AU689972B2 (en) * | 1994-11-29 | 1998-04-09 | Hisamitsu Pharmaceutical Co., Inc. | Antibacterial preparation or bactericide comprising 2-aminothiazole derivative and/or salt thereof |
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| GB9618349D0 (en) | 1996-09-03 | 1996-10-16 | Pharmacia Spa | N-substituted 2-amino-4-phenyl-4-oxo-butanoic acid derivatives with kynurenine-3-hydroxylase inhibitory activity |
| GB9725055D0 (en) | 1997-11-26 | 1998-01-28 | Pharmacia & Upjohn Spa | 1,3,4-thiadiazoles compounds |
| GB9725141D0 (en) | 1997-11-27 | 1998-01-28 | Pharmacia & Upjohn Spa | Benzenesulfonamide compounds |
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| JP2002129048A (ja) * | 2000-10-27 | 2002-05-09 | Fuji Photo Film Co Ltd | ジアゾニウム塩と離脱基を有するカプラーとを用いたアゾカップリング反応方法及びそのカプラーを含有する記録材料 |
| EA200400708A1 (ru) | 2001-11-22 | 2004-10-28 | Биовитрум Аб | Ингибиторы 11-бета-гидроксистероиддегидрогеназы типа 1 |
| IL160630A0 (en) | 2001-11-22 | 2004-07-25 | Biovitrum Ab | Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1 |
| EP1486490A1 (en) * | 2002-02-28 | 2004-12-15 | Takeda Chemical Industries, Ltd. | Azole compounds |
| JP2003292485A (ja) * | 2002-04-01 | 2003-10-15 | Yamanouchi Pharmaceut Co Ltd | スルホンアミド誘導体 |
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| FR2849598B1 (fr) | 2003-01-07 | 2006-09-22 | Merck Sante Sas | Utilisation d'inhibiteurs de la kynurenine-3-hydroxylase pour le traitement du diabete, par augmentation du nombre de cellules des ilots de langerhans |
| US7173030B2 (en) | 2003-05-21 | 2007-02-06 | Biovitrum Ab | Inhibitors of 11-β-hydroxy steroid dehydrogenase type 1 |
| EP1631558A1 (en) | 2003-05-21 | 2006-03-08 | Biovitrum Ab | Inhibitors of 11-beta-hydroxy steroid dehydrogenase type i |
| JP2009513523A (ja) | 2003-07-08 | 2009-04-02 | ノバルティス アクチエンゲゼルシャフト | ベンゼンスルホニルアミノ化合物およびそれらを含む医薬組成物 |
| TW200524888A (en) | 2003-08-08 | 2005-08-01 | Vertex Pharma | Compositions useful as inhibitors of voltage-gated ion channels |
| MXPA06006396A (es) | 2004-01-20 | 2006-08-23 | Warner Lambert Co | Inhibidores de hmg-coa reductasa basados en imidazol. |
| MXPA06012130A (es) | 2004-04-20 | 2007-01-31 | Transtech Pharma Inc | Derivados de tiazol y pirimidina substituidos como moduladores del receptor de melanocortina. |
| RU2008113211A (ru) | 2005-10-06 | 2009-10-10 | Санофи-Авентис (Fr) | N-[1, 3,4]-тиадиазол-2-илбензолсульфонамиды, способы их получения и их применение в качестве лекарственных средств |
| EP2054056A4 (en) | 2006-08-16 | 2010-08-25 | J David Gladstone Inst A Testa | SMALL MOLECULAR INHIBITORS OF KYNURENINE-3-MONOOXYGENASE |
| DK2054397T3 (da) | 2006-08-16 | 2016-01-18 | J David Gladstone Inst A Testamentary Trust Established Under The Will Of J David Gladstone | Småmolekylære hæmmere af kynurenin-3-monooxygenase |
-
2007
- 2007-08-16 DK DK07814178.5T patent/DK2054397T3/da active
- 2007-08-16 EP EP07814178.5A patent/EP2054397B1/en not_active Not-in-force
- 2007-08-16 US US11/840,138 patent/US7994338B2/en active Active
- 2007-08-16 WO PCT/US2007/076139 patent/WO2008022281A1/en not_active Ceased
-
2011
- 2011-06-29 US US13/171,930 patent/US8710237B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US20120022052A1 (en) | 2012-01-26 |
| US20080070905A1 (en) | 2008-03-20 |
| EP2054397A4 (en) | 2009-12-23 |
| EP2054397A1 (en) | 2009-05-06 |
| US7994338B2 (en) | 2011-08-09 |
| EP2054397B1 (en) | 2015-10-07 |
| US8710237B2 (en) | 2014-04-29 |
| WO2008022281A1 (en) | 2008-02-21 |
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