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
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 (38)
| 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) |
| HK (1) | HK1212694A1 (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 |
|---|---|---|---|---|
| WO2013186159A1 (en) | 2012-06-13 | 2013-12-19 | F. Hoffmann-La Roche Ag | New diazaspirocycloalkane and azaspirocycloalkane |
| IN2015DN00960A (es) | 2012-09-25 | 2015-06-12 | Hoffmann La Roche | |
| JP6243921B2 (ja) | 2012-10-26 | 2017-12-06 | イーライ リリー アンド カンパニー | Ｂａｃｅ阻害剤 |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| UA118201C2 (uk) | 2013-11-26 | 2018-12-10 | Ф. Хоффманн-Ля Рош Аг | НОВИЙ ОКТАГІДРОЦИКЛОБУТА[1,2-c;3,4-c']ДИПІРОЛ-2-ІЛ |
| TWI684452B (zh) | 2014-03-14 | 2020-02-11 | 美國禮來大藥廠 | 胺基噻嗪化合物 |
| EA032357B1 (ru) | 2014-03-26 | 2019-05-31 | Ф. Хоффманн-Ля Рош Аг | Конденсированные [1,4]диазепиновые соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa) |
| RS59477B1 (sr) | 2014-03-26 | 2019-12-31 | Hoffmann La Roche | Biciklička jedinjenja kao inhibitori proizvodnje autotaksina (atx) i lizofosfatidne kiseline (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 |
| AR103406A1 (es) * | 2015-01-30 | 2017-05-10 | Lilly Co Eli | Sal de tosilato |
| 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 |
| CR20180058A (es) | 2015-09-04 | 2018-02-26 | Hoffmann La Roche | Nuevos derivados de fenoximetilo |
| PE20180233A1 (es) | 2015-09-24 | 2018-01-31 | Hoffmann La Roche | Nuevos compuestos biciclicos como inhibidores duales de atx / ca |
| PE20180451A1 (es) | 2015-09-24 | 2018-03-05 | Hoffmann La Roche | Nuevos compuestos biciclicos como inhibidores de atx |
| PE20180461A1 (es) | 2015-09-24 | 2018-03-06 | Hoffmann La Roche | Nuevos compuestos biciclicos como inhibidores de la atx |
| WO2017050791A1 (en) | 2015-09-24 | 2017-03-30 | 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 |
| TWI735600B (zh) | 2016-07-01 | 2021-08-11 | 美商美國禮來大藥廠 | 抗－N3pGlu類澱粉β肽抗體及其用途 |
| WO2018112081A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Oxazine derivatives as beta-secretase inhibitors and methods of use |
| EP3555085B1 (en) | 2016-12-15 | 2020-12-02 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| AU2017376445B2 (en) * | 2016-12-15 | 2021-09-30 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
| JP7149272B2 (ja) | 2016-12-15 | 2022-10-06 | アムジエン・インコーポレーテツド | β－セクレターゼ阻害剤としてのチアジン誘導体および使用方法 |
| MA50007A (fr) | 2016-12-15 | 2021-04-07 | Amgen Inc | Dérivés de dioxyde de 1,4-thiazine et de dioxyde de 1,2,4-thiadiazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation |
| CN110382484B (zh) | 2017-03-16 | 2022-12-06 | 豪夫迈·罗氏有限公司 | 新的作为atx抑制剂的二环化合物 |
| BR112019019017A2 (pt) | 2017-03-16 | 2020-04-14 | Hoffmann La Roche | compostos heterocíclicos de utilidade como inibidores duplos de atx/ca |
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 |
| WO2006138264A2 (en) * | 2005-06-14 | 2006-12-28 | Schering Corporation | Aspartyl protease inhibitors |
| US8173642B2 (en) | 2005-10-25 | 2012-05-08 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives |
| 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 |
| RS54311B1 (en) * | 2008-01-18 | 2016-02-29 | Eisai R&D Management Co. Ltd. | KONDEZOVANI AMINODIHYDROTIAZINE DERIVATIVE |
| AU2009239536C1 (en) * | 2008-04-22 | 2012-12-13 | Merck Sharp & Dohme Corp. | Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use |
| 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 |
| CA2738150A1 (en) | 2008-09-30 | 2010-04-08 | 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 |
| EP2511269A4 (en) | 2009-12-11 | 2013-04-24 | Shionogi & Co | FUSED HETEROCYCLIC COMPOUND HAVING AN AMINO GROUP |
| GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| US9145426B2 (en) | 2011-04-07 | 2015-09-29 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
| US8598161B2 (en) | 2011-05-24 | 2013-12-03 | 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 EP EP14712875.5A patent/EP2970336B1/en active Active
- 2014-03-04 SI SI201430430T patent/SI2970336T1/sl unknown
- 2014-03-04 BR BR112015018738A patent/BR112015018738A8/pt not_active Application Discontinuation
- 2014-03-04 CA CA2898500A patent/CA2898500C/en not_active Expired - Fee Related
- 2014-03-04 RS RS20171243A patent/RS56645B1/sr unknown
- 2014-03-04 PT PT147128755T patent/PT2970336T/pt unknown
- 2014-03-04 LT LTEP14712875.5T patent/LT2970336T/lt unknown
- 2014-03-04 PE PE2015001901A patent/PE20151542A1/es active IP Right Grant
- 2014-03-04 SG SG11201507499XA patent/SG11201507499XA/en unknown
- 2014-03-04 MY MYPI2015703056A patent/MY180083A/en unknown
- 2014-03-04 MA MA38390A patent/MA38390B1/fr unknown
- 2014-03-04 MX MX2015012628A patent/MX2015012628A/es unknown
- 2014-03-04 HU HUE14712875A patent/HUE037487T2/hu unknown
- 2014-03-04 ME MEP-2017-252A patent/ME02910B/me unknown
- 2014-03-04 US US14/195,897 patent/US8841293B1/en active Active
- 2014-03-04 CN CN201480014295.6A patent/CN105026404B/zh active Active
- 2014-03-04 KR KR1020157024588A patent/KR101688761B1/ko active IP Right Grant
- 2014-03-04 JP JP2016500566A patent/JP6095844B2/ja active Active
- 2014-03-04 EA EA201591491A patent/EA026006B1/ru not_active IP Right Cessation
- 2014-03-04 PL PL14712875T patent/PL2970336T3/pl unknown
- 2014-03-04 ES ES14712875.5T patent/ES2653421T3/es active Active
- 2014-03-04 NZ NZ71220714A patent/NZ712207A/en not_active IP Right Cessation
- 2014-03-04 AP AP2015008713A patent/AP2015008713A0/xx unknown
- 2014-03-04 WO PCT/US2014/020070 patent/WO2014143579A1/en active Application Filing
- 2014-03-04 DK DK14712875.5T patent/DK2970336T3/da 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
-
2016
- 2016-01-21 HK HK16100629.1A patent/HK1212694A1/zh not_active IP Right Cessation
-
2017
- 2017-11-09 CY CY20171101177T patent/CY1119585T1/el unknown
- 2017-11-28 HR HRP20171851TT patent/HRP20171851T1/hr unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |