AR104208A1 - Compuestos bicíclicos como inhibidores de autotaxina (atx) - Google Patents

Compuestos bicíclicos como inhibidores de autotaxina (atx)

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Publication number
AR104208A1
AR104208A1 ARP160100947A ARP160100947A AR104208A1 AR 104208 A1 AR104208 A1 AR 104208A1 AR P160100947 A ARP160100947 A AR P160100947A AR P160100947 A ARP160100947 A AR P160100947A AR 104208 A1 AR104208 A1 AR 104208A1
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Argentina
Prior art keywords
substituted
alkyl
cycloalkyl
haloalkyl
haloalkoxy
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Application number
ARP160100947A
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English (en)
Inventor
Lee Satz Alexander
Mattei Patrizio
E Martin Rainer
Kuratli Christoph
Hunziker Daniel
Hert Jrme
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Hoffmann La Roche
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Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR104208A1 publication Critical patent/AR104208A1/es

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    • 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
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
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    • 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
    • A61P27/00—Drugs for disorders of the senses
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • 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
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D413/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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    • 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

Abstract

La solicitud proporciona compuestos que tienen la fórmula general (1) en la que R¹, R², R³, R⁴, R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁰, R¹², R¹³, R¹⁴, A¹, A², A³, n y m son tal como se describe en el presente documento. Reivindicación 1: Compuestos de fórmula (1), R¹ es hidroxialquilo, dihidroxialquilo, hidroxicicloalquilo, alcoxi, haloalcoxi, alcoxialcoxialquilo, alcoxialquilo, haloalcoxialquilo, alquilo, haloalquilo, alquilsulfonilo, haloalquilsulfonilo, aminosulfonilalquilo, cianoalquilo, nitratoalquilo cicloalquilo sustituido, cicloalquilalquilo sustituido, hidroxialquilo, dihidroxialquilo, heteroarilo sustituido, heterocicloalquilo sustituido o arilo sustituido, en el que cicloalquilo sustituido, cicloalquilalquilo sustituido, heteroarilo sustituido, heterocicloalquilo sustituido y arilo sustituido se sustituyen con uno a tres sustituyentes seleccionados entre H, amino, alquilo, haloalquilo, alcoxi, haloalcoxi, alquilcarbonilo, carboxi, halógeno y ciano; R² y R³ se seleccionan independientemente entre H, alquilo y cicloalquilo; o R² y R³ junto con el carbono al que están unidos forman un cicloalquilo; A¹ es -CH-, -C(OH)- o -N-; A² es -C(O)-, -C(O)CH₂-, -CH₂-, -NR¹¹C(O)-, -NR¹¹C(O)CH₂-, -S(O)₂-; A³ es -CR⁸- o -N-; uno de R⁴ y R⁵ es H o alquilo y el otro es H, alcoxialquilo, alcoxicarbonilalquilo, haloalcoxicabonilalquilo, alquilo, haloalquilo, carboxialquilo, cicloalquilo o aminocarbonilalquilo sustituido, en el que el aminocarbonilalquilo sustituido se sustituye en el átomo de nitrógeno por dos sustituyentes seleccionados independientemente entre H, alquilo, cicloalquilo y fenilo sustituido, en el que el fenilo sustituido se sustituye con uno a tres sustituyentes seleccionados independientemente entre H, alquilo, haloalquilo y cicloalquilo; o R⁴ y R⁵ junto con los átomos de nitrógeno y carbono a los que están unidos forman un heterocicloalquilo; R⁶ es H o alquilo; R⁷, R⁸ y R⁹ son independientemente H, alquilo, cicloalquilo, halógeno o ciano; R¹⁰ es arilo sustituido o heteroarilo sustituido, en el que el arilo sustituido o el heteroarilo sustituido se sustituyen con uno a tres sustituyentes seleccionados entre H, alquilo, haloalquilo, alcoxi, haloalcoxi, halógeno, nitro, ciano, alquilsulfonilo, haloalquilsulfonilo y pentafluoro-l⁶-sulfanilo; R¹¹ es H, alquilo o cicloalquilo; R¹² y R¹³ son ambos H o R¹² y R¹³ juntos forman -(CH₂)ₚ-; R¹⁴ es H, alquilo o hidroxi; n, m y p son independientemente cero, 1 ó 2; o sales farmacéuticamente aceptables.
ARP160100947A 2015-04-10 2016-04-08 Compuestos bicíclicos como inhibidores de autotaxina (atx) AR104208A1 (es)

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EP15163133 2015-04-10

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AR104208A1 true AR104208A1 (es) 2017-07-05

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US (2) US10676446B2 (es)
EP (1) EP3280707B1 (es)
JP (1) JP6774960B2 (es)
KR (1) KR20170132766A (es)
CN (1) CN107428754B (es)
AR (1) AR104208A1 (es)
AU (1) AU2016245914B2 (es)
BR (1) BR112017021803A2 (es)
CA (1) CA2975664A1 (es)
CL (1) CL2017002452A1 (es)
CO (1) CO2017007635A2 (es)
CR (1) CR20170455A (es)
HK (1) HK1245249A1 (es)
IL (1) IL253588B (es)
MA (1) MA41898A (es)
MX (1) MX2017013036A (es)
PE (1) PE20171737A1 (es)
PH (1) PH12017501825B1 (es)
RU (1) RU2017135520A (es)
SG (2) SG10201909485YA (es)
TW (1) TW201710247A (es)
UA (1) UA121133C2 (es)
WO (1) WO2016162390A1 (es)

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EA036630B1 (ru) 2012-09-25 2020-12-02 Ф. Хоффманн-Ля Рош Аг Бициклические производные
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ES2753549T3 (es) 2014-03-26 2020-04-13 Hoffmann La Roche Compuestos bicíclicos como inhibidores de la producción de autotaxina (ATX) y ácido lisofosfatídico (LPA)
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MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
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BR112017026682A2 (pt) 2015-09-24 2018-08-14 Hoffmann La Roche novos compostos bicíclicos como inibidores de dupla ação de atx/ca
MX2018001890A (es) 2015-09-24 2018-06-20 Hoffmann La Roche Compuestos biciclicos como inhibidores de autotaxina (atx).
KR20190129924A (ko) 2017-03-16 2019-11-20 에프. 호프만-라 로슈 아게 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서 유용한 헤테로환형 화합물
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