AR039779A1 - Ligandos receptores de melanocortina y composicion farmaceutica que contiene el compuesto - Google Patents

Ligandos receptores de melanocortina y composicion farmaceutica que contiene el compuesto

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Publication number
AR039779A1
AR039779A1 ARP030101500A ARP030101500A AR039779A1 AR 039779 A1 AR039779 A1 AR 039779A1 AR P030101500 A ARP030101500 A AR P030101500A AR P030101500 A ARP030101500 A AR P030101500A AR 039779 A1 AR039779 A1 AR 039779A1
Authority
AR
Argentina
Prior art keywords
aromatic
mixtures
substituted
linear
rings
Prior art date
Application number
ARP030101500A
Other languages
English (en)
Inventor
Frank Hallock Ebetino
Xuewei Liu
Mark Gregory Solinsky
John August Wos
Original Assignee
Procter & Gamble
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Publication date
Application filed by Procter & Gamble filed Critical Procter & Gamble
Publication of AR039779A1 publication Critical patent/AR039779A1/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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P3/06—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
    • 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
    • A61P31/10—Antimycotics
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • 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
    • 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
    • C07D211/10—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 radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/16—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 radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with acylated ring nitrogen atom
    • 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

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

Compuestos ligandos con selectividad por receptores MC-3 y/o MC-4, sus enantiómeros, diastómeros y sales farmacéuticamente aceptables del mismo. Composición que comprende una cantidad eficaz de uno o más ligandos receptores de melanocortina de la fórmula (1). Se usan para controlar trastornos de peso corporal como obesidad, anorexia, caquexia. Reivindicación 1: Un compuesto, incluyendo todas las formas enantioméricas y diastereoméricas y las sales farmacéuticamente aceptables de éstas, el compuesto antes mencionado tiene la fórmula (1) en donde R es una unidad de hidrocarburo sustituido o no sustituido que se selecciona del grupo que consiste de: a) anillos carbocíclicos no aromáticos, b) anillos carbocíclicos aromáticos; c) anillos heterocíclicos no aromáticos; y d) anillos heterocíclicos aromáticos; W es una unidad pendiente que tiene la fórmula: -L-Q en donde Q es H o una unidad sustituida o no sustituida que se selecciona de; i) alquilo C1-22 lineal o ramificado; ii) alquenilo C2-22 lineal o ramificado; iii) alquinilo C2-22 lineal o ramificado; iv) anillos heterocíclicos aromáticos C3-13; v) anillos carbocíclicos no aromáticos C3-8; vi) anillos carbocíclicos aromáticos C6-14, vii) anillos heterocíclicos no aromáticos C1-7; viii) anillos heterocíclicos aromáticos C3-13; xix) -(CH2)mCO2R8; xx) -(CH2)mC(O)N(R8)2, y xxi) -SO2R9; cada R8 es H, alquilo C1-6 sustituido o no sustituido, lineal, ramificado, o cíclico, -OH, -SO2R9, y mezclas de éstos; R9 es alquilo o fenilo C1-4; el índice m es 0, 1, o 2; L es un grupo de enlace que tiene la fórmula (2), T se selecciona del grupo que consiste de i) -NR6S(O)2-;ii) -S(O)2NR6-; y iii) mezclas de éstos; el índice w es 0 o 1; R3a, R3b, R4a y R4b cada uno independientemente es: i) H, ii) alquilo C1-4 lineal, ramificado, y cíclico; iii) -N(R6)2; iv) -NR6C(Y)R6; v) R3a y R3b o R4a y R4b se pueden tomar juntos para formar una unidad de carbonilo; y vi) mezclas de éstos; Y es -O-, -S-, =O, =S, =NR6, =NOH, y mezclas de éstos; el índice j es de 0 a 3; el índice k es de 0 a 3; W1 es una unidad pendiente que tiene la fórmula -(CH2)x-R1; R1 es: i) H, ii) anillos carbocíclicos no aromáticos C3-8, sustituidos o no sustituidos, iii) anillos carbocíclicos aromáticos C6-14, sustituidos o no sustituidos, iv) anillos heterocíclicos no aromáticos C1-7, sustituidos o no sustituidos, o v) anillos heterocíclicos aromáticos C3-13, sustituidos o no sustituidos; el índice x es de 0 a 10; W2 es una unidad pendiente que tiene la fórmula (3); R2 es: i) H, ii) anillos carbocíclicos no aromáticos C3-8, iii) anillos carbocíclicos aromáticos C6-14, iv) anillos heterocíclicos no aromáticos C1-7, v) anillos heterocíclicos aromáticos C3-13, vi) -C(Y)R6, vii) -C(Y)2R6, viii) -C(Y)N(R6)2, ix) -C(Y)NR6N(R6)2, x) -CN, xi) -CNO, xii) -[C(R7)2]C(R7)2, xiii) -N(R6)2, xiv) -NR6CN, xv) -NR6C(Y)R6, xvi) -NR6C(Y)N(R6)2, xvii) -NHN(R6)2, xviii) -NHOR6, xix) -NCS, xx) -NO2, xxi) -OR6, xxii) -OCN, xxiii) -OCF3, -OCCI3, -OCBr3, xxiv) -F, -Cl, -Br, -I, y mezclas de éstos, xxv) -SCN, xxvi) -SO3M, xxvii) -OSO3M, xxviii) -SO2N(R6)2, xxix) -SO2R6, xxx) -[C(R6)2]nP(O)(OR6)R6, xxxi) -[C(R6)2]nP(O)(OR6)2, xxxii) y mezclas de éstos; R5a y R5b cada uno son H, o R5a y R5b se toman juntos para formar una unidad de carbonilo; Y es igual que lo anterior; R6 es H, alquilo C1-4 lineal, ramificado o cíclico, alquenilo C2-4 lineal, halógeno, -OH, -NO2, -CN, y mezclas de éstos; M es H o un catión formador de sal, el índice y es de 0 a 10.
ARP030101500A 2002-04-30 2003-04-29 Ligandos receptores de melanocortina y composicion farmaceutica que contiene el compuesto AR039779A1 (es)

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US (2) US7026335B2 (es)
EP (1) EP1499588A1 (es)
JP (1) JP2005525412A (es)
KR (1) KR20040104672A (es)
CN (1) CN1656070A (es)
AR (1) AR039779A1 (es)
AU (1) AU2003230923A1 (es)
BR (1) BR0309744A (es)
CA (1) CA2483787A1 (es)
IL (1) IL164766A0 (es)
MA (1) MA27306A1 (es)
MX (1) MXPA04010761A (es)
NO (1) NO20045136L (es)
NZ (1) NZ536099A (es)
PE (1) PE20040085A1 (es)
PL (1) PL373695A1 (es)
RU (1) RU2004134718A (es)
TW (1) TW200409639A (es)
WO (1) WO2003093234A1 (es)
ZA (1) ZA200408529B (es)

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KR20040104672A (ko) 2004-12-10
PE20040085A1 (es) 2004-04-15
IL164766A0 (en) 2005-12-18
WO2003093234A1 (en) 2003-11-13
CA2483787A1 (en) 2003-11-13
MXPA04010761A (es) 2005-03-07
RU2004134718A (ru) 2005-07-20
MA27306A1 (fr) 2005-05-02
NO20045136L (no) 2005-01-24
JP2005525412A (ja) 2005-08-25
PL373695A1 (en) 2005-09-05
CN1656070A (zh) 2005-08-17
US20030236230A1 (en) 2003-12-25
AU2003230923A1 (en) 2003-11-17
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US7026335B2 (en) 2006-04-11
BR0309744A (pt) 2005-02-09

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