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ES2571057T3 - Inhibidores de beta-secretasa - Google Patents

Inhibidores de beta-secretasa

Info

Publication number
ES2571057T3
ES2571057T3 ES10708684T ES10708684T ES2571057T3 ES 2571057 T3 ES2571057 T3 ES 2571057T3 ES 10708684 T ES10708684 T ES 10708684T ES 10708684 T ES10708684 T ES 10708684T ES 2571057 T3 ES2571057 T3 ES 2571057T3
Authority
ES
Spain
Prior art keywords
alkyl
alkoxy
nr12r13
heterocycloalkyl
cycloalkyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
ES10708684T
Other languages
English (en)
Inventor
Salvacion Cacatian
David A Claremon
Lawrence W Dillard
Klaus Fuchs
Niklas Heine
Lanqi Jia
Katerina Leftheris
Brian Mckeever
Angel Morales-Ramos
Suresh Singh
Shankar Venkatraman
Guosheng Wu
Zhongren Wu
Zhenrong Xu
Jing Yuan
Yajun Zheng
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boehringer Ingelheim International GmbH
Vitae Pharmaceuticals LLC
Original Assignee
Boehringer Ingelheim International GmbH
Vitae Pharmaceuticals LLC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Boehringer Ingelheim International GmbH, Vitae Pharmaceuticals LLC filed Critical Boehringer Ingelheim International GmbH
Application granted granted Critical
Publication of ES2571057T3 publication Critical patent/ES2571057T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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    • C07—ORGANIC CHEMISTRY
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    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/12—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/44—Nitrogen atoms not forming part of a nitro radical
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    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
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    • C07D405/06—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 carbon chain containing only aliphatic carbon atoms
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    • 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
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    • C07D405/14—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 three or more hetero rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • 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
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    • 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
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    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D417/06—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 carbon chain containing only aliphatic carbon atoms
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    • C07D417/10—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 carbon chain containing aromatic rings
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    • 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
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  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Epidemiology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Compuesto representado por la siguiente fórmula estructural: **Fórmula** o sal farmacéuticamente aceptable del mismo, en la que: X es -O-, -CH2- o -CH2-CH2-; W es -N(R14)-, -S- u -O-; Z es -C(>=O)-, -C(>=S)-,-C(>=NR15)-, -O-, -C(>=O)C(R16R17)-, -C(R16R17)C(>=O)-, -C(>=S)C(R16R17)-, -C(R16R17)C(>=S)-, -N(R18)-, -(CR16R17)m-,-O-(CR16R17)- o -(CR16R17)-O-, con la condición de que cuando W es -S- u -O-, Z no sea -O-; R1 es -H, -OH, alcoxilo (C1-C4), alquilo (C1-C6), arilalquilo (C1-C6) o heteroarilalquilo (C1-C6); en los que cada alquilo, arilo y heteroarilo está opcionalmente sustituido con de 1 a 5 sustituyentes seleccionados independientemente de halógeno, -CN, -OH, alquilo (C1-C4), haloalquilo (C1-C4), alcoxilo (C1-C3) y haloalcoxilo (C1-C3); cada R2 se selecciona independientemente de a) -H, -halógeno, -CN, -NO2, -OR5, -NR6R7, -S(O)iR5, -NR11S(O)iR5, -S(O)iNR12R13, -C(>=O)OR5, -OC(>=O)OR5, -C(>=S)OR5, -OC(>=S)R5, -C(>=O)NR12R13, -NR11C(>=O)R5, -C(>=S)NR12R13, -NR11C(>=S)R5, -NR11(C>=O)OR5, -O(C>=O)NR12R13, -NR11(C>=S)OR5, -O(C>=S)NR12R13, -NR11(C>=O)NR12R13, -NR11(C>=S)NR12R13, -C(>=S)R5 y -C(>=O)R5; y b) alquilo (C1-C6), alquenilo (C2-C6), alquinilo (C2-C6), cicloalquilo (C3-C8), cicloalquil (C3-C8)-alquilo (C1-C6), cicloalquil (C3-C8)- alquinilo (C2-C6), cicloalquenilo (C4-C8), heterocicloalquilo (C3-C9), heterocicloalquil (C3-C9)-alquilo (C1-C6), heterocicloalquil (C3-C9)-alquinilo (C2-C6), arilo, arilalquilo (C1-C6), arilalquinilo (C2-C6), heteroarilo, heteroarilalquilo (C1-C6) y heteroarilalquinilo (C2-C6), en los que cada uno de los grupos alquilo (C1-C6), alquenilo (C2-C6), alquinilo (C2-C6), cicloalquilo (C3-C8), cicloalquil (C3-C8)-alquilo (C1-C6), cicloalquil (C3-C8)- alquinilo (C2-C6), cicloalquenilo (C4-C8), heterocicloalquilo (C3-C9), heterocicloalquil (C3-C9)-alquilo (C1-C6), heterocicloalquil (C3-C9)-alquinilo (C2-C6), arilo, arilalquilo (C1-C6), arilalquinilo (C2-C6), heteroarilo, heteroarilalquilo (C1-C6) y heteroarilalquinilo (C2-C6) representados por R2 está opcionalmente sustituido con de 1 a 5 sustituyentes seleccionados independientemente del grupo que consiste en -halógeno, -CN, -NO2, -OR5, -SR5, -NR6R7, -S(O)iR5, -NR11S(>=O)iR5, -S(O)iNR12R13, -C(>=O)OR5, -OC(>=O)R5, -C(>=S)OR5, -OC(>=S)R5, -C(>=O)NR12R13, -NR11C(>=O)R5, -C(>=S)NR12R13, -NR11C(>=S)R5, -C(>=O)R5, -C(>=S)R5, -OC(>=O)OR5, -O(C>=O)NR12R13, -NR11(C>=O)OR5, -NR11(C>=S)OR5, -O(C>=S)NR12R13, -NR11(C>=O)NR12R13, -NR11(C>=S)NR12R13, -C(>=O)R5, -C(>=S)R5, alquilo (C1-C6), alquinilo (C2-C6), cicloalquilo (C3-C8), cicloalquenilo (C4-C8), heterocicloalquilo (C3-C9), alquenilo (C2-C6), haloalquilo (C1-C6), alquil (C1-C3)- sulfonilaminoalquilo, hidroxialquilo (C1-C6), cianoalquilo (C1-C6), alquil (C1-C3)-carbonilaminoalquilo (C1-C6), alcoxilo (C1-C3), haloalcoxilo (C1-C3), alcoxi (C1-C6)-alquilo (C1-C3), arilo y heteroarilo, en los que los grupos cicloalquilo, heterocicloalquilo, arilo y heteroarilo en los sustituyentes de los grupos representados por R2 están cada uno opcionalmente sustituidos con de 1 a 3 sustituyentes seleccionados independientemente de halógeno, -CN, alquilo (C1-C6), haloalquilo (C1-C6), alcoxilo (C1-C3), haloalcoxilo (C1-C3) y alcoxi (C1-C3)- alquilo (C1-C6); R5 es -H, alquilo (C1-C6), haloalquilo (C1-C6), alquenilo (C2-C6), alquinilo (C2-C6), alcoxi (C1-C3)-alquilo (C1- C6), cicloalquilo (C3-C8), cicloalquil (C3-C8)-alquilo (C1-C6), heterocicloalquilo (C3-C9), heterocicloalquil (C3- C9)-alquilo (C1-C6), arilo, arilalquilo (C1-C6), heteroarilo o heteroarilalquilo (C1-C6), cada uno del alquilo, alquenilo, alquinilo, cicloalquilo, heterocicloalquilo, arilo y heteroarilo de los grupos representados por R5 está opcionalmente sustituido con de 1 a 5 sustituyentes seleccionados independientemente del grupo que consiste en halógeno, >=O, -NR6C(>=NH)NR6R7, -C(>=O)ORc, -ORc, -SRc, -C(>=O)NR6R7, -C(>=O)Rc, -S(O)iRc, -NO2, -CN, alquilo (C1-C6), haloalquilo (C1-C6), alcoxi (C1-C3)-alquilo (C1-C6), alcoxilo (C1-C3), haloalcoxilo (C1-C3) y -NR6R7; Rc es -H, alquilo (C1-C3), haloalquilo (C1-C3) o alcoxi (C1-C3)-alquilo (C1-C3); R6 y R7 son cada uno independientemente -H, alquilo (C1-C6), hidroxialquilo (C1-C6), haloalquilo (C1-C6), cicloalquilo (C3-C8), cicloalquil (C3-C8)-alquilo (C1-C6), heterocicloalquilo (C3-C9), heterocicloalquil (C3-C9)- alquilo (C1-C6), arilo, arilalquilo (C1-C6), heteroarilo o heteroarilalquilo (C1-C6), estando todos estos grupos opcionalmente sustituidos con de 1 a 3 sustituyentes seleccionados independientemente del grupo que consiste en halógeno, -CN, alquilo (C1-C6), haloalquilo (C1-C6), alcoxilo (C1-C3), haloalcoxilo (C1-C3) y alcoxi (C1-C3)-alquilo (C1-C6);
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Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8450308B2 (en) 2008-08-19 2013-05-28 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
KR101908255B1 (ko) * 2009-03-13 2018-10-15 비타이 파마슈티컬즈, 인코포레이티드 베타세크리타아제 저해제
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
JP5828848B2 (ja) 2010-02-24 2015-12-09 ヴァイティー ファーマシューティカルズ，インコーポレイテッド ベータセクレターゼインヒビター
US8957083B2 (en) 2010-11-23 2015-02-17 Amgen Inc. Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use
US8415483B2 (en) 2010-12-22 2013-04-09 Astrazeneca Ab Compounds and their use as BACE inhibitors
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
WO2012109165A1 (en) 2011-02-07 2012-08-16 Amgen Inc. 5-amino-oxazepine and 5-amino-thiazepane compounds as beta-secretase antagonists and methods of use
WO2012112462A1 (en) 2011-02-15 2012-08-23 Amgen Inc. Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use
WO2013044092A1 (en) 2011-09-21 2013-03-28 Amgen Inc. Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US9650336B2 (en) 2011-10-10 2017-05-16 Astrazeneca Ab Mono-fluoro beta-secretase inhibitors
TWI557112B (zh) 2012-03-05 2016-11-11 百靈佳殷格翰國際股份有限公司 β－分泌酶抑制劑
EP2847177B1 (en) 2012-05-09 2017-10-11 Boehringer Ingelheim International GmbH Methods for making oxetan-3-ylmethanamines
AR091203A1 (es) 2012-05-30 2015-01-21 Astellas Pharma Inc Compuestos de cromano
EP2669286A1 (en) * 2012-05-31 2013-12-04 Ares Trading S.A. Spiro tetrahydro-benzothiophen derivatives useful for the treatment of neurodegenerative diseases
US9000182B2 (en) * 2012-06-20 2015-04-07 Astrazeneca Ab 2H-imidazol-4-amine compounds and their use as BACE inhibitors
US9000185B2 (en) 2012-06-20 2015-04-07 Astrazeneca Ab Cycloalkyl ether compounds and their use as BACE inhibitors
US9000184B2 (en) 2012-06-20 2015-04-07 Astrazeneca Ab Cyclohexane-1,2′-naphthalene-1′,2″-imidazol compounds and their use as BACE inhibitors
US9000183B2 (en) * 2012-06-20 2015-04-07 Astrazeneca Ab Cyclohexane-1,2′-indene-1′,2″-imidazol compounds and their use as BACE inhibitors
US10548882B2 (en) * 2012-06-21 2020-02-04 Astrazeneca Ab Camsylate salt
TW201422592A (zh) 2012-08-27 2014-06-16 Boehringer Ingelheim Int β－分泌酶抑制劑
US9533986B2 (en) 2012-09-27 2017-01-03 Portola Pharmaceuticals, Inc. Bicyclic dihydropyridone kinase inhibitors
EP2900650A1 (en) 2012-09-28 2015-08-05 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
US9725469B2 (en) 2012-11-15 2017-08-08 Amgen, Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US10550327B2 (en) 2012-11-21 2020-02-04 Merck Patent Gmbh Polymerisable compounds and the use thereof in liquid-crystal displays
WO2014081558A1 (en) 2012-11-21 2014-05-30 Boehringer Ingelheim International Gmbh PROCESS FOR MAKING N-SULFINYL a-AMINO AMIDES
ES2655788T5 (es) 2013-01-28 2024-05-22 Moelnlycke Health Care Ab Dispositivo de aspiración
WO2014160775A1 (en) 2013-03-26 2014-10-02 Saint Louis University Compositions and methods for the treatment of malaria
AR102202A1 (es) 2014-10-07 2017-02-08 Astrazeneca Ab Compuestos de oxazol y su uso como inhibidores de bace de oxazol
JP6319805B2 (ja) * 2014-10-08 2018-05-09 田岡化学工業株式会社 スピロビフルオレン骨格を有するジオール化合物およびその製造方法
CN106083764B (zh) * 2016-07-11 2018-09-18 上海皓元生物医药科技有限公司 一种用于制备axl抑制剂的高纯度中间体的手性拆分方法
WO2018213442A1 (en) * 2017-05-16 2018-11-22 The University Of Chicago Highly diastereoselective construction of the 4,5-spirocycle via palladium-catalyzed intramolecular alkenylation
BR112019025212A2 (pt) * 2017-06-14 2020-06-16 Nippon Soda Co., Ltd. Composto, formulações para controlar organismos nocivos, para controlar ectoparasitas, para controlar pragas de insetos thysanoptera, e, formulação inseticida ou acaricida
KR101969528B1 (ko) 2017-09-29 2019-04-16 에스케이텔레콤 주식회사 터치 디스플레이를 제어하는 장치와 방법 및 터치 디스플레이 시스템
US11760701B2 (en) 2018-02-27 2023-09-19 The Research Foundation For The State University Of New Yrok Difluoromethoxylation and trifluoromethoxylation compositions and methods for synthesizing same
CN108675923B (zh) * 2018-06-27 2021-04-27 沅江华龙催化科技有限公司 一种由环酮化合物与2-芳基丙烯及二甲亚砜共同构建螺环化合物的方法
CN108675922B (zh) * 2018-06-27 2021-04-27 沅江华龙催化科技有限公司 一种螺环化合物及其合成方法
JP7678756B2 (ja) 2019-09-30 2025-05-16 日本ケミファ株式会社 アゼパン誘導体
WO2021217508A1 (en) * 2020-04-29 2021-11-04 Novartis Ag COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF HIF2α AND THEIR METHODS OF USE
WO2023141432A2 (en) 2022-01-18 2023-07-27 Maze Therapeutics, Inc. Apol1 inhibitors and methods of use
WO2025015106A2 (en) * 2023-07-11 2025-01-16 Maze Therapeutics, Inc. Apol1 inhibitors and methods of use thereof
WO2025015104A2 (en) * 2023-07-11 2025-01-16 Maze Therapeutics, Inc. Apol1 inhibitors and methods of use

Family Cites Families (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5745185A (en) * 1980-07-21 1982-03-13 Eisai Co Ltd Hydantoin derivative and its preparation
WO1993005045A1 (en) 1991-08-28 1993-03-18 The Upjohn Company Spirocyclic benzopyran imidazolines
CA2189634A1 (en) * 1994-05-06 1995-11-16 John J. Baldwin Combinatorial dihydrobenzopyran library
US7592348B2 (en) * 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7763609B2 (en) * 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
NZ547462A (en) * 2003-12-15 2010-06-25 Schering Corp Heterocyclic aspartyl protease inhibitors
ES2321853T3 (es) 2004-06-16 2009-06-12 Wyeth Difenilimidazopiridina e -imidazol aminas como inhibidores de b-secretasa".
ES2332659T3 (es) 2004-06-16 2010-02-10 Wyeth Derivados de amino-5,5-difenilimidazolona para la inhibicion de beta-secretasa.
JP2008515989A (ja) 2004-10-13 2008-05-15 メルク エンド カムパニー インコーポレーテッド アルツハイマー病を治療するためのβ−セクレターゼ阻害薬として有用なスピロピペリジン化合物
KR20080025079A (ko) 2005-06-14 2008-03-19 쉐링 코포레이션 아스파르틸 프로테아제 억제제
US7759354B2 (en) 2005-06-14 2010-07-20 Schering Corporation Bicyclic guanidine derivatives as asparyl protease inhibitors, compositions, and uses thereof
TW200738683A (en) 2005-06-30 2007-10-16 Wyeth Corp Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation
AU2006266167A1 (en) 2005-06-30 2007-01-11 Wyeth Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for beta-secretase modulation
JP4870162B2 (ja) * 2005-07-29 2012-02-08 コーニンクレッカ フィリップス エレクトロニクス エヌ ヴィ 蒸気アイロンからの蒸気の噴出を生成する方法
TW200730523A (en) 2005-07-29 2007-08-16 Wyeth Corp Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation
WO2007038271A1 (en) 2005-09-26 2007-04-05 Wyeth Amino-5- [4- (difluoromethoxy) phenyl] -5-phenylimidazolone compounds as inhibitors of the beta-secretase (bace)
US8173642B2 (en) 2005-10-25 2012-05-08 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives
US7872009B2 (en) * 2005-11-21 2011-01-18 Amgen Inc. Beta-Secretase modulators and methods of use
DE102005057688A1 (de) 2005-12-01 2007-06-14 Endress + Hauser Flowtec Ag Vorrichtung zur Bestimmung und/oder Überwachung des Massedurchflusses eines gasförmigen Mediums
JP2009520027A (ja) 2005-12-19 2009-05-21 ワイス ２−アミノ−５−ピペリジニルイミダゾロン化合物およびβ−セクレターゼ調節におけるその使用
EP1974278A4 (en) 2005-12-20 2012-01-04 Fieldbus Foundation SYSTEM AND METHOD FOR IMPLEMENTING INSTRUMENTED SAFETY SYSTEMS
WO2007100536A1 (en) * 2006-02-24 2007-09-07 Wyeth DIHYDROSPIRO[DIBENZO[A,D][7]ANNULENE-5,4'-IMIDAZOL] COMPOUNDS FOR THE INHIBITION OF β-SECRETASE
EP2644600B1 (en) 2006-06-12 2017-01-11 Merck Sharp & Dohme Corp. Heterocyclic aspartyl protease inhibitors
DK2042480T3 (da) * 2006-07-18 2013-05-27 Astellas Pharma Inc Aminoindan-derivat eller salt deraf
JP2010502705A (ja) 2006-09-07 2010-01-28 メルク エンド カムパニー インコーポレーテッド アルツハイマー病の治療用としてのスピロピペリジンベータセクレターゼ阻害剤
WO2008076044A1 (en) 2006-12-20 2008-06-26 Astrazeneca Ab Novel 2-amino-5, 5-diaryl-imidazol-4-ones
TW200831091A (en) 2006-12-20 2008-08-01 Astrazeneca Ab New compounds
TW200831484A (en) 2006-12-20 2008-08-01 Astrazeneca Ab New compounds
CL2008000784A1 (es) 2007-03-20 2008-05-30 Wyeth Corp Compuestos amino-5-[-4-(diflourometoxi) fenil sustituido]-5-fenilmidazolona, inhibidores de b-secretasa; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar alzheimer, deterioro cognitivo, sindrome de down, disminucion co
PE20090617A1 (es) 2007-03-23 2009-05-08 Wyeth Corp Compuestos amino-5-[-4-(difluorometoxi)fenil]-5-fenilimidazolona para la inhibicion de -secretasa
MX2009011498A (es) 2007-04-24 2009-11-10 Shionogi & Co Derivados de aminodihidrotiazina sustituida con un grupo ciclico.
EP2151435A4 (en) * 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
UY31083A1 (es) 2007-05-15 2009-01-05 Astrazeneca Ab Derivados de sulfoximinas para la inhibicion de b-secretasa
ES2398017T3 (es) 2008-02-18 2013-03-13 F. Hoffmann-La Roche Ag Derivados de 4,5-dihidro-oxazol-2-il-amina
TWI431004B (zh) 2008-05-02 2014-03-21 Lilly Co Eli Ｂａｃｅ抑制劑
WO2010013302A1 (ja) 2008-07-28 2010-02-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 スピロアミノジヒドロチアジン誘導体
KR20110048491A (ko) 2008-07-28 2011-05-11 에자이 알앤드디 매니지먼트 가부시키가이샤 스피로아미노디하이드로티아진 유도체들
US8450308B2 (en) 2008-08-19 2013-05-28 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
MX2011002705A (es) * 2008-09-11 2011-09-09 Amgen Inc Compuestos con anillos espiro-triciclicos como moduladores de beta-secretasas y metodos de uso.
CA2743584A1 (en) 2008-11-23 2010-05-27 Pfizer Inc. Lactams as beta secretase inhibitors
KR101908255B1 (ko) 2009-03-13 2018-10-15 비타이 파마슈티컬즈, 인코포레이티드 베타세크리타아제 저해제
WO2011072064A1 (en) 2009-12-08 2011-06-16 Array Biopharma Inc. S piro [chroman - 4, 4 ' - imidazol] ones as beta - secretase inhibitors
JP5828848B2 (ja) 2010-02-24 2015-12-09 ヴァイティー ファーマシューティカルズ，インコーポレイテッド ベータセクレターゼインヒビター
TWI557112B (zh) 2012-03-05 2016-11-11 百靈佳殷格翰國際股份有限公司 β－分泌酶抑制劑
TW201422592A (zh) 2012-08-27 2014-06-16 Boehringer Ingelheim Int β－分泌酶抑制劑
EP2900650A1 (en) * 2012-09-28 2015-08-05 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase

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CN102348698B (zh) 2015-06-03
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US9212153B2 (en) 2015-12-15
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US10336717B2 (en) 2019-07-02
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