AR088567A1 - Derivados de piridopiridazina - Google Patents

Derivados de piridopiridazina

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Publication number
AR088567A1
AR088567A1 ARP120104039A ARP120104039A AR088567A1 AR 088567 A1 AR088567 A1 AR 088567A1 AR P120104039 A ARP120104039 A AR P120104039A AR P120104039 A ARP120104039 A AR P120104039A AR 088567 A1 AR088567 A1 AR 088567A1
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Argentina
Prior art keywords
alkyl
substituted
alkoxy
cr22r23
alkyl substituted
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ARP120104039A
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English (en)
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Astex Therapeutics Ltd
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Publication of AR088567A1 publication Critical patent/AR088567A1/es

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    • 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
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Abstract

Composiciones farmacéuticas que comprenden dichos compuestos, procesos para la preparación de dichos compuestos y uso de dichos compuestos en el tratamiento de enfermedades, por ejemplo, cáncer. Reivindicación 1: Un compuesto de la fórmula (1) ó (2), incluyendo cualquiera de sus formas tautoméricas o estereoquímicamente isoméricas, en donde cada R² está seleccionado, de modo independiente, de hidroxilo, halógeno, ciano, alquilo C₁₋₄, alquenilo C₂₋₄, alquinilo C₂₋₄, alcoxi C₁₋₄, hidroxialquilo C₁₋₄, hidroxialcoxi C₁₋₄, haloalquilo C₁₋₄, haloalcoxi C₁₋₄, hidroxihaloalquilo C₁₋₄, hidroxihaloalcoxi C₁₋₄, alcoxi C₁₋₄-alquilo C₁₋₄, haloalcoxi C₁₋₄-alquilo C₁₋₄, alcoxi C₁₋₄-alquilo C₁₋₄, en donde cada alquilo C₁₋₄ puede estar opcionalmente sustituido con uno o dos grupos hidroxilo, hidroxihaloalcoxi C₁₋₄-alquilo C₁₋₄, R¹³, alquilo C₁₋₄ sustituido con R¹³, alquilo C₁₋₄ sustituido con -C(=O)-R¹³, alcoxi C₁₋₄ sustituido con R¹³, alcoxi C₁₋₄ sustituido con -C(=O)-R¹³, -C(=O)-R¹³, alquilo C₁₋₄ sustituido con -NR⁷R⁸, alquilo C₁₋₄ sustituido con -C(=O)-NR⁷R⁸, alcoxi C₁₋₄ sustituido con -NR⁷R⁸, alcoxi C₁₋₄ sustituido con -C(=O)-NR⁷R⁸, -NR⁷R⁸ y -C(=O)-NR⁷R⁸; o cuando dos grupos R² están unidos a átomos de carbono adyacentes, se pueden tomar juntos para formar un radical de la fórmula: -O-(C(R¹⁷)₂)ₚ-O-; -X-CH=CH-; o -X-CH=N-; en donde R¹⁷ representa hidrógeno o flúor, p representa 1 ó 2 y X representa O ó S; Y representa -CR¹⁸=N-OR¹⁹ o -E-D; D representa un carbociclilo monocíclico o bicíclico de 3 a 12 miembros del anillo o un heterociclilo monocíclico o bicíclico de 3 a 12 miembros del anillo que contiene al menos un heteroátomo seleccionado de N, O ó S, en donde dicho carbociclilo y heterociclilo puede estar opcionalmente sustituido con uno o varios (por ejemplo, 1, 2 ó 3) grupos R¹; E representa un enlace, -(CR²²R²³)ₙ-, alquen C₂₋₄-diílo opcionalmente sustituido con R²², alquin C₂₋₄-diílo opcionalmente sustituido con R²², -CO-(CR²²R²³)ₛ-, -(CR²²R²³)ₛ-CO-, -NR²²-(CR²²R²³)ₛ-, -(CR²²R²³)ₛ-NR²²-, -O-(CR²²R²³)ₛ-, -(CR²²R²³)ₛ-O-, S(O)ₘ-(CR²²R²³)ₛ, -(CR²²R²³)ₛ-S(O)ₘ, -(CR²²R²³)ₛ-CO-NR²²-(CR²²R²³)ₛ- o -(CR²²R²³)ₛ-NR²²-CO-(CR²²R²³)ₛ-; R¹ representa hidrógeno, halo, ciano, alquilo C₁₋₆, alcoxi C₁₋₆, -C(=O)-O-alquilo C₁₋₆, alquenilo C₂₋₄, hidroxialquilo C₁₋₆, haloalquilo C₁₋₆, hidroxihaloalquilo C₁₋₆, cianoalquilo C₁₋₆, alcoxi C₁₋₆-alquilo C₁₋₆, en donde cada alquilo C₁₋₆ puede estar opcionalmente sustituido con uno o dos grupos hidroxilo, -NR⁴R⁵, alquilo C₁₋₆ sustituido con -O-C(=O)-alquilo C₁₋₆, alquilo C₁₋₆ sustituido con -NR⁴R⁵, -C(=O)-NR⁴R⁵, -C(=O)-alquil C₁₋₆-NR⁴R⁵, alquilo C₁₋₆ sustituido con -C(=O)-NR⁴R⁵, -S(=O)₂-alquilo C₁₋₆, -S(=O)₂-haloalquilo C₁₋₆, -S(=O)₂-NR¹⁴R¹⁵, alquilo C₁₋₆ sustituido con -S(=O)₂-alquilo C₁₋₆, alquilo C₁₋₆ sustituido con -S(=O)₂-haloalquilo C₁₋₆, alquilo C₁₋₆ sustituido con -S(=O)₂-NR¹⁴R¹⁵, alquilo C₁₋₆ sustituido con -NH-S(=O)₂-alquilo C₁₋₆, alquilo C₁₋₆ sustituido con -NH-S(=O)₂-haloalquilo C₁₋₆, alquilo C₁₋₆ sustituido con -NR¹²-S(O)₂-NR¹⁴R¹⁵, R⁶, alquilo C₁₋₆ sustituido con R⁶, -C(=O)-R⁶, alquilo C₁₋₆ sustituido con -C(=O)-R⁶, hidroxialquilo C₁₋₆ sustituido con R⁶, alquilo C₁₋₆ sustituido con -Si(CH₃)₃, alquilo C₁₋₆ sustituido con -P(=O)(OH)₂ o alquilo C₁₋₆ sustituido con -P(=O)(O-alquilo C₁₋₆)₂; R³ representa hidroxilo, alcoxi C₁₋₆, hidroxialcoxi C₁₋₆, alcoxi C₁₋₆ sustituido con -NR¹⁰R¹¹, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquilo C₁₋₆ opcionalmente sustituido con -O-C(=O)-alquilo C₁₋₆, hidroxialquilo C₁₋₆ opcionalmente sustituido con -O-C(=O)-alquilo C₁₋₆, hidroxialquenilo C₂₋₆, hidroxialquinilo C₂₋₆, hidroxihaloalquilo C₁₋₆, cianoalquilo C₁₋₆, alquilo C₁₋₆ sustituido con carboxilo, alquilo C₁₋₆ sustituido con -C(=O)-alquilo C₁₋₆, alquilo C₁₋₆ sustituido con -C(=O)-O-alquilo C₁₋₆, alquilo C₁₋₆ sustituido con alcoxi C₁₋₆-alquil C₁₋₆-O-C(=O)-, alquilo C₁₋₆ sustituido con alcoxi C₁₋₆-alquil C₁₋₆-C(=O)-, alquilo C₁₋₆ sustituido con -O-C(=O)-alquilo C₁₋₆, alcoxi C₁₋₆-alquilo C₁₋₆, en donde cada alquilo C₁₋₆ puede estar opcionalmente sustituido con uno o dos grupos hidroxilo o con -O-C(=O)-alquilo C₁₋₆, alquenilo C₂₋₆ sustituido con alcoxi C₁₋₆, alquinilo C₂₋₆ sustituido con alcoxi C₁₋₆, alquilo C₁₋₆ sustituido con R⁹ y opcionalmente sustituido con -O-C(=O)-alquilo C₁₋₆, alquilo C₁₋₆ sustituido con -C(=O)-R⁹, alquilo C₁₋₆ sustituido con hidroxilo y R⁹, alquenilo C₂₋₆ sustituido con R⁹, alquinilo C₂₋₆ sustituido con R⁹, alquilo C₁₋₆ sustituido con -NR¹⁰R¹¹, alquenilo C₂₋₆ sustituido con -NR¹⁰R¹¹, alquinilo C₂₋₆ sustituido con -NR¹⁰R¹¹, alquilo C₁₋₆ sustituido con hidroxilo y -NR¹⁰R¹¹, alquilo C₁₋₆ sustituido con uno o dos halógenos y -NR¹⁰R¹¹, -alquil C₁₋₆-C(R¹²)=N-O-R¹², alquilo C₁₋₆ sustituido con -C(=O)-NR¹⁰R¹¹, alquilo C₁₋₆ sustituido con -O-C(=O)-NR¹⁰R¹¹, -S(=O)₂-alquilo C₁₋₆, -S(=O)₂-haloalquilo C₁₋₆, -S(=O)₂-NR¹⁴R¹⁵, alquilo C₁₋₆ sustituido con -S(=O)₂-alquilo C₁₋₆, alquilo C₁₋₆ sustituido con -S(=O)₂-haloalquilo C₁₋₆, alquilo C₁₋₆ sustituido con -S(=O)₂-NR¹⁴R¹⁵, alquilo C₁₋₆ sustituido con -NR¹²-S(=O)₂-alquilo C₁₋₆, alquilo C₁₋₆ sustituido con -NH-S(=O)₂-haloalquilo C₁₋₆, alquilo C₁₋₆ sustituido con -NR¹²-S(=O)₂-NR¹⁴R¹⁵, R¹³, alquilo C₁₋₆ sustituido con -P(=O)(OH)₂ o alquilo C₁₋₆ sustituido con -P(=O)(O-alquilo C₁₋₆)₂; R⁴ y R⁵ representan cada uno, de modo independiente, hidrógeno, alquilo C₁₋₆, alquilo C₁₋₆ sustituido con -NR¹⁴R¹⁵, hidroxialquilo C₁₋₆, haloalquilo C₁₋₆, hidroxihaloalquilo C₁₋₆, alcoxi C₁₋₆-alquilo C₁₋₆, en donde cada alquilo C₁₋₆ puede estar opcionalmente sustituido con uno o dos grupos hidroxilo, -S(=O)₂-alquilo C₁₋₆, -S(=O)₂-haloalquilo C₁₋₆, -S(=O)₂-NR¹⁴R¹⁵, -C(=O)-NR¹⁴R¹, -C(=O)-O-alquilo C₁₋₆, -C(=O)-R¹³, alquilo C₁₋₆ sustituido con -S(=O)₂-alquilo C₁₋₆, alquilo C₁₋₆ sustituido con -S(=O)₂-haloalquilo C₁₋₆, alquilo C₁₋₆ sustituido con -S(=O)₂-NR¹⁴R¹⁵, alquilo C₁₋₆ sustituido con -NH-S(=O)₂-alquilo C₁₋₆, alquilo C₁₋₆ sustituido con -NH-S(=O)₂-haloalquilo C₁₋₆, alquilo C₁₋₆ sustituido con -NH-S(=O)₂-NR¹⁴R¹⁵, R¹³ o alquilo C₁₋₆ sustituido con R¹³; R⁶ representa
ARP120104039A 2011-10-28 2012-10-26 Derivados de piridopiridazina AR088567A1 (es)

Applications Claiming Priority (2)

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US201161552888P 2011-10-28 2011-10-28
GBGB1118656.6A GB201118656D0 (en) 2011-10-28 2011-10-28 New compounds

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AR088567A1 true AR088567A1 (es) 2014-06-18

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US (2) US9309242B2 (es)
EP (1) EP2776435B1 (es)
JP (1) JP6169583B2 (es)
KR (1) KR102066496B1 (es)
CN (1) CN104011051B (es)
AP (1) AP4060A (es)
AR (1) AR088567A1 (es)
AU (1) AU2012328170B2 (es)
BR (1) BR112014010206B8 (es)
CA (1) CA2853390C (es)
CL (1) CL2014001065A1 (es)
CO (1) CO6940422A2 (es)
CR (1) CR20140190A (es)
DK (1) DK2776435T3 (es)
EA (1) EA027563B1 (es)
EC (1) ECSP14013325A (es)
ES (1) ES2688868T3 (es)
GB (1) GB201118656D0 (es)
HR (1) HRP20181533T1 (es)
IL (1) IL232083B (es)
IN (1) IN2014MN00948A (es)
JO (1) JO3419B1 (es)
LT (1) LT2776435T (es)
MX (1) MX353654B (es)
MY (1) MY185666A (es)
NI (1) NI201400032A (es)
SG (1) SG11201401055XA (es)
SI (1) SI2776435T1 (es)
TW (1) TWI602814B (es)
UA (1) UA111386C2 (es)
UY (1) UY34418A (es)
WO (1) WO2013061080A1 (es)

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GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
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KR20180052631A (ko) 2015-09-23 2018-05-18 얀센 파마슈티카 엔.브이. 비-헤테로아릴 치환된 1,4-벤조디아제핀 및 암의 치료를 위한 이의 용도
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