PE20211790A1 - SUBSTITUTE OXOPYRIDINE DERIVATIVES - Google Patents
SUBSTITUTE OXOPYRIDINE DERIVATIVESInfo
- Publication number
- PE20211790A1 PE20211790A1 PE2021000903A PE2021000903A PE20211790A1 PE 20211790 A1 PE20211790 A1 PE 20211790A1 PE 2021000903 A PE2021000903 A PE 2021000903A PE 2021000903 A PE2021000903 A PE 2021000903A PE 20211790 A1 PE20211790 A1 PE 20211790A1
- Authority
- PE
- Peru
- Prior art keywords
- methyl
- hydrogen
- fluorine
- oxetan
- difluoromethyl
- Prior art date
Links
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 4
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052731 fluorine Inorganic materials 0.000 abstract 3
- 239000011737 fluorine Chemical group 0.000 abstract 3
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 2
- 102100022641 Coagulation factor IX Human genes 0.000 abstract 2
- 108010076282 Factor IX Proteins 0.000 abstract 2
- 229910052801 chlorine Chemical group 0.000 abstract 2
- 239000000460 chlorine Chemical group 0.000 abstract 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 2
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 2
- 229960004222 factor ix Drugs 0.000 abstract 2
- 230000009424 thromboembolic effect Effects 0.000 abstract 2
- 230000001732 thrombotic effect Effects 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000004063 butyryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 238000003776 cleavage reaction Methods 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 230000002255 enzymatic effect Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000004274 oxetan-2-yl group Chemical group [H]C1([H])OC([H])(*)C1([H])[H] 0.000 abstract 1
- 125000006299 oxetan-3-yl group Chemical group [H]C1([H])OC([H])([H])C1([H])* 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 230000007017 scission Effects 0.000 abstract 1
- 239000000758 substrate Substances 0.000 abstract 1
- 125000004192 tetrahydrofuran-2-yl group Chemical group [H]C1([H])OC([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
- 208000019553 vascular disease Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- 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
- A61K31/4353—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 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La invencion se refiere a compuestos derivados de oxopiridina sustituidos de formula (I); en donde R1 es metilo, etilo, difluorometilo o trifluorometilo; R2 es hidrogeno, metilo, difluorometilo o trifluorometilo, o R1 y R2 junto con los atomos de carbono a los cuales estan unidos forman un ciclobutilo; R3 es metilo, etilo o n-propilo, donde el metilo puede estar sustituido con un grupo seleccionado de ciclopropilo, ciclobutilo, oxetan-2-ilo, oxetan-3-ilo, tetrahidrofuran-2-ilo, entre otros; R4 es hidrogeno, R5 representa un grupo de la formula a), b), entre otros; R6 es hidrogeno, fluor o cloro, R7 es hidrogeno, fluor o cloro, R8 representa hidrogeno o fluor. Un compuesto seleccionado es acido 4-[(2S)-2-(11-cloro-7-metil-2-oxo-2,6,7,8-tetrahidro-3H-[3]benzoxocino[2,1-c]piridin-3-il)butanoil]amino}-2-fluorobenzamida. Tambien refiere a procesos para su preparacion. Dichos compuestos inhiben la escision enzimatica de sustratos FXIa, tales como el factor IX (FIX); siendo utiles en el tratamiento y/o la profilaxis de enfermedades, en particular trastornos vasculares, preferentemente trastornos tromboticos o tromboembolicos y/o complicaciones tromboticas o tromboembolicas.The invention relates to substituted oxopyridine derivative compounds of formula (I); wherein R1 is methyl, ethyl, difluoromethyl, or trifluoromethyl; R2 is hydrogen, methyl, difluoromethyl or trifluoromethyl, or R1 and R2 together with the carbon atoms to which they are attached form a cyclobutyl; R3 is methyl, ethyl or n-propyl, where methyl can be substituted with a group selected from cyclopropyl, cyclobutyl, oxetan-2-yl, oxetan-3-yl, tetrahydrofuran-2-yl, among others; R4 is hydrogen, R5 represents a group of formula a), b), among others; R6 is hydrogen, fluorine or chlorine, R7 is hydrogen, fluorine or chlorine, R8 represents hydrogen or fluorine. A selected compound is 4 - [(2S) -2- (11-chloro-7-methyl-2-oxo-2,6,7,8-tetrahydro-3H- [3] benzoxocino [2,1-c] acid pyridin-3-yl) butanoyl] amino} -2-fluorobenzamide. It also refers to processes for its preparation. Said compounds inhibit the enzymatic cleavage of FXIa substrates, such as factor IX (FIX); being useful in the treatment and / or prophylaxis of diseases, in particular vascular disorders, preferably thrombotic or thromboembolic disorders and / or thrombotic or thromboembolic complications.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2018122825 | 2018-12-21 | ||
| PCT/EP2019/085983 WO2020127504A1 (en) | 2018-12-21 | 2019-12-18 | Substituted oxopyridine derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20211790A1 true PE20211790A1 (en) | 2021-09-09 |
Family
ID=69143542
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2021000903A PE20211790A1 (en) | 2018-12-21 | 2019-12-18 | SUBSTITUTE OXOPYRIDINE DERIVATIVES |
Country Status (22)
| Country | Link |
|---|---|
| EP (1) | EP3898633A1 (en) |
| JP (1) | JP2022514303A (en) |
| KR (1) | KR20210106504A (en) |
| CN (1) | CN113474348A (en) |
| AR (1) | AR117435A1 (en) |
| AU (1) | AU2019407909B2 (en) |
| BR (1) | BR112021009435A2 (en) |
| CA (1) | CA3124220A1 (en) |
| CL (1) | CL2021001613A1 (en) |
| CO (1) | CO2021007908A2 (en) |
| CR (1) | CR20210342A (en) |
| DO (1) | DOP2021000128A (en) |
| EA (1) | EA202191764A1 (en) |
| EC (1) | ECSP21043895A (en) |
| IL (1) | IL283990A (en) |
| JO (1) | JOP20210161A1 (en) |
| MA (1) | MA54521A (en) |
| MX (1) | MX2021007508A (en) |
| PE (1) | PE20211790A1 (en) |
| SG (1) | SG11202104384PA (en) |
| TW (1) | TW202039510A (en) |
| WO (1) | WO2020127504A1 (en) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA126940C2 (en) * | 2018-03-15 | 2023-02-22 | Баєр Акціенгезельшафт | METHOD OF PREPARATION OF TWO 4-{[(2S)-2-{4-[5-CHLORO-2-(4-CHLORO-1H-1,2,3-TRIAZOL-1-YL)PHENYL]-5-METHOXY- 2-OXOPYRIDIN-1(2H)-YL}BUTANOYL]AMINO}-2-FLUOROBENZAMIDE |
| CN114105881B (en) | 2020-08-31 | 2024-01-26 | 沈阳海诺威医药科技有限公司 | Platelet aggregation inhibitor, and preparation method and application thereof |
| WO2022189280A1 (en) | 2021-03-09 | 2022-09-15 | Bayer Aktiengesellschaft | Solvates of (4s)-24-chloro-4-ethyl-73-fluoro-35-methoxy-32,5-dioxo-14-(trifluoro-methyl)-32 h-6- aza-3(4,1)-pyridina-1(1)-[1,2,3]triazola-2(1,2),7(1)-dibenzenaheptaphane-74-carboxamide |
| WO2022189279A1 (en) | 2021-03-09 | 2022-09-15 | Bayer Aktiengesellschaft | Crystalline forms of (4s)-24-chloro-4-ethyl-73-fluoro-35-methoxy-32,5-dioxo-14-(trifluoromethyl)-32h-6-aza-3(4,1)-pyridina-1(1)-[1,2,3]triazola-2(1,2),7(1)-5 dibenzenaheptaphane-74-carboxamide |
| CR20230431A (en) | 2021-03-09 | 2023-10-27 | Bayer Ag | Pharmaceutical dosage forms comprising (4s)-24-chloro-4-ethyl-73-fluoro-35-methoxy-32,5- dioxo-14-(trifluoromethyl)-32h-6-aza-3(4,1)-pyridina-1(1)-[1,2,3]triazola-2(1,2),7(1)- dibenzenaheptaphane-74-carboxamide |
| CN114560754A (en) * | 2022-02-25 | 2022-05-31 | 滁州学院 | Preparation method of alkyl alcohol |
| WO2024223790A1 (en) * | 2023-04-28 | 2024-10-31 | Basf Se | Use of alkyl 4-alkoxypentanoates as aroma chemicals |
| CN116874469B (en) * | 2023-09-06 | 2023-11-10 | 成都施贝康生物医药科技有限公司 | Oxo-pyridine compound, intermediate, preparation method and application thereof |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0420722D0 (en) | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
| DE102006032824A1 (en) * | 2006-07-14 | 2008-01-17 | Bayer Healthcare Ag | Substituted indazoles |
| US8163779B2 (en) | 2006-12-20 | 2012-04-24 | Takeda San Diego, Inc. | Glucokinase activators |
| WO2014160592A2 (en) | 2013-03-27 | 2014-10-02 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| TWI633089B (en) * | 2013-03-28 | 2018-08-21 | 拜耳製藥股份有限公司 | Substituted oxopyridine derivatives |
| CN105555767B (en) | 2013-07-23 | 2018-03-23 | 拜耳制药股份公司 | Substituted oxo pyridine derivative and its purposes as factor XI, plasma thromboplastin antecedent A/ blood plasma |
| CN105849109B (en) | 2013-10-30 | 2018-01-23 | 拜耳制药股份公司 | Substituted oxopyridine derivatives |
| EP3197889B1 (en) | 2014-09-24 | 2018-08-01 | Bayer Pharma Aktiengesellschaft | Substituted oxopyridine derivatives |
| ES2712886T3 (en) * | 2014-09-24 | 2019-05-16 | Bayer Pharma AG | Derivatives of pyridobenzazepine and pyridobenzazocine that inhibit factor XIa |
| WO2016046166A1 (en) | 2014-09-24 | 2016-03-31 | Bayer Pharma Aktiengesellschaft | Substituted oxopyridine derivatives |
| EP3197880B1 (en) | 2014-09-24 | 2018-10-24 | Bayer Pharma Aktiengesellschaft | Substituted oxopyridine derivatives with anti-inflammatory and anti-thrombotic effect |
| EP3197896B1 (en) | 2014-09-24 | 2019-01-30 | Bayer Pharma Aktiengesellschaft | Substituted oxopyridine derivatives |
| CA2961981A1 (en) | 2014-09-24 | 2016-03-31 | Bayer Pharma Aktiengesellschaft | Substituted oxopyridine derivatives |
| CA2979937A1 (en) | 2015-03-19 | 2016-09-22 | Bayer Pharma Aktiengesellschaft | Oxo-pyridine-derivatives as factor xia inhibitors for the treatment of thrombosis |
| JO3703B1 (en) | 2015-07-09 | 2021-01-31 | Bayer Pharma AG | Substituted oxopyridine derivatives |
| WO2017037051A1 (en) | 2015-09-04 | 2017-03-09 | Bayer Pharma Aktiengesellschaft | Substituted oxopyridine derivatives |
-
2019
- 2019-12-18 EP EP19832641.5A patent/EP3898633A1/en not_active Withdrawn
- 2019-12-18 SG SG11202104384PA patent/SG11202104384PA/en unknown
- 2019-12-18 CR CR20210342A patent/CR20210342A/en unknown
- 2019-12-18 WO PCT/EP2019/085983 patent/WO2020127504A1/en not_active Ceased
- 2019-12-18 CA CA3124220A patent/CA3124220A1/en active Pending
- 2019-12-18 KR KR1020217022510A patent/KR20210106504A/en not_active Ceased
- 2019-12-18 EA EA202191764A patent/EA202191764A1/en unknown
- 2019-12-18 AU AU2019407909A patent/AU2019407909B2/en not_active Ceased
- 2019-12-18 PE PE2021000903A patent/PE20211790A1/en unknown
- 2019-12-18 MX MX2021007508A patent/MX2021007508A/en unknown
- 2019-12-18 CN CN201980091518.1A patent/CN113474348A/en active Pending
- 2019-12-18 TW TW108146372A patent/TW202039510A/en unknown
- 2019-12-18 MA MA054521A patent/MA54521A/en unknown
- 2019-12-18 JP JP2021535063A patent/JP2022514303A/en active Pending
- 2019-12-18 BR BR112021009435-0A patent/BR112021009435A2/en not_active Application Discontinuation
- 2019-12-18 AR ARP190103745A patent/AR117435A1/en unknown
- 2019-12-18 JO JOP/2021/0161A patent/JOP20210161A1/en unknown
-
2021
- 2021-06-14 IL IL283990A patent/IL283990A/en unknown
- 2021-06-16 EC ECSENADI202143895A patent/ECSP21043895A/en unknown
- 2021-06-16 CO CONC2021/0007908A patent/CO2021007908A2/en unknown
- 2021-06-17 CL CL2021001613A patent/CL2021001613A1/en unknown
- 2021-06-18 DO DO2021000128A patent/DOP2021000128A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2019407909B2 (en) | 2023-05-25 |
| JOP20210161A1 (en) | 2023-01-30 |
| KR20210106504A (en) | 2021-08-30 |
| EA202191764A1 (en) | 2021-10-22 |
| SG11202104384PA (en) | 2021-05-28 |
| MA54521A (en) | 2022-03-30 |
| CR20210342A (en) | 2021-08-09 |
| MX2021007508A (en) | 2021-08-05 |
| EP3898633A1 (en) | 2021-10-27 |
| WO2020127504A1 (en) | 2020-06-25 |
| AU2019407909A1 (en) | 2021-05-27 |
| ECSP21043895A (en) | 2021-07-30 |
| JP2022514303A (en) | 2022-02-10 |
| CL2021001613A1 (en) | 2021-12-03 |
| TW202039510A (en) | 2020-11-01 |
| CO2021007908A2 (en) | 2021-07-19 |
| BR112021009435A2 (en) | 2021-08-17 |
| DOP2021000128A (en) | 2021-09-30 |
| CN113474348A (en) | 2021-10-01 |
| CA3124220A1 (en) | 2020-06-25 |
| IL283990A (en) | 2021-07-29 |
| AR117435A1 (en) | 2021-08-04 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PE20211790A1 (en) | SUBSTITUTE OXOPYRIDINE DERIVATIVES | |
| PH12019502264A1 (en) | Fused imidazo-piperidine jak inhibitors compound | |
| MX2024008497A (en) | Manufacture of compounds and compositions for inhibiting the activity of shp2. | |
| PH12014502866A1 (en) | Fungicidal heterocyclic carboxamides | |
| EA202091016A1 (en) | PYRIMIDINE COMPOUND AS A JAK KINASE INHIBITOR | |
| MX2020006181A (en) | Substituted bicyclic heterocyclic compounds as prmt5 inhibitors. | |
| BR122015016965B8 (en) | 6-(POLYSUBSTITUTED ARYL)-4-AMINOPICOLINATES, HERBICIDAL COMPOSITION, AND METHOD FOR CONTROL OF UNDESIRABLE VEGETATION | |
| BR112018011788A2 (en) | (2r, 4s) -5- (biphenyl-4-yl) -4 - [(3-carboxypropionyl) amino] -2-methylpentanoic acid ethyl ester solid forms, their salts and a preparation method | |
| PE20120690A1 (en) | DERIVATIVES OF 5-FLUOROPYRIMIDINONE | |
| PE20211756A1 (en) | NOVEL POLYMORPHIC FORMS OF A TGFß INHIBITOR | |
| BR112016024443A2 (en) | herbicidal compound, composition and mixture and method for controlling unwanted vegetation growth | |
| PE20161368A1 (en) | DIACILGLICEROL ACILTRANFERASE 2 INHIBITORS | |
| CU20200084A7 (en) | SUBSTITUTE DERIVATIVES OF CARBOXAMIDE DIHYDROPIRAZOLO PIRAZINE | |
| PE20170946A1 (en) | 2-AMINO-6- (DIFLUOROMETIL) - 5,5-DIFLUORO-6-PHENYL-3,4,5,6-TETRAHYDROPYRIDINES AS BACE1 INHIBITORS | |
| PE20120689A1 (en) | 5-FLUORO-2-OXOPYRIMIDINE-1 (2H) -CARBOXYLATE DERIVATIVES | |
| EA201891770A1 (en) | MALATE SALT OF AGONIST TLR7, ITS CRYSTALLINE FORMS C, D AND E, METHODS OF OBTAINING AND APPLICATION OF MALEATIC SALT AND CRYSTALLINE FORMS | |
| AU2015306910A8 (en) | Crystallization process of aripiprazole derivatives in extended release formulations for treatment of schizophrenia | |
| MX369345B (en) | Processes for the preparation of oxytocin analogues. | |
| MX2021007536A (en) | Crystalline and salt forms of an organic compound and pharmaceutical compositions thereof. | |
| MY147951A (en) | Crystalline potassium salt of lipoxin a? analogs | |
| WO2022198062A3 (en) | Derivatives of substituted morpholines and uses thereof | |
| MX389261B (en) | ALPHA-AMINO ESTERS OF HYDROXYPROPYLTHIAZOLIDINE CARBOXAMIDE DERIVATIVES, AND SALT FORMS AND CRYSTALLINE POLYMORPHS THEREOF. | |
| NO20051011L (en) | Chiral oxazole-arylpropionic acid derivatives and their use as PPAR agonists | |
| AR087089A1 (en) | POSITIVE ALLOSTERIC MODULATORS OF NICOTINIC ACETILCOLINE RECEIVER | |
| PE20171349A1 (en) | BACE1 INHIBITORS |