AR101566A2 - PHARMACEUTICAL COMPOSITION OF HETEROBICYCLIC COMPOUNDS CONTAINING NITROGEN - Google Patents

PHARMACEUTICAL COMPOSITION OF HETEROBICYCLIC COMPOUNDS CONTAINING NITROGEN

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Publication number
AR101566A2
AR101566A2 ARP150102632A ARP150102632A AR101566A2 AR 101566 A2 AR101566 A2 AR 101566A2 AR P150102632 A ARP150102632 A AR P150102632A AR P150102632 A ARP150102632 A AR P150102632A AR 101566 A2 AR101566 A2 AR 101566A2
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AR
Argentina
Prior art keywords
group
atom
optionally substituted
alkyl group
halogen atom
Prior art date
Application number
ARP150102632A
Other languages
Spanish (es)
Inventor
Kawaguchi Takayuki
Akatsuka Hidenori
Yamamoto Yasuo
Iijima Toru
Original Assignee
Mitsubishi Tanabe Pharma Corp
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 Mitsubishi Tanabe Pharma Corp filed Critical Mitsubishi Tanabe Pharma Corp
Publication of AR101566A2 publication Critical patent/AR101566A2/en

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  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La presente solicitud hace referencia a una composición farmacéutica de un compuesto, útil como un agente que modula el receptor mineralocorticoide, útil como agente para la prevención y/o tratamiento de enfermedades cardiovasculares y de riñón, o una sal aceptable para uso farmacéutico del mismo. Reivindicación 1: Una composición farmacéutica caracterizada porque comprende como un ingrediente activo un compuesto de la fórmula (1) caracterizado porque el anillo A es un anillo de benceno estando opcionalmente sustituido por uno a tres grupo(s) diferentes a R¹, seleccionados de (a) un átomo de halógeno, (b) un grupo alquilo C₁₋₆ (dicho grupo alquilo estando opcionalmente sustituido por uno a tres grupo(s) seleccionados de un átomo de halógeno, un grupo hidroxilo y un grupo alcoxi C₁₋₆), (c) un grupo hidroxilo, (d) un grupo alcoxi C₁₋₆, (e) un grupo amino, (f) un grupo ciano, (i) un grupo alquenilo C₂₋₁₂, (j) un grupo alcanoilo C₁₋₇ y (k) un grupo cicloalquilo C₃₋₁₀; R¹ es un grupo de la fórmula: RᵃSO₂NH-, RᵃSO₂NH-CH₂- o (Rᵇ)(Rᶜ)NSO₂-, y dicho R¹ sustituye 1 posición 7- de la porciones 1-4-benzoxazina, 1-4-benzotiazina o tetrahidroquinoxalina; Rᵃ es un grupo alquilo C₁₋₆, un grupo cicloalquilo C₃₋₁₀, un grupo amino sustituido en forma opcional con uno o dos grupo(s) alquilo C₁₋₆, un grupo arilo de 6- a 10- miembros monocíclico o bicíclico, o un grupo heteroarilo de 5- a 10- miembros monocíclico o bicíclico conteniendo uno o dos heteroátomo(s) seleccionados de un átomo de oxígeno, un átomo de azufre y un átomo de nitrógeno; Rᵇ y Rᶜ son iguales o diferentes y son cada uno un átomo de hidrógeno, un grupo alquilo C₁₋₆ o un grupo cicloalquilo C₃₋₁₀; uno de R² y R³ es un átomo de hidrogeno, un átomo de halógeno o un grupo alquilo C₁₋₆ y el otro es un átomo de hidrógeno, un grupo alquilo C₁₋₆, un grupo alcoxicarbonilo C₁₋₆; o un grupo fenilo, o R² y R³ se unen entre sí con el átomo de carbono contiguo para formar un grupo cicloalquilo C₃₋₁₀; X es un átomo de oxígeno, un átomo de azufre, o un grupo de la fórmula: -NR⁴-; R⁴ es un átomo de hidrógeno; Y es un grupo de la fórmula: -C(=O)-, -C(=S)- o-CH(R⁵)-; R⁵ es un átomo de hidrógeno, o un grupo fenilo; Ar es un grupo arilo de 6- a 10- miembros mono- o bi-cíclico o un grupo heteroarilo de 5- a 10- miembros monocíclico o bicíclico conteniendo uno a dos heteroátomo(s) seleccionados de un átomo de oxígeno, un átomo de azufre, y un átomo de nitrógeno, y dicho grupo arilo (o heteroarilo) estando opcionalmente sustituido por uno a tres grupo(s) seleccionados de (a) un átomo de halógeno, (b) un grupo hidroxilo, (c) un grupo ciano, (d) un grupo alquilo C₁₋₆ opcionalmente sustituido por uno a tres átomo(s) de halógeno, (e) un grupo hidroxi-alquilo C₁₋₆, (f) un grupo benzoiloximetil, (g) un grupo alcoxi C₁₋₆ opcionalmente sustituido por uno a tres átomo(s) de halógeno, (h) un grupo alcoxi C₁₋₆-carbonil-alcoxi C₁₋₆, (i) un grupo alquil C₁₋₆tio, (j) un grupo alquilen C₁₋₆dioxi opcionalmente sustituido por uno a dos átomo(s) de halógeno, (k) un grupo amino opcionalmente sustituido por uno a dos grupo(s) alquilo C₁₋₆, (l) un grupo acilamino (dicho grupo acilo siendo un grupo alcanoilo C₁₋₇ o un grupo benzoilo), (m) un grupo cicloalquilo C₃₋₁₀ y (n) un grupo alquil C₁₋₆sulfonilo; y Q es un enlace simple, un grupo alquileno C₁₋₆ o un grupo alquenileno C₁₋₆; que excluye N-[4-(7-cianonaftalen-2-il)metil-3-oxo-3,4-dihidro-2H-1,4-benzoxazin-7-il]bencensulfonamida; y N-[4-(7-cianonaftalen-2-il)metil-3-oxo-3,4-dihidro-2H-1,4-benzoxazin-7-il](5-quinolilsulfonamida).The present application refers to a pharmaceutical composition of a compound, useful as an agent that modulates the mineralocorticoid receptor, useful as an agent for the prevention and / or treatment of cardiovascular and kidney diseases, or a salt acceptable for pharmaceutical use thereof. Claim 1: A pharmaceutical composition characterized in that it comprises as an active ingredient a compound of the formula (1) characterized in that ring A is a benzene ring being optionally substituted by one to three group (s) other than R¹, selected from (a ) a halogen atom, (b) a C₁₋₆ alkyl group (said alkyl group being optionally substituted by one to three group (s) selected from a halogen atom, a hydroxyl group and a C₁₋₆ alkoxy group), ( c) a hydroxyl group, (d) a C₁₋₆ alkoxy group, (e) an amino group, (f) a cyano group, (i) a C₂₋₁₂ alkenyl group, (j) a C₁₋₇ alkanoyl group and (k) a C₃₋₁₀ cycloalkyl group; R¹ is a group of the formula: RᵃSO₂NH-, RᵃSO₂NH-CH₂- or (Rᵇ) (Rᶜ) NSO₂-, and said R¹ replaces 1 position 7- of the 1-4-benzoxazine, 1-4-benzothiazine or tetrahydroquinoxaline portions; Rᵃ is a C₁₋₆ alkyl group, a C₃₋₁₀ cycloalkyl group, an amino group optionally substituted with one or two C₁₋₆ alkyl group (s), an aryl group of 6- to 10-monocyclic or bicyclic members, or a 5- to 10-monocyclic or bicyclic heteroaryl group containing one or two heteroatom (s) selected from an oxygen atom, a sulfur atom and a nitrogen atom; Rᵇ and Rᶜ are the same or different and are each a hydrogen atom, a C₁₋₆ alkyl group or a C₃₋₁₀ cycloalkyl group; one of R² and R³ is a hydrogen atom, a halogen atom or a C₁₋₆ alkyl group and the other is a hydrogen atom, a C₁₋₆ alkyl group, a C₁₋₆ alkoxycarbonyl group; or a phenyl group, or R² and R³ join together with the adjacent carbon atom to form a C₃₋₁₀ cycloalkyl group; X is an oxygen atom, a sulfur atom, or a group of the formula: -NR⁴-; R⁴ is a hydrogen atom; Y is a group of the formula: -C (= O) -, -C (= S) - or-CH (R⁵) -; R⁵ is a hydrogen atom, or a phenyl group; Ar is a 6- to 10-mono- or bi-cyclic aryl group or a 5- to 10-monocyclic or bicyclic heteroaryl group containing one to two heteroatom (s) selected from an oxygen atom, an atom of sulfur, and a nitrogen atom, and said aryl (or heteroaryl) group being optionally substituted by one to three group (s) selected from (a) a halogen atom, (b) a hydroxyl group, (c) a cyano group , (d) a C₁₋₆ alkyl group optionally substituted by one to three halogen atom (s), (e) a hydroxy-C₁₋₆ alkyl group, (f) a benzoyloxymethyl group, (g) a C₁₋ alkoxy group ₆ optionally substituted by one to three halogen atom (s), (h) a C₁₋₆-carbonyl-C alco alkoxy group, (i) a C₁₋₆thio alkyl group, (j) a C₁₋₆dioxy alkylene group optionally substituted by one to two halogen atom (s), (k) an amino group optionally substituted by one to two C₁₋₆ alkyl group (s), (l) an aci group lamino (said acyl group being a C₁₋₇ alkanoyl group or a benzoyl group), (m) a C₃₋₁₀ cycloalkyl group and (n) a C₁₋₆sulfonyl alkyl group; and Q is a single bond, a C₁₋₆ alkylene group or a C₁₋₆ alkenylene group; which excludes N- [4- (7-cyanonaphthalen-2-yl) methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-7-yl] benzenesulfonamide; and N- [4- (7-cyanonaphthalen-2-yl) methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-7-yl] (5-quinolyl sulfonamide).

ARP150102632A 2006-02-02 2015-08-14 PHARMACEUTICAL COMPOSITION OF HETEROBICYCLIC COMPOUNDS CONTAINING NITROGEN AR101566A2 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP2006025403 2006-02-02

Publications (1)

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AR101566A2 true AR101566A2 (en) 2016-12-28

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ARP150102632A AR101566A2 (en) 2006-02-02 2015-08-14 PHARMACEUTICAL COMPOSITION OF HETEROBICYCLIC COMPOUNDS CONTAINING NITROGEN
ARP150103659A AR102606A2 (en) 2006-02-02 2015-11-10 HETEROBICYCLIC COMPOUNDS CONTAINING NITROGEN

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ARP150103659A AR102606A2 (en) 2006-02-02 2015-11-10 HETEROBICYCLIC COMPOUNDS CONTAINING NITROGEN

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CN (1) CN101379048B (en)
AR (2) AR101566A2 (en)
ES (1) ES2368598T3 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6014144B2 (en) * 2012-08-08 2016-10-25 田辺三菱製薬株式会社 Process for producing 1,4-benzoxazine compounds
AU2017338161A1 (en) * 2016-09-27 2019-04-18 Mitsubishi Tanabe Pharma Corporation Pharmaceutical composition and method for treatment of non-alcoholic fatty liver disease
CN110684043B (en) * 2019-08-13 2022-09-06 温州大学 C-N axis chiral arylamine compound and preparation method thereof
KR20240021854A (en) * 2021-06-15 2024-02-19 치아타이 티안큉 파마수티컬 그룹 주식회사 Benzoxazinone derivatives

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ES2368598T3 (en) 2011-11-18
CN101379048A (en) 2009-03-04
AR102606A2 (en) 2017-03-15
CN101379048B (en) 2012-03-21

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