CL2013002511A1 - Compuestos derivados de 3,4-dihidropirrolo[1,2-a]pirazin-1-ilamina, inhibidores de (bace); composicion farmaceutica que los comprende; proceso de preparacion; util para el tratamiento o prevencion de la enfermedad de alzheimer, demencia, sindrome de down y otras demencias asociadas con beta-amiloides. - Google Patents
Compuestos derivados de 3,4-dihidropirrolo[1,2-a]pirazin-1-ilamina, inhibidores de (bace); composicion farmaceutica que los comprende; proceso de preparacion; util para el tratamiento o prevencion de la enfermedad de alzheimer, demencia, sindrome de down y otras demencias asociadas con beta-amiloides.Info
- Publication number
- CL2013002511A1 CL2013002511A1 CL2013002511A CL2013002511A CL2013002511A1 CL 2013002511 A1 CL2013002511 A1 CL 2013002511A1 CL 2013002511 A CL2013002511 A CL 2013002511A CL 2013002511 A CL2013002511 A CL 2013002511A CL 2013002511 A1 CL2013002511 A1 CL 2013002511A1
- Authority
- CL
- Chile
- Prior art keywords
- beta
- dementia
- alzheimer
- disease
- down syndrome
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 206010012289 Dementia Diseases 0.000 title abstract 3
- 201000010374 Down Syndrome Diseases 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- MBVCQKKUMUXAMH-UHFFFAOYSA-N 3,4-dihydropyrrolo[1,2-a]pyrazin-1-amine Chemical compound NC1=NCCN2C=CC=C12 MBVCQKKUMUXAMH-UHFFFAOYSA-N 0.000 title 1
- 208000024827 Alzheimer disease Diseases 0.000 title 1
- 101150058765 BACE1 gene Proteins 0.000 title 1
- 206010002022 amyloidosis Diseases 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 238000002360 preparation method Methods 0.000 title 1
- 230000002265 prevention Effects 0.000 title 1
- 102100021257 Beta-secretase 1 Human genes 0.000 abstract 3
- 101710150192 Beta-secretase 1 Proteins 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 206010008190 Cerebrovascular accident Diseases 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 abstract 1
- 208000006011 Stroke Diseases 0.000 abstract 1
- 239000002439 beta secretase inhibitor Substances 0.000 abstract 1
- 208000026106 cerebrovascular disease Diseases 0.000 abstract 1
- 231100000876 cognitive deterioration Toxicity 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- IXHBTMCLRNMKHZ-LBPRGKRZSA-N levobunolol Chemical compound O=C1CCCC2=C1C=CC=C2OC[C@@H](O)CNC(C)(C)C IXHBTMCLRNMKHZ-LBPRGKRZSA-N 0.000 abstract 1
- 210000004558 lewy body Anatomy 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
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)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11157418 | 2011-03-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CL2013002511A1 true CL2013002511A1 (es) | 2014-01-24 |
Family
ID=43833325
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CL2013002511A CL2013002511A1 (es) | 2011-03-09 | 2013-08-30 | Compuestos derivados de 3,4-dihidropirrolo[1,2-a]pirazin-1-ilamina, inhibidores de (bace); composicion farmaceutica que los comprende; proceso de preparacion; util para el tratamiento o prevencion de la enfermedad de alzheimer, demencia, sindrome de down y otras demencias asociadas con beta-amiloides. |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US9845326B2 (enExample) |
| EP (1) | EP2683721B1 (enExample) |
| JP (1) | JP5853035B2 (enExample) |
| KR (1) | KR102012675B1 (enExample) |
| CN (1) | CN103415521B (enExample) |
| AU (1) | AU2012224632B2 (enExample) |
| BR (1) | BR112013022917A2 (enExample) |
| CA (1) | CA2825620C (enExample) |
| CL (1) | CL2013002511A1 (enExample) |
| CO (1) | CO6751283A2 (enExample) |
| EA (1) | EA023824B1 (enExample) |
| ES (1) | ES2534973T3 (enExample) |
| IL (1) | IL228239A (enExample) |
| MX (1) | MX340031B (enExample) |
| MY (1) | MY163346A (enExample) |
| PH (1) | PH12013501805A1 (enExample) |
| SG (1) | SG193342A1 (enExample) |
| UA (1) | UA109687C2 (enExample) |
| WO (1) | WO2012120023A1 (enExample) |
| ZA (1) | ZA201306719B (enExample) |
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| AU2006307314C1 (en) | 2005-10-25 | 2011-08-25 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivative |
| 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 |
| ES2476605T3 (es) | 2007-04-24 | 2014-07-15 | Shionogi & Co., Ltd. | Derivados de aminohidrotiazina sustituidos con grupos cíclicos |
| AU2009258496B8 (en) | 2008-06-13 | 2014-06-26 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity |
| WO2010047372A1 (ja) | 2008-10-22 | 2010-04-29 | 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 |
| UA110467C2 (uk) | 2009-12-11 | 2016-01-12 | Шионогі Енд Ко., Лтд. | Похідні оксазину |
| PH12012502377A1 (en) | 2010-06-09 | 2014-10-14 | Janssen Pharmaceutica Nv | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
| CN103261199A (zh) | 2010-10-29 | 2013-08-21 | 盐野义制药株式会社 | 萘啶衍生物 |
| 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 |
| NZ610948A (en) | 2010-12-22 | 2014-06-27 | Janssen Pharmaceutica Nv | 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (bace) |
| JP5853033B2 (ja) | 2011-03-01 | 2016-02-09 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプＪａｎｓｓｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａ Ｎａａｍｌｏｚｅ Ｖｅｎｎｏｏｔｓｃｈａｐ | β−セクレターゼ（ＢＡＣＥ）の阻害剤として有用な６，７−ジヒドロ−ピラゾロ［１，５−ａ］ピラジン−４−イルアミン誘導体 |
| BR112013022917A2 (pt) | 2011-03-09 | 2016-12-06 | Janssen Pharmaceutica Nv | derivados 3,4-dihidro-pirrolo[1,2-a]pirazino-1-ilamina úteis como inibidores de beta-secretase (bace) |
| CN103608345A (zh) | 2011-04-26 | 2014-02-26 | 盐野义制药株式会社 | 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂 |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| KR102243133B1 (ko) * | 2013-06-12 | 2021-04-22 | 얀센 파마슈티카 엔.브이. | 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-6,7-디하이드로[1,2,3]트리아졸로[1,5-a]피라진 유도체 |
| JP6325092B2 (ja) * | 2013-06-12 | 2018-05-16 | ヤンセン ファーマシューティカ エヌ．ベー． | βーセクレターゼ（ＢＡＣＥ）の阻害剤としての４−アミノ−６−フェニル−５，６−ジヒドロイミダゾ［１，５−Ａ］ピラジン誘導体 |
| KR102243135B1 (ko) * | 2013-06-12 | 2021-04-22 | 얀센 파마슈티카 엔.브이. | 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-5,6-디하이드로이미다조[1,5-a]피라진-3(2h)-온 유도체 |
| 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 |
| EP3233834B1 (en) | 2014-12-18 | 2019-11-13 | Janssen Pharmaceutica NV | 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine derivatives useful as inhibitors of beta-secretase |
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| CN117471007B (zh) * | 2023-10-31 | 2024-08-09 | 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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| CN103608345A (zh) | 2011-04-26 | 2014-02-26 | 盐野义制药株式会社 | 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂 |
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| AU2013363151A1 (en) | 2012-12-20 | 2015-06-04 | Merck Sharp & Dohme Corp. | C5, C6 oxacyclic-fused iminothiazine dioxide compounds as BACE inhibitors |
| JP6325092B2 (ja) | 2013-06-12 | 2018-05-16 | ヤンセン ファーマシューティカ エヌ．ベー． | βーセクレターゼ（ＢＡＣＥ）の阻害剤としての４−アミノ−６−フェニル−５，６−ジヒドロイミダゾ［１，５−Ａ］ピラジン誘導体 |
| KR102243133B1 (ko) | 2013-06-12 | 2021-04-22 | 얀센 파마슈티카 엔.브이. | 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-6,7-디하이드로[1,2,3]트리아졸로[1,5-a]피라진 유도체 |
| KR102243135B1 (ko) | 2013-06-12 | 2021-04-22 | 얀센 파마슈티카 엔.브이. | 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-5,6-디하이드로이미다조[1,5-a]피라진-3(2h)-온 유도체 |
| EP3233834B1 (en) | 2014-12-18 | 2019-11-13 | Janssen Pharmaceutica NV | 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine derivatives useful as inhibitors of beta-secretase |
-
2012
- 2012-03-07 BR BR112013022917A patent/BR112013022917A2/pt not_active Application Discontinuation
- 2012-03-07 JP JP2013557074A patent/JP5853035B2/ja not_active Expired - Fee Related
- 2012-03-07 MY MYPI2013003278A patent/MY163346A/en unknown
- 2012-03-07 CA CA2825620A patent/CA2825620C/en active Active
- 2012-03-07 EA EA201391296A patent/EA023824B1/ru not_active IP Right Cessation
- 2012-03-07 PH PH1/2013/501805A patent/PH12013501805A1/en unknown
- 2012-03-07 MX MX2013010280A patent/MX340031B/es active IP Right Grant
- 2012-03-07 WO PCT/EP2012/053863 patent/WO2012120023A1/en not_active Ceased
- 2012-03-07 EP EP12707319.5A patent/EP2683721B1/en not_active Not-in-force
- 2012-03-07 KR KR1020137022396A patent/KR102012675B1/ko not_active Expired - Fee Related
- 2012-03-07 SG SG2013067210A patent/SG193342A1/en unknown
- 2012-03-07 US US14/003,901 patent/US9845326B2/en active Active
- 2012-03-07 CN CN201280012485.5A patent/CN103415521B/zh not_active Expired - Fee Related
- 2012-03-07 ES ES12707319.5T patent/ES2534973T3/es active Active
- 2012-03-07 AU AU2012224632A patent/AU2012224632B2/en not_active Ceased
- 2012-07-03 UA UAA201308782A patent/UA109687C2/ru unknown
-
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
Also Published As
| Publication number | Publication date |
|---|---|
| MY163346A (en) | 2017-09-15 |
| JP5853035B2 (ja) | 2016-02-09 |
| CA2825620A1 (en) | 2012-09-13 |
| JP2014507455A (ja) | 2014-03-27 |
| NZ615720A (en) | 2014-08-29 |
| AU2012224632B2 (en) | 2016-06-16 |
| EA023824B1 (ru) | 2016-07-29 |
| WO2012120023A1 (en) | 2012-09-13 |
| MX2013010280A (es) | 2013-10-01 |
| CA2825620C (en) | 2019-04-23 |
| KR102012675B1 (ko) | 2019-08-21 |
| PH12013501805A1 (en) | 2013-11-18 |
| BR112013022917A2 (pt) | 2016-12-06 |
| ZA201306719B (en) | 2015-04-29 |
| UA109687C2 (xx) | 2015-09-25 |
| IL228239A (en) | 2016-06-30 |
| CN103415521B (zh) | 2016-01-06 |
| IL228239A0 (en) | 2013-11-25 |
| SG193342A1 (en) | 2013-10-30 |
| MX340031B (es) | 2016-06-21 |
| KR20140019332A (ko) | 2014-02-14 |
| EP2683721B1 (en) | 2015-01-28 |
| US20130345228A1 (en) | 2013-12-26 |
| EA201391296A1 (ru) | 2014-01-30 |
| ES2534973T3 (es) | 2015-04-30 |
| HK1189223A1 (zh) | 2014-05-30 |
| US9845326B2 (en) | 2017-12-19 |
| CN103415521A (zh) | 2013-11-27 |
| EP2683721A1 (en) | 2014-01-15 |
| AU2012224632A1 (en) | 2013-08-01 |
| CO6751283A2 (es) | 2013-09-16 |
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