BR112017009583A2 - 2-amino-6-(difluorometil)-5,5-difluoro-6-fenil-3,4,5,6-tetraidropiridinas como inibidoras da bace1 - Google Patents
2-amino-6-(difluorometil)-5,5-difluoro-6-fenil-3,4,5,6-tetraidropiridinas como inibidoras da bace1Info
- Publication number
- BR112017009583A2 BR112017009583A2 BR112017009583A BR112017009583A BR112017009583A2 BR 112017009583 A2 BR112017009583 A2 BR 112017009583A2 BR 112017009583 A BR112017009583 A BR 112017009583A BR 112017009583 A BR112017009583 A BR 112017009583A BR 112017009583 A2 BR112017009583 A2 BR 112017009583A2
- Authority
- BR
- Brazil
- Prior art keywords
- tetrahydropyridines
- difluoromethyl
- difluoro
- phenyl
- amino
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D417/12—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 linked by a chain containing hetero atoms as chain links
Abstract
a presente invenção se refere a compostos da fórmula (i) os quais são inibidores da enzima bace1. aspectos separados da invenção se referem a composições farmacêuticas compreendendo os referidos compostos e a usos dos compostos no tratamento de transtornos para os quais a redução de depósitos de aß seja benéfica, tal como a doença de alzheimer.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA201400648 | 2014-11-10 | ||
| DKPA201500447 | 2015-08-07 | ||
| PCT/EP2015/076015 WO2016075063A1 (en) | 2014-11-10 | 2015-11-09 | 2-amino-6-(difluoromethyl)- 5,5-difluoro-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112017009583A2 true BR112017009583A2 (pt) | 2017-12-26 |
Family
ID=54783558
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112017009583A BR112017009583A2 (pt) | 2014-11-10 | 2015-11-09 | 2-amino-6-(difluorometil)-5,5-difluoro-6-fenil-3,4,5,6-tetraidropiridinas como inibidoras da bace1 |
Country Status (43)
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CR20170187A (es) | 2014-11-10 | 2018-02-01 | H Lundbeck As | 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer |
| JO3458B1 (ar) | 2014-11-10 | 2020-07-05 | H Lundbeck As | 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1 |
| MA40941A (fr) | 2014-11-10 | 2017-09-19 | H Lundbeck As | 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1 |
| JO3627B1 (ar) | 2015-04-30 | 2020-08-27 | H Lundbeck As | إيميدازو بيرازينونات على هيئة مثبطات pde1 |
| TW201717948A (zh) | 2015-08-10 | 2017-06-01 | Ｈ 朗德貝克公司 | 包括給予２－胺基－３，５，５－三氟－３，４，５，６－四氫吡啶的聯合治療 |
| MX2018001699A (es) * | 2015-08-12 | 2018-05-07 | H Lundbeck As | 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidr opiridinas como inhibidores de bace1. |
| US10034861B2 (en) | 2016-07-04 | 2018-07-31 | H. Lundbeck A/S | 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors |
| JOP20190081A1 (ar) | 2016-10-13 | 2019-04-11 | Novartis Ag | مشتق أوكسازين للاستخدام في علاج أو الوقاية من اعتلال وعائي دماغي نشواني |
| CN109803653A (zh) | 2016-10-28 | 2019-05-24 | H.隆德贝克有限公司 | 包括给予咪唑并吡嗪酮的组合治疗 |
| DK3532064T3 (da) | 2016-10-28 | 2020-08-24 | H Lundbeck As | Kombinationsbehandlinger omfattende imidazopyrazinoner til behandlingen af psykiatriske og/eller kognitive lidelser |
| TW201829394A (zh) | 2016-12-21 | 2018-08-16 | 丹麥商Ｈ 朗德貝克公司 | 作為ｂａｃｅ１抑制劑之６-胺基-５-氟-５-（氟甲基）-２，３，４，５-四氫吡啶-２-基-苯基-５-（甲氧基-ｄ）-吡-２-甲醯胺及其氟化衍生物 |
| SI3723807T1 (sl) | 2017-12-14 | 2022-01-31 | H. Lundbeck A/S | Kombinirana zdravljenja, ki obsegajo dajanje 1H-pirazolo(4,3-b)piridinov |
| AR113926A1 (es) | 2017-12-14 | 2020-07-01 | H Lundbeck As | Derivados de 1h-pirazolo[4,3-b]piridinas |
| CN117447475A (zh) | 2017-12-20 | 2024-01-26 | H.隆德贝克有限公司 | 作为PDE1抑制剂的吡唑并[4,3-b]吡啶和咪唑并[1,5-a]嘧啶 |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002100399A1 (en) | 2001-06-12 | 2002-12-19 | Elan Pharmaceuticals, Inc. | Macrocycles useful in the treatment of alzheimer's disease |
| GB0124928D0 (en) | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| EP2258687B1 (en) | 2002-02-12 | 2012-12-26 | Glaxosmithkline LLC | Nicotinamide derivates useful as P38 inhibitors |
| 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 |
| DK2580200T3 (en) | 2010-06-09 | 2017-01-09 | Janssen Pharmaceutica Nv | 5,6-dihydro-2H- [1,4] oxazin-3-YLAMINDERIVATER THAT COULD BE USED AS INHIBITORS OF BETA-secretase (BACE) |
| CN103429589A (zh) | 2011-01-12 | 2013-12-04 | 诺瓦提斯公司 | 噁嗪衍生物及其在治疗神经障碍中的用途 |
| PL2663561T3 (pl) | 2011-01-13 | 2016-10-31 | Nowe pochodne heterocykliczne i ich zastosowanie w leczeniu zaburzeń neurologicznych | |
| US8754075B2 (en) | 2011-04-11 | 2014-06-17 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE1 and/or BACE2 inhibitors |
| TW201247635A (en) | 2011-04-26 | 2012-12-01 | Shionogi & Co | Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them |
| BR112013031098A2 (pt) * | 2011-06-07 | 2016-12-06 | Hoffmann La Roche | halogeno-alquil-1,3 oxazinas como inibidores de bace1 e/ou bace2 |
| UY34278A (es) | 2011-08-25 | 2013-04-05 | Novartis Ag | Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades |
| US8338413B1 (en) | 2012-03-07 | 2012-12-25 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| CA2867851A1 (en) | 2012-03-20 | 2013-09-26 | Elan Pharmaceuticals, Inc. | Spirocyclic dihydro-thiazine and dihydro-oxazine bace inhibitors, and compositions and uses thereof |
| WO2014056816A1 (en) | 2012-10-10 | 2014-04-17 | F. Hoffmann-La Roche Ag | COMBINATION OF AN Aβ ANTIBODY AND A BACE INHIBITOR |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| AU2014223334C1 (en) | 2013-03-01 | 2018-10-18 | Amgen Inc. | Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| TWI639607B (zh) | 2013-06-18 | 2018-11-01 | 美國禮來大藥廠 | Ｂａｃｅ抑制劑 |
| EP3107897A1 (en) | 2014-02-19 | 2016-12-28 | H. Lundbeck A/S | 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease |
| TW201623295A (zh) | 2014-04-11 | 2016-07-01 | 塩野義製藥股份有限公司 | 具有ｂａｃｅ１抑制活性之二氫噻及二氫衍生物 |
| MA40941A (fr) | 2014-11-10 | 2017-09-19 | H Lundbeck As | 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1 |
| CR20170187A (es) | 2014-11-10 | 2018-02-01 | H Lundbeck As | 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer |
| JO3458B1 (ar) | 2014-11-10 | 2020-07-05 | H Lundbeck As | 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1 |
| TW201717948A (zh) | 2015-08-10 | 2017-06-01 | Ｈ 朗德貝克公司 | 包括給予２－胺基－３，５，５－三氟－３，４，５，６－四氫吡啶的聯合治療 |
| MX2018001699A (es) | 2015-08-12 | 2018-05-07 | H Lundbeck As | 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidr opiridinas como inhibidores de bace1. |
| TW201829394A (zh) | 2016-12-21 | 2018-08-16 | 丹麥商Ｈ 朗德貝克公司 | 作為ｂａｃｅ１抑制劑之６-胺基-５-氟-５-（氟甲基）-２，３，４，５-四氫吡啶-２-基-苯基-５-（甲氧基-ｄ）-吡-２-甲醯胺及其氟化衍生物 |
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2015
- 2015-10-25 JO JOP/2015/0260A patent/JO3458B1/ar active
- 2015-11-05 US US14/933,301 patent/US9346797B1/en active Active
- 2015-11-09 UA UAA201704639A patent/UA119576C2/uk unknown
- 2015-11-09 EA EA201790818A patent/EA032339B1/ru not_active IP Right Cessation
- 2015-11-09 TW TW104136839A patent/TWI690318B/zh not_active IP Right Cessation
- 2015-11-09 SI SI201530464T patent/SI3218365T1/sl unknown
- 2015-11-09 SG SG11201703547XA patent/SG11201703547XA/en unknown
- 2015-11-09 CR CR20170186A patent/CR20170186A/es unknown
- 2015-11-09 EP EP18198764.5A patent/EP3461483A1/en not_active Withdrawn
- 2015-11-09 PT PT15805109T patent/PT3218365T/pt unknown
- 2015-11-09 DK DK15805109.4T patent/DK3218365T3/en active
- 2015-11-09 HU HUE15805109A patent/HUE040304T2/hu unknown
- 2015-11-09 MX MX2017006049A patent/MX2017006049A/es unknown
- 2015-11-09 WO PCT/EP2015/076015 patent/WO2016075063A1/en active Application Filing
- 2015-11-09 GE GEAP201514485A patent/GEP20196949B/en unknown
- 2015-11-09 ES ES15805109.4T patent/ES2694860T3/es active Active
- 2015-11-09 JP JP2017525010A patent/JP6629320B2/ja not_active Expired - Fee Related
- 2015-11-09 PL PL15805109T patent/PL3218365T3/pl unknown
- 2015-11-09 RU RU2017116196A patent/RU2017116196A/ru not_active Application Discontinuation
- 2015-11-09 BR BR112017009583A patent/BR112017009583A2/pt not_active Application Discontinuation
- 2015-11-09 PE PE2017000825A patent/PE20170946A1/es unknown
- 2015-11-09 US US15/524,546 patent/US10045974B2/en not_active Expired - Fee Related
- 2015-11-09 ME MEP-2018-267A patent/ME03723B/me unknown
- 2015-11-09 KR KR1020177012442A patent/KR20170081184A/ko unknown
- 2015-11-09 TN TN2017000144A patent/TN2017000144A1/en unknown
- 2015-11-09 CN CN201580060803.9A patent/CN107074836B/zh not_active Expired - Fee Related
- 2015-11-09 EP EP15805109.4A patent/EP3218365B1/en active Active
- 2015-11-09 AU AU2015345258A patent/AU2015345258B2/en not_active Expired - Fee Related
- 2015-11-09 TR TR2018/16427T patent/TR201816427T4/tr unknown
- 2015-11-09 LT LTEP15805109.4T patent/LT3218365T/lt unknown
- 2015-11-09 MA MA40955A patent/MA40955B1/fr unknown
- 2015-11-09 CA CA2965563A patent/CA2965563A1/en not_active Abandoned
- 2015-11-09 RS RS20181321A patent/RS57946B1/sr unknown
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2017
- 2017-04-20 ZA ZA2017/02797A patent/ZA201702797B/en unknown
- 2017-05-03 IL IL252089A patent/IL252089B/en not_active IP Right Cessation
- 2017-05-03 CO CONC2017/0004465A patent/CO2017004465A2/es unknown
- 2017-05-04 CL CL2017001112A patent/CL2017001112A1/es unknown
- 2017-05-05 PH PH12017500841A patent/PH12017500841A1/en unknown
- 2017-05-09 SV SV2017005435A patent/SV2017005435A/es unknown
- 2017-05-09 DO DO2017000117A patent/DOP2017000117A/es unknown
- 2017-05-09 NI NI201700055A patent/NI201700055A/es unknown
- 2017-05-09 EC ECIEPI201728459A patent/ECSP17028459A/es unknown
- 2017-05-10 GT GT201700099A patent/GT201700099A/es unknown
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2018
- 2018-08-09 US US16/059,715 patent/US10603310B2/en not_active Expired - Fee Related
- 2018-10-17 HR HRP20181698TT patent/HRP20181698T1/hr unknown
- 2018-11-13 CY CY20181101200T patent/CY1120846T1/el unknown
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| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] |
Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS. |
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| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] | ||
| B06U | Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette] | ||
| B11B | Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements |