MX347912B - Derivados de 5,6-dihidro-imidazo[1,2-a]pirazin-8ilaminautiles como inhibidores de beta-secretasa (bace). - Google Patents
Derivados de 5,6-dihidro-imidazo[1,2-a]pirazin-8ilaminautiles como inhibidores de beta-secretasa (bace).Info
- Publication number
- MX347912B MX347912B MX2013007294A MX2013007294A MX347912B MX 347912 B MX347912 B MX 347912B MX 2013007294 A MX2013007294 A MX 2013007294A MX 2013007294 A MX2013007294 A MX 2013007294A MX 347912 B MX347912 B MX 347912B
- Authority
- MX
- Mexico
- Prior art keywords
- beta
- secretase
- dementia
- bace
- pyrazin
- Prior art date
Links
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 title abstract 4
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 title abstract 4
- DZJJKLGKUNDJBW-UHFFFAOYSA-N 5,6-dihydroimidazo[1,2-a]pyrazin-8-amine Chemical class NC1=NCCN2C=CN=C12 DZJJKLGKUNDJBW-UHFFFAOYSA-N 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 102100021257 Beta-secretase 1 Human genes 0.000 abstract 4
- 206010012289 Dementia Diseases 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 208000024827 Alzheimer disease Diseases 0.000 abstract 2
- 101710150192 Beta-secretase 1 Proteins 0.000 abstract 2
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 102000013455 Amyloid beta-Peptides Human genes 0.000 abstract 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 abstract 1
- 206010059245 Angiopathy Diseases 0.000 abstract 1
- 206010067889 Dementia with Lewy bodies Diseases 0.000 abstract 1
- 201000010374 Down Syndrome Diseases 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 201000002832 Lewy body dementia Diseases 0.000 abstract 1
- 208000005314 Multi-Infarct Dementia Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 206010039966 Senile dementia Diseases 0.000 abstract 1
- 208000006011 Stroke Diseases 0.000 abstract 1
- 206010044688 Trisomy 21 Diseases 0.000 abstract 1
- 201000004810 Vascular dementia Diseases 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder 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
- 208000027061 mild cognitive impairment Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 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
- A61P25/14—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
- A61P25/28—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)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente invención se refiere a derivados novedosos de 5,6-dihidro-imidazo[1,2-a]pirazin-8-ilamina como inhibidores de beta-secretasa, conocida también como enzima de separación amiloide del sitio beta, BACE, BACE1, Asp2 o memapsina2; la invención está dirigida también a composiciones farmacéuticas que comprenden dichos compuestos, a procedimientos para preparar dichos compuestos y composiciones, y al uso de dichos compuestos y composiciones para la prevención y el tratamiento de trastornos en los cuales la beta-secretasa está implicada, tal como en enfermedad de Alzheimer (AD), deterioro cognitivo leve, senilidad, demencia, demencia con cuerpos de Lewy, angiopatía amiloide cerebrovascular, demencia por infartos múltiples, síndrome de Down, demencia asociada con accidente cerebrovascular, demencia asociada con enfermedad de Parkinson o demencia asociada con beta-amiloide.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10196568 | 2010-12-22 | ||
| PCT/EP2011/073522 WO2012085038A1 (en) | 2010-12-22 | 2011-12-21 | 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2013007294A MX2013007294A (es) | 2013-08-26 |
| MX347912B true MX347912B (es) | 2017-05-17 |
Family
ID=43923528
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2013007294A MX347912B (es) | 2010-12-22 | 2011-12-21 | Derivados de 5,6-dihidro-imidazo[1,2-a]pirazin-8ilaminautiles como inhibidores de beta-secretasa (bace). |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US9840507B2 (es) |
| EP (1) | EP2655376B1 (es) |
| JP (1) | JP5834091B2 (es) |
| KR (1) | KR101866987B1 (es) |
| CN (1) | CN103403007B (es) |
| AU (1) | AU2011347377B2 (es) |
| BR (1) | BR112013015430A2 (es) |
| CA (1) | CA2819175C (es) |
| CO (1) | CO6721049A2 (es) |
| EA (1) | EA022409B1 (es) |
| ES (1) | ES2648143T3 (es) |
| IL (1) | IL227054A (es) |
| MX (1) | MX347912B (es) |
| MY (1) | MY170715A (es) |
| NZ (1) | NZ610948A (es) |
| SG (1) | SG191097A1 (es) |
| UA (1) | UA109459C2 (es) |
| WO (1) | WO2012085038A1 (es) |
| ZA (1) | ZA201304646B (es) |
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| CN101346357B (zh) | 2005-10-25 | 2014-04-02 | 盐野义制药株式会社 | 氨基二氢噻嗪衍生物 |
| 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 |
| KR101324426B1 (ko) | 2008-06-13 | 2013-10-31 | 시오노기세야쿠 가부시키가이샤 | β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체 |
| 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 |
| KR20120104570A (ko) | 2009-12-11 | 2012-09-21 | 시오노기세야쿠 가부시키가이샤 | 옥사진 유도체 |
| KR101730937B1 (ko) | 2010-06-09 | 2017-04-27 | 얀센 파마슈티카 엔.브이. | 베타-세크레타아제(bace) 저해제로 유용한 5,6-디하이드로-2h-[1,4]옥사진-3-일-아민 유도체 |
| CN103261199A (zh) | 2010-10-29 | 2013-08-21 | 盐野义制药株式会社 | 萘啶衍生物 |
| EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE |
| BR112013015430A2 (pt) * | 2010-12-22 | 2016-09-20 | Janssen Pharmaceutica Nv | derivados de 5,6-diidro-imidazo[1,2-a]pirazin-8-ilamina úteis como inibidores de beta-secretase (bace) |
| CN103415519B (zh) | 2011-03-01 | 2016-03-02 | 詹森药业有限公司 | 作为β-分泌酶(BACE)抑制剂有用的6,7-二氢-吡唑[1,5-a]吡嗪-4-基胺衍生物 |
| PH12013501805A1 (en) | 2011-03-09 | 2013-11-18 | Janssen Pharmaceutica Nv | 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF 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 |
| WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
| WO2014198851A1 (en) * | 2013-06-12 | 2014-12-18 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace) |
| CN105283457B (zh) * | 2013-06-12 | 2018-09-18 | 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-5,6-二氢咪唑并[1,5-A]吡嗪衍生物 |
| US9751886B2 (en) | 2013-06-12 | 2017-09-05 | 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) |
| CN104016925B (zh) * | 2014-06-17 | 2016-03-30 | 遵义医学院 | 4-烷基咪唑-2-羧酸的合成方法 |
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| CN114727974A (zh) | 2019-07-30 | 2022-07-08 | 艾科尼佐治疗股份有限公司 | Hdac6抑制剂及其用途 |
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| KR101730937B1 (ko) | 2010-06-09 | 2017-04-27 | 얀센 파마슈티카 엔.브이. | 베타-세크레타아제(bace) 저해제로 유용한 5,6-디하이드로-2h-[1,4]옥사진-3-일-아민 유도체 |
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| PH12013501805A1 (en) | 2011-03-09 | 2013-11-18 | Janssen Pharmaceutica Nv | 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF 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 |
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| CA2853891C (en) | 2011-12-06 | 2020-03-10 | Janssen Pharmaceutica Nv | 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives |
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| CN105283457B (zh) | 2013-06-12 | 2018-09-18 | 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-5,6-二氢咪唑并[1,5-A]吡嗪衍生物 |
| WO2014198851A1 (en) | 2013-06-12 | 2014-12-18 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace) |
| US9751886B2 (en) | 2013-06-12 | 2017-09-05 | 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) |
| 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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2011
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- 2011-12-21 EA EA201390932A patent/EA022409B1/ru not_active IP Right Cessation
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|---|---|
| EP2655376B1 (en) | 2017-08-23 |
| IL227054A (en) | 2016-09-29 |
| ES2648143T3 (es) | 2017-12-28 |
| KR101866987B1 (ko) | 2018-07-19 |
| AU2011347377A1 (en) | 2013-06-13 |
| MX2013007294A (es) | 2013-08-26 |
| KR20130132556A (ko) | 2013-12-04 |
| US9840507B2 (en) | 2017-12-12 |
| MY170715A (en) | 2019-08-27 |
| UA109459C2 (xx) | 2015-08-25 |
| CN103403007B (zh) | 2015-12-09 |
| CA2819175C (en) | 2019-01-08 |
| CN103403007A (zh) | 2013-11-20 |
| CO6721049A2 (es) | 2013-07-31 |
| EA201390932A1 (ru) | 2013-11-29 |
| BR112013015430A2 (pt) | 2016-09-20 |
| CA2819175A1 (en) | 2012-06-28 |
| WO2012085038A1 (en) | 2012-06-28 |
| EP2655376A1 (en) | 2013-10-30 |
| EA022409B1 (ru) | 2015-12-30 |
| HK1189221A1 (zh) | 2014-05-30 |
| ZA201304646B (en) | 2014-12-23 |
| AU2011347377B2 (en) | 2016-03-03 |
| JP5834091B2 (ja) | 2015-12-16 |
| SG191097A1 (en) | 2013-08-30 |
| NZ610948A (en) | 2014-06-27 |
| JP2014500293A (ja) | 2014-01-09 |
| US20130274266A1 (en) | 2013-10-17 |
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