PE20170327A1 - 2-AMINO-6-METIL-4,4a,5,6-TETRAHIDROPIRANO[3,4d] [1,3] TIAZIN-8a(8H)-IL-1,3-TIAZOL-4-ILAMIDAS - Google Patents
2-AMINO-6-METIL-4,4a,5,6-TETRAHIDROPIRANO[3,4d] [1,3] TIAZIN-8a(8H)-IL-1,3-TIAZOL-4-ILAMIDASInfo
- Publication number
- PE20170327A1 PE20170327A1 PE2016001933A PE2016001933A PE20170327A1 PE 20170327 A1 PE20170327 A1 PE 20170327A1 PE 2016001933 A PE2016001933 A PE 2016001933A PE 2016001933 A PE2016001933 A PE 2016001933A PE 20170327 A1 PE20170327 A1 PE 20170327A1
- Authority
- PE
- Peru
- Prior art keywords
- thiazol
- amino
- methyl
- thiazin
- tetrahydropyrano
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 abstract 4
- 239000003112 inhibitor Substances 0.000 abstract 2
- 125000006763 (C3-C9) cycloalkyl group Chemical group 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 101710137189 Amyloid-beta A4 protein Proteins 0.000 abstract 1
- 101710151993 Amyloid-beta precursor protein Proteins 0.000 abstract 1
- 102100022704 Amyloid-beta precursor protein Human genes 0.000 abstract 1
- 101800001718 Amyloid-beta protein Proteins 0.000 abstract 1
- 102000009091 Amyloidogenic Proteins Human genes 0.000 abstract 1
- 108010048112 Amyloidogenic Proteins Proteins 0.000 abstract 1
- 102100021257 Beta-secretase 1 Human genes 0.000 abstract 1
- 102100021277 Beta-secretase 2 Human genes 0.000 abstract 1
- 125000001313 C5-C10 heteroaryl group Chemical group 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
- 101000894883 Homo sapiens Beta-secretase 2 Proteins 0.000 abstract 1
- ABEZBNOKPIPPHW-BEPCFFQHSA-N NC=1SC[C@H]2[C@@](N1)(CO[C@H](C2)C)C=2SC=C(N2)NC(=O)C=2N=C(OC2)CF Chemical compound NC=1SC[C@H]2[C@@](N1)(CO[C@H](C2)C)C=2SC=C(N2)NC(=O)C=2N=C(OC2)CF ABEZBNOKPIPPHW-BEPCFFQHSA-N 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- DZHSAHHDTRWUTF-SIQRNXPUSA-N amyloid-beta polypeptide 42 Chemical compound C([C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)NCC(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(O)=O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(O)=O)C(C)C)C(C)C)C1=CC=CC=C1 DZHSAHHDTRWUTF-SIQRNXPUSA-N 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 238000003776 cleavage reaction Methods 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
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 230000000626 neurodegenerative effect Effects 0.000 abstract 1
- 230000000926 neurological effect Effects 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000007017 scission Effects 0.000 abstract 1
Classifications
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- 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
-
- 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
- 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
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Emergency Medicine (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Esta invencion proporciona compuestos, tautomeros y sales farmaceuticamente aceptables de derivados de 2-amino-6-metil-4,4a,5,6-tetrahidropirano[3,4-d][1,3]tiazin-8a(8H)-il-1,3-tiazol-4-il-amidas de formula I, en donde: R1 es fenilo, cicloalquilo C3-C9, o heteroarilo de 5 a 10 miembros cualquiera de ellos opcionalmente sustituido con 1 a 3 R2. Entre los compuestos preferidos tenemos: N-{2-[(4aR,6S,8aR)-2-amino-6-metil-4,4a,5,6-tetrahidropirano[3,4-d][1,3]tiazin-8a(8H)-il]-1,3-tiazol-4-il}-5-(difluorometoxi)piridin-2-carboxamida; N-{2-[(4aR,6S,8aR)-2-amino-6-metil-4,4a,5,6-tetrahidropirano[3,4-d][1,3]tiazin-8a(8H)-il]-1,3-tiazol-4-il}-5-(difluorometoxi)pirazin-2-carboxamida; N-{2-[(4aR,6S,8aR)-2-amino-6-metil-4,4a,5,6-tetrahidropirano[3,4-d][1,3]tiazin-8a(8H)-il]-1,3-tiazol-4-il}-2-(fluorometil)-1,3-oxazol-4-carboxamida, entre otros. Estos compuestos son inhibidores de la enzima de escision 1 (BACE1) de la proteina precursora amiloide de sitio ß (APP) e inhibidores de BACE2. Estos compuestos inhiben la produccion de A-beta peptidos que pueden contribuir a la formacion de deposiciones neurologicas de proteina amiloide y son empleados en el tratamiento de la enfermedad de Alzheimer y otros trastornos neurodegenerativos y/o neurologicos.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461977774P | 2014-04-10 | 2014-04-10 | |
| US201562119862P | 2015-02-24 | 2015-02-24 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20170327A1 true PE20170327A1 (es) | 2017-04-21 |
Family
ID=53005609
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2016001933A PE20170327A1 (es) | 2014-04-10 | 2015-03-27 | 2-AMINO-6-METIL-4,4a,5,6-TETRAHIDROPIRANO[3,4d] [1,3] TIAZIN-8a(8H)-IL-1,3-TIAZOL-4-ILAMIDAS |
Country Status (26)
| Country | Link |
|---|---|
| US (5) | US9315520B2 (es) |
| EP (1) | EP3129388A1 (es) |
| JP (1) | JP6111002B1 (es) |
| KR (2) | KR101875811B1 (es) |
| CN (1) | CN106459088A (es) |
| AP (1) | AP2016009493A0 (es) |
| AU (1) | AU2015245260A1 (es) |
| CA (1) | CA2944971C (es) |
| CL (1) | CL2016002510A1 (es) |
| CR (1) | CR20160455A (es) |
| CU (1) | CU20160151A7 (es) |
| DO (1) | DOP2016000276A (es) |
| EA (1) | EA030085B1 (es) |
| EC (1) | ECSP16079730A (es) |
| IL (1) | IL248277A0 (es) |
| MA (1) | MA39866A (es) |
| MD (1) | MD20160105A2 (es) |
| MX (1) | MX2016013329A (es) |
| PE (1) | PE20170327A1 (es) |
| PH (1) | PH12016501977A1 (es) |
| SG (1) | SG11201607896YA (es) |
| SV (1) | SV2016005294A (es) |
| TW (1) | TWI551605B (es) |
| UY (1) | UY36073A (es) |
| WO (1) | WO2015155626A1 (es) |
| ZA (1) | ZA201606517B (es) |
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| JP6043355B2 (ja) | 2011-08-31 | 2016-12-14 | ファイザー・インク | ヘキサヒドロピラノ［３，４−ｄ］［１，３］チアジン−２−アミン化合物 |
| US9403846B2 (en) | 2012-12-19 | 2016-08-02 | Pfizer Inc. | Carbocyclic- and heterocyclic-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| CR20160455A (es) | 2014-04-10 | 2016-12-16 | Pfizer | 2-AMINO-6-METIL-4,4a,5,6-TETRAHIDROPIRANO[3,4-d][1,3]TIAZIN-8a(8H)-IL-1,3-TIAZOL-4-ILA |
| WO2017051294A1 (en) | 2015-09-24 | 2017-03-30 | Pfizer Inc. | N-[2-(3-amino-2,5-dimethyl-1,1-dioxido-5,6-dihydro-2h-1,2,4-thiadiazin-5-yl)-1,3-thiazol-4-yl] amides useful as bace inhibitors |
| WO2017051276A1 (en) * | 2015-09-24 | 2017-03-30 | Pfizer Inc. | N-[2-(2-amino-6,6-disubstituted-4, 4a, 5, 6-tetrahydropyrano [3,4-d][1,3] thiazin-8a (8h)-yl) -1, 3-thiazol-4-yl] amides |
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| KR20230016186A (ko) | 2020-05-26 | 2023-02-01 | 트루바인딩 아이엔씨. | 갈렉틱-3 차단에 의한 염증성 질환의 치료 방법 |
| TW202430031A (zh) | 2022-09-30 | 2024-08-01 | 瑞士商先正達農作物保護股份公司 | 殺微生物之吡唑衍生物 |
| TW202430514A (zh) | 2022-09-30 | 2024-08-01 | 瑞士商先正達農作物保護股份公司 | 殺微生物之吡唑衍生物 |
| WO2025114167A1 (en) | 2023-11-28 | 2025-06-05 | Syngenta Crop Protection Ag | Microbiocidal pyrazole derivatives |
| WO2025191053A1 (en) | 2024-03-14 | 2025-09-18 | Syngenta Crop Protection Ag | Microbiocidal pyrazole derivatives |
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