AR079334A1 - Derivados de oxazin amino - Google Patents
Derivados de oxazin aminoInfo
- Publication number
- AR079334A1 AR079334A1 ARP100104543A ARP100104543A AR079334A1 AR 079334 A1 AR079334 A1 AR 079334A1 AR P100104543 A ARP100104543 A AR P100104543A AR P100104543 A ARP100104543 A AR P100104543A AR 079334 A1 AR079334 A1 AR 079334A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halogen
- alkoxy
- cyano
- group
- Prior art date
Links
- -1 OF OXAZIN AMINO Chemical class 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 19
- 125000003545 alkoxy group Chemical group 0.000 abstract 11
- 229910052736 halogen Inorganic materials 0.000 abstract 7
- 150000002367 halogens Chemical class 0.000 abstract 7
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 5
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004043 oxo group Chemical group O=* 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 102100021277 Beta-secretase 2 Human genes 0.000 abstract 1
- 101000894883 Homo sapiens Beta-secretase 2 Proteins 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/535—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
- A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
-
- 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
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
- C07D265/06—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings
- C07D265/08—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Diabetes (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Estos compuestos son inhibidores de la BACE2 y pueden emplearse como medicamentos para el tratamiento o prevencion de enfermedades, por ejemplo de la diabetes. Procesos de obtencion y composiciones farmacéuticas. Reivindicacion 1: Compuestos de la formula (1) en la que R1 es hidrogeno o alquilo C1-7; R2 es hidrogeno o alquilo C1-7; o R1 y R2 junto con el átomo de C al que están unidos forman un anillo cicloalquilo C3-7; R3 es alquilo C1-7 o cicloalquilo C3-7; o R2 y R3 junto con los átomos de C a los que están unidos forman un anillo cicloalquilo C3-7 o un anillo O-heterociclilo de 3 a 7 eslabones; R4 se elige entre el grupo formado por hidrogeno, alquilo C1-7, halogeno, ciano y alcoxi C1-7; R5 es arilo, sin sustituir o sustituido por uno, dos o tres restos elegidos entre el grupo formado por alquilo C1-7, halogeno, halogeno-alquilo C1-7, alcoxi C1-7, halogeno-alcoxi C1-7, ciano, hidroxi-alquilo C1-7, oxo y fenilo, un heteroarilo, sin sustituir o sustituido por uno, dos o tres restos elegidos entre el grupo formado por alquilo C1-7, halogeno, halogeno-alquilo C1-7, alcoxi C1-7, halogeno-alcoxi C1-7, ciano, hidroxi-alquilo C1-7, oxo y fenilo, alquilo C1-7, sin sustituir o sustituido por uno, dos, tres, cuatro o cinco restos elegidos individualmente entre el grupo formado por halogeno, halogeno-alquilo C1-7, alcoxi C1-7, halogeno-alcoxi C1-7, ciano e hidroxi-alquilo C1-7, anillo cicloalquilo C3-7, sin sustituir o sustituido por uno, dos o tres restos elegidos entre el grupo formado por alquilo C1-7, halogeno, halogeno-alquilo C1-7, alcoxi C1-7, halogeno-alcoxi C1-7, ciano e hidroxi-alquilo C1-7, un anillo O-heterociclilo de 3 a 7 eslabones, sin sustituir o sustituido por uno, dos o tres restos elegidos entre el grupo formado por alquilo C1-7, halogeno, halogeno-alquilo C1-7, alcoxi C1-7, halogeno-alcoxi C1-7, ciano e hidroxi-alquilo C1-7, o las sales farmacéuticamente aceptables de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09178642 | 2009-12-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR079334A1 true AR079334A1 (es) | 2012-01-18 |
Family
ID=43478012
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100104543A AR079334A1 (es) | 2009-12-10 | 2010-12-09 | Derivados de oxazin amino |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US7964594B1 (es) |
| EP (1) | EP2509966B1 (es) |
| JP (2) | JP2013513568A (es) |
| KR (1) | KR101437750B1 (es) |
| CN (1) | CN102652129A (es) |
| AR (1) | AR079334A1 (es) |
| BR (1) | BR112012013322A2 (es) |
| CA (1) | CA2780693A1 (es) |
| MX (1) | MX2012005810A (es) |
| RU (1) | RU2012126083A (es) |
| TW (1) | TW201125863A (es) |
| WO (1) | WO2011070029A1 (es) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2537898T3 (es) | 2005-10-25 | 2015-06-15 | Shionogi & Co., Ltd. | Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1 |
| KR20100017255A (ko) | 2007-04-24 | 2010-02-16 | 시오노기 앤드 컴파니, 리미티드 | 환식기로 치환된 아미노다이하이드로싸이아진 유도체 |
| EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
| EP2305672B1 (en) | 2008-06-13 | 2019-03-27 | Shionogi & Co., Ltd. | SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY |
| CN102186841A (zh) | 2008-10-22 | 2011-09-14 | 盐野义制药株式会社 | 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物 |
| UY32799A (es) | 2009-07-24 | 2011-02-28 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| WO2011044187A1 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| EP2485920B1 (en) | 2009-10-08 | 2016-04-27 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| WO2011071109A1 (ja) * | 2009-12-11 | 2011-06-16 | 塩野義製薬株式会社 | アミノ基を有する縮合ヘテロ環化合物 |
| RU2012129168A (ru) * | 2009-12-11 | 2014-01-20 | Сионоги Энд Ко. Лтд. | Производные оксазина |
| JP5766198B2 (ja) | 2010-10-29 | 2015-08-19 | 塩野義製薬株式会社 | 縮合アミノジヒドロピリミジン誘導体 |
| CN103261199A (zh) | 2010-10-29 | 2013-08-21 | 盐野义制药株式会社 | 萘啶衍生物 |
| US8524897B2 (en) | 2011-01-12 | 2013-09-03 | Novartis Ag | Crystalline oxazine derivative |
| ES2576182T3 (es) | 2011-01-13 | 2016-07-06 | Novartis Ag | Derivados de heterocíclicos novedosos y su uso en el tratamiento de trastornos neurológicos |
| WO2012138590A1 (en) | 2011-04-07 | 2012-10-11 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| WO2012138734A1 (en) | 2011-04-07 | 2012-10-11 | Merck Sharp & Dohme Corp. | C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| US8754075B2 (en) * | 2011-04-11 | 2014-06-17 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE1 and/or BACE2 inhibitors |
| AU2012243329B2 (en) | 2011-04-13 | 2015-09-17 | Merck Sharp & Dohme Corp. | 5-substituted iminothiazines and their mono-and dioxides as BACE inhibitors,compositions,and their use |
| WO2012147763A1 (ja) | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | オキサジン誘導体およびそれを含有するbace1阻害剤 |
| US8785436B2 (en) | 2011-05-16 | 2014-07-22 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE 1 and/or BACE2 inhibitors |
| US9079919B2 (en) * | 2011-05-27 | 2015-07-14 | Hoffmann-La Roche Inc. | Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as BACE1 and/or BACE2 inhibitors |
| US9073909B2 (en) * | 2011-06-07 | 2015-07-07 | Hoffmann-La Roche Inc. | [1,3]oxazines |
| PE20140623A1 (es) * | 2011-06-07 | 2014-05-30 | Hoffmann La Roche | Halogenoalquil-1,3-oxazinas como inhibidores de la bace1 y/o bace2 |
| EP2747769B1 (en) | 2011-08-22 | 2017-08-02 | Merck Sharp & Dohme Corp. | 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use |
| UY34278A (es) | 2011-08-25 | 2013-04-05 | Novartis Ag | Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades |
| US8476264B2 (en) * | 2011-09-21 | 2013-07-02 | Hoffmann-La Roche Inc. | N-(3-(2-amino-6,6-difluoro-4,4A,5,6,7,7A-hexahydro-cyclopenta[E][1,3]oxazin-4-yl)-phenylamides as BACE1 inhibitors |
| US8338413B1 (en) | 2012-03-07 | 2012-12-25 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| BR112014023384A8 (pt) * | 2012-03-20 | 2018-01-16 | R Artis Dean | inibidores de bace espirocíclicos de di-hidro-tiazina e di-hidro-oxazina, e composições e usos dos mesmos. |
| JO3143B1 (ar) * | 2012-04-03 | 2017-09-20 | Lilly Co Eli | مركبات تتراهيدرو بيرولو ثيازين |
| WO2014059185A1 (en) | 2012-10-12 | 2014-04-17 | Amgen Inc. | Amino - dihydrothiazine and amino - dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| WO2014078314A1 (en) | 2012-11-15 | 2014-05-22 | Amgen Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| US9489013B2 (en) | 2012-12-20 | 2016-11-08 | Merck Sharp & Dohme Corp. | C6-azaspiro iminothiadiazine dioxides as bace inhibitors, compositions, and their use |
| AU2014223334C1 (en) | 2013-03-01 | 2018-10-18 | Amgen Inc. | Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| AP2015008716A0 (en) | 2013-03-08 | 2015-09-30 | Amgen Inc | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| US9045477B2 (en) * | 2013-03-15 | 2015-06-02 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| EP2989081A1 (en) * | 2013-04-26 | 2016-03-02 | F. Hoffmann-La Roche AG | Synthesis of bace inhibitors |
| TW201623295A (zh) | 2014-04-11 | 2016-07-01 | 塩野義製藥股份有限公司 | 具有bace1抑制活性之二氫噻及二氫衍生物 |
| US9550762B2 (en) | 2014-08-08 | 2017-01-24 | Amgen, Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| EP3271355B1 (en) | 2015-03-20 | 2020-07-29 | H. Hoffnabb-La Roche Ag | Bace1 inhibitors |
| US11629154B2 (en) | 2018-04-27 | 2023-04-18 | Shionogi & Co., Ltd. | Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1156798E (pt) * | 1999-02-09 | 2003-11-28 | Univ Virginia | Compostos derivados de felbamato |
| EP1562897B1 (en) * | 2002-11-12 | 2009-09-16 | Merck & Co., Inc. | Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer s disease |
| EP1756087B1 (en) | 2004-06-16 | 2009-10-07 | Wyeth | Amino-5,5-diphenylimidazolone derivatives for the inhibition of beta-secretase |
| EP1802587A4 (en) * | 2004-10-15 | 2010-02-17 | Astrazeneca Ab | SUBSTITUTED AMINO BINDINGS AND THEIR APPLICATIONS |
| TW200730523A (en) | 2005-07-29 | 2007-08-16 | Wyeth Corp | Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation |
| ES2537898T3 (es) * | 2005-10-25 | 2015-06-15 | Shionogi & Co., Ltd. | Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1 |
| KR20100017255A (ko) * | 2007-04-24 | 2010-02-16 | 시오노기 앤드 컴파니, 리미티드 | 환식기로 치환된 아미노다이하이드로싸이아진 유도체 |
| SI2233474T1 (sl) | 2008-01-18 | 2015-11-30 | Eisai R&D Management Co., Ltd. | Kondenziran derivat aminodihidrotiazina |
| GB0912778D0 (en) * | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
| WO2011071109A1 (ja) * | 2009-12-11 | 2011-06-16 | 塩野義製薬株式会社 | アミノ基を有する縮合ヘテロ環化合物 |
-
2010
- 2010-12-02 US US12/958,436 patent/US7964594B1/en not_active Expired - Fee Related
- 2010-12-07 CA CA2780693A patent/CA2780693A1/en not_active Abandoned
- 2010-12-07 EP EP10790920.2A patent/EP2509966B1/en not_active Not-in-force
- 2010-12-07 KR KR1020127017733A patent/KR101437750B1/ko not_active Expired - Fee Related
- 2010-12-07 RU RU2012126083/04A patent/RU2012126083A/ru not_active Application Discontinuation
- 2010-12-07 MX MX2012005810A patent/MX2012005810A/es active IP Right Grant
- 2010-12-07 BR BR112012013322A patent/BR112012013322A2/pt not_active IP Right Cessation
- 2010-12-07 CN CN2010800555310A patent/CN102652129A/zh active Pending
- 2010-12-07 WO PCT/EP2010/069098 patent/WO2011070029A1/en not_active Ceased
- 2010-12-07 JP JP2012542524A patent/JP2013513568A/ja active Pending
- 2010-12-09 AR ARP100104543A patent/AR079334A1/es unknown
- 2010-12-09 TW TW099143073A patent/TW201125863A/zh unknown
-
2014
- 2014-11-07 JP JP2014227180A patent/JP2015051992A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| KR20120103694A (ko) | 2012-09-19 |
| JP2013513568A (ja) | 2013-04-22 |
| MX2012005810A (es) | 2012-06-12 |
| CN102652129A (zh) | 2012-08-29 |
| JP2015051992A (ja) | 2015-03-19 |
| RU2012126083A (ru) | 2014-01-20 |
| EP2509966A1 (en) | 2012-10-17 |
| US7964594B1 (en) | 2011-06-21 |
| WO2011070029A1 (en) | 2011-06-16 |
| CA2780693A1 (en) | 2011-06-16 |
| US20110144098A1 (en) | 2011-06-16 |
| TW201125863A (en) | 2011-08-01 |
| BR112012013322A2 (pt) | 2019-09-24 |
| EP2509966B1 (en) | 2014-10-22 |
| KR101437750B1 (ko) | 2014-09-03 |
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