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AR076723A1 - COMPOUNDS CONTAINING CARBOXYL ACID, DERIVATIVES OF THE SAME AND ITS USE AS MODULATORS OF THE GAMMA SECRETASA - Google Patents

COMPOUNDS CONTAINING CARBOXYL ACID, DERIVATIVES OF THE SAME AND ITS USE AS MODULATORS OF THE GAMMA SECRETASA

Info

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
Spanish (es)
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/en

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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

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  • 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.Compounds that modulate gamma secretase (for example, alter the pattern of gamma secretase cleavage) are described herein. Pharmaceutical compositions, methods for modulating gamma secretase activity, and methods for treating Alzheimer's disease using the compounds described herein are also described. Claim 1: A compound of the formula (1) characterized in that: m is 0, 1, 2, 3 or 4; n is 0, 1 or 2; W is -COOH, or a carboxylic acid bioisotero or imitator; Z is N, NR16, CR17 or CR1819; each R1 and R2 is independently H, C1-6 alkyl, C2-6 alkenyl, halo, haloalkyl, C1-6 alkoxy, cyclyl or cyclyl alkyl; or R1 and R2, together with the carbon to which they are attached, can form a saturated or unsaturated 3-7 membered ring, optionally substituted; wherein either R1 or R2 are optionally taken together with R8a or R9a to form a saturated or unsaturated 3-7 membered ring, optionally substituted; A is a bond, NR10, O, S, alkylenyl, amide, ester, carbamate, urea, thiourea or sulfonylurea; B is N or O; R3 is aryl, heteroaryl, cyclyl or heterocyclyl, each of which is optionally substituted with 1-3 R11; each R4 and R5 is independently H, C1-8 alkyl, haloalkyl, cyclyl, cyclylalkyl, aryl or heteroaryl, each of which is optionally substituted with 1-3 R12; or R4 and R5, together with the carbon to which they bind, can form a 3-7 membered ring that is optionally saturated or unsaturated, and substituted or unsubstituted; R6 and R7 are each independently H, C1-8 alkyl, cyclyl, aryl, heteroaryl, cyclyl alkyl or arylalkyl, each of which is optionally substituted with 1-3 R13; where when B is O, R7 is absent; wherein when B is N, R6 and R7, together with the nitrogen to which they bind, they can form a 3-7 membered ring that is optionally saturated or unsaturated, and substituted or unsubstituted with 1-3 R14; and wherein R4 and R6, together with the atoms to which they bind, can form a 3-7 membered ring that is optionally saturated or unsaturated, and substituted or unsubstituted with 1-3 R15; R8a, R8b, R9a and R9b are each independently H, C1-6 alkyl, hydroxy, halo, haloalkyl, or CN; R10 is hydrogen, C1-6 alkyl or haloalkyl; each R11, R12, R13, R14 and R15 is independently C1-6 alkyl, C1-6 alkenyl, C1-6 alkynyl, halo, haloalkyl, alkoxy, haloalkoxy, aryl, heteroaryl, cyclyl, heterocyclyl, hydroxy, arylalkyl, heteroarylalkyl, cyclylalkyl , heterocyclylalkyl, carboxylate, cyano, oxo, nitro, amino, alkylamino, dialkylamino, mercapto, thioalkyl, aryloxy, thioalkoxy, amido, SO3H, sulfate, S (O) NH2, S (O) 2NH2, phosphate or acyl, each of which is optionally substituted; wherein two R11, R12, R13, R14 or R15, together with the atoms to which they bind, can form a 3-7 membered ring, saturated or unsaturated, and optionally substituted; and each R16, R17, R18, and R19 is independently H, C1-6 alkyl, hydroxy, halo, haloalkyl or CN; Each ----- independently represents the presence or absence of a link; wherein when ----- represents the presence of a carbon bond to which R8b binds, R8b is absent; and where when ----- represents the presence of a carbon bond to which R9b binds, R9b is absent; and where when ----- represents the presence of a link to Z, then Z is N or CR17; or a salt, solvate, hydrate, prodrug, tautomer, enantiomer, stereoisomer, analogue or pharmaceutically acceptable derivative thereof, including mixtures thereof in any of the ratios.

ARP100101908A 2009-05-29 2010-05-31 COMPOUNDS CONTAINING CARBOXYL ACID, DERIVATIVES OF THE SAME AND ITS USE AS MODULATORS OF THE GAMMA SECRETASA AR076723A1 (en)

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US18244809P 2009-05-29 2009-05-29
US30279610P 2010-02-09 2010-02-09

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AR (1) AR076723A1 (en)
TW (1) TW201106863A (en)
WO (1) WO2010138901A1 (en)

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