AR084849A1 - Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos - Google Patents
Derivados de oxazina y su uso en el tratamiento de trastornos neurologicosInfo
- Publication number
- AR084849A1 AR084849A1 ARP120100120A ARP120100120A AR084849A1 AR 084849 A1 AR084849 A1 AR 084849A1 AR P120100120 A ARP120100120 A AR P120100120A AR P120100120 A ARP120100120 A AR P120100120A AR 084849 A1 AR084849 A1 AR 084849A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- alkylthio
- halogen
- group
- Prior art date
Links
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
- A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- 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
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- 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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- 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
- A61P3/04—Anorexiants; Antiobesity agents
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- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
Abstract
Composiciones farmacéuticas de los mismos, combinaciones de los mismos, y su uso como medicamentos, particularmente para el tratamiento de la enfermedad de Alzheimer ó la diabetes mediante la inhibición de la BACE-1 ó BACE-2.Reivindicación 1: Un compuesto de la fórmula (1), ó una sal farmacéuticamente aceptable del mismo, en la cual cualquiera, entre X1 es CR1 ó N; X3 es CR3 ó N; X4 es CR4 ó N; X5 es CR5 ó N; en donde al menos uno de X1, X3, X4 y X5 es N y no más de 2 entre X1, X3, X4 y X5 son N; o X1 es CR1 ó N; X3 es CR3, N ó S; X4 es un enlace; X5 es CR5, N ó S; en donde al menos uno de X1, X3 y X5 es N ó S, no más de 2 entre X1, X3 y X5 son N y no más de 1 entre X3 y X5 son S; R1 es hidrógeno, ciano, halógeno, alquilo C1-8, halógeno-alquilo C1-8, alcoxilo C1-8, halógeno-alcoxilo C1-8, alquiltio C1-8, halógeno-alquiltio C1-8, alcoxi C1-8-alquilo C1-8, alcoxi C1-8-alcoxilo C1-8, alcoxi C1-8-alquiltio C1-8, alquiltio C1-8-alquilo C1-8, alquiltio C1-8-alcoxilo C1-8, alquiltio C1-8-alquiltio C1-8, alquenilo C2-8, ó alquinilo C2-8; R2 es un grupo G1 arilo, heteroarilo ó heterocíclico no aromático, tal grupo G1 es opcionalmente sustituido por 1, 2, 3 ó 4 sustituyentes independientemente seleccionados a partir del grupo, que consta de ciano, amino, amino-alquilo C1-8, N-(alquil C1-4)-amino-alquilo C1-8, N,N-di-(alquil C1-4)-amino-alquilo C1-8, aminocarbonilo, tiocarbamoilo, halógeno, alquilo C1-8, halógeno-alquilo C1-8, hidroxilo, oxo, alcoxilo C1-8, halógeno-alcoxilo C1-8, alquiltio C1-8, halógeno-alquiltio C1-8, alcoxi C1-8-alquilo C1-8, cicloalquil C3-8-alcoxilo C1-8, alcoxi C1-8-alcoxilo C1-8, alcoxi C1-8-alquiltio C1-8, alquiltio C1-8-alquilo C1-8, alquiltio C1-8-alcoxilo C1-8, alquiltio C1-8-alquiltio C1-8, alquenilo C2-8, alquinilo C2-8, alquenoxilo C2-8, alquinoxilo C2-8 y un grupo G2 cicloalquilo C3-8, arilo, heteroarilo ó heterocíclico no aromático, tal grupo G2 es opcionalmente sustituido por 1, 2, 3, ó 4 sustituyentes independientemente seleccionados a partir del grupo, que consta de ciano, aminocarbonilo, halógeno, alquilo C1-8, halógeno-alquilo C1-8, hidroxilo, alcoxilo C1-8, halógeno-alcoxilo C1-8, alquiltio C1-8, halógeno-alquiltio C1-8, alcoxi C1-8-alquilo C1-8, alcoxi C1-8-alcoxilo C1-8, alcoxi C1-8-alquiltio C1-8, alquiltio C1-8-alquilo C1-8, alquiltio C1-8-alcoxilo C1-8, alquiltio C1-8-alquiltio C1-8, alquenilo C2-8 y alquinilo C2-8; R3 es hidrógeno, ciano, halógeno, alquilo C1-8, halógeno-alquilo C1-8, alcoxilo C1-8; halógeno-alcoxilo C1-8, alquiltio C1-8, halógeno-alquiltio C1-8, alcoxi C1-8-alquilo C1-8, alcoxi C1-8-alcoxilo C1-8, alcoxi C1-8-alquiltio C1-8, alquiltio C1-8-alquilo C1-8, alquiltio C1-8-alcoxilo C1-8, alquiltio C1-8-alquiltio C1-8, alquenilo C2-8, ó alquinilo C2-8; R4 es hidrógeno, ciano, halógeno, alquilo C1-8, halógeno-alquilo C1-8, alcoxilo C1-8, halógeno-alcoxilo C1-8, alquiltio C1-8, halógeno-alquiltio C1-8, alcoxi C1-8-alquilo C1-8, alcoxi C1-8-alcoxilo C1-8, alcoxi C1-8-alquiltio C1-8, alquiltio C1-8-alquilo C1-8, alquiltio C1-8-alcoxilo C1-8, alquiltio C1-8-alquiltio C1-8, alquenilo C2-8, ó alquinilo C2-8; R5 es hidrógeno, ciano, halógeno, alquilo C1-8, halógeno-alquilo C1-8, alcoxilo C1-8, halógeno-alcoxilo C1-8, alquiltio C1-8, halógeno-alquiltio C1-8, alcoxi C1-8-alquilo C1-8, alcoxi C1-8-alcoxilo C1-8, alcoxi C1-8-alquiltio C1-8, alquiltio C1-8-alquilo C1-8, alquiltio C1-8-alcoxilo C1-8, alquiltio C1-8-alquiltio C1-8, alquenilo C2-8, ó alquinilo C2-8; o R4 y R5, tomados juntos, son -C(H)=C(H)-C(H)=C(H)- ó un grupo alquileno C1-8, en cuyo grupo alquileno C1-8 1 ó 2 - miembros cíclicos de CH2- son opcionalmente reemplazados por miembros heterocíclicos independientemente seleccionados a partir del grupo, que consta de -N(H)-, -N[alquil C1-8]-, -O-, -S-, -S(=O)- ó -S(=O)2-; R6 es alquilo C1-8, halógeno-alquilo C1-8, hidroxi-alquilo C1-8, alcoxi C1-8-alquilo C1-8, mercapto-alquilo C1-8, alquiltio C1-8-alquilo C1-8, amino-alquilo C1-8, N-(alquil C1-4)-amino-alquilo C1-8, N,N-di(alquil C1-4)-amino-alquilo C1-8, alquenilo C2-8, ó alquinilo C2-8; o R5 y R6, tomados juntos, son un grupo alquileno C1-4, en cuyo grupo alquileno C1-4 1 miembro cíclico -CH2- es opcionalmente reemplazado por un miembro heterocíclico independientemente seleccionado a partir del grupo, que consta de -N(H)-, -N[alquilo C1-4]-, -O-, -S-, -S(=O)- ó -S(=O)2-; E1 es -C(R7)(R8)-, ó -C(R7)(R8)-C(R9)(R10)-; E2 es -C(R11)(R12)-, ó -C(R11)(R12)-C(R13)(R14)-; cualquiera, entre cada uno de R7 y R8 es independientemente seleccionado a partir del grupo, que consta de hidrógeno, ciano, halógeno, alquilo C1-8, halógeno-alquilo C1-8, alcoxi C1-8-alquil C1-8 y alquiltio C1-8-alquilo C1-8; o R7 y R8, tomados juntos, son oxo ó -CH2-CH2-; cualquiera, entre cada uno de R9 y R10 es independientemente seleccionado a partir del grupo, que consta de hidrógeno, ciano, halógeno, alquilo C1-8, halógeno-alquilo C1-8, alcoxi C1-8-alquilo C1-8 y alquiltio C1-8-alquilo C1-8; o R9 y R10, tomados juntos, son oxo ó -CH2-CH2-; cualquiera, entre cada uno de R11 y R12 es independientemente seleccionado a partir del grupo, que consta de hidrógeno, ciano, halógeno, alquilo C1-8, halógeno-alquilo C1-8, alcoxi C1-8-alquilo C1-8 y alquiltio C1-8-alquilo C1-8; o R11 y R12, tomados juntos, son oxo ó -CR15R16-CR17R18- en donde R15, R16, R17 y R18 son independientemente seleccionados a partir de hidrógeno y fluoro; y cualquiera, entre cada uno de R13 y R14 es independientemente seleccionado a partir del grupo, que consta de hidrógeno, ciano, halógeno, alquilo C1-8, halógeno-alquilo C1-8, alcoxi C1-8-alquilo C1-8 y alquiltio C1-8-alquil C1-8; o R13 y R14, tomados juntos, son oxo ó -CH2-CH2-.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IN77DE2011 | 2011-01-13 | ||
US201161534591P | 2011-09-14 | 2011-09-14 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR084849A1 true AR084849A1 (es) | 2013-06-26 |
Family
ID=46491227
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP120100120A AR084849A1 (es) | 2011-01-13 | 2012-01-13 | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos |
Country Status (40)
Country | Link |
---|---|
US (6) | US8637508B2 (es) |
EP (1) | EP2663561B1 (es) |
JP (1) | JP5715710B2 (es) |
KR (1) | KR101569260B1 (es) |
CN (2) | CN103403001B (es) |
AP (1) | AP3807A (es) |
AR (1) | AR084849A1 (es) |
AU (1) | AU2012206561B2 (es) |
CA (1) | CA2824220C (es) |
CL (2) | CL2013001964A1 (es) |
CO (1) | CO6751293A2 (es) |
CR (1) | CR20130339A (es) |
CU (1) | CU20130101A7 (es) |
CY (1) | CY1117580T1 (es) |
DK (1) | DK2663561T3 (es) |
EA (1) | EA024059B1 (es) |
ES (1) | ES2576182T3 (es) |
GT (1) | GT201300179A (es) |
HK (1) | HK1188453A1 (es) |
HR (1) | HRP20160647T1 (es) |
HU (1) | HUE029226T2 (es) |
IL (1) | IL227294A (es) |
JO (1) | JO3146B1 (es) |
MA (1) | MA34898B1 (es) |
ME (1) | ME02409B (es) |
MX (1) | MX336966B (es) |
MY (1) | MY162413A (es) |
PE (1) | PE20141110A1 (es) |
PL (1) | PL2663561T3 (es) |
PT (1) | PT2663561E (es) |
RS (1) | RS54782B1 (es) |
SG (1) | SG191812A1 (es) |
SI (1) | SI2663561T1 (es) |
SM (1) | SMT201600144B (es) |
TN (1) | TN2013000285A1 (es) |
TW (1) | TWI531570B (es) |
UA (1) | UA113051C2 (es) |
UY (1) | UY33865A (es) |
WO (1) | WO2012095469A1 (es) |
ZA (1) | ZA201304921B (es) |
Families Citing this family (73)
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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 |
EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
MX2009011498A (es) | 2007-04-24 | 2009-11-10 | Shionogi & Co | Derivados de aminodihidrotiazina sustituida con un grupo ciclico. |
KR20130018370A (ko) | 2008-06-13 | 2013-02-20 | 시오노기세야쿠 가부시키가이샤 | β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체 |
JPWO2010047372A1 (ja) | 2008-10-22 | 2012-03-22 | 塩野義製薬株式会社 | Bace1阻害活性を有する2−アミノピリミジン−4−オンおよび2−アミノピリジン誘導体 |
UY32799A (es) | 2009-07-24 | 2011-02-28 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos |
DK2987487T3 (da) | 2009-08-10 | 2020-12-07 | Samumed Llc | Indazolinhibitorer af wnt-signalvejen og terapeutiske anvendelser deraf |
EP2485920B1 (en) | 2009-10-08 | 2016-04-27 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
US8563543B2 (en) | 2009-10-08 | 2013-10-22 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
WO2011071135A1 (ja) | 2009-12-11 | 2011-06-16 | 塩野義製薬株式会社 | オキサジン誘導体 |
DK3001903T3 (en) | 2009-12-21 | 2017-12-18 | Samumed Llc | 1H-PYRAZOLO [3,4 -?] PYRIDINES AND THERAPEUTIC APPLICATIONS THEREOF |
EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE |
US8927721B2 (en) | 2010-10-29 | 2015-01-06 | Shionogi & Co., Ltd. | Naphthyridine derivative |
CA2824220C (en) | 2011-01-13 | 2020-09-01 | Novartis Ag | Novel heterocyclic derivatives and their use in the treatment of neurological disorders |
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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 |
AU2012308570B2 (en) | 2011-09-14 | 2016-11-10 | Samumed, Llc | Indazole-3-carboxamides and their use as Wnt/b-catenin signaling pathway inhibitors |
AU2012322329A1 (en) | 2011-10-13 | 2014-05-01 | Novartis Ag | Novel oxazine derivatives and their use in the treatment of disease |
PH12017500997A1 (en) | 2012-04-04 | 2018-02-19 | Samumed Llc | Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof |
WO2013161929A1 (ja) * | 2012-04-26 | 2013-10-31 | 塩野義製薬株式会社 | ピリジニルモルホリノン誘導体およびそれらを含有する医薬組成物 |
DK2770994T3 (da) | 2012-05-04 | 2019-11-11 | Samumed Llc | 1h-pyrazolo[3,4-b]pyridiner og terapeutiske anvendelser deraf |
WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
CN105120862A (zh) | 2013-01-08 | 2015-12-02 | 萨穆梅德有限公司 | Wnt信号途径的3-(苯并咪唑-2-基)-吲唑抑制剂及其治疗应用 |
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WO2016040193A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof |
WO2016040190A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof |
WO2016040180A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
WO2016040185A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 2-(1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine and therapeutic uses thereof |
WO2016040181A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
WO2016040188A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
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WO2016040184A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
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 |
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 |
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 |
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