PE20040375A1 - Amino-piperidinas 4,4-disustituidas como ligandos de receptores de melanocortina - Google Patents

Amino-piperidinas 4,4-disustituidas como ligandos de receptores de melanocortina

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Publication number
PE20040375A1
PE20040375A1 PE2003000371A PE2003000371A PE20040375A1 PE 20040375 A1 PE20040375 A1 PE 20040375A1 PE 2003000371 A PE2003000371 A PE 2003000371A PE 2003000371 A PE2003000371 A PE 2003000371A PE 20040375 A1 PE20040375 A1 PE 20040375A1
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PE
Peru
Prior art keywords
aromatic
amino
disustituted
cyclohexil
ona
Prior art date
Application number
PE2003000371A
Other languages
English (en)
Inventor
Frank Hallock Ebetino
Xuewei Liu
John August Wos
Mark Gregory Solinsky
Rashid Naeem Mumin
Original Assignee
Procter & Gamble
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Filing date
Publication date
Application filed by Procter & Gamble filed Critical Procter & Gamble
Publication of PE20040375A1 publication Critical patent/PE20040375A1/es

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    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
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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
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • 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
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D417/02—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
    • C07D417/12—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 chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Reproductive Health (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
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Abstract

SE REFIERE A COMPUESTOS AMINO-PIPERIDINA 4,4-DISUSTITUIDOS DE FORMULA (I) DONDE R ES CICLOALQUILO AROMATICO O NO AROMATICO, HETEROCICLO AROMATICO O NO AROMATICO; W1 ES UNA UNIDAD DE FORMULA a DONDE R1 ES H, CARBOCICLO NO AROMATICO(C3-C8), CARBOCICLO AROMATICO(C3-C8), HETEROCICLO NO AROMATICO(C1-C7) Y AROMATICO(C3-C13); R3a Y R3b SON INDEPENDIENTEMENTE H, METILO, Y JUNTOS PUEDEN FORMAR UN CARBONILO, x ES DE 0 A 10; W2 ES UNA UNIDAD DE FORMULA b DONDE R2 ES H, CARBOCICLO NO AROMATICO(C3-C8), AROMATICO (C6-C14), HETEROCICLO NO AROMATICO(C1-C7), AROMATICO(C3-C13), -C(Y)R4, -C(Y)2R4, -C(Y)N(R4)2, ENTRE OTROS; Y ES -O-, -S-, =O, =S, =NR4, -R4 Y MEZCLAS DE ESTOS; R4 ES H, HALOGENO, ALQUILO(C1-C4), -OH Y MEZCLAS DE ESTOS. SON COMPUESTOS PREFERIDOS: 2-AMINO-3-(4-CLOROFENIL)-1-(4-CICLOHEXIL-4-[1,2,4]TRIAZOL-1-ILMETIL-PIPERIDIN-1-IL)PROPAN-1-ONA, 2-AMINO-3-(4-CLOROFENIL)-1-(4-CICLOHEXIL-4-IMIDAZOL-1-ILMETIL-PIPERIDIN-1-IL)PROPAN-1-ONA, 2-AMINO-3-(4-CLOROFENIL)-1-[4-CICLOHEXIL-4-(TIAZOL-2-ILAMINOMETIL)-PIPERIDIN-1-IL]-PROPAN-1-ONA, ENTRE OTROS, ESTOS COMPUESTOS SON LIGANDOS SELECTIVOS DE LOS RECEPTORES DE MELANOCORTINA (MC) CON ALTA AFINIDAD POR LOS RECEPTORES MC-3 Y/O MC-4, SON UTILES PARA EL TRATAMIENTO DE TRANSTORNOS ALIMENTARIOS
PE2003000371A 2002-04-30 2003-04-11 Amino-piperidinas 4,4-disustituidas como ligandos de receptores de melanocortina PE20040375A1 (es)

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US37672702P 2002-04-30 2002-04-30

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US (2) US20040010010A1 (es)
EP (1) EP1499314A1 (es)
JP (1) JP2005525410A (es)
KR (1) KR20040104671A (es)
CN (1) CN1655785A (es)
AR (1) AR039780A1 (es)
AU (1) AU2003234094B2 (es)
BR (1) BR0309748A (es)
CA (1) CA2483806A1 (es)
IL (1) IL164697A0 (es)
MA (1) MA27593A1 (es)
MX (1) MXPA04010762A (es)
NO (1) NO20045126L (es)
PE (1) PE20040375A1 (es)
PL (1) PL373575A1 (es)
RU (1) RU2004134719A (es)
TW (1) TW200404543A (es)
WO (1) WO2003092690A1 (es)
ZA (1) ZA200408528B (es)

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FR2870244B1 (fr) * 2004-05-11 2011-01-07 Centre Nat Rech Scient Conjugues dipeptidiques antagonistes de l'alpha-msh
FR2870243B1 (fr) 2004-05-11 2010-11-19 Centre Nat Rech Scient Conjugues tripeptidiques agonistes de la msh
EP1773338B1 (en) 2004-07-19 2010-01-06 Merck & Co., Inc. Acylated piperidine derivatives as melanocortin-4 receptor agonists
FR2873690B1 (fr) * 2004-07-29 2006-10-13 Sanofi Synthelabo Derives d'oxopiperidine, leur preparation et leur application en therapeutique
US20070021433A1 (en) 2005-06-03 2007-01-25 Jian-Qiang Fan Pharmacological chaperones for treating obesity
BRPI0616463A2 (pt) 2005-09-29 2011-06-21 Merck & Co Inc composto, composição farmacêutica, e, uso de um composto
EP1940401B1 (en) 2005-10-18 2012-07-11 Merck Sharp & Dohme Corp. Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
EP1826201A1 (en) * 2006-02-23 2007-08-29 Santhera Pharmaceuticals (Schweiz) AG Substituted phenylpiperidine derivatives as melanocortin-4 receptor modulators
WO2007096186A1 (en) * 2006-02-23 2007-08-30 Santhera Pharmaceuticals (Schweiz) Ag Substituted phenylpiperidine derivatives as melanocortin-4 receptor modulators
EP2019100A1 (en) * 2007-07-19 2009-01-28 Santhera Pharmaceuticals (Schweiz) AG Substituted heteroarylpiperidine derivatives as melanocortin-4 receptor modulators
US8759539B2 (en) 2008-11-17 2014-06-24 Merck Sharp & Dohme Corp. Substituted bicyclic amines for the treatment of diabetes
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WO2011011506A1 (en) 2009-07-23 2011-01-27 Schering Corporation Spirocyclic oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
WO2011137024A1 (en) 2010-04-26 2011-11-03 Merck Sharp & Dohme Corp. Novel spiropiperidine prolylcarboxypeptidase inhibitors
EP2568812B1 (en) 2010-05-11 2016-10-26 Merck Sharp & Dohme Corp. Novel prolylcarboxypeptidase inhibitors
US9006268B2 (en) 2010-06-11 2015-04-14 Merck Sharp & Dohme Corp. Prolylcarboxypeptidase inhibitors
WO2012100342A1 (en) 2011-01-27 2012-08-02 Université de Montréal Pyrazolopyridine and pyrazolopyrimidine derivatives as melanocortin-4 receptor modulators

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NO20045126L (no) 2005-01-21
ZA200408528B (en) 2005-07-07
AR039780A1 (es) 2005-03-02
BR0309748A (pt) 2005-02-15
TW200404543A (en) 2004-04-01
KR20040104671A (ko) 2004-12-10
PL373575A1 (en) 2005-09-05
JP2005525410A (ja) 2005-08-25
CA2483806A1 (en) 2003-11-13
IL164697A0 (en) 2005-12-18
CN1655785A (zh) 2005-08-17
AU2003234094B2 (en) 2006-03-09
MXPA04010762A (es) 2005-03-07
MA27593A1 (fr) 2005-11-01
US20050239835A1 (en) 2005-10-27
US20040010010A1 (en) 2004-01-15
WO2003092690A1 (en) 2003-11-13
EP1499314A1 (en) 2005-01-26
AU2003234094A1 (en) 2003-11-17
RU2004134719A (ru) 2005-06-27

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