CL2013002486A1 - Compuestos derivados de 6,7-dihidropirazolo [1,5-a]pirazin-4-il-amina, inhibidores de beta - secretasa (bace); composicion farmaceutica; y uso en el tratamiento de la enfermedad de alzheimer, senilidad, demencia, sindrome de down, entre otras. - Google Patents
Compuestos derivados de 6,7-dihidropirazolo [1,5-a]pirazin-4-il-amina, inhibidores de beta - secretasa (bace); composicion farmaceutica; y uso en el tratamiento de la enfermedad de alzheimer, senilidad, demencia, sindrome de down, entre otras.Info
- Publication number
- CL2013002486A1 CL2013002486A1 CL2013002486A CL2013002486A CL2013002486A1 CL 2013002486 A1 CL2013002486 A1 CL 2013002486A1 CL 2013002486 A CL2013002486 A CL 2013002486A CL 2013002486 A CL2013002486 A CL 2013002486A CL 2013002486 A1 CL2013002486 A1 CL 2013002486A1
- Authority
- CL
- Chile
- Prior art keywords
- dementia
- beta
- bace
- disease
- down syndrome
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Biomedical Technology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Abstract
LA PRESENTE INVENCIÓN SE REFIERE A DERIVADOS DE 6,7-DIHIDROPIRAZOLO[1,5-A]PIRAZIN-4-IL-AMINA COMO INHIBIDORES DE BETA-SECRETASA, CONOCIDA TAMBIÉN COMO LA ENZIMA QUE ESCINDE LA PROTEÍNA PRECURSORA DE AMILOIDE POR EL SITIO BETA, BACE, BACE1, ASP2 O MEMAPSINA 2. LA INVENCIÓN TAMBIÉN SE REFIERE A COMPOSICIONES FARMACÉUTICAS QUE COMPRENDEN TALES COMPUESTOS, Y AL USO DE TALES COMPUESTOS PARA PREVENIR Y TRATAR TRASTORNOS EN LOS QUE PARTICIPA LA BETA-SECRETASA, TALES COMO LA ENFERMEDAD DE ALZHEIMER (EA), EL DETERIORO COGNITIVO LEVE, SENILIDAD, DEMENCIA, DEMENCIA CON CUERPOS DE LEWY, SÍNDROME DE DOWN, DEMENCIA ASOCIADA CON EL ACCIDENTE CEREBROVASCULAR, DEMENCIA ASOCIADA CON LA ENFERMEDAD DE PARKINSON O DEMENCIA ASOCIADA CON BETA-AMILOIDES. LA FÓRMULA GENERAL 1 DE LOS COMPUESTOS DE LA INVENCIÓN CORRESPONDEN A: DONDE R1 , R 2 , R 3 , X 1 , X2 , X3 , X4 , L Y AR SON COMO SE DEFINEN EN LA MEMORIA DESCRIPTIVA.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP11156463 | 2011-03-01 |
Publications (1)
Publication Number | Publication Date |
---|---|
CL2013002486A1 true CL2013002486A1 (es) | 2014-02-21 |
Family
ID=45808845
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CL2013002486A CL2013002486A1 (es) | 2011-03-01 | 2013-08-28 | Compuestos derivados de 6,7-dihidropirazolo [1,5-a]pirazin-4-il-amina, inhibidores de beta - secretasa (bace); composicion farmaceutica; y uso en el tratamiento de la enfermedad de alzheimer, senilidad, demencia, sindrome de down, entre otras. |
Country Status (27)
Country | Link |
---|---|
US (1) | US9346811B2 (es) |
EP (1) | EP2681219B1 (es) |
JP (1) | JP5853033B2 (es) |
KR (1) | KR102012671B1 (es) |
CN (1) | CN103415519B (es) |
AU (1) | AU2012222394B2 (es) |
BR (1) | BR112013022039A2 (es) |
CA (1) | CA2824360C (es) |
CL (1) | CL2013002486A1 (es) |
CO (1) | CO6751282A2 (es) |
CY (1) | CY1117663T1 (es) |
DK (1) | DK2681219T3 (es) |
EA (1) | EA022649B1 (es) |
ES (1) | ES2558779T3 (es) |
HK (1) | HK1188784A1 (es) |
HR (1) | HRP20160030T1 (es) |
HU (1) | HUE026338T2 (es) |
IL (1) | IL228158A (es) |
MX (1) | MX338333B (es) |
MY (1) | MY161407A (es) |
PL (1) | PL2681219T3 (es) |
PT (1) | PT2681219E (es) |
SG (1) | SG192963A1 (es) |
SI (1) | SI2681219T1 (es) |
UA (1) | UA109800C2 (es) |
WO (1) | WO2012117027A1 (es) |
ZA (1) | ZA201306545B (es) |
Families Citing this family (22)
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EP2612854B1 (en) | 2005-10-25 | 2015-04-29 | Shionogi&Co., Ltd. | Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors |
TW200902526A (en) | 2007-04-24 | 2009-01-16 | Shionogi & Amp Co Ltd | Aminodihydrothiazin derivative substituted with a cyclic group |
JP5383483B2 (ja) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | アルツハイマー症治療用医薬組成物 |
NZ589590A (en) | 2008-06-13 | 2012-05-25 | Shionogi & Co | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity |
JPWO2010047372A1 (ja) | 2008-10-22 | 2012-03-22 | 塩野義製薬株式会社 | Bace1阻害活性を有する2−アミノピリミジン−4−オンおよび2−アミノピリジン誘導体 |
US8999980B2 (en) | 2009-12-11 | 2015-04-07 | Shionogi & Co., Ltd. | Oxazine derivatives |
TWI537263B (zh) | 2010-06-09 | 2016-06-11 | 健生藥品公司 | 使用作為β-分泌酶抑制劑之5,6-二氫-2H-[1,4]-3-基-胺衍生物 |
US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
EP2634186A4 (en) | 2010-10-29 | 2014-03-26 | Shionogi & Co | naphthyridine |
AU2011347377B2 (en) | 2010-12-22 | 2016-03-03 | Janssen Pharmaceutica Nv | 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (BACE) |
HUE026338T2 (en) | 2011-03-01 | 2016-05-30 | Janssen Pharmaceutica Nv | Beta-secretase (BACE) inhibitors 6,7-dihydro-pyrazolo [1,5-a] pyrazin-4-ylamine derivatives |
HRP20211967T1 (hr) | 2011-03-01 | 2022-03-18 | NuCana plc | Farmaceutska formulacija koja sadrži fosforamidatni derivat 5-fluoro-2'-deoksiuridina za uporabu u liječenju raka |
SG193342A1 (en) | 2011-03-09 | 2013-10-30 | Janssen Pharmaceutica Nv | 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
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 |
JP2016501827A (ja) | 2012-10-24 | 2016-01-21 | 塩野義製薬株式会社 | Bace1阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体 |
EP3008066B1 (en) * | 2013-06-12 | 2018-08-15 | Janssen Pharmaceutica N.V. | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace) |
CA2911693C (en) * | 2013-06-12 | 2021-08-24 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace) |
EA032662B1 (ru) * | 2013-06-12 | 2019-06-28 | Янссен Фармацевтика Нв | ПРОИЗВОДНЫЕ 4-АМИНО-6-ФЕНИЛ-5,6-ДИГИДРОИМИДАЗО[1,5-а]ПИРАЗИН-3(2H)-ОНА В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (BACE) |
ES2768823T3 (es) | 2014-12-18 | 2020-06-23 | Janssen Pharmaceutica Nv | Derivados de 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2H-pirrol-5-amina útiles como inhibidores de beta-secretasa |
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WO2023243616A1 (ja) * | 2022-06-13 | 2023-12-21 | 塩野義製薬株式会社 | ジヒドロピリジノン誘導体またはその溶媒和物の結晶 |
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AU2011347377B2 (en) | 2010-12-22 | 2016-03-03 | Janssen Pharmaceutica Nv | 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (BACE) |
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HUE026338T2 (en) | 2011-03-01 | 2016-05-30 | Janssen Pharmaceutica Nv | Beta-secretase (BACE) inhibitors 6,7-dihydro-pyrazolo [1,5-a] pyrazin-4-ylamine derivatives |
SG193342A1 (en) | 2011-03-09 | 2013-10-30 | Janssen Pharmaceutica Nv | 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
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-
2012
- 2012-02-29 HU HUE12707276A patent/HUE026338T2/en unknown
- 2012-02-29 DK DK12707276.7T patent/DK2681219T3/en active
- 2012-02-29 JP JP2013555862A patent/JP5853033B2/ja not_active Expired - Fee Related
- 2012-02-29 MX MX2013010040A patent/MX338333B/es active IP Right Grant
- 2012-02-29 CA CA2824360A patent/CA2824360C/en active Active
- 2012-02-29 AU AU2012222394A patent/AU2012222394B2/en not_active Ceased
- 2012-02-29 CN CN201280011146.5A patent/CN103415519B/zh not_active Expired - Fee Related
- 2012-02-29 KR KR1020137022392A patent/KR102012671B1/ko active IP Right Grant
- 2012-02-29 EA EA201391251A patent/EA022649B1/ru not_active IP Right Cessation
- 2012-02-29 BR BR112013022039A patent/BR112013022039A2/pt not_active Application Discontinuation
- 2012-02-29 ES ES12707276.7T patent/ES2558779T3/es active Active
- 2012-02-29 SG SG2013064746A patent/SG192963A1/en unknown
- 2012-02-29 WO PCT/EP2012/053455 patent/WO2012117027A1/en active Application Filing
- 2012-02-29 US US14/002,169 patent/US9346811B2/en active Active
- 2012-02-29 UA UAA201308783A patent/UA109800C2/ru unknown
- 2012-02-29 MY MYPI2013003200A patent/MY161407A/en unknown
- 2012-02-29 EP EP12707276.7A patent/EP2681219B1/en active Active
- 2012-02-29 PL PL12707276T patent/PL2681219T3/pl unknown
- 2012-02-29 PT PT127072767T patent/PT2681219E/pt unknown
- 2012-02-29 SI SI201230429T patent/SI2681219T1/sl unknown
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2013
- 2013-08-28 IL IL228158A patent/IL228158A/en active IP Right Grant
- 2013-08-28 CL CL2013002486A patent/CL2013002486A1/es unknown
- 2013-08-29 CO CO13205178A patent/CO6751282A2/es unknown
- 2013-08-30 ZA ZA2013/06545A patent/ZA201306545B/en unknown
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2014
- 2014-02-27 HK HK14101914.5A patent/HK1188784A1/zh not_active IP Right Cessation
-
2016
- 2016-01-12 HR HRP20160030TT patent/HRP20160030T1/hr unknown
- 2016-01-28 CY CY20161100087T patent/CY1117663T1/el unknown
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