AR094918A1 - Compuestos de tetrahidropirrolotiazina como inhibidores de bace - Google Patents
Compuestos de tetrahidropirrolotiazina como inhibidores de baceInfo
- Publication number
- AR094918A1 AR094918A1 ARP140100629A ARP140100629A AR094918A1 AR 094918 A1 AR094918 A1 AR 094918A1 AR P140100629 A ARP140100629 A AR P140100629A AR P140100629 A ARP140100629 A AR P140100629A AR 094918 A1 AR094918 A1 AR 094918A1
- Authority
- AR
- Argentina
- Prior art keywords
- compounds
- tetrahydropirrolotiazine
- bace inhibitors
- bace
- inhibitors
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
- 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)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Se proporciona un compuesto de fórmula (1), en donde R es H o F; y A es un resto seleccionado del grupo de fórmulas (2); o una sal del mismo farmacéuticamente aceptable. Estos compuestos tienen utilidad en el tratamiento de la enfermedad de Alzheimer.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361776819P | 2013-03-12 | 2013-03-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR094918A1 true AR094918A1 (es) | 2015-09-09 |
Family
ID=50382615
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP140100629A AR094918A1 (es) | 2013-03-12 | 2014-02-27 | Compuestos de tetrahidropirrolotiazina como inhibidores de bace |
Country Status (37)
| Country | Link |
|---|---|
| US (3) | US8841293B1 (es) |
| EP (1) | EP2970336B1 (es) |
| JP (1) | JP6095844B2 (es) |
| KR (1) | KR101688761B1 (es) |
| CN (1) | CN105026404B (es) |
| AP (1) | AP2015008713A0 (es) |
| AR (1) | AR094918A1 (es) |
| BR (1) | BR112015018738A8 (es) |
| CA (1) | CA2898500C (es) |
| CL (1) | CL2015002529A1 (es) |
| CR (1) | CR20150418A (es) |
| CY (1) | CY1119585T1 (es) |
| DK (1) | DK2970336T3 (es) |
| EA (1) | EA026006B1 (es) |
| ES (1) | ES2653421T3 (es) |
| HR (1) | HRP20171851T1 (es) |
| HU (1) | HUE037487T2 (es) |
| IL (1) | IL240903B (es) |
| JO (1) | JO3317B1 (es) |
| LT (1) | LT2970336T (es) |
| MA (1) | MA38390B1 (es) |
| ME (1) | ME02910B (es) |
| MX (1) | MX2015012628A (es) |
| MY (1) | MY180083A (es) |
| NO (1) | NO3039297T3 (es) |
| NZ (1) | NZ712207A (es) |
| PE (1) | PE20151542A1 (es) |
| PH (1) | PH12015502031A1 (es) |
| PL (1) | PL2970336T3 (es) |
| PT (1) | PT2970336T (es) |
| RS (1) | RS56645B1 (es) |
| SG (1) | SG11201507499XA (es) |
| SI (1) | SI2970336T1 (es) |
| TN (1) | TN2015000340A1 (es) |
| TW (1) | TWI593692B (es) |
| UA (1) | UA112941C2 (es) |
| WO (1) | WO2014143579A1 (es) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI633087B (zh) | 2012-06-13 | 2018-08-21 | 赫孚孟拉羅股份公司 | 新穎二氮雜螺環烷及氮雜螺環烷 |
| HRP20191937T1 (hr) | 2012-09-25 | 2020-01-10 | F. Hoffmann - La Roche Ag | Derivati heksahidropirolo [3,4-c]pirola i srodni spojevi kao inhibitori autotaksina (atx) i kao inhibitori proizvodnje lizofosfatidne kiseline (lpa) za liječenje npr. bubrežnih bolesti |
| CN104755484B (zh) | 2012-10-26 | 2016-02-17 | 伊莱利利公司 | Bace抑制剂 |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| LT3074400T (lt) | 2013-11-26 | 2018-02-12 | F. Hoffmann-La Roche Ag | Oktahidro-ciklobuta [1,2-c;3,4-c`]dipirolo dariniai kaip autotaksino inhibitoriai |
| TWI684452B (zh) | 2014-03-14 | 2020-02-11 | 美國禮來大藥廠 | 胺基噻嗪化合物 |
| PE20161223A1 (es) | 2014-03-26 | 2016-11-12 | Hoffmann La Roche | Compuestos condensados de [1,4]diazepina como inhibidores de la produccion de autotaxina (atx) y acido lisofosfatidico (lpa) |
| EA037928B1 (ru) | 2014-03-26 | 2021-06-08 | Ф. Хоффманн-Ля Рош Аг | Бициклические соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa) |
| TWI570127B (zh) * | 2014-09-15 | 2017-02-11 | 美國禮來大藥廠 | 結晶型N-[3-[(4aR,7aS)-2-胺基-6-(5-氟嘧啶-2-基)-4,4a,5,7-四氫吡咯并[3,4-d][1,3]噻嗪-7a-基]-4-氟-苯基]-5-甲氧基-吡嗪-2-甲醯胺、其用途及醫藥組合物 |
| TWI599358B (zh) | 2014-09-16 | 2017-09-21 | 美國禮來大藥廠 | 組合療法 |
| TWI574969B (zh) * | 2015-01-30 | 2017-03-21 | 美國禮來大藥廠 | 甲苯磺酸鹽 |
| AR103680A1 (es) | 2015-02-23 | 2017-05-24 | Lilly Co Eli | Inhibidores selectivos de bace1 |
| MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
| AR104241A1 (es) | 2015-04-29 | 2017-07-05 | Lilly Co Eli | Derivados de tetrahidrofuro tiazina como inhibidores de bace1 selectivos |
| MX377277B (es) | 2015-09-04 | 2025-03-07 | Hoffmann La Roche | Derivados de fenoximetilo. |
| AU2016328535A1 (en) | 2015-09-24 | 2017-11-09 | F. Hoffmann-La Roche Ag | Bicyclic compounds as ATX inhibitors |
| CA2991615A1 (en) | 2015-09-24 | 2017-03-30 | F. Hoffmann-La Roche Ag | Bicyclic compounds as atx inhibitors |
| EP3353178B1 (en) | 2015-09-24 | 2021-07-14 | F. Hoffmann-La Roche AG | Bicyclic compounds as dual atx/ca inhibitors |
| AU2016328365B2 (en) | 2015-09-24 | 2020-04-23 | F. Hoffmann-La Roche Ag | New bicyclic compounds as dual ATX/CA inhibitors |
| TW201740954A (zh) | 2016-03-16 | 2017-12-01 | 美國禮來大藥廠 | 組合療法 |
| TWI798751B (zh) | 2016-07-01 | 2023-04-11 | 美商美國禮來大藥廠 | 抗－N3pGlu類澱粉β肽抗體及其用途 |
| MX387729B (es) | 2016-12-15 | 2025-03-18 | Amgen Inc | Derivados de dióxido de 1,4-tiazina y dióxido 1,2,4-tiadiazina como inhibidores de beta-secretasa y métodos de uso. |
| ES2910367T3 (es) | 2016-12-15 | 2022-05-12 | Amgen Inc | Derivados de tiazina y oxazina bicíclicos como inhibidores de beta-secretasa y métodos de uso |
| US10889579B2 (en) | 2016-12-15 | 2021-01-12 | Amgen Inc. | Thiazine derivatives as β-secretase inhibitors and methods of use |
| AU2017378316B2 (en) | 2016-12-15 | 2021-04-01 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| AU2017376441B2 (en) | 2016-12-15 | 2021-10-14 | Amgen Inc. | Oxazine derivatives as beta-secretase inhibitors and methods of use |
| BR112019019017A2 (pt) | 2017-03-16 | 2020-04-14 | Hoffmann La Roche | compostos heterocíclicos de utilidade como inibidores duplos de atx/ca |
| JP7090099B2 (ja) | 2017-03-16 | 2022-06-23 | エフ．ホフマン－ラ ロシュ アーゲー | Ａｔｘインヒビターとしての新規二環式化合物 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5284957A (en) * | 1992-09-03 | 1994-02-08 | Eli Lilly And Company | Excitatory amino acid receptor antagonists |
| AU2003219955A1 (en) * | 2002-03-22 | 2003-10-13 | Eli Lilly And Company | Isoquinoline-3-carboxylic acid derivatives as excitatory amino acid receptor antagonists |
| AR054617A1 (es) | 2005-06-14 | 2007-07-04 | Schering Corp | Derivados de pirrol[3, 4 - d]pirimidina como inhibidores de aspartil proteasas y composiciones farmacéuticas que los comprenden |
| CN103936690B (zh) | 2005-10-25 | 2016-06-08 | 盐野义制药株式会社 | 氨基二氢噻嗪衍生物 |
| WO2008133273A1 (ja) | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | アルツハイマー症治療用医薬組成物 |
| BRPI0906962B8 (pt) * | 2008-01-18 | 2021-05-25 | Eisai R&D Man Co Ltd | composto de aminodiidrotiazina fundido |
| AR072952A1 (es) | 2008-04-22 | 2010-10-06 | Schering Corp | Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso |
| TWI431004B (zh) * | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Ｂａｃｅ抑制劑 |
| ES2738123T3 (es) | 2008-06-13 | 2020-01-20 | Shionogi & Co | Derivado heterocíclico que contiene azufre que tiene actividad inhibitoria de ß-secretasa |
| US20110207723A1 (en) | 2008-09-30 | 2011-08-25 | Eisai R&D Management Co., Ltd. | Novel fused aminodihydrothiazine derivative |
| 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 |
| 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 |
| GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine 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 |
| EP2694521B1 (en) | 2011-04-07 | 2015-11-25 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| WO2012162334A1 (en) | 2011-05-24 | 2012-11-29 | Bristol-Myers Squibb Company | Compounds for the reduction of beta-amyloid production |
| JO3143B1 (ar) * | 2012-04-03 | 2017-09-20 | Lilly Co Eli | مركبات تتراهيدرو بيرولو ثيازين |
-
2014
- 2014-02-26 TW TW103106569A patent/TWI593692B/zh not_active IP Right Cessation
- 2014-02-27 AR ARP140100629A patent/AR094918A1/es unknown
- 2014-02-27 JO JOP/2014/0061A patent/JO3317B1/ar active
- 2014-03-04 ME MEP-2017-252A patent/ME02910B/me unknown
- 2014-03-04 KR KR1020157024588A patent/KR101688761B1/ko not_active Expired - Fee Related
- 2014-03-04 PL PL14712875T patent/PL2970336T3/pl unknown
- 2014-03-04 LT LTEP14712875.5T patent/LT2970336T/lt unknown
- 2014-03-04 AP AP2015008713A patent/AP2015008713A0/xx unknown
- 2014-03-04 HR HRP20171851TT patent/HRP20171851T1/hr unknown
- 2014-03-04 JP JP2016500566A patent/JP6095844B2/ja active Active
- 2014-03-04 DK DK14712875.5T patent/DK2970336T3/da active
- 2014-03-04 EP EP14712875.5A patent/EP2970336B1/en active Active
- 2014-03-04 BR BR112015018738A patent/BR112015018738A8/pt not_active Application Discontinuation
- 2014-03-04 ES ES14712875.5T patent/ES2653421T3/es active Active
- 2014-03-04 CA CA2898500A patent/CA2898500C/en not_active Expired - Fee Related
- 2014-03-04 PE PE2015001901A patent/PE20151542A1/es active IP Right Grant
- 2014-03-04 MX MX2015012628A patent/MX2015012628A/es unknown
- 2014-03-04 SI SI201430430T patent/SI2970336T1/sl unknown
- 2014-03-04 EA EA201591491A patent/EA026006B1/ru not_active IP Right Cessation
- 2014-03-04 NZ NZ71220714A patent/NZ712207A/en not_active IP Right Cessation
- 2014-03-04 MA MA38390A patent/MA38390B1/fr unknown
- 2014-03-04 WO PCT/US2014/020070 patent/WO2014143579A1/en not_active Ceased
- 2014-03-04 CN CN201480014295.6A patent/CN105026404B/zh active Active
- 2014-03-04 HU HUE14712875A patent/HUE037487T2/hu unknown
- 2014-03-04 PT PT147128755T patent/PT2970336T/pt unknown
- 2014-03-04 RS RS20171243A patent/RS56645B1/sr unknown
- 2014-03-04 SG SG11201507499XA patent/SG11201507499XA/en unknown
- 2014-03-04 MY MYPI2015703056A patent/MY180083A/en unknown
- 2014-03-04 US US14/195,897 patent/US8841293B1/en active Active
- 2014-04-03 UA UAA201508698A patent/UA112941C2/uk unknown
- 2014-08-07 US US14/453,855 patent/US8987254B2/en active Active
- 2014-08-12 NO NO14799063A patent/NO3039297T3/no unknown
-
2015
- 2015-02-19 US US14/626,320 patent/US20150157641A1/en not_active Abandoned
- 2015-08-10 TN TN2015000340A patent/TN2015000340A1/en unknown
- 2015-08-14 CR CR20150418A patent/CR20150418A/es unknown
- 2015-08-27 IL IL240903A patent/IL240903B/en not_active IP Right Cessation
- 2015-09-09 CL CL2015002529A patent/CL2015002529A1/es unknown
- 2015-09-10 PH PH12015502031A patent/PH12015502031A1/en unknown
-
2017
- 2017-11-09 CY CY20171101177T patent/CY1119585T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |