GB201312819D0 - Novel compounds - Google Patents
Novel compoundsInfo
- Publication number
- GB201312819D0 GB201312819D0 GBGB1312819.4A GB201312819A GB201312819D0 GB 201312819 D0 GB201312819 D0 GB 201312819D0 GB 201312819 A GB201312819 A GB 201312819A GB 201312819 D0 GB201312819 D0 GB 201312819D0
- Authority
- GB
- United Kingdom
- Prior art keywords
- dementia
- thiazin
- furo
- fluorophenyl
- tetrahydro
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 206010012289 Dementia Diseases 0.000 abstract 6
- 208000024827 Alzheimer disease Diseases 0.000 abstract 5
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 abstract 2
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 abstract 2
- 208000018737 Parkinson disease Diseases 0.000 abstract 2
- 208000010877 cognitive disease Diseases 0.000 abstract 2
- 230000003412 degenerative effect Effects 0.000 abstract 2
- 230000002401 inhibitory effect Effects 0.000 abstract 2
- 208000027061 mild cognitive impairment Diseases 0.000 abstract 2
- CBRWVECCYCXYSK-FWVNDXEPSA-N 5-[[3-[(4as,5s,7as)-2-amino-5-(trifluoromethyl)-4,4a,5,7-tetrahydrofuro[3,4-d][1,3]thiazin-7a-yl]-4-fluorophenyl]carbamoyl]pyrazine-2-carboxylic acid Chemical compound C=1C=C(F)C([C@@]23N=C(SC[C@@H]2[C@H](OC3)C(F)(F)F)N)=CC=1NC(=O)C1=CN=C(C(O)=O)C=N1 CBRWVECCYCXYSK-FWVNDXEPSA-N 0.000 abstract 1
- 208000018282 ACys amyloidosis Diseases 0.000 abstract 1
- 208000000044 Amnesia Diseases 0.000 abstract 1
- 206010059245 Angiopathy Diseases 0.000 abstract 1
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 abstract 1
- 201000010374 Down Syndrome Diseases 0.000 abstract 1
- 208000007487 Familial Cerebral Amyloid Angiopathy Diseases 0.000 abstract 1
- 208000032849 Hereditary cerebral hemorrhage with amyloidosis Diseases 0.000 abstract 1
- 208000026139 Memory disease Diseases 0.000 abstract 1
- 206010036631 Presenile dementia Diseases 0.000 abstract 1
- 206010039966 Senile dementia Diseases 0.000 abstract 1
- 206010048327 Supranuclear palsy Diseases 0.000 abstract 1
- 206010044688 Trisomy 21 Diseases 0.000 abstract 1
- 230000001054 cortical effect Effects 0.000 abstract 1
- 230000007850 degeneration Effects 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 210000004558 lewy body Anatomy 0.000 abstract 1
- 230000006984 memory degeneration Effects 0.000 abstract 1
- 208000023060 memory loss Diseases 0.000 abstract 1
- HYXVPHRLNWHFCG-HNJNHCNJSA-N n-[3-[(4as,5s,7as)-2-amino-5-(trifluoromethyl)-4,4a,5,7-tetrahydrofuro[3,4-d][1,3]thiazin-7a-yl]-4-fluorophenyl]-5-(hydroxymethyl)pyrazine-2-carboxamide Chemical compound C=1C=C(F)C([C@@]23N=C(SC[C@@H]2[C@H](OC3)C(F)(F)F)N)=CC=1NC(=O)C1=CN=C(CO)C=N1 HYXVPHRLNWHFCG-HNJNHCNJSA-N 0.000 abstract 1
- IRLXHSQYHOTSAB-SCDSUCTJSA-N n-[3-[(4as,5s,7as)-2-amino-5-(trifluoromethyl)-4,4a,5,7-tetrahydrofuro[3,4-d][1,3]thiazin-7a-yl]-4-fluorophenyl]acetamide Chemical compound CC(=O)NC1=CC=C(F)C([C@@]23[C@@H]([C@H](OC2)C(F)(F)F)CSC(N)=N3)=C1 IRLXHSQYHOTSAB-SCDSUCTJSA-N 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 230000000069 prophylactic effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
- 230000002792 vascular Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—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
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/542—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 sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
A compound selected from 5-((3-((4aS,5S,7aS)-2-amino-5-(trifluoromethyl)-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)carbamoyl)pyrazine-2-carboxylic acid (A), N-(3-((4aS,5S,7aS)-2-amino-5-(trifluoromethyl)-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-(hydroxymethyl)pyrazine-2-carboxamide (B) and N-(3-((4aS,5S,7aS)-2-amino-5-(trifluoromethyl)-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)acetamide (C) or pharmaceutically acceptable salts thereof. The compounds have an amyloid β (Aβ) production inhibitory effect or a beta-secretase (BACE1) inhibitory effect and which may be useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ such as Alzheimer-typedementia (AD), Down's syndrome, cerebrovascular amyloid angiopathy (CAA), mild cognitive impairment (MCI), memory loss, presenile dementia, senile dementia, hereditary cerebral hemorrhage with amyloidosis, and other degenerative dementias such as dementias of mixed vascular and degenerative origin, dementia associated with supranuclear palsy, dementia associated with cortical basal degeneration, dementia associated with Parkinson's Disease (PD), and dementia associated with diffuse Lewy Body type of AD.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1212816.1A GB201212816D0 (en) | 2012-07-19 | 2012-07-19 | Novel compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| GB201312819D0 true GB201312819D0 (en) | 2013-12-11 |
| GB2504615A GB2504615A (en) | 2014-02-05 |
Family
ID=46881623
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GBGB1212816.1A Ceased GB201212816D0 (en) | 2012-07-19 | 2012-07-19 | Novel compounds |
| GB1312819.4A Withdrawn GB2504615A (en) | 2012-07-19 | 2013-07-18 | Fused aminodihydrothiazine derivatives |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GBGB1212816.1A Ceased GB201212816D0 (en) | 2012-07-19 | 2012-07-19 | Novel compounds |
Country Status (1)
| Country | Link |
|---|---|
| GB (2) | GB201212816D0 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113439121A (en) * | 2019-02-13 | 2021-09-24 | 普罗拜奥根股份公司 | Transposases with enhanced insertion site selection properties |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR103680A1 (en) * | 2015-02-23 | 2017-05-24 | Lilly Co Eli | BACE1 SELECTIVE INHIBITORS |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201100181D0 (en) * | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| ES2624288T3 (en) * | 2011-01-21 | 2017-07-13 | Eisai R&D Management Co., Ltd. | Methods and compounds useful in the synthesis of condensed aminodihydrotiazine derivatives |
| GB201101139D0 (en) * | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101140D0 (en) * | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
-
2012
- 2012-07-19 GB GBGB1212816.1A patent/GB201212816D0/en not_active Ceased
-
2013
- 2013-07-18 GB GB1312819.4A patent/GB2504615A/en not_active Withdrawn
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113439121A (en) * | 2019-02-13 | 2021-09-24 | 普罗拜奥根股份公司 | Transposases with enhanced insertion site selection properties |
Also Published As
| Publication number | Publication date |
|---|---|
| GB201212816D0 (en) | 2012-09-05 |
| GB2504615A (en) | 2014-02-05 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| WAP | Application withdrawn, taken to be withdrawn or refused ** after publication under section 16(1) |