AR076723A1 - Compuestos que contienen acido carboxilico, derivados de los mismos y su uso como moduladores de la gamma secretasa - Google Patents

Compuestos que contienen acido carboxilico, derivados de los mismos y su uso como moduladores de la gamma secretasa

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Publication number
AR076723A1
AR076723A1 ARP100101908A ARP100101908A AR076723A1 AR 076723 A1 AR076723 A1 AR 076723A1 AR P100101908 A ARP100101908 A AR P100101908A AR P100101908 A ARP100101908 A AR P100101908A AR 076723 A1 AR076723 A1 AR 076723A1
Authority
AR
Argentina
Prior art keywords
alkyl
cyclyl
independently
optionally substituted
haloalkyl
Prior art date
Application number
ARP100101908A
Other languages
English (en)
Original Assignee
Biogen Idec Inc
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 Biogen Idec Inc filed Critical Biogen Idec Inc
Publication of AR076723A1 publication Critical patent/AR076723A1/es

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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
    • A61K31/435—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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/34—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40—Unsaturated compounds
    • C07C59/42—Unsaturated compounds containing hydroxy or O-metal groups
    • C07C59/56—Unsaturated compounds containing hydroxy or O-metal groups containing halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40—Unsaturated compounds
    • C07C59/58—Unsaturated compounds containing ether groups, groups, groups, or groups
    • C07C59/64—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings
    • C07C59/66—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings the non-carboxylic part of the ether containing six-membered aromatic rings
    • C07C59/68—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings the non-carboxylic part of the ether containing six-membered aromatic rings the oxygen atom of the ether group being bound to a non-condensed six-membered aromatic ring
    • 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
    • C07D211/06—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 no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/10—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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/14—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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • 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
    • C07D211/06—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 no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/34—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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole 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
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • C07D263/26—Oxygen atoms attached in position 2 with hetero atoms or acyl radicals directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/30—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biomedical Technology (AREA)
  • Medicinal Chemistry (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Se describen en la presente compuestos que modulan la gamma secretasa (por ejemplo, alteran el patron de desdoblamiento de gamma secretasa). También se describen composiciones farmacéuticas, métodos para modular la actividad de gamma secretasa, y métodos para tratar la enfermedad de Alzheimer usando los compuestos descritos en la presente. Reivindicacion 1: Un compuesto de la formula (1) caracterizado porque: m es 0, 1, 2, 3 o 4; n es 0, 1 o 2; W es -COOH, o un bioisostero o imitador de ácido carboxílico; Z es N, NR16, CR17 o CR1819; cada R1 y R2 es independientemente H, alquilo C1-6, alquenilo C2-6, halo, haloalquilo, alcoxi C1-6, ciclilo o ciclilalquilo; o R1 y R2, junto con el carbono al cual se enlazan, pueden formar un anillo de 3-7 miembros saturado o no saturado, opcionalmente sustituido; en donde ya sea R1 o R2 se toman opcionalmente junto con R8a o R9a para formar un anillo de 3-7 miembros saturado o no saturado, opcionalmente sustituido; A es un enlace, NR10, O, S, alquilenilo, amida, éster, carbamato, urea, tiourea o sulfonilurea; B es N u O; R3 es arilo, heteroarilo, ciclilo o heterociclilo, cada uno de los cuales está opcionalmente sustituido con 1-3 R11; cada R4 y R5 es independientemente H, alquilo C1-8, haloalquilo, ciclilo, ciclilalquilo, arilo o heteroarilo, cada uno de los cuales está opcionalmente sustituido con 1-3 R12; o R4 y R5, junto con el carbono al cual se enlazan, pueden formar un anillo de 3-7 miembros que está opcionalmente saturado o no saturado, y sustituido o no sustituido; R6 y R7 son cada uno independientemente H, alquilo C1-8, ciclilo, arilo, heteroarilo, ciclilalquilo o arilalquilo, cada uno de los cuales está opcionalmente sustituido con 1-3 R13; en donde cuando B es O, R7 está ausente; en donde cuando B es N, R6 y R7, junto con el nitrogeno al cual se enlazan, pueden formar un anillo de 3-7 miembros que está opcionalmente saturado o no saturado, y sustituido o no sustituido con 1-3 R14; y en donde R4 y R6, junto con los átomos a los cuales se enlazan, pueden formar un anillo de 3-7 miembros que está opcionalmente saturado o no saturado, y sustituido o no sustituido con 1-3 R15; R8a, R8b, R9a y R9b son cada uno independientemente H, alquilo C1-6, hidroxi, halo, haloalquilo, o CN; R10 es hidrogeno, alquilo C1-6 o haloalquilo; cada R11, R12, R13, R14 y R15 es independientemente alquilo C1-6, alquenilo C1-6, alquinilo C1-6, halo, haloalquilo, alcoxi, haloalcoxi, arilo, heteroarilo, ciclilo, heterociclilo, hidroxi, arilalquilo, heteroarilalquilo, ciclilalquilo, heterociclilalquilo, carboxilato, ciano, oxo, nitro, amino, alquilamino, dialquilamino, mercapto, tioalquilo, ariloxi, tioalcoxi, amido, SO3H, sulfato, S(O)NH2, S(O)2NH2, fosfato o acilo, cada uno de los cuales está opcionalmente sustituido; en donde dos R11, R12, R13, R14 o R15, junto con los átomos a los cuales se enlazan, pueden formar un anillo de 3-7 miembros, saturado o no saturado, y opcionalmente sustituido; y cada R16, R17, R18, y R19 es independientemente H, alquilo C1-6, hidroxi, halo, haloalquilo o CN; cada ----- independientemente representa la presencia o ausencia de un enlace; en donde cuando ----- representa la presencia de un enlace al carbono al cual R8b se enlaza, R8b está ausente; y en donde cuando ----- representa la presencia de un enlace al carbono al cual R9b se enlaza, R9b está ausente; y en donde cuando ----- representa la presencia de un enlace a Z, entonces Z es N o CR17; o una sal, solvato, hidrato, profármaco, tautomero, enantiomero, estereoisomero, análogo o derivado farmacéuticamente aceptable del mismo, incluyendo mezclas de los mismos en cualquiera de las relaciones.
ARP100101908A 2009-05-29 2010-05-31 Compuestos que contienen acido carboxilico, derivados de los mismos y su uso como moduladores de la gamma secretasa AR076723A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US18244809P 2009-05-29 2009-05-29
US30279610P 2010-02-09 2010-02-09

Publications (1)

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AR076723A1 true AR076723A1 (es) 2011-06-29

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ID=43223116

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ARP100101908A AR076723A1 (es) 2009-05-29 2010-05-31 Compuestos que contienen acido carboxilico, derivados de los mismos y su uso como moduladores de la gamma secretasa

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Country Link
AR (1) AR076723A1 (es)
TW (1) TW201106863A (es)
WO (1) WO2010138901A1 (es)

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US8883839B2 (en) 2010-08-13 2014-11-11 Abbott Laboratories Tetraline and indane derivatives, pharmaceutical compositions containing them, and their use in therapy
US8846743B2 (en) 2010-08-13 2014-09-30 Abbott Laboratories Aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy
US8877794B2 (en) * 2010-08-13 2014-11-04 Abbott Laboratories Phenalkylamine derivatives, pharmaceutical compositions containing them, and their use in therapy
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US9051280B2 (en) 2010-08-13 2015-06-09 AbbVie Deutschland GmbH & Co. KG Tetraline and indane derivatives, pharmaceutical compositions containing them, and their use in therapy
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JP2014533675A (ja) 2011-11-18 2014-12-15 アッヴィ・ドイチュラント・ゲー・エム・ベー・ハー・ウント・コー・カー・ゲー Ｎ置換アミノベンゾシクロヘプテン、アミノテトラリン、アミノインダンおよびフェナルキルアミン誘導体、これらを含有する医薬組成物、および治療におけるこれらの使用
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AU2013227266A1 (en) * 2012-02-28 2014-10-02 Piramal Enterprises Limited Phenyl alkanoic acid derivatives as GPR agonists
US9656955B2 (en) 2013-03-15 2017-05-23 Abbvie Inc. Pyrrolidine derivatives, pharmaceutical compositions containing them, and their use in therapy
US9650334B2 (en) 2013-03-15 2017-05-16 Abbvie Inc. Pyrrolidine derivatives, pharmaceutical compositions containing them, and their use in therapy
AU2014336153A1 (en) 2013-10-17 2016-04-28 AbbVie Deutschland GmbH & Co. KG Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy
JP2016533375A (ja) 2013-10-17 2016-10-27 アッヴィ・ドイチュラント・ゲー・エム・ベー・ハー・ウント・コー・カー・ゲー アミノテトラリン誘導体およびアミノインダン誘導体、これらを含有する医薬組成物、および治療におけるこれらの使用
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TW201920081A (zh) 2017-07-11 2019-06-01 美商維泰克斯製藥公司 作為鈉通道調節劑的羧醯胺
HUE057970T2 (hu) 2018-03-08 2022-06-28 Incyte Corp Aminopirazindiol-vegyületek mint PI3K-Y inhibitorok
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
HUE064554T2 (hu) * 2018-09-03 2024-03-28 Hoffmann La Roche Bicikluszos heteroaril származékok
CN111269125A (zh) * 2018-12-05 2020-06-12 上海复星星泰医药科技有限公司 一种艾乐替尼中间体及其制备方法
CN115124511B (zh) * 2022-07-28 2023-09-26 中国人民解放军北部战区总医院 他克林衍生物及其制备方法与作为cdk2/9抑制剂的应用

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Also Published As

Publication number Publication date
WO2010138901A1 (en) 2010-12-02
TW201106863A (en) 2011-03-01

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