AR078673A1 - Pirimidinas sustituidas con adamantiliminocarbonilo como inhibidores de 11-b-hsd1 826 - Google Patents
Pirimidinas sustituidas con adamantiliminocarbonilo como inhibidores de 11-b-hsd1 826Info
- Publication number
- AR078673A1 AR078673A1 ARP100103811A ARP100103811A AR078673A1 AR 078673 A1 AR078673 A1 AR 078673A1 AR P100103811 A ARP100103811 A AR P100103811A AR P100103811 A ARP100103811 A AR P100103811A AR 078673 A1 AR078673 A1 AR 078673A1
- Authority
- AR
- Argentina
- Prior art keywords
- carboxamide
- pyrimidin
- hydroxiadamantan
- cyclopentyl
- amino
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 150000003230 pyrimidines Chemical class 0.000 title 1
- -1 ethoxy, propoxy, cyclobutoxy, pyrrolidinyl Chemical group 0.000 abstract 14
- QDXGKRWDQCEABB-UHFFFAOYSA-N pyrimidine-5-carboxamide Chemical compound NC(=O)C1=CN=CN=C1 QDXGKRWDQCEABB-UHFFFAOYSA-N 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 abstract 1
- 101100451537 Caenorhabditis elegans hsd-1 gene Proteins 0.000 abstract 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 abstract 1
- 125000003566 oxetanyl group Chemical group 0.000 abstract 1
- 125000005476 oxopyrrolidinyl group Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 abstract 1
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
También se describen su uso en la inhibicion de 11betaHSD1, los procesos para prepararlos y las composiciones farmacéuticas que los comprenden. Reivindicacion 1: Un compuesto de formula (1) o una sal farmacéuticamente aceptable de este donde R1 es trifluorometilo, propilo, ciclobutilo, ciclopentilo, etoxi, propoxi, ciclobutoxi, pirrolidinilo o pirazolilo; R2 es tetrahidrofuranilo, 1-acetilpiperidilo, oxopiperidilo, dioxotiolanilo, hidroxiciclopentilo, hidroxietilo, hidroxipropilo, 2-(dimetilamino)-2-oxoetilo, metoxietilo, oxopirrolidinilo, 1-acetilpirrolidinilo, oxetanilo, hidroxidimetiletilo, 1,1-dioxotianilo, tetrahidropiranilo, (tetrahidrofuranil)metilenilo, (oxopirrolidinil)metilenilo, (metiloxopirrolidinil)metilenilo o pirrolidinilo; R3 es hidroxi, carboxi, carbamoílo o metilsulfonilo; R4 es hidrogeno o metilo; con la condicion de que dicho compuesto no sea: 4-ciclobutil-N-[(2r,5s)-5-hidroxiadamantan-2-iI]-2-[(2-hidroXi-1,1-dimetiletil)amino]pirimidin-5-carboxamida; 4-ciclobutil-N-[(2r,5s)-5-hidroxiadamantan-2-il]-2-[(2-hidroxietil)amino]pirimidin-5-carboxamida; 4-ciclobutil-N-[(2r,5s)-5-hidroxiadamantan-2-il]-2-[(2-hidroxi-2-metilpropil)amino]pirimidin-5-carboxamida; 4-ciclobutil-N-[(2r,5s)-5-hidroxiadamantan-2-il]-2-(oxetan-3-ilamino)pirimidin-5- carboxamida; 4-ciclobutil-2-[(1,1-dioxidotetrahidro-2H-tiopiran-4-il)amino]-N-[(2r,5s)-5-hidroxiadamantan-2-il]pirimidin-5-carboxamida; 4-ciclopentil-N-[(2-r,5s)-5-hidroxiadamantan-2-il]-2-oxetan-3-ilamino)pirimidin-5-carboxamida; 4-ciclopentil-2-[(1,1-dioxotian-4-il)amino]-N-[(2r,5s)-5-hidroxiadamantan-2-il]pirimidin-5-carboxamida; 4-ciclopentil-N-[(2r,5s)-5-hidroxiadamantan-2-il]-2-[(2-hidroxi-2-metilpropil)amino]pirimidin-5-carboxamida; 4-ciclopentil-N-[(2r,5s)-5-hidroxiadamantan-2-iI]-2-(2-hidroxietilamino)pirimidin-5-carboxamida; 4-ciclopentil-N-[(2r5s)-5-hidroxiadamantan-2-il]-2-[(1-hidroxi-2-metilpropan-2-il)amino]pirimidin-5-carboxamida; 4-ciclopentil-N-[(2r,5s)-5-hidroxiadamantan-2-il]-2-(oxan-4-ilamino)pirimidin-5-carboxamida; 4-ciclopentil-N-[(2r,5s)-5-hidroxiadamantan-2-iI]-2-[[(3R)-oxolan-3-il]amino]pirimidin-5-carboxamida; 4-ciclopentil-N-[(2r,5s)-5-hidroxiadamantan-2-iI]-2-[[(3S)-oxolan-3-il]amino]pirimidin-5-carboxamida; 4-etoxi-N-[(2r,5s)-5-hidroxitriciclo[3.3.1.13,7]dec-2-il]-2-(oxetan-3-ilamino)pirimidin-5-carboxamida; o N-[(2r,5s)-5-hidroxitriciclo[3.3.1.13,7]dec-2-il]-4-(1-metiletoxi)-2-(oxetan-3-ilamino)pirimidin-5-carboxamida.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25319109P | 2009-10-20 | 2009-10-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR078673A1 true AR078673A1 (es) | 2011-11-23 |
Family
ID=43879772
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100103811A AR078673A1 (es) | 2009-10-20 | 2010-10-19 | Pirimidinas sustituidas con adamantiliminocarbonilo como inhibidores de 11-b-hsd1 826 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20110092526A1 (es) |
| AR (1) | AR078673A1 (es) |
| TW (1) | TW201118085A (es) |
| UY (1) | UY32954A (es) |
| WO (1) | WO2011049520A1 (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200827346A (en) * | 2006-11-03 | 2008-07-01 | Astrazeneca Ab | Chemical compounds |
| TW200836719A (en) * | 2007-02-12 | 2008-09-16 | Astrazeneca Ab | Chemical compounds |
| EP2244705A1 (en) * | 2008-02-04 | 2010-11-03 | AstraZeneca AB | Novel crystalline forms of 4- [4- (2-adamantylcarbam0yl) -5-tert-butyl-pyrazol-1-yl]benzoic acid |
| KR20110002475A (ko) * | 2008-04-22 | 2011-01-07 | 아스트라제네카 아베 | 치환 피리미딘-5-카르복시아미드 281 |
| ES2575370T3 (es) * | 2011-06-10 | 2016-06-28 | Sk Biopharmaceuticals Co., Ltd. | Derivados de 5-carbamoil-adamantan-2-il amida, sales farmacéuticamente aceptables de los mismos y procesos de preparación de los mismos |
| EP3235813A1 (en) | 2016-04-19 | 2017-10-25 | Cidqo 2012, S.L. | Aza-tetra-cyclo derivatives |
| KR102006547B1 (ko) * | 2017-11-16 | 2019-08-01 | 서울대학교산학협력단 | 벤즈아미드 유도체 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 염증질환의 치료 또는 예방용 약학적 조성물 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE482747T1 (de) * | 2003-04-11 | 2010-10-15 | High Point Pharmaceuticals Llc | Neue amide derivate und deren pharmazeutische verwendungen |
| US20050245534A1 (en) * | 2004-04-29 | 2005-11-03 | Link James T | Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme |
| TW200827346A (en) * | 2006-11-03 | 2008-07-01 | Astrazeneca Ab | Chemical compounds |
| KR20110002475A (ko) * | 2008-04-22 | 2011-01-07 | 아스트라제네카 아베 | 치환 피리미딘-5-카르복시아미드 281 |
-
2010
- 2010-10-19 AR ARP100103811A patent/AR078673A1/es unknown
- 2010-10-19 WO PCT/SE2010/051127 patent/WO2011049520A1/en not_active Ceased
- 2010-10-19 US US12/907,056 patent/US20110092526A1/en not_active Abandoned
- 2010-10-19 TW TW099135633A patent/TW201118085A/zh unknown
- 2010-10-19 UY UY0001032954A patent/UY32954A/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| TW201118085A (en) | 2011-06-01 |
| US20110092526A1 (en) | 2011-04-21 |
| WO2011049520A1 (en) | 2011-04-28 |
| UY32954A (es) | 2011-05-31 |
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