CO6751283A2 - Derivados de 3,4-dihidropirrolo[1,2-a]pirazin-1-ilamina útiles cini inhibidores de beta-secretasa (bace) - Google Patents
Derivados de 3,4-dihidropirrolo[1,2-a]pirazin-1-ilamina útiles cini inhibidores de beta-secretasa (bace)Info
- Publication number
- CO6751283A2 CO6751283A2 CO13205187A CO13205187A CO6751283A2 CO 6751283 A2 CO6751283 A2 CO 6751283A2 CO 13205187 A CO13205187 A CO 13205187A CO 13205187 A CO13205187 A CO 13205187A CO 6751283 A2 CO6751283 A2 CO 6751283A2
- Authority
- CO
- Colombia
- Prior art keywords
- beta
- dementia
- dihydropyrrolo
- bace
- pyrazin
- Prior art date
Links
Classifications
-
- 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
- A61P25/28—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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invención se refiere a derivados de 3,4-dihidropirrolo[1,2-a]pirazin-1-ilamina 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, a procesos para preparar tales compuestos y composiciones, y al uso de tales compuestos y composiciones para prevenir y tratar trastornos en los que participa la beta-secreta, 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.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP11157418 | 2011-03-09 |
Publications (1)
Publication Number | Publication Date |
---|---|
CO6751283A2 true CO6751283A2 (es) | 2013-09-16 |
Family
ID=43833325
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CO13205187A CO6751283A2 (es) | 2011-03-09 | 2013-08-29 | Derivados de 3,4-dihidropirrolo[1,2-a]pirazin-1-ilamina útiles cini inhibidores de beta-secretasa (bace) |
Country Status (20)
Country | Link |
---|---|
US (1) | US9845326B2 (es) |
EP (1) | EP2683721B1 (es) |
JP (1) | JP5853035B2 (es) |
KR (1) | KR102012675B1 (es) |
CN (1) | CN103415521B (es) |
AU (1) | AU2012224632B2 (es) |
BR (1) | BR112013022917A2 (es) |
CA (1) | CA2825620C (es) |
CL (1) | CL2013002511A1 (es) |
CO (1) | CO6751283A2 (es) |
EA (1) | EA023824B1 (es) |
ES (1) | ES2534973T3 (es) |
HK (1) | HK1189223A1 (es) |
IL (1) | IL228239A (es) |
MX (1) | MX340031B (es) |
MY (1) | MY163346A (es) |
SG (1) | SG193342A1 (es) |
UA (1) | UA109687C2 (es) |
WO (1) | WO2012120023A1 (es) |
ZA (1) | ZA201306719B (es) |
Families Citing this family (21)
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WO2007049532A1 (ja) | 2005-10-25 | 2007-05-03 | Shionogi & Co., Ltd. | アミノジヒドロチアジン誘導体 |
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 |
EP2689780A1 (en) | 2007-04-24 | 2014-01-29 | Shionogi & Co., Ltd. | Intermediates for aminodihydrothiazine derivatives substituted with a cyclic group |
CA2727859C (en) | 2008-06-13 | 2016-11-01 | Shionogi & Co., Ltd. | SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY |
US8703785B2 (en) | 2008-10-22 | 2014-04-22 | Shionogi & Co., Ltd. | 2-aminopyrimidin-4-one and 2-aminopyridine derivatives both having BACE1-inhibiting activity |
MX2012006491A (es) | 2009-12-11 | 2012-07-03 | Shionogi & Co | Derivados de oxazina. |
EA021240B1 (ru) | 2010-06-09 | 2015-05-29 | Янссен Фармацевтика Нв | Производные 5,6-дигидро-2h-[1,4]оксазин-3-иламина в качестве ингибиторов бета-секретазы (bace) |
US8927721B2 (en) | 2010-10-29 | 2015-01-06 | Shionogi & Co., Ltd. | Naphthyridine derivative |
EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE |
CA2819175C (en) | 2010-12-22 | 2019-01-08 | Janssen Pharmaceutica Nv | 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (bace) |
UA109800C2 (xx) | 2011-03-01 | 2015-10-12 | ПОХІДНІ 6,7-ДИГІДРОПІРАЗОЛО$1,5-a]ПІРАЗИН-4-ІЛАМІНУ, КОРИСНІ ЯК ІНГІБІТОРИ БЕТА-СЕКРЕТАЗИ (BACE) | |
MX340031B (es) * | 2011-03-09 | 2016-06-21 | Janssen Pharmaceutica Nv | Derivados de 3,4-dihidropirrolo[1,2-a]pirazin-1-ilamina utiles como inhibidores de beta-secretasa (bace). |
US8883779B2 (en) | 2011-04-26 | 2014-11-11 | Shinogi & Co., Ltd. | Oxazine derivatives and a pharmaceutical composition for inhibiting BACE1 containing them |
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 |
CA2911690C (en) * | 2013-06-12 | 2021-08-24 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace) |
AU2014280122B2 (en) * | 2013-06-12 | 2017-12-21 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2H)-one derivatives as inhibitors of beta-secretase (BACE) |
CN105324383B (zh) * | 2013-06-12 | 2017-10-31 | 詹森药业有限公司 | 作为β‑分泌酶(BACE)抑制剂的4‑氨基‑6‑苯基‑6,7‑二氢[1,2,3]三唑并[1,5‑A]吡嗪衍生物 |
RU2572076C2 (ru) * | 2014-03-26 | 2015-12-27 | Федеральное государственное бюджетное научное учреждение "Научно-исследовательский институт фармакологии имени В.В. Закусова" | 1-арилпирроло[1,2-a]пиразин-3-карбоксамиды с нейропсихотропной активностью |
CN107108582B (zh) | 2014-12-18 | 2019-10-18 | 詹森药业有限公司 | β-分泌酶的2,3,4,5-四氢吡啶-6-胺化合物抑制剂 |
WO2018165520A1 (en) | 2017-03-10 | 2018-09-13 | Vps-3, Inc. | Metalloenzyme inhibitor compounds |
CN117471007A (zh) * | 2023-10-31 | 2024-01-30 | 广东省中医院(广州中医药大学第二附属医院、广州中医药大学第二临床医学院、广东省中医药科学院) | 一种血浆β-淀粉样蛋白检测方法 |
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ES2445536T3 (es) | 2009-12-31 | 2014-03-03 | Novartis Ag | Derivados de la pirazina y su uso en el tratamiento de trastornos neurológicos |
EA021240B1 (ru) | 2010-06-09 | 2015-05-29 | Янссен Фармацевтика Нв | Производные 5,6-дигидро-2h-[1,4]оксазин-3-иламина в качестве ингибиторов бета-секретазы (bace) |
SG185652A1 (en) | 2010-06-09 | 2012-12-28 | Janssen Pharmaceutica Nv | 5-amino-3,6-dihydro-1h-pyrazin-2-one derivatives useful as inhibitors of beta-secretase (bace) |
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AU2011306941B2 (en) | 2010-09-22 | 2014-06-12 | Janssen Pharmaceutica Nv | 4,7-dihydro-pyrazolo[1,5-a] pyrazin-6-ylamine derivatives useful as inhibitors of beta-secretase (BACE) |
EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE |
CA2819175C (en) | 2010-12-22 | 2019-01-08 | 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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MX340031B (es) * | 2011-03-09 | 2016-06-21 | Janssen Pharmaceutica Nv | Derivados de 3,4-dihidropirrolo[1,2-a]pirazin-1-ilamina utiles como inhibidores de beta-secretasa (bace). |
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AU2014280122B2 (en) | 2013-06-12 | 2017-12-21 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2H)-one derivatives as inhibitors of beta-secretase (BACE) |
CN105324383B (zh) | 2013-06-12 | 2017-10-31 | 詹森药业有限公司 | 作为β‑分泌酶(BACE)抑制剂的4‑氨基‑6‑苯基‑6,7‑二氢[1,2,3]三唑并[1,5‑A]吡嗪衍生物 |
CA2911690C (en) | 2013-06-12 | 2021-08-24 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace) |
CN107108582B (zh) | 2014-12-18 | 2019-10-18 | 詹森药业有限公司 | β-分泌酶的2,3,4,5-四氢吡啶-6-胺化合物抑制剂 |
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2012
- 2012-03-07 MX MX2013010280A patent/MX340031B/es active IP Right Grant
- 2012-03-07 JP JP2013557074A patent/JP5853035B2/ja not_active Expired - Fee Related
- 2012-03-07 EA EA201391296A patent/EA023824B1/ru not_active IP Right Cessation
- 2012-03-07 CA CA2825620A patent/CA2825620C/en active Active
- 2012-03-07 AU AU2012224632A patent/AU2012224632B2/en not_active Ceased
- 2012-03-07 BR BR112013022917A patent/BR112013022917A2/pt not_active Application Discontinuation
- 2012-03-07 CN CN201280012485.5A patent/CN103415521B/zh not_active Expired - Fee Related
- 2012-03-07 US US14/003,901 patent/US9845326B2/en active Active
- 2012-03-07 KR KR1020137022396A patent/KR102012675B1/ko active IP Right Grant
- 2012-03-07 SG SG2013067210A patent/SG193342A1/en unknown
- 2012-03-07 EP EP12707319.5A patent/EP2683721B1/en not_active Not-in-force
- 2012-03-07 MY MYPI2013003278A patent/MY163346A/en unknown
- 2012-03-07 ES ES12707319.5T patent/ES2534973T3/es active Active
- 2012-03-07 WO PCT/EP2012/053863 patent/WO2012120023A1/en active Application Filing
- 2012-07-03 UA UAA201308782A patent/UA109687C2/ru unknown
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2013
- 2013-08-29 CO CO13205187A patent/CO6751283A2/es active IP Right Grant
- 2013-08-30 CL CL2013002511A patent/CL2013002511A1/es unknown
- 2013-09-02 IL IL228239A patent/IL228239A/en active IP Right Grant
- 2013-09-06 ZA ZA2013/06719A patent/ZA201306719B/en unknown
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2014
- 2014-03-04 HK HK14102159.7A patent/HK1189223A1/zh not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
EP2683721A1 (en) | 2014-01-15 |
SG193342A1 (en) | 2013-10-30 |
US9845326B2 (en) | 2017-12-19 |
CN103415521A (zh) | 2013-11-27 |
MX340031B (es) | 2016-06-21 |
KR20140019332A (ko) | 2014-02-14 |
IL228239A (en) | 2016-06-30 |
CA2825620C (en) | 2019-04-23 |
CN103415521B (zh) | 2016-01-06 |
JP5853035B2 (ja) | 2016-02-09 |
MY163346A (en) | 2017-09-15 |
ES2534973T3 (es) | 2015-04-30 |
KR102012675B1 (ko) | 2019-08-21 |
MX2013010280A (es) | 2013-10-01 |
US20130345228A1 (en) | 2013-12-26 |
HK1189223A1 (zh) | 2014-05-30 |
ZA201306719B (en) | 2015-04-29 |
JP2014507455A (ja) | 2014-03-27 |
AU2012224632A1 (en) | 2013-08-01 |
BR112013022917A2 (pt) | 2016-12-06 |
EA023824B1 (ru) | 2016-07-29 |
AU2012224632B2 (en) | 2016-06-16 |
CL2013002511A1 (es) | 2014-01-24 |
NZ615720A (en) | 2014-08-29 |
EP2683721B1 (en) | 2015-01-28 |
WO2012120023A1 (en) | 2012-09-13 |
IL228239A0 (en) | 2013-11-25 |
UA109687C2 (xx) | 2015-09-25 |
CA2825620A1 (en) | 2012-09-13 |
EA201391296A1 (ru) | 2014-01-30 |
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