AR099489A1 - 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer - Google Patents
2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimerInfo
- Publication number
- AR099489A1 AR099489A1 ARP150100475A ARP150100475A AR099489A1 AR 099489 A1 AR099489 A1 AR 099489A1 AR P150100475 A ARP150100475 A AR P150100475A AR P150100475 A ARP150100475 A AR P150100475A AR 099489 A1 AR099489 A1 AR 099489A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- fluoroalkyl
- alzheimer
- disease
- tetrahydropiridins
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
-
- 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
-
- 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
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D227/00—Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00
- C07D227/02—Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00 with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D227/06—Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00 with only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D227/10—Nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero 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
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
La presente solicitud se dirige a inhibidores de la enzima BACE1 (b-secretasa 1, proteína amiloide b sitio de escisión de enzima precursor 1), composiciones farmacéuticas que comprenden dichos compuestos y usos de los compuestos para tratar trastornos para los cuales la reducción de depósitos de b-amiloides es beneficiosa, tal como la enfermedad de Alzheimer. Reivindicación 1: Un compuesto de fórmula (1), Ar se selecciona del grupo que consiste en fenilo, piridilo, pirimidilo, pirazinilo, imidazolilo, pirazolilo, 1,2,4-triazolilo, tiofenilo, tiazolilo, oxazolilo, isoxazolilo, 1,3,4-tiadiazolilo, isotiazolilo, 1,3,4-oxadiazolilo, 1,2,4-oxadiazolilo, furazanilo y 1,2,4-tiadiazolilo y en donde el Ar está opcionalmente sustituido con uno o más de entre halógeno, CN, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, fluoroalquilo C₁₋₆ o alcoxi C₁₋₆; R¹ es alquilo C₁₋₃ o fluoroalquilo C₁₋₃; R² es hidrógeno, halógeno, fluoroalquilo C₁₋₃ o alquilo C₁₋₃; R³ es alquilo C₁₋₃; o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DKPA201400086 | 2014-02-19 | ||
DKPA201400349 | 2014-07-01 | ||
PCT/EP2015/053327 WO2015124576A1 (en) | 2014-02-19 | 2015-02-17 | 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease |
Publications (1)
Publication Number | Publication Date |
---|---|
AR099489A1 true AR099489A1 (es) | 2016-07-27 |
Family
ID=59009438
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP150100475A AR099489A1 (es) | 2014-02-19 | 2015-02-18 | 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer |
Country Status (25)
Country | Link |
---|---|
US (2) | US20170066741A1 (es) |
EP (1) | EP3107897A1 (es) |
JP (1) | JP6483146B2 (es) |
KR (1) | KR20160115936A (es) |
CN (1) | CN106029639B (es) |
AP (1) | AP2016009370A0 (es) |
AR (1) | AR099489A1 (es) |
AU (1) | AU2015220873A1 (es) |
CA (1) | CA2940028A1 (es) |
CL (1) | CL2016002072A1 (es) |
CR (1) | CR20160352A (es) |
DO (1) | DOP2016000194A (es) |
EA (1) | EA031132B1 (es) |
EC (1) | ECSP16072941A (es) |
GE (1) | GEP20186892B (es) |
IL (1) | IL246875A0 (es) |
MA (1) | MA39225A1 (es) |
MX (1) | MX2016010777A (es) |
PE (1) | PE20161225A1 (es) |
PH (1) | PH12016501600A1 (es) |
RU (1) | RU2016133626A (es) |
SG (1) | SG11201606812WA (es) |
TW (1) | TW201609700A (es) |
UA (1) | UA117695C2 (es) |
WO (1) | WO2015124576A1 (es) |
Families Citing this family (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
UA117695C2 (uk) | 2014-02-19 | 2018-09-10 | Х. Луннбек А/С | 2-аміно-3,5,5-трифтор-3,4,5,6-тетрагідропіридини як інгібітори bace1 для лікування хвороби альцгеймера |
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 |
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 |
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 |
EP3334720A1 (en) * | 2015-08-12 | 2018-06-20 | H. Lundbeck A/S | 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridins as bace1 inhibitors |
EP3347486A4 (en) | 2015-09-09 | 2019-06-19 | The Trustees of Columbia University in the City of New York | REDUCTION OF ER-MAM-LOCALIZED APP-C99 AND METHOD FOR THE TREATMENT OF ALZHEIMER DISEASE |
TW201726651A (zh) * | 2015-09-23 | 2017-08-01 | 健生藥品公司 | 2,3,4,5-四氫吡啶-6-胺衍生物 |
US10034861B2 (en) | 2016-07-04 | 2018-07-31 | H. Lundbeck A/S | 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors |
MA46621A (fr) | 2016-10-28 | 2021-06-02 | H Lundbeck As | Traitements combinés comprenant l'administration d'imidazopyrazinones |
PL3532064T3 (pl) | 2016-10-28 | 2020-11-16 | H. Lundbeck A/S | Terapie skojarzone obejmujące imidazopirazynony do leczenia zaburzeń psychiatrycznych i/lub poznawczych |
BR112018017058A2 (pt) | 2016-12-21 | 2019-07-02 | H Lundbeck As | 6-amino-5-fluoro-5-(fluorometil)-2,3,4,5-tetra-hidropiridin-2-il-fenil-5-(metóxi-d3)-pirazina-2-carboxamidas e derivados fluorados do mesmo como inibidores de bace1 |
LT3691620T (lt) | 2017-10-05 | 2022-09-26 | Fulcrum Therapeutics, Inc. | P38 kinazės inhibitoriai, sumažinantys dux4 ir pasrovinių genų raišką, skirti fshd gydymui |
US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
US11634416B2 (en) | 2017-12-14 | 2023-04-25 | H. Lundbeck A/S | Combination treatments comprising administration of 1H-pyrazolo[4,3-b]pyridines |
AR113926A1 (es) | 2017-12-14 | 2020-07-01 | H Lundbeck As | Derivados de 1h-pirazolo[4,3-b]piridinas |
CN111511742B (zh) | 2017-12-20 | 2023-10-27 | 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 |
KR102507861B1 (ko) | 2018-04-19 | 2023-03-09 | 삼성에스디에스 주식회사 | 부채널 공격에 안전한 연산 장치 및 방법 |
KR102510077B1 (ko) | 2018-04-24 | 2023-03-14 | 삼성에스디에스 주식회사 | 부채널 공격에 안전한 연산 장치 및 방법 |
Family Cites Families (19)
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EP1395257A1 (en) * | 2001-06-12 | 2004-03-10 | 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 |
MXPA04007838A (es) * | 2002-02-12 | 2004-10-15 | Smithkline Beecham Corp | Derivados de nicotamida utiles como inhibidores p38. |
TWI431004B (zh) * | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
KR101730937B1 (ko) | 2010-06-09 | 2017-04-27 | 얀센 파마슈티카 엔.브이. | 베타-세크레타아제(bace) 저해제로 유용한 5,6-디하이드로-2h-[1,4]옥사진-3-일-아민 유도체 |
US8927721B2 (en) * | 2010-10-29 | 2015-01-06 | Shionogi & Co., Ltd. | Naphthyridine derivative |
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 |
CA2824220C (en) | 2011-01-13 | 2020-09-01 | Novartis Ag | Novel heterocyclic derivatives and their use in the treatment of neurological disorders |
US8754075B2 (en) * | 2011-04-11 | 2014-06-17 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE1 and/or BACE2 inhibitors |
WO2012147763A1 (ja) * | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | オキサジン誘導体およびそれを含有するbace1阻害剤 |
WO2012168164A1 (en) * | 2011-06-07 | 2012-12-13 | F. Hoffmann-La Roche Ag | Halogen-alkyl-1,3 oxazines as bace1 and/or bace2 inhibitors |
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 |
JP2015514073A (ja) | 2012-03-20 | 2015-05-18 | エラン ファーマシューティカルズ, リミテッド・ライアビリティ・カンパニー | スピロ環式ジヒドロ−チアジンおよびジヒドロ−オキサジンbace阻害剤、ならびにその組成物および使用 |
WO2014056816A1 (en) | 2012-10-10 | 2014-04-17 | F. Hoffmann-La Roche Ag | COMBINATION OF AN Aβ ANTIBODY AND A BACE INHIBITOR |
WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
WO2014134341A1 (en) | 2013-03-01 | 2014-09-04 | Amgen Inc. | Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
UA117695C2 (uk) | 2014-02-19 | 2018-09-10 | Х. Луннбек А/С | 2-аміно-3,5,5-трифтор-3,4,5,6-тетрагідропіридини як інгібітори bace1 для лікування хвороби альцгеймера |
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 |
-
2015
- 2015-02-17 UA UAA201608414A patent/UA117695C2/uk unknown
- 2015-02-17 EP EP15707304.0A patent/EP3107897A1/en not_active Withdrawn
- 2015-02-17 CA CA2940028A patent/CA2940028A1/en not_active Abandoned
- 2015-02-17 KR KR1020167021930A patent/KR20160115936A/ko unknown
- 2015-02-17 US US15/119,639 patent/US20170066741A1/en not_active Abandoned
- 2015-02-17 WO PCT/EP2015/053327 patent/WO2015124576A1/en active Application Filing
- 2015-02-17 JP JP2016551851A patent/JP6483146B2/ja not_active Expired - Fee Related
- 2015-02-17 EA EA201691447A patent/EA031132B1/ru not_active IP Right Cessation
- 2015-02-17 GE GEAP201514248A patent/GEP20186892B/en unknown
- 2015-02-17 MX MX2016010777A patent/MX2016010777A/es unknown
- 2015-02-17 CN CN201580009034.XA patent/CN106029639B/zh not_active Expired - Fee Related
- 2015-02-17 AP AP2016009370A patent/AP2016009370A0/en unknown
- 2015-02-17 PE PE2016001299A patent/PE20161225A1/es not_active Application Discontinuation
- 2015-02-17 MA MA39225A patent/MA39225A1/fr unknown
- 2015-02-17 RU RU2016133626A patent/RU2016133626A/ru not_active Application Discontinuation
- 2015-02-17 SG SG11201606812WA patent/SG11201606812WA/en unknown
- 2015-02-17 CR CR20160352A patent/CR20160352A/es unknown
- 2015-02-17 AU AU2015220873A patent/AU2015220873A1/en not_active Abandoned
- 2015-02-17 TW TW104105281A patent/TW201609700A/zh unknown
- 2015-02-18 AR ARP150100475A patent/AR099489A1/es unknown
- 2015-02-19 US US14/625,658 patent/US9353084B2/en not_active Expired - Fee Related
-
2016
- 2016-07-21 IL IL246875A patent/IL246875A0/en unknown
- 2016-07-28 DO DO2016000194A patent/DOP2016000194A/es unknown
- 2016-08-11 PH PH12016501600A patent/PH12016501600A1/en unknown
- 2016-08-17 CL CL2016002072A patent/CL2016002072A1/es unknown
- 2016-09-09 EC ECIEPI201672941A patent/ECSP16072941A/es unknown
Also Published As
Publication number | Publication date |
---|---|
RU2016133626A (ru) | 2018-03-20 |
JP2017506237A (ja) | 2017-03-02 |
AU2015220873A1 (en) | 2016-08-11 |
JP6483146B2 (ja) | 2019-03-13 |
CR20160352A (es) | 2016-10-20 |
SG11201606812WA (en) | 2016-09-29 |
EA201691447A1 (ru) | 2016-12-30 |
UA117695C2 (uk) | 2018-09-10 |
AP2016009370A0 (en) | 2016-08-31 |
WO2015124576A1 (en) | 2015-08-27 |
CA2940028A1 (en) | 2015-08-27 |
CN106029639B (zh) | 2019-01-08 |
EA031132B1 (ru) | 2018-11-30 |
CL2016002072A1 (es) | 2017-01-20 |
TW201609700A (zh) | 2016-03-16 |
US20170066741A1 (en) | 2017-03-09 |
PH12016501600A1 (en) | 2017-02-06 |
DOP2016000194A (es) | 2016-09-30 |
PE20161225A1 (es) | 2016-12-04 |
US20150232449A1 (en) | 2015-08-20 |
RU2016133626A3 (es) | 2018-09-25 |
MA39225A1 (fr) | 2017-04-28 |
KR20160115936A (ko) | 2016-10-06 |
MX2016010777A (es) | 2016-10-26 |
ECSP16072941A (es) | 2017-02-24 |
IL246875A0 (en) | 2016-08-31 |
CN106029639A (zh) | 2016-10-12 |
US9353084B2 (en) | 2016-05-31 |
GEP20186892B (en) | 2018-09-10 |
EP3107897A1 (en) | 2016-12-28 |
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