AR074299A1 - DERIVATIVES OF (DIHIDRO) NAFTIRIDINONE AS ANTAGONISTS OF THE H3 HISTAMINE RECEIVER - Google Patents

DERIVATIVES OF (DIHIDRO) NAFTIRIDINONE AS ANTAGONISTS OF THE H3 HISTAMINE RECEIVER

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Publication number
AR074299A1
AR074299A1 ARP090104303A ARP090104303A AR074299A1 AR 074299 A1 AR074299 A1 AR 074299A1 AR P090104303 A ARP090104303 A AR P090104303A AR P090104303 A ARP090104303 A AR P090104303A AR 074299 A1 AR074299 A1 AR 074299A1
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Argentina
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alkyl
alkynyl
alkenyl
optionally substituted
different
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ARP090104303A
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Evotec Neurosciences Gmbh
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Publication of AR074299A1 publication Critical patent/AR074299A1/en

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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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Dichos compuestos son de utilidad como antagonistas del receptor de histamina H3. También composiciones farmacéuticas, la preparación de tales compuestos, así como la producción y el uso como medicamentos. Reivindicación 1: Un compuesto caracterizado por tener la fórmula (1) o una de sus sales, profármacos o metabolitos farmacéuticamente aceptables, en donde uno de X1---X1a, X2---X2a es C(RaR1a)-C(RbR1b); o C(Ra)=C(Rb); y el otro es N(R1)-C(O), con la condición de que N(R1) represente X1 o X2; Ra, Rb, R1a, R1b están seleccionados, de modo independiente, del grupo que consiste en H, halógeno; y alquilo C1-4, en donde alquilo C1-4 está opcionalmente sustituido con uno o varios halógenos, que son iguales o diferentes; opcionalmente al menos uno de los pares Ra/R1a, Rb/R1b se une junto con el átomo de carbono al que está unido para formar cicloalquilo C3-5, en donde cicloalquilo C3-5 está opcionalmente sustituido con uno o varios Rc, que son iguales o diferentes; Rc es halógeno; CN; OH; oxo (=O); alquilo C1-4, u O-alquilo C1-4, en donde alquilo C1-4; y O-alquilo C1-4, están opcionalmente sustituidos con uno o varios sustituyentes, que son iguales o diferentes y están seleccionados del grupo que consiste en halógeno; y OH; R1 es H; alquilo C1-7, alquenilo C2-7, alquinilo C2-7, o T, en donde alquilo C1-7, alquenilo C2-7 y alquinilo C2-7 están opcionalmente sustituidos con uno o varios R1c, que son iguales o diferentes; T es cicloalquilo C3-7 o heterociclilo saturado de 4 a 6 miembros, en donde T está opcionalmente sustituido con uno o varios R1d, que son iguales o diferentes; X3 es N, N-óxido o C(R2) y X4 es N, N-óxido o CH, con la condición de que al menos uno de X3, X4 sea N o N-óxido; R2 es H, halógeno, CN, CH3, CH2F; CHF2, CF3; C(O)N(R3R3a); CH2N(R3R3a), N(R3R3a), CH2OH; OR3; OCH2F; OCHF2 u OCF3; R3, R3a están seleccionados, de modo independiente, del grupo que consiste en H, alquilo C1-5 y cicloalquilo C3-5; opcionalmente R3, R3a se unen con el átomo de nitrógeno al que están unidos para formar un heterociclo saturado de 4 a 7 miembros; X5 es O; S; S(O); S(O)2; N(R4); N*(R4)C(O); N*(R4)S(O)2 o S*(O)2N(R4), en donde el asterisco indica la unión con el resto cíclico aromático en la fórmula (1); R4 es H; alquilo C1-5 o cicloalquilo C3-6, n es 0, 1, 2, 3 o 4: R es heterociclilo saturado de 4 a 7 miembros, en donde un átomo del anillo es nitrógeno y opcionalmente otro átomo del anillo es oxígeno; o cicloalquilo C4-6, en donde R está opcionalmente sustituido con uno o varios R5, que son iguales o diferentes, con la condición de que un nitrógeno del anillo del heterociclo saturado de 4 a 7 miembros sea un nitrógeno terciario o el heterociclo saturado de 4 a 7 miembros y cicloalquilo C4-6 estén sustituidos con al menos un R5 que es N(R6R6a); R1d, R5 están seleccionados, de modo independiente, del grupo que consiste en halógeno; CN, C(O)OR6b, OR6b; C(O)R6b, C(O)N(R6bR6c); S(O)2N(R6bR6c), S(O)N(R6bR6c); S(O)2R6b, S(O)R6b, N(R6b)S(O)2N(R6cR6d); SR6b, N(R6R6a); N(R6bR6c); NO2, OC(O)R6b, N(R6b)C(O)R6c; N(R6b)S(O)2R6c, N(R6b)S(O)R6c, N(R6b)C(O)OR6c; N(R6b)C(O)N(R6cR6d); OC(O)N(R6bR6c), oxo (=O), donde el anillo está al menos parcialmente saturado; T1, alquilo C1-6, alquenilo C2-6 y alquinilo C2-6, en donde alquilo C1-6, alquenilo C2-6 y alquinilo C2-6 están opcionalmente sustituidos con uno o varios R7, que son iguales o diferentes, con la condición de que, cuando R es heterociclilo saturado de 4 a 7 miembros, en donde un átomo del anillo sea nitrógeno y opcionalmente otro átomo del anillo sea oxigeno, R5 es T1; alquilo C1-6, alquenilo C2-6 o alquinilo C2-6, en donde alquilo C1-6, alquenilo C2-6 y alquinilo C2-6 están opcionalmente sustituidos con uno o varios R7, que son iguales o diferentes, cuando R5 está directamente unido con el átomo de nitrógeno del anillo. Opcionalmente dos R5 forman un grupo en puente seleccionado del grupo que consiste en CH2, CH2CH2, CH2CH2CH2, NH; N(CH3); CH2NHCH2, CH2N(CH3)CH2, y O; R6, R6a están seleccionados, de modo independiente, del grupo que consiste en T1; alquilo C1-6, alquenilo C2-6 y alquinilo C2-6, en donde alquilo C1-6, alquenilo C2-6 y alquinilo C2-6 están opcionalmente sustituidos con uno o varios R8, que son iguales o diferentes; opcionalmente, R6, R6a se unen con el átomo de nitrógeno al que están unidos para formar anillo T2 que contiene nitrógeno; R6b, R6c, R6d están seleccionados, de modo independiente, del grupo que consiste en H; T1, alquilo C1-6, alquenilo C2-6 y alquinilo C2-6, en donde alquilo C1-6, alquenilo C2-6 y alquinilo C2-6 están opcionalmente sustituidos con uno o varios R8, que pueden ser iguales o diferentes; R1c, R7, R8 están seleccionados, de modo independiente, del grupo que consiste en halógeno; CN; C(O)OR9, OR9; C(O)R9, C(O)N(R9R9a); S(O)2N(R9R9a), S(O)N(R9R9a); S(O)2R9, S(O)R9, N(R9)S(O)2N(R9aR9b); SR9, N(R9R9a); NO2, OC(O)R9, N(R9)C(O)R9a; N(R9)SO2R9a, N(R9)S(O)R9a, N(R9)C(O)N(R9aR9b); N(R9)C(O)OR9a, OC(O)N(R9R9a); y T1; R9, R9a, R9b están seleccionados, de modo independiente, del grupo que consiste en H, T1, alquilo C1-6, alquenilo C2-6 y alquinilo C2-6, en donde alquilo C1-6, alquenilo C2-6 y alquinilo C2-6 están opcionalmente sustituidos con uno o varios halógenos, que pueden ser iguales o diferentes; T1 es fenilo; naftilo; azulenilo; indenilo; indanilo; cicloalquilo C3-7, heterociclilo de 3 a 7 miembros; o heterobiciclilo de 7 a 11 miembros, en donde T1 está opcionalmente sustituido con uno o varios R10, que son iguales o diferentes; T2 es un heterociclo de 3 a 7 miembros que contiene nitrógeno, en donde T2 está opcionalmente sustituido con uno o varios R10, que son iguales o diferentes; R10 es halógeno; CN, C(O)OR11, OR11; C(O)R11, C(O)N(R11R11a); S(O)2N(R11R11a), S(O)N(R11R11a); S(O)2R11, S(O)R11, N(R11)S(O)2N(R11aR11b); SR11, N(R11R11a); NO2, OC(O)R11, N(R11)C(O)R11a; N(R11)S(O)2R11a, N(R11)S(O)R11a, N(R11)C(O)OR11a, N(R11)C(O)N(R11aR11b); OC(O)N(R11R11a), oxo (=O), donde el anillo está al menos parcialmente saturado; alquilo C1-6, alquenilo C2-6 o alquinilo C2-6, en donde alquilo C1-6, alquenilo C2-6 y alquinilo C2-6 están opcionalmente sustituidos con uno o varios halógenos, que son iguales o diferentes; R11, R11a, R11b están seleccionados, de modo independiente, del grupo que consiste en H, alquilo C1-6, alquenilo C2-6; y alquinilo C2-6, en donde alquilo C1-6, alquenilo C2-6 y alquinilo C2-6 están opcionalmente sustituidos con uno o varios halógenos, que pueden ser iguales o diferentes.Such compounds are useful as histamine H3 receptor antagonists. Also pharmaceutical compositions, the preparation of such compounds, as well as the production and use as medicaments. Claim 1: A compound characterized by having the formula (1) or a pharmaceutically acceptable salt, prodrug or metabolite thereof, wherein one of X1 --- X1a, X2 --- X2a is C (RaR1a) -C (RbR1b) ; or C (Ra) = C (Rb); and the other is N (R1) -C (O), with the proviso that N (R1) represents X1 or X2; Ra, Rb, R1a, R1b are independently selected from the group consisting of H, halogen; and C1-4 alkyl, wherein C1-4 alkyl is optionally substituted with one or more halogens, which are the same or different; optionally at least one of the Ra / R1a, Rb / R1b pairs binds together with the carbon atom to which it is attached to form C3-5 cycloalkyl, wherein C3-5 cycloalkyl is optionally substituted with one or more Rc, which are same or different; Rc is halogen; CN; OH; oxo (= O); C1-4 alkyl, or O-C1-4 alkyl, wherein C1-4 alkyl; and C 1-4 alkyl, are optionally substituted with one or more substituents, which are the same or different and are selected from the group consisting of halogen; and OH; R1 is H; C 1-7 alkyl, C 2-7 alkenyl, C 2-7 alkynyl, or T, wherein C 1-7 alkyl, C 2-7 alkenyl and C 2-7 alkynyl are optionally substituted with one or more R 1c, which are the same or different; T is C3-7 cycloalkyl or saturated 4-6 membered heterocyclyl, wherein T is optionally substituted with one or more R1d, which are the same or different; X3 is N, N-oxide or C (R2) and X4 is N, N-oxide or CH, with the proviso that at least one of X3, X4 is N or N-oxide; R2 is H, halogen, CN, CH3, CH2F; CHF2, CF3; C (O) N (R3R3a); CH2N (R3R3a), N (R3R3a), CH2OH; OR3; OCH2F; OCHF2 or OCF3; R3, R3a are independently selected from the group consisting of H, C1-5 alkyl and C3-5 cycloalkyl; optionally R3, R3a bind with the nitrogen atom to which they are attached to form a saturated 4- to 7-membered heterocycle; X5 is O; S; SW); S (O) 2; N (R4); N * (R4) C (O); N * (R4) S (O) 2 or S * (O) 2N (R4), wherein the asterisk indicates the union with the aromatic cyclic moiety in the formula (1); R4 is H; C1-5 alkyl or C3-6 cycloalkyl, n is 0, 1, 2, 3 or 4: R is 4 to 7 membered saturated heterocyclyl, wherein one ring atom is nitrogen and optionally another ring atom is oxygen; or C4-6 cycloalkyl, wherein R is optionally substituted with one or more R5, which are the same or different, with the proviso that a 4- to 7-membered saturated heterocycle ring nitrogen is a tertiary nitrogen or the saturated heterocycle of 4 to 7 members and C4-6 cycloalkyl are substituted with at least one R5 which is N (R6R6a); R1d, R5 are independently selected from the group consisting of halogen; CN, C (O) OR6b, OR6b; C (O) R6b, C (O) N (R6bR6c); S (O) 2N (R6bR6c), S (O) N (R6bR6c); S (O) 2R6b, S (O) R6b, N (R6b) S (O) 2N (R6cR6d); SR6b, N (R6R6a); N (R6bR6c); NO2, OC (O) R6b, N (R6b) C (O) R6c; N (R6b) S (O) 2R6c, N (R6b) S (O) R6c, N (R6b) C (O) OR6c; N (R6b) C (O) N (R6cR6d); OC (O) N (R6bR6c), oxo (= O), where the ring is at least partially saturated; T1, C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl, wherein C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl are optionally substituted with one or more R7, which are the same or different, with the provided that, when R is 4 to 7-membered saturated heterocyclyl, where one ring atom is nitrogen and optionally another ring atom is oxygen, R5 is T1; C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl, wherein C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl are optionally substituted with one or more R7, which are the same or different, when R5 is directly bound with the ring nitrogen atom. Optionally two R5 form a bridged group selected from the group consisting of CH2, CH2CH2, CH2CH2CH2, NH; N (CH3); CH2NHCH2, CH2N (CH3) CH2, and O; R6, R6a are independently selected from the group consisting of T1; C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl, wherein C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl are optionally substituted with one or more R8, which are the same or different; optionally, R6, R6a bind with the nitrogen atom to which they are attached to form a nitrogen-containing T2 ring; R6b, R6c, R6d are independently selected from the group consisting of H; T1, C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl, wherein C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl are optionally substituted with one or more R8, which may be the same or different; R1c, R7, R8 are independently selected from the group consisting of halogen; CN; C (O) OR9, OR9; C (O) R9, C (O) N (R9R9a); S (O) 2N (R9R9a), S (O) N (R9R9a); S (O) 2R9, S (O) R9, N (R9) S (O) 2N (R9aR9b); SR9, N (R9R9a); NO2, OC (O) R9, N (R9) C (O) R9a; N (R9) SO2R9a, N (R9) S (O) R9a, N (R9) C (O) N (R9aR9b); N (R9) C (O) OR9a, OC (O) N (R9R9a); and T1; R9, R9a, R9b are independently selected from the group consisting of H, T1, C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl, wherein C1-6 alkyl, C2-6 alkenyl and C2 alkynyl -6 are optionally substituted with one or more halogens, which may be the same or different; T1 is phenyl; naphthyl; azulenyl; indenyl; indanyl; C3-7 cycloalkyl, 3- to 7-membered heterocyclyl; or 7 to 11-membered heterobicyclyl, wherein T1 is optionally substituted with one or more R10, which are the same or different; T2 is a 3- to 7-membered nitrogen-containing heterocycle, wherein T2 is optionally substituted with one or more R10, which are the same or different; R10 is halogen; CN, C (O) OR11, OR11; C (O) R11, C (O) N (R11R11a); S (O) 2N (R11R11a), S (O) N (R11R11a); S (O) 2R11, S (O) R11, N (R11) S (O) 2N (R11aR11b); SR11, N (R11R11a); NO2, OC (O) R11, N (R11) C (O) R11a; N (R11) S (O) 2R11a, N (R11) S (O) R11a, N (R11) C (O) OR11a, N (R11) C (O) N (R11aR11b); OC (O) N (R11R11a), oxo (= O), where the ring is at least partially saturated; C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl, wherein C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl are optionally substituted with one or more halogens, which are the same or different; R11, R11a, R11b are independently selected from the group consisting of H, C1-6 alkyl, C2-6 alkenyl; and C2-6 alkynyl, wherein C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl are optionally substituted with one or more halogens, which may be the same or different.

ARP090104303A 2008-11-07 2009-11-06 DERIVATIVES OF (DIHIDRO) NAFTIRIDINONE AS ANTAGONISTS OF THE H3 HISTAMINE RECEIVER AR074299A1 (en)

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US8912176B2 (en) 2009-02-02 2014-12-16 Evotec Ag Azetidines as histamine H3 receptor antagonists
CN102532006A (en) * 2012-01-31 2012-07-04 江西华士药业有限公司 Preparation method of key intermediate 6-methylpyridine-3-formaldehyde of drug for treating rheumatic arthritis and rheumatoid arthritis
WO2013151982A1 (en) 2012-04-03 2013-10-10 Arena Pharmaceuticals, Inc. Methods and compounds useful in treating pruritus, and methods for identifying such compounds
GB201416754D0 (en) 2014-09-23 2014-11-05 Mission Therapeutics Ltd Novel compounds
CN105061305A (en) * 2015-08-31 2015-11-18 河南师范大学 Method for synthesizing 3-methylpyridine-2-carboxylic acid methyl ester in one step
EP4105216A4 (en) * 2020-02-13 2024-02-28 Genfleet Therapeutics Shanghai Inc Dihydronaphthyridinone compound, and preparation method therefor and medical use thereof

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AU2002254114A1 (en) * 2001-03-23 2002-10-08 Eli Lilly And Company Non-imidazole aryl alkylamines compounds as histamine h3 receptor antagonists, preparation and therapeutic uses
EP1595881A1 (en) * 2004-05-12 2005-11-16 Pfizer Limited Tetrahydronaphthyridine derivates useful as histamine H3 receptor ligands

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