AR094762A1 - Compuestos de hexahidropirano[3,4-d][1,3]tiazin-2-amina sustituida con heteroarilo - Google Patents
Compuestos de hexahidropirano[3,4-d][1,3]tiazin-2-amina sustituida con heteroariloInfo
- Publication number
- AR094762A1 AR094762A1 ARP140100441A ARP140100441A AR094762A1 AR 094762 A1 AR094762 A1 AR 094762A1 AR P140100441 A ARP140100441 A AR P140100441A AR P140100441 A ARP140100441 A AR P140100441A AR 094762 A1 AR094762 A1 AR 094762A1
- Authority
- AR
- Argentina
- Prior art keywords
- cr5ar5b
- alkyl
- optionally substituted
- cycloalkyl
- methyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 5
- 229910052731 fluorine Inorganic materials 0.000 abstract 4
- 239000011737 fluorine Substances 0.000 abstract 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 abstract 2
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 2
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 abstract 2
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 238000001308 synthesis method Methods 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
Classifications
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- 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
- 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
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Endocrinology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
También se describen composiciones farmacéuticas, métodos de tratamiento, métodos de síntesis e intermediarios correspondientes. Reivindicación 1: Un compuesto de la fórmula (1) en donde R¹ es hidrógeno o metilo, en donde el metilo se sustituye opcionalmente con uno a tres flúor; R² es un heteroarilo de 5 a 10 miembros, que tiene de 1 a 4 heteroátomos seleccionados independientemente de N, O ó S, en donde al menos uno de los heteroátomos es N y en donde N se sustituye opcionalmente con R⁴; y en donde el heteroarilo de 5 a 10 miembros se sustituye opcionalmente sobre carbón con uno a tres R³; R³, en cada caso, se selecciona independientemente del grupo que consiste en halógeno, hidroxi, ciano, alquilo C₁₋₆, alcoxi C₁₋₆, alcoxi C₁₋₆-alquilo C₁₋₆, cicloalcoxi C₃₋₆, cicloalcoxi C₃₋₆-(CR⁵ᵃR⁵ᵇ)ₘ-, cicloalquil C₃₋₆-(CR⁵ᵃR⁵ᵇ)ₙ-O-, -(CR⁵ᵃR⁵ᵇ)ₘ-cicloalquilo C₃₋₆ o -(CR⁵ᵃR⁵ᵇ)ₘ-(heterocicloalquilo de 4 a 6 miembros); en donde cada uno de alquilo C₁₋₆, alcoxi C₁₋₆ o alcoxi C₁₋₆-alquilo C₁₋₆ se sustituye opcionalmente con 1 a 3 flúor y en donde el cicloalquilo C₃₋₆, cicloalcoxi C₃₋₆ y las porciones (heterocicloalquilo de 4 a 6 miembros) se sustituyen opcionalmente con 1 a 3 sustituyentes seleccionados independientemente del grupo que consiste en flúor, metilo, fluorometilo, difluorometilo o trifluorometilo; R⁴ es hidrógeno, alquilo C₁₋₆, -(CR⁵ᵃR⁵ᵇ)ₘ-cicloalquilo C₃₋₆ o -(CR⁵ᵃR⁵ᵇ)ₘ-(heterocicloalquilo de 4 a 6 miembros); en donde cada uno de alquilo C₁₋₆, cicloalquilo C₃₋₆ y las porciones -(heterocicloalquilo de 4 a 6 miembros) se sustituyen opcionalmente con 1 a 3 sustituyentes seleccionados independientemente de flúor, metilo, trifluorometilo, metoxi o trifluorometoxi; R⁵ᵃ y R⁵ᵇ son independientemente hidrógeno, metilo, fluorometilo, difluorometilo, trifluorometilo o metoxi; m, en cada caso, es independientemente 0, 1 ó 2; y n es 1, 2 ó 3; o un tautómero de aquel, o una sal aceptable desde el punto de vista farmacéutico del compuesto o tautómero.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361764185P | 2013-02-13 | 2013-02-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR094762A1 true AR094762A1 (es) | 2015-08-26 |
Family
ID=50114462
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP140100441A AR094762A1 (es) | 2013-02-13 | 2014-02-12 | Compuestos de hexahidropirano[3,4-d][1,3]tiazin-2-amina sustituida con heteroarilo |
Country Status (8)
| Country | Link |
|---|---|
| US (3) | US8865706B2 (es) |
| EP (1) | EP2956458B1 (es) |
| JP (1) | JP2016507551A (es) |
| AR (1) | AR094762A1 (es) |
| CA (1) | CA2897678A1 (es) |
| TW (1) | TW201443064A (es) |
| UY (1) | UY35320A (es) |
| WO (1) | WO2014125394A1 (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013030713A1 (en) | 2011-08-31 | 2013-03-07 | Pfizer Inc. | Hexahydropyrano [3,4-d][1,3] thiazin-2-amine compounds |
| WO2013164730A1 (en) * | 2012-05-04 | 2013-11-07 | Pfizer Inc. | Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin- 2 -amine compounds as inhibitors of app, bace1 and bace 2. |
| EP2897964A1 (en) | 2012-09-20 | 2015-07-29 | Pfizer Inc. | Alkyl-substituted hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds |
| CA2893256A1 (en) | 2012-12-11 | 2014-06-19 | Pfizer Inc. | Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds as inhibitors of bace1 |
| JP6162820B2 (ja) | 2012-12-19 | 2017-07-12 | ファイザー・インク | 炭素環式および複素環式置換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 |
| WO2014125394A1 (en) * | 2013-02-13 | 2014-08-21 | Pfizer Inc. | HETEROARYL-SUBSTITUTED HEXAHYDROPYRANO [3,4-d][1,3] THIAZIN-2-AMINE COMPOUNDS |
| US9233981B1 (en) | 2013-02-15 | 2016-01-12 | Pfizer Inc. | Substituted phenyl hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| CN106459088A (zh) | 2014-04-10 | 2017-02-22 | 辉瑞公司 | 2‑氨基‑6‑甲基‑4,4a,5,6‑四氢吡喃并[3,4‑d][1,3]噻嗪‑8a(8H)‑基‑1,3‑噻唑‑4‑基酰胺 |
| 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 |
| BR112018003489A2 (pt) | 2015-09-24 | 2018-09-25 | Pfizer | n-[2-(2-amino-6,6-dissubstituído-4,4a,5,6-tetra-hidropirano[3,4-d][1,3]tiazin-8a(8h)-il)-1,3-tiazol-4-il]amidas |
| JP2018531924A (ja) | 2015-09-24 | 2018-11-01 | ファイザー・インク | テトラヒドロピラノ[3,4−d][1,3]オキサジン誘導体、およびbace阻害剤としてのその使用 |
| EP3497105A1 (en) * | 2016-08-11 | 2019-06-19 | Eli Lilly And Company | Aminothiazines and their use as bace1 inhibitors |
| CN107235978B (zh) * | 2017-08-01 | 2019-05-21 | 上海泓博智源医药股份有限公司 | 一种abt-199中间体的制备方法 |
| WO2020087031A1 (en) | 2018-10-26 | 2020-04-30 | The Research Foundation For The State University Of New York | Combination serotonin specific reuptake inhibitor and serotonin 1a receptor partial agonist for reducing l-dopa-induced dyskinesia |
| CN115272385B (zh) * | 2021-04-30 | 2025-05-16 | 中国医学科学院基础医学研究所 | 基于自动生成标签的脑出血和周围水肿的协同交叉分割系统 |
| CN116768797A (zh) * | 2022-03-16 | 2023-09-19 | 成都苑东生物制药股份有限公司 | 一种吡唑类衍生物、其制备方法及用途 |
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| AR077277A1 (es) | 2009-07-09 | 2011-08-17 | Lilly Co Eli | Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer |
| US8188079B2 (en) | 2009-08-19 | 2012-05-29 | Hoffman-La Roche Inc. | 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines |
| JPWO2011071109A1 (ja) * | 2009-12-11 | 2013-04-22 | 塩野義製薬株式会社 | アミノ基を有する縮合ヘテロ環化合物 |
| GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| WO2012162334A1 (en) | 2011-05-24 | 2012-11-29 | Bristol-Myers Squibb Company | Compounds for the reduction of beta-amyloid production |
| WO2013030713A1 (en) | 2011-08-31 | 2013-03-07 | Pfizer Inc. | Hexahydropyrano [3,4-d][1,3] thiazin-2-amine compounds |
| WO2013164730A1 (en) * | 2012-05-04 | 2013-11-07 | Pfizer Inc. | Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin- 2 -amine compounds as inhibitors of app, bace1 and bace 2. |
| CA2893256A1 (en) | 2012-12-11 | 2014-06-19 | Pfizer Inc. | Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds as inhibitors of bace1 |
| WO2014125394A1 (en) * | 2013-02-13 | 2014-08-21 | Pfizer Inc. | HETEROARYL-SUBSTITUTED HEXAHYDROPYRANO [3,4-d][1,3] THIAZIN-2-AMINE COMPOUNDS |
| EP3119347B1 (en) | 2014-03-21 | 2023-06-07 | Align Technology, Inc. | Segmented orthodontic appliance with elastics |
-
2014
- 2014-02-03 WO PCT/IB2014/058760 patent/WO2014125394A1/en not_active Ceased
- 2014-02-03 EP EP14704927.4A patent/EP2956458B1/en not_active Not-in-force
- 2014-02-03 CA CA2897678A patent/CA2897678A1/en not_active Abandoned
- 2014-02-03 JP JP2015556596A patent/JP2016507551A/ja active Pending
- 2014-02-11 TW TW103104416A patent/TW201443064A/zh unknown
- 2014-02-12 US US14/178,470 patent/US8865706B2/en not_active Expired - Fee Related
- 2014-02-12 AR ARP140100441A patent/AR094762A1/es unknown
- 2014-02-12 UY UY0001035320A patent/UY35320A/es not_active Application Discontinuation
- 2014-08-21 US US14/464,935 patent/US9045499B2/en not_active Expired - Fee Related
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2015
- 2015-04-23 US US14/694,288 patent/US9192612B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| TW201443064A (zh) | 2014-11-16 |
| JP2016507551A (ja) | 2016-03-10 |
| US20140228356A1 (en) | 2014-08-14 |
| US20140364426A1 (en) | 2014-12-11 |
| US20150224110A1 (en) | 2015-08-13 |
| EP2956458B1 (en) | 2017-08-09 |
| WO2014125394A1 (en) | 2014-08-21 |
| US9192612B2 (en) | 2015-11-24 |
| EP2956458A1 (en) | 2015-12-23 |
| UY35320A (es) | 2014-09-30 |
| CA2897678A1 (en) | 2014-08-21 |
| US8865706B2 (en) | 2014-10-21 |
| US9045499B2 (en) | 2015-06-02 |
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