AR045498A1 - Derivados bencimidazol 2- substituidos como antagonistas selectivos del receptor de la hormona concentradora de melanina, para el tratamiento de la obesidad y desordenes relacionados - Google Patents

Derivados bencimidazol 2- substituidos como antagonistas selectivos del receptor de la hormona concentradora de melanina, para el tratamiento de la obesidad y desordenes relacionados

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Publication number
AR045498A1
AR045498A1 ARP040103057A ARP040103057A AR045498A1 AR 045498 A1 AR045498 A1 AR 045498A1 AR P040103057 A ARP040103057 A AR P040103057A AR P040103057 A ARP040103057 A AR P040103057A AR 045498 A1 AR045498 A1 AR 045498A1
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AR
Argentina
Prior art keywords
substituted
alkyl
aryl
heteroaryl
hydrogen
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Application number
ARP040103057A
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English (en)
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Schering Corp
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Publication of AR045498A1 publication Critical patent/AR045498A1/es

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    • 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
    • C07D401/06—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 only aliphatic carbon atoms
    • 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
    • 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
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • C07D417/14—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 three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente describe un compuesto y una composición farmacéutica que comprende antagonistas de MCH, así como también métodos para el uso de los mismos para tratar la obesidad, los desórdenes metabólicos, los desórdenes de la alimentación, tales como hiperfagia y diabetes. Reivindicación 1: Un compuesto representado por la fórmula estructural (1), o una sal o solvato de los mismos farmacéuticamente aceptable, donde la línea de trazos de fórmula (2), junto con el enlace simple adjunto, representan conjuntamente un enlace doble, un ciclopropilo o ciclobutilo; Ar es arilo, heteroarilo, arilo R4-sustituido o heteroarilo R4-sustituido; R1 es hidrógeno, alquilo, aralquilo, arilo, cicloalquilo, cicloalquilalquilo, heteroaralquilo, heteroarilo, aralquilo R4-sustituido, arilo R4-sustituido, cicloalquilo R4-sustituido, cicloalquilalquilo R4-sustituido, heteroaralquilo R4-sustituido, heteroarilo R4-sustituido, alquilenilo-C(O)R8, -C(O)R2, -S(O2)R7, -S(O2)NR2R3, -C(O)NR2R3 o - C(O)OR7; R2 es hidrógeno, heteroarilo, alquilo o arilo; R3 es hidrógeno, heteroarilo, alquilo, o arilo, donde R2 y R3 pueden estar opcionalmente conjuntamente unidos y con el nitrógeno al cual están unidos forman un anillo heterocíclico, donde dicho anillo heterocíclico puede estar opcionalmente sustituido con un sustituyente del sistema de anillo, estando cada uno independientemente seleccionado del grupo que consiste en alquilo, alquenilo, alquinilo, arilo, heteroarilo, aralquilo, alquilarilo, heteroaralquilo, heteroarilalquenilo, heteroarilalquinilo, alquilheteroarilo, hidroxi, hidroxialquilo, alcoxi, ariloxi, aralcoxi, acilo, aroilo, halógeno, nitro, ciano, carboxi, alcoxicarbonilo, ariloxicarbonilo, aralcoxicarbonilo, alquilsulfonilo, arilsulfonilo, heteroarilsulfonilo, alquiltio, ariltio, heteroariltio, aralquiltio, heteroaralquiltio, cicloalquilo, heterociclilo, -C(=N-CN)-NH2, -C(=NH)-NH2, -C(=NH)-NH(alquilo), Y1Y2N-, Y1Y2N-alquilo-, Y1Y2NC(O)-, Y1Y2NSO2- y - SO2NY1Y2, donde Y1 y Y2 pueden ser iguales o diferentes y están independientemente seleccionados del grupo que consiste en hidrógeno, alquilo, arilo, cicloalquilo y aralquilo; R4 representa 1 a 5 porciones y cada R4 está independientemente seleccionado del grupo que consiste en hidrógeno, heterociclilo, heterociclilo R8-sustituido, heterociclilalquilo, heterociclilalquilo R8-sustituido, arilo, cicloalquilo, cicloalquilalquilo, heteroaralquilo, heteroarilo, arilo R8-sustituido, cicloalquilo R8-sustituido, cicloalquilalquilo R8-sustituido, heteroaralquilo R8-sustituido, heteroarilo R8-sustituido, -OH, alcoxi, -OCF3, -CN, alquilo, halógeno, -NR5R6, -NR5C(O)R7, -C(O)NR5R6, -NR5S(O2)R7, -S(O2)NR5R6, -S(O2)R7, -C(O)R7, - C(O)OR5, -CF3, -alquilenoNR5R6, -alquilenoNR6C(O)R7, -alquilenoNR6S(O2)R7, alquenilo, -NR5C(O)NR5R6, -alquilenoNR5C(O)OR7, CHO y -C=NOR5; R5 es hidrógeno o alquilo; R6 es hidrógeno, alquilo, arilo, aralquilo, heteroarilo o heteroaralquilo; R7 es alquilo, arilo, aralquilo, heteroarilo o heteroaralquilo; R8 es alquilo, -OH o hidroxialquilo; R11 representa de 1 a 4 porciones y cada R11está independientemente seleccionado del grupo que consiste en hidrógeno, alcoxi, alquilo, halógeno, -OH, - OCF3, CN y -CF3; y X representa de 1 a 4 porciones y cada X está independientemente seleccionada entre hidrógeno, alquilo, arilo, cicloalquilo, heteroarilo, heterociclilo, halógeno, arilo R4-sustituido, cicloalquilo R4-sustituido, heteroarilo R4- sustituido, heterociclilo R4-sustituido, -CF3, -OCF3, -OR2, -CN, -C(O)R2, -S(O2)R7, -C(O)NR5R6, -C(O)OR7 y -NR5C(O)R7.
ARP040103057A 2003-08-25 2004-08-25 Derivados bencimidazol 2- substituidos como antagonistas selectivos del receptor de la hormona concentradora de melanina, para el tratamiento de la obesidad y desordenes relacionados AR045498A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US49783703P 2003-08-25 2003-08-25
US53233303P 2003-12-23 2003-12-23

Publications (1)

Publication Number Publication Date
AR045498A1 true AR045498A1 (es) 2005-11-02

Family

ID=34278564

Family Applications (1)

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ARP040103057A AR045498A1 (es) 2003-08-25 2004-08-25 Derivados bencimidazol 2- substituidos como antagonistas selectivos del receptor de la hormona concentradora de melanina, para el tratamiento de la obesidad y desordenes relacionados

Country Status (8)

Country Link
US (1) US7214691B2 (es)
EP (1) EP1660478A1 (es)
JP (2) JP4476291B2 (es)
AR (1) AR045498A1 (es)
CA (1) CA2536544C (es)
MX (1) MXPA06002201A (es)
TW (1) TWI290140B (es)
WO (1) WO2005021528A1 (es)

Families Citing this family (16)

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CA2515717A1 (en) * 2003-02-10 2004-08-19 Banyu Pharmaceutical Co., Ltd. Melanin-concentrating hormone receptor antagonists containing piperidine derivatives as the active ingredient
TWI290140B (en) * 2003-08-25 2007-11-21 Schering Corp 2-Substituted benzimidazole derivatives as selective melanin concentrating hormone receptor antagonists for thr treatment of obesity and related disorders
CA2579820A1 (en) * 2004-09-20 2006-03-30 Targacept, Inc. Azaspiroalkene and azapiroalkane compounds with nicotinic cholinergic receptor activity
ATE429428T1 (de) * 2005-09-30 2009-05-15 Hoffmann La Roche Indanderivate als antagonisten des mch-rezeptors
CA2741125A1 (en) 2008-10-22 2010-04-29 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
CN102271509A (zh) 2008-10-31 2011-12-07 默沙东公司 用于抗糖尿病药的新型环苯并咪唑衍生物
WO2011106273A1 (en) 2010-02-25 2011-09-01 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
KR101668514B1 (ko) 2011-02-25 2016-10-21 머크 샤프 앤드 돔 코포레이션 항당뇨병제로서 유용한 신규 시클릭 아자벤즈이미다졸 유도체
PL2828301T3 (pl) 2012-03-20 2017-06-30 Trinseo Europe Gmbh Zmodyfikowane kompozycje polimerowe
US20140045746A1 (en) 2012-08-02 2014-02-13 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
BR112015019836A2 (pt) 2013-02-22 2017-07-18 Merck Sharp & Dohme composto, composição farmacêutica, e, uso de um composto
EP2970119B1 (en) 2013-03-14 2021-11-03 Merck Sharp & Dohme Corp. Novel indole derivatives useful as anti-diabetic agents
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
US11072602B2 (en) 2016-12-06 2021-07-27 Merck Sharp & Dohme Corp. Antidiabetic heterocyclic compounds
WO2018118670A1 (en) 2016-12-20 2018-06-28 Merck Sharp & Dohme Corp. Antidiabetic spirochroman compounds
TWI767148B (zh) 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)

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JP3681388B2 (ja) * 1993-07-13 2005-08-10 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 抗アレルギー性イミダゾアゼピン
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JPH111481A (ja) * 1997-06-10 1999-01-06 Sumitomo Pharmaceut Co Ltd ピペリジニルフタラジン誘導体
MXPA01009871A (es) * 1999-04-01 2002-04-24 Pfizer Prod Inc Aminopiridinas como inhibidores de la sorbitol deshidrogenasa.
EP1318996B1 (en) * 2000-09-20 2004-12-01 Schering Corporation Substituted imidazoles as dual histamine h1 and h3 agonists or antagonists
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CA2473236A1 (en) * 2002-01-10 2003-07-24 Neurogen Corporation Melanin concentrating hormone receptor ligands: substituted 2-(4-benzyl-piperazin-1-ylmethyl)- and 2-(4-benzyl-diazepan-1-ylmethyl)-1h-benzoimidazole analogues
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TWI290140B (en) * 2003-08-25 2007-11-21 Schering Corp 2-Substituted benzimidazole derivatives as selective melanin concentrating hormone receptor antagonists for thr treatment of obesity and related disorders

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Publication number Publication date
US7214691B2 (en) 2007-05-08
JP2007503444A (ja) 2007-02-22
JP2010047618A (ja) 2010-03-04
CA2536544C (en) 2010-05-11
US20050049269A1 (en) 2005-03-03
WO2005021528A1 (en) 2005-03-10
CA2536544A1 (en) 2005-03-10
MXPA06002201A (es) 2006-04-27
JP4476291B2 (ja) 2010-06-09
TWI290140B (en) 2007-11-21
EP1660478A1 (en) 2006-05-31

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