AR084944A1 - COMPUESTOS PARA REDUCIR LA PRODUCCION DE AMILOIDE b - Google Patents

COMPUESTOS PARA REDUCIR LA PRODUCCION DE AMILOIDE b

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Publication number
AR084944A1
AR084944A1 ARP120100283A ARP120100283A AR084944A1 AR 084944 A1 AR084944 A1 AR 084944A1 AR P120100283 A ARP120100283 A AR P120100283A AR P120100283 A ARP120100283 A AR P120100283A AR 084944 A1 AR084944 A1 AR 084944A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
cycloalkyl
hydrogen
hydroxy
Prior art date
Application number
ARP120100283A
Other languages
English (en)
Inventor
John E Macor
Jason M Guernon
Jianliang Shi
Richard E Olson
Yong Wu
Dmitry S Jin-Zuev
Kenneth M Boy
Yunhui Zhang
Lorin A Thompson Iii
Li Xu
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AR084944A1 publication Critical patent/AR084944A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D401/04—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
    • 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
    • C07D487/10—Spiro-condensed systems
    • 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
    • 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
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • C07D491/10—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Compuestos de la formula (1) que modulan la producción del péptido amiloide b (AP b) y son útiles para el tratamiento de la enfermedad de Alzheimer y otros trastornos afectados por la producción del péptido amiloide b (AP b).Reivindicación 1: Un compuesto caracterizado por la fórmula (1) o una sal de este aceptable desde el punto de vista farmacéutico, en donde A es un grupo nitrito; B se selecciona de fenilo y piridinilo, en donde el fenilo y piridinilo se sustituyen opcionalmente con uno o dos sustituyentes seleccionados independientemente de los siguientes: alcoxi C1-6, alquilo C1-6, alquilamino C1-3-alcoxi C1-6, ciano, dialquilamino C1-3-alcoxi C1-6, halo, haloalcoxi C1-6, haloalquilo C1-6, hidroxi, metilamino y amino; D se selecciona del grupo de formulas (2); la “línea ondulada” indica el punto de unión con el átomo de nitrógeno de la molécula de origen; la “doble línea ondulada” indica el punto de unión con la porción ‘E’; Ra se selecciona de hidrógeno, alquilo C1-6, alquenilo C2-6 e hidroxi; Rb es NRxRy, en donde Rx y Ry se seleccionan independientemente de hidrógeno, alcoxi C1-4, alcoxi C1-4-alquilo C1-4, alcoxicarbonilo C1-4, alquilo C1-6, cicloalquilo C3-7, (cicloalquil C3-7)alquilo C1-4, hidroxi-alquilo C1-4 y trideuterometilo, en donde la parte alquilo de (cicloalquil C3-7)alquilo C1-4 se puede sustituir opcionalmente con un grupo alcoxi C1-4; o Rx y Ry, junto con el átomo de nitrógeno al que están unidos, forman un anillo monocíclico o bicíclico de 4 a 7 miembros que contiene, opcionalmente, un enlace doble y un heteroátomo adicional seleccionado de O, NRz y S; en donde Rz se selecciona de hidrógeno, alquilo C1-6 y alcoxicarbonilo C1-4; y en donde el anillo se sustituye opcionalmente con uno o dos sustituyentes seleccionados independientemente de halo de alcoxi C1-6, alquilo C1-6, halo, haloalquilo C1-4, hidroxi, -NRfRg, oxo, dioxolanilo espirocíclico; en donde Rf y Rg se seleccionan independientemente de hidrógeno, alcoxi C1-4carbonilo y alquilo C1-6; Rc se selecciona de hidrógeno, alquilsulfonilo C1-4, alquilsulfonilamido C1-4, amino, alquilamino C1-6, dialquilamino C1-6, cicloalquil C3-7amino, hidroxi y alcoxi C1-4; Rd se selecciona de hidrógeno, alquilo C1-6, alcoxi C1-4alquilcarbonilo C1-4, alcoxi C1-6carbonilo, alquilcarbonilo C1-6, alquilsulfonilo C1-6, cicloalquil C3-7sulfonilo, cicloalquil C3-7carbonilo, dialquilamino C1-6 alquilcarbonilo C1-4 y haloalquilo C1-4, en donde la parte alquilo de alcoxicarbonilo, alquilcarbonilo y alquilsulfonilo se sustituye opcionalmente con un sustituyente seleccionado de dialquilamino C1-6 y alcoxi C1-4; y E se selecciona de alquilo C1-6, cicloalquilo C4-6, (cicloalquil C4-7)alquilo C1-4, bencilo, fenilo y un anillo heteroaromático de 5 a 6 miembros que contiene uno o dos átomos de nitrógeno, en donde el fenilo, la parte fenilo del bencilo y el anillo heteroaromático se sustituyen opcionalmente con 1, 2 ó 3 sustituyentes seleccionados independientemente de alquilo C1-6, alcoxi C1-6, ciano, halo, haloalcoxi C1-6 y haloalquilo C1-6.
ARP120100283A 2011-01-28 2012-01-27 COMPUESTOS PARA REDUCIR LA PRODUCCION DE AMILOIDE b AR084944A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161437279P 2011-01-28 2011-01-28

Publications (1)

Publication Number Publication Date
AR084944A1 true AR084944A1 (es) 2013-07-10

Family

ID=45688981

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120100283A AR084944A1 (es) 2011-01-28 2012-01-27 COMPUESTOS PARA REDUCIR LA PRODUCCION DE AMILOIDE b

Country Status (15)

Country Link
US (1) US8710061B2 (es)
EP (1) EP2668168B1 (es)
JP (1) JP5908499B2 (es)
KR (1) KR20140014152A (es)
CN (1) CN103328451B (es)
AR (1) AR084944A1 (es)
AU (1) AU2012211301B2 (es)
BR (1) BR112013018298A2 (es)
CA (1) CA2825906A1 (es)
EA (1) EA201391097A1 (es)
IL (1) IL226677A (es)
MX (1) MX2013008699A (es)
SG (1) SG191840A1 (es)
TW (1) TW201309655A (es)
WO (1) WO2012103297A1 (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014172190A1 (en) 2013-04-15 2014-10-23 E. I. Du Pont De Nemours And Company Fungicidal amides
JP6688503B2 (ja) * 2014-11-21 2020-04-28 大学共同利用機関法人自然科学研究機構 医薬用組成物
CN107801397B (zh) * 2015-02-13 2021-07-30 达纳－法伯癌症研究所公司 Lrrk2抑制剂及其制备和使用方法
CN105017046A (zh) * 2015-07-15 2015-11-04 上海博康精细化工有限公司 一种4-环丙胺基丁酸乙酯的制备方法
CN106366093B (zh) * 2015-07-21 2020-08-18 广州再极医药科技有限公司 稠环嘧啶类化合物、中间体、其制备方法、组合物和应用
JP7335242B2 (ja) * 2017-11-27 2023-08-29 エフ． ホフマン－ラ ロシュ アーゲー ピリミジン誘導体
JP7248255B2 (ja) * 2019-01-29 2023-03-29 シャンドン スアンズ ファーマ カンパニー，リミテッド ヘキソングルコキナーゼ阻害剤およびその使用
CN112028839B (zh) * 2020-09-30 2022-04-12 中国海洋大学 一种医药中间体环烷烃并嘧啶二酮化合物的合成方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1698627A1 (en) 2000-09-15 2006-09-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US20100311965A1 (en) 2007-12-28 2010-12-09 Carna Biosciences Inc. 2-aminoquinazoline derivative
TW201030002A (en) * 2009-01-16 2010-08-16 Bristol Myers Squibb Co Bicyclic compounds for the reduction of beta-amyloid production
US8637525B2 (en) * 2009-07-31 2014-01-28 Bristol-Myers Squibb Company Compounds for the reduction of beta-amyloid production
TWI468402B (zh) * 2009-07-31 2015-01-11 必治妥美雅史谷比公司 降低β－類澱粉生成之化合物

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Publication number Publication date
MX2013008699A (es) 2013-08-21
EP2668168A1 (en) 2013-12-04
SG191840A1 (en) 2013-08-30
EA201391097A1 (ru) 2013-11-29
JP2014503590A (ja) 2014-02-13
CN103328451B (zh) 2015-06-10
EP2668168B1 (en) 2017-03-01
CN103328451A (zh) 2013-09-25
WO2012103297A1 (en) 2012-08-02
TW201309655A (zh) 2013-03-01
IL226677A (en) 2014-11-30
CA2825906A1 (en) 2012-08-02
KR20140014152A (ko) 2014-02-05
AU2012211301A1 (en) 2013-09-19
US8710061B2 (en) 2014-04-29
BR112013018298A2 (pt) 2016-11-16
JP5908499B2 (ja) 2016-04-26
AU2012211301B2 (en) 2016-02-25
US20130030011A1 (en) 2013-01-31

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