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AR076328A1 - Derivados de 4-azetidinil-1-fenil-ciclohexano antagonistas de ccr2 - Google Patents

Derivados de 4-azetidinil-1-fenil-ciclohexano antagonistas de ccr2

Info

Publication number
AR076328A1
AR076328A1 ARP100101287A ARP100101287A AR076328A1 AR 076328 A1 AR076328 A1 AR 076328A1 AR P100101287 A ARP100101287 A AR P100101287A AR P100101287 A ARP100101287 A AR P100101287A AR 076328 A1 AR076328 A1 AR 076328A1
Authority
AR
Argentina
Prior art keywords
alkyl
dihydro
phenyl
onyl
benzo
Prior art date
Application number
ARP100101287A
Other languages
English (en)
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR076328A1 publication Critical patent/AR076328A1/es

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A61K31/36—Compounds containing methylenedioxyphenyl groups, e.g. sesamin
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
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    • A61P11/00—Drugs for disorders of the respiratory system
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
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    • A61P17/00—Drugs for dermatological disorders
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    • A61P17/04—Antipruritics
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P27/00—Drugs for disorders of the senses
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    • A61P27/14—Decongestants or antiallergics
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P37/08—Antiallergic agents
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    • 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
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    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • 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
    • C07D401/08—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 carbon chain containing alicyclic rings
    • 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
    • C07D403/08—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 carbon chain containing alicyclic rings
    • 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
    • C07D403/10—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 carbon chain containing aromatic rings
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    • 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
    • C07D405/08—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 carbon chain containing alicyclic rings
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    • C07D413/08—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 carbon chain containing alicyclic rings
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/08—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing alicyclic rings

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  • Organic Chemistry (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
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  • Otolaryngology (AREA)
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Abstract

Composicion farmacéutica. También se describe el uso de los mismos para preparar un medicamento para prevenir, tratar o mejorar un síndrome, trastorno o enfermedad, en donde el síndrome, trastorno o enfermedad es diabetes tipo II, obesidad y asma. También se describe el uso de los mismos para preparar un medicamento para inhibir la actividad del CCR2 en un mamífero. Reivindicacion 1: Un compuesto de formula (1) en donde X es NH2, F, H, SH, S(O)CH3, SCH3, SO2CH3, u OH; R1 es fenilo sustituido, opcionalmente, con uno o dos sustituyentes, uno de los cuales se selecciona del grupo que consiste de: O-alquilo C1-4, S-alquilo C1-4, SO-alquilo C1-4, SO2-alquilo C1-4, -OSO2NH2, -SO2NH-alquilo C1-4, -OSO2NH2, -SO2NH2, N(alquilo C1-4)2, NH2, NH-alquilo C1-4, NHSO2-alquilo C1-4, N(SO2CH3)2, OH, O-alquilo C1-4CO2-alquilo C1-4, O-alquilo C1-4CO2H, OCH2CH2N(alquilo C1-4)2, F, Cl, CH2CN, CN, alquilo C1-4, NHCO2H, NHCO2-alquilo C1-4, NHCO-alquilo C1-4, -CsCH, CONH2, NHCONH2, NHCONH-alquilo C1-4, CONH-alquilo C1-4, CH2CONH-alquilo C1-4, alquilo C1-4-CONH2, alquilo C1-4CO2alquilo C1-4, alquilo C1-4CO2H, CO2H, CH2C(NH)NH2, CO2-alquilo C1-4, CF3, OCHF2, CHF2, OCF3, OCH2CF3, cicloalquilo, heterociclilo, fenoxi, fenilo, CH2-fenilo, CH2-heteroarilo, y heteroarilo; y el segundo sustituyente, si está presente, se selecciona del grupo que consiste de F, alquilo C2-4 y OCH3, o dicho fenilo puede sustituirse en dos átomos de carbono adyacentes para formar un sistema bicíclico fusionado, seleccionado del grupo que consiste de benzotiazolilo, benzooxazolilo, benzofuranilo, indolilo, quinolinilo, isoquinolinilo, benzo[b]tiofenilo, 3H-benzotiazol-2-onilo, 3H-benzooxazol-2-onilo, 1,3-dihidro-benzoimidazol-2-onilo, 1-metil-1H-benzoimidazolilo, benzo[1,3]dioxolilo, 2,3-dihidro-benzofuranilo, 2,3-dihidro-benzo[1,4]dioxinilo, en donde dicho 3H-benzooxazol-2-onilo, 1,3-dihidro-benzoimidazol-2-onilo, y 1-metil-1H-benzoimidazolilo, se sustituyen, opcionalmente, en cualquier átomo de nitrogeno con alquilo C1-4; R2 es H, alquilo C1-4, NH2, NO2, NHCH2CH2OH, N(alquilo C1-4)2, N(SO2CH3)2, NHCONH-alquilo C1-4, CN, F, Cl, Br, CF3, cicloalquilo, heterociclilo, OCF3, OCF2H, CF2H, u O-alquilo C1-4; R3 es F, Cl, CF3, u O-alquilo C1-4; alternativamente, R2 y R3 pueden tomarse junto con su fenilo unido para formar un grupo benzo[1,3]dioxolilo, 2,3-dihidro-benzofuranilo, o 2,3-dihidro-benzo[1,4]dioxinilo; R4 es H, O-alquilo C1-4, o F; solvatos, hidratos, tautomeros y profármacos, y sales farmacéuticamente aceptables de éstos.
ARP100101287A 2009-04-17 2010-04-19 Derivados de 4-azetidinil-1-fenil-ciclohexano antagonistas de ccr2 AR076328A1 (es)

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US17030709P 2009-04-17 2009-04-17

Publications (1)

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AR076328A1 true AR076328A1 (es) 2011-06-01

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Country Link
US (2) US20100267689A1 (es)
EP (1) EP2419419B1 (es)
JP (1) JP5675773B2 (es)
KR (1) KR20120006544A (es)
CN (1) CN102459227B (es)
AR (1) AR076328A1 (es)
AU (1) AU2010236346B2 (es)
BR (1) BRPI1016189A2 (es)
CA (1) CA2758934A1 (es)
ES (1) ES2528625T3 (es)
MX (1) MX2011010964A (es)
NZ (1) NZ595432A (es)
TW (1) TW201102377A (es)
WO (1) WO2010121046A1 (es)

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WO2010121046A1 (en) 2010-10-21
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TW201102377A (en) 2011-01-16
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US8513229B2 (en) 2013-08-20
EP2419419B1 (en) 2014-12-03
US20120040960A1 (en) 2012-02-16
MX2011010964A (es) 2011-11-02
CN102459227A (zh) 2012-05-16
BRPI1016189A2 (pt) 2016-04-19
US20100267689A1 (en) 2010-10-21
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